Showing papers on "Allicin published in 2009"

Garlic: nature's protection against physiological threats.

Abstract: Currently reliance on natural products is gaining popularity to combat various physiological threats including oxidative stress, cardiovascular complexities, cancer insurgence, and immune dysfunction. The use of traditional remedies may encounter more frequently due to an array of scientific evidence in their favor. Garlic (Allium sativum) holds a unique position in history and was recognized for its therapeutic potential. Recent advancements in the field of immunonutrition, physiology, and pharmacology further explored its importance as a functional food against various pathologies. Extensive research work has been carried out on the health promoting properties of garlic, often referred to its sulfur containing metabolites i.e. allicin and its derivatives. Garlic in its preparations are effective against health risks and even used as dietary supplements such as age garlic extract (AGE) and garlic oil etc. Its components/formulations can scavenge free radicals and protect membranes from damage and maintains cell integrity. It also provides cardiovascular protection mediated by lowering of cholesterol, blood pressure, anti-platelet activities, and thromboxane formation thus providing protection against atherosclerosis and associated disorders. Besides this, it possesses antimutagenic and antiproliferative properties that are interesting in chemopreventive interventions. Several mechanisms have been reviewed in this context like activation of detoxification phase-I and II enzymes, reactive oxygen species (ROS) generation, and reducing DNA damage etc. Garlic could be useful in preventing the suppression of immune response associated with increased risk of malignancy as it stimulates the proliferation of lymphocytes, macrophage phagocytosis, stimulates the release of interleukin-2, tumor necrosis factor-alpha and interferon-gamma, and enhances natural killer cells. In this paper much emphasis has been placed on garlic's ability to ameliorate oxidative stress, core role in cardiovascular cure, chemopreventive strategies, and indeed its prospective as immune booster.

Antibacterial Potential of Garlic-Derived Allicin and Its Cancellation by Sulfhydryl Compounds

Abstract: Allicin (allyl 2-propenethiosulfinate), an antibacterial principle of garlic, has drawn much attention, since it has potent antimicrobial activity against a range of microorganisms, including methicillin-resistant Staphylococcus aureus. There have been many reports on the antibacterial properties of allicin, but no quantitative comparison of antibacterial activities between freshly prepared garlic extract and clinically useful antibiotics has been performed. To verify the substantial antibacterial effect of aqueous garlic extract, we compared it with those of allicin and several clinically useful antibiotics using two representative bacteria commonly found in the human environment, Gram-positive S. aureus and Gram-negative Escherichia coli. The garlic extract had more potent anti-staphylococcal activity than an equal amount of allicin. In terms of antibiotic potency against Gram-positive and Gram-negative bacteria, authentic allicin had roughly 1-2% of the potency of streptomycin (vs. S. aureus), 8% of that of vancomycin (vs. S. aureus), and only 0.2% of that of colistin (vs. E. coli). The antibacterial activity of allicin was completely abolished by cysteine, glutathione and coenzyme A, but not by non-SH-compounds. The oxygen in the structure (-S(=O)-S-) of allicin therefore functions to liberate the S-allyl moiety, which might be an offensive tool against bacteria.

Allicin up-regulates cellular glutathione level in vascular endothelial cells

Abstract: Allicin in garlic is the primary active compound known to rapidly interact with free thiols. To examine the effect of allicin on gene expression and glutathione cellular level in vascular endothelial cells. Cultured endothelial cells were exposed to allicin; mRNA was prepared and subjected to Micro-array and Real-Time PCR. Glutathione cellular level was determined on cell lysates. Micro-array analysis demonstrated allicin-induced up- and down-regulation of 116 and 100 genes, respectively. Up-regulated genes included the phase II detoxifying enzymes thioredoxin reductase 1 and 2, heme oxygenase-1 and glutamate cysteine lygaze modifier subunit, the rate limiting enzyme in glutathione biosynthesis. Endothelial cells exposed to allicin and its derivatives containing glutathione or cysteine residues increased cellular glutathione. Allicin increased the glutathione level in a concentration and time-dependent manner up to 8-fold at a concentration of 10–20 µM after 28 h exposure. Furthermore, allicin derivative-treated cultures demonstrated a 50% decrease in tBuOOH cytotoxicity. These results may suggest a putative role for allicin and its derivatives in preventing reactive oxygen species damage by up-regulating the phase II detoxifying enzymes and increasing the cellular glutathione level.

