Pharmacological basis for the medicinal use of Rhus coriaria in hyperactive gut disorders

This study was aimed at providing the pharmacological basis for the medicinal use of Rhus coriaria in diarrhea. In mice, the crude of R. coriaria demonstrated antisecretory and antidiarrheal effects against castor oil-induced fluid accumulation and diarrhea at at 100 and 300 mg/kg, respectively, and was found safe up to tested dose of 5 g/kg. In isolated rabbit jejunum, R. coriaria exhibited concentration-dependent (0.01-3.0 mg/mL) relaxation of spontaneous and high K+ (80 mM)-induced contractions, similar to verapamil. The Ca++ antagonist activity was confirmed when pretreatment of R. coriaria shifted Ca++ concentration-response curves to the right with suppression of maximal response, similar to verapamil. R. coriaria also suppressed the high K+-evoked transient contractile peaks similar to the effect of cyclopiazonic acid and verapamil. This study indicates that R. coriaria possesses antisecretory, antidiarrheal and antispasmodic properties mediated possibly through Ca++ antagonist pathway, thus providing evidence to its medicinal use in diarrhea and abdominal spasm

Spasmolytic effect of grewia asiatica fruit extract on isolated smooth muscles is mediated via multiple pathways

Background: Grewia asiatica Linn, or phalsa, is a commonly consumed fruit in Pakistan. The fruit is employed in the traditional medicine practice of Pakistan as a smooth muscle relaxant in different gastrointestinal (GI) and cardiovascular diseases. In this investigation, we show the antispasmodic and vasorelaxant actions of Grewia asiatica fruit extract.Methods: A 70% methanolic crude extract of the plant material was prepared (Ga.Cr). Different isolated GI tissue preparations and endothelium-intact aortas from rats were utilized to observe the pharmacological actions of the extract.Results: Ga.Cr, in increasing concentrations, inhibited the spontaneously contracting rabbit jejunum. In an effort to determine the mechanism of this relaxant action, contractions were induced in jejunum and ileum tissues with K+ (80 mM). Ga.Cr was able to only partially inhibit these induced contractions indicating that the mechanism might not be completely through a blockade of Ca2+ channels (CCB). When tested on low K+-(25 mM) sustained contractions, Ga.Cr cumulatively suppressed these contractions (0.1-10 mg/ml), indicating an opening of K+ channels (KCO) as the mechanism. Cromakalim, a standard KCO, was also more specific in blocking low K+-induced contractions. For the effect in aorta tissues, Ga.Cr suppressed the agonist-induced contractions from 0.3 mg/ml to 10 mg/ml. Upon challenge with L-NAME, a nitric oxide (NO) blocker, the extract response curve shifted right, indicating vasodilation was mediated via endothelial NO.Conclusion: This study shows that GI antispasmodic and vasodilator activities of Ga.Cr may be mediated via a KCO mechanism in the GI tract and through the release of NO from vascular endothelium

Pharmacological basis for the medicinal use of Valeriana wallichii in constipation

Valeriana wallichii D.C. (Valerianaceae) is widely used in folk medicine for the treatment of hypo-motility disorder of the gut. The aim of the present study was to scientifically rationalize its usefulness in the constipation. The V. wallichii leaves crude extract, which tested positive for the presence of anthraquinones, flavonoids, saponins, sterols, tannins and terpenes caused concentration-dependent (3-10 mg/mL) contractile effect in isolated guinea-pig ileum. Pretreatment of tissues with atropine (1 μM) completely abolished the stimulatory effect of V. wallichii leaves crude extract, similar to that of acetylcholine. These results indicate that the spasmogenic effect of V. wallichii is mediated possibly through the activation of muscarinic receptors, which provides sound mechanistic background for its medicinal use in constipation.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Studies on antidyslipidemic effects of Morinda citrifolia (Noni) fruit, leaves and root extracts

<p>Abstract</p> <p>Background</p> <p>The objective of present study was to provide the pharmacological basis for the medicinal use of <it>Morinda citrifolia </it>Linn in dyslipidemia using the aqueous-ethanolic extracts of its fruits (Mc.Cr.F), leaves (Mc.Cr.L) and roots (Mc.Cr.R).</p> <p>Results</p> <p>Mc.Cr.F, Mc.Cr.L and Mc.Cr.R showed antidyslipidemic effects in both triton (WR-1339) and high fat diet-induced dyslipidemic rat models to variable extents. All three extracts caused reduction in total cholesterol and triglyceride levels in triton-induced dyslipidemia. In high fat diet-induced dyslipidemia all these extracts caused significant reduction in total cholesterol, triglyceride, low density lipoprotein-cholesterol (LDL-C), atherogenic index and TC/HDL ratio. Mc.Cr.R extract also caused increase in high density lipoprotein-cholesterol (HDL-C). The Mc.Cr.L and Mc.Cr.R reduced gain in body weight with a reduction in daily diet consumption but Mc.Cr.F had no effect on body weight and daily diet consumption.</p> <p>Conclusions</p> <p>These data indicate that the antidyslipidemic effect of the plant extracts was meditated through the inhibition of biosynthesis, absorption and secretion of lipids. This may be possibly due partly to the presence of antioxidant constituents in this plant. Therefore, this study rationalizes the medicinal use of <it>Morinda citrifolia </it>in dyslipidemia.</p

