Cai Yuee, Fang Xiefan, He Chengwei, Li Peng, Xiao Fei, Wang Yitao, Chen Meiwan
* State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau 999078, P.R. China.
† Department of Pediatrics, College of Medicine, University of Florida, Gainesville, FL 32610, USA.
Am J Chin Med. 2015;43(7):1331-50. doi: 10.1142/S0192415X15500755. Epub 2015 Oct 27.
Cucurbitacins are highly oxidized tetracyclic triterpenoids that are widely present in traditional Chinese medicines (Cucurbitaceae family), possess strong anticancer activity, and are divided into 12 classes from A to T with over 200 derivatives. The eight most active cucurbitacin components against cancer are cucurbitacin B, D, E, I, IIa, L glucoside, Q, and R. Their mechanisms of action include antiproliferation, inhibition of migration and invasion, proapoptosis, and cell cycle arrest promotion. Cucurbitacins are also found to be the inhibitors of JAK-STAT3, Wnt, PI3K/Akt, and MAPK signaling pathways, which play important roles in the apoptosis and survival of cancer cells. Recently, new studies have discovered synergistic anticancer effects by using cucurbitacins together with clinically approved chemotherapeutic drugs, such as docetaxel and methotrexate. This paper provides a summary of recent research progress on the anticancer property of cucurbitacins and the various intracellular signaling pathways involved in the regulation of cancer cell proliferation, death, invasion, and migration. Therefore, cucurbitacins are a class of promising anticancer drugs to be used alone or be intergraded in current chemotherapies and radiotherapies to treat many types of cancers.
葫芦素是高度氧化的四环三萜类化合物,广泛存在于传统中药(葫芦科)中,具有很强的抗癌活性,分为从A到T的12类,有200多种衍生物。八种对癌症最具活性的葫芦素成分是葫芦素B、D、E、I、IIa、L糖苷、Q和R。它们的作用机制包括抗增殖、抑制迁移和侵袭、促凋亡以及促进细胞周期停滞。葫芦素还被发现是JAK-STAT3、Wnt、PI3K/Akt和MAPK信号通路的抑制剂,这些信号通路在癌细胞的凋亡和存活中起重要作用。最近,新的研究发现将葫芦素与临床批准的化疗药物(如多西他赛和甲氨蝶呤)联合使用具有协同抗癌作用。本文总结了葫芦素抗癌特性的最新研究进展以及参与调节癌细胞增殖、死亡、侵袭和迁移的各种细胞内信号通路。因此,葫芦素是一类有前景的抗癌药物,可单独使用或整合到当前的化疗和放疗中用于治疗多种癌症。