Garlic: empiricism or science?

Abstract: Garlic (Allium sativum L. fam. Alliaceae) is one of the best-researched, best-selling herbal remedies and is also commonly used as a food and a spice. Garlic constituents include enzymes (for example, alliinase) and sulfur-containing compounds, including alliin, and compounds produced enzymatically from alliin (for example, allicin). Traditionally, it has been employed to treat infections, wounds, diarrhea, rheumatism, heart disease, diabetes, and many other disorders. Experimentally, it has been shown to exert antilipidemic, antihypertensive, antineoplastic, antibacterial, immunostimulant and hypoglycemic actions. Clinically, garlic has been evaluated for a number of conditions, including hypertension, hypercholesterolemia, intermittent claudication, diabetes, rheumatoid arthritis, common cold, as an insect repellent, and for the prevention of arteriosclerosis and cancer. Systematic reviews are available for the possible antilipidemic, antihypertensive, antithrombotic and chemopreventive effects. However, the clinical evidence is far from compelling. Garlic appears to be generally safe although allergic reactions may occur.

Peroxyl-radical-scavenging activity of garlic: 2-propenesulfenic acid versus allicin.

Abstract: The OOH radical reactions with allicin and its Cope elimination products (2-propenesulfenic acid and thioacrolein) in aqueous solution have been studied. The CBS-QB3 quantum chemistry method has been used, with geometries and frequencies at BHandHLYP/6-311++G(d,p) level and conventional transition state theory. 2-Propenesulfenic acid is predicted to be over 1000 times more reactive toward OOH radical than allicin (2.60 x 10(7) vs 7.38 x 10(3) L mol(-1) s(-1), at 298 K). Accordingly, our results strongly support the novel suggestion by Vaidya et al. (Angew. Chem., Int. Ed. 2009, 48, 157) that the active ingredient responsible for the free radical scavenging activity of garlic is actually 2-propenesulfenic acid and not allicin. In addition, direct reaction branching ratios and product distribution for the three studied reactions are proposed for the first time.

Variability of Solids, Organosulfur Compounds, Pungency and Health-Enhancing Traits in Garlic (Allium sativum L.) Cultivars Belonging to Different Ecophysiological Groups

Abstract: Garlic is a vegetable mainly agamically propagated, and it has been dispersed all around the world. Garlic cultivars have been classified in different ecophysiological groups (EG) according to their bulbing requirements. The variability in organosulfur composition (ACSOs), solids content (SC), pungency (PC) and antiplatelet activity (IAA) and the correlation among these traits in garlic clones belonging to three EG was studied. We found variability for ACSOs, SC, PC and IAA between clones belonging to different EG and also among clones belonging to the same EG. Cutivars EG III presented more variability than EG IV for ACSOs, thiosulfinates, allicin and PC, while for SC, EG IV was the most variable. The correlations found suggested that IAA observed was mainly due to organosulfur composition. Finally recommendations about the most suitable cultivars for fresh consumption, pharmaceutical and dehydration industry are made.

Drying Kinetics and Allicin Potential in Garlic Slices during Different Methods of Drying

Abstract: Drying kinetics of garlic cloves was investigated by drying 5 mm thick slices in air, vacuum, and nitrogen atmosphere. The drying coefficient and lag factor were estimated from the slope and intercept of the moisture ratio time plot based on a model by Dincer-Hussain. Both drying coefficient and lag factor increased with increasing drying temperature. The diffusivity estimated from the Fick's law of diffusion and Dincer-Hussain's model differed, because Fick's law assumes negligible external mass transfer, whereas Dincer-Hussain's model considers both internal and external mass transfer resistance. Allicin, which is rapidly produced by the action of alliinase on alliin when fresh tissue is crushed, is the main biologically active phytochemical of garlic. Air drying at 50°C, vacuum drying at 50 and 60°C, nitrogen atmosphere drying at 40°C gave lowest losses of allicin potential. In general, the loss of allicin potential increased with increasing drying temperature, and drying below 50°C should be the best ...

