Posted by admin on Nov 30, 2019 in |
Protein tyrosine phosphatase 1B (PTP1B) is an important target for diabetes since inhibition of PTP1B offers therapeutic benefits in insulin-resistant diabetes. Considering this fact in present investigation various heterocyclic derivatives of chalcone were synthesized and evaluated for their PTP1B inhibitory activity as antihyperglycemic agents. Heterocyclic derivatives; isoxazoline (II A-II E), and pyrazoline (III A – III E / VIA-VIC) were synthesized through cyclization of chalcone intermediates and structures of final compounds were established using various spectral analysis techniques such as; IR, 1H-NMR and mass. Compounds were screened for their antihyperglycemic activity using sucrose loaded diabetic model. Isoxazoline derivatives offered potent antihyperglycemic response than correspondence pyrazoline derivatives. Compounds bearing isoxazoline ring II A and II E showed maximum % fall of blood glucose level than control group which was comparable to the standard drug metformin. The newer compounds VIA, VIB, and VIC also evaluated for their anti-hyperglycemic activities, compound VIC showed appreciable response (62.5% antihyperglycemic activity). The result of biological activity was also anticipated by molecular docking study which was...
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Posted by admin on Nov 30, 2019 in |
Introduction: In spite of the progress made in surgical techniques for cataract removal all over the world during last ten years; still age related cataract remains the leading cause of visual impairment. The etiology of cataract is multi-factorial and oxidative damage is one of the causes. Aim: To estimate oxidative stress by markers like enzymatic antioxidant Superoxide Dismutase (SOD) and lipid peroxiation product Malondialdehyde (MDA) in age related cataract (ARC) subjects and compare them with healthy control subjects. Materials and Methods: This case control study was performed in 100 subjects divided into 2 groups – 50 subjects with age related cataract and 50 age and gender matched healthy controls. Oxidative stress was assessed by estimation of erythrocytic SOD and serum MDA. Results: Serum MDA levels were significantly high and erythrocytic SOD levels were significantly low in age related cataract than controls (P<0.05). There was no significant difference in these parameters in subjects with different subtypes of age related cataract. Conclusion: Oxidative stress with increased oxidants and decreased antioxidants defense...
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Posted by admin on Nov 30, 2019 in |
Depression is the most common and spreadable disorder in recent age as people are going through a lot of pressure in their daily work caliber and so many unconditional events. A new approach called derivatization spectroscopy was developed for the anti-depressant agent, marketed formulation of Bupropion hydrochloride, to confirm the interfering substances from the excipients of solid dosage form, in addition to that the stability parameters to assure the analysis time with the minimum usage of the reference standard and sample solution. The present work aims to develop simple, sensitive stability indicating the method to develop a model to estimate BPH in the solid dosage form by using derivative spectroscopy tool to avoid the excipients interferences in the developed assay method. First, made the stock solution of 100 µg/ml from 1000 µg/ml previously prepared solution. The method was validated over the concentration range of 5-50 µg/ml of marketed formulation of Bupropion Hydrochloride. The assay method & derivatization was performed using UV spectroscopy at 252 nm wavelength. The intra-assay &...
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Posted by admin on Nov 30, 2019 in |
In this manuscript, we designed and synthesized 1,4-naphthoquinone derivatives. These derivatives were characterized using the different analytical techniques such as 1H NMR, 13C NMR, FTIR, Mass spectroscopy, melting point, and elemental analysis. The synthesized compounds (MB (1-10)) further subjected to assess the anticancer activity using different cancer cell lines such as MCF-7, HeLa, and HepG2. The compound MB-10 was observed to be the most active against these three cancer cell lines i.e. MCF-7 (IC50 = 16.13± 0.29 µM), HeLa (IC50 = 12.98 ± 0.37 µM) and HepG2 (IC50 = 18.73 ± 0.65 µM). Compound MB10 has also shown potent tyrosine kinase inhibitory activity with IC50 = 1.23 ± 0.12 µM. Moreover, molecular docking investigation revealed that compound MB-10 has strong binding affinity to the amino residue of the active site of enzyme protein tyrosine kinase, which contingent the cytotoxic activities. These outcomes give promising beginning stages to assist in the improvement of cancer as novel and powerful anticancer...
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Posted by admin on Nov 30, 2019 in |
A simple, efficient HPLC method has been developed and validated for simultaneous determination of Amantadine hydrochloride and Oseltamivir phosphate using pre-column derivatization with phenyl isothiocyanate (PITC). The chromatography separation was achieved on Phenomenex C18 column of 250 × 4.6 mm 5 µm particle size, mobile phase used for chromatographic run consisted of acetonitrile and water (60: 40% v/v) with a flow rate of 2 mL/min. The analysis was performed at ambient temperature, and the eluent was monitored at 250 nm using a UV detector. The retention time of Amantadine hydrochloride and Oseltamivir phosphate was found to be 7.1 min and 3.2 min. The limit of detection (LOD) for Amantadine hydrochloride and Oseltamivir phosphate was observed to be 0.1µg/mL and 0.25 µg/mL, respectively. Limit of quantification (LOQ) was found to be 0.5 µg/mL and 0.25 µg/mL. The developed method was validated as per ICH guidelines using parameters like linearity, specificity, precision, linearity, accuracy, ruggedness, robustness, LOD, and LOQ. All the validation parameters were found to be well within the acceptance...
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