Insight into the possible mechanism of antidiarrheal and antispasmodic activities of piperine

Taqvi, Syed Intasar Husain; Shah, Abdul Jabbar; Gilani, Anwarul Hassan

doi:10.1080/13880200902918352

Cited by 16 publications

(10 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…9 Our previous studies show that piperidine derivatives perform direct action on cardiac muscle, exhibiting a cardiodepressant effect mediated through calcium channel blockade. 10,11 Our recent study 12 demonstrates that piperine mediates spasmolytic effect through calcium antagonism. On the basis of these observations and the heterogeneous nature of calcium channels, 13 we studied the effect of piperine on blood pressure and demonstrated that it lowers blood pressure at lower doses; at higher doses, the decrease in blood pressure is accompanied by vasoconstrictor effect.…”

Section: Introductionmentioning

confidence: 99%

Blood Pressure Lowering and Vasomodulator Effects of Piperine

Taqvi¹,

Shah²,

Gilani³

2008

Journal of Cardiovascular Pharmacology

Self Cite

127

View full text Add to dashboard Cite

This study was aimed to explore underlying mechanism(s) of cardiovascular effects of piperine. Intravenous administration of piperine caused a dose-dependent (1 to 10 mg/kg) decrease in mean arterial pressure (MAP) in normotensive anesthetized rats; the next higher dose (30 mg/kg) did not cause any further change in MAP. The fall in blood pressure (BP) was followed by small increase in MAP after each dose. In Langendorrf's rabbit heart preparation, piperine caused partial inhibition and verapamil caused complete inhibition of force and rate of ventricular contractions and coronary flow. In rabbit aortic rings, piperine inhibited high K+ (80 mM) precontractions and partially inhibited phenylephrine (PE), suggesting Ca2+ channel blockade (CCB), which was further confirmed when pretreatment of tissues with piperine caused rightward shift in Ca2+ concentration-response curves, similar to verapamil. In Ca2+-free medium, piperine (1 to 30 microM) exhibited vasoconstrictor effect. In rat aorta, piperine demonstrated endothelium-independent vasodilator effect and was more potent against high K+ precontractions than PE. In bovine coronary artery preparations, piperine inhibited high K+ precontractions completely. These data indicate that piperine possesses a blood pressure-lowering effect mediated possibly through CCB, while consistent decrease in BP was restricted by associated vasoconstrictor effect. Additionally, species selectivity exists in the CCB effect of piperine.

show abstract

Section: Introductionmentioning

confidence: 99%

Blood Pressure Lowering and Vasomodulator Effects of Piperine

Taqvi¹,

Shah²,

Gilani³

2008

Journal of Cardiovascular Pharmacology

Self Cite

127

View full text Add to dashboard Cite

show abstract

“…All the test animals were observed continuously for changes in behavior, physiological parameters, restlessness, and seizures for 6 hours, and then intermittently monitored for any morbidity and mortality up to 24 hours 17 . Castor oil-induced diarrhoea Mice (20-25g) of either sex were used as described earlier 18 . Briefly, the animals were divided into five groups composed of five animals, which were housed in individual cages.…”

Section: In Vivo Experimentsmentioning

confidence: 99%

Studies to determine antidiarrhoeal and spasmolytic activities of extract of Aegle marmelos. L fruit

Taqvi

Versiani

Imran

et al. 2018

Bangladesh J Med Sci

Self Cite

View full text Add to dashboard Cite

Objective: To investigate and determine the antidiarrhoeal and spasmolytic potential of fruit of Aegle marmelos is due to CCBs compounds and not tannic acid. Materials and methods: The extract of ripe and dry fruit of A. marmelos (Am.Cr) was prepared in methanol: water (70:30). The antidiarrhoeal activities of the extract, loperamide and tannic acid were studied in vivo; in castor oil induced diarrhoeal model in mice whereas spasmolytic effect was studied in vitro; in isolated mice ileum. Calcium channel blocking (CCB) activity was investigated after preincubation of mice ileum by Am. Cr or loperamide and subsequent adding of K + 80 mM. Results: Am. Cr inhibited castor oil-induced diarrhoea: onset of diarrhoea, total no. of faeces, and total no. of wet faeces dose-dependently, the dose of 800 mg/mL was found statistically significant, total weight of feces and total weight of wet faeces were also inhibited. Concentration-dependent inhibition of spontaneous contraction and contractile effect of K + 80 mM after pre-incubation by Am. Cr were confirmed in isolated mice ileum. The results of Am. Cr are comparable with Loperamide. Tannic acid produced neither antidiarrhoeal effect nor exhibited CCB activity, however relaxant effect was observed in isolated mice ileum. Conclusion: The antidiarrhoeal and spasmolytic effects of Am.Cr may be mediated through compounds which posses CCB effect. Tannic acid exhibited relaxant effect only which is not sufficient evidence scientifically to classify as antidiarrhoeal.

show abstract

“…However, other authors attribute the antispasmodic effect to (i) capsaicin-sensitive neurons, (ii) the participation of vanilloid receptors [ 167 ], (iii) the activation of K + ATP channels, (iv) the blockade of Na + channels and muscarinic receptors, (v) the reduction of extracellular Ca 2+ , or (vi) the blockade of Ca 2+ channels [ 22 , 168 , 169 ]. The above is merely a reflection of the ambiguity of the studies showing the mechanisms of action of the antispasmodic compounds [ 36 ]. For example, the hydroalcoholic extract of Marrubium vulgare showed antispasmodic effect, having the ability to inhibit the neurotransmitters acetylcholine, bradykinin, prostaglandin E2, histamine, and oxytocin [ 170 ], whereas a dual effect of antidiarrheal and laxative activities was reported in Fumaria parviflora [ 171 ].…”

Section: Spasmodic Compoundsmentioning

confidence: 99%

Natural Antispasmodics: Source, Stereochemical Configuration, and Biological Activity

Martínez-Pérez

Juárez

Hernández

et al. 2018

BioMed Research International

View full text Add to dashboard Cite

Natural products with antispasmodic activity have been used in traditional medicine to alleviate different illnesses since the remote past. We searched the literature and compiled the antispasmodic activity of 248 natural compounds isolated from terrestrial plants. In this review, we summarized all the natural products reported with antispasmodic activity until the end of 2017. We also provided chemical information about their extraction as well as the model used to test their activities. Results showed that members of the Lamiaceae and Asteraceae families had the highest number of isolated compounds with antispasmodic activity. Moreover, monoterpenoids, flavonoids, triterpenes, and alkaloids were the chemical groups with the highest number of antispasmodic compounds. Lastly, a structural comparison of natural versus synthetic compounds was discussed.

show abstract

Insight into the possible mechanism of antidiarrheal and antispasmodic activities of piperine

Cited by 16 publications

References 21 publications

Blood Pressure Lowering and Vasomodulator Effects of Piperine

Blood Pressure Lowering and Vasomodulator Effects of Piperine

Studies to determine antidiarrhoeal and spasmolytic activities of extract of Aegle marmelos. L fruit

Natural Antispasmodics: Source, Stereochemical Configuration, and Biological Activity

Contact Info

Product

Resources

About