Antibacterial Activity of Garlic Varieties (Ophioscordon and Sativum) on Enteric Pathogens

Abstract: The present study aimed at assessing the antibacterial activity of two varieties of garlic (ophioscordon and sativum) against enteric pathogens such as Escherichia coli, Proteus m irabilis, Salmonella typhi, Shigella flexineri and Enterobacter aerogenes. Aqueous extract of both the garlic varieties inhibited the growth of enteric pathogens at the concentrations of 200,300,400 and 500mg.However Enterobacter aerogenes was not susceptible to the aqueous extract of both the garlic varieties. Ethanolic extract of sativum was found to be highly effective against all the bacteria tested. HPTLC analyses of garlic varieties confirm the presence of allicin in various concentrations. Further analysis using GC-MS identified other compounds such as n-hexadecanoic acid, 3-deoxy-d-mannoic lactone, thymine and hexanedioic, bis (2-ethylhexyl) ester.

The vacuole-targeting fungicidal activity of amphotericin B against the pathogenic fungus Candida albicans and its enhancement by allicin

Abstract: In this study, the vacuole disruptive activity was evaluated as a cause of amphotericin B (AmB) lethality against the pathogenic fungus Candida albicans in terms of its enhancement by allicin, an allyl-sulfur compound from garlic. Vacuole disruption was observed in parallel to AmB-induced cell death when the antibiotic was used at a lethal concentration and at a non-lethal concentration in combination with allicin. Allicin did not enhance AmB-induced cell death and the accompanying vacuole disruption when the cells were incubated with exogenous ergosterol for its enrichment in the vacuole. The vacuoles isolated from intact cells could be directly disrupted by the action of AmB to the same extent in the absence and presence of allicin, whereas the organelles isolated from ergosterol-enriched cells were resistant to its direct disruptive action. AmB was similarly incorporated into the fungal cytoplasm in cells with or without ergosterol enrichment, supporting the fact that AmB-induced vacuole disruption depends on its direct disruptive action on the organelle. In agreement with these findings, allicin was found to inhibit ergosterol transport from the plasma membrane to the cytoplasm, which is considered to be a cellular protective response to AmB-induced vacuole disruption in S. cerevisiae. Our study suggests that AmB lethality against C. albicans depends at least in part on its vacuole disruptive activity under the physiological condition permissive for invasive growth of the fungus.

Anti-fungal efficacy of polybutylcyanoacrylate nanoparticles of allicin and comparison with pure allicin.

Abstract: Although garlic has been used in Chinese traditional medicine for its medical properties for thousands of years, investigations into its mode of action are relatively recent. The purpose of this study was to evaluate the in vitro anti-fungal efficacy of the active principle of garlic, pure allicin and polybutylcyanoacrylate (PBCA) nanoparticles (NPs) loaded with allicin. Pure allicin was prepared by reacting synthetic alliin with a stabilized process of the garlic enzyme alliinase. PBCA NPs were prepared by emulsion polymerization method and pure allicin was wrapped into it. The in vitro efficacy of pure allicin and PBCA-allicin NPs to Candida albicans, Cryputococcus neoformans, Trichophyton rubum, Microsporum gypseum, M. canis and Epidermophyton floccosum was examined and evaluated by MIC and MFC. The MIC of PBCA-allicin NPs to C. albicans (2.93 x 10(-2)mg/ml), T. rubum (1.46 x 10(-2)mg/ml) and E. floccosum (1.46 x 10(-2)mg/ml) was significantly lower than that of pure allicin (5.86 x 10(-2)mg/ml, 2.93 x 10(-2)mg/ml, 2.93 x 10(-2)mg/ml, respectively); accordingly, the MFC of PBCA-allicin NPs to C. albicans (5.86 x 10(-2)mg/ml), T. rubum (2.93 x 10(-2)mg/ml), E. floccosum (2.93 x 10(-2)mg/ml) and M. canis (2.93 x 10(-2)mg/ml) also decreased dramatically. These favourable results indicated that pure allicin has stronger in vitro anti-fungal efficacy to six tested fungi than alliinase and alliin. Moreover, it has improved significantly after pure allicin being wrapped into PBCA NP, which may be due to the NP's good prolonged release effect and nano-scale dimensions.

