Aqueous Extract of Flueggea leucopyrus Increases Urine Output in Rats

Purpose: To investigate the effect of Flueggea leucopyrus Wild aqueous extract (FLAE) on the urinary output of rats.Method: Three different doses of FLAE (500, 1000 and 1500 mgkg-1), furosemide (13 mg kg-1 as diuretic reference) and distilled water (as control) were orally administered to healthy adult hydrated rats. Cumulative urine output was monitored hourly over 6 h. Selected urinary parameters were determined for 1500 mg kg-1 dose, furosemide, and water-treated groups to investigate the possible mode of action. Using these data, standard urine indices were calculated. Glomerular filtration rate (GFR) in terms of creatinine clearance, overt toxicity, renal toxicity, liver toxicity, as well as phytochemical screening were also determined.Results: The highest dose (1500 mgkg-1) significantly increased urine output (control vs. treated: 0.74 ± 0.07 vs. 1.38 ± 0.09 mL/100 g) (p < 0.05) r2 = 0.925). The effect of FLAE was dose-dependent. Increase in urine output was observed from the 1st hour, peaked at 2nd hour and lasted till the 6th hour. Furthermore, 1500 mgkg-1 dose of FLAE caused a significant (p < 0.05) increase in urinary K+ level, aldosterone secretion index, thiazide secretion index and GFR at 24 h. However, significant decrease in urinary Na+ level (control vs. treated: 7915.2 ± 423.1 vs. 6611.2 ± 181.3 ppm) was noted with the highest dose (p < 0.05). Serum alanine transaminase (ALT), serum aspartate transaminase (AST) and urea levels were not altered significantly (p > 0.05). However, serum creatinine level was elevated significantly (p < 0.05). Phytochemical screening showed that FLAE contains primary, secondary, tertiary, quaternary alkaloids/amine oxides, triterpenoids, unsaturated sterols, leucoanthocyanins, tannins of pyrogallol type and cyanogenic glycoside.Conclusion: The results show that FLAE exhibits moderate oral aquaretic activity.Keywords: Flueggea leucopyrus, Diuretic, Aquaretic, Urine output, Toxicity, Phytochemica

Expression and function of G-protein-coupled receptorsin the male reproductive tract

This review focuses on the expression and function of muscarinic acetylcholine receptors (mAChRs), α1-adrenoceptors and relaxin receptors in the male reproductive tract. The localization and differential expression of mAChR and α1-adrenoceptor subtypes in specific compartments of the efferent ductules, epididymis, vas deferens, seminal vesicle and prostate of various species indicate a role for these receptors in the modulation of luminal fluid composition and smooth muscle contraction, including effects on male fertility. Furthermore, the activation of mAChRs induces transactivation of the epidermal growth factor receptor (EGFR) and the Sertoli cell proliferation. The relaxin receptors are present in the testis, RXFP1 in elongated spermatids and Sertoli cells from rat, and RXFP2 in Leydig and germ cells from rat and human, suggesting a role for these receptors in the spermatogenic process. The localization of both receptors in the apical portion of epithelial cells and smooth muscle layers of the vas deferens suggests an involvement of these receptors in the contraction and regulation of secretion.Esta revisão enfatiza a expressão e a função dos receptores muscarínicos, adrenoceptores α1 e receptores para relaxina no sistema reprodutor masculino. A expressão dos receptores muscarínicos e adrenoceptores α1 em compartimentos específicos de dúctulos eferentes, epidídimo, ductos deferentes, vesícula seminal e próstata de várias espécies indica o envolvimento destes receptores na modulação da composição do fluido luminal e na contração do músculo liso, incluindo efeitos na fertilidade masculina. Além disso, a ativação dos receptores muscarínicos leva à transativação do receptor para o fator crescimento epidermal e proliferação das células de Sertoli. Os receptores para relaxina estão presentes no testículo, RXFP1 nas espermátides alongadas e células de Sertoli de rato e RXFP2 nas células de Leydig e germinativas de ratos e humano, sugerindo o envolvimento destes receptores no processo espermatogênico. A localização de ambos os receptores na porção apical das células epiteliais e no músculo liso dos ductos deferentes de rato sugere um papel na contração e na regulação da secreção.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Universidade Federal de São Paulo (UNIFESP) Escola Paulista de Medicina Departamento de FarmacologiaUNIFESP, EPM, Depto. de FarmacologiaSciEL

