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Acylated Aminooligosaccharides from the Yellow Sea Streptomyces sp. HO1518 as Both α-Glucosidase and Lipase Inhibitors
Authors:Jian-Lin Xu  Hai-Li Liu  Zhi-Feng Liu  Yu-Hong Ren  Yong Wang
Affiliation:1.Key Laboratory of Synthetic Biology, CAS Center for Excellence in Molecular Plant Sciences, Institute of Plant Physiology and Ecology, Chinese Academy of Sciences, Shanghai 200032, China; (J.-L.X.); (Z.-F.L.);2.University of Chinese Academy of Sciences, Beijing 100039, China;3.State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai 200237, China;
Abstract:Three new acylated aminooligosaccharide (1–3), along with five known congeners (4–8), were isolated from the marine-derived Streptomyces sp. HO1518. Their structures were fully elucidated by extensive spectroscopic analysis, mainly based on 1D-selective and 2D TOCSY, HSQC-TOCSY, and HRESIMS spectrometry measurements, and by chemical transformations. All of the compounds were evaluated for their α-glucosidase and pancreatic lipase inhibitory activities. Among the isolates, D6-O-isobutyryl-acarviostatin II03 (3) and D6-O-acetyl-acarviostatin II03 (8), sharing acarviostatin II03-type structure, showed the most potent α-glucosidase and lipase inhibitory effects, far stronger than the antidiabetic acarbose towards α-glucosidase and almost equal to the anti-obesity orlistat towards lipase in vitro. This is the first report on inhibitory activities against the two major digestive enzymes for acylated aminooligosaccharides. The results from our investigation highlight the potential of acylated aminooligosaccharides for the future development of multi-target anti-diabetic drug.
Keywords:Streptomyces sp. HO1518, acylated aminooligosaccharides, α  -glucosidase, α  -amylase, sucrase, lipase
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