| This topic employed four unsaturated derivates synthisized by chosing as the templet:1,3-di(but-3-enyl)trisulfan,1,3-bis(3-methylbut-2-enyl)trisulfane,1,3-di (pent-4-enyl)trisulfane and 1,3-di(hex-5-enyl)trisulfane. Stimulant effect of these five compounds on macrophage cultured in vitro were compared, screening the stimulant drugs and temperature to obtain macrophage to the greatest extent.Anti-cancer effect caused by the changes of macrophage's morphous, vigor, phagotrophic ability, cytokine such as (IL-2,TNF-aand IFN—γ), NO, SOD and other related factors resulting from regulating Ca+ by these five compounds under different concentrations, is researched, and one or two derivates with good activity are obtained, the relationgship between biological activity and texture parameters is found by analyzing texture parameters of allicin and its derivates in order to synthisize compounds with better biological activity and stability.It demonstrated that stimulating mouse cultrued in 37℃by C3HNaO2S can offer macrophage to the greatest extent.It found that allicin and derivates can activated macrophage and increase the bulk.According to the result of MTT assay, allicin shows no significant effect on the vigor of macrophage, and improve the phagotrophic ability of macrophage to neutral red in every concentration to some extent and with the concentration increasing, it show dose-dependent tendency. Among all compounds, under 160μg/mL, 1,3-di(but-3-enyl)trisulfane has the best effect, the OD value assayed by Microplate Reader at 490nm is 0.270±0.018 which increased nearly 2.2 fold compared with the control.The cytotoxicity to PC-3 macrophage produced and mediated by allicin derivates was assayed. By calculating the apoptosis rate of PC-3, it was found that at 20μg/mL, allicin and its derivates do not improve the apoptosis rate of PC-3 through macrophage, but increasing the concentration to 40μg/mL, the apoptosis rate of PC-3 ascensus sharply and show dose-dependent tendency, in 1,3-di(but-3-enyl)trisulfane and 1,3-bis(3-methylbut-2-enyl) trisulfane group, the apoptosis rate is upon 85% at the maximum concentration.secretory volume of macrophage cytokines (IL-2,TNF-a and IFN—γ) is also assayed by ELISA Kit. The result indicated that secretory volume of IL-2,TNF-a and IFN—γdose not increase significantly at the concentration of 160μg/mL. with the increasing of concentration, secretory volume goes up. All compounds show great stimulant effect on IL-2,TNF-a, and only at the concentration of 160μg/mL, show significant effect on IFN—γ. In order to reflect the volume of NO macrophage released, the concentration of NO2- in the clear supernatant liquid was assayed by Griess method. The assay was took at 24h and 36h of macrophage cultured. with the concentration of compounds and time increased, the volume of released NO has the dose-dependent and time-dependent tendency. Compounds at 160μg/mL can improve the level of SOD assayed by Pyrogallol.The concentration of liber Ca+ was also assayed by adding Fμra-2 to the macrophage and detecting the fluorescence intensity. When concentraton increased to 80μg/mL, the concentration of liber Ca+ show the dose-dependent tendency, while higher than 80μg/mL, the tendency reversed.The molecular structure energy of allicin and its derivates is optimized by MM2 of chemoffice. it demonstrated that as extension of the carbon chain and the increasing of carbon in allicin and its derivates, hydrophobicity ClogP increased from 3.71 to 5.73 and the value of 1,3-bis(3-methylbut-2-enyl) trisulfane is higher than 1,3-di(pent-4-enyl)trisulfane. at the same time, HF and total energy reduced,HF value of 1,3-bis(3-methylbut-2-enyl) trisulfane is 30.61 which is almost one fold to the value of 1,3-di(pent-4-enyl)trisulfane 19.28, but total energy of them are almost the same.Based on the research of pharmacological activity, when the value of ClogP is over 4.8, prolong the carbon chain gives no help to the improvment of activity, and the compound with higher HF has better biological activity than its isomeride. meanwhile, the total energy reduced when the carbon chain is prolonging which make the derivates have better stabilityTo sum up, allicin and its derivates can improve the anti-cancer ability of macrophage, meanwhile, show negative effect on the growth of macrophage in vitro at the concentration of 160μg/mL. In different concertrations, all compounds can both improve the ability phagocytosis and anti-cancer. The main reason of this phenomonon was that all compounds can activate macrophage, increase the level of Ca+ and mediate cytokine such as IL-2,TNF-a,和NO, Based on the data that assayed, 1,3-di(but-3-enyl) trisulfane and 1,3-bis(3-methylbut-2-enyl) trisulfane, which can be employed in producing immunostimulants and anticancer agents for further research,have the good activities.In structure-function relationship, ClogP, MR, HF and total energy can offer valuable advices fot synthisizing allicin derivates..
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