Potentiating effect of Phragmanthera capitata extract in haematopoietic activities in Wistar rats (original) (raw)
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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 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 Ca 2+ -free Tyrode medium and in the presence of adrenergic antagonists was also investigated.
The antispasmodic and spasmolytic effects of methanolic extract of seeds of Garcinia kola Heckel were studied on smooth muscle preparations in vitro. The influence of the extract on rat duodenum, jejunum and ileum was investigated using acetylcholine and barium chloride as agonists. The extract exhibited dose-dependent antispasmodic effects on contractions induced by acetylcholine, and dose-dependent spasmolytic effects on spasms induced by cumulatively increased concentrations of acetylcholine and barium chloride. The graded log concentration-response curves for acetylcholine were non-parallel but shifted to the right in the presence of the extract. It is concluded that the Garcinia kola extract inhibits smooth muscle activity via other mechanisms but not involving neither cholinergic nor adrenergic receptor interaction.
Pharmaceutical Biology, 2016
Context: Psidium guajava L. (Myrtaceae) is widely used in traditional medicine for the treatment of various ailments including cardiovascular and gastrointestinal disorders. Objectives: The current study investigated the chemical composition and cardiovascular and gastrointestinal effects of the essential oil of P. guajava. Materials and methods: The chemical composition of the essential oil was investigated using gas chromatography-mass spectrometry (GC-MS) technique. The biological activity of the essential oil was tested on rabbit aorta and jejunum. All changes in isometric tension were recorded through a force transducer coupled with a bridge amplifier data acquisition system. Results and discussion: GC-MS analysis showed the presence of butanoic acid methyl ester, 3-methyl glutaric anhydride, 1-butanol, 3-hexenal, cinnamyl alcohol, 1-hexanol and hexane as the major components. In isolated rabbit aorta preparations, the essential oil showed vasorelaxation at doses of 3-10 mg/mL against high K þ and phenylephrine pre-contractions with EC 50 values of 5.52 (5-6.04) and 6.23 mg/mL (5.0-7.46). The essential oil inhibited spontaneous and high K þ induced contractions in isolated rabbit jejunum with EC 50 values of 0.84 (0.3-1.38) and 0.71 mg/mL (0.3-1.12) and shifted Ca þ 2 concentration curves to the right, similar to verapamil, suggesting spasmolytic activity mediated possibly through Ca þ 2 channel blockade. Conclusions: In summary, the data indicated the presence of seven different phytoconstituents in the essential oil of P. guajava and calcium channel blocking activity, which provides a pharmacological base to the traditional use of P. guajava in cardiovascular and gastrointestinal disorders. Further studies are suggested to explore the molecular nature of these effects.
Journal of Traditional and Complementary Medicine, 2017
This study was undertaken to examine the antinociceptive, antihyperglycemic, and membrane stabilizing activity with phytochemical screening of methanolic extract of Garcinia lanceifolia whole plant. The extracts were subjected to in-vivo antinociceptive, antihyperglycemic activity in laboratory animals and in-vitro membrane stabilizing activity. In peripheral antinociceptive activity, G. lanceifolia (400 and 200 mg/kg) exhibited significant (P < 0.001) inhibition of writhing with 59.15% and 49.30% respectively comparable to standard Diclofenac (54.92% inhibition). In central antinociceptive activity, the extract (400 and 200 mg/kg) exhibited significant analgesic activity having 78.31% (P < 0.05) and 89.95% (P < 0.01) elongation of reaction time respectively in 90 min after administration of sample comparable to the standard Morphine (708.99% elongation). In hypoglycemic activity, the extract (400 and 200 mg/ kg) exhibit statistically significant (P < 0.001) antihyperglycemic activity compared to standard drug Glibenclamide (10 mg/kg) at different time interval. In membrane stabilizing activity assay, clearly evident that the methanolic extracts of G. lanceifolia were highly effective to prevent the lyses of erythrocytes induced by heat. The outcomes of the present study revealed that this plant possess noteworthy pharmacological activities that may be basis for further research to disclose feasible mode of action of the plant part.
