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Health properties of coconut oil
Abstract
Coconut oil has a long history of use throughout the world as both a food and as a medicine. Over the past 50 years research has shown that coconut oil possesses unique properties with important nutritional and medical applications. Coconut oil is unique in that it is composed predominately of a special group of saturated fats known as medium-chain triglycerides (MCT). Although MCT are classified as saturated fats they do not contribute to cardiovascular disease. Evidence shows they may actually protect against it. Studies have shown that populations that use coconut oil as their primary source of dietary fat have very low rates of cardiovascular disease. Coconut oil is easier to digest than other fats, improves nutrient absorption, does not contribute to weight gain, stimulates metabolism, boosts energy, possesses potent antimicrobial properties, and improves energy metabolism in the brain. All these features suggest that coconut oil is a healthy choice with important nutritional and medicinal applications.
... Due to its rapid metabolism, MCT oils are beneficial in preventing and treating obesity. MCT oil unique physicochemical properties are also known to be beneficial for improving health condition in general and lipid profile in particular [4][5][6][7][8]. ...
... High levels of HDL-C have been considered as a good indicator of a healthy heart. HDL-C below 40 mg/dl is considered as major risk factor of cardiovascular disease, whereas HDL-C higher than 60 mg/dl is considered optimal [7,21,28]. ...
Objective: The objective of this study was to investigate the effect of virgin coconut oil (VCO) and hydrolyzed VCO (HVCO) on lipid profile and liver enzymes in dyslipidemic rats.Methods: VCO was hydrolyzed using lipase from Rhizomucor miehei (active on sn-1,3 position). Thirty male rats (150–200 g) were induced with 2 ml/kg body weight (BW) egg yolk and lard oil twice a day for 30 days. Rats were divided into six groups which were given with sodium carboxymethylcellulose 0.5%, atorvastatin, VCO (4 and 6 ml/kg BW), and HVCO (4 and 6 ml/kg BW). Lipid profile including total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), very low-density lipoprotein cholesterol (VLDL-C), and liver enzymes including serum glutamic oxaloacetic transaminase (SGOT) and serum glutamic pyruvic transaminase (SGPT) were measured after 14 days of treatment.Results: The results of this study show that VCO and HVCO improve lipid profile (decrease in TC, TG, LDL-C, and VLDL-C, but increase in HDL-C). VCO and HVCO also lower atherogenic index, TC/HDL-C ratio, LDL-C/HDL-C ratio, SGOT, and SGPT. Result shows that HVCO improves lipid profile and liver enzymes better than VCO does.Conclusion: VCO and HVCO improve lipid profile in dyslipidemic rats, not atherogenic, and not toxic to the liver. HVCO causes better lipid profile improvement, especially with 6 ml/kg BW dosage.
... This medium-chain triglyceride is claimed to have greater anti-viral and anti-bacterial properties [12]. Studies have shown that palm kernel oil, coconut oil and laurel oil are composed of approximately 50 percent of the lauric acid [13]. Lauric acid has been shown to be associated with deleterious effect in atherosclerosis [14]. ...
... However, the high content of lauric acid in coconut oil can significantly increase the high-density lipoprotein (HDL) cholesterol level, thus reducing the risk of developing cardiovascular diseases. Therefore, lauric acid is widely used in nutritional and medical applications due to its lack of hypercholesterolemic effects properties [13]. ...
Objective: To investigate the effect of different concentrations of lauric acid on Intercellular Adhesion Molecule-1 (ICAM-1) and Vascular Cell Adhesion Molecule-1 (VCAM-1) expression in IFN-γ stimulated human monocytic THP-1 cell line.
Methods: THP-1 cell were cultured using Roswell Park Memorial Institute medium supplemented with 10% fetal bovine serum. THP-1 monocytes were firstly differentiated into macrophages by using phorbol-12-myristate-13-acetate. IFN-γ response test was performed and total cellular RNA was extracted using TRI Reagent® LS before q-RT-PCR was carried out. Subsequently, IFN-γ treated THP-1 macrophages were stimulated with increasing doses of lauric acid for another 24 h, before q-RT-PCR.
Results: The mRNA expression levels of ICAM-1 and VCAM-1 were normalized to β-actin and relatived to the untreated cells. The expressions of ICAM-1 and VCAM-1 were significantly induced in cells treated with 10 ng/mL of IFN-γ. This showed that IFN-γ could up-regulate inflammatory process and may cause atheroma formation. MTT assay was carried out to investigate the effect of lauric acid on undifferentiated and differentiated THP-1 cells. Although lauric acid did not have any significant impact on undifferentiated and differentiated THP-1 cell viability, the normalized fold expressions of ICAM-1 and VCAM-1 in IFN-γ-treated THP-1 macrophages were decreased significantly in a dose dependent manner with the presence of increasing doses of lauric acid.
Conclusions: This study successfully proved that lauric acid was able to antagonize the up-regulatory effect of IFN-γ on ICAM-1 and VCAM-1 expressions in THP-1 macrophages. This indicates that lauric acid may be an anti-inflammatory therapeutic and prophylaxis agent for atherosclerosis.
