[Objectives] To study the effects of Mangiferin( MGF) on TNF-α,iNOS,ICAM-1 and its mRNA expression in the heart,brain and kidneys of spontaneously hypertensive rats( SHR),and reveal the mechanism of its anti-inflamma...[Objectives] To study the effects of Mangiferin( MGF) on TNF-α,iNOS,ICAM-1 and its mRNA expression in the heart,brain and kidneys of spontaneously hypertensive rats( SHR),and reveal the mechanism of its anti-inflammatory injury in hypertension target organs.[Methods]SHRs were randomly divided into 5 groups: the model group,the high-dose,medium-dose,low-dose MGF groups and the Benazepril group,with 8 rats in each group,WKY rats were used for the normal control group. Besides,on-invasive blood pressure( BP) instruments were used to measure systolic blood pressure in the rats' tail artery,western blot was used to analyze the expression of TNF-α,iNOS,ICAM-1 and reverse transcription-polymerase chain reaction( RT-PCR) was used to analyze the expression of TNF-α,iNOS,ICAM-1 mRNA.[Results]Compared with the normal control group,the model group's BP level was significantly increased( P <0. 01)),but the MGF had no significant lowering BP effect( P > 0. 05); compared with the normal control group,the expression of TNF-α,iNOS,ICAM-1 and its' mRNA in the model group was significantly increased( P < 0. 05 or P < 0. 01),and MGF could reduce the level of expression of these inflammatory cytokines( P < 0. 05 or P < 0. 01); between the Benazepril group and high-dose,medium-dose,low-dose MGF groups,most of the indicators had no significant difference( P > 0. 05). [Conclusions]MGF had no significant lowering BP effect,SHR showed inflammatory injury in the heart,brain and kidneys,MGF showed improvement on the inflammatory injury,and the anti-inflammation mechanism may be associated with lowering TNF-α,i NOS and ICAM-1 and its mRNA expression.展开更多
[Objectives]The anti-tumor,anti-bacterial,anti-acetylcholinesterase and anti-α-glucosidase activity in vitro of five chromenes isolated from Helianthus annuus disk was studied,in order to provide reference for the de...[Objectives]The anti-tumor,anti-bacterial,anti-acetylcholinesterase and anti-α-glucosidase activity in vitro of five chromenes isolated from Helianthus annuus disk was studied,in order to provide reference for the development and utilization of H.annuus disk resources.[Methods]The effect of different concentrations of chromenes on the survival rate of leukemia HL-60 cells,lung cancer A549 cells,liver cancer SMMC-7721 cells,breast cancer MCF-7 cells and colon cancer SW480 cells was detected by MTS method,and the IC50 was calculated.The inhibitory activity of chromenes against Escherichia coli,Staphylococcus aureus subsp.aureus,Salmonella enterica subsp.enterica,Pseudomonas aeruginosa and Candida albicans was detected by microdilution method.The DTNB substrate method was used to detect the inhibitory activity of chromenes on acetylcholine.The PNPG substrate method was used to detect the inhibitory activity of chromenes onα-glucosidase.[Results]The five chromenes had no obvious in vitro inhibitory activity on the five kinds of tumor cells,with IC50 greater than 40μM.The five chromenes had no obvious in vitro inhibitory activity against the four kinds of bacteria and C.albicans.The five chromenes had certain inhibitory activity on acetylcholinesterase,and among them,6-acetyl-2,2-dimethylchromene and 6-acetyl-7-hydroxy-2,3-dimethylchromene showed strong inhibitory activity on acetylcholinesterase,with IC50 of 28.253 and 16.945μM,respectively,both smaller than that(0.275μM)of the positive control tacrine(P<0.01).The five chromenes showed good inhibitory effect onα-glucosidase,and among them,7-hydroxy-6-hydroxyacetyl-2,2-dimethylchromene and 6-acetyl-7-hydroxy-2,3-dimethylchromene had stronger inhibitory activity,with IC50 of 20.240 and 21.052μM,respectively,significantly better than that(169.780μM)of the positive control acarbose(P<0.01).[Conclusions]The five chromenes in H.annuus disk have certain in vitro inhibitory activity against acetylcholinesterase andα-glucosidase and certain potential in fighting neurodegenerative diseases and diabetes.展开更多
