Original Article

In vitro anti-cancer activity of chamaejasmenin B and neochamaejasmin C isolated from the root of Stellera chamaejasme L

Chong Zhang, Shuang-shuang Zhou, Lin-yi Feng, Da-yong Zhang, Neng-ming Lin, Li-huang Zhang, Jian-ping Pan, Jun-bo Wang, Jie Li
DOI: 10.1038/aps.2012.158


Chong ZHANG1, *, Shuang-shuang ZHOU1, Lin-yi FENG1, Da-yong ZHANG1, Neng-ming LIN2, Li-huang ZHANG1, Jian-ping PAN1, Jun-bo WANG1, Jie LI1, *
1School of Medicine and Life Science, Zhejiang University City College, Hangzhou 310015, China; 2Laboratory of Clinical Pharmacy, Zhejiang Cancer Hospital, Hangzhou 310022, China

Aim: To examine the anti-cancer effects of chamaejasmenin B and neochamaejasmin C, two biflavonones isolated from the root of Stellera chamaejasme L (known as the traditional Chinese herb Rui Xiang Lang Du) in vitro.

Methods: Human liver carcinoma cell lines (HepG2 and SMMC-7721), a human non-small cell lung cancer cell line (A549), human osteosarcoma cell lines (MG63, U2OS, and KHOS), a human colon cancer cell line (HCT-116) and a human cervical cancer cell line (HeLa) were used. The anti-proliferative effects of the compounds were measured using SRB cytotoxicity assay. DNA damage was detected by immunofluorescence and Western blotting. Apoptosis and cell cycle distribution were assessed using flow cytometry analysis. The expression of the related proteins was examined with Western blotting analysis.

Results: Both chamaejasmenin B and neochamaejasmin C exerted potent anti-proliferative effects in the 8 human solid tumor cell lines. Chamaejasmenin B (the IC50 values ranged from 1.08 to 10.8 μmol/L) was slightly more potent than neochamaejasmin C (the IC50 values ranged from 3.07 to 15.97 μmol/L). In the most sensitive A549 and KHOS cells, the mechanisms underlying the anti-proliferative effects were characterized. The two compounds induced prominent expression of the DNA damage marker γ-H2AX as well as apoptosis. Furthermore, treatment of the cells with the two compounds caused prominent G0/G1 phase arrest.

Conclusion: Chamaejasmenin B and neochamaejasmin C are potential anti-proliferative agents in 8 human solid tumor cell lines in vitro via inducing cell cycle arrest, apoptosis and DNA damage.

Keywords: chamaejasmenin B; neochamaejasmin C; biflavones; Stellera chamaejasme L; anticancer agent; cell cycle arrest; apoptosis; DNA damage

The authors gratefully acknowledge financial support from the Teachers Research Fund of Zhejiang University City College (J-12019 and J-12021), the Zhejiang Provincial Foundation of National Science (Y2100682, LQ12H31001, and LQ12H30003), the Science Research Foundation of Zhejiang Health Bureau (2012KYA068 and 2012KYB066), the Zhejiang Provincial Program for the Cultivation of High-level Innovative Health talents (2010-190-4), the Scientific Research Fund of Zhejiang Provincial Education Department (Y201120633) and the Student Research Fund of Zhejiang University City College (XZ2012562091 and X2012562098).
* To whom correspondence should be addressed.
E-mail lijie@zucc.edu.cn (Jie LI); zhangchong@zucc.edu.cn (Chong ZHANG)
Received 2012-07-12 Accepted 2012-09-24

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