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Biomedical subjects

A U De

Publications and source records attributed to A U De.

13 recordsLinked to original sources

Effect of two cardiac glycosides, digitoxin and digoxin on blood lipids.

Two cardiac glycosides, namely digitoxin and digoxin when treated with goat blood, were found to alter the lipid constitution as measured by their phosphorus content, fatty acid composition and malonaldehyde content. There was significant increase in the poly-unsaturated fatty acids (PUFA) and malonaldehyde contents in blood treated with these drugs. Possible correlation between the lipophilicity of the drugs and their biological activity is discussed.

Animals

Effect of propranolol hydrochloride on blood cell lipids in relation to partition coefficient and biological activity.

Considering the high lipophilicity of propranolol (log P = 3.56), its interactions with the cell membrane lipids of goat blood have been investigated. It is observed that lipid loss after incubation of blood cells with propranolol hydrochloride in salt glucose medium for varying periods of time was accompanied with significant increases in PUFAs. Amongst the PUFAs studied the omega 3 and omega 6 fatty acids, the two important precursors of eicosenoids, have shown increase in varying amounts. This phenomenon is presumably responsible for the significant cardiovascular activity of this drug.

Animals

Possible antineoplastic agents: Part XIII. Synthesis, biological evaluation and QSAR studies of some 1-(substituted benzenesulphonyl)-5-oxopyrrolidine-2-carboxylic acid derivatives.

Twelve analogues of 1-(substituted benzenesulphonyl)-5-oxopyrrolidine-2- carboxylic acid have been synthesized and tested for antineoplastic activity in Swiss albino mice with an Ehrlich ascites carcinoma (EAC) cell line. The values of percent inhibition of growth, both in ascitic cell count and fluid weight, have been taken as activity parameters. Quantitative structure-activity relationships (QSAR) have been studied using the LFER model. The best correlation (R2 = 93.0%) was found using molar refractivity (MR), which measures the molar volume and polarizability of the substituents.

Animals

Correlation of phospholipid loss in goat whole blood with solvochromic properties of antiamebics like emetine, metronidazole and diloxanide furoate.

Phospholipid content of whole blood lipid decreases significantly when goat blood is incubated for different length of time with different amebicidal agents (e.g., emetine, metronidazole and diloxanide furoate). The plots of relative per cent phosphate loss against incubation period show biphasic nature and suggest that the rates of phospholipid loss bears some relation with the drug's lipophilicity (log P in 1 octanol/water system). The absolute phospholipid loss seems to be governed by the drug's aquasolubility. Implication of these finding were discussed in terms of their clinical profiles assuming that the loss of phospholipid is due to drug's binding with the phospholipid layer in amebic cyst-coat, being the first step which may trigger a chain of events leading to the onset of drug action.

Amebicides

Effect of lignocaine on blood lipid in relation to partition coefficient and biological activity.

To correlate lipophilicity of lignocaine with changes in lipid composition of blood as a result of in vitro incubation with the drug, phosphorus content and fatty acid compositions of blood lipids before and after lignocaine treatment have been compared with those of a standard phospholipid, lecithin, under similar conditions of drug treatment. The change in fatty acid constituents has been correlated with the biological activity (both therapeutic and toxic) of lignocaine.

Animals

Possible antineoplastic agents I.

A few thalidomide and glutarimide derivatives were synthesized. Several compounds possessed significant antineoplastic activity against Ehrlich ascites carcinoma in Swiss albino mice.

Animals

Indolizines II: search for potential oral hypoglycemic agents.

A few 1,2-bis(N-alkylaminomethyl)indolizines, simple indolizinecarboxylic acids, and several 6-alkoxyindolizine-2-carboxylic acids were synthesized and screened as possible oral hypoglycemic agents. The absence of any significant hypoglycemic activity excludes these compounds from the predicted structural lead provided by some hypoglycemic Vinca alkaloids, such as vincamine, vindoline, and vindolinine, having the indolizine ring as one structural component. But an extension of the rationale that indolizines are also the structural components of some carcinolytic Vinca alkaloids, such as vincristine and vinblastine, used in cancer chemotherapy provided encouraging results. One indolizine derivative showed significant antineoplastic activity in Ehrlich ascites carcinoma.

Administration, Oral