Study on the Synthesis and Biological Activity of Diacid Solanesyl Galactosyl Diesters

Wang Chaojie,  Wang Yuxia,   Song Jinyong,  Zhao Jin
(Henan Provincial Key Laboratory of Special Functional Materials, Henan University, Kaifeng  475001)

Abstract  Six compounds of diacid solanesyl galactosyl diesters 4a～4f were first designed and synthesized by the reaction of O-acetylpyranosyl bromide with diacid solanesyl monoesters in the presence of tetrabutyl ammonium bromide. The structures of all the target compounds were characterized by IR, ¹H NMR, MS and elemental analysis. Compound 4d was tested preliminarily for biological evalution on KB、Bel-7402、HCT-8、5-HT、TcAChE inhibitor models. The results show that this kind of compounds have only weak inhibitions on Bel-7402、HCT-8、5-HT、TcAChE inhibitor biomodels and no effect on KB cell.
Key words   Diacid solanesyl monoester,  Diacid solanesyl galactosyl diester,  Synthesis,  Biological activity

茄呢醇半乳糖酯的合成及生理活性测试

王超杰  王玉霞  宋金勇  赵 瑾
(河南大学特种功能材料省重点实验室  开封  475001)

摘要  六个二元酸茄呢醇单酯分别与溴代半乙酰半乳糖在相转移催化剂四丁基溴化铵的催化下反应生成对应的糖酯4a～4f，这六个化合物均为新化合物，其结构经过元素分析、IR、¹H NMR和MS确证。对化合物4d进行了初步的体外生理活性研究，结果表明4d对Bel-7402(人肝癌细胞)、HCT-8(人结肠癌细胞)、5-HT(重摄取抗抑郁)、乙酰胆碱酯酶四种生物模型有弱的抑制活性，对KB(人口腔上皮癌细胞)生物模型无活性。
关键词  二元酸茄呢醇单酯  二元酸茄呢醇半乳糖二酯  合成  生理活性

王超杰  男，38岁，博士，主要从事天然产物的分离及药物合成。
河南省重点攻关(0323024000)，河南省自然基金(0311020900)及河南大学重点学科资助项目
2003-06-05收稿，2003-09-13接受

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