Posted by admin on Sep 30, 2016 in |
Coccinia grandis (Linn.) Voigt (Cucurbitaceae) has been widely used for the management of diabetes mellitus in Sri Lankan traditional medicine. The aim of the present study was to investigate antihyperlipidemic, antioxidative effects of the leaf extract of C. grandis in sterptozotocin induced diabetic rats and to standardize the leaf extract of C. grandis by standard analytical methods. The results showed that the concentration of serum total cholesterol, triglycerides and low density lipoprotein cholesterol were significantly lower in C. grandis (0.75 g/kg) treated rats than in diabetic control rats (P < 0.05). In addition, an improvement in the antioxidant potential is also showed in C. grandis treated diabetic rats. P < 0.05). The polyphenolic compounds, alkaloids flavonoids, saponins and sterols/tritepenoids were present in the C. grandis extract. The results revealed that the aqueous leaf extract of C. grandis (0.75 g/kg) exerted antihyperlipidemic and antioxidative effects in diabetic rats, corroborating the therapeutic use of C. grandis leaf extract in the management of diabetic complications in traditional...
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Posted by admin on Sep 30, 2016 in |
Background and Aim: Valproic acid (VPA) is a widely used antiepileptic drug. The main pathway of its elimination is through conjugation by UDP-glucuronosyltransferases with several polymorphic forms. In this study, we aimed to examine the effect of polymorphism in UGT1A6 enzyme-coding gene at two loci, namely, 541A>G and 552A>C on clinical outcome in Egyptian children with idiopathic epilepsy. Clinical outcome investigations involved VPA serum level, seizure control and incidence of adverse drug reactions (ADR). Methods: Genetic polymorphisms were detected in 48 patients receiving VPA monotherapy by PCR-RFLP. Steady state concentrations at trough level were determined by homogenous enzyme immunoassay technique. Patients were monitored for ADR, seizure frequency as well as seizure severity (SS). Results: Variant genotype group (AC & CC) had lower concentration to dose ratios (CDR) than those with (AA) genotype for UGT1A6 552A>C (p=0.029). Variant allele carriers had significantly lower CDR than wild allele carriers for both 541A>G and 552A>C (p= 0.047 and p= 0.001, respectively). Wild genotype for 552A>C had higher SS scores on Chalfont scale...
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Posted by admin on Sep 30, 2016 in |
In this study, homology modeling and molecular docking studies were performed to explore structural features and binding mechanism of synthesized benzimidazole derivatives as ubiquitin inhibitors. A homology modeling procedure was employed to construct a 3D model of ubiquitin protein by using MODELLER9.15. For this procedure, the X-ray crystal structure of Gumby / fam105b in Complex with linear Di-ubiquitin (PDB ID: 4KSL) at 2.83 Å resolution was used as template. The predicted model was analyzed by PROCHECK. The 3D structure of predicted model shows 93.9% of amino acids in most favored region. The predicted model was used for molecular docking studies by using Autodock4.2. All the synthesized benzimidazole derivatives show good binding energy and interactions with the model. Compound one shows three interactions with Asp348, Leu297 and...
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Posted by admin on Sep 30, 2016 in |
Curcuminoids are dietary phytochemicals obtained from dried rhizomes of turmeric plant (Curcuma longa). Curcuminoids are mixture of curcumin, demethoxy curcumin and bisdemethoxy curcumin in which curcumin is a major constituent. Several polymorphic forms of curcumin were reported. The present study relates to the preparation of different solid forms of curcuminoids and to study the influence of other constituents of curcuminoids on the polymorphic behaviour of curcumin. The developed solid forms were characterized by various spectral methods like Fourier Transform Infrared Spectroscopy (FTIR), Powder X- ray diffraction (PXRD), Differential Scanning Calorimetry (DSC) and Scanning Electron microscopy (SEM). On crystallization from ethanol and upon melt crystallization, curcuminoids underwent transformation into an amorphous form. Grinding did not affect the polymorphic nature of curcuminoids. These findings suggest that curcuminoids undergo polymorphic modifications very similar to...
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Posted by admin on Sep 30, 2016 in |
Nanoparticles (NPs) have been extensively studied during the past few decades due to their well-recognised applicability. Thus, the present study was aimed to fabricate Carvedilol (CVD) a β-adrenoceptor antagonist, as NPs aiming towards the optimal physicochemical characteristics and improved solubility. The prepared NPs demonstrated a linear increase in the mean particle size from253 ± 19 to 598 ± 21 nm and entrapment efficiency (%EE) from 58.6% to 91.1%, when drug-to-polymer mass ratio was increased from 1:1 to 1:5. In vitro release studies showed significant variation in the rate and extent of CVD release from polymeric matrix at various pHs of release media (pH 1.2, pH 6.8 and distilled water) and drug-to-polymer mass ratios. The present study highlighted the optimal formulation conditions to fabricate CVD-loaded NPs with best physicochemical characteristics, improved solubility of incorporated drug and explored the prospects of manipulation and optimisation of the NPs for intended...
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