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PubMed2000

Garlic elicits a nitric oxide-dependent relaxation and inhibits hypoxic pulmonary vasoconstriction in rats.

1. The aims of the present study were to determine the characteristics of garlic extract-induced relaxation in rat isolated pulmonary arteries, its susceptibility to changes in oxygen tension and its protective effect against hypoxic pulmonary vasoconstriction. 2. In normoxia, garlic extract (3-500 microg/mL) produced a dose- and nitric oxide (NO)-dependent relaxation. Following 60 min hypoxia, maximum garlic relaxation was reduced compared with control (mean (-SEM) -86 +/- 3 vs-69 +/- 2% of phenylephrine (PE) precontraction, respectively), but recovered after 60 min reoxygenation (-85 +/- 3% PE precontraction). 3. Acetylcholine (0.1 micromol/L)-induced NO-dependent relaxation was reduced from a control value of -76 +/- 1% to -46 +/- 4% during hypoxia and was further reduced to -35 +/- 2 % after reoxygenation. 4. In endothelium-intact arteries, hypoxic exposure resulted in a triphasic response: early transient contraction (+24 +/- 4%), followed by transient relaxation (-37 +/- 7%) and then sustained contraction (+62 +/- 5%). 5. Pretreatment with NG-nitro-L-arginine methyl ester abolished the early transient contraction, moderately attenuated the sustained contraction and had no effect on the transient relaxation. Mechanical endothelial disruption inhibited all hypoxia-induced vascular changes. 6. Garlic pretreatment had no effect on the early transient contraction (+25 +/- 4%), but inhibited the transient relaxation (-5 +/- 3%; P<0.05) and the sustained contraction (+26 +/- 5%; 7. Garlic also significantly inhibited endothelin-l-induced contractions in a dose-dependent manner. 8. These findings show that garlic extract modulates the production and function of both endothelium-derived relaxing and constricting factors and this may contribute to its protective effect against hypoxic pulmonary vasoconstriction.

Acetylcholine↗
PubMed2001

Allicin release under simulated gastrointestinal conditions from garlic powder tablets employed in clinical trials on serum cholesterol.

The failure of five recent clinical trials to show significant reduction in elevated serum cholesterol by a single brand of allicin-standardized garlic powder tablets is in contrast to many prior positive studies with the same brand. The hypocholesterolemic activity of garlic is mainly due to allicin, a compound that is produced by the acid-sensitive garlic enzyme, alliinase, only after tablet consumption. Therefore, the allicin-releasing ability of ten lots of these tablets--manufactured over the same years that the positive and negative clinical trials were conducted (1989-1997)--was determined under simulated gastrointestinal dissolution conditions, as defined by U.S. Pharmacopeia Method 724A. It was found that the older lots were more resistant to acid-disintegration (2.5 h vs. 1.3 h, P < 0.001) and that they released three times as much allicin (44% vs. 15 % of their potential, P < 0.001) as the newer lots. A second brand of tablets employed in a recent negative trial released no detectable amount of allicin, while a third set of tablets with high allicin release was used in a trial that gave positive effects. Hence, the persons involved in the recent negative clinical trials probably received considerably less allicin than did those in the older positive studies, possibly accounting for much of the discrepancy in the outcomes. In conclusion, clinical trials using garlic powder tablets to assess any effect of garlic that might be related to allicin, as most are, cannot be considered valid for garlic when the trial shows no effect, unless the expected allicin release from the tablets has at least been determined under standardized drug release conditions (USP 724A).

Cholesterol↗
PubMed1994

Antioxidant and radical scavenging effects of aged garlic extract and its constituents.

The antioxidant properties of three garlic preparations and organosulfur compounds in garlic have been determined. Aged garlic extract inhibited the emission of low level chemiluminescence and the early formation of thiobarbituric acid-reactive substances (TBA-RS) in liver microsomal fraction initiated by t-butyl hydroperoxide. However, the water extracts of raw and heat-treated garlic enhanced the emission of low level chemiluminescence. Among the variety of organosulfur compounds, S-allylcysteine (SAC) and S-allylmercaptocysteine (SAMC), the major organosulfur compounds found in aged garlic extract, showed radical scavenging activity in both chemiluminescence and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays, indicating that these compounds may play an important role in the antioxidative activity of aged garlic extract.

