Francisco Díaz

Synthesis and hypolipidaemic evaluation of a series of α-asarone analogues related to clofibrate in mice

A series of α‐asarone analogues related to clofibrate, containing an acetic acid group at C‐2 of the aromatic ring, has been prepared as the acids or as the ethyl and methyl esters. The corresponding alcohols were also synthesized by reduction of the ethyl esters. The compounds were examined in hyperlipidaemic male mice to evaluate their ability to modify serum lipoprotein cholesterol, low‐density lipoprotein cholesterol, high‐density lipoprotein cholesterol and triglycerides after oral administration of 40 and 80 mg kg−1 for 6 days.

Hypolipidaemic activity of dimethoxy unconjugated propenyl side‐chain analogs of α‐asarone in mice

The hypolipidaemic activity of several dimethoxy unconjugated propenyl side‐chain analogs of α‐asarone were investigated in hyperlipidaemic mice after six days of treatment. Eugenol and the α‐asarone analog with amino groups on the C‐4 position of the aromatic ring were observed to be the most effective hypolipidaemic agents at the dose of 80 mg/kg/day p.o. These compounds significantly lowered total serum cholesterol, low density lipoprotein (LDL‐cholesterol), and triglycerides content. On the other hand, high density lipoprotein (HDL‐cholesterol) was increased by administration of these hypolipidaemic agents. The ability to modulate the levels of these lipids suggests that these agents could be effective in the treatment of hyperlipidaemic states. These compounds appeared to be safe when administered at an oral dose of 80 mg/kg/day, which is within the therapeutic range in mice. Drug Dev. Res. 43:105–108, 1998.

Dominant lethal study of α-asarone in male and female mice after sub-chronic treatment

Dominant lethal studies were conducted in male and female mice with α‐asarone, the active hypolipidaemic component of Guatteria gaumeri Greenman, by per os sub‐chronic treatment (10 and 20 mg/kg, 5 days/week, for 8 weeks) and subsequent mating. α‐Asarone did not produce germinal mutations in either males or females. Epididymal sperm examination of male mice immediately after treatment failed toreveal any alteration in sperm count on shape. No significant alterations were observed in testicular or epididymal weights or testicular histology. Copyright