Anantha Naik Nagappa

Antidiabetic activity of Terminalia catappa Linn fruits.

In view of alleged antidiabetic potential, effect of the petroleum ether, methanol, and aqueous extracts of Terminalia catappa Linn (combretaceae) fruit, on fasting blood sugar levels and serum biochemical analysis in alloxan-induced diabetic rats were investigated. All the three extracts of Terminalia catappa produced a significant antidiabetic activity at dose levels 1/5 of their lethal doses. Concurrent histological studies of the pancreas of these animals showed comparable regeneration by methanolic and aqueous extracts which were earlier, necrosed by alloxan.

Wound healing activity of the aqueous extract of Thespesia populnea fruit

Villagers have traditionally used the poultice prepared from the fruits of Thespesia populnea to treat a variety of skin ailments including wounds. In the present study, the aqueous extract of T. populnea fruit showed significant wound healing activity in the excision wound and incision wound models in rats following topical and oral administration, respectively.

Design and Development of Integrase Inhibitors as Anti-HIV Agents

A review is presented on different categories of compounds that have been studied for the inhibition of the HIV-1 integrase to develop anti-HIV agents. These compounds are: oligonucleotides (double-stranded, triplex, and G-quartet), curcumin analogues, polyhydroxylated aromatic compounds, diketo acids, caffeoyl- and galloyl - based compounds, hydrazides and amides, tetracyclines, and depsides and depsidones. For all these compounds, the important structural features essential for the inhibition of the integrase are pointed out.

Strategies for enhanced drug delivery to the central nervous system

Treating central nervous system diseases is very challenging because of the presence of a variety of formidable obstacles that impede drug delivery. Physiological barriers like the blood-brain barrier and blood-cerebrospinal fluid barrier as well as various efflux transporter proteins make the entry of drugs into the central nervous system very difficult. The present review provides a brief account of the blood brain barrier, the P-glycoprotein efflux and various strategies for enhancing drug delivery to the central nervous system.

Liquid membrane phenomena in anticancer drugs. Studies on 5-fluorouracil and its derivatives

Liquid membrane phenomena in 5-fluorouracil and its two derivatives: 1-(2-tetrahydrofuryl)-5-fluorouracil and 1-hexyl-carbamoyl-5-fluorouracil have been studied. Modification in the transport of folic acid, vitamin B12 and a few relevant amino acids in the presence of the liquid membrane generated by these drugs in series with a supporting membrane has been studied. The data indicate that modification in the transport of the relevant permeants due to the liquid membranes likely to be generated by these drugs at their respective sites of action may also contribute to their anticancer activity.

Synergy of gatifloxacin with cefoperazone and cefoperazone-sulbactam against resistant strains of Pseudomonas aeruginosa

Chequerboard and time-kill methods were used to compare the in vitro efficacies of the combinations gatifloxacin (GAT) with cefoperazone (CFP) and GAT with cefoperazone-sulbactam (CFP-SUL) against 58 clinical isolates of Pseudomonas aeruginosa. The combinations GAT+CFP and GAT+CFP-SUL were shown to be synergistic for 36.2 and 58.6 % of isolates tested, respectively, using the chequerboard method. Time-kill studies with 11 strains showed synergy in 54.5 % for the GAT+CFP combination and 72.7 % for the GAT+CFP-SUL combination. The agreement between these two methods was found to be 72-81 %. There was a significant difference in synergy between the two combinations tested (P=0.011).

Role of surface activity in mechanism of actions of tricyclic antidepressants

The role of surface activity has been studied in the mechanism of action of tricyclic antidepressants (TCAs). TCAs have been shown to generate liquid membranes in series with a supporting membrane by the virtue of their amphiphillicity. Transport of important biogenic amines (adrenaline, nor-adrenaline, dopamine and 5-hydroxy tryptamine) and ions (potassium, sodium and calcium) have been studied in the presence of liquid membranes generated by surface-active TCAs. The data on the modifications in the permeability of important biogenic amines and ions indicates that the liquid membranes generated by TCAs may play a significant role in the mechanism of their anti depressant action. The surface-active nature of the drugs has been discussed with relevance to their pharmacological effects.

Preparation, validation and user-testing of pictogram-based patient information leaflets for hemodialysis patients.

Background: Patient information leaflets are universally-accepted resources to educate the patients/users about their medications, disease and lifestyle modification. Objectives: The objective of the study was to prepare, validate and perform user-testing of pictogram-based patient information leaflets (P-PILs) among hemodialysis (HD) patients. Methods: The P-PILs are prepared by referring to the primary, secondary and tertiary resources. The content and pictograms of the leaflet have been validated by an expert committee consisting of three nephrologists and two academic pharmacists. The Baker Able Leaflet Design has been applied to develop the layout and design of the P-PILs. Results: Quasi-experimental pre- and post-test design without control group was conducted on 81 HD patients for user-testing of P-PILs. The mean Baker Able Leaflet Design assessment score for English version of the leaflet was 28, and 26 for Kannada version. The overall user-testing knowledge assessment mean scores were observed to have significantly improved from 44.25 to 69.62 with p value <0.001. Conclusion: The overall user opinion of content and legibility of the leaflets was good. Pictogram-based patient information leaflets can be considered an effective educational tool for HD patients.

Role of liquid membrane hypothesis in the biological actions of β-blockers

Abstract The liquid membrane hypothesis in anti-hypertensive drugs, namely, propranolol, metoprolol and atenolol have been investigated. Adreneceptor antagonist drugs have been shown to generate liquid membranes in series with a supporting membrane. Transport through liquid membrane generated by lecithin, cholesterol and lecithin–cholesterol mixture has been studied in the presence of adreneceptor antagonists. The data indicate that the transport of cations and neurotransmitters of physiological importance is impeded in presence of the liquid membrane. Relevance of this observation to anti-hypertensive action and anti-arrythmic action of these drugs has been discussed.

Evaluation of Web Sites for Quality and Contents of Asthma Patient Education

The patients and health care professionals worldwide depend largely on the internet for health care information due to its easy ubiquitous accessibility and economy, unlike the print media. The clinicians, health care professionals and asthma patients depend on the internet resources. The authentication of information on the web is an unmet demand. There is a growing need to provide quality information to the patients who desire education in the internet. As there is no system of validation of quality of information on internet, there can be a possibility of misleading or biased information on the internet. The present study aimed to evaluate the quality and content of information of websites providing patient education of asthma. Google search engine were used to identify 192 websites providing education on asthma, among which 42 were analyzed by Health on the Net Foundation Code of Conduct (HON code); Core Educational Concepts and Health Summit Working Group (HSWG) guidelines. On the basis of core educational concepts and HSWG criteria, websites were graded as excellent, good and average. Among the 42 websites, the HON code compliance was found to be very low (19%). A majority of the sites were compliant to basic HSWG criteria while lacking in few key elements. The HSWG scores were affected by development factors, and higher among those developed from public organizations of developed countries with non commercial interest. HSWG criteria and information on missing core educational concepts of HON code must be incorporated for an enhanced quality of information for asthma patient education.