Synthesis and in vitro antitumor evaluation of betulin acid ester derivatives as novel apoptosis inducers

Eur J Med Chem. 2015 Sep 18:102:249-55. doi: 10.1016/j.ejmech.2015.08.004.

Sheng-Jie Yang ¹, Ming-Chuan Liu ¹, Hong-Mei Xiang ², Qi Zhao ², Wei Xue ², Song Yang ³

Affiliations

1 State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China; Sinphar Tian-Li Pharmaceutical Co., LTD, Hangzhou 311100, PR China.
2 State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China.
3 State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China. Electronic address: jhzx.msm@gmail.com.

PMID: 26280921 DOI: 10.1016/j.ejmech.2015.08.004

Abstract

Nineteen betulin derivatives modified at the C-3 and C-28 positions were synthesized and assessed for antitumor activities against the MGC-803, PC3, Bcap-37, A375, and MCF-7 human Cancer cell lines in vitro by MTT assay. Some derivatives (compounds 3a-3d and 5) displayed strong antitumor properties, with IC50 values between 4 and 18 μM. Compound 3c, containing piperidine group at C-28 position, had IC50 values of 4.3, 4.5, 5.2, 7.5, and 5.2 μM on the five Cancer cell lines, respectively. Subsequent fluorescence staining and flow cytometric analysis indicated that compound 3c induced Apoptosis in MGC-803 cell line, with an Apoptosis ratio of 31.11% after 36 h of treatment at 10 μM 3c.

Keywords

Antitumor; Apoptosis; Betulin derivatives; Cancer cells; Synthesis.

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