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Four new cycloartane triterpenes, named gardenoins E-H (1-4), were isolated from the apical buds of Gardenia obtusifolia, together with five known cycloartanes. Only compound 1 displayed cytotoxicity against colon, hepatic and lung cancer cell lines. 相似文献
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Zongwei Yue Hiu C. Lam Kaiqi Chen Ittipon Siridechakorn Yaxi Liu Khanitha Pudhom Xiaoguang Lei 《Angewandte Chemie (International ed. in English)》2020,59(10):4115-4120
The rhytidenone family comprises spirobisnaphthalene natural products isolated from the mangrove endophytic fungus Rhytidhysteron rufulum AS21B. The biomimetic synthesis of rhytidenone A was achieved by a Michael reaction/aldol/lactonization cascade in a single step from the proposed biosynthetic precursor rhytidenone F. Moreover, the mode of action of the highly cytotoxic rhytidenone F was investigated. The pulldown assay coupled with mass spectrometry analysis revealed the target protein PA28γ is covalently attached to rhytidenone F at the Cys92 residue. The interactions of rhytidenone F with PA28γ lead to the accumulation of p53, which is an essential tumor suppressor in humans. Consequently, the Fas‐dependent signaling pathway is activated to initiate cellular apoptosis. These studies have identified the first small‐molecule inhibitor targeting PA28γ, suggesting rhytidenone F may serve as a promising natural product lead for future anticancer drug development. 相似文献
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Zongwei Yue Dr. Hiu C. Lam Kaiqi Chen Dr. Ittipon Siridechakorn Yaxi Liu Prof. Dr. Khanitha Pudhom Prof. Dr. Xiaoguang Lei 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2020,132(10):4144-4149
The rhytidenone family comprises spirobisnaphthalene natural products isolated from the mangrove endophytic fungus Rhytidhysteron rufulum AS21B. The biomimetic synthesis of rhytidenone A was achieved by a Michael reaction/aldol/lactonization cascade in a single step from the proposed biosynthetic precursor rhytidenone F. Moreover, the mode of action of the highly cytotoxic rhytidenone F was investigated. The pulldown assay coupled with mass spectrometry analysis revealed the target protein PA28γ is covalently attached to rhytidenone F at the Cys92 residue. The interactions of rhytidenone F with PA28γ lead to the accumulation of p53, which is an essential tumor suppressor in humans. Consequently, the Fas-dependent signaling pathway is activated to initiate cellular apoptosis. These studies have identified the first small-molecule inhibitor targeting PA28γ, suggesting rhytidenone F may serve as a promising natural product lead for future anticancer drug development. 相似文献
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