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1.
Zhongcaoyao ; Zhongcaoyao;(24): 3554-3559, 2017.
Article in Chinese | WPRIM | ID: wpr-852558

ABSTRACT

Objective To explore the protective effects of glycyrrhetic acid derivatives (TY501) on carbon tetrachloride-induced liver fibrosis in mice. Methods The mice liver fibrosis was established by classical CCl4, and TY501 was given in three kinds of dosage (45, 15, and 5 mg/kg), with colchicine serving as control. After 30 d treatment, the liver function, fibrosis and the levels of Hyp and TGF-β1 were detected. Moreover, the histopathological changes were detected by HE and Masson staining. Results Compared with model group, the levels of ALT, AST, ALP, ALB, HA, LN, PCIII, CIV, Hyp, and TGF-β1 were all decreased, with high-dose group being the most significant (P < 0.05, 0.01). Histopathological examination showed that liver fibrosis of those mice treated with TY501 was improved to some extent. Conclusion TY501 can significantly protect carbon tetrachloride-induced hepatic fibrosis.

2.
Article in Chinese | WPRIM | ID: wpr-493729

ABSTRACT

Deoxyglycychloxazol (TY501) is a glycyrrhetinic acid derivative which exhibits high anti-inflammatory activity and reduced pseudoaldosteronism compared to glycyrrhetinic acid. In this study, a sensitive and rapid liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was established for the quantitation of TY501 in rat plasma. Plasma samples were treated by precipitating protein with methanol and supernatants were separated by a Symmetry C8 column with the mobile phase consisting of me-thanol and 10 mM ammonium formate (containing 0.1%of formic acid) (90:10, v/v). The selected reaction monitoring (SRM) transitions were performed at m/z 647.4-191.2 for TY501 and m/z 473.3-143.3 for astragaloside aglycone (IS) in the positive ion mode with atmospheric pressure chemical ionization (APCI) source. Calibration curve was linear over the concentration range of 5–5000 ng/mL. The lower limit of quantification was 5 ng/mL. The mean recovery was over 88%. The intra-and inter-day precisions were lower than 6.0% and 12.8%, respectively, and the accuracy was within 71.3%. TY501 was stable under usual storage conditions and handling procedure. The validated method has been successfully applied to a pharmacokinetic study after oral administration of TY501 to rats at a dosage of 10 mg/kg.

3.
Chinese Pharmacological Bulletin ; (12): 210-215, 2015.
Article in Chinese | WPRIM | ID: wpr-473693

ABSTRACT

Aim To investigate TY501′s role in bleo-mycin ( BLM )-induced pulmonary fibrosis in rats. Methods Forty rats were randomly divided into 5 groups, including the sham operation, BLM, PFD, TY501(high and low dose) groups. After administra-tion of BLM intratracheally, PFD and TY501 were giv-en in each group daily, according to the dosage de-signed during 21 days. Lung coefficient, PaO2 were tested before killing the rats. The contents of ALB, ALP, LDH, GSH, HYP were detected by regent kit respectively. PCⅢ and COL4 were determined by ELISA. Results ( 1 ) Some indicators of alveolitis in early stage of IPF: the contents of lung coefficient in three treatment groups were lower and PaO2 was higher than those in BLM group ( P<0. 05 ); compared with BLM group, the contents of ALB, ALP, LDH in the treatment groups reduced on 21 st day ( P<0. 05 );the expression of GSH in BLM group was increased for feedback regulation and higher than the treatment groups and the sham operation group (P<0. 05);(2) some indicators of pulmonary interstitial fibrosis in late stage of IPF:the expressions of HYP, PCⅢand COL4 were reduced after the treatment. There were signifi-cant differences compared with BLM group ( P <0. 05 ) . Conclusions TY501 is valuable for the ther-apy of IPF, the same as the positive drug pirfenidone. TY501 attenuates BLM-induced pulmonary fibrosis, which may be related to the affection of TGF-βpathway and inhibition of MMPs.

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