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OBJECTIVE@#To investigate the mechanism of Radix Kansui (RK) stir-fried with vinegar (VRK) decreased hepatotoxicity in mice.@*METHODS@#According to a random number table, 40 mice were randomly divided into negative control group (0.5% carboxymethylcellulose sodium, 20 mL/kg), positive control group (0.1% mixture of carbon tetrachloride in soybean oil, 20 mL/kg), RK group (the ethyl acetate extracts of RK, 250 g crude drug/kg) and VRK group (the ethyl acetate extracts of VRK, 250 g crude drug/kg) with 10 mice per group. All mice were administered orally by gavage daily for 7 continuous days. The morphology of liver tissues was examined to assess the liver injury by a transmission electron microscope. Hepatocyte apoptosis in vivo was determined by terminal deoxynucleotidyltransferase-mediated dUTP-biotin nickend labeling (TUNEL) assay. Immunohistochemical technique was adopted to detect the expression of particular antiapoptotic and proapoptotic proteins in the mitochondrial pathways, including B-cell lymphoma (Bcl-2) and caspase-3, as well as the expression of inflammatory mediators, including nuclear factor kappa B (NF- κ B) and intercellular adhesion molecule-1 (ICAM-1).@*RESULTS@#Liver injury and hepatocyte apoptosis were observed in RK mice, and the liver injury were significantly reduced in VRK-treated mice. In immunohistochemistry study, compared with the negative control group, RK inhibited dramatically the Bcl-2 protein expression and significantly increased the expression of caspase-3, NF- κ B and ICAM-1 (all P<0.01). Compared with the RK group, VRK group induced significant increase on Bcl-2 protein expression, and decreased the caspase-3, NF- κ B and ICAM-1 protein expression (P<0.05 or P<0.01).@*CONCLUSION@#The mechanism of reduced hepatotoxicity of VRK may be associated with the reduced inflammation, regulation of antiapoptotic and proapoptotic mediators in the mitochondrial pathway.
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Mineral medicine is an indispensable part of traditional Chinese medicine and has a long history of application. Among them， mineral-based hemostatics have been widely applied for the treatment of various hemorrhagic diseases with extensive clinical experience and established efficacy. Gypsum Fibrosum （GF）， a commonly used mineral medicine in clinical， can clear away heat， and relieve anxiety and thirst. Gypsum Ustum （GU） is the processed product of GF after calcining at high temperature. It is mainly composed of anhydrous calcium sulfate （CaSO4） with the functions of moisturizing， promoting muscle growth， astringent sores and hemostasis. GU is often used externally to treat ulcer， itching， eczema， water and fire scalds， trauma bleeding， etc. Studies on the mechanism of hemostasis have shown that Ca2+ （coagulation factor Ⅳ） is involved in many key processes of the internal and external coagulation cascades and can prevent bleeding by regulating platelet activation and aggregation， and promoting the production of insoluble fibrin and the ultimate formation of a blood clot. GF and GU both contain Ca2+ which provide an important material basis of hemostatic effect for both compounds， but GU has a significant hemostatic effect， while GF has no hemostatic effect. After processing， the taste and efficacy of the GF have been obviously changed which reflects the characteristics of processing， but the processing mechanism of GU has not been fully clarified. Therefore， based on studies of GF before and after calcining， this paper focused on these aspects including calcining process， crystal form comparison， element content， efficacy comparison， and summarized various aspects of Ca2+ involved in hemostasis. In addition， the hemostatic properties of other calcium-containing mineral medicines and new calcium-containing hemostatic materials such as calcium alginate， mesoporous calcium silicate and nanogel hemostatic materials were also discussed. The paper aimed to provide a reference for elucidating processing mechanism and clinical dialectical use of GU， also to promote development of new calcium-containing hemostatic materials.
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AIM@#To establish an LC-MS/MS method for determination of isorhamnetin-3-O-neohesperidoside and investigate its application on pharmacokinetic study in rats.@*METHODS@#Eight rats were given 5 mg·kg(-1) isorhamnetin-3-O-neohesperidoside after intravenous administration. A highly sensitive liquid chromatography-tandem mass spectrometry method was developed and validated for the determination of isorhamnetin-3-O-neohesperidosidein rat plasma using rutin as internal standard. The analytes and rutin (internal standard) were extracted with methanol followed by a rapid isocratic elution with 10 mmol·L(-1) ammonium acetate buffer/methanol (20 : 80, V/V) on a C18 column (150 mm × 2.1 mm, I.D., 5 μm) and subsequent analysis by mass spectrometry in the multi-eaction-monitoring mode.@*RESULTS@#The assays were linear over the concentration range of 0.01-10 μg·mL(-1) for isorhamnetin-3-O-neohesperidosidein rat plasma. The lower limit of quantifications for isorhamnetin-3-O-neohesperidoside was 0.01 μg·mL(-1).@*CONCLUSION@#The validated method is successfully applied to determine the plasma concentrations of isorhamnetin-3-O-neohesperidosidein in rats.