Key Laboratory of Marine Drugs of Ministry of Education, Shandong Provincial Key Laboratory of Glycoscience and Glycotechnology, School of Medicine and Pharmacy, Ocean University of China, Qingdao, 266003, China.
Key Laboratory of Marine Drugs of Ministry of Education, Shandong Provincial Key Laboratory of Glycoscience and Glycotechnology, School of Medicine and Pharmacy, Ocean University of China, Qingdao, 266003, China; Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology (Qingdao), Qingdao, 266237, China.
Anaerobe. 2021 Apr;68:102289. doi: 10.1016/j.anaerobe.2020.102289. Epub 2020 Nov 1.
Heparin and its derivative are commonly used as injectable anticoagulants in clinical procedures, but possess poor oral bioavailability. To explore the role of gut microbiota in the poor oral effect of heparin, the degradation profiles of heparin on six human gut microbiota were investigated. The heparin-degradation ability varied significantly among individuals. Furthermore, two strains of heparin-degrading bacteria, Bacteroides ovatus A2 and Bacteroides cellulosilyticus B19, were isolated from the gut microbiota of different individuals and the degradation products of the isolates were profiled. The ΔUA2S-GlcNS6S was the major end product with almost no desulfation. 3-O-sulfo group-containing tetrasaccharides were detected, which indicated that the antithrombin binding site was broken and this explained the lost anticoagulant activity of heparin. Collectively, the present study assessed the degradation profiles of heparin by human gut microbiota and provided references for the development of oral administration of heparin from a gut microbiota perspective.
肝素及其衍生物通常被用作临床操作中的可注射抗凝剂，但口服生物利用度差。为了探讨肠道微生物群在肝素口服效果不佳中的作用，研究了肝素在六种人体肠道微生物群中的降解谱。肝素的降解能力在个体之间有显著差异。此外，从不同个体的肠道微生物群中分离到两种肝素降解细菌，即卵形拟杆菌 A2 和纤维二糖分解拟杆菌 B19，并对分离株的降解产物进行了分析。ΔUA2S-GlcNS6S 是主要的末端产物，几乎没有脱硫酸。检测到含有 3-O-磺酸基的四糖，这表明抗凝血酶结合位点被破坏，这解释了肝素抗凝活性的丧失。综上所述，本研究评估了肝素在人体肠道微生物群中的降解谱，为从肠道微生物群角度开发肝素口服制剂提供了参考。