... Lauric acid which is a disease-fighting substance that has many health benefits303132, is abundant in coconut oil. Fife [33] also mentioned that coconut oil improves nutrient absorption, boosts energy, possesses potent antimicrobial properties, and improves energy metabolism in the brain. There have been emerging fundamental evidences to explain the positive clinical effects of VCO on human health. ...
... However, after VCO supplementation , the mean score of the intervention group declined and no significant difference between the two groups was detected. Coconut oil is unique, known as medium-chain triglycerides that are usually used to improve patients' nutritional status [32,33]. In addition, maintaining a good appetite can promote wound healing and encourage a speedy recovery from illness [7]. ...
Background
Breast cancer is the most common cancer amongst Malaysian women. Both the disease and its treatment can disrupt the lives of the woman and adversely affect all aspects of life and thus can alter a woman’s quality of life. The aim of this study was to examine the effect of virgin coconut oil (VCO) on the quality of life (QOL) of patients diagnosed with breast cancer.
Methods
This was a prospective study of breast cancer patients admitted into the Oncology Unit of Hospital Universiti Sains Malaysia, Kubang Kerian, Kelantan, Malaysia. The sample consisted of 60 patients with stage III and IV breast cancer allocated to either an intervention group (n = 30) or a control group (n = 30) using a simple random table. QOL was evaluated from the first cycle of chemotherapy to the sixth cycle, and data were collected using a validated Bahasa Malaysia version of the European Organization for Research and Treatment of Cancer Quality of Life Questionnaire Breast Cancer Module (EORTC QLQ-C30) and its breast-specific module (QLQ-BR 23).
Results
The mean age of breast cancer patients was 50.2 (SD = 13.5) years. There were significant mean score differences for functioning and global QOL between groups (α < 0.01). The intervention group also had better scores for symptoms including fatigue, dyspnea, sleep difficulties, and loss of appetite compared to the control group. Although there are deteriorations for sexual enjoyment, the intervention group exhibited improvement in breast functioning and symptom scores for body image, sexual function, future perspective, breast symptoms, and systemic therapy side effects.
Conclusion
VCO consumption during chemotherapy helped improve the functional status and global QOL of breast cancer patients. In addition, it reduced the symptoms related to side effects of chemotherapy.
... Its antibacterial effects are attributed to the active compound monolaurin (product of lauric acid metabolization), which destroys the fatty layer of RNA/DNA of pathogenic bacteria, virus, fungi, and protozoa. 39,40 A study by Aritonang et al 39 tested the shelf life of poultry chicken at room temperature submersed in virgin coconut oil (VCO) for the following 4 different durations: (1) 0 hour (control), (2) 1 hour, (3) 2 hours, and (4) 3 hours. They reported that chicken meat submersed in VCO showed decreased moisture content and decreased bacteria colonies whereas increased protein content in comparison with chicken meat with no submersion. ...
Formalin, a common laboratory fixative, is a type 1 carcinogen, a biohazard with risks, environmental, disposal and legal costs, and a chemical modifier of protein epitopes in tissue. A less toxic tissue preservation method is therefore badly needed. We have developed a novel tissue preservation media, Amber, composed of Low Potassium Dextran Glucose (LPDG), 10% honey and 1% coconut oil. This work investigates Amber as compared to formalin with respect to: (1) histological preservation, (2) epitope integrity with immunohistochemistry (IHC) and immunofluorescence (IF), and (3) integrity of tissue RNA. Rat and human lung, liver, kidney and heart tissues were collected and stored for 24 h at 4 °C in Amber or formalin. Tissues were evaluated with: Hematoxylin and Eosin (H&E); IHC: Thyroid Transcription Factor (TTF-1), Muscle Specific Actin (MSA), Hepatocyte Specific Antigen (HepPar1) and Common Acute Lymphoblastic Leukemia Antigen (CD10); and IF: VE-cadherin, vimentin (VIM) and muscle specific actin (MSA). RNA quality upon extraction was also assessed. Amber demonstrated superior and/or non-inferior performance in rat and human tissue evaluation with respect to standard techniques of histology, immunohistochemistry, immunofluorescence, and extracted RNA quality. Amber maintains high quality morphology without compromising the ability to perform IHC and nucleic acid extraction. As such, Amber could be a safer and superior substitute to formalin for clinical tissue preservation for contemporary pathological examination.
... Our study focuses on lauric acid, a 12-carbon saturated medium chain fatty acid (MCFA). Lauric acid is the main saturated fatty acid that found abundantly in coconut oil and palm oil (Fife 2013). Although lauric acid is a saturated fatty acid, it is less obesogenic as compared to long chain fatty acid (LCFA) intakes (McCarty & DiNicolantonio 2016). ...
