Current Issue : April - June Volume : 2010 Issue Number : 1 Articles : 7 Articles
This review shows the targeted site for the prevention of cancer. In normal human, cell proliferation and cell destruction process is controlled by positive and negative regulation. In positive control, two families of proteins; cyclin and cyclin dependent kinases (cdks) have a major role. Each cdk is inactive until it binds to a cyclin, the binding enabling the cdk to phosphorylate the protein(s) necessary for a particular step in the cell cycle. In negative regulation, the mediators either stop the cell cycle or produce cell death (apoptosis). In, lung cancer and other cancer imbalance between positive and negative regulator take place. That means Activation of the positive regulator and inhibition of negative regulator may lead to different cancer. So the cell(s) under goes uncontrollable cell division and differentiation. Worldwide, lung cancer is the most common cancer in terms of both incidence and mortality (1.35 million new cases per year and 1.18 million deaths), with the highest rates in Europe and North America. It is the second most commonly occurring form of cancer in most Western countries Mostly it is develop by inactivation of tumor suppressor genes. Damage to chromosomes 3p, 5q, 13q, and 17p are particularly common in small cell lung carcinoma. The p53 tumor suppressor gene, located on chromosome 17p, is affected in 60-75% of cases also Mutations and amplification of EGFR are common in non-small cell lung cancer and inhibit the programmable cell death that means the apoptosis which play major roll in cell death. So these all are the main target for the anti cancer therapy....
Renal ischemia reperfusion (I/R) causes distant organ damage such as cardiac injury and diabetes mellitus type 2 (T2DM) increases sensitivity to I/R and cardiac injury. Hence, the present study examined whether treatment with exenatide improve the cardiac injury in a renal I/R injury using a T2DM rat model. To fulfill the objective, male wistar rats were divided into five groups. In vivo renal I/R were performed in both T2DM and normal rats. Each protocol comprised ischemia for 30 min followed by reperfusion 24 hrs and exenatide treatment period 14 days before induction of ischemia. Diabetic rats that underwent renal I/R in exhibited significant increase in the serum concentrations of lactate dehydrogenase (p < 0.01) and creatinine kinase (p < 0.01) as compared to non-diabetic rats. Lipid peroxidation, xanthine oxidase activity, myeloperoxidase activity and nitric oxide level in cardiac tissue were significantly (p < 0.05) increased after I/R in diabetic rats compared to non-diabetic rats. Antioxidant enzymes like glutathione (p < 0.05) and catalase (p < 0.05) were significantly reduced after I/R in diabetic rats compared to non-diabetic rats. Exenatide treatment significantly (p < 0.05) normalized these biochemical parameters compared to diabetic I/R rats. In conclusion, exenatide treatment attenuated cardiac injury induced by renal I/R in diabetic rats. This is the first study in which exenatide was used to prevent cardiac injury induced by I/R in diabetes via NO generation and neutrophil sequestration in the cardiac tissue....
Embelia ribes Burm. is a large scandent shrub with long, slender, flexible branches belongs to the family Myrsinaceae. The plant is used traditionally in treating renal disorders. Current study was designed to scientifically evaluate the traditional claims of nephroprotective effect of Embelia ribes fruits alone and in combination with vitamin E against gentamicin-induced nephrotoxicity in rats. Nephroprotective effects of ethanol extract of Embelia ribes fruits alone (200 and 400 mg/kg, p.o), and in combination with vitamin E (α-tocopherol) (200 mg/kg, p.o) was studied against gentamicin (40mg/kg/day, i.p)-induced nephrotoxicity in rats for 14 days. Serum urea, creatinine and blood urea nitrogen were the parameters evaluated. The serum urea, creatinine and blood urea nitrogen levels in the gentamicin alone treated group were significantly elevated (P<0.01) with respect to control group, whereas the body weight was significantly lowered with respect to control group. The serum urea, creatinine and blood urea nitrogen levels were reduced in the Embelia ribes fruits extract treated and vitamin E treated groups. The renal levels of reduced glutathione (GSH) were declined in gentamicin alone treated group. The level of GSH were elevated significantly (P<0.05) the Embelia ribes fruits) and Embelia ribes fruits (200 mg/kg) with vitamin E (200 mg/kg) treated groups. Ethanol extract of Embelia ribes fruits alone and in combination with vitamin E, partially ameliorated gentamicin-induced nephrotoxicity....
