Posted by admin on Nov 30, 2019 in |
Cancer is one of the emergings, and best-understood neoplasm’s from a genetic perspective, yet it remains the second most common cause of cancer-related death, indicating that some of its cancer cells are not removing completely by current therapies. Chitosan is a polysaccharide β-linked D-glucosamine and N-acetyl-D-glucosamine were used as conjugate to 5Fluorouracil. 5FU is one of the most commonly used drugs to treat cancer. The present invention relates the 5 Fluorouracil drug react with chitosan and formed chitosan – 5FU conjugate and used as Nobel anticancer models in zebrafish as an alternative model. The conjugated drug may highly selective and sustain release of drug to treat effectively colon cancer models in zebrafish. 5-fluorouracil react with chloroacetic acid in presence of potassium hydroxide gives 5-fluorouracil acetic acid. 5-fluorouracil acetic acid reacts with chitosan and formed chitosan -5FU conjugate. Characterization of chitosan folic acid and chitosan 5FU studied details by FTIR and NMR and showed well structural...
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Posted by admin on Nov 30, 2019 in |
2-Pyrazolines are well known, and important nitrogen-containing five-membered heterocyclic compounds which belong to the family of azoles and have been found to possess considerable activities, like anticancer, antibacterial, antifungal, immunosuppressant and antiamoebic activity. In the present work, ten novel pyrazolines were prepared from chalcones, characterized and evaluated for their antibacterial activity against Staphylococcus aureus and Escherichia coli using Ciprofloxacin as standard and using DMSO as a solvent. Their activity was evaluated by measuring the zone of inhibition in mm. All the compounds exhibited antibacterial activity against Staphylococcus aureus and Escherichia coli. Among ten derivatives of compounds synthesized, the derivative with 2-chloro and 4-chloro substituted phenyl rings attached to pyrazolines exhibited the highest activity against both types of organisms. The derivatives with an unsubstituted phenyl group attached to pyrazolines exhibited comparatively less activity. Thus it can be concluded that pyrazolines containing substituted phenyl groups are effective broad spectrum antibacterial agents, and they can be developed as effective antibacterial...
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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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