This paper reviews the research progress of Guizhi Fuling Pill in the clinical application of gynecology,such as the treatment of uterine leiomyoma,ovarian cyst,infertility and dysmenorrhea,in order to provide further...This paper reviews the research progress of Guizhi Fuling Pill in the clinical application of gynecology,such as the treatment of uterine leiomyoma,ovarian cyst,infertility and dysmenorrhea,in order to provide further research ideas for clinical researchers.展开更多
OBJECTIVE To evaluate the effect of Guizhi Fuling Capsule active pharmaceutical ingredient(API)and its fractions on human breast cancer cells proliferation by high-throughput screening assay.METHODS The crude fraction...OBJECTIVE To evaluate the effect of Guizhi Fuling Capsule active pharmaceutical ingredient(API)and its fractions on human breast cancer cells proliferation by high-throughput screening assay.METHODS The crude fractions were obtained from the extraction and elution of the API of Guizhi Fuling Capsule,and 929 standard fractions were obtained by the optimal separation conditions.Sulforhodamine B(SRB)method was used to evaluate the effects of the Guizhi Fuling capsule API and929 kinds of fractions on the proliferation of human breast cancer cells MCF-7 and MDA-MB-231.RESULTS The Guizhi Fuling capsule API had a strong ability to inhibit the proliferation of MCF-7 cells at high concentration and the ability to inhibit MDA-MB-231 cells' proliferate at low concentration following 72 h treatment;some samples of 929 fractions(5μg·mL^(-1))was found to have a breast cancer cell growth inhibition rate above 50%,without toxicity on HUVECs proliferation.CONCLUSION The API of Guizhi Fuling capsule had significant cytotoxicity effects on these two human breast cancer cells,with significant concentration-and time-dependent manner.展开更多
Objective:To explore the main active components and mechanism of Guizhi Fuling pill in the treatment of ovarian cancer based on network pharmacology and molecular docking technology.Methods:TCMSP database was used to ...Objective:To explore the main active components and mechanism of Guizhi Fuling pill in the treatment of ovarian cancer based on network pharmacology and molecular docking technology.Methods:TCMSP database was used to retrieve and screen the active components of each Chinese medicine in Guizhi Fuling pill.The main active components of the medicine were screened through the network analysis function of Cytoscape software,and the target of the main active components of the medicine was found in UniProt database.Using genecards,OMIM,digsee,TTD,and drugbank database to retrieve the related targets of ovarian cancer.The interaction between the target of the main active components of the drug and the related target of ovarian cancer was obtained by R software.The intersection targets are imported into string database for PPI analysis,and then the results are imported into Cytoscape to get the hub gene using the cyclohubba plug-in.KEGG pathway analysis and go enrichment analysis were carried out in metascape database.At last,autodock tools was used to verify the main active ingredients and the selected target proteins.PyMOL and LigPlus software visualized the results.Results:The main active components of Guizhi Fuling pills were quercetin,β-sitosterol,kaempferol,hederagenin,catechin,ellagic acid,stigmasterol and Douglas fir.There are 20 pivotal genes of drug effect on ovarian cancer,including VEGFA,AKT1,mapk8,Jun,MMP9,IL6,TNF,CXCL8,PTGS2,TP53,CASP3,mapk1,EGF,ESR1,EGFR,Myc,FOS,CCL2,CXCL8 and IL1B.According to KEGG pathway analysis,10 pathways with the highest correlation were found:cancer signaling pathway,MAPK signaling pathway,fluid shear stress and atherosclerosis,hepatitis B,trypanosomiasis,age-rage signaling pathway in diabetic complications,tumor necrosis factor signaling pathway,pertussis,IL-17 signaling pathway,and bladder cancer.Go enrichment analysis has screened out 10 important items in molecular biological function,cell components and biological process.The proteins encoded by IL6,mapk1,VEGFA,AKT1,TP53,TNF and CCL2 were used as targets to dock with the main active components of the drug respectively,and the best results were TNFαand ellagic acid.Conclusion:The main active components of Guizhi Fuling pill regulate multiple signal pathways by regulating IL6,VEGFA,CCL2,TNF,MMP9 and other cytokines,and inhibit the proliferation and metastasis of cancer cells.展开更多
