Gastrointestinal lipase inhibitors are molecules of pharmaceutical interest due to their use as anti-obesity drugs. In this study, forty strains isolated from soil and sediments were identified with the ability to produce inhibition of gastrointestinal lipase activity. The biomass extract of these strains showed at least 50% inhibition in the hydrolysis of tributyrin by recombinant human pancreatic lipase (rHPL) or rabbit gastric lipase (RGL) by in vitro assays. Based on gene sequencing, the isolates were identified mainly as Streptomycetes. Moreover, none of the identified strains has been reported to be lipase inhibitor producers, so they can be viewed as potential sources for obtaining new drugs. IC₅₀ values of the three best inhibitor extracts showed that AC104-10 was the most promising strain for production of gastrointestinal lipase inhibitors. AC104-10 shows 99% homology (16S rRNA gene fragment) to Streptomyces cinereoruber strain NBRC 12756. An inhibitory study over trypsin activity revealed that AC104-10 extract, as well as THL, had no significant effect on the activity of this protease, showing its specificity for lipases. In addition, analyzes by MALDI-TOF mass spectrometry of the enzyme-inhibitor complex revealed that there is a covalent interaction of the AC104-10 inhibitor with the catalytic serine of the pancreatic lipase, and that the molecular weight of the inhibitor is approximately 686.19 Da.

中文翻译：

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从土壤和湖泊沉积物中分离出的微生物产生的胃肠道脂肪酶抑制剂的筛选。

胃肠道脂肪酶抑制剂由于其用作抗肥胖药而成为药物学上感兴趣的分子。在这项研究中，从土壤和沉积物中分离出的40株菌株具有抑制胃肠道脂肪酶活性的能力。这些菌株的生物质提取物在体外测定中显示了重组人胰脂肪酶（rHPL）或兔胃脂肪酶（RGL）对三丁酸甘油酯水解的抑制作用至少有50％。基于基因测序，分离物主要鉴定为链霉菌。此外，没有发现任何已鉴定的菌株是脂肪酶抑制剂的产生者，因此它们可以被视为获得新药的潜在来源。IC ₅₀三种最佳抑制剂提取物的pH值表明，AC104-10是生产胃肠道脂肪酶抑制剂的最有希望的菌株。AC104-10与灰链霉菌NBRC 12756表现出99％的同源性（16S rRNA基因片段）。对胰蛋白酶活性的抑制研究表明，AC104-10提取物以及THL对这种蛋白酶的活性均无明显影响，表明它对脂肪酶的特异性。此外，通过酶抑制剂复合物的MALDI-TOF质谱分析表明，AC104-10抑制剂与胰腺脂肪酶的催化丝氨酸存在共价相互作用，并且该抑制剂的分子量约为686.19 Da 。