Effects of allicin on CYP2C19 and CYP3A4 activity in healthy volunteers with different CYP2C19 genotypes

Abstract: To investigate the interaction between allicin and omeprazole and to observe the effects of allicin on CYP2C19 and CYP3A4 activity in healthy Chinese male volunteers with different CYP2C19 genotypes. Eighteen subjects (six CYP2C19*1/CYP2C19*1, four CYP2C19*1/CYP2C19*2, two CYP2C19*1/ CYP2C19*3, and six CYP2C19*2/ CYP2C19*2) were enrolled in a two-phase randomized crossover trial. In each phase, all subjects received placebo or a 180 mg allicin capsule once daily for 14 consecutive days. The pharmacokinetics of omeprazole (20 mg orally on day 15) was determined for up to 12 h following administration by high-performance liquid chromatography. In carriers of the CYP2C19*1/CYP2C19*1 and CYP2C19*1/CYP2C19*2 or *3 genotype, allicin treatment increased the peak plasma concentration (Cmax) of omeprazole by 49.7 ± 7.2 (p < 0.001) and 54.2 ± 9.2% (p < 0.001), and increased the area under the plasma time–concentration curve ( $${\text{AUC}}_{\left( {0 - \infty } \right)} $$ ) of omeprazole by 48.1 ± 9.0 (p = 0.001) and 73.6 ± 26.7% (p < 0.001), respectively. The ratio of $${\text{AUC}}_{\left( {0 - \infty } \right)} $$ of 5-hydroxyomeprazole to omeprazole (a marker for CYP2C19 activity) decreased significantly (p < 0.001 and p = 0.001, respectively). However, no pharmacokinetic parameters were significantly changed by allicin in CYP2C19*2/CYP2C19*2. The Cmax and $${\text{AUC}}_{\left( {0 - \infty } \right)} $$ of omeprazole sulfone were unchanged in all three genotypes. Allicin reduced the metabolism of omeprazole by inhibiting CYP2C19 activity in individuals with the CYP2C19*1/CYP2C19*1 and CYP2C19*1/CYP2C19*2 or *3 genotypes, but not in those with the CYP2C19*2/ CYP2C19*2 genotype. Allicin did not significantly affect the activity of CYP3A4 in all subjects.

Enhancement of the fungicidal activity of amphotericin B by allicin: effects on intracellular ergosterol trafficking.

Abstract: In Saccharomyces cerevisiae, ergosterol was visible in the plasma membrane of untreated cells and was enriched in the vacuole membrane in response to amphotericin B (AmB) treatment at a non-lethal concentration. The simultaneous addition of allicin was inhibitory to AmB-induced ergosterol enrichment in the vacuole membrane, resulting in increased sensitivity of the organelles to the disruptive action of AmB. Allicin was also inhibitory to ergosterol enrichment in the vacuole membrane that was achieved by its external addition to cells. The combined fungicidal activity of AmB and allicin was suppressed together with suppression of vacuole membrane damage in cells where ergosterol had been fully enriched in the vacuole membrane. AmB caused direct disruptive damage of the isolated vacuoles, but the antibiotic was apparently less effective in disrupting the organelles that were isolated after ergosterol enrichment. These findings suggest that allicin enhances AmB-induced vacuole membrane damage by inhibiting ergosterol trafficking from the plasma membrane to the vacuole membrane.

Effects of Allium hirtifolium (Iranian shallot) and its allicin on microtubule and cancer cell lines

Abstract: Allium hirtifolim Boiss. (Iranian Shallot) belongs to Allium genus (Alliaceae family). Microtubule proteins (MTs) are crucial in maintenance of cell shape as well as cell division and mitosis. The present study aims at defining the anti-microtubule activities of A. hirtifolium and its allicin and examining its effects on nerve cell microtubules. MTs were prepared from sheep brain through two cycles of polymerization and depolymerization. The cell growth inhibition was measured by 3-(4,5-dimethylthiazol 2-yl)-2,5-diphenyl tetrazolium bromide (MTT) after treatment with A. hirtifolium and its allicin on HeLa and MCF-7 and L-929 cell lines. A. hirtifolium displayed growth inhibitory activity against HeLa and MCF-7 cells with IC (50) value of 20 and 24 mg/L, respectively, for 72 h and obviously showed cell growth inhibition on these cell lines at non-toxic concentration (lower than 1 g/L). Inhibition of MTs polymerization induced by A. hirtifolium and its ability to bind to tubulin as a ligand was tested through turbidimetry assay then investigated by Transmission Electron Microscopy (TEM). The concentration of A. hirtifolium necessary to inhibit the assembly of MTs by 50% was 1.2 g/L, while an inhibition higher than 80% was observed in the presence of 4 g/L of A. hirtifolium. This plant decreased MTs polymerization; therefore we suggest A. hirtifolium can be an effective ligand for cancer therapy.

Effects of allicin on invasion and metastasis of colon cancer LoVo cell line in vitro

Abstract: Objective To study the effect of allicin on invasion and metastasis of human colon cancer cell line LoVo in vitro and furthermore elucidate its anticancer mechanisms. Methods MTT assay was used to test dynamically the effect of cell growth inhibition.The inhibitory effects of allicin on movement, adhesiveness and invasiveness of LoVo cells were evaluated by the migratory test, adhesion test and Transwell chamber experiment.Quantitative real-time reverse transcription PCR (real-time RT-PCR) was performed to quantify the mRNA expression of MMP-2, TIMP-2, CD147, VEGF, nm23-H1, HPA and uPAR. Results Allicin had inhibitive effects on growth of LoVo cells in a dose and time-dependent manner.Allicin at non-cytotoxic concentration (3 and 6μg/ml) could obviously suppress the movement, adhesion and invasive capability of LoVo cells.In the allicin-treated group(3 and 6 μg/ml), after 24 hours, the inhibition rates of migratory time were 24% and 50%(t=4.543, 12.348, P=0.010, 0.001), the inhibition rates of adhesion were 19% and 28%(t=6.145, 6.355, P=0.004, 0.003), the inhibition rates of migration were 28% and 46%(t=8.065, 28.435,both P<0.01), and the inhibition rates of invasion were 44% and 65% respectively (t=21.274, 26.288, both P<0.01).Allicin at non-cytotoxic concentration could down-regulate the mRNA levels of VEGF, uPAR and HPA in a dose-dependent manner in LoVo cells (t=7.129, 6.764, 8.497, P=0.002, 0.002, 0.001) while the mRNA levels of TIMP-2, CD147 and nm23-H1 remained basically unchanged with the same treatment (t=0.341, 1.889, 0.914, P=0.059, 0.132, 0.412).The expression of MMP-2 had not been detected in LoVo cells. Conclusion Allicin in vitro inhibits invasion and metastasis of human colon carcinoma cell LoVo at non-cytotoxic concentration through down-regulating the expression of VEGF, uPAR and HPA mRNA. Key words: Colonic neoplasms; Garlic; Cell proliferation; Cell adhesion; Neoplasm metastasis志谢江苏省淮安市科技支撑计划(HAS08009)支持

Disulfide-mediated apoptosis of human T-lymphotrophc virus type-I (HTLV-I)-infected cells in patients with HTLV-I-associated myelopathy/tropical spastic paraparesis.

Abstract: Background This study was conducted to construct a basis for a therapeutic strategy against human T-lymphotropic virus type-I (HTLV-I)-associated myelopathy/tropical spastic paraparesis (HAM/TSP) using a compound that contained a disulfide moiety, prosultiamine, which is a homologue of allithiamine originally synthesized by allicin and thiamine-thiol, for the targeting of HTLV-I-infected cells. Methods First, we analysed the apoptotic pathway in allicin or prosultiamine treatment against an HTLV-I-infected T-cell line (HCT-1), derived from an HAM/TSP patient, by flow cytometry and western blot. Second, we evaluated the effect of targeting HTLV-I-infected cells in a prosultiamine in vitro treatment and in a clinical trial in HAM/TSP patients by quantitative PCR analysis of HTLV-I proviral load. Results Prosultiamine, like allicin, induced caspase-dependent apoptosis against HCT-1 cells. The fact that the loss of mitochondrial membrane potential was recovered in z-VAD-fmk-pretreated HCT-1 cells with prosultiamine treatment suggested that prosultiamine can induce caspase-dependent apoptosis through the mitochondrial pathway. On the basis of data showing that prosultiamine in vitro treatment against peripheral blood CD4(+) T-cells of HAM/TSP patients induced a significant decrease of HTLV-I proviral copy numbers by apoptosis of HTLV-I-infected cells, we treated six HAM/TSP patients with intravenous administration of prosultiamine for 14 days. As a result of this treatment, the copy numbers of HTLV-I provirus in peripheral blood decreased to approximately 30-50% of their pretreatment levels with some clinical benefits in all patients. Conclusions Our results suggest that prosultiamine has the potential to be a new therapeutic tool that targets HTLV-I-infected cells in HAM/TSP.

