葫芦素具有四环素葫芦烷核骨架并且高度氧化,现代药理研究表明其具有抗肿瘤、保肝、抗炎、提高机体免疫等多种生物活性,其中葫芦素 B、葫芦素 D、葫芦素 E、葫芦素 I、雪胆甲素、雪胆乙素有抗肿瘤活性,对肝癌、乳腺癌、前列腺癌、肺癌及其他肿瘤细胞均有诱导凋亡、抑制增殖的药理作用;能够通过调节信号转导及转录活化因子 3(STAT3)、丝裂原活化蛋白激酶(MAPK)和其他信号通路、阻滞细胞周期、影响细胞骨架等,发挥抗肿瘤作用,对部分恶性肿瘤的治疗药物开发具有深远意义。

Cucurbitin has tetracycline cucurbitane nuclear skeleton and is highly oxidized. Modern pharmacological studies have shown that it has various biological activities such as anti-tumor, liver protection, anti-inflammatory, and improving the body's immunity, among which cucurbitin B, cucurbitin D, cucurbitin E, cucurbitin I, hemslecin A and 23,24-dihydrocucurbitacin F have anti-tumor activities. It can induce apoptosis and inhibit proliferation of liver cancer, breast cancer, prostate cancer, lung cancer and other tumor cells. By regulating signal transduction and transcriptional activation factor 3 (STAT3), mitogen activated protein kinase (MAPK) and other signaling pathways, blocking cell cycle and affecting cytoskeleton, it can play an anti-tumor role, which has farreaching significance for the development of therapeutic drugs for some malignant tumors.

R285.5

释药技术与药代动力学国家重点实验室(天津药物研究院)开放课题资助项目(010161003)