Meng Yan-qiu, Liu Dan, Bai Zhong-wei, Cai Ling-li, Ai Hong-ru
Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China.
Yao Xue Xue Bao. 2011 May;46(5):556-60.
Structure of natural product-ursolic acid was modified for increasing its antitumor activity. Ursolic acid was acylated, esterified, hydrolized or oxidized to obtain target pentacyclic triterpenoid compounds with different substitutes. Sixteen derivatives of ursolic acid were designed and synthesized including eleven new compounds. Anti-tumor activities of ursolic acid and these derivatives against HeLa, SKOV3 and BGC-823 cells in vitro were investigated by MTT assay. The results indicated that compounds 7a and 8a were found to have stronger cell growth inhibitory than ursolic acid on HeLa cells and SKOV3 cells separately, and are worth to be intensively studied further.
对天然产物熊果酸的结构进行修饰以提高其抗肿瘤活性。对熊果酸进行酰化、酯化、水解或氧化，以获得具有不同取代基的目标五环三萜类化合物。设计并合成了16种熊果酸衍生物，其中包括11种新化合物。通过MTT法研究了熊果酸及其衍生物对HeLa、SKOV3和BGC-823细胞的体外抗肿瘤活性。结果表明，化合物7a和8a分别对HeLa细胞和SKOV3细胞具有比熊果酸更强的细胞生长抑制作用，值得进一步深入研究。
