Background:The incidence and prevalence of atherosclerosis(AS)is increasing every year and has becoming a major health issue of global concern.Polygoni Cuspidati Rhizoma(PCR)is a Chinese herb that is widely used clini...Background:The incidence and prevalence of atherosclerosis(AS)is increasing every year and has becoming a major health issue of global concern.Polygoni Cuspidati Rhizoma(PCR)is a Chinese herb that is widely used clinically for the treating of AS.However,its pertinent targets and probable mechanisms,still need to be completely explored.Methods:Active compounds and targets for PCR and AS targets were screened using public databases.A“drug-component-disease target”network map was created and analyzed after using the Venn online tool to identify common targets and Cytoscape software to screen drug-disease core targets.Critical targets pathway enrichment analyses are conducted using the Metascape database.Using AutoDock Vina and Pymol software,docking validation and visualization of active components and core targets were carried out.Results:PCR was obtained for ten compounds with 105 AS-related targets.Rhein,quercetin,beta-sitosterol,and luteolin may be drug candidates,and the genes for AKT1,TNF,IL-6,EGFR,TP53,IL-1,RELA,and VEGFA are potential therapeutic targets,according to network analysis.PCR might modulate the AGE/RAGE,PI3K/Akt,IL-17 and NF-ᴋB signaling pathways against the development of AS.Molecular docking indicated that quercetin has high affinity for AKT1 and TNF gene targets.Conclusion:This study provides rare information and scientific basis for further exploration of PC in the treatment of AS.展开更多
The epidermal growth factor receptors(EGFRs)in some tumor cells are significant targets for drug discovery.In this work,we have developed an EGFR cell membrane chromatography and online high performance liquid chromat...The epidermal growth factor receptors(EGFRs)in some tumor cells are significant targets for drug discovery.In this work,we have developed an EGFR cell membrane chromatography and online high performance liquid chromatography/mass spectrometry system for screening active component from Rhizoma Polygoni Cuspidati.As a result,resveratrol from Rhizoma Polygoni Cuspidati was found to be the active component acting on EGFR like gefitinib.There was a good relationship between their inhibiting effects on EGFR secretion and HEK293 EGFR cell growth in vitro.The EGFR/CMC-online-HPLC/MS system demonstrated fast and effective characteristics for screening leading compounds from traditional Chinese medicine.展开更多
Objective：To explore the effects of Rhizoma Polygoni Cuspidati and Ramulus Cinnamomicompatibility（PR） on uric acid metabolism and the expression of urinary neutrophil gelatinase-associated lipocalin（NGAL） and kid...Objective：To explore the effects of Rhizoma Polygoni Cuspidati and Ramulus Cinnamomicompatibility（PR） on uric acid metabolism and the expression of urinary neutrophil gelatinase-associated lipocalin（NGAL） and kidney injury molecule-1（KIM-1） in rats with hyperuricemia. Methods：Seventy male Sprague Dawley（SD） rats were randomly divided into 7 groups with 10 rats per group, including the normal group, model group, allopurinol group, benzbromarone group and PR groups at 3 doses（3.5, 7, 14 g/kg）. Except the normal group, rats of the other groups were intragastrically administered 100 mg/kg hypoxanthine and 250 mg/kg ethambutol, and subcutaneously injected with 200 mg/kg potassium oxonate. All rats were continuously modeled for 17 days, and gavaged with corresponding drugs. The rats of the normal and model groups were gavaged with saline, once a day, for 2 weeks. The levels of serum uric acid（SUA）, blood urea nitrogen（BUN） and creatinine（Cr） were determined. In addition, the contents of NGAL and KIM-1 in urine and the m RNA and protein expressions of xanthine oxidase（XOD） in liver of hyperuricemia rats were measured by reverse transcription polymerase chain reaction（RT-PCR） and Western blot, respectively. Moreover, the pathological changes of kidney were analyzed by hematoxylin and eosin（HE） stain method. Results：Compared with the normal group, the levels of SUA, BUN, NGAL and