Animals↗
PubMed2004

The effect of garlic on arteriosclerotic nanoplaque formation and size.

OBJECTIVE: In an in vitro biosensor model (PCT/EP 97/05212), the interplay between different lipoproteins in arteriosclerotic nanoplaque formation, as well as aqueous garlic extract (0.2-5.0 g/l from LI 111 powder) as a possible candidate drug against arterio/atherosclerosis were tested within the frame of a high throughput screening. METHODS: The processes described below were studied by ellipsometric techniques quantifying the adsorbed amount (nanoplaque formation) and layer thickness (nanoplaque size). A thorough description of the experimental setup has been given previously. RESULTS: Proteoheparan sulfate (HS-PG) adsorption to hydrophobic silica was monoexponential and after approximately 30 min constant. The addition of 2.52 mmol/l Ca2+ led to a further increase in HS-PG adsorption because Ca2+ was bound to the polyanionic glycosaminoglycan (GAG) chains thus screening their negative fixed charges and turning the whole molecule more hydrophobic. Incubation with 0.2 g/l aqueous garlic extract (GE) for 30 min did not change the adsorption of HS-PG. However, the following addition of Ca2+ ions reduced the increase in adsorption by 50.8% within 40 min. The adsorption of a second Ca2+ step to 10.08 mmol/l was reduced by even 82.1% within the next 40 min. Having detected this inhibition of receptor calcification, it could be expected that the build-up of the ternary nanoplaque complex is also affected by garlic. The LDL plasma fraction (100 mg/dl) from a healthy probationer showed beginning arteriosclerotic nanoplaque formation already at a normal blood Ca2+ concentration, with a strong increase at higher Ca2+ concentrations. GE, preferably in a concentration of 1 g/l, applied acutely in the experiment, markedly slowed down this process of ternary aggregational nanoplaque complexation at all Ca2+ concentrations used. In a normal blood Ca2+ concentration of 2.52 mmol/l, the garlic induced reduction of nanoplaque formation and molecular size amounted to 14.8% and 3.9%, respectively, as compared to the controls. Furthermore, after ternary complex build-up, GE similar to HDL, was able to reduce nanoplaque formation and size. The incubation time for HDL and garlic was only 30 min each in these experiments. Nevertheless, after this short time the deposition of the ternary complex decreased by 6.2% resp. 16.5%, i.e. the complex aggregates were basically resolvable. CONCLUSIONS: These experiments clearly proved that garlic extract strongly inhibits Ca2+ binding to HS-PG. In consequence, the formation of the ternary HS-PG/LDL/Ca2+ complex, initially responsible for the 'nanoplaque' composition and ultimately for the arteriosclerotic plaque generation, is decisively blunted.

Arteriosclerosis↗
PubMed1997

Modulation of phase I and phase II xenobiotic-metabolizing enzymes by selenium-enriched garlic in rats.

Previous research showed that treatment with selenium-enriched garlic (Se-garlic) was able to inhibit the initiation phase of mammary carcinogenesis in the dimethyl-benz[a]anthracene (DMBA) model in rats. The present study was designed to investigate the following parameters: 1) DMBA-DNA adduct formation in liver and mammary gland, 2) urinary excretion of DMBA metabolites, 3) phase I and phase II xenobiotic-metabolizing enzymes, and 4) tissue selenium levels as a function of Se-garlic supplementation. Prior feeding with an Se-garlic-containing diet (at 3 ppm Se) for two weeks resulted in a consistent reduction of all DMBA adducts in liver and mammary gland. This was accompanied by a 40% increase in urinary excretion of DMBA metabolites over a two-day period. Several liver P-450 enzymes were examined in rats fed a diet supplemented with 1, 2, or 3 ppm Se. Compared with controls receiving 0.1 ppm Se, no significant alteration in activity was detected with respect to P-450 1A1 (responsible for DMBA activation), 1A2, 2B1, 2E1, and 3A4. In contrast, glutathione S-transferase and uridine 5'-diphosphate-glucuronyltransferase activities were elevated to a maximum of 2- to 2.5-fold in liver and kidney. As expected, there was a dose-dependent elevation of selenium concentrations in liver, kidney, mammary gland, and plasma as a function of the level of Se-garlic supplementation. Our data seem to suggest that an increased detoxification of carcinogen via the phase II conjugating enzymes might represent a mechanism of tumor suppression by Se-garlic.

