Anti-diarrheal activity of methanolic extract of Tephrosia purpurea.

BACKGROUND: The metabolic syndrome (MS) is a combination of metabolic abnormalities that lead to an increased risk of cardiovascular diseases. Due to its rising incidence and demanding life-long use of multiple drugs, there is a growing interest in testing and developing new allopathic, complementary and alternative therapies for controlling or curing disorders of MS. The discovery of new therapeutic modalities requires animal models of disease and currently available models have limitations. Developing an appropriate animal model for MS to achieve various therapeutic targets remains a challenge and this study aims to develop a rat model which closely depicts MS in humans. METHODOLOGY: Rat model of MS was developed by replacing 60% of diet with fructose. Four groups of Sprague-Dawley rats were either given whole wheat or refined flour with and without fructose for 8 weeks. Data were analyzed on SPSS and Graphpad Prism using ANOVA with Tukey\u27s and Bonferonni tests for multiple group comparison. A p-value of less than 0.05 was considered significant for differences between groups. RESULTS: Replacing whole wheat with refined wheat flour in rat chow in 60% fructose-fed Sprague-Dawley rats resulted in hypertension (p 0.01), hyper-insulinemia (p \u3c 0.001), hyperglycemia (p 0.03) and a reduction in HDL levels (p 0.002) at 4 weeks while hyper-triglyceridemia (p 0.001) with endothelial dysfunction was observed at 8 weeks. CONCLUSION: It is concluded that the refined wheat flour with 60% fructose in diet hastens the development of metabolic syndrome in 4 weeks and replacing whole wheat flour with refined flour in diet induces a more effective abnormality including a low HDL. Further studies may be directed to assess the associated pathological changes, which can be used to study the effect of different therapeutic modalities on an animal model of MS with low HD

Aqueous-methanolic extract of sweet flag (Acorus calamus) possesses cardiac depressant and endothelial-derived hyperpolarizing factor-mediated coronary vasodilator effects.

This investigation was aimed to probe the pharmacological base of medicinal use of Acorus calamus in ischemic heart diseases. Effect on heart parameters was studied in isolated rabbit heart while coronary vasodilator effect was studied in isolated bovine coronary arterial rings, suspended in tissue baths filled with Krebs solution, maintained at 37degreesC, aerated with carbogen and responses were measured on PowerLab data acquisition system. In Langendorrf\u27s perfused rabbit heart, the crude extract of Acorus calamus (Ac.Cr) at 0.01-10 mg/mL partially suppressed force of ventricular contractions (FVC), heart rate (HR) and coronary flow (CF). The ethylacetate fraction completely suppressed FVC, partially suppressed HR and CF, while the nHexane fraction exhibited similar effect on FVC and HR but increased CF, similar to methacholine and arachidonic acid. In bovine coronary arterial preparations, Ac.Cr caused inhibition of U46619 (20 nM)-precontractions, which was blocked in presence of increasing concentration of K(+) (4.8-20 mM), tetraethylammonium (1 muM) and SKF525A (10 muM), similar to arachidonic acid and methacholine, indicating K(+) channels activation and possible involvement of endothelial-derived hyperpolarizing factor (EDHF). Activity-directed fractionation revealed that EDHF-mediated activity is concentrated in the nHexane fraction. When tested against high K(+), the ethylacetate fraction was found more potent than parent crude extract and nHexane fraction. These data indicate that Ac.Cr mediates coronary vasodilator effect primarily through EDHF, responsible for the increase in CF, while the cardiac depressant effects may be due to the presence of additional cardiac depressant constituent(s), thus provides possible mechanistic basis to its medicinal use in ischemic heart diseases

Airways and cardiovascular inhibitory effects of Olea europea and Terminalia bellerica aqueous fractions

This study describes the bronchodilatory, vaso-relaxant and cardiac inhibitory effects of aqueous fractions of Olea europea (Oe.Aq) and Terminalia bellerica (Tb.Aq) fruits. In guinea-pig tracheal preparations, Oe.Aq and Tb.Aq caused concentrationdependent (0.03-5 mg/mL) relaxation of carbachol (CCh, 1 μM) and high potassium (80 mM)-induced contractions. When tested on rabbit aortic rings, against phenylephrine (PE, 1 μM) and potassium (K+)-induced contractions, Oe.Aq and Tb.Aq caused non-specific inhibition of the induced contractions. In isolated guinea-pig atria, Oe.Aq and Tb.Aq exhibited a suppressive effect on the atrial force and the rate of contractions. These data indicate that Olea europea and Terminalia bellerica aqueous fractions possess airways and cardiovascular inhibitory activities, via calcium antagonism like verapamil

Antisecretory and analgesic activities of Terminalia bellerica

This study describes the antisecretory and analgesic activities of the crude extract of Terminalia bellerica (Tb.Cr). T. bellerica extract inhibited the castor oil-induced intestinal fluid secretion in mice at the dose range of 300 - 1000 mg/kg. The extract also dose-dependently (50 - 100 mg/kg) reduced the numbers of acetic acid-mediated writhes in mice. These results indicate that T. bellerica exhibit antisecretory and anti-nociceptive effects, hence justifying its medicinal use in diarrhea and pain

Pharmacodynamic evaluation of Terminalia bellerica for its antihypertensive effect.