The metabolism of alcohol involves cytochrome P450 2E1 (CYP2E1)-induced oxidative stress, with the association of phosphatidylinositol-3-kinases (PI3K) and nuclear factor kappa B (NFκB) signalling pathways. CYP2E1 is primarily involved in the microsomal ethanol oxidising system, which generates massive reactive oxygen species (ROS) and ultimately leads to oxidative stress and tissue damage. Lauric acid, a major fatty acid in palm kernel oil, has been shown as a potential antioxidant. Here, we aimed to evaluate the use of lauric acid as a potential antioxidant against ethanol-mediated oxidative stress by investigating its effect on CYP2E1 mRNA expression and the signalling pathway in ethanol-induced HepG2 cells. HepG2 cells were firstly treated with different concentrations of ethanol, and subsequently co-treated with different concentrations of lauric acid for 24 h. Total cellular RNA and total protein were extracted, and qPCR and Western blot was carried out. Ethanol induced the mRNA expression of CYP2E1 significantly, but lauric acid was able to downregulate the induced CYP2E1 expression in a dose-dependent manner. Similarly, Western blot analysis and densitometry analysis showed that the phosphorylated PI3K p85 (Tyr458) protein was significantly elevated in ethanol-treated HepG2 cells, but co-treatment with lauric acid repressed the activation of PI3K. However, there was no significant difference in NFκB pathway, in which the normalised NFκB p105 (Ser933) phosphorylation remained constant in any treatment conditions in this study. This suggests that ethanol induced CYP2E1 expression by activating PI3K p85 (Tyr458) pathway, but not the NFκB p105 (Ser933) pathway in HepG2 cells.
... The principal biochemical components of coconut oil and their potential health benefits are *Address correspondence to this author at the Division of Physiology, Biochemistry and Post Harvest Technology (PB&PHT), ICAR-Central Plantation Crops Research Institute (ICAR-CPCRI), Kasaragod, Kerala, India; E-mail: ramesh.sv@icar.gov.in presented in Table 1 [2][3][4][5][6][7][8][9][10]. Coconut oil is rich in mediumchain triglycerides (MCTs) (C6 to C12 fatty acids). ...
Background: COVID-19 caused by the novel SARS Coronavirus-2 (SARS-CoV-2) is causing serious blockades in the global public health sphere. In the absence of a powerful antiviral treatment, exploration of plant-based products with antiviral potential has gained interest.
Scope and Approach: This commentary presents the prospects of utilizing coconut oil directly or its derivatives such as monolaurin in treating COVID-19 with a special emphasis on their biochemical characteristics features. The potential pitfalls therein and way forward are also highlighted.
Keyfindings and conclusions: There are enough research-backed evidences to demonstrate the antiviral capabilities of coconut oil and monolaurin. Possibility of developing a medium chain fatty acid-based nasal spray as a prophylactic or therapeutic is also discussed. Nevertheless, the potential impediments in devising suitable therapeutic models to treat SARS-CoV-2 are presented.
... The pro-inflammatory effect of PPARs is demonstrated in the SFA study, 11 which shows that SFA is pro-inflammatory and amplify the monocyte or macrophage that can contribute to the pathophysiology of several inflammatory diseases like atherosclerosis and diabetes. 11,23,24 SFAs, including virgin coconut oil, are usually consumed by Indonesian as cooking oil. It is usually used repeatedly in the deep frying method. ...
Humans require macronutrients and micronutrients to fulfill daily energy requirements, and triglyceride is a notable example, belonging to the fat family. This is particularly consumed frequently, and is composed of glycerol, and the fatty acid, specifically differentiated into unsaturated, saturated, trans, and cis forms. Furthermore, these constituents are known to play many roles in the body, including in the hematopoietic process. This involves oxidation and consequently stem cell differentiation into many blood cells in long-term, although the effect short-term is currently unknown. The study aimed, therefore, to investigate the effect of short-term intake of different fatty acid types on hematological profile in an animal model, conducted at the Animal Laboratory, Universitas Padjadjaran in October 2018. In addition, each group comprised 6 mice, orally administered distilled water as control (Group A), fish oil (Group B), virgin coconut oil (Group C), and used-cooking oil (Group D), at a dose of 5 μl/g body weight/day for 2 weeks. Subsequently, analysis was performed using blood measurement with hematology analyzer. The results showed lower white blood cell (WBC) count in Group B compared to D (p<0.05), alongside lymphocyte count (p<0.01). Moreover, the WBC in Group C was lower than D (p<0.01), also observed in lymphocyte count (p<0.001), % lymphocyte (p<0.01), while the % granulocyte count was higher than group D (p<0.01). Therefore, the highest total leukocyte and lymphocyte number among the other groups, as well as higher percentage of differential lymphocyte count was observed with mice provided with used-cooking oil compared to coconut oil, alongside a lower percentage of differential granulocyte count (p<0.05). However, fatty acid intake in group A, B, C, and D had no significant impact on RBC and platelet parameters. In conclusion, used-cooking oil induces a change in hematological profiles compared to fish oil and virgin coconut oil, featuring the increased total white blood cells and lymphocyte, as well as reduced % granulocyte.Keywords: Fatty acid, hematological profile, leucocyte Efek Pemberian Minyak Ikan, Minyak Kelapa Murni, dan Minyak Jelantah Terhadap Profil Hematologi MencitAbstrakManusia membutuhkan makronutrien dan mikronutrien untuk memenuhi kebutuhan energi harian. Salah satu sumber makronutrien adalah trigliserida yang merupakan salah satu jenis lemak yang paling sering dikonsumsi. Senyawa ini tersusun atas asam lemak dan gliserol. Terdapat banyak jenis asam lemak seperti asam lemak jenuh, asam lemak tidak jenuh, asam lemak trans, dan asam lemak cis. Rantai asam lemak memiliki banyak peran dalam tubuh, salah satunya adalah hematopoiesis sel stem. Pada konsumsi lemak jangka panjang, hematopoiesis ini terjadi melalui oksidasi asam lemak yang selanjutnya akan menstimulasi diferensiasi sel stem menjadi sel-sel darah di perifer, tetapi efeknya dalam jangka pendek belum diketahui. Oleh karena itu, penelitian ini bertujuan untuk menginvestigasi efek jangka pendek dari konsumsi berbagai jenis asam lemak terhadap profil hematologi mencit yang dilakukan di Laboratorium Hewan, Universitas Padjadjaran pada Oktober 2018. Mencit diberikan air suling sebagai kontrol (Grup A), minyak ikan (Grup B), minyak kelapa murni (Grup C), dan minyak jelantah (Grup D) dengan dosis 5μl/g berat badan/hari secara oral selama dua minggu. Profil hematologi diukur menggunakan hematology analyzer. Hasilnya, grup B memiliki jumlah leukosit lebih rendah dibandingkan grup D (p<0,05) dan limfosit yang lebih rendah dibandingkan grup D (p<0,01). Grup C memiliki jumlah leukosit lebih rendah dibandingkan grup D (p<0,01), jumlah limfosit yang lebih rendah dibandingkan grup D (p<0,001), % limfosit lebih rendah dibanding grup D (p<0,01), dan % granulosit lebih tinggi dibanding grup D (p<0,01). Selain itu, konsumsi asam lemak pada grup A, B, C, dan D tidak memengaruhi indeks RBC dan platelet secara signifikan. Sebagai simpulan, minyak jelantah memberikan efek terhadap perubahan profil hematologi mencit dibandingkan minyak ikan dan minyak kelapa murni, yaitu meningkatkan leukosit dan limfosit dan menurunkan % granulosit.Kata kunci: Asam lemak, leukosit, profil hematologi
... Most conspicuously, lauric acid and its monoglyceride derivative, monolaurin, have been demonstrated to possess anti-microbial properties against gram positive bacteria (Projan et al 1994, Peterson et al., 2004), and many viruses such as Junin virus (JUNV), vesicular stomatitis virus, Simian immunodeficiency virus (SIV) etc. infecting humans (Thormar et al., 1987;Hornung et al., 1994;Bartolotta, et al., 2001;Duke 2009;Li et al., 2009). Administration of coconut oil has been found to be an effective remedy for the treatment of many of the enveloped viruses such as such as Cytomegalovirus, Epstein-Barr virus, hepatitis C virus, influenza virus, leukemia virus (Enig 2010;Dayrit 2000;Fife 2013). The antiviral property of monolaurin has been attributed to its common role in disrupting the phospholipid layers in the membranes of the enveloped viruses causing their ultimate disintegration. ...
... Products from coconut processing industries are well recognized giving beneficial impact for human life, such as for food, cosmetics, and pharmaceuticals [1], [2]. For example, virgin coconut oil, the main product in the coconut processing industry, has proven beneficial function in antidiabetic treatment [3]. ...
... The first component, LA, is a saturated fatty acid with a 12-carbon atom chain. It comprises about half of the fatty acid content in coconut milk, coconut oil, laurel oil, and palm kernel oil and therefore is non-toxic and safe to handle [33]. More importantly, the melting point of LA is 43.8°C, which is a more suitable phase-change temperature for a PCM to avoid accidental triggering and also thermal injury. ...
Near-infrared (NIR) light as noninvasive external stimuli to trigger on-demand drug release has attracted great attention in recent years. However, the current existing NIR-related drug delivery systems (DDSs) still have difficulty in controlling the release of the individual drug separately. In the present work, a dot array-like DDS was developed for accurately controlling the release of multiple drugs. Each dot had a drug core and an outer protective layer. The outer protective layer consisted of lauric acid (LA) and polylactic acid (PLA). LA is a kind of phase-change material (PCM) with melting point of 43.8 °C. When loaded with polypyrrole nanoparticles (PPy NPs) that acted as photothermal transducers, the outer protective layer became NIR light responsive and was able to convert light into heat to melt the LA. As a result, the drugs stored inside were released. By changing the PPy loading, NIR light power density, and mass ratio of LA to PLA, the drug release profile could be carefully controlled. Such a NIR-responsive DDS may find great potential applications in treating diseases that require long-term therapies using more than one drug.
