Comparing the advantages of CBDA over CBD.
Why Cannabidiolic Acid (CBDa) is more potent at modulating receptors and enzymes than its neutral congener, Cannabidiol (CBD) Formerly thought to be the inactive natural precursor of CBD, CBDa is now being recognized by the scientific and cannabis communities for its own unique and powerful attributes.
Listed here are several validating observations regarding pharmacologic CBDa’s advantages over CBD, and the future market potential of stabilized acid cannabinoid containing products like Chylobinoid®:
A study in 2013 by EM Rock and LA Parker observed the effectiveness of CBDa as an anti-nausea and antiemetic treatment in rats and shrews. Experiments testing for the minimally effective dose of CBDa to reduce gaping reaction in shrews and tongue protrusions in rats (surrogate markers for human nausea and vomiting) showed that the amount of CBDa necessary to decrease nausea is approximately 1000x lower than CBD.
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Cannabidiol (CBD), a major non-psychotropic constituent of fiber-type cannabis plant, has been reported to possess diverse biological activities, including anti-proliferative effect on cancer cells. Although CBD is obtained from non-enzymatic decarboxylation of its parent molecule, cannabidiolic acid (CBDA), few studies have investigated whether CBDA itself is biologically active. Results of the current investigation revealed that CBDA inhibits migration of the highly invasive MDA-MB-231 human breast cancer cells, apparently through a mechanism involving inhibition of cAMP-dependent protein kinase A, coupled with an activation of the small GTPase, RhoA. It is established that activation of the RhoA signaling pathway leads to inhibition of the mobility of various cancer cells, including MDA-MB-231 cells. The data presented in this report suggest for the first time that as an active component in the cannabis plant, CBDA offers potential therapeutic modality in the abrogation of cancer cell migration, including aggressive breast cancers.
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Our data showed that cannabidiol, via TRPV2, induces cell proliferation blockage, mitophagy, and changes in the expression of differentiation markers in chronic myeloid leukemia cells. Cannabidiol acts synergistically with imatinib and it also reduces cell viability of imatinib‐resistant cells.
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The analysis of drug-like properties related to bioavailability, toxicity risk, and ADME-Tox indicated that the chosen candidate drug compounds had very favorable drug-use characteristics. In contrast, the reference drugs Tamoxifen and Erlotinib displayed several aberrations and toxicity risks. This suggests that the proposed drugs’ phytochemicals structures are likely to be more stable in the EGFR protein pocket, thus enabling them to reach their therapeutic target against breast and lung cancer cell growth with greater efficacy than Tamoxifen and Erlotinib. Molecular dynamics simulations conducted over a 200 ns trajectory further confirmed the stability of the target EGFR protein structure, as well as the ideal fit between the EGFR protein structure and the isolated samples of cannabinoids and terpenes phytochemicals . Consequently, the phytochemicals CBDA, CBD, THCV, Δ-9-THC, Δ-8-THC, CBL, THCA, BCP, and γ-Ele discussed in this study could be employed as structural keys for the development of new drugs that act as EGFR-TKIs for breast and lung cancer.
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CBDa & Cancer Symptoms
Indeed, whether at present and undoubtedly, the cannabinoids are in use for the control of adverse reactions to conventional cancer treatments, an additional important direct role of these compounds in the development, progression, and metastasis of tumors is emerging. Furthermore, increasing the body of in vitro and in vivo evidence supports apoptosis, proliferation, and inflammation such as underlying mechanisms through which cannabinoids exert their anticancer effects (schematically reported in Figure 4). In addition, several pieces of evidence indicate that the activity of phytocannabinoids might be more effective in combinational therapies, encouraging novel combinations and treatment schedules. However, the translation of cannabinoids use into clinical practice is still now in the initial phases.
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Rationale: The purpose of this study was to evaluate the potential of oral combined cannabis constituents to reduce nausea.
Objective: The objective of this study was to determine the effect of combining subthreshold oral doses of Δ(9)-tetrahydrocannabinol (THC) and cannabidiolic acid (CBDA) on acute and anticipatory nausea in rat models of conditioned gaping.
Material and methods: The potential of intragastric (i.g.) administration of THC, CBDA, or combined doses, to interfere with acute nausea-induced conditioned gaping (acute nausea) or the expression of contextually elicited conditioned gaping (anticipatory nausea), was evaluated.
Results: For acute nausea, i.g. administration of subthreshold doses of THC (0.5 and 1 mg/kg) or CBDA (0.5 and 1 μg/kg) significantly suppressed acute nausea-induced gaping, whereas higher individual doses of both THC and CBDA were maximally effective. Combined i.g. administration of higher doses of THC and CBDA (2.5 mg/kg THC-2.5 μg/kg CBDA; 10 mg/kg THC-10 μg/kg CBDA; 20 mg/kg THC-20 μg/kg CBDA) also enhanced positive hedonic reactions elicited by saccharin solution during conditioning. For anticipatory nausea, combined subthreshold i.g. doses of THC (0.1 mg/kg) and CBDA (0.1 μg/kg) suppressed contextually elicited conditioned gaping. When administered i.g., THC was effective on its own at doses ranging from 1 to 10 mg/kg, but CBDA was only effective at 10 μg/kg. THC alone was equally effective by intraperitoneal (i.p.) and i.g. administration, whereas CBDA alone was more effective by i.p. administration (Rock et al. in Psychopharmacol (Berl) 232:4445-4454, 2015) than by i.g. administration.
Conclusions: Oral administration of subthreshold doses of THC and CBDA may be an effective new treatment for acute nausea and anticipatory nausea and appetite enhancement in chemotherapy patients.
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Most studies related to hemp are focused on Cannabidiol (CBD) and Tetrahydrocannabinol (THC); however, up to 120 types of phytocannabinoids are present in hemp. Hemp leaves contain large amounts of Cannabidiolic acid (CBDA) and Tetrahydrocannabinolic acid (THCA), which are acidic variants of CBD and THC and account for the largest proportion of CBDA. In recent studies, CBDA exhibited anti-hyperalgesia and anti-inflammatory effects. THCA also showed anti-inflammatory and neuroprotective effects that may be beneficial for treating neurodegenerative diseases. CBDA and THCA can penetrate the blood–brain barrier (BBB) and affect the central nervous system. The purpose of this study was to determine whether CBDA and THCA ameliorate Alzheimer’s disease (AD)-like features in vitro and in vivo. The effect of CBDA and THCA was evaluated in the Aβ1–42-treated mouse model. We observed that Aβ1–42-treated mice had more hippocampal Aβ and p-tau levels, pathological markers of AD, and loss of cognitive function compared with PBS-treated mice. However, CBDA- and THCA-treated mice showed decreased hippocampal Aβ and p-tau and superior cognitive function compared with Aβ1–42-treated mice. In addition, CBDA and THCA lowered Aβ and p-tau levels, alleviated calcium dyshomeostasis, and exhibited neuroprotective effects in primary neurons. Our results suggest that CBDA and THCA have anti-AD effects and mitigate memory loss and resilience to increased hippocampal Ca2+, Aβ, and p-tau levels. Together, CBDA and THCA may be useful therapeutic agents for treating AD.
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This study was conducted using the compound HU-580, which is Cannabidiolic acid methyl ester, a biologically synthetic version of CBDa, however they go on to say that CBDa has been shown and could be even more potent than the synthetic version.
