Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 2 de 2
Filtrar
Adicionar filtros








Intervalo de ano
1.
China Journal of Chinese Materia Medica ; (24): 1076-1081, 2020.
Artigo em Chinês | WPRIM | ID: wpr-1008475

RESUMO

To prepare the herpetolide A nanosuspension lyophilized powder(HPA-NS-LP), in order to investigate its anti-hepatitis B virus(HBV) activity and the dissolution in vitro. Herpetolide A nanosuspension(HPA-NS) was prepared by ultrasonic precipitation method. The formulation and process of HPA-NS were optimized by the single factor experiment. Lyophilized powder(HPA-NS-LP) was prepared by freeze-drying method. Scanning electron microscopy was used to observe morphology of HPA-NS-LP. Paddle method was used to determinate the dissolution of HPT-NS-LP in vitro. The anti-HBV activity of herpetolide A coarse suspension lyophilized powder(HPA-CS-LP) and HPA-NS-LP was evaluated by HepG2.2.15 cell model. The mean particle size of optimized HPA-NS was(173.46±4.36) nm, with a polydispersity index of 0.110±0.012. After redispersion, the mean particle size and the polydispersity index of HPA-NS-LP increased, with changes within a rational range. Scanning electron microscopy showed that HPA-NS-LP was spherical in shape. Cumulative dissolution rate of HPA-NS-LP was more than 90% in 2 hours, which was higher than that of HPA-CS-LP. Both HPA-CS-LP and HPA-NS-LP could effectively inhibit the secretion of HepG2.2.15 cell antigens(HBsAg and HBeAg), and the inhibitory effect of HPA-NS-LP was significantly higher than that of HPA CS-LP(P<0.05). HBV-DNA test showed that high, medium and low-dose HPA-NS-LP(50, 25, 12.5 mg·kg~(-1)) significantly decreased the level of HBV-DNA(P<0.05), and the effect was better than that of the same dose of HPA-CS-LP(P<0.05). The results revealed that HPA-NS-LP exhibited anti-HBV activity in vitro, and its effect was superior to that of HPA-CS-LP.


Assuntos
Humanos , Cumarínicos/farmacologia , Cucurbitaceae/química , Células Hep G2 , Vírus da Hepatite B/efeitos dos fármacos , Nanopartículas , Tamanho da Partícula , Compostos Fitoquímicos/farmacologia , Solubilidade , Suspensões
2.
Acta Pharmaceutica Sinica ; (12): 1140-1145, 2017.
Artigo em Chinês | WPRIM | ID: wpr-779705

RESUMO

In this study, eleven containing gallic acid moiety derivatives of Matijin-Su(MTS)were synthesized and evaluated for their anti-HBV activities in HepG2 2.2.15 cells in an effort to find novel effective anti-hepatitis B virus(HBV)agents. Compounds 5c, 6c and 6d exhibited significant anti-HBV activity with IC50 values of 6.12, 8.44 and 9.86 μmol·L-1, respectively. Incorporation of gallic acid moiety into MTS derivatives can lead to profound changes in their anti-HBV activity, and could be worth of further research.

SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA