C21 steroidal glycosides from Cynanchum stauntonii induce apoptosis in HepG2 cells

Zhi-Qi Yin; Shu-Le Yu; Yu-Jian Wei; Lin Ma; Zheng-Feng Wu; Lei Wang; Qing-Wen Zhang; Ming Zhao; Wen-Cai Ye; Chun-Tao Che; Jian Zhang

doi:10.1016/j.steroids.2015.12.008

C21 steroidal glycosides from Cynanchum stauntonii induce apoptosis in HepG2 cells

Steroids. 2016 Feb:106:55-61. doi: 10.1016/j.steroids.2015.12.008. Epub 2015 Dec 19.

Authors

Zhi-Qi Yin¹, Shu-Le Yu², Yu-Jian Wei³, Lin Ma², Zheng-Feng Wu², Lei Wang⁴, Qing-Wen Zhang⁵, Ming Zhao⁶, Wen-Cai Ye⁴, Chun-Tao Che⁶, Jian Zhang⁷

Affiliations

¹ Department of Natural Medicinal Chemistry & State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China. Electronic address: [email protected].
² Department of Natural Medicinal Chemistry & State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China; Laboratory of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, China.
³ The First Clinical Medical Institute, Nanjing Medical University, Nanjing 210000, China.
⁴ Institute of Traditional Chinese Medicine and Natural Products & Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drugs Research, Jinan University, Guangzhou 510632, China.
⁵ State Key Laboratory of Quality Research in Chinese Medicine and Institute of Chinese Medical Sciences, University of Macau, Macao SAR, China.
⁶ Department of Medicinal Chemistry and Pharmacognosy, and WHO Collaborating Center for Tradition Medicine, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA.
⁷ Laboratory of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, China. Electronic address: [email protected].

PMID: 26708267
DOI: 10.1016/j.steroids.2015.12.008

Abstract

Two new (1-2) and three known (3-5) C21 steroidal glycosides were isolated from Cynanchum stauntonii. Their structures were elucidated on the basis of 1D and 2D-NMR spectroscopic data as well as HRTOFMS analysis. The cytotoxicity of the compounds against A549, HepG2, and 4T1 cell lines were evaluated by MTT assay. Compound 4 exhibited good inhibitory activities with the IC50 values 26.82, 12.24, and 44.12 μM, respectively. Furthermore, compound 4 could induce G1 phase arrest, upregulate the expression levels of caspases-3, -9, and Bax, and downregulate the expression level of Bcl-2. These results indicated that compound 4 might be valuable to anticancer drug candidates.

Keywords: Apoptosis; C(21) steroidal glycoside; Caspase; Cynanchum stauntonii.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antineoplastic Agents, Phytogenic / chemistry*
Antineoplastic Agents, Phytogenic / isolation & purification
Antineoplastic Agents, Phytogenic / pharmacology*
Apoptosis / drug effects*
Cell Line, Tumor
Cynanchum / chemistry*
G1 Phase Cell Cycle Checkpoints / drug effects
Glycosides / chemistry*
Glycosides / isolation & purification
Glycosides / pharmacology*
Hep G2 Cells
Humans
Rats
Steroids / chemistry*

Substances

Antineoplastic Agents, Phytogenic
Glycosides
Steroids