Cannabidiolic acid methyl ester (HU-580) is a more stable compound than cannabidiolic acid (CBDA) which has been shown to be effective in reducing nausea, anxiety, depression behaviors in animal models. Here we extend the investigation of this compound to determine its effect on the sleep-wake cycle in male Wistar rats. HU-580 dose-dependently (0.1, 1.0 or 100 μg/Kg, i.p.) prolonged wakefulness (W) and decreased slow wave sleep (SWS) duration whereas rapid eye movement sleep (REMS) showed no statistical change. In addition, the brain microdialysis probes either placed at nucleus accumbens (NAc) or into the basal forebrain in freely moving animals were used to evaluate the effects of HU-580 treatment on neurotransmitters related to the sleep-wake cycle modulation. HU-580 enhanced extracellular levels of dopamine, serotonin collected from NAc while adenosine and acetylcholine were increased in the basal forebrain. In summary, HU-580 seems to possess wake-promoting pharmacological properties and enhances the levels of wake-related neurochemicals. This is the first report of effects of HU-580 on sleep modulation expanding the very limited existent data on the neurobiological effects of HU-580 on rats.
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In the present study it was revealed that cannabidiolic acid (CBDA) selectively inhibited cyclooxygenase (COX)-2 activity with an IC(50) value (50% inhibition concentration) around 2 microM, having 9-fold higher selectivity than COX-1 inhibition. In contrast, Delta(9)-tetrahydrocannabinolic acid (Delta(9)-THCA) was a much less potent inhibitor of COX-2 (IC(50) > 100 microM). Nonsteroidal anti-inflammatory drugs containing a carboxyl group in their chemical structures such as salicylic acid are known to inhibit non selectively both COX-1 and COX-2. CBDA and Delta(9)-THCA have a salicylic acid moiety in their structures. Thus, the structural requirements for the CBDA-mediated COX-2 inhibition were next studied. There is a structural difference between CBDA and Delta(9)-THCA; phenolic hydroxyl groups of CBDA are freed from the ring formation with the terpene moiety, although Delta(9)-THCA has dibenzopyran ring structure. It was assumed that the whole structure of CBDA is important for COX-2 selective inhibition because beta-resorcylic acid itself did not inhibit COX-2 activity. Methylation of the carboxylic acid moiety of CBDA led to disappearance of COX-2 selectivity. Thus, it was suggested that the carboxylic acid moiety in CBDA is a key determinant for the inhibition. Furthermore, the crude extract of cannabis containing mainly CBDA was shown to have a selective inhibitory effect on COX-2. Taken together, these lines of evidence in this study suggest that naturally occurring CBDA in cannabis is a selective inhibitor for COX-2.
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Background and purpose: Cannabidiol is a Cannabis-derived non-psychotropic compound that exerts a plethora of pharmacological actions, including anti-inflammatory, neuroprotective and antitumour effects, with potential therapeutic interest. However, the actions of cannabidiol in the digestive tract are largely unexplored. In the present study, we investigated the effect of cannabidiol on intestinal motility in normal (control) mice and in mice with intestinal inflammation.
Experimental approach: Motility in vivo was measured by evaluating the distribution of an orally administered fluorescent marker along the small intestine; intestinal inflammation was induced by the irritant croton oil; contractility in vitro was evaluated by stimulating the isolated ileum, in an organ bath, with ACh.
Key results: In vivo, cannabidiol did not affect motility in control mice, but normalized croton oil-induced hypermotility. The inhibitory effect of cannabidiol was counteracted by the cannabinoid CB1 receptor antagonist rimonabant, but not by the cannabinoid CB2 receptor antagonist but by the opioid receptor antagonist naloxone or by the alpha2-adrenergic antagonist yohimbine. Cannabidiol did not reduce motility in animals treated with the fatty acid amide hydrolase (FAAH) inhibitor, whereas loperamide was still effective. In vitro, cannabidiol inhibited ACh-induced contractions in the isolated ileum from both control and croton oil-treated mice.
Conclusions and implications: Cannabidiol selectively reduces croton oil-induced hypermotility in mice in vivo and this effect involves cannabinoid CB1 receptors and FAAH. In view of its low toxicity in humans, cannabidiol may represent a good candidate to normalize motility in patients with inflammatory bowel disease.
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This was a highly experimental study on mice, however it’s been replicated on smaller scales with similar results.
Inflammatory bowel disease affects millions of individuals; nevertheless, pharmacological treatment is disappointingly unsatisfactory. Cannabidiol, a safe and non-psychotropic ingredient of marijuana, exerts pharmacological effects (e.g., antioxidant) and mechanisms (e.g., inhibition of endocannabinoids enzymatic degradation) potentially beneficial for the inflamed gut. Thus, we investigated the effect of cannabidiol in a murine model of colitis. Colitis was induced in mice by intracolonic administration of dinitrobenzene sulfonic acid. Inflammation was assessed both macroscopically and histologically. In the inflamed colon, cyclooxygenase-2 and inducible nitric oxide synthase (iNOS) were evaluated by Western blot, interleukin-1beta and interleukin-10 by ELISA, and endocannabinoids by isotope dilution liquid chromatography-mass spectrometry. Human colon adenocarcinoma (Caco-2) cells were used to evaluate the effect of cannabidiol on oxidative stress. Cannabidiol reduced colon injury, inducible iNOS (but not cyclooxygenase-2) expression, and interleukin-1beta, interleukin-10, and endocannabinoid changes associated with 2,4,6-dinitrobenzene sulfonic acid administration. In Caco-2 cells, cannabidiol reduced reactive oxygen species production and lipid peroxidation. In conclusion, cannabidiol, a likely safe compound, prevents experimental colitis in mice.
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The primary objective of this study was to evaluate the efficacy of GWP42003-P as an adjunctive treatment in reducing the number of drop seizures when compared with placebo in participants with Lennox-Gastaut syndrome (LGS).
This was completed on the Epidiolex product created by GW Pharmaceuticals, there isn’t a published formula of this product however it is a synergised blend of CBDa and CBD.
This study was a 1:1:1 randomized, double-blind, 14-week comparison of 2 dose levels (10 milligram [mg] per kilogram [kg] per day [mg/kg/day] and 20 mg/kg/day) of GWP42003-P versus placebo. Participants who satisfied all inclusion and none of the exclusion criteria began a 28-day baseline observation period. The treatment period consisted of a 2-week titration period followed by a 12-week maintenance period. The 20 mg/kg/day dose was recommended by the Data Safety Monitoring Committee (DSMC) after assessment of safety and pharmacokinetic data from Part A of study GWEP1332 (NCT02091206). The 10 mg/kg/day dose was defined as 50% of the 20 mg/kg/day dose. The first participant was not enrolled into this study until the DSMC had reviewed the safety data from Part A of study GWEP1332.
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Cannabidiolic Acid (CBDA) Derivative in Treating Diet- and Genetic-Induced Obesity.
