RESUMO
A new lignan, (7'R,8'R)-threo-strebluslignanol-2-O-beta-D-glucopyranoside, along with 8 known compounds (2-9) were isolated from the water-soluble part of the MeOH extract of the heartwood of Streblus asper. Their structures were elucidated through various spectroscopic methods, including 1D NMR (1H NMR, 13C NMR), 2D NMR (HMQC, HMBC, and NOESY), and HRMS. The stereochemistry at the chiral centers was determined using the CD spectrum, as well as analyses of coupling constants and optical rotation data. In the preliminary bioassay, the isolated compounds did not show anti-HBV activities in vitro using the HBV transfected HepG2.2.15 cell line.
Assuntos
Moraceae/química , Extratos Vegetais/análise , Vírus da Hepatite B/efeitos dos fármacos , Lignanas/análise , Lignanas/química , Lignanas/farmacologia , Espectroscopia de Ressonância Magnética , Solubilidade , Água/químicaRESUMO
The extracts from leaves, heartwood, barks and roots of the Streblus asper were investigated for anti-HBV activities, separately. The results suggested that the MeOH extracts of the heartwood, barks, and roots exhibited good anti-HBV activities. Further investigations displayed that ethyl acetate and n-butanol soluble parts of their MeOH extracts showed more significant anti-HBV activities. Moreover, a new lignan, together with 11 known compounds, was isolated from n-butanol-soluble part of MeOH extract of the roots of S. asper. The structures were elucidated by spectroscopic methods, including 1D NMR ((1)H NMR, (13)C NMR), 2D NMR (HMQC, HMBC) and HR-EI-MS experiments. Compounds 1-3 were evaluated for their anti-HBV activities. Honokiol showed significant anti-HBV activity with IC(50) values of 3.14µM and 4.74µM for HBsAg and HBeAg with no cytotoxicity respectively, while lamivudine (3TC, positive control) exhibited weak anti-HBV activity with IC(50) values of 11.81µM and 25.80µM for HBsAg and HBeAg respectively.
Assuntos
Antivirais/uso terapêutico , Compostos de Bifenilo/uso terapêutico , Vírus da Hepatite B/efeitos dos fármacos , Hepatite B/tratamento farmacológico , Lignanas/uso terapêutico , Moraceae/química , Fitoterapia , Extratos Vegetais/uso terapêutico , Antivirais/isolamento & purificação , Antivirais/farmacologia , Compostos de Bifenilo/isolamento & purificação , Compostos de Bifenilo/farmacologia , Células Hep G2 , Hepatite B/virologia , Humanos , Concentração Inibidora 50 , Lamivudina/isolamento & purificação , Lamivudina/farmacologia , Lignanas/isolamento & purificação , Lignanas/farmacologia , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Estruturas VegetaisRESUMO
The various fractions of the barks of Cyclocarya paliurus were systematically tested for hypoglycemic effects in alloxan-induced diabetic rats. The results showed that the chloroform fraction of the 75% EtOH extract of the barks of this plant exhibited significant blood sugar reducing activity, most of which were significantly higher than that of positive-drug metformin hydrochloride. A new compound, together with nine known compounds, was isolated from the most active fraction. The structure elucidation was based on spectroscopic methods, including two-dimensional NMR experiments (¹H-¹H COSY, HMQC, and HMBC). All of the isolates were evaluated for their α-glycosidase and glycogen phosphorylase inhibitory activities.