The Protective Effect of Garlic Extract against Acetaminophen-Induced Loss of Mitochondrial Membrane Potential in Freshly Isolated Rat Hepatocytes

Abstract: Overdose of acetaminophen causes severe hepatic necrosis in humans and experimental animals. Studies on its hepatotoxicity remain a very active area since some of current data are still uncertain. In this study, freshly isolated rat hepatocytes were used to determine the effects of garlic extract and its component, allicin on the acetaminophen-induced cell cytotoxicity and to compare with the effect of Nacetyl cysteine as a standard treatment. Garlic extract was prepared via a standard method and its allicin and allyl mercaptan contents were determined using analytical and preparative high performance liquid chromatography (HPLC). Rat hepatocytes were isolated using collagenase perfusion and mitochondrial membrane potential and cell cytotoxicity were determined using Rhodamine 123 fluorescence and trypan blue exclusion, respectively. Inclusion of garlic extract and/or N-acetyl cysteine resulted in a reduction in the loss of mitochondrial membrane potential as well as cell death which occurred after acetaminophen addition and therefore, illustrated considerable hepatoprotective effects without significant differences between two treatments. In contrast, pure allicin was not effective significantly. The hepatoprotective effects of garlic extract may be due to the compounds other than allicin such as allyl mercaptan, as allicin has been shown to transform to allyl mercaptan as a major metabolite.

Biological Constituents of Aged Garlic Extract as Biomarker

Abstract: Garlic (Allium sativum) are an agronomically important genus because of their sulfur flavour components. The majority of the volatiles flavour principles are generated through the enzymatic hydrolysis of the non-volatile organosulfur compounds. However, these compounds may be possible sources of new novel bioactive and therapeutic principles. Garlic has strong antioxidant activity, and epidemiological studies support the fact that diets rich of garlic may prevent some of the chronic diseases. The health cares of garlic likely arise from a wide variety of components, which may work synergistically. The chemical changes of garlic composition makes it plausible that a variation in processing can lead to acquisition of differential chemical compositions of garlic products. Especially highly unstable allicin can easily disappear during processing and are quickly transformed into a various organosulfur compounds. Various supplements of garlic, particularly aged garlic extract (AGE), are known to possess a promising antioxidant potential and are effective in prevention of chronic diseases because of the bioactive constituents. Although all of active ingredients of AGE are not elucidated, water-soluble components of AGE, including S-allylcysteine, S-allylmercaptane, steroid saponins, tetrahydro-β-carboline derivatives, and fructosyl-arginine, appears to be associated with the pharmacological effects of AGE. Consequently, the allicin free garlic components such as S-allylcysteine, S-allylmercaptane, steroid saponins, tetrahydro-β-carboline derivatives, and fructosyl-arginine can be applicable to standardization of the quality of commercial garlic products. This review provides an insight into garlic's biomarkers and presents evidence that they may either prevent or delay chronic disease associated with aging.

Antibacterial activity of allicin from Allium sativum against antibiotic resistant uropathogens

Abstract: Antibacterial activity of A. sativum was tested against gram-positive and gram-negative bacterial isolates from Urinary Tract of Indian patients, which were confirmed for resistant against commonly used antibiotics for urinary tract infections. In present study, only five quantities (10, 20, 30, 40 and 50μg) of aqueous allicin from A. sativum cloves and leaves were used, which has antibacterial activity against test isolates by disc diffusion method. The maximum inhibitory activity of allicin against all test isolates was observed at 40μg and the quantity was found statistically significant (P< 0.01) for antibacterial activity of allicin extracted from A. sativum cloves and leaves against UT bacterial isolates.