Obesity is a global medical problem; its common form is known as diet-induced obesity (DIO); however, there are several rare genetic disorders, such as Prader–Willi syndrome (PWS), that are also associated with obesity (genetic-induced obesity, GIO). The currently available therapeutics for treating DIO and GIO are very limited, and they result in only a partial improvement. Cannabidiolic acid (CBDA), a constituent of Cannabis sativa, gradually decarboxylates to cannabidiol (CBD). Whereas the anti-obesity properties of CBD have been reasonably identified, our knowledge of the pharmacology of CBDA is more limited due to its instability. To stabilize CBDA, a new derivative, CBDA-O-methyl ester (HU-580, EPM301), was synthesized. The therapeutic potential of EPM301 in appetite reduction, weight loss, and metabolic improvements in DIO and GIO was tested in vivo. EPM 301 (40 mg/kg/d, i.p.) successfully resulted in weight loss, increased ambulation, as well as improved glycemic and lipid profiles in DIO mice. Additionally, EPM301 ameliorated DIO-induced hepatic dysfunction and steatosis. Importantly, EPM 301 (20 and 40 mg/kg/d, i.p.) effectively reduced body weight and hyperphagia in a high-fat diet-fed Magel2 Null mouse model for PWS. In addition, when given to standard-diet-fed Magel2 Null mice as a preventive treatment, EPM301 completely inhibited weight gain and adiposity. Lastly, EPM301 increased the oxidation of different nutrients in each strain. All together, EPM301 ameliorated obesity and its metabolic abnormalities in both DIO and GIO. These results support the idea to further promote this synthetic CBDA derivative toward clinical evaluation in humans.
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Cannabinoids Block Cellular Entry of SARS-CoV-2 and the Emerging Variants.
As a complement to vaccines, small-molecule therapeutic agents are needed to treat or prevent infections by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) and its variants, which cause COVID-19. Affinity selection-mass spectrometry was used for the discovery of botanical ligands to the SARS-CoV-2 spike protein. Cannabinoid acids from hemp (Cannabis sativa) were found to be allosteric as well as orthosteric ligands with micromolar affinity for the spike protein. In follow-up virus neutralization assays, cannabigerolic acid and cannabidiolic acid prevented infection of human epithelial cells by a pseudovirus expressing the SARS-CoV-2 spike protein and prevented entry of live SARS-CoV-2 into cells. Importantly, cannabigerolic acid and cannabidiolic acid were equally effective against the SARS-CoV-2 alpha variant B.1.1.7 and the beta variant B.1.351. Orally bioavailable and with a long history of safe human use, these cannabinoids, isolated or in hemp extracts, have the potential to prevent as well as treat infection by SARS-CoV-2.
Van Breemen and collaborators, including scientists at Oregon Health & Science University, found that a pair of cannabinoid acids bind to the SARS-CoV-2 spike protein, blocking a critical step in the process the virus uses to infect people.
The compounds are cannabigerolic acid, or CBGA, and cannabidiolic acid, CBDA, and the spike protein is the same drug target used in COVID-19 vaccines and antibody therapy. A drug target is any molecule critical to the process a disease follows, meaning its disruption can thwart infection or disease progression.
“These cannabinoid acids are abundant in hemp and in many hemp extracts,” van Breemen said. “They are not controlled substances like THC, the psychoactive ingredient in marijuana, and have a good safety profile in humans. And our research showed the hemp compounds were equally effective against variants of SARS-CoV-2, including variant B.1.1.7, which was first detected in the United Kingdom, and variant B.1.351, first detected in South Africa.”
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The cellular microenvironment plays a critical role in the maintenance of bone marrow-derived mesenchymal stem cells (BM-MSCs) and their subsequent cell lineage differentiation. Recent studies suggested that individuals with adipocyte-related metabolic disorders have altered function and adipogenic potential of adipose stem cell subpopulations, primarily BM-MSCs, increasing the risk of heart attack, stroke or diabetes. In this study, we explored the potential therapeutic effect of some of the most abundant non-euphoric compounds derived from the Cannabis sativa plant (or phytocannabinoids) including tetrahydrocannabivarin (THCV), cannabidiol (CBD), cannabigerol (CBG), cannabidiolic acid (CBDA) and cannabigerolic acid (CBGA), by analyzing their pharmacological activity on viability of endogenous BM-MSCs as well as their ability to alter BM-MSC proliferation and differentiation into mature adipocytes. We provide evidence that CBD, CBDA, CBGA and THCV (5 µM) increase the number of viable BM-MSCs; whereas only CBG (5 µM) and CBD (5 µM) alone or in combination promote BM-MSCs maturation into adipocytes via distinct molecular mechanisms. These effects were revealed both in vitro and in vivo. In addition, phytocannabinoids prevented the insulin signaling impairment induced by palmitate in adipocytes differentiated from BM-MSCs. Our study highlights phytocannabinoids as a potential novel pharmacological tool to regain control of functional adipose tissue in unregulated energy homeostasis often occurring in metabolic disorders including type 2 diabetes mellitus (T2DM), aging and lipodystrophy.
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Chronic Treatment with Cannabidiolic Acid (CBDA) Reduces Thermal Pain Sensitivity in Male Mice and Rescues Hyperalgesia in a Mouse Model of Rett Syndrome.
Rett syndrome (RTT) is a rare neurologic disorder, characterized by severe behavioral and physiological symptoms. RTT is caused by mutations in the MECP2 gene in about 95% of cases and to date no cure is available. Recent evidence suggests that non-euphoric phytocannabinoids (pCBs) extracted from Cannabis sativa may represent innovative therapeutic molecules for RTT, with the cannabinoid cannabidivarin having beneficial effects on behavioral and brain molecular alterations in RTT mouse models. The present study evaluated the potential therapeutic efficacy for RTT of cannabidiolic acid (CBDA; 0.2, 2, 20 mg/kg through intraperitoneal injections for 14 days), a pCB that has proved to be effective for the treatment of nausea and anxiety in rodents. This study demonstrates that systemic treatment with the low dose of CBDA has anti-nociceptive effects and reduces the thermal hyperalgesia in 8 month-old MeCP2-308 male mice, a validated RTT mouse model. CBDA did not affect other behavioral or molecular parameters. These results provide support to the antinociceptive effects of CBDA and stress the need for further studies aimed at clarifying the mechanisms underlying the abnormal pain perception in RTT.
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The clinical use of cannabidiol and cannabidiolic acid–rich hemp in veterinary medicine and lessons from human medicine
The endocannabinoid system (ECS) is an integral neuromodulatory system involved in neuronal development, synaptic plasticity, and homeostasis regarding immunity, as well as brain and other physiological functions such as anxiety, pain, metabolic regulation, and bone growth. Cannabis is a plant that contains exogenous cannabinoids, which have the potential for profound interplay within the ECS as enzymatic inhibitors or receptor-mediated interactions. Activation of cannabinoid receptors leads to various intracellular signaling processes that are involved in cellular functions, but those interactions are diverse due to different affinities of each cannabinoid with relevant receptors. Among the exogenous cannabinoids, cannabidiol (CBD) has drawn attention due to its potential anticancer, antiangiogenic, anti-inflammatory, and antiseizure properties using in vitro and in vivo models. Although scientific evidence is limited in dogs, there appears to be cautious optimism regarding the utilization of CBD in conjunction with other therapeutics for a range of disorders. This review will primarily focus on current scientific research on the efficacy of CBD on seizure, anxiety, osteoarthritis, and atopic dermatitis, following a brief discussion of endo- and exogenous cannabinoids, ECS, their molecular mechanism, and potential side effects in veterinary medicine. Cannabinoid pharmacology and pharmacokinetics will be addressed in the companion Currents in One Health by Schwark and Wakshlag, AJVR, May 2023.
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Novel antibacterial activity of monolaurin compared with conventional antibiotics against organisms from skin infections: an in vitro study.
Introduction
Surveillance of the Seneca Valley virus (SVV) shows a disproportionately higher incidence on Chinese pig farms. Currently, there are no vaccines or drugs to treat SVV infection effectively and effective treatment options are urgently needed.
Methods
In this study, we evaluated the antiviral activity of the following medium-chain fatty acids (MCFAs) or triglycerides (MCTs) against SVV: caprylic acid, caprylic monoglyceride, capric monoglyceride, and monolaurin.
