2. Academic Validation
  3. Synthesis and biological evaluation of betulonic acid derivatives as antitumor agents

Synthesis and biological evaluation of betulonic acid derivatives as antitumor agents

  • Eur J Med Chem. 2015;96:58-65. doi: 10.1016/j.ejmech.2015.04.006.
Sheng-Jie Yang 1,  Ming-Chuan Liu 2,  Qi Zhao 3,  De-Yu Hu 3,  Wei Xue 3,  Song Yang 4
Affiliations

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; Research Institute, Sinphar Tian-Li Pharmaceutical Co., Ltd, Hangzhou 311100, PR China; Research Institute of Traditional Chinese Medicine, Yangtze River Pharmaceutical Group Co., Ltd, Taizhou 225321, 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; Research Institute, Sinphar Tian-Li Pharmaceutical Co., Ltd, Hangzhou 311100, 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.
  • 4 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: 25874331 DOI: 10.1016/j.ejmech.2015.04.006
Abstract

Structural modification was performed at the C-28 position of betulonic acid (BetA). Twenty-five BetA derivatives were synthesized, and evaluated for their antitumor activities against MGC-803, PC3, Bcap-37, A375, and MCF-7 human Cancer cell lines by MTT assay. Among the derivatives, most of the derivatives had significant antiproliferative ability (IC50 < 19 μM). Compound 3k, the most active compound, showed IC50 values of 3.6, 5.6, 4.2, 7.8, and 5.2 μM on the five Cancer cell lines respectively, and was selected to investigate cell Apoptosis by subsequent florescence staining and flow cytometry analysis. The results revealed that compound 3k could induce Apoptosis in MGC-803 cell lines, and the Apoptosis ratios reached 28.33% after 36 h of treatment at 10 μM. In addition, the study of Cancer cell apoptotic signaling pathway indicated that the Apoptosis of MGC-803 cells induced by compound 3k could be through the mitochondrial intrinsic pathway.

Keywords

Antitumor; Apoptosis; Betulonic acid derivatives; Mitochondrial pathway; Synthesis.

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