Advances in mechanism of methotrexate on toxicity in various organs / 中国药理学通报

As a widely used anti-tumor drug and anti-rheumatic drug in clinic, methotrexate (MTX) has many toxic and side effects, including gastrointestinal mucosa injury, central nervous system injury, liver and kidney function injury, etc. They often bring great trouble to the follow-up treatment of patients. The clarification of the mechanism of MTX toxicity to various organs has become the key to rescue the toxicity. The purpose of the article is to review the toxicity mechanism of MTX in various organs, so as to save the patients from the adverse reactions in clinical treatment.

Study on effects of dioscin against depression and its mechanisms / 中国药理学通报

Aim To investigate the effects and possible molecular mechanisms of dioscin(DIO)against depression in mice.Methods Eighty mice were randomly divided into control group, DIO control group, model group, DIO groups(20, 40 and 80 mg·kg-1 DIO)and FLU group(20 mg·kg-1 fluoxetine).After establishing the depression model with chronic unpredictable moderate stress(CUMS)in mice, the corresponding drugs were administered by gavage continuously for four weeks in each group.The behavior of mice was tested, and the contents of corticosterone(CORT), brain-derived neurotrophic factor(BDNF), 5-hydroxytryptamine(5-HT), malondialdehyde(MDA), superoxide dismutase(SOD)and catalase(CAT)were evaluated by ELISA or enzyme labeling method.In addition, HE staining, Nissl staining and PET scanning were operated for the brain tissues.Western blot was used to detect the protein expressions.Results Compared with model group, DIO significantly improved the behaviors of depressed mice.And it reduced the contents of CORT in serum, increased BDNF and 5-HT in hippocampus.Meanwhile, DIO obviously reduced MDA in serum, increased SOD in serum and CAT in brain tissues.DIO improved the steatosis of brain tissues, disorder and looseness of neurons, and increased glucose metabolism in brain tissues of depressed mice.The molecular mechanism suggested that compared with model group, DIO significantly increased the protein level of UCP2 to adjust the levels of Nrf2, SOD2, GLUT1 and G6Pase.Conclusions DIO improves the depression symptoms of depressed mice, which should be through adjusting UCP2-mediated oxidative stress and glucose metabolism.

Advances in study of dioscin--a natural product / 中国中药杂志

Dioscin, a typical saponin, is widely present in the family of Dioscoreaceae, Liliaceae, Caryophyllaceae and Rosaceae, especially in Dioscoreaceae, including Discorea nipponica Makino, Dioscorea zingiberensis C. H. Wright and Dioscorea panthaica Prain et Burkill. Traditional Chinese medicine reported that dioscin plays a role in expectorant, relaxing the muscles and stimulating the blood circulation, aiding digestion and diuresis. With the development of science and technology in recent years, some new extraction and separation techniques and methods have been applied to the study of dioscin, and more and more pharmacological effects were found. Modern pharmacology studies have confirmed that dioscin had some activities on desensitization, anti-inflammatory, lipid-lowering, anti-tumor, hepatoprotection and anti-viral. After oral administration, dioscin is metabolized to diosgenin, which is the true active ingredient and is an important raw material to synthesize steroid hormone drugs. Therefore, the studies on dioscin are valueable and promising. In this review, we make a summary on the researches of dioscin including the extraction technology, separation and prepara- tion, chemical synthesis, drug metabolism, determination and pharmacological researches.

Research progress of effect of anti-diabetic traditional Chinese medicines based on regulation of glucose metabolic enzyme / 中国中药杂志

Diabetes is a global threat threatening human health in the world, with an increasing incidence rate in recent years. The disorder of glucose metabolism is one of the major factors. As relevant glucose metabolic enzymes such as alpha-glucosidase, glucose-6-phosphatase (G-6-P), glycogen phosphorylase (GP) and glycogen synthase kinase-3 (GSK-3) get involved in and control the process of glucose metabolism, the regulation of the activity of glucose metabolic enzymes is of significance to the treatment of diabetes. Traditional Chinese medicines (TCMs) have been widely researched because of their low toxicology and high efficiency, and many extracts and components from TCMs have been proven to be regulators of glucose metabolic enzymes. Compared with anti-diabetic western medicines, anti-diabetic TCMs feature safety, reliability and low price. This essay summarizes the anti-diabetic effect of TCMs on regulating glucose metabolic enzymes.

