UM
Shikonin derivative DMAKO-05 inhibits akt signal activation and melanoma proliferation
Yang Y.-Y.3; He H.-Q.3; Cui J.-H.3; Nie Y.-J.3; Wu Y.-X.3; Wang R.1; Wang G.2; Zheng J.-N.2; Ye R.D.3; Wu Q.1; Li S.-S.3; Qian F.3
2016-06-01
Source PublicationChemical Biology and Drug Design
ISSN17470285 17470277
Volume87Issue:6Pages:895-904
AbstractDMAKO-05((S)-1-((5E,8E)-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. The novel oxime derivative of shikonin DMAKO-05 was found toxic to melanoma cell B16F0. DMAKO-05 remarkably inhibited the phosphorylation of Akt, induced G1 cell cycle arrest, and promoted B16F0 melanoma cell apoptosis. DMAKO-05 might serve as a potential inhibitor for melanoma.
Keywordapoptosis cell cycle arrest cytotoxicity DMAKO-05 melanoma cell B16F0 shikonin
DOI10.1111/cbdd.12722
URLView the original
Language英語
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Cited Times [WOS]:10   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.Bengbu Medical College
2.XuZhou Medical University
3.Shanghai Jiao Tong University
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Yang Y.-Y.,He H.-Q.,Cui J.-H.,et al. Shikonin derivative DMAKO-05 inhibits akt signal activation and melanoma proliferation[J]. Chemical Biology and Drug Design,2016,87(6):895-904.
APA Yang Y.-Y..,He H.-Q..,Cui J.-H..,Nie Y.-J..,Wu Y.-X..,...&Qian F..(2016).Shikonin derivative DMAKO-05 inhibits akt signal activation and melanoma proliferation.Chemical Biology and Drug Design,87(6),895-904.
MLA Yang Y.-Y.,et al."Shikonin derivative DMAKO-05 inhibits akt signal activation and melanoma proliferation".Chemical Biology and Drug Design 87.6(2016):895-904.
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