In vivo studies on the bronchodilatory and analgesic activities of Hyoscyamus niger and Aspalathus linearis

The present study describes the in vivo bronchodilatory and analgesic activities of the crude extract of Hyoscyamus niger (Hn.Cr) and Aspalathus linearis (Al.Cr), which tested positive for alkaloids, coumarins, flavonoids, sterols, tannins, terpenes and flavonoids, tannins, saponins respectively. Hn.Cr (0.3-3.0 mg/kg) and Al.Cr (10-100 mg/kg) caused inhibition of the CCh (1 μmol/kg)-induced increase in the inspiratory pressure of anaesthetized rats. Hn.Cr and Al.Cr dose-dependently (50-100 mg/kg) reduced the numbers of acetic acid-mediated writhes in mice. These results indicate that Hyoscyamus niger and Aspalathus linearis exhibit airways-relaxant and anti-nociceptive effects, hence justifying their medicinal use in asthma and pain.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Antidiarrheal and bronchodilatory activities of olive extract

This study describes the antidiarrheal and airways-relaxant effects of the olive or Olea europea crude extract (Oe.Cr). Oe.Cr which tested positive for the presence of flavonoids and saponins, inhibited the castor oil-induced diarrhea in mice at the dose range of 100-300 mg/kg. When tested against carbachol (CCh)-mediated bronchoconstriction in rats under anesthesia, Oe.Cr dose-dependently (30-300 mg/kg) suppressed the CCh (1 μmol/kg)-induced increase in the inspiratory pressure. In isolated guineapig trachea, Oe.Cr caused relaxation of both CCh (1μM) and high K+ (80 mM)-induced contractions, like that caused by verapamil, suggestive of Ca++ channel blockade. These results indicate that olive exhibit antidiarrheal, bronchodilatory and tracheo-relaxant activities.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Antidiarrhoeal, antisecretory and antispasmodic activities of matricaria chamomilla are mediated predominantly through K+-channels activation

Background: Matricaria chamomilla commonly known as “Chamomile” (Asteraceae) is a popular medicinal herb widely used in indigenous system of medicine for a variety of ailments. However, there is no detailed study available showing its effectiveness in hyperactive gut disorders like, abdominal colic and diarrhoea. This study was designed to determine the pharmacological basis for the folkloric use of Matricaria chamomilla in diarrhoea. Methods: The crude aqueous-methanolic extract of Matricaria chamomilla (Mc.Cr) was studied for its protective effect in mice against castor oil-induced diarrhoea and intestinal fluid accumulation. The isolated rabbit jejunum was selected for the in-vitro experiments using tissue bath assembly coupled with PowerLab data acquisition system. Results: Oral administration of Mc.Cr to mice at 150 and 300 mg/kg showed marked antidiarrhoeal and antisecretory effects against castor oil-induced diarrhoea and intestinal fluid accumulation, simultaneously, similar to the effects of cromakalim and loperamide. These effects of plant extract were attenuated in animals pretreated with K+ channel antagonist, glibenclamide (GB) or 4-aminopyridine (4-AP). When tested in isolated rabbit jejunum, Mc.Cr caused a dose-dependent (0.3-3 mg/ml) relaxation of spontaneous and low K+ (25 mM)-induced contractions, while it exhibited weak inhibitory effect on high K+ (80 mM). The inhibitory effect of Mc.Cr on low K+-induced contractions was partially inhibited in the presence of GB, while completely blocked by 4-AP. Cromakalim, an ATP-sensitive K+ channel opener, caused complete relaxation of low K+-induced contractions with little effect on high K+. Pretreatment of tissues with GB blocked the inhibitory effects of cromakalim on low K+, while the presence of 4-AP did not alter the original effect. Verapamil, a Ca++ channel antagonist, caused complete relaxation of both low and high K+-induced contractions with similar potency. The inhibitory effect of verapamil was insensitive to GB or 4-AP. When assessed for Ca++ antagonist like activity, Mc.Cr at high concentrations caused rightward shift in the Ca++ concentration-response curves with suppression of the maximum response, similar to the effect of verapamil, while cromakalim did not show similar effect. Conclusions: This study indicates that Matricaria chamomilla possesses antidiarrhoeal, antisecretory and antispasmodic activities mediated predominantly through K+-channels activation along with weak Ca++ antagonist effect