Objective: Hypertension is a low-grade infammation state of the disease and was easily complicated by kidneys’ infammatory response. Mangiferin(MGF), a pharmacologically active compound in various plants including Ma...Objective: Hypertension is a low-grade infammation state of the disease and was easily complicated by kidneys’ infammatory response. Mangiferin(MGF), a pharmacologically active compound in various plants including Mangifera indica, has a strong anti-infammatory activity. However, the effects of MGF on renal infammatory injury in spontaneously hypertensive rats(SHRs) remain unclear. The purpose of this study was to investigate the protective effects and mechanisms of MGF on renal infammatory injury in SHRs.Methods: MGF was used in SHRs at the doses of 10, 20, 40 mg/kg/d for 8 weeks consecutively. The blood and urine were collected for assessment of renal function. Renal tissues were collected for histological,immunohistochemistry, ELISA, Western blot and real time reverse transcription PCR(RT-PCR) analysis.Results: The results showed that the levels of interleukin 6(IL-6), tumor necrosis factor-a(TNF-a), monocyte chemoattractant protein-1(MCP-1) and recombinant chemokine C-C-Motif receptor 2(CCR2) were increased in SHRs, meanwhile, the level of IL-10 was decreased in SHR. Treatment of MGF inhibited the expression of IL-6, TNF-a, MCP-1 and CCR2, and promoted the expression of IL-10. Furthermore, the content of blood urea nitrogen(BUN) and serum uric acid(SUA) was significantly increased in the model group, and treatment of MGF had no obvious effects on these parameters at all dose levels.Conclusion: Our study proved that the kidneys of SHRs had significant infammatory injury, and MGF had the protective effects on renal infammatory injury in SHRs;The protective mechanism may be mediated partly by the MCP-1/CCR2 signaling pathway. Thus, it is a potential new drug for the treatment of hypertension.展开更多
Zedoary tumeric(Curcumae Rhizoma,Ezhu in Chinese)has a long history of application and has great potential in the treatment of liver cancer.The antiliver cancer effect of zedoary tumeric depends on the combined action...Zedoary tumeric(Curcumae Rhizoma,Ezhu in Chinese)has a long history of application and has great potential in the treatment of liver cancer.The antiliver cancer effect of zedoary tumeric depends on the combined action of multiple pharmacodynamic substances.In order to clarify the specific mechanism of zedoary tumeric against liver cancer,this paper first analyzes the mechanism of its single pharmacodynamic substance against liver cancer,and then verifies the joint anti liver cancer mechanism of its“pharmacodynamic group”.By searching the research on the antihepatoma effect of active components of zedoary tumeric in recent years,we found that pharmacodynamic substances,including curcumol,zedoarondiol,curcumenol,curzerenone,curdione,curcumin,germacrone,β-elemene,can act on multi-target and multi-channel to play an antihepatoma role.For example,curcumin can regulate miR,GLO1,CD133,VEGF,YAP,LIN28B,GPR81,HCAR-1,P53 and PI3K/Akt/mTOR,HSP70/TLR4 and NF-κB.Wnt/TGF/EMT,Nrf2/Keap1,JAK/STAT and other pathways play an antihepatoma role.Network pharmacological analysis showed that the core targets of the“pharmacodynamic group”for anti-life cancer are AKT1,EGFR,MAPK8,etc,and the core pathways are neuroactive live receiver interaction,nitrogen metabolism,HIF-1 signaling pathway,etc.At the same time,by comparing and analyzing the relationship between the specific mechanisms of pharmacodynamic substance and“pharmacodynamic group”,it is found that they have great reference significance in target,pathway,biological function,determination of core pharmacodynamic components,formation of core target protein interaction,in-depth research of single pharmacodynamic substance,increasing curative effect and so on.By analyzing the internal mechanism of zedoary tumeric pharmacodynamic substance and“pharmacodynamic group”in the treatment of liver cancer,this paper intends to provide some ideas and references for the deeper pharmacological research of zedoary tumeric and the relationship between pharmacodynamic substance and“pharmacodynamic group”.展开更多