Results
In vitro experiments showed that monolaurin inhibited viral replication by up to 80%, while in vivo studies showed that monolaurin reduced clinical manifestations, viral load, and organ damage in SVV-infected piglets. Monolaurin significantly reduced the release of inflammatory cytokines and promoted the release of interferon-γ, which enhanced the viral clearance activity of this type of MCFA.
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“Some of the viruses inactivated by monolaurin include measles, Herpes simplex-1, vesicular stomatitis, visna virus, and cytomegalovirus. In addition, a number of fungi, yeasts, and protozoa are reported to be inactivated or killed by monolaurin, including several species of ringworm. Candida albicans and the protozoan parasite Giardia lamblia were both reported to be killed by monolaurin.”
Lieberman S, Enig MG, Preuss HG. A Review of Monolaurin and Lauric Acid Natural Virucidal and Bactericidal Agents. Alternative & Complementary Therapies, December 2006. 12(6): 310-314.
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“Lipids can inactivate enveloped viruses, bacteria, fungi, and protozoa…Medium chain length antiviral lipids can be added to human blood products that contain ___ and reduce the cell-free virus concentration by as much as 11 log10 TCID50/ml. The presence of lipids does not interfere with most clinical assays performed on human blood samples. Antimicrobial lipids can disrupt cell membranes and therefore lyse leukocytes which potentially carry viruses.”
Isaacs CE, Kim KS, Thormar H. Inactivation of enveloped viruses in human bodily fluids by purified lipids. Annals of the New York Academy of Sciences. 1994 Jun 6;724:457-64.
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“Unsaturated monoglycerides and alcohols of chain lengths of 16 or 18 carbons were found to be extremely potent inactivators of two enveloped viruses, herpes simplex virus type 2 and bacteriophage phi6”
Sands J, Auperin D, Snipes W. Extreme sensitivity of enveloped viruses, including Herpes Simplex, to long chain unsaturated monoglycerides and alcohols. Antimicrobial Agents and Chemotherapy. 15; 1:67-73, 1979.
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“Glycerol monolaurate (GML) has been proposed as a microbicide component to enhance efficacy by blocking these transmission-facilitating innate immune responses to vaginal exposure. We show here in an especially rigorous test of protection in the SIV-rhesus macaque model of HIV-1 transmission to women, that GML used daily and before vaginal challenge protects against repeat high doses of SIV by criteria that include virological and immunological assays to detect occult infection. We also provide evidence for indirect mechanisms of action in GML-mediated protection.”
Haase AT, Rakasz E, Schultz-Darken N, Nephew K, Weisgrau KL, Reilly CS, Li Q, Southern PJ, Rothenberger M, Peterson ML, Schlievert PM. Glycerol Monolaurate Microbicide Protection against Repeat High-Dose SIV Vaginal Challenge. PLoS One. 2015 Jun 9;10(6):e0129465. doi: 10.1371/journal.pone.0129465. eCollection 2015.
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“Monolaurin is lauric acid but in a safe form for human ingestion and performs the exact same anti-microbial function. From the study, it is seen that lauric acid destroys lipid coated viruses by binding to the lipid protein envelope of virus thereby preventing it from attaching and entering host cells, this kills the viral envelope seen as no growth sign in our observations, thereby killing the virus.”
Ezigbo, Veronica O., Mbaegbu Emmanuella A. Extraction of Lauric Acid from Coconut Oil, Its Applications and Health Implications On Some Microorganisms. African Journal of Education, Science and Technology, April, 2016 Vol 3, No. 2 p144-147
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RNA & DNA Enveloped Viruses, including Herpes
“Monolaurin … were tested for in vitro virucidal activity against 14 human RNA and DNA enveloped viruses in cell culture. At concentrations of 1% additive in the reaction mixture for 1 h at 23°C, all viruses were reduced in infectivity by >99.9%”
Hierholzer, J.C. and Kabara, J.J. In Vitro Effects of Monolaurin Compounds on Enveloped RNA and DNA Viruses. Journal of Food Safety 4:1-12 (1982)
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“Antiviral fatty acids were found to affect the viral envelope, causing leakage and at higher concentrations, a complete disintegration of the envelope and the viral particles. They also caused disintegration of the plasma membranes of tissue culture cells resulting in cell lysis and death.”
Thormar H, Isaacs CE, Brown HR, Barshatzky MR, Pessolano T. Inactivation of enveloped viruses and killing of cells by fatty acids and monoglycerides. AntimicrobialAgents and Chemotherapy. 1987 Jan;31(1):27-31.
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“The antiviral action, attributed to monolaurin (the monoglyceride of lauric acid), is that of solubilizing the lipids and phospholipids in the envelope of the pathogenic organisms causing the disintegration of their outer membrane. There is also evidence that medium-chain fatty acids (MCFA) interfere with the organism’s signal transduction and the antimicrobial effect in viruses is due to interference with virus assembly and viral maturation.”
Arora R, Chawla R, Marwah R, Arora P, Sharma RK, Kaushik V, Goel R, Kaur A, Silambarasan M, Tripathi RP, Bharwaj JR. Potential of Complementary and Alternative Medicine in Preventive Management of NovelH1N1 Flu (Swine Flu) Pandemic: Thwarting Potential Disasters in the Bud. Evidence-Based Complementary and Alternative Medicine Volume 2011 (2011), Article ID 586506, 16 pages
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“Our data indicate that C(12) (lauric acid) is the most inhibitory saturated fatty acid against gram-positive organisms”
Kabara JJ, Swieczkowski DM, Conley AJ, Truant JP. Fatty acids and derivatives as antimicrobial agents. Antimicrobial Agents and Chemotherapy. 1972 Jul;2(1):23-8.
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“Gram (+) bacteria and yeasts but not Gram (-) bacteria were affected by these agents (monolaurin) “
Kabara JJ, Vrable R. Antimicrobial lipids: natural and synthetic fatty acids and monoglycerides. Lipids. 1977 Sep;12(9):753-9.
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“Lauric acid had the same inhibitory action as did capric and myristic acids but monolaurin was inhibitory to V. parahaemolyticus at concentrations as low as 5 mcg/ml. The stronger anti- Vibrio activity of monocaprin and, especially, monolaurin confirms reports by Kato and Shibasaki (7, 10) that fatty acids esters of glycerol do exhibit retarding effects on gram-negative bacteria. Monocaprin and monolaurin had a strong enhancing effect on the thermal destruction of E. coli and P. aeruginosa.”
Beuchat LA. Comparison of antiviral activities of potassium sorbate, sodium benzoate and glycerol and sucrose esters of fatty acids. Appi. Environ. Microbiol. 39:1178, 1980
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“In the presence of Monolaurin… monolaurate had the highest bactericidal activity against E. coli and other Gram-negative bacteria… It may be concluded from various experimental results that the transport of monolaurin into the cell membrane of E. coli was stimulated by the action of citric or polyphosphoric acid”
Kabara JJ. The Pharmacological Effect of Lipids. Champaign, Ill, USA: American Oil Chemist’s Society; 1978. Page 92
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Lyme Disease (caused by Borrelia burgdorferi and Borrelia Garinii)
“The most effective antimicrobial compounds against all morphological forms of the two tested Borrelia sp. were baicalein and monolaurin. This might indicate that the presence of fatty acid and phenyl groups is important for comprehensive antibacterial activity.”
