In vitro antiviral, antioxidant and in vivo antipyretic activity of three South Africa medicinal plants crude extracts / Actividad antiviral, antioxidante y antipirética in vivo de tres extractos crudos de plantas medicinales de Sudáfrica

This study investigated anti-viral, antioxidant activity and anti-pyretic of crude extract from Artemisia afra, Artemisia absinthium and Pittiosporum viridflorum leaves. The crude extracts were prepared by maceration using aqueous, methanol and dichloromethane respectively. Antiviral studies were evaluated with influenza virus using Fluorescence based - Neuraminidase inhibitors. Antioxidant activities determined with DPPH, Nitric oxide, hydroxyl and super oxide anion radicals' Anti-pyretic activities were evaluated using rats with yeast induced pyrexia. Total phenol, flavonoids, and pro-anthocyanin contents of the plants samples were evaluated using standard protocols. The crude extracts exhibited neuraminidase inhibitory activity against the influenza virus at different thresholds. Artemisia absinthiumaqueous extract showed the best activity against A/Sydney/5/97. Whereas Artemisia afra methanol crude extract displayed highest antioxidant potential against the tested antioxidant parameters. All the crude extracts significantly reversed yeast induced pyrexia in rats, similar to paracetamol. Thus, they could serve as natural remedy for respiratory diseases such as Influenza.

Este estudio investigó la actividad antiviral, antioxidante y antipirética del extracto crudo de hojas de Artemisia afra, Artemisia absinthium y Pittiosporum viridflorum. Los extractos crudos se prepararon mediante maceración utilizando metanol acuoso y diclorometano respectivamente. Los estudios antivirales se evaluaron con el virus de la influenza utilizando inhibidores de neuraminidasa basados en fluorescencia. Actividades antioxidantes determinadas con DPPH, radicales aniónicos de óxido nítrico, hidroxilo y superóxido. Las actividades antipiréticas se evaluaron utilizando ratas con pirexia inducida por levaduras. El contenido total de fenol, flavonoides y proantocianina de las muestras de plantas se evaluó utilizando protocolos estándar. Los extractos crudos mostraron actividad inhibidora de neuraminidasa contra el virus de la influenza en diferentes umbrales. El extracto acuoso de Artemisia absinthium mostró la mejor actividad contra A/Sydney/5/97. Mientras que el extracto crudo de Artemisia aframetanol mostró el mayor potencial antioxidante contra los parámetros antioxidantes probados. Todos los extractos crudos revirtieron significativamente la pirexia inducida por levaduras en ratas, similar al paracetamol. Por tanto, podrían servir como remedio natural para enfermedades respiratorias como la Influenza.

DL0410, a candidate for anti-Alzheimer disease with multiple targets in multiple pathways / 中国药理学与毒理学杂志

OBJECTIVE To find a promising candidate for anti- Alzheimer disease (AD) with multiple targets in multiple pathways. METHODS A series of classifiers were constructed for predicting the active compounds against 51 key targets toward Alzheimer disease (AD) using the multitarget-quantitative structure- activity relationships (mt- QSAR) method. While drug screening assays were established to evaluate the predicted active molecules. In addition, various cellular models and animal models related with AD were set up to further study the effects of the active compounds. RESULTS A system for the discovery of Multitarget-Directed Ligands against AD was set up and applied, the predicted active compounds were validated by the drug screening assays, and several active compounds with multiple targets were discovered. Among them, DL0410 exerted high activity on H3R, α7nAChR, AChE and ERα, also displayed the most significant effect in improving the ability of memory and learning in several AD animal models. The study on its action mechanisms showed that it's effect may partially through increasing neurotransmitter, inhibiting oxidative emergency, inhibiting the expression of APP, and promoting long- term potentiation. Besides, DL0410 is of more safety than the first- line clinical medicines. CONCLUSION DL0410 is a promising candidate for further development for AD treatment.