Objective:To investigate the mechanism of action of Guizhi Fuling pill in the treatment of atherosclerosis with network pharmacology.Methods:The active components of Guizhi Fuling pill were screened by specific ADME f...Objective:To investigate the mechanism of action of Guizhi Fuling pill in the treatment of atherosclerosis with network pharmacology.Methods:The active components of Guizhi Fuling pill were screened by specific ADME features on Traditional Chinese Medicine Systems Pharmacology platform,and their targets were obtained.Targets of atherosclerosis were extracted and screened from GeneCards database,OMIM database,DrugBank database and DisGeNET database,and the intersection of component targets and disease targets were regarded as potential targets.The protein-protein interaction network of potential targets was constructed by STRING database and Cytoscape 3.7.2.GO analysis and KEGG pathway analysis of potential targets were performed by Metascape platform.The“drugs-componenst-targets-pathways”network was constructed by Cytoscape 3.7.2.SwissDock was used for molecular docking of active components and key targets.Results:The main components of Guizhi Fuling pill in the treatment of atherosclerosis were quercetin,beta-sitosterol,kaempfero,hederagenin,baicalein,etc.The key targets mainly included PGST2,RELA,AKT1,etc.Molecular docking analysis showed that the binding energy of the main active components to the core target was less than-7 kcal/mol.The associated pathways mainly included fluid shear stress and atherosclerosis,PI3K-Akt signaling pathway and AGE-RAGE signaling pathway.Conclusion:Through this study,we initially revealed the possible mechanism of Guizhi Fuling pill in treating atherosclerosis through anti-inflammatory,reducing blood lipids,and regulating endothelial function.展开更多
Objective:To investigate the effect of Guizhi Fuling Capsule on sex hormones and tumor markers in patients with uterine fibroids, and observe its clinical efficacy.Methods: A total of 120 patients with uterine fibroid...Objective:To investigate the effect of Guizhi Fuling Capsule on sex hormones and tumor markers in patients with uterine fibroids, and observe its clinical efficacy.Methods: A total of 120 patients with uterine fibroids who were treated in our hospital from August 2016 to August 2017 were selected according to the order of treatment and divided into observation group and control group, 60 cases each. Mifepristone was administered to the control group and mifepristone combined with Guizhi Fuling Capsules was administered to the observation group. The levels of hemoglobin, vascular endothelial growth factor (VEGF), sex hormones, tumor markers, and inflammatory factors before and after treatment were compared between the two groups.Result:The levels of hemoglobin, vascular endothelial growth factor (VEGF), sex hormones, tumor markers, and inflammatory factors before and after treatment were compared between the two groups. After treatment, hemoglobin levels increased significantly in the two groups, VEGF, sex hormones FSH, LH and E2, tumor markers HE4, CA125, inflammatory cytokines TNF-α and IFN-γ levels decreased significantly. The hemoglobin level of the observation group was (117.09±11.51) g/L higher than that of the control group , and the level of VEGF was (0.69±0.06) pg/mL lower than that of the control group. The levels of sex hormone FSH, LH and E2 in the observation group were (15.87±1.56) U/L, (10.69±1.06) U/L and (4.95±0.51) pmol/L lower than those of the control group. The levels of HE4, CA125, TNF-α and IFN-γ gamma in the observation group were (52.47±5.24) pmol/L, (15.46±1.53) U/mL, (40.41±4.05) and (16.72±1.62) pg/mL lower than those of the control group.Conclusion:Guizhi Fuling Capsule can significantly improve the level of sex hormones and tumor markers, relieve inflammatory stress and improve the therapeutic effect.展开更多
