High blood pressure is the main risk factor for cardiovascular diseases, it affects many people worldwide and is a public health problem. This study explored the acute and chronic actions of a mixture of turmeric (95%...High blood pressure is the main risk factor for cardiovascular diseases, it affects many people worldwide and is a public health problem. This study explored the acute and chronic actions of a mixture of turmeric (95% curcumin) plus black pepper (95% piperine) extracts, in the blood pressure pattern in spontaneously hypertensive rats (SHR) along they age. For the acute study male adult (4 - 7 months old) SHR and their control Wistar Kyoto rats (WKY) were used. A single oral dose of the mixture of turmeric/black pepper extracts (200 mg/2mg, respectively) suspension was administered. Tail-cuff was used to determine blood pressure during 180 min. For the chronic study, young (1-month-old) male SHR and their control WKY rats were fed with standard chow, or standard chow combined with cocoa, or combined with cocoa plus the mixture of turmeric/black pepper extracts;tail-cuff was used to determine blood pressure once a week, along 12 weeks. In a second chronic assay adult (5 months old) male SHR and their control WKY rats were fed with standard chow, or standard chow combined with cocoa, or combined with cocoa plus the mixture of turmeric/black pepper extracts;tail-cuff was used to determine blood pressure once a week, along 12 weeks. In all three studies, a decrease in systolic, diastolic and mean blood pressure was observed, being higher in SHR and negligible in WKY rats. The mixture of turmeric/black pepper extracts showed antihypertensive actions in SHR rats with no effect on WKY rats. The mixture delayed the onset of hypertension in young SHR rats.展开更多
Objective:To determine the depressant-like effects and the possible mechanism of action of tilianin isolated from active methanol extract of Agastache mexicana(A.mexicana).Also,to establish the pharmacophoric requirem...Objective:To determine the depressant-like effects and the possible mechanism of action of tilianin isolated from active methanol extract of Agastache mexicana(A.mexicana).Also,to establish the pharmacophoric requirements of tilianin,as a possible ligand of GABA_A/BZD receptor,by the alignment of diazepam.CGS-9896 and diindole,using a previously described pharmacophoric model.Methods:Tilianin(30 to 300 mg/kg.ip.and 300 mg/kg,pa.) and methanol crude extract(10 to 300 mg/kg,ip.and 300 mg/kg po.) from A.mexicana were evaluated for potential sedative and anxiolytic-like response drugs by using open-field,hole-board,cylinder of exploration,plus-maze and sodium pentobarbital-induced hypnosis mice methods.Results:Methanol extract and tilianin showed anxiolytic-like activity from a dosage of 30 mg/kg,ip.or 300 mg/kg,po.and were less potent than diazepam 0.1 mg/kg.a reference anxiolytic drug used.Moreover,depressant activity of both potentiates sodium pentobarbital(SP)-induced sleeping time.The anxiolytic-like effect of 30 mg/kg ip.observed for the extract and tilianin,by using the plus-maze model,was partially prevented in the presence of flumazenil(a GABA_A/BZD antagonist,5 mg/kg ip.) but not in the presence of WAY100635(a selective 5-HT_(1A) receptor antagonist,0.32 mg/kg.ip.).Pharmacophoric modeling alignments of three agonist of GABA_A/BZD allow identify seven chemical features.Tilianin contains six of the seven features previously determined.Conclusions:Results indicate that tilianin is one of the bioactive metabolites in the anxiolytic-like activity of 4.mexicana.reinforcing its central nervous system uses,where GABA_A/BZD,but not 5-HT_(1A),receptors are partially involved.展开更多
Objective:To assess the relaxant effect of several organic extracts obtained from Agastache mexicana(A.mexicana),Cochlospermum vitifolium(C.vitifolium),Cordia morelosana(C.morelosana),Lepechinia caulescens(L.caulescen...Objective:To assess the relaxant effect of several organic extracts obtained from Agastache mexicana(A.mexicana),Cochlospermum vitifolium(C.vitifolium),Cordia morelosana(C.morelosana),Lepechinia caulescens(L.caulescens)and Talauma mexicana(71 mexicana)used in Mexican traditional medicine for the treatment of several diseases.Methods:Extracts were obtained by maceration at room temperature using hexane,dicliloromethane and methanol for each plant material.The organic extracts were evaluated ex vivo to determine their relaxant activity on the contractions induced by carbaehol(cholinergic receptor agonist,1μmol/L in isolated rat tracheal rings.Results:A total of 15 extracts were evaluated(three for each species).All test samples showed significant relaxant effect,in a concentration-dependent manner,on the contractions induced by 1μmol/L carbachol,with exception of extracts from C.morelosana.Active extracts were less potent than theophylline[phosphodiesterase inhibitor,EC_(50):(28.79±0.82)μg/mL]that was used as positive control.Concentration-response curves revealed that the extracts with more significant effects were dichloromethanic extracts of T.mexhxma[E_(max):(103.03±3.32)%and EC_(50):(159.39±3.72)μg/mL)and C.vitifolium[Emax:(106.58±2.42)%and EC_(50):(219.54±7.61)μg/mL].Finally,hexanic and dichloromethanic extracts from A.mexicana were fully effective but less potent than T.mexicana,and C.vitifolium.Conclusions:Less polar extracts obtained from A.mexicana,71 mexicana and C.vitifolium exhibited greater relaxant effect on tracheal rat rings,which allows us to suggest them as sources for the isolation of bioactive molecules with potential therapeutic value in the treatment of asthma.展开更多
文摘High blood pressure is the main risk factor for cardiovascular diseases, it affects many people worldwide and is a public health problem. This study explored the acute and chronic actions of a mixture of turmeric (95% curcumin) plus black pepper (95% piperine) extracts, in the blood pressure pattern in spontaneously hypertensive rats (SHR) along they age. For the acute study male adult (4 - 7 months old) SHR and their control Wistar Kyoto rats (WKY) were used. A single oral dose of the mixture of turmeric/black pepper extracts (200 mg/2mg, respectively) suspension was administered. Tail-cuff was used to determine blood pressure during 180 min. For the chronic study, young (1-month-old) male SHR and their control WKY rats were fed with standard chow, or standard chow combined with cocoa, or combined with cocoa plus the mixture of turmeric/black pepper extracts;tail-cuff was used to determine blood pressure once a week, along 12 weeks. In a second chronic assay adult (5 months old) male SHR and their control WKY rats were fed with standard chow, or standard chow combined with cocoa, or combined with cocoa plus the mixture of turmeric/black pepper extracts;tail-cuff was used to determine blood pressure once a week, along 12 weeks. In all three studies, a decrease in systolic, diastolic and mean blood pressure was observed, being higher in SHR and negligible in WKY rats. The mixture of turmeric/black pepper extracts showed antihypertensive actions in SHR rats with no effect on WKY rats. The mixture delayed the onset of hypertension in young SHR rats.