In vitro Antiglycation and Cross-Link Breaking Activities of Sri Lankan Low-Grown Orthodox Orange Pekoe Grade Black Tea (Camellia sinensis L)

Purpose: To investigate the antiglycation and cross-link breaking activities of Sri Lankan low-grown orthodox Orange Pekoe grade black tea (Camellia sinensis L)Methods: Five concentrations (6.25, 12.5, 25.0, 50.0 or 100.0 ìg/ml) of Black tea brew (BTB) were made using Sri Lankan low-grown Orange Pekoe (O.P.) grade tea. Antiglycation and advanced glycation end products (AGEs) cross-link breaking activities of BTB as well as the antiglycation activityof rutin were determined in vitro on bovine serum albumin/glucose system using fluorescence spectroscopy.Results: BTB induced significant (p<0.05) antiglycation activity (IC50, 19.04 ± 5.18 µg/ml) and AGEs cross-link breaking activities (IC50, 82.89 ± 3.44 ìg/ml). These effects were dose-dependent. Further, the antiglycation activity of BTB was comparable to rutin, a well-known antiglycation agent (IC50, 21.88 ± 2.82 ìg/ml).Conclusion: These results show that Sri Lankan low-grown O.P. grade black tea possesses both antiglycation and AGEs cross-link breaking activities in vitro and thus provides scientific justification for the use of black tea in Sri Lankan indigenous medicine for the management of diabetic  complications.Keywords: Diabetic complications, Antiglycation, Glycotoxin, Black tea, Cross-link breakers, Sri Lankan tea, Orange Pekoe te

Antidiuretic Activity of the Methanol Extract of Aporusa lindleyana Wight (Euphorbiacea) Baillon in Rats

Purpose: To determine the diuretic activity of Aporusa lindleyana in rats following its claimed use in Sri Lankan traditional medicine.Methods: Three doses (500, 1000 and 1500 mg/kg) of the methanol extract (ME) of Aporusa lindleyana (Leaf and bark in 5:1 ratio) were orally administered to female, adult Sprague Dawley rats. Furosemide, vasopressin (antidiuretic hormone) and distilled water were used as diuretic reference, antidiuretic reference and control, respectively. Urine output was recorded up to 6 h at hourly intervals. To investigate the mode of action, pH, specific gravity, conductivity, total dissolve solids, Na+, K+, Ca2+, Mg2+, leucocytes, nitrite, urobilinogen, protein, blood, ketones, bilirubin and glucose were tested in the urine of 500 mg/kg treated and control rats. Six hours later, serum electrolyte levels (Na+, K+, Ca2+ and Mg2+) were evaluated. Glomerular filtration rate (GFR) was also determined in terms of creatinine clearance. Overt toxicity, hepatotoxicity, nephrotoxicity and a phytochemical studies were conducted.Results: Significant (p < 0.05) reduction of urine output (by 45 %) and aldosterone secretion index (Na+/K+) were observed while sodium (by 38 %) and potassium (by 114 %) levels were increased significantly (p < 0.05). GFR was not changed significantly (p > 0.05). Further, the methanol extract (leaf/bark in 5:1 ratio) was non-toxic in terms of overt signs of toxicity, serum alanine transaminase (ALT) and aspartate aminotransferase (AST), urea and creatinine levels. Phytochemical evaluation revealed the presence of alkaloids, unsaturated sterols, unsaturated terpenes, unsaturated lactones, lucocyanins, tannins and polyphenols and cyanogenic glycosides.Conclusion: The methanol extract of Aporusa lindleyana has moderate and safe oral antidiuretic activity.Keywords: Aporusa lindleyana, Antidiuretic, Diuretic, Toxicity, Phytochemicals, Sri Lankan traditional medicin