Synthesis And Antitumor Activities Of Stigmasterol Derivatives

The stigmasterol is a component of phytosterol, and is isolated from a natural plant steroidal, It not only revealed significant anti-oxidation, anti-tumor, anti-cardiovascular disease and other pharmacological activity, but also to the starting material of the synthesis of steroid drugs. Because of high activity, low toxicity, wide application and other advantages, It becomes a research focus of the majority of scientists in recent years.In this paper, the natural extract of Stigmasterol as the raw material,11derivatives of Stigmasterol compounds are synthesized. The structures are confirmed by1H NMR, MS and element analysis, Biological activity of synthetic compounds are investigated. The main content of this article is divided into three parts:First, the recent progress of the pharmacological activities and synthesis for phytosterol, Stigmasterol and their derivatives were summarized, the significance and the main research works of the article were reviewed.Second, stigmasterol as the raw material, according to stigmasterol function group,11kinds of derivatives of stigmasterol were designed and synthesized. AB-l-AB-4and AB-6-AB-9were obtained by modifing the hydroxyl group of stigmasterol. AB-5is a compound that modifing the stigmasterol double bond by bromine addition. The structure of all Compounds were confirmed by1H NMR, MS and element analysis, and the melting point of the compounds were determinedThe third, adriamycin as the positive control, Stigmasterol and the synthetic derivatives AB-1-11were initially evaluated for their anti-tumor activity in NKM45、SKOV3、HEPG-2and MDA-MB-231cell lines by MTT method. Overall, stigmasterol and11derivatives showed anti-tumor specificity of NKM45and SKOV3inhibitory effect was not significant, while it showed different inhibitory activity in the HEPG-2, MDA-MB-231. Particularly, AB-5, AB-6, AB-8, and AB-10that the inhibition rate of tumor cells is greater than the positive control adriamycinin the best time and the range of optimum concentration. It laid the foundation for the subsequent experiments.