Goc, A., Niedzwiecki, A. and Rath, M. (2015), In vitro evaluation of antibacterial activity of phytochemicals and micronutrients against Borrelia Burgdorferi and Borrelia Garinii. J Appl Microbiol, 119: 1561–1572. doi:10.1111/jam.12970
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“Monolaurin, a coconut oil extract, has also recently been shown to have the ability to significantly affect three morphological forms of Borrelia Burgdorferi and Borrelia Garinii: spirochetes, latent round body forms, and borrelia biofilms, while simultaneously decreasing yeast overgrowth in the GI tract.”
Horowitz, Richard. How Can I Get Better?: An Action Plan for Treating Resistant Lyme & Chronic Disease. St. Martin’s Griffin, 2017. P73
Candida albicans (yeast infections)
“The results show that capric acid, a 10-carbon saturated fatty acid, causes the fastest and most effective killing of all three strains of C. albicans tested, leaving the cytoplasm disorganized and shrunken because of a disrupted or disintegrated plasma membrane. Lauric acid, a 12-carbon saturated fatty acid, was the most active at lower concentrations and after a longer incubation time. In summary, the results show that both capric and lauric acids are active in killing C. albicans and may therefore be useful for treatment of infections caused by that pathogen or others that infect the skin and mucosa.”
Bergsson G, Arnfinnsson J, Steingrímsson O, and Thormar H. In Vitro Killing of Candida albicans by Fatty Acids and Monoglycerides. Antimicrobial Agents and Chemotherapy. 2001 November; 45(11): 3209–3212
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“We recently compared the antimicrobial efficacy of oregano oil and other essential oils as well as monolaurin in vitro by examining a fungus (C albicans) and many different bacteria using a microdilution method. In vivo experiments in mice showed oregano oil and monolaurin, individually and combined, to be as effective as some antibiotics. Oregano oil and/or monolaurin could prove to be useful antimicrobial agents for prevention and therapy of a variety of dangerous infectious organisms under many different circumstances.”
Preuss HG, Echard B, Zonosi RR. The potential for developing natural antibiotics: Examining oregano and monolaurin. Original Internist 2005;12:119–124
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“The kinetics of killing results showed that the [Monolaurin] killed over 90% of yeast cells rapidly within 15 min and caused a complete loss of viability in 120 min. Results of anti-yeast activity in liquid medium by broth (monolaurin) dilution method showed that the growth of both Candida albicans and Saccharomyces cerevisiae was completely inhibited.”
Zhang H, Xu Y, Wu L, Zheng X, Zhu S, Feng F, Shen L. Anti-yeast activity of a food-grade dilution-stable microemulsion. Applied Microbiology and Biotechnology. 2010 July;87(3):1101-8
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“The results from this study showed that lauric acid has an antimicrobial effect. It is most effective against Candida albicans and then staphylococcus followed by Aspergillus Flavus… This goes to say that it is effective against fungus, several viruses and … gram positive bacteria. The study proves that lauric acid is effective against viral, bacterial (gram positive) and fungal infections such as common cold, swine flu, genital herpes, blister etc.”
Ezigbo, Veronica O., Mbaegbu Emmanuella A. Extraction of Lauric Acid from Coconut Oil, Its Applications and Health Implications On Some Microorganisms. African Journal of Education, Science and Technology, April, 2016 Vol 3, No. 2 p144-147
SOURCE INFORMATION: ONLINE LINK
“The lipids… showed high activity against H. pylori, monocaprin and monolaurin being the most active. The high activity of monoglycerides against H. pylori suggests that they may be useful as active ingredients in pharmaceutical formulations.
Bergsson G, Steingrı́msson O, Thormar H. Bactericidal effects of fatty acids and monoglycerides on Helicobacter pylori. International Journal of Antimicrobial Agents. Volume 20, Issue 4, October 2002, Pages 258–262
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“H. pylori were extremely sensitive to monolaurin. Because of their longstanding safety record, origanum and/or monolaurin, alone or combined with antibiotics, might prove useful in the prevention and treatment of severe bacterial infections, especially those that are difficult to treat and/or are antibiotic resistant.”
Preuss HG, Echard B, Enig M, Brook I, Elliott TB. Minimum inhibitory concentrations of herbal essential oils and monolaurin for gram-positive and gram-negative bacteria. Molecular and Cellular Biochemistry. 2005 Apr;272(1-2):29-34.
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“Collectively, our data demonstrate that H. pylori is rapidly inactivated by medium-chain monoacylglycerol esters (monolaurin) and lauric acid and exhibits a relatively low frequency of spontaneous development of resistance to the bactericidal activity of MGs.”
Petschow BW, Batema RP, Ford LL. Susceptibility of Helicobacter pylori to bactericidal properties of medium-chain monoglycerides and free fatty acids. Antimicrobial Agents and Chemotherapy. February 1996 vol. 40 no. 2 302-306
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“These results suggest that H. pylori present in the stomach contents (but not necessarily within the mucus barrier) should be rapidly killed by the millimolar concentrations of fatty acids and monoglycerides (monolaurin) that are produced by pre-intestinal lipase(s) acting on suitable triglycerides such as milkfat”
“The results in this research provide a possible strategy for a new treatment for H. pylori infection that would be characterized by minimal side-effects and low bacterial resistance”
Sun CQ, O’Connor CJ, Roberton AM. Antibacterial actions of fatty acids and monoglycerides against Helicobacter pylori. FEMS Immunology and Medical Microbiology 36 (2003) 9-17
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“Virgin Coconut Oil (VCO) and its most active individual fatty acids were tested to evaluate their antimicrobial effect on C. difficile in vitro. The data indicate that exposure to lauric acid (C12) was the most inhibitory to growth (P<.001), as determined by a reduction in colony-forming units per milliliter.”
Shilling M, Matt L Rubin E Visitacion MP., Haller N. A., Grey S. F., and Woolverton C. J. Antimicrobial Effects of Virgin Coconut Oil and Its Medium-Chain Fatty Acids on Clostridium difficile. Journal of Medicinal Food. December 2013, 16(12): 1079-1085.
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“Entamoeba Histolytica (E. histolytica) and Giardia lamblia (G. lamblia) are common causes of diarrhea and malabsorption in humans. Monolaurin, the monoglyceride of lauric acid, is the most powerful antiviral, antibacterial and antifungal fatty acid found in coconut oil. It has the greatest overall antimicrobial effect. It also had an antiparasitic effect on blastocysts in vitro. Monolaurin which is a natural compound derived from coconut was evaluated for its antigiardial effects on giardia. In the group (4) receiving monolaurin post infection, the number of trophozoites and cysts forms of G. lamblia in intestinal contents were 87.34 and 91.15%, respectively compared to the infected control group.”
Fahmy ZH, Aly E, Shalsh I, Mohamed AH. The effect of medium chain saturated fatty acid (monolaurin) on levels of the cytokines on experimental animals in Entamoeba Histolytica and Giardia lamblia infection. African Journal of Pharmacy and Pharmacology. January 2014.
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Listeria monocytogenes (causes listeriosis)
“Decrease in the pH and temperature values have increased the antilisterial activity of monolaurin and the essential oil. The lowest MIC value of monolaurin and essential oil was observed at pH 5 and 5˚C. According to our results, the oil alone or in combination with monolaurin at low pH and temperature conditions showed a promising inhibitory effect on L. monocytogenes.”
