益母草活性成分芫花素对小鼠凝血及抗炎作用的研究
|
摘要
目的研究益母草中的活性物质芫花素对小鼠凝血及抗炎的药理作用。方法采用毛细玻管法及玻片法考察芫花素对小鼠凝血功能的影响;采用醋酸致小鼠疼痛扭体、二甲苯致小鼠耳廓肿胀及血管通透性模型研究芫花素的抗炎镇痛作用。结果芫花素中剂量、大剂量组小鼠凝血时间均较空白对照组明显缩短(P<0.05);芫花素中剂量组和模型对照组相比,小鼠凝血时间显著缩短(P<0.05);芫花素大剂量组与模型对照组相比较,扭体次数显著减少(P<0.01)。芫花素对二甲苯致小鼠耳廓肿胀的影响结果表明,阳性对照阿司匹林组与模型对照组比较,左右耳片重差值差异有统计学意义(P<0.01),芫花素大剂量组与模型对照组相比差异有统计学意义(P<0.05)。在芫花素对小鼠腹腔毛细血管通透性影响的试验中,阳性对照阿司匹林组与模型对照组比较,A值减小(P<0.01);芫花素小剂量组与模型对照组相比,A值无明显改变(P>0.05);芫花素中剂量组与模型对照组比较,A值显著减小(P<0.05);芫花素大剂量组较模型对照组A值显著减小(P<0.01)。结论芫花素可促进小鼠凝血功能;减少醋酸致小鼠扭体疼痛次数,有一定的镇痛作用;抑制二甲苯致小鼠耳廓肿胀及降低小鼠腹腔毛细血管通透性,具有一定的抗炎作用。这为其治疗痛经及子宫内膜炎等疾病提供了临床依据。
Objective To investigate the pharmacological effects of genkwanin,the active ingredient in Leonurus on coagulation and anti-inflammation in mice.Methods The body torsion pain caused by acetic acid model,auricle swelling induced by xylene,and the blood capillary permeability model were used to investigate the analgesic and anti-inflammatory effects of genkwanin in mice.Results The clotting time was significantly reduced in mediumand high-dose genkwanin groups compared with the control group(P<0.05).The times of mice's body torsion pain caused by acetic acid was significantly reduced at 10 minutes after administration in the large-dose group compared with the control group(P<0.01).Compared with the model group,the positive control(aspirin)group had a significant difference(P <0.01)in the difference value of left-and right-ear weights,the high-dose group had significant difference(P<0.05).In the experiment on the influence of genkwanin on blood capillary permeability of the mice abdominal cavity,compared with the model group,a marked decrease of A value(P<0.01)was found in the positive control group,but there was no significant difference of A value(P >0.05)in the low-dose genkwanin group,a significant reduce of A value(P<0.05)in the medium-dose group,and an extremely significant decrease of A value(P<0.01)in the high-dose group.Conclusion Genkwanin can promote blood coagulation function of mice,and reduce the times of their body torsion pain caused by acetic acid,showing obvious analgesic effects.Furthermore,genkwanin can inhibit auricle swelling of mice induced by xylene and reduce the blood capillary permeability of their abdominal cavity,suggesting its mild anti-inflammatory effects.The findings can provide clinical evidence for treating dysmenorrheal and endometritis.
Objective To investigate the pharmacological effects of genkwanin,the active ingredient in Leonurus on coagulation and anti-inflammation in mice.Methods The body torsion pain caused by acetic acid model,auricle swelling induced by xylene,and the blood capillary permeability model were used to investigate the analgesic and anti-inflammatory effects of genkwanin in mice.Results The clotting time was significantly reduced in mediumand high-dose genkwanin groups compared with the control group(P<0.05).The times of mice's body torsion pain caused by acetic acid was significantly reduced at 10 minutes after administration in the large-dose group compared with the control group(P<0.01).Compared with the model group,the positive control(aspirin)group had a significant difference(P <0.01)in the difference value of left-and right-ear weights,the high-dose group had significant difference(P<0.05).In the experiment on the influence of genkwanin on blood capillary permeability of the mice abdominal cavity,compared with the model group,a marked decrease of A value(P<0.01)was found in the positive control group,but there was no significant difference of A value(P >0.05)in the low-dose genkwanin group,a significant reduce of A value(P<0.05)in the medium-dose group,and an extremely significant decrease of A value(P<0.01)in the high-dose group.Conclusion Genkwanin can promote blood coagulation function of mice,and reduce the times of their body torsion pain caused by acetic acid,showing obvious analgesic effects.Furthermore,genkwanin can inhibit auricle swelling of mice induced by xylene and reduce the blood capillary permeability of their abdominal cavity,suggesting its mild anti-inflammatory effects.The findings can provide clinical evidence for treating dysmenorrheal and endometritis.
