An article Synthesis, biological evaluation and mechanism studies of C-23 modified 23-hydroxybetulinic acid derivatives as anticancer agents WOS:000496896600061 published article about IN-VITRO; ANTITUMOR-ACTIVITY; BETULINIC ACID; APOPTOSIS; CANCER in [Lu, Lixue; Zhang, Hengyuan; Liu, Yang; Wang, Yiwei; Xu, Shengtao; Xu, Jinyi] China Pharmaceut Univ, State Key Lab Nat Med, 24 Tong Jia Xiang, Nanjing 210009, Jiangsu, Peoples R China; [Lu, Lixue; Zhang, Hengyuan; Liu, Yang; Wang, Yiwei; Xu, Shengtao; Xu, Jinyi] China Pharmaceut Univ, Dept Med Chem, 24 Tong Jia Xiang, Nanjing 210009, Jiangsu, Peoples R China; [Lu, Lixue; Liu, Jie] China Pharmaceut Univ, Dept Organ Chem, 24 Tong Jia Xiang, Nanjing 210009, Jiangsu, Peoples R China; [Zhu, Zheying] Univ Nottingham, Sch Pharm, Div Mol Therapeut & Formulat, Univ Pk Campus, Nottingham NG7 2RD, England in 2019, Cited 18. Recommanded Product: 4-Nitrobenzoic acid. The Name is 4-Nitrobenzoic acid. Through research, I have a further understanding and discovery of 62-23-7
A series of C-23 modified 23-hydroxybetulinic acid (HBA) derivatives were synthesized and evaluated for their antiproliferative activity against a panel of cancer cell lines (A2780, A375, B16, MCF-7 and HepG2). The biological screening results showed that most of the derivatives exhibited more potent antiproliferative activity than HBA, and compound 6e exhibited the most potent activity with IC50 values of 2.14 mu M, 2.89 mu M, and 3.97 mu M against A2780, B16, and MCF-7 cells, respectively. Further anticancer mechanism studies revealed that compound 6e induced the generation of intracellular reactive oxygen species (ROS) and reduction of mitochondrial membrane potential (MMP) of B16 cells in a dose-dependent manner. Moreover, western blot analysis indicated that compound 6e downregulated the expression of anti-apoptotic protein Bcl-2 and upregulated the expression of proapoptotic protein Bax, activation of caspase 3 to induce cell apoptosis. Meanwhile, compound 6e significantly inhibited the phosphorylation of MEK, ERK, and Akt without affecting the expression of MEK, ERK, and Akt. Furthermore, the in vivo anti-tumor activity of 6e was validated (tumor inhibitory ratio of 68.4% at the dose of 30 mg/kg) in mice with B16 melanoma. (C) 2019 Elsevier Masson SAS. All rights reserved.
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