Discriminant analysis has been used to study the data for naphthoquinones as antitumor agents in three different animal tumor systems. In each case the most significant variables for classifying the compounds into two groups according to their antitumor activities were determined by a stepwise procedure. The usefulness of discriminant analysis in the design of drugs is discussed.
Compounds having the basic structure N-(R)-substituted ring-substituted 4-iminocyclohexadienone have been synthesized and tested as antitumor agents against the ascitic sarcoma 180 tumor in Swiss mice. Among these compounds, the dimethylindoanilines [R = 4-(CH3)2NC6H4] are most stable in water at pH 7.0 and at 25 degrees C, the oximes (R = oh) are less stable, and the N-halo compounds (R = Br and Cl) are least stable. The N-halo derivatives have the highest redox potentials under the conditions used, the greatest effect against ascitic sarcoma 180 in Swiss mice, and the greatest acute toxicity when injected ip in the Swiss mice. Discriminant analysis of the results indicates that substituents with positive values of F and negative values of pi increase the antitumor activities, whereas those with positive values of sigma and R should lower the toxicity. The redox potential, a molecular parameter, is the best single variable for discriminating between the groups based on antitumor activities.
Background: Alpinia galanga is an ayurvedic herb recognized and used across many traditional medicine systems for its analgesic and anti-inflammatory activity. The present study scientifically validates the potential anti nociceptive action of ethanolic extract of Alpinia galanga by chemical, neurogenic and inflammatory nociception model in mice followed by identification of potential lead compound by computational analysis.Methods: The assessment of anti nociceptive action is evaluated by Acetic acid induced abdominal constrictions and Formalin assay on ethonolic extract of Alpinia galanga, followed by 20 compounds with known chemical structure of Alpinia galanga is subjected to computational analysis to predict possible lead compound with desirable pharmacokinetic and drug like features.Results: The percentage inhibition rate of Aspirin (100mg/kg) was 82.15% compared to Alpinia galanga (100mg/kg) 19.63%, (200mg/kg) 33.02% and (400mg/kg) 57.13% by acetic acid induced abdominal constrictions antinociceptive mice model. Alpinia galanga 400mg/kg (71.70%) had comparable percentage inhibition of nociception to standard group indomethacin (88.71%) in formalin induced nociceptive mice model. Among 20 compounds screened for pharmacokinetic and drug like features, Galanal B had the binding free energy -56.664 when compared to control compound 2AZ5-56.000.Conclusions: The Alpinia galanga extract had significant anti nociceptive activity and followed by computational analysis of 20 compounds with known chemical structure predicted Galanal B as lead compound with best insilico pharmacokinetic and drug like features.
Background: Alpinia galanga belonging to Zingiberaceae family was traditionally used to treat numerous inflammatory disorders. The rationale behind its use since ages has to be scientifically validated for developing newer therapeutic agents. Aims and Objectives: Anti-inflammatory activity of ethanolic extract of A. galanga in carrageenan induced pleurisy rats. Materials and Methods: This study was investigated on the ethanolic extract of A. galanga rhizome by scientifically validated anti-inflammatory screening technique on rats by carrageenan induced pleurisy. This pleurisy model is considered to be an excellent acute inflammatory model in which fluid extravasations, leukocyte migration and the various biochemical parameters involved in the inflammatory response can be measured easily in the exudates. Results: The results obtained indicate that the ethanolic extract had significant activity in rats in all the tested groups A. galanga 100, 200 and 400 mg with P < 0.005 compared to that of control. Conclusion: The study confirms the potential anti-inflammatory activity of ethanolic extract of A. galanga rhizome.
Background: Pharmacology enables medical students with the art of rational prescriptions of drugs. It is one of the rapidly evolving subjects in medical sciences. The purpose of the study was to assess whether teaching-learning methodologies and evaluation methods are supporting the curriculum goals and what modifications can be made for the benefit of medical students.Methods: After approval by the Institutional Ethics Committee the study was carried out in January-February 2017. A total of 128 students of 2nd MBBS were administered a pre-validated questionnaire after explaining the purpose of the study. Descriptive statistics were used for analysis of data. Frequency was expressed as percentage.Results: A total response rate of 93.75% was observed. Most of the students mentioned cardiovascular system (20.8%) as the most interesting topic. 78.3% preferred teaching by use of combination of both audio-visual aids and chalk and board. Majority of the students rated practical classes as similar to theory (34.2%). 91.7% students mentioned that seminars are useful to them. 95% of students are interested in continuation of the integrated classes conducted at the end of each chapter. 98.3% of students for written tests and 90% for viva voce responded positively for the need of such periodic evaluation in addition to university prescribed evaluations. 95% students mentioned that field visits helps them in better understanding of pharmacology.Conclusions: The present study helped us to elicit student preferences regarding teaching and evaluation methods in pharmacology. Implementation of the same would be helpful for better outcome of students.
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