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1.
Org Lett ; 26(27): 5695-5699, 2024 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-38912656

RESUMO

One rare stephacidin-asperochratide hybrid, stephaochratidin A (1), was isolated from the deep-sea-derived Aspergillus ochraceus MCCC 3A00521. The relative structure of 1 was determined by comprehensive analyses of its 1D and 2D NMR data as well as HRESIMS data. And the absolute configuration was unambiguously assigned by ECD calculations and the X-ray single-crystal diffraction analysis. Plausible biosynthetic pathway of 1 was proposed. Stephaochratidin A (1) exhibited significant ferroptosis inhibitory activity with the EC50 value of 15.4 µM by downregulating HMOX-1 expression and lipid peroxidation.


Assuntos
Aspergillus ochraceus , Ferroptose , Ferroptose/efeitos dos fármacos , Estrutura Molecular , Aspergillus ochraceus/química , Humanos , Peroxidação de Lipídeos/efeitos dos fármacos
2.
Bioorg Med Chem Lett ; 23(23): 6421-6, 2013 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-24120543

RESUMO

In the present study, andrographolide (Andro, 1) derivatives were screened to identify potent inhibitors against tumor-cell migration and invasion, and associated structure-activity relationships were studied. Compared to 1, compounds 8a-8d exhibited more potent activities against migration in SGC-7901, PC-3, A549, HT-29 and Ec109 cell lines. Improved activities against tumor-cell migration and invasion were proved to be associated with the down-regulation of MMPs.


Assuntos
Movimento Celular/efeitos dos fármacos , Diterpenos/química , Diterpenos/farmacologia , Neoplasias/tratamento farmacológico , Proliferação de Células/efeitos dos fármacos , Diterpenos/síntese química , Ensaios de Seleção de Medicamentos Antitumorais , Células HT29 , Humanos , Neoplasias/patologia , Relação Estrutura-Atividade
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