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1.
Article in Chinese | WPRIM | ID: wpr-872929

ABSTRACT

Objective:To study the components with urate anion transporter 1(URAT1) regulation effect and their combination mechanisms of Lagotis brevituba by integrating techniques of HK-2 cell capture,UPLC-Q-TOF-MS and molecular docking,so as to provide material and theory bases for the development of new hypouricemic medicines based on L. brevituba. Method:The HK-2 cells were applied to capture the components of L. brevituba. UPLC-Q-TOF-MS was used to identify those components. The molecular docking technique was adopted to study the interaction mechanism between the compounds and URAT1. Result:Eight components were successfully screened and identified as hyperoside,plantamajoside,kaempferol-3-O-glucoside,lugrandoside,nepitrin,isolugrandoside,homoplantaginin,luteolin,respectively. Those components could combine with URAT1 mainly through hydrogen bond,van der Waals force and hydrophobic action,which were closely related to structure and compound types. Furthermore,the LibDock score of phenylethanoids was higher than that of flavonoids. Conclusion:The integration of target cell capture,UPLC-Q-TOF-MS and molecular docking techniques could be successfully used to identify captured compounds of L. brevituba with URAT1 regulation effects and illustrate their potential combination mechanisms as well as the structure-activity relationships. The findings may provide material and theory bases for the development of new hypouricemic medicines based on L. brevituba.

2.
Article in Chinese | WPRIM | ID: wpr-872794

ABSTRACT

Objective::To established the model of chronic alcoholic liver injury in rats by long-term(8 weeks) alcoholic gavage, to study the effects of Tibetan medicine Lagotis brachystachys extracts on Toll-like receptor(TLR)2/myeloid differentiation factor 88(MyD88)/nuclear factor kappa B (NF-κB)and NOD like receptor protein 3(NALP3) signaling pathways and study preliminary the mechanism of action of chronic alcoholic liver injury. Method::Sixty male Sprague-Dawley rats were randomly divided into normal group, model group, bifendate positive drug group (0.1 g·kg-1) and L. brachystachys low, medium and high-dose groups (0.5, 1, 2 g·kg-1), the corresponding drugs were given at 10 mL·kg-1 in each morning, and the 56 degree Liquor was administered by the afternoon gradient alcoholic gavage method.After 8 weeks, the levels of serum aspartate transaminase (AST), serum alanineaminotransfease(ALT), serum total cholesterol(TC), triglyceride(TG), interleukin-1β(IL-1β), and the liver levels of L-glutathione(GSH)were measured. The expression of TLR2, MyD88, NF-κB and NALP3 protein in liver were detected by Western blot.Hematoxylin-eosin (HE) staining was used to observe the pathological changes of liver tissue. Result::Compared with normal group, the serum levels of AST, ALT, TC, TG and IL-1β in model group were significantly increased (P<0.05, P<0.01). Compared with model group, the serum AST, ALT, TC, TG and IL-1β levels were decreased in the various doses of L. brachystachys, and the high dose group was particularly effective (P<0.05, P<0.01). Compared with normal group, the GSH level in the liver homogenate of model group decreased significantly, and the difference was not statistically significant. The levels of TLR2, MyD88, NF-κB and NALP3 in the liver tissue of model group were significantly increased (P<0.05, P<0.01). The GSH levels in the liver and the protein expression of TLR2, MyD88, NF-κB and NALP3 were decreased in L. brachystachys group (P<0.05, P<0.01). The liver pathological section showed that L. brachystachys can improve the pathological changes of rat liver tissue. Conclusion::L. brachystachys can protect liver from alcohol-induced chronic liver injury in rats. The mechanism was related to TLR2/MyD88/NF-κB and NALP3 signaling pathway.