Despite the advances in low-field nuclear magnetic resonance (NMR), there are limited spectroscopic applications for untargeted analysis and metabolomics. To evaluate its potential, we combined high-field and low-field NMR with chemometrics for the differentiation between virgin and refined coconut oil and for the detection of adulteration in blended samples. Although low-field NMR has less spectral resolution and sensitivity compared to high-field NMR, it was still able to achieve a differentiation between virgin and refined coconut oils, as well as between virgin coconut oil and blends, using principal component analysis (PCA), partial least squares discriminant analysis (PLS-DA), and random forest techniques. These techniques were not able to distinguish between blends with different levels of adulteration; however, partial least squares regression (PLSR) enabled the quantification of adulteration levels for both NMR approaches. Given the significant benefits of low-field NMR, including economic and user-friendly analysis and fitting in an industrial environment, this study establishes the proof of concept for its utilization in the challenging scenario of coconut oil authentication. Also, this method has the potential to be used for other similar applications that involve untargeted analysis.
Medium-chain fatty acids (MCFAs) and their monoesters were tested for their antibacterial activity against the Gram-negative pathogen Aeromonas hydrophila . The antimicrobial effect was evaluated at two temperatures (4 °C and 37 °C) using a standardized microdilution method in a 96-well microtitration plate. The minimum inhibitory concentrations of selected MCFAs were determined as the lowest concentration limiting the growth of A. hydrophila in wells compared to a positive control of ≥ 80%. The results indicated that the most effective compound against A. hydrophila was sucrose monocaprate after incubation at 37 °C (0.625 mg ml ⁻¹ ), whereas monocaprylin was the most effective compound after incubation at 4 °C (1.25 mg ml ⁻¹ ). Free MCFAs showed no antibacterial effects towards this bacterium. Low solubility and sensory properties could limit the use of fatty acids in aquatic environment, which should be the subject of further studies.
Cardiovascular disease (CVD) is the leading cause of mortality in the Philippines and in the world. In an effort to explore the benefits of natural products for possibly reducing CVD-related morbidity and mortality, a pilot study on the cardioprotective influence of virgin coconut Cocos nucifera oil (VCO) against experimental myocardial infarction (MI) in an animal model was conducted. In this study, the effects of oral supplementation with VCO on cardiac histology of rats with isoproterenol (ISO)-induced MI were assessed. Forty (40) adult male Sprague- Dawley rats were randomized to five groups (n=8), namely: sham control (plain normal saline solution [PNSS] only); ISO control (PNSS and ISO); and three (3) experimental groups: VCO1, VCO5 and VCO10 (1, 5 and 10 mL/kg body weight, respectively). Oral pre-treatment with VCO was done once daily for 45 days via gastric gavage. ISO control and experimental groups were given two subcutaneous doses of ISO 85 mg/kg/dose on the 46th and 47th days (24 hours apart) to induce MI. Immediately following the second dose of ISO, the hearts were excised under inhalational ether anesthesia. Histologic examination of the left ventricular wall was performed under light microscopy. The extent of myocardial damage, edema and inflammation was graded using a standard numerical scheme. There was no mortality in any of the subjects during and post-induction of MI. Results showed normal cardiac tissue in the sham control and extensive myocardial injury (grade 3) in ISO control (p<0.001), confirming the histologic diagnosis of MI. When compared with the ISO control, the VCO groups showed less severe MI: VCO1 with moderate (grade 2) injury (p=0.035); VCO5 and VCO10 with minimal (grade 1) injury (p<0.001), suggesting dose-dependent attenuation of the myocardial damage. No statistical difference between VCO5 and VCO10, however, was observed (p=0.635). Oral supplementation of adult male Sprague-Dawley rats with VCO given at 1, 5 and 10 mL/kg body weight for 45 days significantly protected against myocardial damage induced by subsequent subcutaneous administration of isoproterenol. This cardioprotective effect may be attributable to antioxidant and anti-inflammatory components of VCO specifically short- and medium-chain fatty acids contained therein.
Coconut and its by-products have been used for centuries as culinary, cosmetic, and medicinal agents. More recently, virgin coconut oil (VCO) is gaining recognition as a functional food due to its perceived health benefits. Virgin coconut oil has a high proportion of medium-chain triglycerides, which unlike the long-chain triglycerides, are oxidized to energy in the liver. In addition to its excellent antioxidant profile, coconut oil is said to have antimicrobial and hypolipidemic properties too. This review focuses on the historical and functional aspects of coconut oil, with special emphasis on its health properties.
Alzheimer's disease (AD) is characterized by early and region-specific declines in cerebral glucose metabolism. Ketone bodies are produced by the body during glucose deprivation and are metabolized by the brain. An oral ketogenic compound, AC-1202, was tested in subjects with probable AD to examine if ketosis could improve cognitive performance.
