Lim H, Kubota K, Kobayashi A, Seki T, Ariga T
Department of Nutrition and Food Science, Ochanomizu University, Tokyo, Japan.
Biosci Biotechnol Biochem. 1999 Feb;63(2):298-301. doi: 10.1271/bbb.63.298.
The inhibitory effects of three pure compounds isolated from wood garlic, 2,4,5-trithiahexane (I), 2,4,5,7-tetrathiaoctane (II), and 2,4,5,7-tetrathiaoctane 2,2-dioxide (III), on rabbit platelet aggregation induced by collagen, arachidonic acid, U46619, ADP (adenosine 5'-diphosphate), PAF (platelet aggregating factor), and thrombin were studied in vitro. The anti-aggregating activity of 2,4,5,7-tetrathiaoctane 4,4-dioxide (IV) was also measured with collagen and arachidonic acid. I, II, III, and IV inhibited the platelet aggregation induced by all tested agonists. I, II, and III exhibited a stronger inhibitory effect against the thrombin-induced aggregation of GFP (gel-filtered platelets) than against the aggregation induced by the other agonists. Notably, the IC50 value for III was 4 microM, which is approximately 2.5 times stronger than MATS (methyl allyl trisulfide), a major anti-platelet compound isolated from garlic. In inhibiting collagen-induced aggregation, II was as potent as MATS and aspirin, with a marked disaggregation effect on the secondary aggregation by arachidonic acid, at the rate of 47.05%/min at a concentration of 10(-4) M. I, II, and III also suppressed U46619-induced aggregation. These results suggest that sulfur-containing compounds in wood garlic not only inhibit arachidonic acid metabolism but also suppress aggregation in association with the function of the platelet plasma membrane.
研究了从木蒜中分离出的三种纯化合物,即2,4,5-三硫己烷(I)、2,4,5,7-四硫辛烷(II)和2,4,5,7-四硫辛烷2,2-二氧化物(III)对胶原、花生四烯酸、U46619、ADP(腺苷5'-二磷酸)、PAF(血小板聚集因子)和凝血酶诱导的兔血小板聚集的体外抑制作用。还测定了2,4,5,7-四硫辛烷4,4-二氧化物(IV)对胶原和花生四烯酸的抗聚集活性。I、II、III和IV均抑制了所有测试激动剂诱导的血小板聚集。I、II和III对凝血酶诱导的绿色荧光蛋白(凝胶过滤血小板)聚集的抑制作用比对其他激动剂诱导的聚集作用更强。值得注意的是,III的IC50值为4 microM,约为从大蒜中分离出的主要抗血小板化合物MATS(甲基烯丙基三硫化物)的2.5倍。在抑制胶原诱导的聚集方面,II与MATS和阿司匹林一样有效,对花生四烯酸诱导的二次聚集有明显的解聚作用,在10(-4) M浓度下解聚速率为47.05%/分钟。I、II和III也抑制了U46619诱导的聚集。这些结果表明,木蒜中的含硫化合物不仅抑制花生四烯酸代谢,还与血小板质膜功能相关地抑制聚集。