引文
[1]SHANG X,PAN H,WANG X,et al.Leonurus japonicus Houtt:Ethnopharmacology,phytochemistry and pharmacology of an important traditional Chinese medicine[J].J Ethnopharmacol,2014,152(1):14-32.
[2]FAN JB,WEI F,ZHANG Y,et al.Combining Sprague-Dawley rat uterus cell membrane chromatography with HPLC/MS to screen active components from Leonurus Artemisia[J].Pharm Biol,2016,54(2):279-284.
[3]DONG S,HE J,HOU H,et al.Quality assessment of Herba Leonuri based on the analysis of multiple components using normal-and reversed-phase chromatographic methods[J].J Sep Sci,2017,40(23):4482-4494.
[4]ALTINIER G,SOSA S,AQUINO RP,et al.Characterization of topical antiinflammatory compounds in Rosmarinusofficinalis L[J].Agric Food Chem,2007,55(5):1718-1723.
[5]YANG MX,LIANG YG,CHEN HR,et al.Isolation of flavonoids from wild aquilaria sinensis leaves by an improved preparative high-speed counter-current chromatography apparatus[J].J Chromatogr Sci,2018,56(1):18-24.
[6]WU H,DAI A,CHEN X,et al.Leonurine ameliorates the inflammatory responses in lipopolysaccharide-induced endometritis[J].Int Immunopharmacol,2018,61:156-161.
[7]HU YM,LIU WJ,LI MX,et al.Two new labdane diterpenoids from aerial parts of Leonurus japonicus and their anti-inflammatory activity[J].Nat Prod Res,2018,9:1-8.
[8]GAO Y,LIU F,FANG L,et al.Genkwanin inhibits proinflammatory mediators mainly through the regulation of miR-101/MKP-1/MAPK pathway in LPS-activated macrophages[J].PLoS One,2014,9(5):e96741.
[9]LUCARINI R,TOZATTI MG,SILVA ML,et al.Antibacterial and anti-inflammatory activities of an extract,fractions,and compounds isolated from Gochnatia pulchra aerial parts[J].Braz J Med Biol Res,2015,48(9):822-830.
[10]KRAFT C,JENETT-SIEMS K,SIEMS K,et al.In vitro antiplasmodial evaluation of medicinal plants from Zimbabwe[J].Phytother Res,2003,17(2):123-128.
[11]KIYEKBAYEVA L,MOHAMED NM,YERKEBULAN O,et al.Phytochemical constituents and antioxidant activity of Echinops albicaulis[J].Nat Prod Res,2018,32(10):1203-1207.
[12]ZHANG CF,ZHANG SL,HE X,et al.Antioxidant effects of Genkwa flos flavonoids on Freund's adjuvant-induced rheumatoid arthritis in rats[J].Ethnopharmacol,2014,153(3):793-800.
[13]NASR BOUZAIENE N,CHAABANE F,SASSI A,et al.Effect of apigenin-7-glucoside,genkwanin and naringenin on tyrosinase activity and melanin synthesis in B16F10melanoma cells[J].Life Sci,2016,144:80-85.
[14]LI Y,HONG J,LI H,et al.Genkwanin nanosuspensions:A novel and potential antitumor drug in breast carcinoma therapy[J].Drug Deliv,2017,24(1):1491-1500.
[15]WANG X,SONG ZJ,HE X,et al.Antitumor and immunomodulatory activity of genkwanin on colorectal cancer in the APC(Min/+)mice[J].Int Immunopharmacol,2015,29(2):701-707.
[16]SITAREK P,KOWALCZYK T,SANTANGELO S,et al.The extract of Leonurus sibiricus transgenic roots with AtPAP1transcriptional factor induces apoptosis via DNA damage and down regulation of selected epigenetic factors in human cancer cells[J].Neurochem Res,2018,43(7):1363-1370.
[17]ZHANG RH,LIU ZK,YANG DS,et al.Phytochemistry and pharmacology of the genus Leonurus:The herb to benefit the mothers and more[J].Phytochemistry,2018,147:167-183.
[18]XIONG L,PENG C,ZHOU QM,et al.Chemical composition and antibacterial activity of essential oils from different parts of Leonurus japonicus Houtt[J].Molecules,2013,18(1):963-973.