Terminalia bellerica has been used as a folk medicine in a variety of ailments including hypertension. Our aim was to investigate the possible mechanism of its blood pressure (BP)-lowering effect. The crude extract of Terminalia bellerica fruit (Tb.Cr) which tested positive for flavonoids, sterols and tannins induced a dose-dependent (10-100 mg/kg) fall in the arterial BP of rats under anaesthesia. In isolated guinea-pig atria, Tb.Cr inhibited the force and rate of atrial contractions. In rabbit thoracic aorta, Tb.Cr relaxed the phenylephrine (PE, 1 μM) and K+ (80 mM)-induced contractions as well as suppressed the PE (1 μM) control peaks in the Ca++-free medium, similar to that caused by verapamil. The vasodilator effect of Tb.Cr was endothelium-independent as it was not opposed by Nω-nitro-L-arginine methyl ester in endothelium-intact rat aortic preparations and it occurred at the similar concentration in the endothelium-denuded tissues. These results indicate that Terminalia bellerica lowers BP through Ca++ antagonist mechanism and thus provides a sound mechanistic background for its medicinal use in hypertensio

Aqueous Extract of Nigella sativa Seeds Suppresses Testicular Steroidogenesis in Mice Leydig Cells in vitro.

10ABSTRACT 11Nigella sativa (black seed) is an important medicinal herb with folkloric use in wide range of diseases. It is 12well studied for its biological activities. However, there is limited information regarding its effect on the 13male reproductive system. This study describes the effect of the aqueous extract of N. sativa (NSE) on 14 testicular steroidogenesis from mice Leydig cells in vitro. Mice testicular cells were incubated in a media 15 containing either no treatment or NSE or LH alone or combination of LH and NSE. Incubations were 16 carried out for three hours in a shaking water bath at 34°C. Testosterone was measured by 17 radioimmunoassay. At all doses, NSE significantly (p \u3c 0.05) inhibited both basal and LH-stimulated in 18 vitro testosterone secretion. At a dose of l000 μg, NSE inhibited 52% of basal testosterone and 97% of 19 LH-stimulated testosterone, compared to control (0.32 ± 0.008 ng/ml) and LH alone (0.33 ± 0.01 ng/ml) 20 respectively. Thus, it is concluded that that both the basal and the LH-stimulated secretion of testosterone 21 from Leydig cells are suppressed significantly in the presence of different doses of NSE in vitro. However, 22 further studies are needed to explore the effect of chronic treatment with NSE in male and its potential to 23 be used as a contraceptive in male

Fiber-free white flour with fructose offers a better model of metabolic syndrome

BACKGROUND: The metabolic syndrome (MS) is a combination of metabolic abnormalities that lead to an increased risk of cardiovascular diseases. Due to its rising incidence and demanding life-long use of multiple drugs, there is a growing interest in testing and developing new allopathic, complementary and alternative therapies for controlling or curing disorders of MS. The discovery of new therapeutic modalities requires animal models of disease and currently available models have limitations. Developing an appropriate animal model for MS to achieve various therapeutic targets remains a challenge and this study aims to develop a rat model which closely depicts MS in humans. METHODOLOGY: Rat model of MS was developed by replacing 60% of diet with fructose. Four groups of Sprague-Dawley rats were either given whole wheat or refined flour with and without fructose for 8 weeks. Data were analyzed on SPSS and Graphpad Prism using ANOVA with Tukey\u27s and Bonferonni tests for multiple group comparison. A p-value of less than 0.05 was considered significant for differences between groups. RESULTS: Replacing whole wheat with refined wheat flour in rat chow in 60% fructose-fed Sprague-Dawley rats resulted in hypertension (p 0.01), hyper-insulinemia (p \u3c 0.001), hyperglycemia (p 0.03) and a reduction in HDL levels (p 0.002) at 4 weeks while hyper-triglyceridemia (p 0.001) with endothelial dysfunction was observed at 8 weeks. CONCLUSION: It is concluded that the refined wheat flour with 60% fructose in diet hastens the development of metabolic syndrome in 4 weeks and replacing whole wheat flour with refined flour in diet induces a more effective abnormality including a low HDL. Further studies may be directed to assess the associated pathological changes, which can be used to study the effect of different therapeutic modalities on an animal model of MS with low HDL