9,10-Dimethyl-1,2-benzanthracene↗
PubMed2005

Nutraceutical applications of garlic and the intervention of biotechnology.

Garlic (Allium sativum L.) is an important and widely cultivated plant with both culinary and medicinal uses stemming from its biological activities, which include antibiotic, anticancer, anti-thrombotic, and lipid-lowering cardiovascular effects. Though such medicinal use of garlic existed for centuries, there was little scientific support for its therapeutic and pharmacological properties. However, there has been a recent upsurge of research on garlic aiming to understand its exact mechanism of action in each case so that garlic and its products may have more judicious future applications. Since garlic is vegetatively propagated, its improvement for desired traits through conventional means is difficult. The intervention of biotechnological methods such as tissue culture and gene transfer protocols developed recently hold great promise for improving this crop. Due to new innovations in instrumentation and processing technologies coupled with more judicious experimental models, better products are foreseen in the market. The objective of this article was to review the recent developments made towards understanding the mechanism by which garlic imparts different therapeutic effects as well as to review what biotechnology can offer to improve this crop and its products.

Agriculture↗
PubMed2004

Anticarcinogenic properties of garlic: a review.

Garlic is a popular spice added to several edible preparations and is a remedy for a variety of ailments. Epidemeological as well as laboratory studies have shown that garlic consumption reduces certain cancer incidences in the stomach, colon, mammary, cervical, etc. This article focuses on the general chemistry, metabolism, anticarcinogenic properties, mechanism of action behind the anticarcinogenic effects, functional foods based on garlic; and future areas of research. Garlic has been shown to metabolized into N-aceryl-S-allyl cysteine, allyl mercaptan, diallyl disulfide, diallyl sulfide, diallyl sulfoxide, diallyl sulfone, and allyl methyl sulfide. Garlic has been thought to bring about its anticarcinogenic effect through a number of mechanisms, such as the scavenging of radicals, increasing gluathione levels, increasing the activities of enzymes such as glutathione S-transferase, catalase, inhibition of cytochrome p4502E1, DNA repair mechanisms, prevention of chromosomal damage etc. Future research should standardize the dosage of garlic and type, ie., whether it should be taken fresh, cooked, or aged. The formulation of odorless functional foods with the retention of anticarcinogenic activity should be further studied.

Animals↗
PubMed2005

A comparison of the antimicrobial activity of garlic, ginger, carrot, and turmeric pastes against Escherichia coli O157:H7 in laboratory buffer and ground beef.

The antimicrobial effects of garlic, ginger, carrot and turmeric pastes against Escherichia coli O157:H7 in laboratory buffer and model food system were investigated. Turmeric paste, fresh carrot, ginger and garlic pastes from roots, and commercial ginger and garlic paste were heated alone or with buffered peptone water (BPW) or ground beef at 70 degrees C for 7 min. All samples were inoculated with a three strain cocktail of overnight cultures of E. coli O157: H7 and stored at 4 degrees C and 8 degrees C for 2 weeks. Each paste exhibited different antimicrobial effects alone and in ground beef or BPW at 4 degrees C and 8 degrees C for 2 weeks. Commercial ginger paste and fresh garlic paste showed the strongest antimicrobial activity with complete inactivation of E. coli O157:H7 in the paste at 3 days at 4 degrees C and 8 degrees C. Carrot and turmeric pastes did not show any antimicrobial activity both at 4 degrees C and 8 degrees C. Commercial garlic showed antimicrobial activity at both 4 degrees C and 8 degrees C (about 1 log CFU/g reduction) in the paste. However, fresh ginger paste showed antimicrobial activity only at 8 degrees C. Only commercial ginger paste had antimicrobial activity in BPW at 4 degrees C for 2 weeks. However, commercial ginger paste showed antimicrobial activity in ground beef at 3 days and after (about 1-2 log CFU/g) compared to control samples at 8 degrees C for 2 weeks. Fresh garlic paste showed antimicrobial activity only in BPW (1.3 log CFU/g) at 8 degrees C. These results indicate that the antimicrobial activity of these pastes is decreased in ground beef and laboratory buffer.

