Hypolipidemic activity of Indan--1--acetic acids.

To study the hyoplipidemic activity of non-methoxy and methoxy substituted--alkyl indan acetic acids in normogenic and hypergenic animal models. The hyoplipidemic activity was evaluated using normogenic and hypergenic rat models. Indan acids synthesized in our laboratory (50 mg/kg) and the standard drug clofibrate (50 mg/kg) were used for this study. Dimethoxy substituted -methyl and -ethyl indan acetic acids (9 & 10) exhibited significant hypocholesterolemic activity in both animal models. Clofibrate showed cholesterol lowering activity of 18% in normogenic rats while test agents 9 and 10 produced a similar activity of 20% and 17% respectively. Liver cholesterol and liver weight of the animals tested were found normal in case of the test compounds while liver weight was increased by 15% in clofibrate treated rats. LDL and VLDL cholesterol levels were also affected by compounds No. 9 and 10. Compounds having a smaller alkyl groups (R = CH3, C2H5) at--carbon atom of the acetic acid moiety exhibited significant hypocholesterolemic activity.

Farmacologia do fibratos / Pharmacology of fibrates

Os fibratos são as drogas de escolha nas hipertrigliceridemias. Após sua absorção, os fibratos são metabolizados pelo fígado, utilizando isoenzimas P450 não compartilhadas pelas estatinas. Entretanto, para alguns fibratos, como o genfibrozil, uma interação com estatinas pode ocorrer durante a sua glucuronidação, ou pelo deslocamento de frações livres de estatina ligadas às proteínas plasmáticas. A vida-média plasmática é variável entre os fibratos (2-80 h). Recentemente, foi demonstrado que os fibratos promovem suas ações lipídicas pelo estímulo dos PPAR-alfa. Através dessa ação, existe um incremento na transcrição de alguns genes relacionados com o metabolismo lipídico, como a LLP, APOAI, APOAII, ABCA-1, bem como uma diminuição na expressão da APOCIII, e muitas outras ações.

Effect of chemically different calcium antagonists on lipid profile in rats fed on a high fat diet.

Different classes of calcium antagonists, viz. verapamil (diphenylalkylamine), diltiazem (benzothiazepine), nifedipine, felodipine and nimodipine (dihydropyridines), were examined for their effects on lipid profile in rats. Clofibrate was the reference standard. Clofibrate significantly prevented the rise of serum triglycerides and total cholesterol produced by high fat diet and raised antiatherogenic index to 1.6 times than that of high fat diet controls. Of the calcium antagonists studied, felodipine was most effective in preventing the rise of serum triglycerides and total cholesterol in high fat diet fed rats. Felodipine's antiatherogenic index was very high (886%)--much more than that of clofibrate (303%). Diltiazem and nimodipine which also significantly prevented the rise in triglycerides and total cholesterol produced by high fat diet had a moderately beneficial antiatherogenic index similar to that of clofibrate. Though verapamil and nifedipine slightly increased the triglyceride levels, total cholesterol levels were reduced only by verapamil and not by nifedipine. Despite this both these drugs moderately raised antiatherogenic index similar to clofibrate.

Antiatherosclerotic effects of alfalfa meal ingestion in chicks: a biochemical evaluation.

Feeding Alfalfa seed extract to chicks resulted in significant reduction of total cholesterol, phospholipid, triglyceride, LDL-Cholesterol and VLDL-cholesterol. Simultaneously, an increased in the HDL-cholesterol/total cholesterol ratio occurred with reduction in total cholesterol and phospholipid contents of liver and (ventricular) muscle of the heart. Results obtained with alfalfa seed extract ingestion were evaluated with a standard drug, compound, clofibrate.

Uterotropic effect of clofibrate and phenylbutazone in immature female rats.

The uterotropic effect of clofibrate and phenylbutazone was studied in immature female rats. A significant increase in the uterine wet weight was observed following clofibrate and phenylbutazone administration. Clofibrate but not phenylbutazone synergized with the uterotropic effect of ethinyl-oestradiol. Phenylbutazone pretreatment significantly decreased the pentobarbitone sleeping time. The uterotropic effect of clofibrate and phenylbutazone might involve displacement of 17-beta oestradiol (or ethinyl oestradiol) from plasma albumin binding sites in rats.