Raeisi M, Tajik H, Razavi Rohani SM, Tepe B, Kiani H, Khoshbakht R, Shirzad Aski H, Tadrisi H. Inhibitory effect of Zataria multiflora Boiss. essential oil, alone and in combination with monolaurin, on Listeria monocytogenes. Vet Res Forum. 2016 Winter;7(1):7-11. Epub 2016 Mar 15.
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“We show that [monolaurin] inhibits the synthesis of most staphylococcal toxins and other exoproteins and that it does so at the level of transcription. We find that [monolaurin] blocks the induction but not the constitutive synthesis of beta-lactamase, suggesting that it acts by interfering with signal transduction.”
Projan SJ, Brown-Skrobot S, Schlievert PM, Vandenesch F, Novick RP. Glycerol monolaurate inhibits the production of beta-lactamase, toxic shock toxin-1, and other staphylococcal exoproteins by interfering with signal transduction. Journal of Bacteriology. 1994 Jul;176(14):4204-9.
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“Lauric acid, present in heavy concentrations in coconuts, forms monolaurin in the body that can inhibit the growth of pathogenic microbes… monolaurin may prove to be useful antimicrobial agents for prevention and therapy of Staphylococcus aureus infections”
Preuss HG, Echard B, Dadgar A, Talpur N, Manohar V, Enig M, Bagchi D, Ingram C. Effects of Essential Oils and Monolaurin on Staphylococcus aureus: In Vitro and In Vivo Studies. Toxicology Mechanisms and Methods. 2005; 15(4):279-85
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“With Lauric Acid, Staph. Aureus and Strep Agalactiae were reduced 81.3 and 49.6%, respectively”
Boddie RL, Nickerson SC. Evaluation of postmilking teat germicides containing Lauricidin, saturated fatty acids, and lactic acid. Journal of Dairy Science. 1992 Jun ;75(6):1725-30.
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“Microbial killing by milk lipids is due primarily to free fatty acids (FFAs) and monoglycerides (MGs) released from milk triglycerides by lipases and can be duplicated using purified FFAs and MGs (ie: monolaurin)”
Isaacs CE, Thormar H. The role of milk-derived antimicrobial lipids as antiviral and antibacterial agents. Advances in Experimental Medicine and Biology. 1991; 310:159-65
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“Glycerol monolaurate inhibited lipase production by S. Aureusand S. Epidermidis at concentrations that did not adversely affect bacterial cell growth. GML can be used to inhibit ocular bacterial lipase production without proving detrimental to commensal bacteria viability.”
Flanagan JL, Khandekar N, Zhu H, Watanabe K, Markoulli M, Flanagan JT, Papas E. Glycerol Monolaurate Inhibits Lipase Production by Clinical Ocular Isolates Without Affecting Bacterial Cell Viability. Investigative Ophthalmology & Visual Science February 2016, Vol.57, 544-550. doi:10.1167/iovs.15-17180
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“Sensitivity rates of Gram-positive Staphylococcus aureus, Streptococcus spp., and coagulase-negative Staphylococcus, Gram-negative E. vulneris, Enterobacter spp., and Enterococcus spp. to 20 mg/ml monolaurin was 100% and of Klebsiella rhinoscleromatis was 92.31%. Escherichia coli had progressively less dense colony growths at increasing monolaurin concentrations, and at 20 mg/ml was less dense than the control. Staphylococcus aureus, coagulase-negative Staphylococcus, and Streptococcus spp. did not exhibit any resistance to monolaurin and had statistically significant (P <.05) differences in resistance rates to these antibiotics….Monolaurin has statistically significant in vitro broad-spectrum sensitivity against Gram-positive and Gram-negative bacterial isolates from superficial skin infections. Most of the bacteria did not exhibit resistance to it.”
Carpo BG, Verallo-Rowell VM, Kabara J. Novel antibacterial activity of monolaurin compared with conventional antibiotics against organisms from skin infections: an in vitro study. J Drugs Dermatol. 2007 Oct;6(10):991-8.
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Biofilms (Biofilm “Buster”)
“Biofilm provides a bacterial hiding place by forming a physical barrier and causing physiological changes in cells. The elimination of biofilm is the main goal of hygiene. Monoacylglycerols (monolaurin) are recognized as safe and are used in food as emulsifiers… Monoacylglycerols with two specific lengths of fatty acid moiety, monolaurin and Monobehenin, were found to have strong inhibitory activity toward bacterial biofilm formation of S. Mutans, X. Oryzae, and Y. Enterocolitica in a strain specific manner.”
Ham Y, Kim T-J. Inhibitory activity of monoacylglycerols on biofilm formation in Aeromonas Hydrophila, Streptococcus Mutans, Xanthomonas Oryzae, and Yersinia Enterocolitica. SpringerPlus. 2016;5(1):1526. doi:10.1186/s40064-016-3182-5
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“Both Glycerol Monolaurate and lauric acid were effective in inhibiting biofilm development as measured by decreased numbers of viable biofilm-associated bacteria as well as decreased biofilm biomass. Compared with lauric acid on a molar basis, GML represented a more effective inhibitor of biofilms formed by either S. aureus or E. faecalis.”
Hess DJ, Henry-Stanley MJ, Wells CL. The Natural Surfactant Glycerol Monolaurate Significantly Reduces Development of Staphylococcus aureus and Enterococcus faecalis Biofilms. Surg Infect (Larchmt). 2015 Oct;16(5):538-42. doi: 10.1089/sur.2014.162. Epub 2015 Jun 25.
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Monolaurin & Drug Resistance
“Monolaurin has statistically significant in vitro broad-spectrum sensitivity against Gram-positive and Gram-negative bacterial isolates from superficial skin infections. Most of the bacteria did not exhibit resistance to it.”
Carpo BG, Verallo-Rowell VM, Kabara J Novel. Antibacterial activity of Monolaurin compared with conventional antibiotics against organisms from skin infections: an in vitro study. Journal of Drugs in Dermatology : JDD [2007, 6(10):991-998]
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“Glycerol monolaurate (GML) is a surfactant that has been found to inhibit the post-exponential phase activation of virulence factor production and the induction of beta-lactamase in Staphylococcus aureus. We found that GML suppresses growth of vancomycin-resistant Enterococcus faecalis on plates with vancomycin and blocks the induction of vancomycin resistance, which involves a membrane-associated signal transduction mechanism, either at or before initiation of transcription.”
Ruzin A, Novick RP. Glycerol monolaurate inhibits induction of vancomycin resistance in Enterococcus faecalis. Journal of Bacteriology. 1998 Jan; 180(1):182-5
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“Glycerol monolaurate (GML) inhibits the expression of virulence factors in Staphylococcus aureus and the induction of vancomycin resistance in Enterococcus faecalis, presumably by blocking signal transduction”
Ruzin A, Novick RP. Equivalence of lauric acid and glycerol monolaurate as inhibitors of signal transduction in Staphylococcus aureus. Journal of Bacteriology. 2000 May; 182(9):2668-71
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“Because of their longstanding safety record, origanum and/or monolaurin, alone or combined with antibiotics, might prove useful in the prevention and treatment of severe bacterial infections, especially those that are difficult to treat and/or are antibiotic resistant.”
Preuss HG, Echard B, Enig M, Brook I, Elliott TB. Minimum inhibitory concentrations of herbal essential oils and monolaurin for gram-positive and gram-negative bacteria. Molecular and Cellular Biochemistry. 2005 Apr;272(1-2):29-34.