Daily administration of AC-1202 was evaluated in 152 subjects diagnosed with mild to moderate AD in a US-based, 90-day, randomized, double-blind, placebo-controlled, parallel-group study. Subjects were on a normal diet and continued taking approved AD medications. Primary cognitive end points were mean change from Baseline in the AD Assessment Scale-Cognitive subscale (ADAS-Cog), and global scores in the AD Cooperative Study - Clinical Global Impression of Change (ADCS-CGIC). AC-1202 was compared to Placebo in several population groups, including: intention-to-treat (ITT), per protocol, and dosage compliant groups. Results were also stratified by APOE4 carriage status (a predefined analysis based on the epsilon 4 (E4) variant of the apolipoprotein E gene). This trial was registered with ClinicalTrials.gov, registry number NCT00142805, information available at http://clinicaltrials.gov/ct2/show/NCT00142805
AC-1202 significantly elevated a serum ketone body (beta-hydroxybutyrate) 2 hours after administration when compared to Placebo. In each of the population groups, a significant difference was found between AC-1202 and Placebo in mean change from Baseline in ADAS-Cog score on Day 45: 1.9 point difference, p = 0.0235 in ITT; 2.53 point difference, p = 0.0324 in per protocol; 2.6 point difference, p = 0.0215 in dosage compliant. Among participants who did not carry the APOE4 allele (E4(-)), a significant difference was found between AC-1202 and Placebo in mean change from Baseline in ADAS-Cog score on Day 45 and Day 90. In the ITT population, E4(-) participants (N = 55) administered AC-1202 had a significant 4.77 point difference in mean change from Baseline in ADAS-Cog scores at Day 45 (p = 0.0005) and a 3.36 point difference at Day 90 (p = 0.0148) compared to Placebo. In the per protocol population, E4(-) participants receiving AC-1202 (N = 37) differed from placebo by 5.73 points at Day 45 (p = 0.0027) and by 4.39 points at Day 90 (p = 0.0143). In the dosage compliant population, E4(-) participants receiving AC-1202 differed from placebo by 6.26 points at Day 45 (p = 0.0011, N = 38) and 5.33 points at Day 90 (p = 0.0063, N = 35). Furthermore, a significant pharmacologic response was observed between serum beta-hydroxybutyrate levels and change in ADAS-Cog scores in E4(-) subjects at Day 90 (p = 0.008). Adverse events occurred more frequently in AC-1202 subjects, were primarily restricted to the gastrointestinal system, and were mainly mild to moderate in severity and transient in nature.
AC-1202 rapidly elevated serum ketone bodies in AD patients and resulted in significant differences in ADAS-Cog scores compared to the Placebo. Effects were most notable in APOE4(-) subjects who were dosage compliant.
The strong bactericidal properties of lauric acid (C12:0), a middle chain-free fatty acid commonly found in natural products, have been shown in a number of studies. However, it has not been demonstrated whether lauric acid can be used for acne treatment as a natural antibiotic against Propionibacterium acnes (P. acnes), which promotes follicular inflammation (inflammatory acne). This study evaluated the antimicrobial property of lauric acid against P. acnes both in vitro and in vivo. Incubation of the skin bacteria P. acnes, Staphylococcus aureus (S. aureus), and Staphylococcus epidermidis (S. epidermidis) with lauric acid yielded minimal inhibitory concentration (MIC) values against the bacterial growth over 15 times lower than those of benzoyl peroxide (BPO). The lower MIC values of lauric acid indicate stronger antimicrobial properties than that of BPO. The detected values of half maximal effective concentration (EC(50)) of lauric acid on P. acnes, S. aureus, and S. epidermidis growth indicate that P. acnes is the most sensitive to lauric acid among these bacteria. In addition, lauric acid did not induce cytotoxicity to human sebocytes. Notably, both intradermal injection and epicutaneous application of lauric acid effectively decreased the number of P. acnes colonized with mouse ears, thereby relieving P. acnes-induced ear swelling and granulomatous inflammation. The obtained data highlight the potential of using lauric acid as an alternative treatment for antibiotic therapy of acne vulgaris.
The study was designed to determine whether overfeeding rats with a diet containing medium-chain triglyceride (MCT) as the major fat source (45% of calories) would impede the expected gain in weight and body fat as compared to rats overfed with isocaloric amounts of diet containing long-chain triglyceride (LCT). For 6 wk rats were fed either MCT diet or LCT diet twice daily via a gastrostomy tube. MCT-fed rats gained 20% less weight (P less than 0.001) and possessed fat depots weighing 23% less (p less than 0.001) than LCT)-fed rats. Mean adipocyte size was smaller (p less than 0.005) in MCT- than in LCT-fed rats. Weights of carcass protein and water were similar for both groups as were concentrations of serum insulin and levels of physical activity. The decreased deposition of fat in the MCT-fed rats may have resulted from obligatory oxidation of MCT-derived fatty acids in the liver after being transported there via the portal vein, leaving almost no MCT derivatives for incorporation into body fat. MCT may have potential for dietary prevention of human obesity.