Inclusion of the allicin mimic S-p-tolyl t-butylthiosulphinate in β-cyclodextrin

Abstract: Allicin, the active thiosulphinate present in freshly crushed garlic, has potent antimicrobial activity but is chemically labile. As part of a study aimed at producing stable allicin analogues as potential antimicrobial agents, the allicin mimic S-p-tolyl t-butylthiosulphinate was synthesised and complexed with β-cyclodextrin (β-CD). The inclusion complex, β-CD·S-p-tolyl t-butylthiosulphinate·12.5H2O, was characterised by thermal analysis techniques (HSM, TG, DSC), powder X-ray diffraction and single-crystal X-ray diffraction. The inclusion complex is dimeric (space group C2221) with the guest disordered over three positions. Within each β-CD molecule of the dimer, each disordered guest component is located in the host cavity with the t-butyl group protruding slightly from the primary hydroxyl side, while the phenyl ring is situated near the secondary hydroxyl side and the thiosulphinate moiety is centrally located within the host cavity. Stereoselectivity of guest inclusion is implicit in the disordered ...

Allicin external preparation and prepration method thereof

Abstract: The invention relates to an allicin external preparation and a prepration method thereof. The external preparation comprises ointment,plaster, inclusion plaster, gels and so on. Allicin is taken as an active effective ingredient, pharmaceutical excipients for the external preparation and the like are added for preparation, the weight percentage of the allicin is 0.1-10 percent, and the rest is the pharmaceutical excipients for the external preparation. The allicin has stronger anti-bacterial and anti-inflammatory effects and can inhibit or kill a variety of coccus (staphylococcus, streptococcus, and the like), bacilli (dysentery, typhoid, colon, whooping cough), fungi (candida albicans, yeast, and the like), viruses and so on. The allicin external preparation can be used for treating acute bacillary dysentery, amoebic dysentery, whooping cough, infant diarrhea, lobar pneumonia, tuberculosis, deep fungal infection (cryptococcal meningitis, candida albicans pyosepticemia, respiratory fungal infection, and the like), wound suppuration, psoriasis, trachoma and so on.

Alliin/alliinase dualistic drug-releasing multilayer tablet that can resist infection diseases caused by helicobacter pylori and candida albicans and the like

Abstract: The invention discloses a method for preparing an alliin/alliinase dualistic drug-releasing multilayer tablet that can resist infection diseases caused by helicobacter pylori and candida albicans and on the like The tablet is composed of three layers, namely, an alliin layer, a separation layer and an alliinase layer The outside of the tablet is wrapped by an intestine-dissolving film coat (for oral administration) or a common film coat (for vagina application) When the tablet is swallowed, the intestine-dissolving film coat (for oral administration) or the common film coat (for vagina application) is dissolved by body fluid, and the alliin and the alliinase meet each other and generate catalysis effect to produce allicin, thus having the drug effect of anribacterium to pathogenic bacterium such as the helicobacter pylori and candida albicans and the like

Method for producing deodorized garlic highly containing alliin

Abstract: PROBLEM TO BE SOLVED: To provide a method for producing deodorized garlic highly containing alliin, and deodorized garlic extract, and to provide a garlic material having flavor with almost no odor, or food added with the material.SOLUTION: (1) The method for producing the deodorized garlic highly containing alliin includes mixing with the edible part of garlic, an acid substance or a solution in which the substance is dissolved, and crushing the mixture so as to bring the pH of the crushed product to ≤3.0, preferably ≤2.8. (2) Alternatively, the method for producing the deodorized garlic highly containing alliin includes mixing with the edible part of garlic, a basic substance or a solution in which the substance is dissolved, and crushing the mixture so as to bring the pH of the crushed product to ≥10.0, preferably ≥10.3. (3) The deodorized garlic food material highly containing alliin (slurry, powder, extract or the like) and prevented from converting alliin in garlic to allicin by the method is also provided.