Animals↗
PubMed1981

Effect of garlic on blood lipids in patients with coronary heart disease.

The study was conducted on two groups of individuals. Group A consisted of 20 healthy volunteers who were fed garlic for 6 months and then followed for another 2 months without garlic. Garlic administration significantly lowered the serum cholesterol and triglycerides while raising the high-density lipoproteins. Group B consisted of 62 patients with coronary heart disease with elevated serum cholesterol. They were randomly divided into two subgroups: B1 was fed garlic for 10 months while B2 served as a control. Garlic decreased the serum cholesterol (p less than 0.05), triglycerides (p less than 0.05) and low density lipoprotein (p less than 0.05) while increasing the high-density fraction (p less than 0.001). The change reached statistically significant levels at the end of 8 months and persisted for the next 2 months of follow-up. Thus, the essential oil of garlic has shown a distinct hypolipidemic action in both healthy individuals and patients of coronary heart disease.

Cholesterol↗
PubMed2006

A randomized factorial study of the effects of long-term garlic and micronutrient supplementation and of 2-wk antibiotic treatment for Helicobacter pylori infection on serum cholesterol and lipoproteins.

BACKGROUND: Little is known about the long-term effects of garlic or micronutrient supplementation on total, HDL, and LDL cholesterol in disease-free persons. OBJECTIVE: We aimed to assess the effects of long-term supplementation with garlic and micronutrients and of short-term amoxicillin and omeprazole treatment on serum total, HDL, and LDL cholesterol in a rural Chinese population. DESIGN: We conducted a randomized, double-blind, placebo-controlled, 2 x 2 x 2 and 2 x 2 factorial study of precancerous gastric lesions in 3411 subjects in Linqu County, Shandong Province, China. Thirty-four subjects were randomly selected from each of 12 treatment strata. Sera were analyzed at 3.3 and 7.3 y to measure effects on total, HDL, and LDL cholesterol after 2-wk twice-daily treatment with 1 g amoxicillin and 20 mg omeprazole and supplementation throughout the study with 1) 2 capsules twice daily, each containing 200 mg aged garlic extract and 1 mg steam-distilled garlic oil, or 2) twice-daily micronutrient capsules containing 250 mg vitamin C, 100 IU vitamin E, and 37.5 mg selenium. RESULTS: Regressions adjusted for covariates indicated increases of 0.22 mmol total cholesterol/L (P = 0.01) and 0.19 mmol LDL/L (P = 0.02) after 7.3 y of micronutrient supplementation, but no effect of garlic supplementation or short-term amoxicillin and omeprazole treatment. CONCLUSIONS: In this rural Chinese population with low meat intake and moderate cholesterol concentrations, long-term garlic supplementation had no effect on lipid profiles, whereas micronutrient supplementation was associated with small but significant increases in total and LDL-cholesterol concentrations at 7.3 y.

Amoxicillin↗
PubMed1999

Antibacterial effect of garlic and omeprazole on Helicobacter pylori.

The antibacterial effect of a home-made raw garlic extract and commercial garlic tablets alone and in combination with antibiotics or omeprazole was determined against clinical isolates of Helicobacter pylori. MIC values of raw garlic extract and three types of commercial garlic tablets ranged from 10,000 to 17,500 mg/L. When MIC values of the commercial tablets were based on the allicin content, no differences between the three types were observed. The combination of garlic and omeprazole, studied with killing curves, showed a synergic effect which was concentration dependent. Further clinical evaluation of garlic in combination with the conventional agents for H. pylori treatment seems warranted.

Anti-Bacterial Agents↗
PubMed2003

Garlic extract and two diallyl sulphides inhibit methicillin-resistant Staphylococcus aureus infection in BALB/cA mice.