The mechanism whereby overfeeding with diet containing medium chain triglyceride (MCT) results in diminished body weight and fat was studied. Fifteen male Sprague-Dawley rats were fitted under anesthesia with gastrostomy tubes and divided into two groups. One group was fed MCT diet, the other an isocaloric diet containing long chain triglyceride (LCT) in excess (150%) of spontaneous calorie intake. Both diets, fed for 6 wk, derived 50% of calories from fat. Basal and norepinephrine (25 micrograms/100 g) stimulated 02 consumption and CO2 production, as well as metabolic rate were measured. After the rats were killed, total dissectible fat and fat cell size and number were determined. MCT rats gained 15% less weight than LCT controls (p less than 0.001). Total dissectible fat was significantly lower (p less than 0.001) in MCT group, as was mean adipocyte size (p less than 0.001). Resting and maximal norepinephrine-stimulated 02 consumptions were 39.7 and 22.1% higher in MCT than in LCT group, respectively. Resting and norepinephrine-stimulated metabolic rates were 38.8 and 22.2% higher in MCT than LCT fed rats, respectively. Overfeeding MCT diet results in decreased body fat related to increased metabolic rate and thermogenesis.
Two populations of Polynesians living on atolls near the equator provide an opportunity to investigate the relative effects of saturated fat and dietary cholesterol in determining serum cholesterol levels. The habitual diets of the toll dwellers from both Pukapuka and Tokelau are high in saturated fat but low in dietary cholesterol and sucrose. Coconut is the chief source of energy for both groups. Tokelauans obtain a much higher percentage of energy from coconut than the Pukapukans, 63% compared with 34%, so their intake of saturated fat is higher. The serum cholesterol levels are 35 to 40 mg higher in Tokelauans than in Pukapukans. These major differences in serum cholesterol levels are considered to be due to the higher saturated fat intake of the Tokelauans. Analysis of a variety of food samples, and human fat biopsies show a high lauric (12:0) and myristic (14:0) content. Vascular disease is uncommon in both populations and there is no evidence of the high saturated fat intake having a harmful effect in these populations.
Glycerol monolaurate (GML) is a naturally occurring surfactant that is used widely as an emulsifier in the food and cosmetics industries and is generally regarded as lacking in important biological activities. The recent observation that it inhibits the production of staphylococcal toxic shock toxin-1 (P. M. Schlievert, J. R. Deringer, M. H. Kim, S. J. Projan, and R. P. Novick, Antimicrob. Agents Chemother. 36:626-631, 1992) is therefore rather surprising and raises the interesting question of how such a compound might interact with cells. In this report, we show that GML inhibits the synthesis of most staphylococcal toxins and other exoproteins and that it does so at the level of transcription. We find that GML blocks the induction but not the constitutive synthesis of beta-lactamase, suggesting that it acts by interfering with signal transduction.
Glucose is the brain's principal energy substrate. In Alzheimer's disease (AD), there appears to be a pathological decrease in the brain's ability to use glucose. Neurobiological evidence suggests that ketone bodies are an effective alternative energy substrate for the brain. Elevation of plasma ketone body levels through an oral dose of medium chain triglycerides (MCTs) may improve cognitive functioning in older adults with memory disorders. On separate days, 20 subjects with AD or mild cognitive impairment consumed a drink containing emulsified MCTs or placebo. Significant increases in levels of the ketone body beta-hydroxybutyrate (beta-OHB) were observed 90 min after treatment (P=0.007) when cognitive tests were administered. beta-OHB elevations were moderated by apolipoprotein E (APOE) genotype (P=0.036). For 4+ subjects, beta-OHB levels continued to rise between the 90 and 120 min blood draws in the treatment condition, while the beta-OHB levels of 4- subjects held constant (P<0.009). On cognitive testing, MCT treatment facilitated performance on the Alzheimer's Disease Assessment Scale-Cognitive Subscale (ADAS-cog) for 4- subjects, but not for 4+ subjects (P=0.04). Higher ketone values were associated with greater improvement in paragraph recall with MCT treatment relative to placebo across all subjects (P=0.02). Additional research is warranted to determine the therapeutic benefits of MCTs for patients with AD and how APOE-4 status may mediate beta-OHB efficacy.
The antibacterial activity of the medium chain fatty acids and their 1-monoglycerides was evaluated towards several Gram-positive strains belonging to the genera Staphylococcus, Corynebacterium, Bacillus, Listeria and Streptococcus. The 1-monoglycerides were more active than the fatty acids with monolaurin being the most active compound. Interesting effects were observed when the streptococcal strain Streptococcus pyogenes was used as a test microorganism. First, blocking of the hydroxyl groups of the glycerol moiety of monolaurin led to a compound with remarkable antibacterial activity (MIC, 3.9 microg/ml). Secondly, synergistic relationships were observed between monolaurin and monocaprin as well as between monolaurin and the poorly active lauric acid when their two component mixtures were examined. The mixtures in which one of the components was 2-fold more predominant than the other one were much more active than the pure components taken individually. Moreover, the presence of the components in ratio 1:1 was disadvantageous. Synergistic relationships were also found between monolaurin and monomyristin towards Staphylococcus aureus 209 when monomyristin was in the same quantity as monolaurin or in shortage.
The effect of medium-chain triglycerides (MCT) on the absorption of calcium and magnesium in premature infants was studied in 34 infants with birth weights lower than 2,000 gm. The infants were divided into three groups and fed three formulas similar in nutrient content except for the type of fat, as follows: group 1 (control): corn oil, oleo, and coconut oil (39:41:20); group 2: MCT, corn oil, and coconut oil (40:40:20); group 3: MCT and corn oil (80:20). The infants fed MCT-containing formulas absorbed significantly more calcium than the control group. Magnesium absorption was significantly increased in the 80% MCT group.
