The Novel Compound NO-1886 Activates Lipoprotein Lipase in Primary Cultured Adipose and Skeletal Muscle Cells

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As previously reported, we have discovered that a novel compound, NO-1886 (diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl] benzylphosphonate) has a powerful lipoprotein lipase (LPL) stimulating activity. Oral administration of NO-1886 increased LPL activity in postheparin plasma of experimental animals, resulting in the reduction of plasma triglyceride with concomitant elevation of high density lipoprotein cholesterol. However, the mechanism of NO-1886 on LPL activity is not clearly understood. To address this problem, we examined the effect of NO-1886 on LPL activity in primary rat cell culture isolated from adipose and skeletal muscle tissue. NO-1886 increased total LPL activity 18% and 23% in adipocytes at a dose of 3 and 10 μg/ml, respectively, and 43% at a dose of 10 μg/ml in skeletal muscle cells. These results indicate that NO-1886 may act directly on LPL-producing cells such as adipose and skeletal muscle.
公益社団法人日本薬学会の論文
1997-10-15