Structure Identification and In Vitro Anticancer Activity of Lathyrol-3-phenylacetate-5,15-diacetate

Jian-ye Zhang, Wen-jing Huang, Hong-mei Sun, Yun Liu, Xiao-qin Zhao, Si-li Tang, Ming-na Sun, Sheng Wang, Jia-jun Li, Ling-ling Zhang, Jun-hua Zhou, Qian-rong Pan (+1 others)
2017 Molecules  
Natural products from the genus Euphorbia show attention-attracting activities, such as anticancer activity. In this article, classical isolation and structure identification were used in a study on Caper Euphorbia Seed. Subsequently, MTT and wound healing assays, flow cytometry, western blotting, Hoechst 33258 staining and fluorescence microscopy examination were applied to investigate the anticancer activity of the obtained compounds. In a result, lathyrol-3-phenyl-acetate-5,15-diacetate
more » ... 5,15-diacetate (deoxy Euphorbia factor L1, DEFL1) was isolated from Caper Euphorbia Seed. Moreover, the NMR signals were totally assigned. DEFL1 showed potent inhibition against lung cancer A549 cells, with an IC 50 value of 17.51 ± 0.85 µM. Furthermore, DEFL1 suppressed wound healing of A549 cells in a concentration-dependent manner. Mechanically, DEFL1 induced apoptosis, with involvement of an increase of reactive oxygen species (ROS), decrease of mitochondrial membrane potential (∆Ψm), release of cytochrome c, activity raise of caspase-9 and 3. Characteristic features of apoptosis were observed by fluorescence microscopy. In summary, DEFL1 inhibited growth and induced apoptosis in lung cancer A549 cells via a mitochondrial pathway. performed the experiments; Ming-na Sun, Sheng Wang, Jia-jun Li and Ling-ling Zhang analyzed the data; Jun-hua Zhou and Qian-rong Pan contributed analysis tools; Wen-jing Huang and Jian-ye Zhang wrote the paper. Conflicts of Interest: The authors declare no conflict of interest.
doi:10.3390/molecules22091412 pmid:28841191 fatcat:usj7c7kdi5gi5bjkz3q2g5nip4