title: Bioassay-guided isolation of DPP-4 inhibitory fractions from extracts of submerged cultured of Inonotus obliquus.
abstract: Inonotus obliquus is a medicinal mushroom used in Russian and Eastern European folk medicine for the treatment of gastrointestinal cancer, cardiovascular disease and diabetes. Previous studies in our laboratory have demonstrated that the mycelium powders of I. obliquus possess significant antihyperglycemic effects in a mouse model of diabetic disease induced by alloxan. However, the active ingredients of mycelium powders responsible for the diabetes activity have not been identified. This study aims to identify the active ingredients of I. obliquus mycelium powders by a bioassay-guided fractionation approach and explore the mechanism of action of these active ingredients by using a  well-established DPP-4 (an important enzyme as a new therapeutic target for diabetes) inhibitory assay model. The results showed the chloroform extract of mycelium was potential inhibitory against DPP-4. Bioactivity guided fractionation led to the identification of 19 compounds using UPLC-Q-TOF-MS. Molecular docking between the compounds and DPP-4 revealed that compounds 5, 8, 9, 14, 15 may be the active components responsible for the DPP-4 inhibitory activity.
authors: School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, Jiangsu, China.
authors: Yan
authors: Y
authors: Geng
authors: Zhen-Ming
authors: ZM
authors: Lu
authors: Wei
authors: W
authors: Huang
authors: Hong-Yu
authors: HY
authors: Xu
authors: Jin-Song
authors: JS
authors: Shi
authors: Zheng-Hong
authors: ZH
authors: Xu
mesh_terms: D000363:Agaricales / Q000737:chemistry*; D046508:Culture Techniques; D018819:Dipeptidyl Peptidase 4 / Q000737:chemistry*; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000737:chemistry / Q000302:isolation & purification*; D057075:Enzyme Assays; D005285:Fermentation; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000302:isolation & purification; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000302:isolation & purification; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D008970:Molecular Weight; D025282:Mycelium / Q000737:chemistry*; D011485:Protein Binding
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; D006571:Heterocyclic Compounds; D007004:Hypoglycemic Agents; D018819:Dipeptidyl Peptidase 4