Anti-cancer activity of Zuojinwan in vivo and influence to tumor markers in mice transplanted with sarcoma 180 / 中国中药杂志

<p><b>OBJECTIVE</b>To study the anticancer action of Zuojinwan in mice transplanted with sarcoma 180 in vivo, and detect the activities of five kinds of tumor markers (TM) including acid phosphotase (ACP), alkaline phosphotase (AKP), creatine kinase (CK), aldolase (ALD) and lactate dehydrogenase (LDH) in serum compared with Coptis chinensis and Evodia rutaecarpa.</p><p><b>METHOD</b>The transplanted S180 tumor mice model was established, and the mice were divided randomly five groups. The extract of Zuojinwan (850.8 mg kg(-1)), C. chinensis (729.2 mg kg(-1)) and E. rutaecarpa (121.6 mg kg(-1)) were administrated, respectively for 10 d. Then, the changes of body weight, spleen index of mice, the inhibition rates of tumor, and the increase of life span (ILS) were all tested. In addition, the activities of ACP, AKP, CK, ALD and LDH on different test groups were also determined.</p><p><b>RESULT</b>Zuojinwan could inhibit the S180 tumor growth significantly with the inhibition rate of 50.54% and the ILS of mice reached to 64.91%. Meanwhile, the activities of ACP (126.72 +/- 11.16) U 100 mL(-1) and AKP (67.27 +/- 13.49) U 100 mL(-1) were increased, and the activities of CK (20.65 +/- 4.28) U mL(-1), ALD (319.13 +/- 53.87) U L(-1) and LDH (1,029.04 +/- 468.56) U L(-1) were decreased significantly by Zuojinwan treated group compared with C. chinensis and E. rutaecarpa treated groups (P<0.01).</p><p><b>CONCLUSION</b>In the prescription of Zuojinwan, the enhancement of compatibility of anticancer activity was observed by the interaction of C. chinensis and E. rutaecarpa. The mechanism might be in according with to influence the activities of the five kinds of tumor markers (TM) in mice serum.</p>

Preparative separation of gentiopicrin from Radix Gentianae by high-speed counter-current chromatography with macroporous resin / 中国中药杂志

<p><b>OBJECTIVE</b>To develop a method for the preparative separation of gentiopicrin from Radix Gentianae by high-speed counter-current chromatography (HSCCC).</p><p><b>METHOD</b>The crude alcohol extracts were eluted on a macroporous resin column and then purified by high speed counter-current chromatography (HSCCC). A two-phase solvent system composed of ethyl acetate: n-butanol: water (2 : 1 : 3) was used, and the lower phase was used as the mobile phase at a flow rate of 1.5 mL x min(-1), while the apparatus rotated at 800 r x min(-1) and the eluate was detected at 254 nm.</p><p><b>RESULT</b>136 mg gentiopicrin with purity of 99.6% determined by HPLC were obtained from 300 mg crude extraction only in one-step separation and less than 200 minutes.</p><p><b>CONCLUSION</b>The established method is simple, high efficiency and suitable for large-scale separation of gentiopicrin.</p>

Isolation and structure identification of chemical constituents from Patrinia villosa / 药学学报

<p><b>AIM</b>To study the chemical constituents of Patrinia villosa Juss.</p><p><b>METHODS</b>Solvent extraction, silica gel column and preparative liquid chromatography were used to separate the chemical constituents, and the chemical structures were elucidated by physico-chemical properties and spectra data.</p><p><b>RESULTS</b>Eight compounds were isolated and identified as bolusanthol B (1), (2S)-5, 7, 2', 6'-tetrahydroxy-6,8-di (gamma,gamma-dimethylallyl) flavanone (2), orotinin (3), (2S)-5, 7, 2', 6'-tetrahydroxy-6-lavandulylated flavanone (4), 3'-prenyl-apigenine (5), luteolin (6), quercetin (7) and apigenin (8).</p><p><b>CONCLUSION</b>Compound 2 and 4 are new compounds, compounds 1, 3 and 5 were separated from Patrinia genius for the first time, compounds 6, 7 and 8 were isolated from Patrinia vollosa Juss for the first time.</p>

Studies on chemical constituents of Patrinia villosa / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents of Patrinia villosa.</p><p><b>METHOD</b>The chemical constituents were isolated by silica gel column chromatography and semi-preparative high-performance liquid chromatography, and identified by physicochemical properties and spectral analysis (MS, 1H-NMR and 13C-NMR).</p><p><b>RESULT</b>Seven compounds were isolated from ethyl acetate and n-butanol extract and identified as: 5-hydroxyl-7, 3', 4'-trimethoxy flavone (I), 5-hydroxyl-7, 4'-dimethoxy flavone (II), luteolin (III), quercetin (IV), isoorientin (V), isovitexin (VI) and 8-C glucosylprunetin (VII).</p><p><b>CONCLUSION</b>Compounds I , II, III, V, VI and VIII were obtained from the plant of genus Patrinia for the first time, compound IV was separated from P. villosa for the first time.</p>

The contents of paeoniflorin in different combination jingzhixuefuzhuyu / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the contents of paeoniflorin in different combination Jingzhixuefuzhuyu.</p><p><b>METHOD</b>Using RP-HPLC to determine the contents of paeoniflorin in different combination Jingzhixuefuzhuyu extracts, an ODS column was used with a mobile phase of MeOH-H2O-HAC(25:75:0.15) and DAD detector at the wavelength of 230 nm.</p><p><b>RESULT AND CONCLUSION</b>Different combinations of Jingzhixuefu zhuyu had great influence to the contents of paeoniflorin.</p>