ABSTRACT
Aim To study the regulation and mechanism of phloroglucinol in bladder smooth muscle spasm. Methods In vitro the experiment used bladder muscle strip to verify the relieving effect of phloro-glucinol on bladder spasm by different drugs. At the same time,RT-qPCR and Western blot were used to detect the expression levels of genes involved in the calcium signaling pathway caused by the antispasmodic effect of phloroglucinol. Results Phloroglucinol could relieve bladder spasm, and the antispasmodic effect was enhanced with the increase of concentration, and the expression of calponin 1 and MYLK3 in tissue cells increased. The results of RT-qPCR showed that the expression of Gprc5b G,Ppp2r5a, Chptl, Prkar2b ,Abcd2 and Rasdl genes in mouse bladder tissue significantly decreased, which was consistent with the sequencing results of RNA-seq.Conclusions Phloroglucinol can relieve bladder smooth muscle spasm, and its mechanism is related to calcium signaling pathway. Meanwhile, phloroglucinol also inhibits the expression of Rasdl gene, suggesting that it may be related to cell cycle , protein phosphorylation, choline metabolism, ATP synthesis and tumor-related pathways.
ABSTRACT
Aims: Garcinia kola is used in West African countries for the treatment of various ailments such as cough, tooth decay, asthma and menstrual cramps. The inhibitory effect of Garcinia kola seed extract (GKE) on drug-induced contractions was studied on iliac smooth muscle preparations of guinea pig to ascertain the validity of the use of Garcinia kola in traditional medicine and to elucidate its possible mechanism of action. Place and Duration of Study: The study was done in Post Graduate Laboratory, Department of Pharmacology, College of Medical Sciences, University of Calabar, Calabar-Nigeria, between November 2013 and April 2014. Methodology: The antispasmodic influence of GKE (0.02 – 1 mg/ml) on acetylcholine, histamine and potassium chloride -induced contractions were carried out. The effect of GKE in a Ca2+-free Tyrode medium and in the presence of adrenergic antagonists was also investigated. Results: The results revealed that GKE inhibited or attenuated the spasmogenic effects of histamine and potassium chloride in a dose-dependent manner and shifted their log. doseresponse curves to the right, with pA2 values of 2.09±0.06 and 3.25±0.07 respectively. Preadministration of propranolol, prazosin or labetalol had no attenuating influence on the antispasmodic effect of GKE. Iliac smooth muscle responses to cumulative increased [Ca2+] in a depolarizing bathing medium and in a Ca2+- free Tyrode solution were also blocked. Comparative antispasmodic potencies indicated that papaverine and aminophylline were more potent than the extract. Conclusion: These findings suggest that Garcinia kola seed extract acts neither via cholinergic nor adrenergic receptor mediation, but may involve interference with Ca2+ mobilization, thus sharing with papaverine and/or aminophylline similar mechanism(s) of action.
ABSTRACT
Objective: To study the anti-asthma action and biological potency differences of Ephedra Herba from 37 different habitats. Methods: Taking the isolated tracheal smooth muscle from guinea pig to establish antiasthma pharmacological model, the ephedra decoction at different concentration was added to the sink by cumulative metrology method, antispasmodic percentage and biological potency value of Ephedra Herba from different habitats were calculated and the cluster analysis for the biological potency value of Ephedra Herba from different habitats was conducted. Results: Ephedra Herba had the antispasmodic acction to the isolated tracheal smooth muscle of guinea pig caused by histamine phosphate, and compared with the control medicine, Ephedra Herba from 20 habitats showed significant differences (P 0.05); Compared with the control medicine, the antiasthma biological potency of Ephedra Herba from 37 different habitats existed significant or very significant differences (P < 0.05, 0.01), and the antiasthma biological potency value was 22.35-489.04 U/g, while FL% was 13.15%-38.97%, which revealed that the high potency level had a difference of 21.88 times from the low one. And the antiasthma biological potency of Ephedra Herba had lowly significant correlation differences with the total determination of ephedrine and D-pseudephedrine; The Ephedra Herba with different antiasthma biological potency could be identified by cluster analysis method, in which the biological potency from 24 ones in total of 37 Ephedra Herba was higher than that in the control medicine and accounted for 64.86% of the total samples. Conclusion: The anti-asthma biological potency value of Ephedra Herba could quantitatively evaluate the quality of Ephedra Herba from different habitats.
ABSTRACT
The aqueous extract of the aerial parts of Lippia integrifolia has been assayed for its choleretic and antispasmodic effects. Doses of 250, 500 and 750 mg/kg administered orally in rats significantly increased the bile flow and the bile acid output. The extract also showed a significant reduction of the contractions induced by acetylcholine, CaCl2 and KCl on isolated rat jejunum. The total caffeoyl quinic acids derivatives content, expressed as chlorogenic acid was 0.10 percent w/v by spectrophotometric determination.
O extrato aquoso das partes aéreas de Lippia integrifolia foi ensaiado quanto aos seus efeitos colerético e antiespasmódico. Doses de 250, 500 e 750 mg/kg administradas oralmente em ratos aumentaram significativamente o fluxo biliar e a saída de ácidos biliares. O extrato também exibiu uma significativa redução das contrações induzidas por acetilcolina, CaCl2 e KCl em jejuno isolado de rato. O conteúdo total de derivados dos ácidos cafeoilquínicos, expressado como ácido clorogênico foi de 0.10 por cento w/v através de determinação espectrofotométrica.