OBJECTIVES: The inhibitory effect of garlic extract, diallyl sulphide and diallyl disulphide against methicillin-resistant Staphylococcus aureus (MRSA) infection in BALB/cA mice was studied. The influence of these agents upon the levels of fibronectin, interleukin-6 and lipid oxidation in MRSA-infected mice was examined. METHODS: Garlic extract at 100% and 50%; diallyl sulphide (DAS) at 10% and 5%; diallyl disulphide (DADS) at 1% and 0.5% were used in this study. Sixteen clinical MRSA isolates obtained from infected patients were used in this study (n=16). Mice were infected by injecting 200 microL MRSA-PBS solution, which contained 10(7) cfu, via the tail vein. At 16 h post-infection (p.i.), garlic extract, DAS or DADS at 200 microL was administrated orally. At 24 h p.i., mice were killed and blood, liver, kidney and spleen of each mouse were collected. Plasma and the filtrate from each organ and serial dilutions were used to determine colony count. Plasma fibronectin level was determined by rabbit anti-rat fibronectin antibody and quantified by ELISA. Interleukin-6 levels were determined by commercial kit. Lipid oxidation was determined by measuring malondialdehyde levels. RESULTS: The oral administration of these agents significantly decreased the viability of MRSA, in plasma, liver, kidney and spleen (P<0.05). MRSA infection significantly increased fibronectin and interleukin-6 levels in plasma of MRSA-infected mice (P<0.05); however, the oral administration of garlic extract and two diallyl sulphides significantly reduced both fibronectin and interleukin-6 levels (P<0.05). MRSA infection also significantly enhanced lipid oxidation in plasma and three organs (P<0.05). The treatments of garlic extract and two diallyl sulphides significantly decreased the malondialdehyde level and showed antioxidant protection (P<0.05). CONCLUSIONS: These data strongly supported the conclusion that garlic extract, diallyl sulphide and diallyl disulphide possessed multiple protective functions against MRSA infection, in which diallyl sulphide and diallyl disulphide could be considered as novel therapeutic agents for the treatment of MRSA infection.

Allyl Compounds↗
PubMed2001

Saponins in garlic as modifiers of the risk of cardiovascular disease.

Most chemical and biological studies about garlic have been conducted using organosulfur compounds. However, a variety of steroid saponins from garlic and related Allium species are being increasingly recognized for their importance in biological processes. This report demonstrates the isolation and structure determination of steroid saponins from garlic and aged garlic extract (AGE). In addition, the in vitro antifungal antitumor cytotoxicity and blood coagulability effects of steroid saponins from garlic and related Allium species are provided. Animal studies on the cholesterol-lowering effects of the saponin fractions from garlic are also summarized.

Animals↗
PubMed2001

Effects of garlic preparations on the gastrointestinal mucosa.

The effects of garlic preparations, including dehydrated raw garlic powder (RGP), dehydrated boiled garlic powder (BGP) and aged garlic extract (AGE), on the gastric mucosa were determined using a newly established endoscopic air-powder delivery system, which can deliver solid materials directly into the stomach. Among the three preparations, RGP caused severe damage, including erosion. BGP also caused reddening of the mucosa, whereas AGE did not cause any undesirable effects. The safety of enteric-coated garlic products was also determined. Direct administration of pulverized enteric-coated products on the gastric mucosa caused reddening of the mucosa. When an enteric-coated tablet was administered orally, it caused loss of epithelial cells at the top of crypts in the ileum. These results suggest that caution be used with regard to safety and effectiveness when choosing a garlic preparation because some preparations may have undesirable effects, including gastrointestinal problems.

Animals↗
PubMed2006

Preclinical perspectives on garlic and cancer.