3.
Article in Chinese | WPRIM | ID: wpr-777517

ABSTRACT

Chrysosplenium nudicaule,Tibetan name " Yajima",is recorded as an effective medicine for the treatment of liver and gallbladder diseases by Tibetan Pharmacopoeia published in the past dynasties,but its traditional efficacy has not yet been investigated by means of modern pharmacological research methods. In this paper,the protective effect of extract of C. nudicaule(ECN) on liver injury in mice was observed by using the mice model of intrahepatic cholestasis(IC) induced by α-naphthyl isothiocyanate(ANIT) and the possible mechanism by which ECN work as the therapeutic agent was discussed. The results showed that the serum levels of AST,ALT,ALP,DBIL,TBIL and TBA of the model mice were notably reduced in dose-dependent manner(P<0. 01,P<0. 05). The activity of SOD and GSH-Px in the liver homogenate of mice was increased,while the content of MDA was decreased(P<0. 01,P<0. 05).Pathological examination of liver in mice showed that ECN could improve the pathological changes of liver tissue in mice. The mRNA expression level of genes related to bile acid metabolism were detected by RT-PCR and the results suggested that ECN could significantly increase the expression of genes such as BSEP,FXR and MRP2(P<0. 01,P<0. 05),meanwhile significantly reduce the expression of CYP7 A1(P<0. 01,P<0. 05). These results confirmed the protective effect of ECN on intrahepatic cholestasis-induced liver injury in mice,and indicated that the mechanism may be related to activating FXR and its target genes,reducing bile acid synthesis and increasing bile acid excretion. This study provides a modern pharmacological basis for the clinical application of Yajima in Tibetan medicine.


Subject(s)
Animals , Cholestasis, Intrahepatic , Drug Therapy , Liver , Medicine, Tibetan Traditional , Mice , Plant Preparations , Pharmacology , Saxifragaceae , Chemistry
4.
Article in Chinese | WPRIM | ID: wpr-773143

ABSTRACT

In this study,mouse models of benign prostatic hyperplasia induced by subcutaneous injection of testosterone propionate was used to investigate the therapeutic effect and mechanism of Urtica hyperborean( UW) extracts on prostate hyperplasia in mice. The effects of UW extracts on prostate index,serum epidermal growth factor( EGF) and dihydrotestosterone( DHT) in model mice were observed,and the EGF and anti-apoptotic factor( Bcl-2) mRNA expression levels were detected as well as pathological changes in prostate tissue. The results showed that the ethyl acetate extraction and alcohol soluble fraction of the UW could significantly reduce the prostate index,reduce the serum DHT and EGF levels( P<0. 01),and significantly decrease the EGF and Bcl-2 mRNA expression( P<0. 01),significantly improved the morphological structure of prostate tissue. The above results confirmed that ethyl acetate extract and alcohol-soluble parts of UW have a good preventive effect on mice prostatic hyperplasia model,and its mechanism may be to reduce androgen levels by regulating polypeptide growth factors and/or inhibiting cell hyperproliferation and promoting apoptosis. This study laid the foundation for the further research on UW.


Subject(s)
Animals , Dihydrotestosterone , Blood , Epidermal Growth Factor , Blood , Male , Medicine, Tibetan Traditional , Mice , Plant Extracts , Pharmacology , Prostatic Hyperplasia , Drug Therapy , Proto-Oncogene Proteins c-bcl-2 , Metabolism , Testosterone Propionate , Urticaceae , Chemistry
5.
Article in Chinese | WPRIM | ID: wpr-801956

ABSTRACT

Gout is caused by the nucleation and growth of monosodium rate crystals in tissues and around joints, which is followed by long-standing hyperuricemia and serum urate of above the saturation threshold. It could cause a series of complications, such as cardiovascular, hypertension, and renal complications. Over the past two decades, the incidences of hyperuricemia and gout have been increasing due to the continuous improvement of living standards and the changes in dietary structure. The prime and most important therapy for hyperuricemia and gout is to reduce serum uric acid levels, but the western medicine for reducing uric acid in clinical application has serious toxic and side effects. With the rapid development of modern science and technology, the application and development of different screening methods for effective ingredients with a low toxicity and side effects from Chinese herbal medicines for reducing serum uric acid levels has attracted much attention in the research and development of drugs for the prevention and treatment of hyperuricemia and gout. In this study, the screening methods for extracts, fractions, active monomer components and other effective substances were reviewed and analyzed. According to the findings, the screening methods had a considerable progress both in vivo and in vitro. The results showed that the in vivo methods were mainly applied for studying the urate lowing effect and mechanisms of herbal extracts, while the studies for xanthine oxidase(XOD) inhibitors mainly depended on the in vitro methods. Molecular docking homology modeling and liquid chromatography-mass spectrometry have become a new trend for screening effective substances with XOD inhibitory activities and uric acid excretion activities, while cell model will open up a new way for screening effective substances for uric acid excretion. The review provides certain reference for effective components screening of hyperuricemia and gout.

