Isolation of Actinomycetes and Screening for Lipase Inhibitors Production

Q4 Pharmacology, Toxicology and Pharmaceutics Current Enzyme Inhibition Pub Date : 2021-07-28 DOI:10.2174/1573408017666210728141245
Shivabai Chandwad, Chandrasen Chandwad, S. Gutte
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Abstract

Background: Obesity is a growing global health problem. Obesity leads to cardiovascular disorders, musculoskeletal disorders, diabetes, and certain types of cancer. One of the approach to control and treatment of obesity has involved inhibition of dietary lipid digestion by pancreatic lipase inhibitors. Microbes and plant source provide a rich source of enzyme inhibitors including pancreatic lipase inhibitors that can be developed as a drug for obesity treatment. Objective: Objective of the work mainly focuses and highlights on the isolation of actinomycetes and screening for pancreatic lipase inhibitors production. Methods: Actinomycetes were isolated from soil samples by pre-treatment of samples and using selective growth medium with and without antibiotics. Isolated actinomycetes were grown in fermentation condition and metabolites were extracted with isopropyl alcohol and solvent evaporated to get crude material. Extract of each isolate screened for pancreatic lipase inhibition using p- nitrophenyl palmitate as substrate by spectroscopic method. Results: Total 86 actinomycetes strains were isolated from soil samples. Out of 86 extracts,10 extracts have shown positive results for porcine pancreatic lipase inhibition and inhibition activity was in the range of 10-80%. 50 % inhibitory concentration determined using 1 to 8 mg/mL extract in the assay. Extract of isolate A9, B3 and C6 having 50 % inhibitory activity below 3 mg/mL concentration and Orlistat as a standard has shown 50 % inhibitory activity at below 1 mg/mL concentration. Conclusion: The results conclude that actinomycetes are potential source of lipase inhibitors, which may lead to valuable novel drugs for obesity treatment.
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放线菌的分离及脂肪酶抑制剂的筛选
背景:肥胖是一个日益严重的全球性健康问题。肥胖会导致心血管疾病、肌肉骨骼疾病、糖尿病和某些类型的癌症。控制和治疗肥胖的方法之一涉及通过胰脂肪酶抑制剂抑制膳食脂质消化。微生物和植物来源提供了丰富的酶抑制剂来源,包括胰脂肪酶抑制剂,可作为治疗肥胖的药物开发。目的:研究放线菌的分离和胰脂肪酶抑制剂的筛选。方法:通过对土壤样品进行预处理,并使用选择性生长培养基(含和不含抗生素)从土壤样品中分离放线菌。分离的放线菌在发酵条件下生长,用异丙醇提取代谢产物,蒸发溶剂得到粗品。以对硝基苯基棕榈酸酯为底物,通过光谱法筛选每种分离物的提取物对胰脂肪酶的抑制作用。结果:从土壤样品中分离到86株放线菌。在86种提取物中,有10种提取物显示出对猪胰脂肪酶抑制的阳性结果,并且抑制活性在10-80%范围内。在测定中使用1-8mg/mL提取物测定50%的抑制浓度。分离物A9、B3和C6的提取物在低于3mg/mL浓度时具有50%的抑制活性,奥利司他作为标准品在低于1mg/mL浓度时显示出50%的抑制作用。结论:放线菌是脂肪酶抑制剂的潜在来源,可能为肥胖的治疗提供有价值的新药。
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来源期刊
Current Enzyme Inhibition
Current Enzyme Inhibition Pharmacology, Toxicology and Pharmaceutics-Drug Discovery
CiteScore
1.30
自引率
0.00%
发文量
30
期刊介绍: Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.
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