Evidence continues to point to the anticancer properties of fresh garlic extracts, aged garlic, garlic oil, and a number of specific organosulfur compounds generated by processing garlic. These anticarcinogenic and antitumorigenic characteristics appear to arise through both dose- and temporal-related changes in a number of cellular events involved with the cancer process, including those involving drug metabolism, immunocompetence, cell cycle regulation, apoptosis, and angiogenesis. The ability of garlic and related allyl sulfur compounds to block tumors in the colon, lung, breast, and liver suggests general mechanisms that are not tissue specific. Whereas relatively few studies have compared the relative efficacy of water- and lipid-soluble allyl sulfur compounds, those that have when using chemically induced carcinogen models suggest little difference in response, whereas tumor proliferation/apoptosis is highly dependent on the species provided. A shift in sulfhydryl groups, alterations in glutathione:oxidized glutathione ratios, and resultant changes in cellular redox status may be involved in some of the phenotypic changes caused by allyl sulfur compounds. Such changes in thiols by allyl sulfurs may also account for the observed hyperphosphorylation of specific cell cycle proteins and the histone hyperacetylation that has been correlated with suppressed tumor cell proliferation. Whereas the anticarcinogenic and antitumorigenic data to date are impressive, additional studies are needed with more modest exposure to allyl sulfur compounds over prolonged periods. Likewise, additional studies are needed that incorporate transgenic and knockout models to assist in the identification of molecular targets for garlic and its associated allyl sulfur components.

Allyl Compounds↗
PubMed2006

European perspective on garlic and its regulation.

Garlic products are marketed in the European Union (EU) as foodstuffs and as herbal medicinal products. All EU countries have garlic foodstuffs on their markets. In contrast, garlic medicinal products are available only in a limited number of EU member states. This difference is due to discrepancies among the national laws of EU member states. This article gives an overview of the status of garlic products in EU countries and their approved medical claims and discusses legislative options for the authorization of garlic products as medicinal products. Developments in the food area that could affect the status of and health claims on garlic foodstuffs are also presented.

Europe↗
PubMed2002

Effects of dietary garlic on cholesterol metabolism in laying hens.

Experiments were conducted to evaluate the potential for dietary garlic to influence egg yolk cholesterol concentrations and overall performance in different layer strains. Thirty-six, 28-wk-old, Hisex Brown,Isa Brown, Lohmann, Starcross, Babcock, and Starcross-579 strains (six hens per strain) were fed diets supplemented with 0 (control), 2, 4, 6, 8, or 10% sun-dried garlic paste for 6 wk. There were no differences (P > 0.05) among diets or strains in egg weight, egg mass, feed consumption, feed efficiency, and BW gain as averaged over 6 wk. Yolk weight, however, responded quadratically with increasing levels of dietary garlic and differed among strains (P < 0.05). Egg production and yolk weights were significantly higher in the Babcock strain in comparison with other strains. Serum and egg yolk cholesterol concentrations decreased linearly (P < 0.05) with increasing levels of dietary garlic. Serum and egg yolk cholesterol concentrations also differed among different strains (P < 0.05). It was concluded that garlic paste in the diets of laying hens reduced serum and yolk cholesterol concentrations. It was also concluded that dietary garlic paste had no adverse effects on layer performance.

Animal Nutritional Physiological Phenomena↗
PubMed1998

Treatment of hepatopulmonary syndrome with Allium sativum L. (garlic): a pilot trial.

No medical therapy exists for subjects with hepatopulmonary syndrome (HPS). A patient with HPS was reported to have improvement in arterial oxygenation while self-administering garlic. Our goal was to determine whether a standardized garlic powder improves arterial oxygenation and dyspnea in subjects with HPS. A prospective, open label uncontrolled pilot study in 15 subjects with HPS were administered garlic powder capsules daily for a minimum of 6 months. Arterial blood gases were determined every 4-8 weeks, in the same position on room air, and a subjective dyspnea transition index was reported. Six of 15 subjects (40%, confidence interval: 0.15-65) had at least a 10 mmHg increase in the P(O2) or decrease in the alveolar-arterial gradient. The mean pre- and postarterial difference in these patients were: P(O2) (14+/-4 mmHg) and alveolar-arterial gradient (18+/-5 mmHg). All 6 subjects who responded to garlic had less dyspnea on exertion. Garlic improved arterial oxygenation in younger subjects (mean 40 versus 56 years old; p = 0.021) or those with lower macroaggregated albumin shunt fractions (mean 21 versus 44%, p = 0.058). Garlic may improve arterial oxygenation and symptoms in patients with hepatopulmonary syndrome and warrants further investigation.

Adult↗