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

• Published in: Acta pharmacologica Sinica Vol. 34; no. 2; pp. 262 - 270
• Main Authors: Zhang, Chong, Zhou, Shuang-shuang, Feng, Lin-yi, Zhang, Da-yong, Lin, Neng-ming, Zhang, Li-huang, Pan, Jian-ping, Wang, Jun-bo, Li, Jie
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 01.02.2013; Nature Publishing Group
• Subjects: Antineoplastic Agents, Phytogenic - isolation & purification; Antineoplastic Agents, Phytogenic - pharmacology; Apoptosis - drug effects; Biomedical and Life Sciences; Biomedicine; blot分析; Cell Cycle Checkpoints - drug effects; Cell Line, Tumor; Cell Proliferation - drug effects; DNA Damage - drug effects; DNA损伤; Humans; Immunology; Internal Medicine; Medical Microbiology; Neoplasms - drug therapy; Neoplasms - genetics; Neoplasms - pathology; Original; original-article; Pharmacology/Toxicology; Plant Roots - chemistry; Thymelaeaceae - chemistry; Vaccine; Western印迹法; 人肝癌细胞株; 体外分离; 抗肿瘤活性; 瑞香狼毒; 非小细胞肺癌; chamaejasmenin B; neochamaejasmin C; DNA damage; apoptosis; L; cell cycle arrest; anticancer agent; biflavones
• ISSN: 1671-4083; 1745-7254; 1745-7254
• DOI: 10.1038/aps.2012.158

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, U20S, 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 ICso values ranged from 1.08 to 10.8 μmol/L） was slightly more potent than neochamaejasmin C （the IC5o 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 -H2AX as well as apoptosis. Furthermore, treatment of the cells with the two compounds caused prominent Go/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.