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@#A novel allicin pro-drug tablet containing antacid pellets was developed to realize pH-regulated allicin release and to guarantee allicin yield in stomach environment.Firstly, allicin precursor pellets containing antacid pellet were prepared and artificial gastric juice was used as the medium to determine the yield of the allicin.Then, the total lipid cholesterol (TC), triglyceride cholesterol (TG), high density lipoprotein (HDL-C) and low-density lipoprotein (LDL-C) were used as indicators to study the hypolipidemic effect of allicin precursor pellets in rats.The dissolution test showed that in artificial gastric juice, the yield of allicin-containing antacid pellets exceeded 90%.In pharmacodynamic studies, it was found that antacid pellets showed the expected hypolipidemic effect on hyperlipidemia rats compared without antacid pellets.There was a very significant difference in blood lipid levels between the two test groups (P < 0.05).The allicin pro-drug tablets containing antacid pellets can effectively lower blood lipids.
ABSTRACT
Aims: To facilitate allicin generation in-situ from pure diastereomers of alliin by enzymatic reaction of alliinase and assess its anti-cancerous/anti-bacterial activities. Study Design: Chemical synthesis and in-vitro assay of anti-cancerous/anti-bacterial activities. Place and Duration of Study: Protein Research Laboratory, Research Resources Center, University of Illinois at Chicago, between February 2014 and February 2015. Methodology: Cancer cell viability assay MTT assay, bacterial plate-diffusion growth inhibition assay, and flow cytometry cell cycle analysis have been used to demonstrate the anticancerous/ anti-pathogen activities of the in-situ allicin. Diastereomers of alliin are produced by H2O2 oxidation of deoxyalliin, which is prepared by mixing L-cysteine and allyl bromide. Deoxyalliin and diastereomers of alliin are purified to high purity with repeated fractional crystallization. In addition, fluorenylmethyloxycarbonyl (Fmoc) protected alliin and alliin methyl ester are synthesized and purified with RP-HPLC to test the importance of amino and carboxyl groups of alliin in alliinase enzymatic reaction. Alliinase is produced by a simple and effective method from an aqueous garlic extract Results: Results from spectrophotometric alliinase activity assay indicate that (+)-L-alliin is more reactive toward alliinase than (-)-L-alliin, and both amino and carboxyl groups of the cysteine portion of alliin are critical in alliinase enzymatic reaction. Results from cancer cell viability assay MTT assay, bacterial plate-diffusion growth inhibition, and flow cytometry cell cycle analysis confirm that the in-situ allicin is as active as allicin purified from aqueous garlic extract or allicin synthesized chemically in a dose-dependent manner. Conclusion: We describe here facile pathways to synthesize diastereomerically pure alliins and isolate allinase. The in-situ allicin conversed from alliin by allinase is very active. The data obtained here provide useful information on the design of the in-situ allicin strategy.
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Garlic is a bulb from generalized liliaceous plant Alli-um sativum, it plays an essential role in the prevention and treat-ment of cardiovascular diseases, tumors and pathogenic microor-ganisms. Through consulting domestic and foreign references, the main active ingredients of garlic and their pharmacological effects are reviewed, the problems and achievement in Chinese research are also discussed. It can provide a certain reference for the further study of garlic and new drug development.
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S-allylcysteine sulfoxide (alliin), a colouless and odorless solid, existed in intact garlic (Allium sativum L.) cloves. Alliin itself possessed no antibacterial activity, but it quickly converts into allicin, an antibacterial component by the enzyme alliinase, which naturally occurs in garlic. This paper reported an isolation method for alliin from garlic that was in pilot scale
Subject(s)
Cysteine , AlliumABSTRACT
AIM: To establish a RP HPLC method to determine the content of alliin in Allium sativum Linn. METHODS: Chromatographic separation was performed on ODS column with a mobile phase composed of methanol water (3∶7 by volume). The eluate was monitored at 214nm wavelength. RESULTS: The average recovery of sample for alliin was 98.7%, The RSD of within day was 1.1%. The RSD of between day was 1.9%. CONCLUSION: The method is simple, rapid with good suitability.
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Objective: To develop HPLC method for determination of alliin concentration in mice plasma. Methods: The plasma samples were extracted with methanol. The analysis involved a ODS 1 column as stationary phase and distilled water as mobile phase. The flow rate was 0.5mL?min -1 , UV detection wavelength was at 220nm. 5 Fu was used as the internal standard. Results: The calibration curve was linear over a range from 14.8?g?mL -1 to 148.1?g?mL -1 with a correlation coefficient of 0.9992. Conclusion: The method is economic, simple, sensitive and accurate.
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AIM: To develop an HPLC method for determintion of alliin concentration in rat plasma and to study its pharmacokinetics in rat. METHODS : The plasma samples were extracted with methanol. The analysis involved a ODS-1 column as stationary phase and distilled water as mobile phase. The flow rate was 0.5mL?min -1 ,UV detection wavelength was at 220nm. 5-fluorouracil was used as the internal standard. RESULTS : The calibration curve was linear over the range from 3?g?mL -1 to 75?g?mL -1 with a correlation coefficient of 0.9989 . The mean recovery was 95%. The RSD of within-day and between-day were all less than 5%. The HPLC method of determination of alliin in the plasma was established. After single dose of 300mg?mL -1 in 6 rat,the main pharmacokinetic parameters were estimated to be as follows: CL( 0.048 )mg?min -1 ?kg -1 ,K_ 12 ( 0.0071 )min -1 ,K_ 21 ( 0.0093 )min -1 ,K_a(0.1915)min -1 ,t_ 1/2? ( 26.85 )min -1 ,t_ 1/2? ( 131.15 )min -1 , AUC( 6228.48 )?g?min -1 ?mL -1 . CONCLUSION : This method is quick,precise and reliable. It is shown that alliin is absorbed quickly in rat.