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| 1 | Evaluation and SAR analysis of the cytotoxicity of tanshinones in colon cancer cells显示文摘AIM:This study was designed to evaluate the anti-cancer actions of tanshinone I and tanshinone IIA,and six derivatives of tanshinone IIA on normal and cancerous colon cells.Structure activity relationship(SAR) analysis was conducted to delineate the significance of the structural modifications of tanshinones for improved anti-cancer action.METHOD:Tanshinone derivatives were designed and synthesized according to the literature.The cytotoxicity of different compounds on colon cancer cells was determined by the MTT assay.Apoptotic activity of the tanshinones was measured by flow cytometry(FCM).RESULTS:Tanshinone I and tanshinone IIA both exhibited significant cytotoxicity on colon cancer cells.They are more effective in p53+/+ colon cancer cell line.It was also noted that the anti-cancer activity of tanshinone I was more potent and selective.Two of the derivatives of tanshinone IIA(N1 and N2) also exhibited cytotoxicity on colon cancer cells.CONCLUSIONS:The anti-colon cancer activity of tanshinone I was more potent and selective than tanshinone IIA,and is p53 dependent.The derivatives obtained by structural modifications of tanshinone IIA exhibited lower cytotoxicity on both normal and colon cancer cells.From steric and electronic characteristics point of view,it was concluded that structural modifications of ring A and furan or dihydrofuran ring D on the basic structure of tanshinones influences the activity.An increase of the delocalization of the A and B rings could enhance the cytotoxicity of such compounds,while a non-planar and small sized D ring region would provide improved anti-cancer activity. | WANG Lin LIU An ZHANG Fei-Long Yeung John H.K. LI Xu-Qin CHO Chi-Hin | 2014 | Chinese Journal of Natural Medicines2014，12，3： | 6 |
| 2 | 丹参酮ⅡA及其类似物的全合成和结构修饰研究进展显示文摘丹参酮ⅡA具有抗肿瘤、抗炎抑菌及抗心血管疾病等广泛药理活性,但该化合物同时存在脂溶性高、半衰期短和生物利用度低等缺点,使其临床应用受到限制。因此研究人员不断尝试对丹参酮ⅡA进行结构改造,以期改善其理化性质和药动学参数。综述丹参酮ⅡA及其类似物的全合成和结构修饰的研究进展。 | 许昌胜 陈莉 | 2013 | 药学进展2013，37，2： | 4 |
| 3 | 丹参酮IIA衍生物的合成显示文摘目的:丹参酮IIA是中药丹参的脂溶性成分,具有抗肿瘤、抗氧化、抗心脑血管疾病等多种生理活性。本文拟对其进行结构改造以获得活性更好的丹参酮IIA衍生物。方法:首先,以丹参酮IIA为原料,通过Vilsmeier反应在其16-位引入醛基,再与醋酸胺进行还原胺化反应,以较高收率得到16-位胺甲基取代的丹参酮IIA衍生物。接着,对其氨基进行修饰,得到10个不同N-取代的丹参酮IIA衍生物。同时考察反应温度、反应溶剂和反应时间等条件对还原胺化反应的影响,确定最佳反应条件。结果:通过1H-NMR、13C-NMR以及LC-MS对所有产物结构进行了确认。还原胺化反应的最佳反应条件为:以1,2-二氯乙烷为溶剂,温度保持40℃,反应时间为2h。结论:反应步骤简单、条件温和、产率较高,是合成16-位取代的丹参酮IIA衍生物的理想方法。 | 姚连琦 秦立玙 李雯 刘德龙 | 2018 | 现代生物医学进展2018，18，2： | 0 |
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