Yang Shengjie, Liang Na, Li Hu, Xue Wei, Hu Deyu, Jin Linhong, Zhao Qi, Yang Song
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, P,R, China.
Chem Cent J. 2012 Nov 23;6(1):141. doi: 10.1186/1752-153X-6-141.
Tumor, is one of the major reason for human death, due to its widespread occurrence. Betulinic acid derivatives have attracted considerable attention as cancer chemopreventive agents and also as cancer therapeutics. Many of its derivatives inhibit the growth of human cancer cell lines by triggering apoptosis. With this background, we planned to synthesize a series of betulinic acid derivatives to assess their antiproliferation efficacy on human cancer cell lines.
A series of novel betulinic acid derivatives were designed and synthesized as highlighted by the preliminary antitumor evaluation against MGC-803, PC3, A375, Bcap-37 and A431 human cancer cell lines in vitro. The pharmacological results showed that some of the compounds displayed moderate to high levels of antitumor activities with most of new exhibiting higher inhibitory activities compared to BA. The IC50 values of compound 3c on the five cancer cell lines were 2.3, 4.6, 3.3, 3.6, and 4.3 μM, respectively. Subsequent fluorescence staining and flow cytometry analysis (FCM) indicated that compound 3c could induce apoptosis in MGC-803 and PC3 cell lines, and the apoptosis ratios reached the peak (37.38% and 33.74%) after 36 h of treatment at 10 μM.
This study suggests that most of betulinic acid derivatives could inhibit the growth of human cancer cell lines. Furthermore, compound 3c could induce apoptosis of cancer cells.
肿瘤是导致人类死亡的主要原因之一，因其广泛发生。桦木酸衍生物作为癌症化学预防剂和癌症治疗剂已引起了相当大的关注。其许多衍生物通过触发细胞凋亡来抑制人类癌细胞系的生长。在此背景下，我们计划合成一系列桦木酸衍生物，以评估它们对人类癌细胞系的抗增殖功效。
设计并合成了一系列新型桦木酸衍生物，体外针对MGC-803、PC3、A375、Bcap-37和A431人类癌细胞系的初步抗肿瘤评估突出显示了这些衍生物。药理结果表明，一些化合物表现出中度至高度的抗肿瘤活性，与桦木酸相比，大多数新化合物表现出更高的抑制活性。化合物3c对五种癌细胞系的IC50值分别为2.3、4.6、3.3、3.6和4.3μM。随后的荧光染色和流式细胞术分析（FCM）表明，化合物3c可诱导MGC-803和PC3细胞系凋亡，在10μM处理36小时后，凋亡率达到峰值（37.38%和33.74%）。
本研究表明，大多数桦木酸衍生物可抑制人类癌细胞系的生长。此外，化合物3c可诱导癌细胞凋亡。
