Reduced bioavailability of cyclosporine A in rats by mung bean seed coat extract

Mung bean seed coat (MBSC) is a healthcare product in Asian countries. The aim of this study was to investigate the effect of an MBSC ethanol extract on the bioavailability of cyclosporine A (CsA) in rats. Rats were orally dosed with CsA alone or in combination with MBSC ethanol extracts (500 mg/kg, p.o.). The blood levels of CsA were assayed by liquid chromatography with an electrospray ionization source and tandem mass spectrometry (LC-MS/MS). The everted rat intestinal sac technique was used to determine the influence of MBSC on the absorption of CsA. The results reveal that combined CsA intake with MBSC decreased the Cmax, AUC0-t, t1/2z and MRT0-t values of CsA by 24.96%, 47.28%, 34.73% and 23.58%, respectively (P<0.05), and significantly raised the CL/F by 51.97% (P<0.01). The in vitro results demonstrated that significantly less CsA was absorbed (P<0.05). The overall results indicate that after being concomitantly ingested, MBSC reduced the bioavailability of CsA, at least partially, in the absorption phase.

O tegumento da semente de feijão-mungo (MBSC) é um produto para tratamento de saúde em países asiáticos. O objetivo deste estudo foi investigar o efeito de extrato etanólico de MBSC na biodisponibilidade da ciclosporina A (CVsA) em ratos. Administrou-se aos ratos CsA sozinha ou em associação com extrato etanólico de MBSC (500 mg/kg, p.o.), por via oral. Os níveis sanguíneos de CSA foram determinados por cromatografia a líquido com ionização por electrospray, associada à espectrometria de massas (LC-MS/MS). Utilizou-se a técnica de inversão do saco intestinal de rato para determinar a influência do MBSC na absorção de CsA. Os resultados revelaram que a ingestão combinada de CsA e MBSC diminuiu os valores de Cmax, AUC0-t, t1/2z e MRT0-t de CsA em 24%, 47,28%, 34,73% e 23,58%, respectivamente (P<0.05), e aumentou, significativamente, CL/F em 51,79% (P<0.05). Os resultados in vitro demostraram que, significativamente, menos CsA foi absorvida (P<0.05). Os resultados totais indicaram que após ser concomitantemente ingerida, a MBSC reduziu, ao menos parcialmente, a biodisponibilidade de CsA, na fase de absorção.

Preparation of Anti-HER2 Monoclonal Antibody-paclitaxel Immunoconjugate and Its Biological Evaluation / 华中科技大学学报（医学）（英德文版）

Anti-HER2 monoclonal antibody (Sc7301)-paclitaxel (TAX) immunoconjugate was prepared and its specific binding to tumor cells was investigated in this study.Sc7301 was conjugated to　TAX by the active ester method and then the TAX-Sc7301 immunoconjugate was obtained.After purification and labeling by Cyano-fluorescein isothiocyanate (FITC),the specific binding of TAX-Sc7301to HER2-positive tumor cells (SKOV3) and HER2-negative tumor cells (HepG2) was evaluated respectively.TAX-Sc7301 (20 nmol/L) showed distinct specific binding to SKOV3 cells rather than HepG2cells.And the uptake of the immunoconjugate by SKOV3 cells was increased with the TAX-Sc7301concentration (3-48 nmol/L) and the incubation time (P＜0.05).It was concluded that the TAX-Sc7301immunoconjugate is potentially applicable as a targeted agent against HER2-positive tumor cells.