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首页> 外文期刊>American Journal of Physiology >Inhibition of gastrointestinal lipolysis by Orlistat during digestion of test meals in healthy volunteers.
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Inhibition of gastrointestinal lipolysis by Orlistat during digestion of test meals in healthy volunteers.

机译：在健康志愿者体内，测试食品消化过程中，奥利司他对胃肠道脂肪分解的抑制作用。

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摘要

The inhibition of digestive lipases by the antiobesity drug Orlistat along with lipolysis levels and fecal fat excretion were measured in healthy humans. Orlistat was found to be a powerful gastric lipase inhibitor, achieving 46.6--91.4% enzyme inhibition and thus greatly reducing gastric lipolysis of solid and liquid meals (11--33% of respective controls). Gastric lipase inhibition by Orlistat was extremely fast (half-inhibition time < 1 min). Duodenal lipolysis was reduced significantly by Orlistat given with the solid meal (32.6--37.6% of controls) but was only slightly reduced by Orlistat given with the liquid meal (74.5--100% of controls). Human pancreatic lipase (HPL) inhibition was found to be high (51.2--82.6%), however, regardless of the meal. These paradoxical results were explained when in vitro lipolysis experiments were performed. The rates of HPL inhibition by Orlistat were found to be similar with both types of meals (half-inhibition time 5--6 min), but the preemulsified triglycerides ofthe liquid meal were rapidly hydrolyzed by HPL before the enzyme was significantly inhibited by Orlistat. With the solid meal, the rate of hydrolysis of the meal triglycerides by HPL was slower than the rate of HPL inhibition by Orlistat. As predicted from the previous results, the effects of Orlistat on fat excretion levels were found to be much greater with the solid (40.5--57.4% of ingested fat) than with the liquid (4.2--18.8%) test meal.
机译：在健康人中测量了抗肥胖药Orlistat对消化脂肪酶的抑制作用以及脂解水平和粪便脂肪排泄。发现奥利司他是一种强大的胃脂肪酶抑制剂，可实现46.6--91.4％的酶抑制作用，从而大大减少了固体和液体餐的胃脂肪分解（分别为对照组的11--33％）。 Orlistat对胃脂肪酶的抑制作用非常快（半抑制时间<1分钟）。固体餐给予奥利司他显着降低了十二指肠的脂解作用（对照组的32.6--37.6％），而液体餐给予奥利司他所致的十二指肠脂解作用却仅有轻微的降低（对照组的74.5--100％）。发现人胰脂肪酶（HPL）的抑制作用很高（51.2--82.6％），无论膳食如何。这些矛盾的结果在进行体外脂解实验时得到了解释。发现奥利司他对HPL的抑制率与两种类型的膳食相似（半抑制时间为5--6分钟），但是在HPL对酶的显着抑制之前，液体膳食的预乳化甘油三酸酯被HPL快速水解。对于固体粗粉，HPL对粗粉甘油三酸酯的水解速率比Orlistat抑制HPL的速率慢。如先前结果所预测，发现固体食物（摄入脂肪的40.5--57.4％）比液体食物（4.2--18.8％）的奥利司他对脂肪排泄水平的影响要大得多。

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