6.
Article in Chinese | WPRIM | ID: wpr-689873

ABSTRACT

Potential xanthine oxidase (XOD) inhibitors in Lagotis brevituba were captured by using affinity and ultrafiltration. The structures of the captured components were identified by ultra-performance liquid chromatography coupled with Q-TOF mass spectrometry (UPLC-Q-TOF-MS). The binding intensity and binding mechanism between the captured components and XOD were analyzed by using molecular docking software Autodock 4.2. A total of 17 compounds were identified, including 9 flavonoids, 5 phenolic acids and 3 triterpenes. Molecular docking results showed that all the captured components could be spontaneously bound with XOD mainly via hydrogen bond, Van der Waals' force and hydrophobic interaction. From the perspective of binding energy and scoring function, the collected fractions all had potential prospects for XOD inhibitors, and the flavonoid luteolin-3',7 glucuronide had the best effect. The results also showed that affinity and ultrafiltration, ultra-performance liquid chromatography-mass spectrometry (UPLC-MS) and molecular docking technology can provide a powerful tool for the analysis of XOD inhibitor components in natural products.

7.
Article in Chinese | WPRIM | ID: wpr-338225

ABSTRACT

Seven compounds(deacetylasperulasidic acid methyl ester, gardenoside, chlorogenic acid, geniposide, crocin-Ⅰ, crocin-Ⅱ, chikusetsu saponin Ⅳa)were determined simultaneously by multiple wavelength HPLC with diode array detector(DAD) in different parts of Gardenia jasminoides. The results showed that these components in different parts of G. jasminoides had a different distribution, and there was a large difference in content of each component. Geniposide was mainly distributed in fruits and leaves; chikusetsu saponin Ⅳa was mainly distributed in roots and stems; crocus glycosides existed mainly in fruits; chlorogenic acid had a higher distribution in leaves and stems; gardenoside had a higher distribution in leaves and roots, while ceacetylasperulasidic acid methyl ester had a higher distribution in roots and stems. Based on the analysis of the chemical composition and content difference in different parts of G. jasminoides, the basis for the comprehensive utilization and quality evaluation of resources of G. jasminoides was provided.

8.
Article in Chinese | WPRIM | ID: wpr-246148

ABSTRACT

<p><b>OBJECTIVE</b>ITS2 of DNA barcoding was used to study genetic polymorphism of Platycodon grandiflorum.</p><p><b>METHOD</b>Total genomic DNA was isolated from P. grandiflorum. PCR was used to amplified the region of internal transcribed spacer 2 (ITS2), and PCR products were sequenced. The sequences of ITS2 were analyzed and compared by Clustal. The intraspecies genetic distance was calculated based on Kimura 2-parameter model by using MEGA 5.05. The ITS2 sequence of Codonopsis pilosula was used as the outreach value for plants of the genus, and the phylogenic tree used constructed by Neighbor-Joining (NJ) method.</p><p><b>RESULT</b>The K2-P's genetic distance of all samples were ranged from 0 to 0.930. The K2-P's genetic distance of samples at the same area were ranged from 0 to 0.178. The K2-P's genetic distance of samples at different areas were ranged from 0.735 to 0.930. The analytical result showed that the degree of genetic variation were heavy in intraspecies of P. grandiflorum and significantly correlated with geographical location.</p><p><b>CONCLUSION</b>The DNA barcoding of ITS2 can applied to study the intraspecific genetic diversity, it provides a reference for further development of DNA barcoding technology applications.</p>


Subject(s)
China , DNA Barcoding, Taxonomic , DNA, Plant , Genetics , DNA, Ribosomal Spacer , Genetics , Molecular Sequence Data , Phylogeny , Platycodon , Classification , Genetics , Polymorphism, Genetic
9.
Article in Chinese | WPRIM | ID: wpr-276626

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effects of processing Phellodendron anurene with salt on anti-gout.</p><p><b>METHOD</b>The mouse serum uric acid level and liver xanthine oxidase activity were used to evaluate anti-gout effects of raw and processing P. amurense with salt.</p><p><b>RESULT</b>Both raw and processing P. amurense with salt reduced serum uric acid levels in the in hyperuricemic mice, and inhibited activities of liver xanthine oxidase at the low and high doses respectively, thus exhibiting anti-gout effects. Moreover, they showed the tendency to decrease the uric acid levels in the normal animal only at the high dose. The latter was a little weaker than the former.</p><p><b>CONCLUSION</b>Processing with salt might not significantly change anti-gout effect of P. amurense.</p>


Subject(s)
Animals , Drugs, Chinese Herbal , Pharmacology , Gout Suppressants , Pharmacology , Hot Temperature , Hyperuricemia , Blood , Liver , Male , Mice , Phellodendron , Chemistry , Plants, Medicinal , Chemistry , Random Allocation , Sodium Chloride , Technology, Pharmaceutical , Methods , Uric Acid , Blood , Xanthine Oxidase , Metabolism
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