2026-09-13T15:18:33Zhttps://buleria.unileon.es/server/oai/request

oai:buleria.unileon.es:10612/191022026-07-24T01:01:38Zcom_10612_17col_10612_18

Microbiologia Barúa Chamorro, Javier E. Cruz Moreno, Mercedes de la Pedro, Nuria de Cautain, Bastien Hermosa, Rosa Cardoza Silva, Rosa Elena Gutiérrez Martín, Santiago 1965- Monte Vázquez, Enrique Vicente Pérez, María Francisca González Collado, Isidro [EN] Trichothecene mycotoxins are recognized as highly bioactive compounds that can be used in the design of new useful bioactive molecules. In Trichoderma brevicompactum, the first specific step in trichothecene biosynthesis is carried out by a terpene cyclase, trichodiene synthase, that catalyzes the conversion of farnesyl diphosphate to trichodiene and is encoded by the tri5 gene. Overexpression of tri5 resulted in increased levels of trichodermin, a trichothecene-type toxin, which is a valuable tool in preparing new molecules with a trichothecene skeleton. In this work, we developed the hemisynthesis of trichodermin and trichodermol derivatives in order to evaluate their antimicrobial and cytotoxic activities and to study the chemo-modulation of their bioactivity. Some derivatives with a short chain at the C-4 position displayed selective antimicrobial activity against Candida albicans and they showed MIC values similar to those displayed by trichodermin. It is important to highlight the cytotoxic selectivity observed for compounds 9, 13, and 15, which presented average IC50 values of 2 µg/mL and were cytotoxic against tumorigenic cell line MCF-7 (breast carcinoma) and not against Fa2N4 (non-tumoral immortalized human hepatocytes) https://hdl.handle.net/10612/19102 spa MDPI Synthesis of Trichodermin Derivatives and Their Antimicrobial and Cytotoxic Activities info:eu-repo/semantics/article TEXT BULERIA. Repositorio Institucional de la Universidad de León Hispana