葫蘆素具有四環(huán)素葫蘆烷核骨架并且高度氧化,現(xiàn)代藥理研究表明其具有抗腫瘤、保肝、抗炎、提高機體免疫等多種生物活性,其中葫蘆素 B、葫蘆素 D、葫蘆素 E、葫蘆素 I、雪膽甲素、雪膽乙素有抗腫瘤活性,對肝癌、乳腺癌、前列腺癌、肺癌及其他腫瘤細胞均有誘導(dǎo)凋亡、抑制增殖的藥理作用;能夠通過調(diào)節(jié)信號轉(zhuǎn)導(dǎo)及轉(zhuǎn)錄活化因子 3(STAT3)、絲裂原活化蛋白激酶(MAPK)和其他信號通路、阻滯細胞周期、影響細胞骨架等,發(fā)揮抗腫瘤作用,對部分惡性腫瘤的治療藥物開發(fā)具有深遠意義。

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

釋藥技術(shù)與藥代動力學(xué)國家重點實驗室(天津藥物研究院)開放課題資助項目(010161003)