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- Title
Shikonin Derivative DMAKO-05 Inhibits Akt Signal Activation and Melanoma Proliferation.
- Authors
Yang, Yao ‐ yao; He, Hui ‐ qiong; Cui, Jia ‐ hua; Nie, Yun ‐ juan; Wu, Ya ‐ xian; Wang, Rui; Wang, Gang; Zheng, Jun ‐ Nian; Ye, Richard D.; Wu, Qiong; Li, Shao ‐ shun; Qian, Feng
- Abstract
DMAKO-05(( S)-1-((5 E,8 E)-5,8-bis(hydroxyimino)-1,4-dimethoxy-5,8-dihydronaphthalen-2-yl)-4-methylpent-3-enyl 3-methylbutanoate) is a novel oxime derivative of shikonin, the major component extracted from Chinese herb Lithospermun erythrorhizon. Here, we report that DMAKO-05 had an antitumor activity against mouse melanoma cell line B16F0. Our studies indicated that DMAKO-05 not only inhibited B16F0 proliferation and migration but also led to cell cycle arrest at G1 phase and cell apoptosis, in which DMAKO-05 triggered mitochondrial-mediated apoptosis signal including caspase-9/3 and PARP. In response to DMAKO-05 treatment, the Akt-mediated survival signals were remarkably attenuated in B16F0 cells. Collectively, DMAKO-05 has a strong cytotoxicity in B16F0 cells via inhibiting Akt activation, inducing G1 arrest, and promoting B16F0 cell apoptosis. DMAKO-05 might serve as a potential candidate lead compound for melanoma.
- Subjects
SHIKONIN; NAPHTHALENE derivatives; ISOPENTANE; MELANOMA; PROTEIN kinase B; APOPTOSIS; METHOXY compounds; CELL cycle
- Publication
Chemical Biology & Drug Design, 2016, Vol 87, Issue 6, p895
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12722