RESUMEN
Five caffeoyl phenylethanoid glycosides, including two new ones linderruelliosides A (1) and B (2), were isolated from the leaves and stems of Lindernia ruellioides. Their structures were elucidated on the basis of spectroscopic methods, including extensive NMR and MS spectra. In addition, all these compounds were tested for their anti-HBV activity. Compounds 1, 3, and 4 showed anti-HBV activities, with IC50 values of 54.87, 30.74, and 69.02 µM for HBsAg and 26.70, 5.17, and 7.08 µM for HBeAg, respectively.
Asunto(s)
Antivirales/farmacología , Virus de la Hepatitis B/efectos de los fármacos , Scrophulariaceae/química , Antivirales/química , Línea Celular , China , Antígenos de Superficie de la Hepatitis B/análisis , Humanos , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Estructura Molecular , Extractos Vegetales/química , Espectrometría de Masa por Ionización de Electrospray , Espectrofotometría Infrarroja , Espectrofotometría UltravioletaRESUMEN
Twenty-eight protostane triterpenoids, including a new degraded one (1), nine new ones (2 - 10), and two new natural ones (11 and 12), have been isolated from the dried rhizomes of Alisma orientale. Alisol R (1) was the first 20,21,22,23,24,25,26,27-octanorprotostane triterpenoid. The absolute configurations of 25-methoxyalisol F (2) and 16ß-hydroperoxyalisol B 23-acetate (3) were determined by X-ray diffraction analysis. In addition, alismaketone-B 23-acetate (28) showed potent vasorelaxant activity on endothelium-intact thoracic aorta rings precontracted with KCl.
Asunto(s)
Alisma/química , Terpenos/química , 11-beta-Hidroxiesteroide Deshidrogenasas/antagonistas & inhibidores , 11-beta-Hidroxiesteroide Deshidrogenasas/metabolismo , Alisma/metabolismo , Animales , Aorta/efectos de los fármacos , Aorta/metabolismo , Humanos , Espectroscopía de Resonancia Magnética , Ratones , Conformación Molecular , Extractos Vegetales/química , Cloruro de Potasio/toxicidad , Ratas , Rizoma/química , Rizoma/metabolismo , Terpenos/metabolismo , Terpenos/farmacología , Triterpenos/química , Triterpenos/aislamiento & purificación , Triterpenos/farmacología , Vasodilatadores/química , Vasodilatadores/aislamiento & purificación , Vasodilatadores/farmacología , Difracción de Rayos XRESUMEN
Chemical constituents investigation on the seeds of Machilus yunnanensis led to two new phenolic compounds 8-O-acetyl-phenylethanoid-4-O-ß-D-glucopyranoside (1) and (E)-2,3-bis(4-hydroxyphenyl)acrylaldehyde (2), together with 16 known compounds. Their structures were elucidated on the basis of spectroscopic data analysis (IR, MS, 1D, and 2D NMR). Meanwhile, compounds 1-3, 6-13, 17, and 18 were evaluated for vasorelaxant effects on the rat endothelium-intact thoracic aorta rings precontracted with phenylephrine (PE) or KCl. The bioassay results showed that compound 17 had significant vasorelaxant effect on the endothelium-intact thoracic aorta rings precontracted with KCl.
Asunto(s)
Medicamentos Herbarios Chinos/aislamiento & purificación , Glucósidos/aislamiento & purificación , Lauraceae/química , Fenoles/aislamiento & purificación , Semillas/química , Animales , Aorta Torácica/efectos de los fármacos , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Endotelio Vascular/efectos de los fármacos , Glucósidos/química , Glucósidos/farmacología , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Fenoles/química , Fenoles/farmacología , Cloruro de Potasio/farmacología , Ratas , Vasodilatadores/aislamiento & purificación , Vasodilatadores/farmacologíaRESUMEN
OBJECTIVE: To determine the concentration of quercetin in mouse plasma by HPLC-DAD in different time after oral administration with Gualou Xiebai decoction and Gualou decoction, and to explore the influence of the compatibility of Gualou and Xiebai on pharmacokinetics of quercetin in Gualou. METHODS: The plasma sample was simply deproteinized with acetonitrile, extracted three times by aceticether, evaporated to dryness with a gentle N2 stream, dissolved with methanol and determined by HPLC. The pharmacokinetic parameters were separately calculated and compared with data processing software DAS 2. 0 and SPSS 11. 5 software. RESULTS: After oral administration with Gualou Xiebai decoction and Gualou decoction, the pharmacokinetics of quercetin in mouse plasma accorded with the two-compartment model, and t1/2α, t1/2ß, AUC0-t, AUC0-∞, Cmax, tmax, Ka, K10, K12, K21, CL/F and V1/F all had significant differences(P <0. 05 or P <0. 01). CONCLUSION: Xiebai in Gualou Xiebai decoction has a remarkable effect on pharmacokinetic character of quercetin in Gualou, it can promote the absorption and distribution and reduce the elimination of quercetin, in vivo, as well as increase the bioavailability of quercetin.