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Vol. 25 No. 9 (2013): Vol 25 Issue 9

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Synthesis and Antitumor Evaluation of One Novel Tetramethylpyrazine-Rhein Derivative

https://doi.org/10.14233/ajchem.2013.14135
Peng-Long Wang
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, P.R. China
Ya-Tao Cheng
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, P.R. China
Kuo Xu
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, P.R. China
Ya-Wen An
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, P.R. China
Wei Wang
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, P.R. China
Qu-Sheng Li
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, P.R. China
Qiu-Jun Han
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, P.R. China
Qiang Li
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, P.R. China
Hong-Gui Zhang
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, P.R. China
Hai-Min Lei
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, P.R. China

Corresponding Author(s) : Hai-Min Lei

hm_lei@yahoo.cn

Asian Journal of Chemistry, Vol. 25 No. 9 (2013): Vol 25 Issue 9

Abstract

To discover multi-effective and low toxic anticancer lead compound from traditional Chinese medicine prescription, we synthesized one novel tetramethylpyrazine-rhein derivative which was composed of two main antitumor ingredients of Huazhenghuisheng Pian. The design idea was enlightened by "combination principle" in drug discovery and "compatibility principle" in traditional Chinese medicine. Compound 5's antitumor activity was evaluated by human cancer cell Bel-7402, while the angiogenesis activity was valued by the chick chorioallantoic membrane (CAM) assays. The stability test was carried on artificial gastric juice and artificial intestinal juice; furthermore, compound 5's acute toxicity was evaluated in vivo. The results showed that compound 5 not only displayed antiproliferative activity on Bel-7402 cell (IC50 = 26.4 μM), but also dramatically suppressed normal angiogenesis in chick chorioallantoic membrane. And there was no hydrolysis or structural damage during 24 h in artificial digestive solution. The LD50 value of the compound 5 exceeded 3.2 g/kg by oral administration in mice.

Keywords

Angiogenesis Antitumor Combination principles Tetramethylpyrazine-rhein derivative Multi-effective Low toxicity TCM
Wang, P.-L., Cheng, Y.-T., Xu, K., An, Y.-W., Wang, W., Li, Q.-S., … Lei, H.-M. (2013). Synthesis and Antitumor Evaluation of One Novel Tetramethylpyrazine-Rhein Derivative. Asian Journal of Chemistry, 25(9), 4885–4888. https://doi.org/10.14233/ajchem.2013.14135
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