Objective To observe the effects of Guizhi Fuling capsule(GZFLC)on RPMI 8226 cells and explore the mechanisms.Methods Cell Counting Kit-8(CCK-8)assays and flow cytometry were used to detect the viability and apoptosis...Objective To observe the effects of Guizhi Fuling capsule(GZFLC)on RPMI 8226 cells and explore the mechanisms.Methods Cell Counting Kit-8(CCK-8)assays and flow cytometry were used to detect the viability and apoptosis levels of RPMI 8226 cells.The effects on mitochondria were examined by ROS and JC-1 assays.Western blotting was used to detect the expression of B cell lymphoma-2(Bcl-2),Bax,cleaved caspase-3,and Apoptotic protease-activating factor 1(Apaf-1).Results GZFLC drug serum decreased the viability and increased the apoptosis of RPMI 8226 cells.In addition,this drug increased ROS levels and decreased the mitochondrial membrane potential(MMP).Western blotting showed that the Bcl-2/Bax ratios were decreased in the GZFLC drug serum-treated groups,whereas the expression levels of cleaved caspase-3 and Apaf-1 were increased.Conclusion GZFLC promoted apoptosis of myeloma cells through the mitochondrial apoptosis pathway.展开更多
桂枝茯苓丸出自《金匮要略》,为临床常用经方,具有温经活血、化瘀通络的功效,广泛用于盆腔炎性疾病后遗症(sequelae of pelvic inflammatory diseases,SPID)的治疗。SPID主要表现为盆腔内组织广泛增生、粘连,形成瘢痕,容易导致输卵管的...桂枝茯苓丸出自《金匮要略》,为临床常用经方,具有温经活血、化瘀通络的功效,广泛用于盆腔炎性疾病后遗症(sequelae of pelvic inflammatory diseases,SPID)的治疗。SPID主要表现为盆腔内组织广泛增生、粘连,形成瘢痕,容易导致输卵管的堵塞,进而发展为不孕症。其病因及发病机制多与免疫、病原体感染等多种因素相关。动物实验及临床研究均表明桂枝茯苓丸治疗SPID具有多层次、多途径、多靶点的优势。在临床应用上,桂枝茯苓丸化裁或其中成药联合常规西医治疗SPID效果明确,能明显改善患者症状及体征,并可有效地控制疾病的发展,提高病人的生活质量,不良反应小,安全性高。但该方的实验手段、研究方案等尚需改进,其作用机制也需进一步研究。该文通过查阅和整理有关文献,对近几年来桂枝茯苓丸治疗SPID的机制和临床研究成果进行了系统性的归纳和综合分析,同时也对其存在的缺陷提出建议。以期为桂枝茯苓丸的进一步应用提供理论和数据支持,并为其在临床上的合理使用提供实践指导。展开更多
文摘This paper reviews the research progress of Guizhi Fuling Pill in the clinical application of gynecology,such as the treatment of uterine leiomyoma,ovarian cyst,infertility and dysmenorrhea,in order to provide further research ideas for clinical researchers.
基金supported by National Science and Technology Major Projects of China(2013ZX09402203,2013ZX09508104)Medical and Health Science and Technology Innovation Engineering of Chinese Academy of Medical Sciences(2016-I2M-3-007)National Natural Science Foundation of China(81573454)
文摘OBJECTIVE To evaluate the effect of Guizhi Fuling Capsule active pharmaceutical ingredient(API)and its fractions on human breast cancer cells proliferation by high-throughput screening assay.METHODS The crude fractions were obtained from the extraction and elution of the API of Guizhi Fuling Capsule,and 929 standard fractions were obtained by the optimal separation conditions.Sulforhodamine B(SRB)method was used to evaluate the effects of the Guizhi Fuling capsule API and929 kinds of fractions on the proliferation of human breast cancer cells MCF-7 and MDA-MB-231.RESULTS The Guizhi Fuling capsule API had a strong ability to inhibit the proliferation of MCF-7 cells at high concentration and the ability to inhibit MDA-MB-231 cells' proliferate at low concentration following 72 h treatment;some samples of 929 fractions(5μg·mL^(-1))was found to have a breast cancer cell growth inhibition rate above 50%,without toxicity on HUVECs proliferation.CONCLUSION The API of Guizhi Fuling capsule had significant cytotoxicity effects on these two human breast cancer cells,with significant concentration-and time-dependent manner.