SPASMOLYTIC, BRONCHODILATOR AND VASORELAXANT ACTIVITY OF METHANOLIC EXTRACT OF TEPHROSIA PURPUREA

The methanolic extract of the whole plant of Tephrosia pupurea, Linn. was subjected to find out itspossible therapeutic utility to validate its folkloric use in native systems of medicine. The extract on applicationto spontaneous contractions in isolated rabbit jejunum preparations exerted a concentration dependent(0.003-3.0 mg/mL) relaxant effect. The extract also caused concentration dependent relaxation of K+ (80 mM)-induced spastic contractions. These findings were further supported by the observations that the extract causeda concentration dependent right ward shift of the Ca2+ response curves in manner similar to that of verapamil.The extract exhibited a relaxant effect on carbachol and high K+ (80 mM)-induced contractions of isolated rabbittracheal preparations in a manner similar to verapamil. The observed non-specific bronchodilator responseis possibly mediated through Ca2+ channel blockade. Moreover, the extract also exhibited a dose dependentrelaxant effect on phenylephrine (1 μM) and K+ (80 mM)-induced contractions in a manner similar to verapamil.On the basis of the above-mentioned findings, it can be concluded that the use of Tephrosia purpurea, in gastrointestinalspasm, asthma and hypertension is likely to be mediated through calcium channel blockage

Vasodilator effect of 1-trifluoromethoxyphenyl-3-(1- propionylpiperidin-4-yl) urea is predominantly mediated through activation of voltage-dependent K+ channels

Purpose: To determine the mechanism of vasorelaxant effect of 1-trifluoromethoxyphenyl – 3 -(1-propionylpiperidin–4-yl) urea (TPPU) in cardiovascular diseases, including hypertension.Methods: Isolated rat thoracic aortic tissue preparations were mounted in an organ bath set up integrated with isometric transducer and a Power Lab assembly. TPPU (0.3 - 100 μM) was tested for vasorelaxant effect against low K+ (25 mM) and high K+ (80 mM)-induced contractions and its mechanism was determined in the presence of different antagonists (glibenclamide, 4- aminopyridine and tetraethyl ammonium).Results: In rat aortic preparations, TPPU showed a concentration-dependent (0.3 – 100 μM) and significant (p &lt; 0.001) inhibition of low K+ induced contractions with complete inhibition obtained at 100 μM. TPPU produced significant (p &lt; 0.05) inhibition of high K+ induced contractions with maximum relaxation of 15.36 ± 1.95 % and 15.85 ± 3.35 % at 30 and 100 μM, respectively. Glibenclamide (Gb,10 μM) pretreatment partially inhibited the vasorelaxant effect of TPPU against low K+ in a concentration range of 1 - 30 μM. 4-Aminopyridine (4-AP, 1 mM) and tetraethyl ammonium (TEA, 10 mM), markedly inhibited the vasorelexant effect of TPPU against low K+ induced contractions with maximum relaxation of 20.09 ± 2.40 and 21.67 ± 0.88 %, respectively, at 100 μM.Conclusion: TPPU possesses marked vasorelaxant properties which provides sound pharmacological evidence for its use as a potential drug candidate in the management of hypertension.Keywords: 1-Trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea, Hypertension, vasodilator, K+- channel activation, Ca+- channel antagonis

Valuable Nutrients and Functional Bioactives in Different Parts of Olive (Olea europaea L.)—A Review

The Olive tree (Olea europaea L.), a native of the Mediterranean basin and parts of Asia, is now widely cultivated in many other parts of the world for production of olive oil and table olives. Olive is a rich source of valuable nutrients and bioactives of medicinal and therapeutic interest. Olive fruit contains appreciable concentration, 1–3% of fresh pulp weight, of hydrophilic (phenolic acids, phenolic alchohols, flavonoids and secoiridoids) and lipophilic (cresols) phenolic compounds that are known to possess multiple biological activities such as antioxidant, anticarcinogenic, antiinflammatory, antimicrobial, antihypertensive, antidyslipidemic, cardiotonic, laxative, and antiplatelet. Other important compounds present in olive fruit are pectin, organic acids, and pigments. Virgin olive oil (VOO), extracted mechanically from the fruit, is also very popular for its nutritive and health-promoting potential, especially against cardiovascular disorders due to the presence of high levels of monounsaturates and other valuable minor components such as phenolics, phytosterols, tocopherols, carotenoids, chlorophyll and squalene. The cultivar, area of production, harvest time, and the processing techniques employed are some of the factors shown to influence the composition of olive fruit and olive oil. This review focuses comprehensively on the nutrients and high-value bioactives profile as well as medicinal and functional aspects of different parts of olives and its byproducts. Various factors affecting the composition of this food commodity of medicinal value are also discussed