Over the past few decades, the determination of antioxidant activity by chemical probe has been widely reported, but in vivo evaluation via model organisms of Drosophila melanogaster and rapid discovery system has not...Over the past few decades, the determination of antioxidant activity by chemical probe has been widely reported, but in vivo evaluation via model organisms of Drosophila melanogaster and rapid discovery system has not been studied adequately. In this study, we determined the antioxidant activity of lees and demonstrated the ability of compounds in lees to scavenge H_2O_2 in vitro and in vivo by different chemical probes. Lees increased the ability of Drosophila against oxidative stress and antioxidant enzyme activity in vivo. Five ingredients of organic acids and flavones in lees extract that rapidly scavenged H_2O_2 were revealed by a post-column-derived HPLC-UV-FLD system based on 4-hydroxyphenylacetic acid(PHPAA)chemiluminescence. Additionally, another fluorescent probe,N-borylbenzyloxycarbonyl-3,7-dihydroxyphenoxazine(NBCD), was selected to evaluate the reactive oxygen species(ROS) scavenging capacity of lees in living Drosophila melanogaster using a microfluidic injection test coupled with microscopic imaging analysis, and similar effects were observed in flies when they were treated with tartaric acid and caffeic acid. The results demonstrated that the novel integrated system was suitable for screening and evaluating antioxidant ingredients from natural products.展开更多
基金Supported by the Guangxi Science and Technology Infrastructure Construction Project of China(09-007-06)
文摘[Objectives] To study the effects of Mangiferin( MGF) on TNF-α,iNOS,ICAM-1 and its mRNA expression in the heart,brain and kidneys of spontaneously hypertensive rats( SHR),and reveal the mechanism of its anti-inflammatory injury in hypertension target organs.[Methods]SHRs were randomly divided into 5 groups: the model group,the high-dose,medium-dose,low-dose MGF groups and the Benazepril group,with 8 rats in each group,WKY rats were used for the normal control group. Besides,on-invasive blood pressure( BP) instruments were used to measure systolic blood pressure in the rats' tail artery,western blot was used to analyze the expression of TNF-α,iNOS,ICAM-1 and reverse transcription-polymerase chain reaction( RT-PCR) was used to analyze the expression of TNF-α,iNOS,ICAM-1 mRNA.[Results]Compared with the normal control group,the model group's BP level was significantly increased( P <0. 01)),but the MGF had no significant lowering BP effect( P > 0. 05); compared with the normal control group,the expression of TNF-α,iNOS,ICAM-1 and its' mRNA in the model group was significantly increased( P < 0. 05 or P < 0. 01),and MGF could reduce the level of expression of these inflammatory cytokines( P < 0. 05 or P < 0. 01); between the Benazepril group and high-dose,medium-dose,low-dose MGF groups,most of the indicators had no significant difference( P > 0. 05). [Conclusions]MGF had no significant lowering BP effect,SHR showed inflammatory injury in the heart,brain and kidneys,MGF showed improvement on the inflammatory injury,and the anti-inflammation mechanism may be associated with lowering TNF-α,i NOS and ICAM-1 and its mRNA expression.
基金Natural Science Foundation of Guangxi(General Program No.2020GXNSFAA238033)Guangxi Collaborative Innovation Center of Study on Functional Ingredients of Agricultural Residues(CICAR2019-P4)+1 种基金Guangxi Key Laboratory of Pharmacodynamics Research of Traditional Chinese Medicine(19-050-39)Key Laboratory of Chinese Medicine Extraction,Purification and Quality Analysis in Guangxi Universities(Gui Jiao Ke Yan[2014]6).