基金National Natural Science Foundation of China(No.81473566)。
文摘Objective:To explore the main active components and mechanism of Guizhi Fuling pill in the treatment of ovarian cancer based on network pharmacology and molecular docking technology.Methods:TCMSP database was used to retrieve and screen the active components of each Chinese medicine in Guizhi Fuling pill.The main active components of the medicine were screened through the network analysis function of Cytoscape software,and the target of the main active components of the medicine was found in UniProt database.Using genecards,OMIM,digsee,TTD,and drugbank database to retrieve the related targets of ovarian cancer.The interaction between the target of the main active components of the drug and the related target of ovarian cancer was obtained by R software.The intersection targets are imported into string database for PPI analysis,and then the results are imported into Cytoscape to get the hub gene using the cyclohubba plug-in.KEGG pathway analysis and go enrichment analysis were carried out in metascape database.At last,autodock tools was used to verify the main active ingredients and the selected target proteins.PyMOL and LigPlus software visualized the results.Results:The main active components of Guizhi Fuling pills were quercetin,β-sitosterol,kaempferol,hederagenin,catechin,ellagic acid,stigmasterol and Douglas fir.There are 20 pivotal genes of drug effect on ovarian cancer,including VEGFA,AKT1,mapk8,Jun,MMP9,IL6,TNF,CXCL8,PTGS2,TP53,CASP3,mapk1,EGF,ESR1,EGFR,Myc,FOS,CCL2,CXCL8 and IL1B.According to KEGG pathway analysis,10 pathways with the highest correlation were found:cancer signaling pathway,MAPK signaling pathway,fluid shear stress and atherosclerosis,hepatitis B,trypanosomiasis,age-rage signaling pathway in diabetic complications,tumor necrosis factor signaling pathway,pertussis,IL-17 signaling pathway,and bladder cancer.Go enrichment analysis has screened out 10 important items in molecular biological function,cell components and biological process.The proteins encoded by IL6,mapk1,VEGFA,AKT1,TP53,TNF and CCL2 were used as targets to dock with the main active components of the drug respectively,and the best results were TNFαand ellagic acid.Conclusion:The main active components of Guizhi Fuling pill regulate multiple signal pathways by regulating IL6,VEGFA,CCL2,TNF,MMP9 and other cytokines,and inhibit the proliferation and metastasis of cancer cells.
基金This study was supported by National Science Foundation of China(81973645,81673805,81704058,and 81774100)Natural Science Foundation of Guangdong(2019A1515011560)Traditional Chinese Medicine Bureau of Guangdong Province(20161167,20201392).
文摘Objective:To investigate the mechanism of action of Guizhi Fuling pill in the treatment of atherosclerosis with network pharmacology.Methods:The active components of Guizhi Fuling pill were screened by specific ADME features on Traditional Chinese Medicine Systems Pharmacology platform,and their targets were obtained.Targets of atherosclerosis were extracted and screened from GeneCards database,OMIM database,DrugBank database and DisGeNET database,and the intersection of component targets and disease targets were regarded as potential targets.The protein-protein interaction network of potential targets was constructed by STRING database and Cytoscape 3.7.2.GO analysis and KEGG pathway analysis of potential targets were performed by Metascape platform.The“drugs-componenst-targets-pathways”network was constructed by Cytoscape 3.7.2.SwissDock was used for molecular docking of active components and key targets.Results:The main components of Guizhi Fuling pill in the treatment of atherosclerosis were quercetin,beta-sitosterol,kaempfero,hederagenin,baicalein,etc.The key targets mainly included PGST2,RELA,AKT1,etc.Molecular docking analysis showed that the binding energy of the main active components to the core target was less than-7 kcal/mol.The associated pathways mainly included fluid shear stress and atherosclerosis,PI3K-Akt signaling pathway and AGE-RAGE signaling pathway.Conclusion:Through this study,we initially revealed the possible mechanism of Guizhi Fuling pill in treating atherosclerosis through anti-inflammatory,reducing blood lipids,and regulating endothelial function.