基金partially supported by CONACYT 80811.NC123280 grantFaculty of Pharmacy Budgets(FECES 2011 and 2012)
文摘Objective:To determine the depressant-like effects and the possible mechanism of action of tilianin isolated from active methanol extract of Agastache mexicana(A.mexicana).Also,to establish the pharmacophoric requirements of tilianin,as a possible ligand of GABA_A/BZD receptor,by the alignment of diazepam.CGS-9896 and diindole,using a previously described pharmacophoric model.Methods:Tilianin(30 to 300 mg/kg.ip.and 300 mg/kg,pa.) and methanol crude extract(10 to 300 mg/kg,ip.and 300 mg/kg po.) from A.mexicana were evaluated for potential sedative and anxiolytic-like response drugs by using open-field,hole-board,cylinder of exploration,plus-maze and sodium pentobarbital-induced hypnosis mice methods.Results:Methanol extract and tilianin showed anxiolytic-like activity from a dosage of 30 mg/kg,ip.or 300 mg/kg,po.and were less potent than diazepam 0.1 mg/kg.a reference anxiolytic drug used.Moreover,depressant activity of both potentiates sodium pentobarbital(SP)-induced sleeping time.The anxiolytic-like effect of 30 mg/kg ip.observed for the extract and tilianin,by using the plus-maze model,was partially prevented in the presence of flumazenil(a GABA_A/BZD antagonist,5 mg/kg ip.) but not in the presence of WAY100635(a selective 5-HT_(1A) receptor antagonist,0.32 mg/kg.ip.).Pharmacophoric modeling alignments of three agonist of GABA_A/BZD allow identify seven chemical features.Tilianin contains six of the seven features previously determined.Conclusions:Results indicate that tilianin is one of the bioactive metabolites in the anxiolytic-like activity of 4.mexicana.reinforcing its central nervous system uses,where GABA_A/BZD,but not 5-HT_(1A),receptors are partially involved.
基金financed by a grant from"Apoyo a la Mejora del Perfil Individual del profesorado de tiempo completo.(Fondo para la Consolidacin de las Universidades Públicas Estatales y con Apoyo Solidario Ejereicio 2009)"Faculty of Pharmacy budgets(2010 and 2011)grants from CONACyT-CIENCIA BASICA CB-2011-01(167044)
文摘Objective:To assess the relaxant effect of several organic extracts obtained from Agastache mexicana(A.mexicana),Cochlospermum vitifolium(C.vitifolium),Cordia morelosana(C.morelosana),Lepechinia caulescens(L.caulescens)and Talauma mexicana(71 mexicana)used in Mexican traditional medicine for the treatment of several diseases.Methods:Extracts were obtained by maceration at room temperature using hexane,dicliloromethane and methanol for each plant material.The organic extracts were evaluated ex vivo to determine their relaxant activity on the contractions induced by carbaehol(cholinergic receptor agonist,1μmol/L in isolated rat tracheal rings.Results:A total of 15 extracts were evaluated(three for each species).All test samples showed significant relaxant effect,in a concentration-dependent manner,on the contractions induced by 1μmol/L carbachol,with exception of extracts from C.morelosana.Active extracts were less potent than theophylline[phosphodiesterase inhibitor,EC_(50):(28.79±0.82)μg/mL]that was used as positive control.Concentration-response curves revealed that the extracts with more significant effects were dichloromethanic extracts of T.mexhxma[E_(max):(103.03±3.32)%and EC_(50):(159.39±3.72)μg/mL)and C.vitifolium[Emax:(106.58±2.42)%and EC_(50):(219.54±7.61)μg/mL].Finally,hexanic and dichloromethanic extracts from A.mexicana were fully effective but less potent than T.mexicana,and C.vitifolium.Conclusions:Less polar extracts obtained from A.mexicana,71 mexicana and C.vitifolium exhibited greater relaxant effect on tracheal rat rings,which allows us to suggest them as sources for the isolation of bioactive molecules with potential therapeutic value in the treatment of asthma.