Evaluating the antidiabetic and antioxidant properties of 5- benzyl-1,3,4-oxadiazole-2-thiol

Purpose: To evaluate 5-Benzyl-1,3,4-oxadiazole-2-thiol (OXPA) for antidiabetic and antioxidant properties. Methods: Antidiabetic activity was evaluated using three in vitro models, glucose uptake by yeast cells, alpha amylase inhibition assay and hemoglobin glycosylation inhibition assays. Antioxidant potential was determined by DPPH radical scavenging, reducing power and lipid peroxidation assays. Results: OXPA showed antidiabetic activity in all the three models. The activity of the compound was comparable with that of metronidazole in glucose uptake by yeast cells, but the alpha amylase inhibition activity of the compound was slightly lower than that of acarbose, whereas the hemoglobin glycosylation inhibition activity of the compound was higher than that of vitamin E. DPPH free radical and hydrogen peroxide scavenging activity of the compound was comparable with that of vitamin C. In reducing power assay, the activity of the compound was lower than that of vitamin C (p > 0.05). Conclusion: The results of antidiabetic and antioxidant activity indicate that OXPA may be a drugcandidate for treating both diabetes and its associated oxidative stress

Bryophyllum pinnatum: BOTANICAL DESCRIPTION, VERNACULAR NAMES, PARTS USED, TRADITIONAL USES, PHYTOCHEMICAL AND PHRMACOLOGICAL ACTIVITIES

Bryophyllum pinnatum (Family: Crassulaceae) is a traditional herb that has widely been used for removal of kidney stones and is found to possess a number of pharmacological activities such as antiviral, antipyretic, antimicrobial, anti-inflammatory, antitumor, hypocholesterolemic, antioxidant, diuretic, antiulcer, styptic, antidiabetic, astringent, antiseptic, antilithic, cough suppressant, anticancer, antihypertensive, fungitoxic and uterine relaxant. The plant contains flavonoids, tannins, anthocyanins, glycosides, alkaloids, phenols, bufadienolides, saponins, coumarins, carotenoids, sitosterols, quinines, tocopherol and lectins. The flavonoids rutin, quercetin, luteolin and luteolin 7-O-β-d-glucoside detected in the plant might be a responsible factor for the anti-inflammatory effect. Diuretic and antioxidant activity of the plant could be responsible for its wide use against urolithiasis. Anthocyanidines could be responsible for the antimicrobial activity of the plant. Kaempferol 3-O-α-l-arabinopyranosyl (1→2) α-l-rhamnopyranoside) and two other polar flavonoids (quercetin 3-O-α-l- arabinopyranosyl (1→2) α-l-rhamnopyranoside and 4′, 5-dihydroxy-3′, 8-dimethoxyflavone 7-O-β-d- glucopyranoside) are responsible for the antileshmanial activity. Bufodienolides are found to have cytotoxic property and hence might be responsible for the anticancer effect. The present study is undertaken to update and ease the researchers to get a comprehensive summary of the plant regarding its botanical description, common name, parts used, traditional uses, phytochemical evaluation and pharmacological activities

Promiscuous prediction and conservancy analysis of CTL binding epitopes of HCV 3a viral proteome from Punjab Pakistan: an In Silico Approach

<p>Abstract</p> <p>Background</p> <p>HCV is a positive sense RNA virus affecting approximately 180 million people world wide and about 10 million Pakistani populations. HCV genotype 3a is the major cause of infection in Pakistani population. One of the major problems of HCV infection especially in the developing countries that limits the limits the antiviral therapy is the long term treatment, high dosage and side effects. Studies of antigenic epitopes of viral sequences of a specific origin can provide an effective way to overcome the mutation rate and to determine the promiscuous binders to be used for epitope based subunit vaccine design. An <it>in silico </it>approach was applied for the analysis of entire HCV proteome of Pakistani origin, aimed to identify the viral epitopes and their conservancy in HCV genotypes 1, 2 and 3 of diverse origin.</p> <p>Results</p> <p>Immunoinformatic tools were applied for the predictive analysis of HCV 3a antigenic epitopes of Pakistani origin. All the predicted epitopes were then subjected for their conservancy analysis in HCV genotypes 1, 2 and 3 of diverse origin (worldwide). Using freely available web servers, 150 MHC II epitopes were predicted as promiscuous binders against 51 subjected alleles. E2 protein represented the 20% of all the predicted MHC II epitopes. 75.33% of the predicted MHC II epitopes were (77-100%) conserve in genotype 3; 47.33% and 40.66% in genotype 1 and 2 respectively. 69 MHC I epitopes were predicted as promiscuous binders against 47 subjected alleles. NS4b represented 26% of all the MHC I predicted epitopes. Significantly higher epitope conservancy was represented by genotype 3 i.e. 78.26% and 21.05% for genotype 1 and 2.</p> <p>Conclusions</p> <p>The study revealed comprehensive catalogue of potential HCV derived CTL epitopes from viral proteome of Pakistan origin. A considerable number of predicted epitopes were found to be conserved in different HCV genotype. However, the number of conserved epitopes in HCV genotype 3 was significantly higher in contrast to its conservancy in HCV genotype 1 and 2. Despite of the lower conservancy in genotype 1 and 2, all the predicted epitopes have important implications in diagnostics as well as CTL-based rational vaccine design, effective for most population of the world and especially the Pakistani Population.</p

