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Chem Pharm Bull (Tokyo) ; 72(7): 693-699, 2024.
Article in English | MEDLINE | ID: mdl-39048375

ABSTRACT

This study evaluated the ability of isolated or semisynthesized trichothecene sesquiterpenes to prevent cancer emergence and proliferation and inhibit signal transducer and activator of transcription-3 (STAT3) phosphorylation through in vitro assays. Trichothecinol A (TTC-A), which bears a hydroxy group at C3, exhibited greater cancer prevention, antiproliferation, and STAT3 phosphorylation inhibition effects than trichothecin (TTC), which lacks a hydroxy group at C3. Furthermore, trichothecinol B (TTC-B), which is a reduced derivative of TTC and has similar cytotoxic effect, showed substantially weaker chemoprotection and STAT3 phosphorylation inhibition effects than TTC. These results clearly indicate that the hydroxy group at C3 and carbonyl group at C8 are crucial for inducing both potent chemoprevention and STAT3 phosphorylation inhibition.


Subject(s)
Cell Proliferation , STAT3 Transcription Factor , Trichothecenes , STAT3 Transcription Factor/antagonists & inhibitors , STAT3 Transcription Factor/metabolism , Trichothecenes/chemistry , Trichothecenes/pharmacology , Trichothecenes/antagonists & inhibitors , Humans , Cell Proliferation/drug effects , Structure-Activity Relationship , Phosphorylation/drug effects , Cell Line, Tumor , Molecular Structure , Drug Screening Assays, Antitumor , Dose-Response Relationship, Drug , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry
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