RESUMEN
We studied Phellinus lonicerinus to determine the cytotoxic effect and the dual estrogenic activities of methyl-hispolon and their relation to estrogen signals in vivo and in vitro. The Glide scores of methyl-hispolon-estrogen receptor α (ERα) and methyl-hispolon-ERß docked complexes were -7.29 kcal/mol and -6.68 kcal/mol in docking simulations. Methyl-hispolon had a significant antiproliferative effect for estrogen-sensitive ER(+) MCF-7 cells in the absence of estrogen, and it exhibited dual estrogen activities. Methyl-hispolon increased the serum E2 in rats with premature ovarian failure and fulfilled the estrogenic function in the uterus and ovary. Methyl-hispolon significantly inhibited the expression of Ras, API, ERα, C-myc, and cyclinDl, as well as their gene transcription in RL95-2 cells. The phosphorylation of ERK1/2 was inhibited by methyl-hispolon. Thus, methyl-hispolon has potential use in treating estrogen deficiency-related diseases, with good antitumor effects and estrogenic activity.
Asunto(s)
Envejecimiento Prematuro/tratamiento farmacológico , Basidiomycota/química , Catecoles/farmacología , Moduladores de los Receptores de Estrógeno/farmacología , Estrógenos/metabolismo , Sistema de Señalización de MAP Quinasas/efectos de los fármacos , Animales , Catecoles/química , Proliferación Celular/efectos de los fármacos , Moduladores de los Receptores de Estrógeno/química , Receptor alfa de Estrógeno/metabolismo , Receptor beta de Estrógeno/metabolismo , Femenino , Terapia de Reemplazo de Hormonas , Humanos , Células MCF-7 , Simulación del Acoplamiento Molecular , Ovario/efectos de los fármacos , Fosforilación , Fitoestrógenos/metabolismo , Ratas , Ratas Sprague-Dawley , Útero/efectos de los fármacosRESUMEN
OBJECTIVE: To screen out fungus strains with acetylcholinesterase inhibitory activity from Huperzia serrata. METHOD: Endophytic fungi fermentation products from 59 H. serrata strains were stained with acetylcholinesterase hydrolyzed alpha-naphthaleneacetic ethyl ester and fast blue B salt, and screened for acetylcholinesterase inhibitory activity with thin-layer chromatography-bioautography. Target strains were classified and identified through the sequence analysis on 18s rDNA and 5.8s rDNA combined with morphological characteristics. RESULT: Fungus strain LQ2F01 from H. serrata showed positive color reaction in the screening for acetylcholinesterase inhibitory activity. The sequence analysis on 18s rDNA and 5.8s rDNA combined with morphological characteristics showed the strain LQ2F01 belonged to Acremonium. CONCLUSION: Endophytic Fungi LQ2F01 from H. serrata shows identical acetylcholinesterase inhibitory activity with the host plant, which is of great significance to the development of natural medicines and the studies on the relationship between the endophytic gungi and the host plant.
Asunto(s)
Acetilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/metabolismo , Hongos/metabolismo , Huperzia/microbiología , Acremonium/genética , Acremonium/metabolismo , Inhibidores de la Colinesterasa/aislamiento & purificación , Cromatografía en Capa Delgada , ADN de Hongos/química , ADN de Hongos/genética , ADN Ribosómico/química , ADN Ribosómico/genética , Compuestos de Diazonio/metabolismo , Hongos/clasificación , Hongos/genética , Hidrólisis , Ácidos Naftalenoacéticos/metabolismo , Filogenia , ARN Ribosómico 18S/clasificación , ARN Ribosómico 18S/genética , ARN Ribosómico 5.8S/clasificación , ARN Ribosómico 5.8S/genética , Análisis de Secuencia de ADNRESUMEN
OBJECTIVE: The purpose of study was to discover the phylogenetic relations and plant barcoding of 17 plants from Huperziaceae. METHODS: Phylogenetic tree of chloroplast trnH-psbA gene of 17 plants from Huperziaceae was constructed by software. RESULTS: It showed that Huperziaceae could be divided into two genera Huperzia and Phlegmariurus and bootstrap value reached 91%. CONCLUSIONS: Holub and Qing' taxonomy was supported and 17 species in Huperziaceae were monophyletic groups and it suggested that trnH-psbA could be used as a DNA barcode to identify plants.