Maneenet Juthamart, Omar Ashraf M, Sun Sijia, Kim Min Jo, Daodee Supawadee, Monthakantirat Orawon, Boonyarat Chantana, Chulikhit Yaowared, Awale Suresh
Natural Drug Discovery Laboratory, Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama, Japan.
Graduate School of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, Thailand.
Z Naturforsch C J Biosci. 2021 May 24;76(9-10):401-406. doi: 10.1515/znc-2020-0304. Print 2021 Sep 27.
Ethanolic extract of petals showed preferential cytotoxic activity against HeLa human cervical cancer cell line with a PC value of 10.4 μg/mL. This active extract was subjected to a phytochemical investigation study which led to the isolation of nine benzylisoquinoline alkaloids (-). The isolated compounds exhibited potent antiausterity activities. Moreover, under nutrient-deprived conditions, (-)-lirinidine () induced remarkable alterations in HeLa cell morphology including cell shrinkage and plasma blebbing leading to total cell death within 10 h. Mechanistically, was found to inhibit Akt/mTOR signaling pathway. It also induced apoptosis by promoting caspase-3 activation and inhibiting Bcl-2 expression. Therefore, benzylisoquinoline alkaloids skeleton can be considered as a promising scaffold for the anticancer drug development against cervical cancer.
花瓣的乙醇提取物对人宫颈癌HeLa细胞系显示出优先的细胞毒性活性，PC值为10.4μg/mL。对该活性提取物进行了植物化学研究，从中分离出九种苄基异喹啉生物碱（-）。分离出的化合物表现出强大的抗紧缩活性。此外，在营养缺乏的条件下，（-）-去甲乌药碱（）引起HeLa细胞形态的显著变化，包括细胞收缩和质膜起泡，导致10小时内细胞全部死亡。从机制上讲，发现其抑制Akt/mTOR信号通路。它还通过促进caspase-3激活和抑制Bcl-2表达来诱导细胞凋亡。因此，苄基异喹啉生物碱骨架可被视为开发抗宫颈癌抗癌药物的有前景的支架。