文摘Objective:To investigate the effect of Guizhi Fuling Capsule on sex hormones and tumor markers in patients with uterine fibroids, and observe its clinical efficacy.Methods: A total of 120 patients with uterine fibroids who were treated in our hospital from August 2016 to August 2017 were selected according to the order of treatment and divided into observation group and control group, 60 cases each. Mifepristone was administered to the control group and mifepristone combined with Guizhi Fuling Capsules was administered to the observation group. The levels of hemoglobin, vascular endothelial growth factor (VEGF), sex hormones, tumor markers, and inflammatory factors before and after treatment were compared between the two groups.Result:The levels of hemoglobin, vascular endothelial growth factor (VEGF), sex hormones, tumor markers, and inflammatory factors before and after treatment were compared between the two groups. After treatment, hemoglobin levels increased significantly in the two groups, VEGF, sex hormones FSH, LH and E2, tumor markers HE4, CA125, inflammatory cytokines TNF-α and IFN-γ levels decreased significantly. The hemoglobin level of the observation group was (117.09±11.51) g/L higher than that of the control group , and the level of VEGF was (0.69±0.06) pg/mL lower than that of the control group. The levels of sex hormone FSH, LH and E2 in the observation group were (15.87±1.56) U/L, (10.69±1.06) U/L and (4.95±0.51) pmol/L lower than those of the control group. The levels of HE4, CA125, TNF-α and IFN-γ gamma in the observation group were (52.47±5.24) pmol/L, (15.46±1.53) U/mL, (40.41±4.05) and (16.72±1.62) pg/mL lower than those of the control group.Conclusion:Guizhi Fuling Capsule can significantly improve the level of sex hormones and tumor markers, relieve inflammatory stress and improve the therapeutic effect.
基金This work was supported by the National Natural Science Foundation of China(No.82074348)the Taishan Scholar Project(tsqn201812145)the Key Technology Research and Development Program of Shandong(No.2019GSF108162).
文摘Objective To observe the effects of Guizhi Fuling capsule(GZFLC)on RPMI 8226 cells and explore the mechanisms.Methods Cell Counting Kit-8(CCK-8)assays and flow cytometry were used to detect the viability and apoptosis levels of RPMI 8226 cells.The effects on mitochondria were examined by ROS and JC-1 assays.Western blotting was used to detect the expression of B cell lymphoma-2(Bcl-2),Bax,cleaved caspase-3,and Apoptotic protease-activating factor 1(Apaf-1).Results GZFLC drug serum decreased the viability and increased the apoptosis of RPMI 8226 cells.In addition,this drug increased ROS levels and decreased the mitochondrial membrane potential(MMP).Western blotting showed that the Bcl-2/Bax ratios were decreased in the GZFLC drug serum-treated groups,whereas the expression levels of cleaved caspase-3 and Apaf-1 were increased.Conclusion GZFLC promoted apoptosis of myeloma cells through the mitochondrial apoptosis pathway.
文摘桂枝茯苓丸出自《金匮要略》,为临床常用经方,具有温经活血、化瘀通络的功效,广泛用于盆腔炎性疾病后遗症(sequelae of pelvic inflammatory diseases,SPID)的治疗。SPID主要表现为盆腔内组织广泛增生、粘连,形成瘢痕,容易导致输卵管的堵塞,进而发展为不孕症。其病因及发病机制多与免疫、病原体感染等多种因素相关。动物实验及临床研究均表明桂枝茯苓丸治疗SPID具有多层次、多途径、多靶点的优势。在临床应用上,桂枝茯苓丸化裁或其中成药联合常规西医治疗SPID效果明确,能明显改善患者症状及体征,并可有效地控制疾病的发展,提高病人的生活质量,不良反应小,安全性高。但该方的实验手段、研究方案等尚需改进,其作用机制也需进一步研究。该文通过查阅和整理有关文献,对近几年来桂枝茯苓丸治疗SPID的机制和临床研究成果进行了系统性的归纳和综合分析,同时也对其存在的缺陷提出建议。以期为桂枝茯苓丸的进一步应用提供理论和数据支持,并为其在临床上的合理使用提供实践指导。
