TY - JOUR
T1 - Structure identification and in vitro anticancer activity of lathyrol-3-phenylacetate-5,15-diacetate
AU - Zhang, Jian Ye
AU - Huang, Wen Jing
AU - Sun, Hong Mei
AU - Liu, Yun
AU - Zhao, Xiao Qin
AU - Tang, Si Li
AU - Sun, Ming Na
AU - Wang, Sheng
AU - Li, Jia Jun
AU - Zhang, Ling Ling
AU - Zhou, Jun Hua
AU - Pan, Qian Rong
AU - Chen, Hubiao
N1 - Funding Information:
Acknowledgments: The work was supported by National Natural Science Foundation of China (81473320), Fund of Guangdong Science and Technology Department (2016A020226024), Fund of Guangdong Education Department (2015KTSCX112), Fund of Guangzhou Science and Technology Program (201707010048), Fund of Traditional Chinese Medicine Bureau of Guangdong Province (20161181) and Research Fund of undergraduates from Guangzhou Medical University.
PY - 2017/9
Y1 - 2017/9
N2 - Natural products fromthe genus Euphorbia showattention-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 (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 IC50 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 (δΨm), 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.
AB - Natural products fromthe genus Euphorbia showattention-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 (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 IC50 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 (δΨm), 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.
KW - Apoptosis
KW - Caper Euphorbia Seed
KW - Diterpenoids
KW - Lathyrol-3-phenylacetate-5,15-diacetate
KW - Lung cancer
KW - Natural products
UR - http://www.scopus.com/inward/record.url?scp=85029665691&partnerID=8YFLogxK
U2 - 10.3390/molecules22091412
DO - 10.3390/molecules22091412
M3 - Journal article
C2 - 28841191
AN - SCOPUS:85029665691
SN - 1420-3049
VL - 22
JO - Molecules
JF - Molecules
IS - 9
M1 - 1412
ER -
