Objective: The study is aimed to evaluate the antiparkinsonian effect of polyherbal formulation containing methanolic extract of Prunus amygdalus, Arachis hypogaea, and Citrullus lanatus (MEPAC) in chlorpromazine (CPZ)-induced Parkinson’s disease in Wistar albino rats. Methods: The antiparkinsonian activity of polyherbal formulation was studied in CPZ (3 mg/kg i.p.) induced Parkinson rat model. Rats were subjected to treatment with MEPAC and standard drug for a period of 21 days. The behavioral assessments, i.e., catalepsy and locomotor activity were assessed during the treatment period. Then animals were sacrificed, brains were isolated and homogenized for the estimation of biochemical parameters such as dopamine (DA), lipid peroxidation (LPO), glutathione (GSH), and superoxide dismutase (SOD). Histopathology of the brains was also done. Results: The cataleptic score of MEPAC (200 mg/kg and 400 mg/kg) treated rats was significantly reduced. On the other hand, there was improved in the locomotor activity. MEPAC (200 mg/kg and 400 mg/kg) treated rats showed increase in the level of DA, reduced GSH, SOD, and decreased LPO significantly. Conclusion: It may be concluded that methanolic extract of polyherbal formulation consisting of P. amygdalus, A. hypogaea, and C. lanatus showed a good antioxidant and neuroprotective effect in CPZ-induced Parkinson rats.
Nasal cavity is lined by vascularized epithelium which provides larger surface area useful for drug absorption. It has low enzymatic activity in contrast to the di-ABSTRACT The objective of this study was to develop novel intranasal microemulsion containing oxcarbazepine (OXC) for treatment of epilepsy. Optimized ratio of Tween 80: Polyethylene glycol and isopropyl myristate was selected after developing pseudoternary phase diagrams and microemulsions were prepared. The prepared microemulsions were characterized for drug content, pH, particle size, polydispersity index, zeta potential, conductivity, viscosity and in vitro release. Ex vivo permeation study for selected microemulsion was performed through sheep nasal mucosa. Further pharmacodynamic performance was evaluated in mice by electrically induced seizures. It was found that selected microemulsion was transparent with average globule size of 20.5 nm and cumulative percentage drug permeated was 95.60 %. Pharmacodynamic evaluation of selected formulation also indicated lesser intensity of seizures with low dose in mice in comparison to oral suspension of OXC. OXC intranasal delivery system is an effective alternate therapy for treatment of epilepsy.
A series of potential bioactive compounds, 4-Amino-5-mercapto-3-(4-chlorophenyl)-1, 2, 4-triazole (1d), 4-Amino-5-mercapto-3-(4-nitrophenyl)-1, 2, 4-triazole (2d) , 4-Amino-5-mercapto-3-(2, 4-dichlorophenyl)-1, 2, 4-triazole (3d), 4-Amino-5-mercapto-3-(2-chlorophenyl)-1, 2, 4-triazole (4d), 4-Amino-5-mercapto-3-(2-methylphenyl)-1, 2, 4-triazole (5d), 4-Amino-5-mercapto-, 2, 4-triazole (6d) were synthesized according to the 1 literature methods. The synthesized compounds were characterized by FT-IR, H NMR spectroscopy, C H N analysis and anticancer activity was evaluated.Male Swiss albino mice has been used as test animal. Tumor cells used for anticancer activity were EAC (Ehrlich Ascites Carcinoma). Compounds were given at a dose of 25 mg/kg body weight intraperitoneally. groups were found to reduce tumor volume, viable cell count and increase the tumor weight (%) inhibition, ascites cells (%) inhibition and non-viable cell count and increase in life span (%ILS). All the compounds exhibited the significant (P< 0.01) anticancer activity compared to control and the compound 4d is found to be the most potent one. The standard drug was used as 5-Fluorouracil (20mg/kg, body weight).Keywords: 1, 2, 4-triazole, anticancer activity, tumor cell count, tumor weight inhibition. 3-(4-methoxyophenyl)-1 Compounds treated (III-VIII)ABSTRACT
Endothelin (ET) is the most potent vasoconstrictor. It is secreted by the endothelial cells. At low concentration, it acts as an agonist for endothelium-derived relaxing factors and thereby causes vasodilatation, and at higher concentration it acts as a potent vasoconstrictor. It is synthesized by proteolytic cleavage of preproendothelin to proendothelin by the action of metallopeptidases and chymase, which is further cleaved into mature form of ET by endothelin converting enzyme. There are four isoforms of ET, namely, ET-1, ET-2, ET-3, and ET-4. ET acts on 2 types of receptors. Binding of ET-1 to ETA receptor at the vascular smooth muscle cells induces vasoconstriction. It also produces vasoconstriction by acting on the ETB2 receptor of vascular smooth muscle cells but promotes vasodilatation at ETB1 receptor present on the endothelial cell.
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