[關(guān)鍵詞]
[摘要]
摘 要：目的 設(shè)計(jì)合成薯蕷皂苷元衍生物，并評(píng)價(jià)其體內(nèi)抗血栓形成活性。方法 以薯蕷皂苷元為先導(dǎo)物，經(jīng)過(guò)酯化等反應(yīng)得到薯蕷皂苷元酯類衍生物，選擇動(dòng)靜脈旁路血栓形成模型，評(píng)價(jià)體內(nèi)抗血栓形成活性。結(jié)果 合成了6個(gè)目標(biāo)化合物，結(jié)構(gòu)經(jīng)過(guò)1H-NMR、13C-NMR、MS確證?？寡ㄐ纬苫钚院Y選結(jié)果顯示，目標(biāo)化合物3β-薯蕷皂苷元丁二酸單酯具有較好的抗血栓形成活性。結(jié)論 C-3位適當(dāng)親水性基團(tuán)的引入，有助于增強(qiáng)薯蕷皂苷元的抗血栓形成活性。
[Key word]
[Abstract]
Abstract: Objective To design and synthesize diosgenin derivative, and to evaluate their antithrombotic activity in vivo. Methods Taking diosgenin as lead compound, diosgenin derivatives were obtained by esterification reactions, and the antithrombotic effect of synthesized compounds was evaluated with the thrombogenesis model of artery-vein bypass in rats. Results Six target compounds were prepared and their structures were confirmed by 1H-NMR, 13C-NMR, and MS. Among these compounds, 3β- diosgeninyl monosuccinate showed promising antithrombotic activity in screening experiment. Conclusion A proper hydrophilic substitution on C-3 of diosgenin should be possible to improve the antithrombotic activity of diosgenin.
[中圖分類號(hào)]
[基金項(xiàng)目]
天津市自然科學(xué)基金資助項(xiàng)目（07TCZDJC05300）