SOURCE INFORMATION: ONLINE LINK
“Medium-chain saturated fatty acids are well known for their virucidal effects against viruses with lipid membranes as well as against numerous other pathogenic organisms. These antimicrobial fatty acids and their derivatives are essentially non toxic to man; they are produced in vivo by humans when they ingest those foods that contain adequate levels of the appropriate medium-chain saturated fatty acids such as lauric acid. The lauric oils such as coconut oil or palm kernel oil, both of which are GRAS, can provide a unique source of both antimicrobial lipids and needed calories.”
Enig M. Lauric oils as antimicrobial agents: Theory of effect, scientific rationale, and dietary application as adjunct nutritional support for H_V infected individuals. In: Watson R, ed. Nutrients and Foods in AIDS. Boca Raton, FL: CRC Press, 1998.
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“The data demonstrated that the fatty acids exhibited patterns of inhibition against oral bacteria with some specificity that appeared related more to the bacterial species that the general structural characteristics of the microorganism”
Huang CB, Alimova Y, Myers TM, Ebersole JL. Short- and medium-chain fatty acids exhibit antimicrobial activity for oral microorganisms. Archives of Oral Biology. 2011 July; 56(7):650-4
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“Even if lipids are toxic in cell cultures, studies have shown that they are not toxic to skin and mucosa at much higher concentrations. Thus, hydrogels containing monocaprin at a concentration of 5 mg/ml (20 mM) have been shown not to cause irritation of the vaginal mucosas of mice and rabbits or the skin of hairless mice.”
Bergsson G, Arnfinnsson J, Steingrímsson O, and Thormar H. In Vitro Killing of Candida albicans by Fatty Acids and Monoglycerides. Antimicrobial Agents and Chemotherapy. 2001 November; 45(11): 3209–3212
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In laboratory experiments using rodents infected with Entamoeba Histolytica and Giardia lamblia (protozoan which cause diarrhea), monolaurin was used to treat the infection. For subjects infected with Giardia lamblia, those who were treated with monolaurin pre-infection saw a 74% reduction in cysts, for those treated with monolaurin post-infection saw a 91% reduction of cysts. For subjects infected with E. histolytica, those treated before infection saw a 77% reduction in cysts and those treated after infection saw a 90% reduction in cysts. Control groups saw a 0% reduction.
Fahmy ZH, Aly E, Shalsh I, Mohamed AH. The effect of medium chain saturated fatty acid (monolaurin) on levels of the cytokines on experimental animals in Entamoeba Histolytica and Giardia lamblia infection. African Journal of Pharmacy and Pharmacology. January 2014.
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“A daily intake of 3-9g of Monolaurin has been found to be required to provide a pharmacological effect. Thus the provision of this quantity of monolaurin to be derived from coconut oil would require an unrealistic intake of 100-300mL/day”
Kabara JJ. Pharmacological effects of coconut oil vs. monoglycerides. Inform June 2005; Volume 16 p386-7.
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“In vivo, the groups receiving vancomycin, monolaurin, or the combination showed some protection – 50-70% survival, whereas the protection from the coconut oils were virtually the same as control-0-16% survival. Although we did not find that the two coconut oils are helpful to overcome S. aureus infections”
Manohar V, Echard B, Perricone N, Ingram C, Enig M, Bagchi D, Preuss HG. In vitro and in vivo effects of two coconut oils in comparison to monolaurin on Staphylococcus aureus: rodent studies. Journal of Medicinal Food. 2013 June.
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“In humans, lauric acid cannot be ingested in order to cure these infections as it is highly irritating, but monolaurin which is lauric acid chemically bonded to glycerin can be ingested to perform these activities. Lauric acid is not an antibiotic, it has no effect on desirable digestive bacteria – only on unwanted microorganisms. The use of coconut oil as an alternative to many chemical supplements for cure of fungal, viral and bacterial infections is evident from the study.”
Ezigbo, Veronica O., Mbaegbu Emmanuella A. Extraction of Lauric Acid from Coconut Oil, Its Applications and Health Implications On Some Microorganisms. African Journal of Education, Science and Technology, April, 2016 Vol 3, No. 2 p144-147
SOURCE INFORMATION: ONLINE LINK
Cells from human colostrum, collected from mothers within 48 hours of delivery, were examined for their capacity to phagocytose and kill Eschericia coli and Candida albicans. The phagocytic power of colostral cells was comparable to that of blood leukocytes from the same individuals. In contrast, the capacity of colostral cells to kill microorganisms was significantly less than that of blood leukocytes. Preincubation of blood leukocytes with colostrum supernatant did not reduce phagocytic indices, but reduced E. coli killing by 48% and C. albicans killing by 66%. The role of colostral cells in protecting the neonate from infection is discussed in the light of these findings.
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Colostrum and Lactoferrin Protect against Side Effects of Therapy with Antibiotics, Anti-inflammatory Drugs and Steroids, and Psychophysical Stress: A Comprehensive Review
LF and complete native colostrum, preferably administered with probiotic bacteria, are highly recommended for inclusion in therapeutic protocols in NSAIDs and corticosteroid anti-inflammatory, as well as antibiotic, therapies.
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Nowadays, the search for food products that promote consumers’ health has gained interest, and dairy by-products, due to their biological quality, could have a prominent position among products with health benefits. However, little is known about their activity on cancer cells.
This study aimed to provide evidence about the effect of ovine colostrum and milk whey on K562 cells, a model of the human chronic myeloid leukemia cell line. The exposure of K562 cells to a single administration of sheep by-products at different concentrations for three days and three treatments for three days was carried out. Using a flow cytometric approach, we found that CD235a expression remained stable in the cells exposed to ovine whey (milk and colostrum) at concentrations ranging from 1 ng/mL to 100 μg/mL, after three days from one or three administrations, respectively. A significant reduction in fluorescent cells was observed in the populations exposed to 1 mg/mL of both milk and colostrum at the same time points. In these conditions, the size and granularity of the leukemic cells also changed, with a substantial reduction in the number of actively dividing cells in the S phase of the cell cycle. This phenomenon was highlighted by the Annexin V/PI cytofluorimetric test, which is able to provide quantitative results regarding the population of cells in early or late apoptosis or necrotic cells after exposure to a single dose or three doses of colostrum or sheep whey for three days, respectively. This report showed that both colostrum and milk whey were able to modify the phenotypic profile and cell cycle of the K562 cell line, inducing apoptosis at the highest concentration.
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BC is reported as safe for human consumption. There are no contraindications regarding high dose intake and few side effects of clinical relevance have been registered [16,17]. Due to its composition, BC consumption is being encouraged as a nutritional supplement for newborns, children, and adults who have no restrictions on bovine milk consumption [18]. An increasing number of clinical trials gather significant results that advocate in favor of the use of bovine colostrum as a nutraceutical food or supplement (e.g. https://trialbulletin.com/lib/trials/term=Colostrum). Its beneficial effects on prophylaxis and treatment of gastrointestinal disorders (Fig. 1) are mainly related to the numerous immunomodulating components, which maintain and recover gastrointestinal tract health [19]. Several studies indicate that colostrum consumption can reduce the occurrence and severity of digestive disorders such as diarrhea and alleviate inflammatory bowel disease. It can also contribute to preventing and treating colon problems, short bowel syndrome and constipation [4,16,[20], [21], [22]]. Furthermore, there is evidence showing the relationship between the immune responses triggered in the intestine by BC supplementation and the immunity of the respiratory system [23].
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We provide a review of BC composition and its effects in infants and children in health and selected diseases (diarrhea, infection, growth-failure, preterm birth, necrotizing enterocolitis (NEC), short-bowel syndrome, and mucositis). Human trials and animal studies (mainly in piglets) are reviewed to assess the scientific evidence of whether BC is a safe and effective antimicrobial and immunomodulatory nutritional supplement that reduces clinical complications related to preterm birth, infections, and gut disorders.