[19]TAHMOUZI S,GHODSI M.Optimum extraction of polysaccharides from motherwort leaf and its antioxidant and antimicrobial activities[J].Carbohydr Polym,2014,112:396-403.
[2]FAN JB,WEI F,ZHANG Y,et al.Combining Sprague-Dawley rat uterus cell membrane chromatography with HPLC/MS to screen active components from Leonurus Artemisia[J].Pharm Biol,2016,54(2):279-284.
[3]DONG S,HE J,HOU H,et al.Quality assessment of Herba Leonuri based on the analysis of multiple components using normal-and reversed-phase chromatographic methods[J].J Sep Sci,2017,40(23):4482-4494.
[4]ALTINIER G,SOSA S,AQUINO RP,et al.Characterization of topical antiinflammatory compounds in Rosmarinusofficinalis L[J].Agric Food Chem,2007,55(5):1718-1723.
[5]YANG MX,LIANG YG,CHEN HR,et al.Isolation of flavonoids from wild aquilaria sinensis leaves by an improved preparative high-speed counter-current chromatography apparatus[J].J Chromatogr Sci,2018,56(1):18-24.
[6]WU H,DAI A,CHEN X,et al.Leonurine ameliorates the inflammatory responses in lipopolysaccharide-induced endometritis[J].Int Immunopharmacol,2018,61:156-161.
[7]HU YM,LIU WJ,LI MX,et al.Two new labdane diterpenoids from aerial parts of Leonurus japonicus and their anti-inflammatory activity[J].Nat Prod Res,2018,9:1-8.
[8]GAO Y,LIU F,FANG L,et al.Genkwanin inhibits proinflammatory mediators mainly through the regulation of miR-101/MKP-1/MAPK pathway in LPS-activated macrophages[J].PLoS One,2014,9(5):e96741.
[9]LUCARINI R,TOZATTI MG,SILVA ML,et al.Antibacterial and anti-inflammatory activities of an extract,fractions,and compounds isolated from Gochnatia pulchra aerial parts[J].Braz J Med Biol Res,2015,48(9):822-830.
[10]KRAFT C,JENETT-SIEMS K,SIEMS K,et al.In vitro antiplasmodial evaluation of medicinal plants from Zimbabwe[J].Phytother Res,2003,17(2):123-128.
[11]KIYEKBAYEVA L,MOHAMED NM,YERKEBULAN O,et al.Phytochemical constituents and antioxidant activity of Echinops albicaulis[J].Nat Prod Res,2018,32(10):1203-1207.
[12]ZHANG CF,ZHANG SL,HE X,et al.Antioxidant effects of Genkwa flos flavonoids on Freund's adjuvant-induced rheumatoid arthritis in rats[J].Ethnopharmacol,2014,153(3):793-800.
[13]NASR BOUZAIENE N,CHAABANE F,SASSI A,et al.Effect of apigenin-7-glucoside,genkwanin and naringenin on tyrosinase activity and melanin synthesis in B16F10melanoma cells[J].Life Sci,2016,144:80-85.
[14]LI Y,HONG J,LI H,et al.Genkwanin nanosuspensions:A novel and potential antitumor drug in breast carcinoma therapy[J].Drug Deliv,2017,24(1):1491-1500.
[15]WANG X,SONG ZJ,HE X,et al.Antitumor and immunomodulatory activity of genkwanin on colorectal cancer in the APC(Min/+)mice[J].Int Immunopharmacol,2015,29(2):701-707.
[16]SITAREK P,KOWALCZYK T,SANTANGELO S,et al.The extract of Leonurus sibiricus transgenic roots with AtPAP1transcriptional factor induces apoptosis via DNA damage and down regulation of selected epigenetic factors in human cancer cells[J].Neurochem Res,2018,43(7):1363-1370.
[17]ZHANG RH,LIU ZK,YANG DS,et al.Phytochemistry and pharmacology of the genus Leonurus:The herb to benefit the mothers and more[J].Phytochemistry,2018,147:167-183.
[18]XIONG L,PENG C,ZHOU QM,et al.Chemical composition and antibacterial activity of essential oils from different parts of Leonurus japonicus Houtt[J].Molecules,2013,18(1):963-973.
[19]TAHMOUZI S,GHODSI M.Optimum extraction of polysaccharides from motherwort leaf and its antioxidant and antimicrobial activities[J].Carbohydr Polym,2014,112:396-403.