An in vivo study on the diuretic activity of Holarrhena antidysenterica

Holarrhena antidysenterica is used as diuretic in traditional medicine. The aim of this study was to evaluate the crude extract of H. antidysentrica seeds (Ha.Cr) and its fractions, n-hexane (Ha.Hx), n-butanol (Ha.Bu) and aqueous (Ha.Aq), for their diuretic effect in Wistar rats and to investigate whether the activity is concentrated in any of the fractions. Wistar rats kept on fasting for 24 h with water ad labium, divided into normal, positive control and treated groups were orally given normal saline (20 ml/kg), hydrochlorothiazide (HCT; 10 mg/kg) and different doses of the plant material, respectively. Immediately after dosing, the rats were housed in the metabolic cages. The urine was collected at 2 h interval for 6 h and volume, pH and electrolytes levels were measured. Ha.Cr caused dose-dependent (30 and 100 mg/kg) increase in urine output, indicating the diuretic effect. In addition, Ha.Cr increased urine contents of Na+ and K+, suggesting that the diuretic effect is mediated through increased electrolyte excretion. Similarly, the reference drug, HCT (10 mg/kg), increased urine volume and Na+ and K+ excretion. None of the resultant fractions exhibited diuretic effect comparable to that of the parent crude extract. Ha.Hx was devoid of diuretic effect, Ha.Bu exhibited a mild diuretic effect at 30 mg/kg, whereas, Ha.Aq caused a significant increase in urine output only at 100 mg/kg, indicating that the diuretic activity is distributed among fractions but in an order of increasing polarity of the solvent. The enhanced diuretic effect in the crude extract as compared to any individual fraction is suggestive of the existence of additive and/or synergistic effect in the crude extract. This study shows the presence of diuretic activity in the H. antidysentrica possibly mediated through its saluretic effect, which rationalizes its medicinal use as diuretic

Antispasmodic, Bronchodilator and Blood Pressure Lowering Properties of Hypericum oblongifolium - Possible Mechanism of Action

The crude extract of Hypericum oblongifolium (Ho.Cr), which tested positive for flavonoids, saponins and tannins caused concentration-dependent (0.1-1.0 mg/mL) relaxation of spontaneous and high K(+) (80 mM)-induced contractions in isolated rabbit jejunum preparations, suggesting a Ca(++) antagonistic effect, which was confirmed when pretreatment of the tissue with Ho.Cr produced a rightward shift in the Ca(++) concentration-response curves, like that caused by verapamil. Ho.Cr relaxed carbachol (1 mu M) and high K(+)-induced contractions in guinea pig tracheal preparations. It caused a dose-dependent (3-100 mg/kg) fall in arterial blood pressure of rats under anesthesia. In isolated guinea pig atria, Ho.Cr caused inhibition of both atrial force and rate of spontaneous contractions. When tested in rabbit aortic rings, Ho.Cr exhibited a vasodilator effect against phenylephrine (1 mu M) and high K(+)-induced contractions. These results indicate that Ho.Cr possesses gastrointestinal, respiratory and cardiovascular inhibitory effects, mediated via a Ca(++) antagonist mechanism

Studies on the in vitro and in vivo antiurolithic activity of Holarrhena antidysenterica

Background: Holarrhena antidysenterica has a traditional use in the treatment of urolithiasis, therefore, its crude extract has been investigated for possible antiurolithic effect. Materials and methods: The crude aqueous-methanolic extract of Holarrhena antidysenterica (Ha.Cr) was studied using the in vitro and in vivo methods. Results: In the in vitro experiments, Ha.Cr demonstrated a concentration-dependent (0.25–4 mg/ml) inhibitory effect on the slope of aggregation. It decreased the size of crystals and transformed the calcium oxalate monohydrate (COM) to calcium oxalate dehydrate (COD) crystals, in calcium oxalate metastable solutions. It also showed concentration-dependent antioxidant effect against 2,2-diphenyl-1-picrylhydrazyl free radical (DPPH) free radicals and lipid peroxidation induced in rat kidney tissue homogenate. Ha.Cr (0.3 mg/ml) reduced (p \u3c 0.05) the cell toxicity and LDH release in renal epithelial cells (MDCK) exposed to oxalate (0.5 mM) and COM (66 μg/cm2) crystals. In male Wistar rats, receiving 0.75% ethylene glycol (EG) for 21 days along with 1% ammonium chloride (AC) in drinking water, Ha.Cr treatment (30–100 mg/kg) prevented the toxic changes caused by lithogenic agents; EG and AC, like loss of body weight, polyurea, oxaluria, raised serum urea and creatinine levels and crystal deposition in kidneys compared to their respective controls. Conclusion: These data indicate that Holarrhena antidysenterica possesses antiurolithic activity, possibly mediated through inhibition of CaOx crystal aggregation, antioxidant and renal epithelial cell protective activities and may provide base for designing future studies to establish its efficacy and safety for clinical use