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Lauric acid (LA) has a broad spectrum of anti-microbiological activities against enveloped viruses and various bacteria, and might be useful to protect against microbial infection and control the balance and distribution of bacteria in human gut microbiota. It is not necessarily more difficult to measure antimicrobial activity the traditional way, but it is, however, more laborious. In the present study, we developed a new method to measure the antimicrobial activity of LA in multiple samples with a microplate reader. A “test complex” (TC) was produced consisting of 100 μL of agar medium with LA in the bottom layer and 300 μL of broth in the top layer in 96-well deep-well microplates. Afterward, analysis of the broth in the top layer showed that the antimicrobial activity was the same as that of the “control complex,” (CC) which consisted of 100 μL of agar medium in the bottom layer and 300 μL of broth with LA in the top layer. Furthermore, evaluation of the antimicrobial effect of the TC when using a microplate reader was the same as that with the use of the colony counting method. The colony counting method has confirmed that the antimicrobial activity of LA when bacteria are inoculated into the broth was equivalent between CC and TC, and we validated this by correlating the number of bacteria with absorbance. In addition, the broth itself in TC was transparent enough that the turbidity of broth can be used as an index of the number of bacteria, which enabled the use of a microplate reader for multiple samples. For human gut microbes, LA was shown to have low antimicrobial activity against commensal lactic acid bacteria, but high antimicrobial activity against Pathogenic Bacteroides and Clostridium, suggesting that LA might modulate intestinal health, as confirmed by the proposed method.
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SOURCE INFORMATION: ONLINE LINK
Lauric acid, a 12‑carbon atom medium chain fatty acid (MCFA), has strong antioxidant and antidiabetic activities. However, whether lauric acid can ameliorate hyperglycemia-induced male reproductive damage remains unclear. The study aimed to determine the optimal dose of lauric acid with glucose-lowering activity, antioxidant potential and tissue-protective effects on the testis and epididymis of streptozotocin (STZ)-induced diabetic rats. Hyperglycaemia was induced in Sprague Dawley rats by an intravenous injection of STZ at a dose of 40 mg/kg body weight (BWT). Lauric acid (25, 50 and 100 mg/kg BWT) was administered orally for eight weeks. Weekly fasting blood glucose (FBG), glucose tolerance and insulin sensitivity were examined. Hormonal profiles (insulin and testosterone), lipid peroxidation (MDA) and antioxidant enzyme (SOD and CAT) activities were measured in the serum, testis and epididymis. The reproductive analyses were evaluated based on sperm quality and histomorphometry. Lauric acid administration significantly improved FBG levels, glucose tolerance, hormones-related fertility and oxidant-antioxidant balance in the serum, testis and epididymis compared to untreated diabetic rats. Treatment with lauric acid preserved the testicular and epididymal histomorphometry, along with the significant improvements in sperm characteristics. It is shown for the first time that lauric acid treatment at 50 mg/kg BWT is the optimal dose for ameliorating hyperglycemia-induced male reproductive complications. We conclude that lauric acid reduces hyperglycemia by restoring insulin and glucose homeostasis, which attributes to the regeneration of tissue damage and sperm quality in STZ-induced diabetic rats. These findings support the correlation between oxidative stress and hyperglycemia-induced male reproductive dysfunctions.
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Nowadays, the search for food products that promote consumers’ health has gained interest, and dairy by-products, due to their biological quality, could have a prominent position among products with health benefits. However, little is known about their activity on cancer cells.
Butyric-lauric acid structural lipid relieves liver inflammation and small intestinal microbial disturbance: In obese male C57BL/6 mice
Butyric acid and lauric acid are short chain and medium chain fatty acids, respectively. Their anti-inflammatory and lipid metabolism regulating functions are reported, while their structural lipid functional activity still needs to be verified. In this study, obese mice induced by a high-fat diet (HFD) were used to investigate the effects of butyric-lauric acid structural lipid (SBL) on inflammation and small intestinal microbes. In vivo, although SBL did not significantly reduce body weight (P > 0.05), it might have a positive effect on mouse liver health. Compared to the corresponding physical mixture (MBL), SBL treatment could better downregulate hepatic TNF-α, IL-1β and IL-6 expression and stimulate IL-10 expression. Similarly, compared with the HF group, the liver IL-1β and TNF-α levels in the LSBL treatment group decreased by 15.2% and 22.9%, respectively (P < 0.05). In addition, HSBL treatment increased the content of IL-10 in the liver of obese mice (increased by 26.8%, P < 0.05). Moreover, SBL more significantly upregulated Bifidobacterium abundance and inhibited the high-fat diet-induced increase in Faecal Baculum abundance. In all, SBL ameliorated HFD-induced liver inflammation and these improvements are closely associated with its positive effects on small intestinal microbiota. This study aimed to provide support and new perspectives for the development and functional exploration of short-and medium-chain fatty acid structural lipids.
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SOURCE INFORMATION: ONLINE LINK
Virgin Coconut Oil is usually extracted from well matured and fresh coconut through specialized processes without damaging its natural nutrition. In this work, formulation, characterization and efficacy of VCO-SLPs have been studied. VCO-SLPs were prepared using ultra-sonification of molten stearic acid and virgin coconut oil in an aqueous solution and particles with the size of 0.608 µm have been obtained. 20% concentration of VCO-SLPs of 0.608 µm particle size was added into the base lotion. Sensory study and skin evaluation study was conducted to compare the difference between lotion containing VCO-SLPs and lotion without VCO-SLPs. Moisturizing lotion incorporated with VCO-SLPs was found to increase skin hydration and skin elasticity by 24.8% and 2.60% respectively from day 0 to day 28. This shows that solid lipid particles have the potential to be utilized as a carrier for improved dermal delivery of VCO.
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Lauric acid, a naturally occurring medium-chain saturated fatty acid, is known to exhibit high intestinal absorption and a higher propensity for lymphatic absorption. To tap these advantages for nanoparticle-mediated sustained drug delivery, solid lipid nanoparticles of lauric acid (LA-SLN) were prepared by the hot homogenization method. A fluorescent lipophilic dye, Rhodamine B (RhB), was incorporated into the LA-SLN (R-LA-SLN) as a model drug. The particle size and the zeta potential of the LA-SLN were 21.42 ± 1.83 nm and −3.17 ± 0.21 mV, respectively, in the phosphate buffer. The encapsulation efficiency and drug loading capacity achieved by R-LA-SLN were about 80.31 ± 0.18 % and 1.02 ± 0.02 %, respectively. In vitro studies revealed a biphasic drug release pattern and were found to follow a Fickian diffusion model. It was found that 52 % RhB was released from R-LA-SLN in the initial 4 h and 71 % in 10 h. The cytotoxic response of LA-SLN was tested on colorectal cancer cells and it elicited only mild cytotoxicity. The cellular uptake studies conducted with colon cancer cells revealed that R-LA-SLN uptake by the cells was twice that of free RhB. The confocal microscopy and Raman mapping showed localization of R-LA-SLN in the cytoplasm on cellular uptake. R-LA-SLN was found to mediate tight junction opening and increased the paracellular permeability by 6 times over free RhB. Mucoadhesion of LA-SLN to the rat intestinal colon mucosa was 1.7 times higher than that of chitosan control, indicating the probability of a longer-duration drug release in the colon.
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