RESUMEN
BACKGROUND: Antrodia camphorata, a traditional Chinese medicine, is widely used in the treatment of liver diseases and cancers. Anti-inflammatory properties have also been described. HSV infection represents one of the most serious public health concerns globally because of its devastating impact. Searching for new antiviral agents, especially those with different mechanisms of action, is a crucial goal and there is an unmet need for alternative and complementary therapy against HSV infection. In this study, anti-herpes screening was performed with extracts from A. camphorata mycelia. METHODS: MTT assay, fractional inhibitory concentration index and median-effect principle were used to evaluate antiviral activity and to calculate drug combination effect. RESULTS: Crude ethanol extracts and isolated constituents showed inhibition of HSV replication at a very low concentration. Fraction A and antrodin A showed viral inhibitory effect with reduction of viral cell-to-cell spread. In addition, neither fraction A nor antrodin A showed interaction in combination with acyclovir. CONCLUSIONS: A. camphorata mycelia and antrodin A might have potential use as anti-HSV agents and are promising candidates for future antiviral drug design.
Asunto(s)
Antivirales/farmacología , Antrodia , Medicamentos Herbarios Chinos/farmacología , Herpesvirus Humano 1/efectos de los fármacos , Herpesvirus Humano 2/efectos de los fármacos , Anhídridos Maleicos/farmacología , Aciclovir/farmacología , Animales , Antivirales/química , Antivirales/aislamiento & purificación , Antrodia/química , Chlorocebus aethiops , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/aislamiento & purificación , Herpes Simple/tratamiento farmacológico , Herpes Simple/virología , Herpesvirus Humano 1/fisiología , Herpesvirus Humano 2/fisiología , Humanos , Anhídridos Maleicos/química , Anhídridos Maleicos/aislamiento & purificación , Medicina Tradicional China , Pruebas de Sensibilidad Microbiana , Micelio/química , Células Vero , Ensayo de Placa Viral , Replicación Viral/efectos de los fármacosRESUMEN
This work presents the metabolites of isocorynoxeine (ICOR), which is one of four bioactive tetracyclic oxindole alkaloids isolated from Uncaria hooks used commonly in the traditional Chinese medicines and Kampo medicines. After oral administration of 40 mg kg(-1) ICOR to rats, bile was drained and analyzed by LC-MS. Two phase I metabolites, namely 11-hydroxyisocorynoxeine (M1) and 10-hydroxyisocorynoxeine (M2), and two phase II metabolites, namely 11-hydroxyisocorynoxeine 11-O-ß-D-glucuronide (M3) and 10-hydroxyisocorynoxeine 10-O-ß-D-glucuronide (M4), were isolated from rat excreta and bile, respectively, whose structures were elucidated on the basis of CD, NMR, and MS.
