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Bioassay-Guided Isolation of DPP-4 Inhibitory Fractions from Extracts of Submerged Cultured of Inonotus obliquus
School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, Jiangsu, China
Tianjin Key Laboratory for Industrial Biological Systems and Bioprocessing Engineering, Tianjin Institute of Industrial Biotechnology, Chinese Academy of Sciences, Tianjin 300308, China
These authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 21 November 2012; in revised form: 7 December 2012 / Accepted: 14 January 2013 / Published: 16 January 2013
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.
Keywords: Inonotus obliquus; DPP-4 inhibitor; bioassay-guided isolation; UPLC-Q-TOF-MS; molecular docking
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MDPI and ACS Style
Geng, Y.; Lu, Z.-M.; Huang, W.; Xu, H.-Y.; Shi, J.-S.; Xu, Z.-H. Bioassay-Guided Isolation of DPP-4 Inhibitory Fractions from Extracts of Submerged Cultured of Inonotus obliquus. Molecules 2013, 18, 1150-1161.
Geng Y, Lu Z-M, Huang W, Xu H-Y, Shi J-S, Xu Z-H. Bioassay-Guided Isolation of DPP-4 Inhibitory Fractions from Extracts of Submerged Cultured of Inonotus obliquus. Molecules. 2013; 18(1):1150-1161.
Geng, Yan; Lu, Zhen-Ming; Huang, Wei; Xu, Hong-Yu; Shi, Jin-Song; Xu, Zheng-Hong. 2013. "Bioassay-Guided Isolation of DPP-4 Inhibitory Fractions from Extracts of Submerged Cultured of Inonotus obliquus." Molecules 18, no. 1: 1150-1161.