Glutathione sulfotransferase inhibition activity of a self-fermented beverage, Kanji

Context: Kanji, a liquid preparation of roots of Daucus carota L. ssp. sativus (Hoffm.) Arcang. var. vavilovii Mazk. (Apiaceae), may inhibit glutathione sulfotransferase (GST) activity due to ferulic acid content. Objectives: GST inhibition activity and characterization of Kanji and methanol extract of D. carota roots, and oral absorption pattern of ferulic acid from Kanji in rats. Materials and methods: GST inhibition activity of Kanji and methanol extract of D. carota roots in concentration range 0.001–100.00 mg/mL was determined using Sprague Dawley rat liver cytosolic fraction. Methanol extract upon column chromatography gave ferulic acid, which was used to characterize Kanji and determine its oral absorption pattern in Wistar rats. Results: The GST inhibition activity of Kanji (100.00 μg/mL), methanol extract of D. carota roots (100.00 μg/mL) and tannic acid (10.00 μg/mL, positive control) was found to be 0.162 ± 0.016, 0.106 ± 0.013 and 0.073 ± 0.004 μM/min/mg, respectively. Different Kanji samples and methanol extract contained ferulic acid (0.222–0.316 mg/g) and 0.77 mg/g, respectively. Ferulic acid did not appear in plasma after oral administration of Kanji. Discussion: Kanji having solid contents 80.0 μg/mL, equivalent to 0.0025 μg/mL ferulic acid, does not inhibit the activity of GST. The oral administration of Kanji, in human equivalent dose (528 mg/kg, 16.67 μg ferulic acid), to rats indicated poor absorption of ferulic acid. Conclusion: Kanji having solid contents 14–36 mg/mL does not inhibit GST activity, hence may not interfere with drugs that are the substrates of GST, if taken concomitantly

Glutathione sulfotransferase inhibition activity of a self-fermented beverage, <i>Kanji</i>

<p><b>Context:</b><i>Kanji,</i> a liquid preparation of roots of <i>Daucus carota</i> L. ssp. <i>sativus</i> (Hoffm.) Arcang. var. <i>vavilovii</i> Mazk. (Apiaceae), may inhibit glutathione sulfotransferase (GST) activity due to ferulic acid content.</p> <p><b>Objectives:</b> GST inhibition activity and characterization of <i>Kanji</i> and methanol extract of <i>D. carota</i> roots, and oral absorption pattern of ferulic acid from <i>Kanji</i> in rats.</p> <p><b>Materials and methods:</b> GST inhibition activity of <i>Kanji</i> and methanol extract of <i>D. carota</i> roots in concentration range 0.001–100.00 mg/mL was determined using Sprague Dawley rat liver cytosolic fraction. Methanol extract upon column chromatography gave ferulic acid, which was used to characterize <i>Kanji</i> and determine its oral absorption pattern in Wistar rats.</p> <p><b>Results:</b> The GST inhibition activity of <i>Kanji</i> (100.00 μg/mL), methanol extract of <i>D. carota</i> roots (100.00 μg/mL) and tannic acid (10.00 μg/mL, positive control) was found to be 0.162 ± 0.016, 0.106 ± 0.013 and 0.073 ± 0.004 μM/min/mg, respectively. Different <i>Kanji</i> samples and methanol extract contained ferulic acid (0.222–0.316 mg/g) and 0.77 mg/g, respectively. Ferulic acid did not appear in plasma after oral administration of <i>Kanji.</i></p> <p><b>Discussion:</b><i>Kanji</i> having solid contents 80.0 μg/mL, equivalent to 0.0025 μg/mL ferulic acid, does not inhibit the activity of GST. The oral administration of <i>Kanji,</i> in human equivalent dose (528 mg/kg, 16.67 μg ferulic acid), to rats indicated poor absorption of ferulic acid.</p> <p><b>Conclusion:</b><i>Kanji</i> having solid contents 14–36 mg/mL does not inhibit GST activity, hence may not interfere with drugs that are the substrates of GST, if taken concomitantly.</p

Chemical and pharmacological comparison of modern and traditional dosage forms of <i>Joshanda</i>

<p>Recently, a traditional remedy (<i>Joshanda)</i> has been replaced largely by modern ready-to-use dosage forms, which have not been compared to the original remedy. Therefore, the present study aimed to compare a number of modern dosage forms with traditional remedy. Seven brands, 3 batches each, were compared with a Lab-made formulation with reference to analytical (proximate analyses, spectroscopic and chromatographic metabolomes) and pharmacological profiles (anti-inflammatory and antibacterial activities). Chemical and pharmacological differences were found between Lab-made <i>Joshanda</i> and modern dosage forms. Such variations were also found within the brands and batches of modern formulations (<i>p</i> < 0.05). The Lab-made <i>Joshanda</i> showed significantly higher pharmacological activities as compared to modern brands (<i>p</i> ). The results of the present study indicate that modern dosage forms are unstandardised and less effective than the traditional remedy. Characteristic profiles obtained from Lab-made <i>Joshanda</i> may be used as reference to produce comparable dosage forms.</p