Phytotherapy …, 1995
Muscle relaxant activities of six compounds isolated from Malaysian medicinal plants were investigated on the smooth muscles of the rat aorta and longitudinal muscle of the guinea-pig ileum. Except for goniothalamin, the other five compounds exhibited varying degrees of muscle relaxant activities on the two smooth muscles. Dicentrine, isocorydine, altholactone and usnic acid reduced the contractions to KCI and phenylephrine in the rat aorta, whilst atranorin slightly reduced the contractions to phenylephrine but not KCI. In addition, dicentrine and isocorydine markedly reduced the contractile response to phenylephrine in Ca2+-free Krebs solution. In the longitudinal muscle of the guinea-pig ileum, altholactone, atranorin, dicentrine and isocorydine inhibited to a greater extent the phasic than the tonic responses to KCI. All four compounds similarly inhibited the contractions induced by ACh. The results suggest that the relaxant activities of the compounds are attributed mainly to inhibition of Ca2+ influx via the calcium channels in the membrane of the smooth muscles. Furthermore, the greater sensitivity of dicentrine, isocorydine and altholactone against phenylephrine-induced contractions or KCI-induced phasic contractions are due to their abilities to inhibit intracellular Ca2+ release in these muscles.
Fundamental & Clinical Pharmacology, 2005
The relaxant effects of the Taxodium mucronatum Ten leaf hexane extract on intestinal and tracheal smooth muscle were evaluated in vitro by testing spontaneous contractions of rabbit jejunum and agonist-induced contractions of guinea pig ileum and rat trachea. The extract produced a concentration-dependent relaxation of the spontaneous contractions of rabbit jejunum (EC 50 : 4.9 ± ± ± ± 0.5 µg/ml) that was equipotent to papaverine. Following incubation of guinea pig ileum with the extract, the concentration-response curves to acetylcholine, histamine, 5-hydroxytryptamine and Ca 2+ were displaced to the right and the maximum response was significantly reduced. K + -induced contraction of the ileal tissue was completely abolished with 31.6 µg/ml of the extract. In rat tracheal rings, the extract inhibited both 1 µM carbachol (EC 50 : 33.9 ± ± ± ± 2.5 µg/ml) and 60 mM K + (EC 50 : 20.6 ± ± ± ± 1.1 µg/ml)-induced contractions. It also caused the concentration-response to Ca 2+ curves to shift to the right in a noncompetitive manner. These results demonstrate a non-specific relaxant effect that could be mediated through inhibition of calcium influx via both voltage-and receptor-gated calcium channels. The relaxant activity induced by this extract provides a rational basis for the traditional use of T. mucronatum to treat disorders of the gastrointestinal and respiratory tracts.
Revista Vitae, 2017
Background: The treatment of symptoms of prostatic hyperplasia is among the traditional uses of Achyrocline bogotensis (Kunth) [N.V. "Vira Vira", Compositae] in Colombia. Pharmacological therapy for this disorder depends mainly on alpha-1 antiadrenergic agents, and the mechanism has not been studied previously using A. bogotensis. Objectives: To assess the alpha-1 antiadrenergic effect of the extract obtained from the aerial parts of A. bogotensis in isolated aortic rings from Wistar rats. Methods: The study compared the effects of the ethanol extract of A. bogotensis, prazosin (reference) and DMSO (control) in rings stimulated with phenylephrine (PE) or KCl. The capacity to reduce the PE pressor effect by the ethanol extract (pD 2 ' value) was determined. To quantify the A. bogotensis relaxant potency, increasing concentrations of the ethanol extract (0.1 µg/mL-0.1 mg/mL), were added cumulatively to isolated aortic rings pre-contracted with PE (0.1 µM) or KCl (80 mM). To explore the possible participation of nitric oxide (NO), L-NAME (100 µM) was administered to aortic rings exposed to cumulatively increasing concentrations of PE in isolated aortic rings in the presence of the extract (10 µg/mL). Aqueous, butanol and dichloromethane fractions (10 µg/mL) obtained from the ethanol extract were assayed. Phytochemical screening was also performed. Results: Prazosin and A. bogotensis extract notably reduced the contraction induced by PE whereas their inhibitory effect in rings contracted with KCl were lower. A. bogotensis ethanol extract showed a high capacity for reducing the PE pressor response (pD´2: 5.51) as well as total efficacy for relaxing rings previously precontracted with PE. The relaxant efficacy and potency of A. bogotensis extract against rings previously contracted with KCl were notably lower. L-NAME partly reverted the inhibitory effect of A. bogotensis. Aqueous, butanol and dichloromethane fractions gave inhibitory responses lower than that obtained with the ethanol extract. Phytochemical screening of A. bogotensis extract revealed the significant presence of flavonoid and triterpene metabolites. Conclusions: These results suggest that A. bogotensis elicits a smooth muscle relaxant effect related to the alpha-1 antiadrenergic mechanism. This response is partially NO dependent and seems to be due to interactions among active metabolites likely to be of flavonoid and/or terpenoid nature.
