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1.
Niger J Physiol Sci ; 22(1-2): 43-7, 2007.
Artigo em Inglês | MEDLINE | ID: mdl-18379617

RESUMO

The effects of mefloquine on the mechanical activity of the mouse isolated rectal smooth muscle was studied. Mefloquine (4.1 x 10(-5) - 5.2 x 10(-3)M) when applied alone and separately exerted variable effects on the rectum. In some preparations, it caused slight phasic contractions while in others no response was elicited. When the external Ca(2+) was increased from 1.8 mM to 300 mM mefloquine produced phasic contractile activity which was abolished on return to normal 1.8mM suggesting that the contractile activity was due to extracellular Ca(2+) influx. Mefloquine [4.1 x 10(-6)M - 4.1 x 10(-4)M] caused contraction-dependent inhibition of KCL, Carbachol and CaCl2 [in depolarizing Tyrode solution]. Mefloquine [2.1 x 10(-4)M] blocked KCL, but not carbachol contractions which were largely reversed by increasing [Ca2+]. The results show that mefloquine possesses anticholinergic and appreciable calcium channel blocking activity.


Assuntos
Antimaláricos/farmacologia , Bloqueadores dos Canais de Cálcio/farmacologia , Antagonistas Colinérgicos/farmacologia , Mefloquina/farmacologia , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Reto/efeitos dos fármacos , Animais , Antimaláricos/efeitos adversos , Bloqueadores dos Canais de Cálcio/efeitos adversos , Cloreto de Cálcio/metabolismo , Carbacol/farmacologia , Agonistas Colinérgicos/farmacologia , Antagonistas Colinérgicos/efeitos adversos , Relação Dose-Resposta a Droga , Técnicas In Vitro , Masculino , Mefloquina/efeitos adversos , Camundongos , Músculo Liso/metabolismo , Cloreto de Potássio/farmacologia , Reto/metabolismo
2.
Artigo em Inglês | AIM | ID: biblio-1259236

RESUMO

Background : The treatment of peptic ulcer disease poses therapeutic challenges to both patients and physicians alike because of the tendency of ulcers to relapse. Drugs used in the treatment of this disease are either costly or are associated with high incidence of adverse effects. Synclisia scabrida is a plant used in ethnomedicine for the treatment of various forms of stomach disorders and menstrual pains. The medicinal properties of the plants are claimed to reside in the roots; stems; and the leaves. Aim : This study; therefore; is to verify this claim and elucidate the probable mechanism of action by using crude stem extracts of this plant on drug- and stress-induced ulcer models in albino mice. Materials and Methods : Crude ethanol and hot water extracts; EE and HWE respectively; of the stem were prepared. These extracts were fractionated and separated by chromatographic methods and the fractions pooled together as fractions (PF-1; PF-2; PF-3 respectively) based on their chromatographic mobility and color reactions. Phytochemical analysis was done on the extracts. Ulcer models were induced in albino mice by means of indomethacin; histamine; and stress after prior cytoprotection with orally administered crude extracts and control (cimetidine). Results : Phytochemical analysis of the crude extracts and their fractions revealed the presence of cardiac glycosides (+++); tannins (+++); saponins (+); flavonoids (++); carbohydrates (++) and alkaloids (+++). Acute toxicity study on the crude extracts and their fractions revealed relative safety at the dose of 5000 mg/kg. The crude extracts (EE and HWE) and their fractions (PF-1; PF-2; PF-3) significantly (P = 0.001) protected against indomethacin-; histamine- and stress-induced ulcers. The decrease in GIT motility produced by these extracts was comparable to that produced by atropine sulfate. Conclusion : The findings suggest that these extracts of Synclisia scabrida possess antiulcer and antispasmodic properties; which justify the claims for its use in the treatment of various forms of stomach disorders


Assuntos
Úlcera Péptica , Ratos
3.
Artigo em Inglês | AIM | ID: biblio-1259241

RESUMO

The treatment of peptic ulcer disease poses therapeutic challenges to both patients and physicians alike because of the tendency of ulcers to relapse. Drugs used in the treatment of this disease are either costly or are associated with high incidence of adverse effects. Synclisia scabrida is a plant used in ethnomedicine for the treatment of various forms of stomach disorders and menstrual pains. The medicinal properties of the plants are claimed to reside in the roots; stems; and the leaves. Aim : This study; therefore; is to verify this claim and elucidate the probable mechanism of action by using crude stem extracts of this plant on drug- and stress-induced ulcer models in albino mice. Materials and Methods : Crude ethanol and hot water extracts; EE and HWE respectively; of the stem were prepared. These extracts were fractionated and separated by chromatographic methods and the fractions pooled together as fractions (PF-1; PF-2; PF-3 respectively) based on their chromatographic mobility and color reactions. Phytochemical analysis was done on the extracts. Ulcer models were induced in albino mice by means of indomethacin; histamine; and stress after prior cytoprotection with orally administered crude extracts and control (cimetidine). Results : Phytochemical analysis of the crude extracts and their fractions revealed the presence of cardiac glycosides (+++); tannins (+++); saponins (+); flavonoids (++); carbohydrates (++) and alkaloids (+++). Acute toxicity study on the crude extracts and their fractions revealed relative safety at the dose of 5000 mg/kg. The crude extracts (EE and HWE) and their fractions (PF-1; PF-2; PF-3) significantly (P = 0.001) protected against indomethacin-; histamine- and stress-induced ulcers. The decrease in GIT motility produced by these extracts was comparable to that produced by atropine sulfate. Conclusion : The findings suggest that these extracts of Synclisia scabrida possess antiulcer and antispasmodic properties; which justify the claims for its use in the treatment of various forms of stomach disorders


Assuntos
Dismenorreia , Camundongos , Úlcera Péptica , Medicamentos sob Prescrição , Gastropatias
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