P. aeruginosa is responsible for severe chronic infections in patients which suffer from chronic lung diseases. Current therapies for treatment infections include dual antibiotic therapies. However P. aeruginosa has developed resistance to many of these antibiotics and the microenvironment of the lung in these patients and various survival strategies of this pathogen decrease the affectivity of the antibiotics which has resulted in urgent need for new therapeutics and new approaches for treatment. In this study effect of mixture of extracts of A. calamus and S. anacardium were studied on chronic P. aeruginosa lung infections in rats. Results show eradication of bacteria from lungs of rats, decreased inflammation and oxidative stress and recovery of lung function marked by initiation of regeneration of alveolar walls....
The aim of this study is to characterize the intestinal transport of vincristine and to predict the human intestinal permeability and fraction absorbed using SPIP.Permeability Coefficient and the effect of P-gp modulators on Vincristine Sulphate were studied in anaesthetized rats. Single Pass Intestinal Perfusion was performed in the jejunal segment. The rationale for the selection of jejenum is due to the overexpression of P-glycoprotein when compared with other segments. Drug solution (150µg/ml) in phosphate buffer saline was perfused at a flow rate of 0.2ml/min.Besides,P-gp inhibitor verapamil(200 µg/ml) and inducer Rifampicin (60mg/ml) were coperfused with Vincristine to detect its disposition characteristics affected by P-gp .Drug concentrations in samples were analyzed using HPLC. Stability studies were conducted to ensure the loss of Vincristine due to absorption.The effective permeability value of Vincristine (150µg/ml) in the jejunal segment was found to be lower due to the efflux mediated by P-gp.When coperfused with verapamil its permeability significantly enhanced as it is a P-gp inhibitor and vice versa with Rifampicin which is a P-gp inducer. Subsequently the human intestinal permeability was estimated considering Peff(human) =1.04 Peff(rat)-0.0003. P-Glycoprotein mediated drug resistance is one of the serious limitations of Vincristine efficacy and jejunal segment is found to have major MDR expression. The Peff value of Vincristine was found to be increased upon the co-perfusion with verapamil and similarly reduced with Rifampicin which are inhibitors & inducers respectively indicating Vincristine is efficiently transported by P-gp. Hence, vincristine satisfies all the prerequisites to be a P-gp substrate....
Mitomycin C prodrug was prepared by capping its pharmacophore with a 27 aa nanopeptide. The drug activity was suppressed for 8 hrs when the prodrug was added to HEp2 cells....
Aim of this review is to give complete information about this new drug Tapentadol. It is a centrally-acting opioid analgesic, having a potency between morphine and tramadol. Tapentadol has been approved as immediate release tablets in 50 mg, 75 mg and 100 mg formulation by the United States Food and drug administration.The U.S. Drug Enforcement Agency has placed Tapentadol (which is now being marketed as brand name NUCYNTA(TM) [New synthetic]), into Schedule II of the Controlled Substances Act.3 The chemical name for tapentadol is (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol.4It has a unique dual mode of action as an agonist at the μ-opioid receptor and as a norepinephrine reuptake inhibitor1. As a mu-opioid agonist, it binds to and activates mu-opioid receptors in the central nervous system. It modifies sensory and affective aspects of pain, inhibits the transmission of pain at the spinal cord and affects activity at parts of the brain that control pain perception. After oral administration 32% of the drug is absorbed. It is widely distributed in the body. The plasma protein binding is low and amounts to approximately 20%. It can be given in the form of oral tablets dose of 50 mg, 75 mg, or 100 mg every 4 to 6 hours depending on pain intensity. It has efficacy in a broad spectrum of acute and chronic pain models and possibly an improved tolerability profile....
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