Posted by admin on May 31, 2017 in |
In the present study, a series of novel biologically active 8-benzylidene-6-tert-butyl-4-phenyl- 5, 6, 7, 8-tetrahydro-benzo-1, 3-thiazin – 2 -imines (TB1-TB12) were synthesized and evaluated for their biological activities. Initially, 2,6-dibenzylidene-4-tert-butylcyclohexanones were synthesized by Claisen-Schmidt condensation of 4-tert-butylcyclohexanone with various aromatic aldehydes in the presence of dilute sodium hydroxide. Further these compounds were subjected to cyclocondensation with thiourea, in isopropyl alcohol, catalyzed by aqueous potassium hydroxide to form 4-aryl-8-arylidene-5,6,7,8-tetrahydro-1H-benzo[d][1,3]thiazin-2(4H)-imines (TB1-TB12). The structures of the newly synthesized compounds have been established on the basis of their spectral data and elemental analysis. Anticonvulsant activity was performed by Maximal electroshocks (MES) method by using Diazepam as standard reference. These compounds were subjected to molecular properties prediction, drug-likeness, lipophilicity and solubility parameters determination using Molinspiration, Osiris program was used for prediction of the toxicity, and also Molsoft and ALOGPS 2.1 softwares. Among all compounds TB5 and TB8 containing lipophilic methoxyl and isopropyl group were more potent whereas TB12 containing hydroxyl groups were least potent among the...
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Posted by admin on May 31, 2017 in |
Pharmacological activities have been reported for the fruit, leaf and root extracts of Morinda citrifolia L. (Noni); however, the plant has not been widely studied for its antidyslipidemic effects on obesity and metabolic syndrome (MS). Objective: to evaluate the effects of aqueous M. citrifolia leaf extract on obesity and adipose tissue cell dynamics associated with triacylglycerol and adiponectin levels in Wistar rats with MS. Methodology: four groups of rats were used; control, metabolic syndrome (MS), M. citrifolia (Mc) and M. citrifolia plus sucrose (Mc-Suc). The dose of extract was 200 mg/kg of body weight for 2 weeks. Results: we observed differences in the weights of abdominal fat between the Mc and MS groups. The Mc-Suc and Mc groups showed significantly lower triacylglycerol concentrations than the MS group. Moreover, the adiponectin serum concentrations were higher in control, Mc-Suc and Mc groups than in the MS group. Finally, the MS group showed an increase in the percentage of fat cells with areas between 1001 and 1501 µm2 compared with the Mc...
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Posted by admin on May 31, 2017 in |
The purpose of the current investigation was to ameliorate the aqueous solubility and dissolution rate of an anti diabetic drug Glimepiride by cyclodextrin ternary complexes employing aminoacids. Initially, Glimepiride (GMP) binary complexes with β-Cyclodextrin (βCD) and Hydroxy propyl β-Cyclodextrin (HPβCD) were formulated by physical mixing, kneading, solvent evaporation and spray drying techniques which was followed by ternary complex preparation of selected GMP-Cyclodextrin binary complex employing various aminoacids by kneading method. The kneading method was used in preparing ternary complexes of GMP, because it was proved to be the best method comparatively in yielding promising binary complexes of glimepiride in the initial stage of this study. GMP formed 1:1 M stoichiometric binary and ternary inclusion complexes as demonstrated by the AL-type of phase solubility curve. An increment in the stability constant value (Kc) of GMP- βCD/HPβCD complex in the presence of aminoacids conceded higher complexation competency. FTIR and DSC studies evidenced the perfect inclusion complex formation. Ternary complexes ameliorated drug dissolution compared with GMP and GMP-βCD. The ternary complex containg...
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Posted by admin on May 31, 2017 in |
The aim of the present study was to evaluate the anxiolytic effects and motor coordination activity of Huperzine-A in rats. Wistar rats were treated orally with Huperzine-A (0.5, 1, 2 & 4 mg/kg) and diazepam (2 mg/kg p.o) as a standard anxiolytic drug then exposed to Elevated plus Maze (EPM) and Light Dark Box (LDB). The effects of the Huperzine-A on motor coordination were evaluated by actophotometer test. The rats treated with Huperzine-A drug (2mg/kg and 4mg/kg) showed significant increase in the percentage of entries and time spent in open arms of EPM, which is thought to reflect anxiolytic-like effects. Furthermore, Huperzine-A extracts (1, 2 & 4 mg/kg) significantly increased the percentage of time spent and number of transitions in the Light box in LDB test, indicating the anxiolytic effects of the substance. This anxiolytic effect of the huperzine-A was comparable to that of the diazepam, taken as standard. Also the Huperzine-A (2 mg/kg and 4 mg/kg) showed significant alteration in motor coordination compared to that of normal control...
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Posted by admin on May 31, 2017 in |
Background: Increase prevalence of viral infection such as hepatitis B or/and hepatitis C are followed by high incidence of mortality among hemodialysis patients. Objective: To determine prevalence and correlation of viral infection (Hepatitis B or/and Hepatitis C) among Hemodialysis Patients that died for the last five years in Indonesia and Malaysia in relation to gender, age, causes, and country. Method: A retrospective study was done in this research. The study included only hepatitis patients (hepatitis B and / or hepatitis C) passed away from 2010 to 2015. Universal sampling was used to select 185 patients from Indonesia hospital and 14 patients in Malaysia hospital but only 108 patients in Indonesia and 5 patients in Malaysia were included in this research. Results: The result indicates that more than 50 % patients have hepatitis C (63 patients). Hepatitis C mostly occurred among male and hypertensive patients between 51-60 years old. There is a significant correlation (P value ≤ 0.05) between age and type of infection for all hemodialysis hepatitis patients. Also,...
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