The novel compound NO-1886 activates lipoprotein lipase in primary cultured adipose and skeletal muscle cells.
The novel compound NO-1886 activates lipoprotein lipase in primary cultured adipose and skeletal muscle cells.
复制标题
新型化合物 NO-1886 可激活原代培养的脂肪和骨骼肌细胞中的脂蛋白脂肪酶。
DOI：
10.1248/bpb.20.1108
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发表时间：
1997
影响因子：
2
通讯作者：
K. Tsutsumi
中科院分区：
文献类型：
--
作者：
A. Hagi;I. Hirai;H. Kohri;K. Tsutsumi
如前所述，我们发现了一种新的化合物NO-1886（二乙基4-[（4-溴-2-氰基苯基）氨基甲酰基]苄基膦酸酯）具有强大的脂蛋白脂肪酶（LPL）刺激活性。口服NO-1886可增加实验动物肝素后血浆中LPL活性，导致血浆甘油三酯降低，同时高密度脂蛋白胆固醇升高。然而，NO-1886对LPL活性的作用机制尚不清楚。为了解决这个问题，我们研究了NO-1886对从脂肪和骨骼肌组织分离的原代大鼠细胞培养物中LPL活性的影响。NO-1886在3和10微克/毫升的剂量下分别使脂肪细胞中的总LPL活性增加18%和23%，在10微克/毫升的剂量下使骨骼肌细胞中的总LPL活性增加43%。这些结果表明，NO-1886可能直接作用于LPL产生细胞，如脂肪和骨骼肌。
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 micrograms/ml, respectively, and 43% at a dose of 10 micrograms/ml in skeletal muscle cells. These results indicate that NO-1886 may act directly on LPL-producing cells such as adipose and skeletal muscle.