文摘[Objectives]The anti-tumor,anti-bacterial,anti-acetylcholinesterase and anti-α-glucosidase activity in vitro of five chromenes isolated from Helianthus annuus disk was studied,in order to provide reference for the development and utilization of H.annuus disk resources.[Methods]The effect of different concentrations of chromenes on the survival rate of leukemia HL-60 cells,lung cancer A549 cells,liver cancer SMMC-7721 cells,breast cancer MCF-7 cells and colon cancer SW480 cells was detected by MTS method,and the IC50 was calculated.The inhibitory activity of chromenes against Escherichia coli,Staphylococcus aureus subsp.aureus,Salmonella enterica subsp.enterica,Pseudomonas aeruginosa and Candida albicans was detected by microdilution method.The DTNB substrate method was used to detect the inhibitory activity of chromenes on acetylcholine.The PNPG substrate method was used to detect the inhibitory activity of chromenes onα-glucosidase.[Results]The five chromenes had no obvious in vitro inhibitory activity on the five kinds of tumor cells,with IC50 greater than 40μM.The five chromenes had no obvious in vitro inhibitory activity against the four kinds of bacteria and C.albicans.The five chromenes had certain inhibitory activity on acetylcholinesterase,and among them,6-acetyl-2,2-dimethylchromene and 6-acetyl-7-hydroxy-2,3-dimethylchromene showed strong inhibitory activity on acetylcholinesterase,with IC50 of 28.253 and 16.945μM,respectively,both smaller than that(0.275μM)of the positive control tacrine(P<0.01).The five chromenes showed good inhibitory effect onα-glucosidase,and among them,7-hydroxy-6-hydroxyacetyl-2,2-dimethylchromene and 6-acetyl-7-hydroxy-2,3-dimethylchromene had stronger inhibitory activity,with IC50 of 20.240 and 21.052μM,respectively,significantly better than that(169.780μM)of the positive control acarbose(P<0.01).[Conclusions]The five chromenes in H.annuus disk have certain in vitro inhibitory activity against acetylcholinesterase andα-glucosidase and certain potential in fighting neurodegenerative diseases and diabetes.
基金supported by Natural Science Foundation of Guangxi Province (No. 2013GXNSFAA019114)Guangxi Key Laboratory of Efficacy Study on Chinese Materia Medica Project (No. 12-071-08)。
文摘Objective: Hypertension is a low-grade infammation state of the disease and was easily complicated by kidneys’ infammatory response. Mangiferin(MGF), a pharmacologically active compound in various plants including Mangifera indica, has a strong anti-infammatory activity. However, the effects of MGF on renal infammatory injury in spontaneously hypertensive rats(SHRs) remain unclear. The purpose of this study was to investigate the protective effects and mechanisms of MGF on renal infammatory injury in SHRs.Methods: MGF was used in SHRs at the doses of 10, 20, 40 mg/kg/d for 8 weeks consecutively. The blood and urine were collected for assessment of renal function. Renal tissues were collected for histological,immunohistochemistry, ELISA, Western blot and real time reverse transcription PCR(RT-PCR) analysis.Results: The results showed that the levels of interleukin 6(IL-6), tumor necrosis factor-a(TNF-a), monocyte chemoattractant protein-1(MCP-1) and recombinant chemokine C-C-Motif receptor 2(CCR2) were increased in SHRs, meanwhile, the level of IL-10 was decreased in SHR. Treatment of MGF inhibited the expression of IL-6, TNF-a, MCP-1 and CCR2, and promoted the expression of IL-10. Furthermore, the content of blood urea nitrogen(BUN) and serum uric acid(SUA) was significantly increased in the model group, and treatment of MGF had no obvious effects on these parameters at all dose levels.Conclusion: Our study proved that the kidneys of SHRs had significant infammatory injury, and MGF had the protective effects on renal infammatory injury in SHRs;The protective mechanism may be mediated partly by the MCP-1/CCR2 signaling pathway. Thus, it is a potential new drug for the treatment of hypertension.