KIM-1 and the expressions of hepatic XOD m RNA and protein in the hyperuricemia rats were increased significantly（P〈0.01）. PR significantly decreased the levels of SUA, BUN, NGAL and KIM-1 and down-regulated the m RNA and protein expressions of hepatic XOD（P〈0.05 or P〈0.01）. In addition, the pathological changes of kidney were significantly suppressed by oral administration of PR. Conclusions：PR ameliorated uric acid metabolism and protected renal function, the underlying mechanism was mediated by decreasing the levels of SUA, BUN, NGAL and KIM-1, inhibiting the expression of hepatic XOD and ameliorating the pathological change of kidney.展开更多
Objective To investigate the effects of Polygoni Cuspidati Rhizoma et Radix （PCRR） and its ingredient resveratrol （Res） on experimental autoimmune myasthenia gravis （EAMG）. Methods EAMG was induced in Lewis rats...Objective To investigate the effects of Polygoni Cuspidati Rhizoma et Radix （PCRR） and its ingredient resveratrol （Res） on experimental autoimmune myasthenia gravis （EAMG）. Methods EAMG was induced in Lewis rats by the immunization of a synthetic peptide corresponding to region 97-116 of the rat acetylcholine receptor （AChR） α subunit （R97-116）. EAMG rats were randomly divided into PCRR group, Res group, and control （C） group, and were ig administered respectively with PCRR （2 g/kg）, Res （20 mg/kg）, and DMSO （0.4 mL/kg） every day from day 5 after immunization to day 42. Clinical evaluation, lymphocyte proliferation, cytokines, and anti-97-116 antibodies were performed for examination of their therapeutic effects. Results Treatments with PCRR and Res significantly ameliorated clinical symptoms, down-regulated TNF-α and up-regulated IL-10 in serum and culture supernatants of lymphocytes stimulated with R97-116, and decreased levels of anti-R97-116 IgG1 and IgG2a in serum compared with C group. Unexpectedly, PCRR but not Res inhibited lymphocyte proliferation compared with C group. Conclusion PCRR and Res ameliorating EAMG is associated with suppressing immune response, and indicates a therapeutic potential for EAMG and even human myasthenia gravis （MG）. Res may be the main effective ingredient from PCRR ameliorating EAMG, but further experiments are necessary.展开更多
目的应用RP-HPLC对不同产地虎杖药材进行指纹图谱研究。方法K rom as il C18色谱柱(150 mm×4.6mm,5μm),乙腈-水二元梯度洗脱,体积流量:1 mL/m in,检测波长303 nm。结果根据选择的色谱条件制订了不同产地虎杖药材的指纹图谱。结论...目的应用RP-HPLC对不同产地虎杖药材进行指纹图谱研究。方法K rom as il C18色谱柱(150 mm×4.6mm,5μm),乙腈-水二元梯度洗脱,体积流量:1 mL/m in,检测波长303 nm。结果根据选择的色谱条件制订了不同产地虎杖药材的指纹图谱。结论色谱图对各产地虎杖药材中各成分得到了很好的分离,可作为虎杖药材的专属性指纹图谱。展开更多
基金supported by Project of first-class discipline construction in Yunnan Province(2022YS13).
文摘Background:The incidence and prevalence of atherosclerosis(AS)is increasing every year and has becoming a major health issue of global concern.Polygoni Cuspidati Rhizoma(PCR)is a Chinese herb that is widely used clinically for the treating of AS.However,its pertinent targets and probable mechanisms,still need to be completely explored.Methods:Active compounds and targets for PCR and AS targets were screened using public databases.A“drug-component-disease target”network map was created and analyzed after using the Venn online tool to identify common targets and Cytoscape software to screen drug-disease core targets.Critical targets pathway enrichment analyses are conducted using the Metascape database.Using AutoDock Vina and Pymol software,docking validation and visualization of active components and core targets were carried out.Results:PCR was obtained for ten compounds with 105 AS-related targets.Rhein,quercetin,beta-sitosterol,and luteolin may be drug candidates,and the genes for AKT1,TNF,IL-6,EGFR,TP53,IL-1,RELA,and VEGFA are potential therapeutic targets,according to network analysis.PCR might modulate the AGE/RAGE,PI3K/Akt,IL-17 and NF-ᴋB signaling pathways against the development of AS.Molecular docking indicated that quercetin has high affinity for AKT1 and TNF gene targets.Conclusion:This study provides rare information and scientific basis for further exploration of PC in the treatment of AS.
基金This work was supported by the National Natural Science Foundation of China(Grant number 30730110).