Inhibitory Effects of Allicin on TNF-α-induced ICAM-1 Expression is Associated with Catalase

Abstract: Allicin, a garlic componente, is believed to provide protection against various diseases including inflammation. Since interactions of the cell adhesion molecules are known to play important roles in mediating inflammation, inhibiting adhesion protein upregulation is a possible therapeutic target. In this study, we demonstrate that TNF-α- and catalase-induced expression of ICAM-1 on human lung epithelial cells (A549) in a dose-dependent manner and catalase expression and activity were also increased in TNF-α-treated cells. Treatment of the TNF-α-treated cells with catalase inhibitor 3-amino-1,2,4-triazole resulted in a significant decreased the level of ICAM-1. These data suggest that induction of ICAM-1 expression by TNF-α is associated with catalase. In addition, allicin was found to inhibit the TNF-α induced expression of ICAM-1 on the A549 cells. This compound also inhibited the production of catalase induced by TNF-α, which suggests that the inhibition of ICAM-1 expression by allicin may be due to the modulated production of catalase.

A process of functional garlic vineger

Abstract: PURPOSE: A method for producing functional garlic vinegar is provided to preserve allicin, which is a main pharmacological ingredient of garlic and ensure anti-cancer and sterilization activities. CONSTITUTION: A step of producing functional garlic vinegar comprises: a step of preparing garlic(S1); a step of mixing garlic, inorganic salt, acetic acid, sugar or honey, and purified water then fermenting at 60°C for 45 days(S2); a step of inoculating acetobacter to mixture of fermented garlic composition, medium and ethanol and shaking at 35°C and 120rpm(S3); and a step of fermenting for 30 days and maturing for 35 days(S4). In the second step(S2), the mixture contains 40 weight% of garlic, 19 weight% of inorganic salt, 1.0 weight% of acetic acid, 10 weight% of saccharides(sugar or honey), and 30 weight% of purified water.

Allicin enhances cytotoxicity of CPT-11 to colon cancer LoVo cell in vitro.

Abstract: Objective:To study the effect of allicin on human colon cancer cell line LoVo and the combined effect of allicin and CPT-11 on this cancer cell line.Method:The LoVo cells were cultured in vitro and treated with allicin in different concentrations.MTT assay was used to test dynamically the cell growth inhibiting effect.Apoptosis induction(Annexin-V-FITC/PI) and modulation of DNA cell cycle were measured by flow cytometry.The change of cytotoxicity of CPT-11 after combination of allicin at the concentration of 4.0,8.0 mg·L-1 were investigated.Result:Allicin had inhibitive effect on growth of LoVo cells in a dose and time dependent manner,with IC50 value of 32.23,10.74,6.58 mg·L-1 at 24 h,48 h and 72 h,respectively.The apoptosis rate of LoVo cells increased progressively as the cells were treated with increasing concentration of allicin in 24 h,while the apoptosis rate achieved peak value when the cells were treated with allicin at the concentration of 8 mg·L-1 in 48 h.The result indicated the low concentrations of allicin( 4 mg·L-1) lead to G2/M cell cycle arrest,and higer concentrations(4 mg·L-1) exert G1 + G2/M cell cycle arrest in 24 h.Compared with single use of CPT-11,the combined use of CPT-11 and allicin(4.0,8.0 mg·L-1,respectively) showed increasing cytotoxicity on the LoVo cells,with IC50 of 24 h decreasing from 47.5 to 7.4 and 7.2 mg·L-1,respectively.Conclusion:Allicin has significant anti-proliferation effect on human colon cancer cell line LoVo by induction of apoptosis and arrestment of cell cycle and can enhance the cytotoxicity of CPT-11 on the colon cancer LoVo cell.

Composition used for treating AIDS and associated diseases and preparation method thereof

Abstract: The invention relates to a pharmaceutical composition, in particular to a composition used for treating AIDS. The composition for treating AIDS and associated diseases comprises the following components (wt%): 30-40% of diallyl disulfide (DADS), about 40-50% of diallyl trisulfide (DATS), namely allicin, and 10-30% of allyl methyl disulfide. A preparation method of the composition used for treating AIDS and associated diseases comprises the following steps of: selecting big and plump garlic; peeling off, washing and mashing the same; putting the garlic spread in a distilling device, adding distilled water or pure water; distilling, collecting volatile oil in a brown glass bottle; preserving at 0-5 DEG C. the composition of the invention can act on HIV-1 virus and has comparatively good effect on AIDS and associated diseases.