Hunter S J, Rosen C J, Gay C V
Department of Zoology, University of Maine, Orono 04469.
J Bone Miner Res. 1991 Jan;6(1):61-6. doi: 10.1002/jbmr.5650060111.
A potent inhibitor of carbonic anhydrase, 5-[3-hydroxybenzoyl]thiophene-2-sulfonamide (HTS), was shown to cause a 37% reduction in the area of resorption pits formed by isolated chick osteoclasts when used at a dose of 10(-7) M. HTS at doses of 10(-9) and 10(-7) M was also effective in reducing acid formation by the osteoclasts (14 and 36%, respectively). Additionally, the effect of HTS was found to be readily reversed by removing the agent, showing that it does not exert a toxic effect on the cells. This study indicates that the inhibitory effect of HTS on bone resorption is at the level of the acid-forming mechanism in osteoclasts and supports the view that carbonic anhydrase has a central role in the process.
一种强效碳酸酐酶抑制剂5-[3-羟基苯甲酰基]噻吩-2-磺酰胺(HTS),当以10⁻⁷ M的剂量使用时,可使分离的鸡破骨细胞形成的吸收陷窝面积减少37%。10⁻⁹ M和10⁻⁷ M剂量的HTS在减少破骨细胞酸生成方面也有效(分别为14%和36%)。此外,发现去除该药物后HTS的作用很容易逆转,表明它对细胞没有毒性作用。这项研究表明,HTS对骨吸收的抑制作用是在破骨细胞的酸生成机制水平上,并支持碳酸酐酶在该过程中起核心作用的观点。