文摘The epidermal growth factor receptors(EGFRs)in some tumor cells are significant targets for drug discovery.In this work,we have developed an EGFR cell membrane chromatography and online high performance liquid chromatography/mass spectrometry system for screening active component from Rhizoma Polygoni Cuspidati.As a result,resveratrol from Rhizoma Polygoni Cuspidati was found to be the active component acting on EGFR like gefitinib.There was a good relationship between their inhibiting effects on EGFR secretion and HEK293 EGFR cell growth in vitro.The EGFR/CMC-online-HPLC/MS system demonstrated fast and effective characteristics for screening leading compounds from traditional Chinese medicine.
基金Supported by the National Natural Science Foundation of China(No.81173194)
文摘Objective：To explore the effects of Rhizoma Polygoni Cuspidati and Ramulus Cinnamomicompatibility（PR） on uric acid metabolism and the expression of urinary neutrophil gelatinase-associated lipocalin（NGAL） and kidney injury molecule-1（KIM-1） in rats with hyperuricemia. Methods：Seventy male Sprague Dawley（SD） rats were randomly divided into 7 groups with 10 rats per group, including the normal group, model group, allopurinol group, benzbromarone group and PR groups at 3 doses（3.5, 7, 14 g/kg）. Except the normal group, rats of the other groups were intragastrically administered 100 mg/kg hypoxanthine and 250 mg/kg ethambutol, and subcutaneously injected with 200 mg/kg potassium oxonate. All rats were continuously modeled for 17 days, and gavaged with corresponding drugs. The rats of the normal and model groups were gavaged with saline, once a day, for 2 weeks. The levels of serum uric acid（SUA）, blood urea nitrogen（BUN） and creatinine（Cr） were determined. In addition, the contents of NGAL and KIM-1 in urine and the m RNA and protein expressions of xanthine oxidase（XOD） in liver of hyperuricemia rats were measured by reverse transcription polymerase chain reaction（RT-PCR） and Western blot, respectively. Moreover, the pathological changes of kidney were analyzed by hematoxylin and eosin（HE） stain method. Results：Compared with the normal group, the levels of SUA, BUN, NGAL and KIM-1 and the expressions of hepatic XOD m RNA and protein in the hyperuricemia rats were increased significantly（P〈0.01）. PR significantly decreased the levels of SUA, BUN, NGAL and KIM-1 and down-regulated the m RNA and protein expressions of hepatic XOD（P〈0.05 or P〈0.01）. In addition, the pathological changes of kidney were significantly suppressed by oral administration of PR. Conclusions：PR ameliorated uric acid metabolism and protected renal function, the underlying mechanism was mediated by decreasing the levels of SUA, BUN, NGAL and KIM-1, inhibiting the expression of hepatic XOD and ameliorating the pathological change of kidney.
文摘Objective To investigate the effects of Polygoni Cuspidati Rhizoma et Radix （PCRR） and its ingredient resveratrol （Res） on experimental autoimmune myasthenia gravis （EAMG）. Methods EAMG was induced in Lewis rats by the immunization of a synthetic peptide corresponding to region 97-116 of the rat acetylcholine receptor （AChR） α subunit （R97-116）. EAMG rats were randomly divided into PCRR group, Res group, and control （C） group, and were ig administered respectively with PCRR （2 g/kg）, Res （20 mg/kg）, and DMSO （0.4 mL/kg） every day from day 5 after immunization to day 42. Clinical evaluation, lymphocyte proliferation, cytokines, and anti-97-116 antibodies were performed for examination of their therapeutic effects. Results Treatments with PCRR and Res significantly ameliorated clinical symptoms, down-regulated TNF-α and up-regulated IL-10 in serum and culture supernatants of lymphocytes stimulated with R97-116, and decreased levels of anti-R97-116 IgG1 and IgG2a in serum compared with C group. Unexpectedly, PCRR but not Res inhibited lymphocyte proliferation compared with C group. Conclusion PCRR and Res ameliorating EAMG is associated with suppressing immune response, and indicates a therapeutic potential for EAMG and even human myasthenia gravis （MG）. Res may be the main effective ingredient from PCRR ameliorating EAMG, but further experiments are necessary.
文摘目的应用RP-HPLC对不同产地虎杖药材进行指纹图谱研究。方法K rom as il C18色谱柱(150 mm×4.6mm,5μm),乙腈-水二元梯度洗脱,体积流量:1 mL/m in,检测波长303 nm。结果根据选择的色谱条件制订了不同产地虎杖药材的指纹图谱。结论色谱图对各产地虎杖药材中各成分得到了很好的分离,可作为虎杖药材的专属性指纹图谱。
