Posted by admin on Sep 30, 2017 in |
The renin-angiotensin system (RAS) plays an important role in pathogenesis of hypertension, congestive heart failure, and chronic renal failure. In addition to a discussion of the current understanding of the chemical structures and the modes of action of angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor (ATR) antagonists, review includes their SAR analysis and chemical modification for improving their activity. Nowadays different modeling strategies are underway to develop tailor made molecules with the best of properties among nonpeptide renin inhibitors, dual action receptor antagonists (e.g. angiotensin and endothelin antagonists, ACE/NEP inhibitors, AT1/TxA2 antagonists, balanced AT1/AT2 antagonists), triple inhibitors. In the first part is given an overview of various ACE inhibitors. The second part is devoted to overview of angiotensin receptor antagonists. The advances that have been made, new opportunities, and future directions of design and development of these classes have been...
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Posted by admin on Sep 30, 2017 in |
The present study was assessed to determine the effect of various grades of phospholipids on liposomes. The various grades of synthetic phospholipids such as Phospholipon 90G® (PL90G), Phospholipon 80H® (PL80H) and Phospholipon 90H® (PL90H) were used along with cholesterol in stoichiometric ratio (1:0.25, 1:0.5, 1:1, 1:2, 1:3). Using these ratios the paclitaxel liposome was formulated by film hydration method. The prepared liposomes were assessed for characterization using entrapment efficiency, vesicular size, in vitro release and hemolytic toxicity assay. The synthetic grades of phospholipids significantly influenced paclitaxel liposomal formulations. The stoichiometric ratio (1:1) between cholesterol and various synthetic phospholipids was found to be optimized one, from rest of ratios. The characterization confirmed the formation of liposomes. The entrapment efficiency was observed to be high as increasing the ratios between cholesterol and phospholipids, but then declined suddenly as further increasing the ratio. The best liposomal formulations showed the spherical shape with size ranging from <10µm. The optimized paclitaxel liposomes % release in phosphate buffer (pH 7.4) enhanced significantly, and rest of...
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Posted by admin on Sep 30, 2017 in |
Bombax ceiba Linn. is one of the important plant species used in various system of medicine. Almost every part of plant is used as medicine and its roots and flowers are used for curing maximum number of ailments. Leaves of the plants are also containing different important secondary metabolites. For the use as safe herbal medicine the plant material (leaves) has to be standardized with the establishment of a consistent biological activity. Pharmacognistic studies includes different Physicochemical parameters like Proximate analysis of plant material such as Fluorescence Analysis, percentage of loss on drying (Moisture content), Total ash, Acid Insoluble ash, Water Soluble ash, used for the standardization, as per guideline of the in Indian Pharmacopoeia. Evaluation of drug in this ways was done for the confirmation of its identity and determination of its quality and purity and detection of nature of adulteration. Sterols present in plant called as Phytosterols. Phytoesterols with the principle advantage that inhibit the absorption of cholesterol and lower serum cholesterol levels was detected by basic...
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Posted by admin on Sep 30, 2017 in |
Modification of a drug molecule of a series having optimal activity is widely used and continues to be an important factor necessary for new drug discovery. Infectious diseases which increase dramatically by resistant and multi resistant microbes are now a days the second major cause of death worldwide and the third leading cause of death in the developed countries. Although, the search for new lead structures for the development of antimicrobial agent is an increasingly important problem in medicinal chemistry. The treatment of infectious diseases still remains an important and challenging area of research due to multidrug resistance by microbes. The increasing incident of drug resistance in treatment of microbial diseases emphasizes worldwide need for newer antimicrobial agents. To treat these infectious diseases, a route is established to synthesize the pharmacological active novel chromone based sulfonamide derivatives i.e. substituted N- (3 –formyl -4-oxo -4H –chromen -2-yl) -N-phenyl benzene sulfonamide having antibacterial and antifungal activities. The objectives of the present work are: 1) To synthesize various derivatives of substituted N-(3-formyl-4-oxo-4H-chromen-2-yl)-N-phenyl...
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Posted by admin on Sep 30, 2017 in |
Type 2 diabetes (T2D) is one of the risk factor for dry eye disease (DED) and known factor for diabetic retinopathy (DR). There are few studies have been already reported the prevalence of DED nevertheless studies shown prevalence of DED and DR by sex in patients with T2D. The study was carried out with 100 T2D patients. DED was assessed with Tear break up time and Schirmer tests. All the subjects were examined by slit lamp bio-microscopy and colored fundus photographs. Diabetic retinopathy (DR) was graded according to early Treatment Diabetic Retinopathy (ETDRS) criteria. Out of 100 T2D patients, the prevalence of DED was noticed in 53 patients. Out of 53 DED cases, 14 (43.8%) were males and 39 (57.4%) were females. Next we assessed the association of DED with DR and it was found 47.6% in males and 69.4% in females. In our study, the prevalence of DED was high in T2D patients and showed to have a high correlation with DR. Prevalence of DED was more in...
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