To test whether excess dietary energy as medium-chain triglycerides (MCT) affects thermogenesis differently from excess dietary energy as long chain triglycerides (LCT), ten male volunteers (ages 22 to 44) were overfed (150% of estimated energy requirement) liquid formula diets containing 40% of fat as either MCT or LCT. Each patient was studied for one week on each diet in a double-blind, crossover design. Resting metabolic rate (RMR) did not change during either week of overfeeding. The thermic response to food (TEF) was greater on day 1 following a meal (1,000 kcal) containing MCT than following an isocaloric meal containing LCT (8 +/- .8% v 5.8 +/- .8% of ingested energy; P less than .05). Moreover, the TEF observed after a 1,000 kcal meal containing MCT increased significantly to 12% (+/- 1.3%) overfeeding. The TEF of the 1,000 kcal meal containing LCT was unchanged by five days of LCT overfeeding (6.6 +/- 1.0% of ingested energy). Energy expenditure during a 20-hour continuous enteral infusion of the diet on day 7 was also significantly higher with the MCT diet than with the LCT diet (15.7 +/- 1.7% v 7.3 +/- .9% of ingested energy; P less than .05). Our results demonstrate that excess dietary energy as MCT stimulates thermogenesis to a greater degree than does excess energy as LCT. This increased energy expenditure, most likely due to lipogenesis in the liver, provides evidence that excess energy derived from MCT is stored with a lesser efficiency than is excess energy derived from dietary LCT.
How long-term dietary intake of essential fatty acids affects the fatty-acid content of aortic plaques is not clear. We compared the fatty-acid composition of aortic plaques with that of post-mortem serum and adipose tissue, in which essential fatty-acid content reflects dietary intake. Positive associations were found between serum and plaque omega 6 (r = 0.75) and omega 3 (r = 0.93) polyunsaturated fatty acids, and monounsaturates (r = 0.70), and also between adipose tissue and plaque omega 6 polyunsaturated fatty acids (r = 0.89). No associations were found with saturated fatty acids. These findings imply a direct influence of dietary polyunsaturated fatty acids on aortic plaque formation and suggest that current trends favouring increased intake of polyunsaturated fatty acids should be reconsidered.
In the presence of lauric acid (C12), the production of infectious vesicular stomatitis virus (VSV) was inhibited in a dose-dependent manner. The inhibitory effect was reversible; after removal of C12 the antiviral effect disappeared. In addition, the chain length of the monocarboxylic acids proved to be crucial, as those with shorter or longer chains were less effective or had no antiviral activity. Concomitant with the C12-induced inhibition was the stimulation of triacylglycerol synthesis, increasing the amount up to ninefold. Analysis of the antiviral mechanism of C12 revealed that the correct assembly of the viral components was disturbed, but viral RNA and protein synthesis remained unimpaired. By cell fractionation and Western blot analysis the amount of viral M protein located in the plasma membrane was found to be markedly reduced after treatment with C12, whereas in the cytoplasm the quantity of M protein was similar to that in untreated cells. C12 did not influence M protein synthesis, but prevented the binding of M protein to the host cell membrane, where the protein plays an essential role in virus assembly. Thus, treatment of VSV-infected cells with C12 resulted in inhibition of virus release. It is suggested that the newly synthesized triacylglycerols might interact with the host cell plasma membrane and interfere with virus maturation.
Giardia duodenalis is a protozoal, intestinal parasite that is a common aetiological agent of infectious diarrhoea in humans worldwide. Chemotherapeutic intervention presently offers a limited range of drugs and these are usually only employed after clinical diagnosis. Moreover, these drugs are ineffective against the infectious cysts, can produce unpleasant side effects, and are expensive with limited availability in developing countries. Frequent reports of drug toxicity, treatment failure and parasite drug resistance have, in some instances, also resulted in the increasing reluctance to over-prescribe synthetic anti-microbials. Alternatively, there is now mounting evidence to suggest that some of the naturally derived, medium-chain, saturated fatty acids (MCSFAs) possess anti-microbial and anti-parasitic properties. We have therefore examined the effects of four different fatty acids on G. duodenalis trophozoites in vitro. Cytotoxicity was determined using fluorescence, scanning and transmission electron microscopic techniques and standard cytotoxicity assays. Our studies have confirmed that the MCSFA, dodecanoic acid (C: 12) (common name: lauric acid), is anti-giardial, with an LD50 concentration comparable to that of metronidazole, the drug of choice in the treatment of giardiasis. Dodecanoic acid appeared to induce trophozoite death by accumulating within the parasite cytoplasm resulting in rupture of the cell membrane. This study has opened fresh avenues for development of natural drug therapy in which food supplementation may augment, or even replace, some of the standard chemotherapeutic agents presently employed in the treatment of giardiasis and possibly other infectious intestinal diseases.