基金supported by the National Natural Science Foundation of China(Grant No.82060762)China ASEAN Joint Laboratory for International Cooperation in Traditional Medicine Research(phase II)New Center Construction Project(Grant Nocicar2017-z1)Guangxi Innovation-driven Major Project(Grant No.guike aa181180492 and aa192540334)。
文摘Zedoary tumeric(Curcumae Rhizoma,Ezhu in Chinese)has a long history of application and has great potential in the treatment of liver cancer.The antiliver cancer effect of zedoary tumeric depends on the combined action of multiple pharmacodynamic substances.In order to clarify the specific mechanism of zedoary tumeric against liver cancer,this paper first analyzes the mechanism of its single pharmacodynamic substance against liver cancer,and then verifies the joint anti liver cancer mechanism of its“pharmacodynamic group”.By searching the research on the antihepatoma effect of active components of zedoary tumeric in recent years,we found that pharmacodynamic substances,including curcumol,zedoarondiol,curcumenol,curzerenone,curdione,curcumin,germacrone,β-elemene,can act on multi-target and multi-channel to play an antihepatoma role.For example,curcumin can regulate miR,GLO1,CD133,VEGF,YAP,LIN28B,GPR81,HCAR-1,P53 and PI3K/Akt/mTOR,HSP70/TLR4 and NF-κB.Wnt/TGF/EMT,Nrf2/Keap1,JAK/STAT and other pathways play an antihepatoma role.Network pharmacological analysis showed that the core targets of the“pharmacodynamic group”for anti-life cancer are AKT1,EGFR,MAPK8,etc,and the core pathways are neuroactive live receiver interaction,nitrogen metabolism,HIF-1 signaling pathway,etc.At the same time,by comparing and analyzing the relationship between the specific mechanisms of pharmacodynamic substance and“pharmacodynamic group”,it is found that they have great reference significance in target,pathway,biological function,determination of core pharmacodynamic components,formation of core target protein interaction,in-depth research of single pharmacodynamic substance,increasing curative effect and so on.By analyzing the internal mechanism of zedoary tumeric pharmacodynamic substance and“pharmacodynamic group”in the treatment of liver cancer,this paper intends to provide some ideas and references for the deeper pharmacological research of zedoary tumeric and the relationship between pharmacodynamic substance and“pharmacodynamic group”.
基金financially supported by the Collaborative Innovation Center of Research on Functional Ingredients from Agricultural Residues (Guangxi University of Chinese medicine,No. CICAR 2015-B2)
文摘Over the past few decades, the determination of antioxidant activity by chemical probe has been widely reported, but in vivo evaluation via model organisms of Drosophila melanogaster and rapid discovery system has not been studied adequately. In this study, we determined the antioxidant activity of lees and demonstrated the ability of compounds in lees to scavenge H_2O_2 in vitro and in vivo by different chemical probes. Lees increased the ability of Drosophila against oxidative stress and antioxidant enzyme activity in vivo. Five ingredients of organic acids and flavones in lees extract that rapidly scavenged H_2O_2 were revealed by a post-column-derived HPLC-UV-FLD system based on 4-hydroxyphenylacetic acid(PHPAA)chemiluminescence. Additionally, another fluorescent probe,N-borylbenzyloxycarbonyl-3,7-dihydroxyphenoxazine(NBCD), was selected to evaluate the reactive oxygen species(ROS) scavenging capacity of lees in living Drosophila melanogaster using a microfluidic injection test coupled with microscopic imaging analysis, and similar effects were observed in flies when they were treated with tartaric acid and caffeic acid. The results demonstrated that the novel integrated system was suitable for screening and evaluating antioxidant ingredients from natural products.