VASORELAXANT AND ANTISPASMODIC EFFECTS OF SOME POLYPHENOLS AND GLYCOSIDE IN RAT SMOOTH MUSCLES
Objective: The present study was undertaken to investigate the effect of Luteolin, chlorogenic acid, amygdalin and tannic acid on vascular smooth muscle contractility. Materials and Methods: The effect of different concentrations of some polyphenols and glycosides on contractile responses of isolated aorta, ileum and trachea to Acetylcholine, KCl and phenylephrine (PE) were evaluated. Results: The results of the current study indicated that luteolin and chlorogenic acid has potent relaxant effects on KCl and PE-induced contractions in rat's aortic ring. Amygdalin and tannic acid reduced ACh-induced ileum contractions significantly. Conclusions: The inhibitory effect of luteolin and chlorogenic acid on the contraction induced by PE and KCl may be due to their anti-adrenergic and anti-hyperpolarizing effect.
Journal of Ethnopharmacology, 2007
The present work describes the mechanisms involved in the muscle relaxant effect of ethanol:water (40:60, 60:40 and 80:20) aerial parts extracts of Pimpinella anisum. Three hidroalcoholic extracts in which the proportion of ethanol was 40% (HA 40% ), 60% (HA 60% ) or 80% (HA 80% ) were tested for activity in the rat anococcygeus smooth muscle. The three extracts (50 g/mL) inhibited acetylcholine-induced contraction. The extract HA 60% (5-50 g/mL) concentration dependently relaxed acetylcholine-pre-contracted tissues (31.55 ± 3.56%). Conversely, HA 40% and HA 80% did not exert relaxant action. Pre-incubation of the preparations with N G -nitro-l-arginine methyl ester (l-NAME, 100 M), 1H-[1,2,4]oxadiazolo[4,3a]quinoxalin-1-one (ODQ, 3 M) and oxyhemoglobin (10 M) reduced the relaxation induced by HA 60% (percentage of relaxation: 6.81 ± 1.86%, 13.13 ± 5.87% and 2.12 ± 1.46%, respectively). Neither indomethacin (10 M) nor tetraethylammonium (1 mM) affected the relaxation induced by HA 60% . Incubation of the tissues with l-NAME significantly enhanced the maximal contraction induced by acetylcholine, indicating an inhibitory role for NO in the modulation of the contractile response of anococcygeus smooth muscle to acetylcholine. However, simultaneous addition of l-NAME and HA 60% resulted in an effect similar to that observed with l-NAME alone, further confirming the observation that Pimpinella anisum acts by realizing NO. Additionally, HA 60% did not alter CaCl 2 -induced contraction. Collectively, our results provide functional evidence that the effects elicited by the hidroalcoholic extract of Pimpinella anisum involve the participation of NO and subsequent activation of the NO-cGMP pathway. The relaxant action displayed by Pimpinella anisum justifies its use in the folk medicine as an antispasmodic agent.
2007
The present work describes the mechanisms involved in the muscle relaxant effect of ethanol:water (40:60, 60:40 and 80:20) aerial parts extracts of Pimpinella anisum. Three hidroalcoholic extracts in which the proportion of ethanol was 40% (HA 40%), 60% (HA 60%) or 80% (HA 80%) were tested for activity in the rat anococcygeus smooth muscle. The three extracts (50 g/mL) inhibited acetylcholine-induced contraction. The extract HA 60% (5-50 g/mL) concentration dependently relaxed acetylcholine-pre-contracted tissues (31.55 ± 3.56%). Conversely, HA 40% and HA 80% did not exert relaxant action. Pre-incubation of the preparations with N G-nitro-l-arginine methyl ester (l-NAME, 100 M), 1H-[1,2,4]oxadiazolo[4,3a]quinoxalin-1-one (ODQ, 3 M) and oxyhemoglobin (10 M) reduced the relaxation induced by HA 60% (percentage of relaxation: 6.81 ± 1.86%, 13.13 ± 5.87% and 2.12 ± 1.46%, respectively). Neither indomethacin (10 M) nor tetraethylammonium (1 mM) affected the relaxation induced by HA 60%. Incubation of the tissues with l-NAME significantly enhanced the maximal contraction induced by acetylcholine, indicating an inhibitory role for NO in the modulation of the contractile response of anococcygeus smooth muscle to acetylcholine. However, simultaneous addition of l-NAME and HA 60% resulted in an effect similar to that observed with l-NAME alone, further confirming the observation that Pimpinella anisum acts by realizing NO. Additionally, HA 60% did not alter CaCl 2-induced contraction. Collectively, our results provide functional evidence that the effects elicited by the hidroalcoholic extract of Pimpinella anisum involve the participation of NO and subsequent activation of the NO-cGMP pathway. The relaxant action displayed by Pimpinella anisum justifies its use in the folk medicine as an antispasmodic agent.