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Article

Bioassay-Guided Isolation of DPP-4 Inhibitory Fractions from Extracts of Submerged Cultured of Inonotus obliquus

1
School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, Jiangsu, China
2
Tianjin Key Laboratory for Industrial Biological Systems and Bioprocessing Engineering, Tianjin Institute of Industrial Biotechnology, Chinese Academy of Sciences, Tianjin 300308, China
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2013, 18(1), 1150-1161; https://doi.org/10.3390/molecules18011150
Received: 21 November 2012 / Revised: 7 December 2012 / Accepted: 14 January 2013 / Published: 16 January 2013
(This article belongs to the Section Natural Products Chemistry)
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. View Full-Text
Keywords: Inonotus obliquus; DPP-4 inhibitor; bioassay-guided isolation; UPLC-Q-TOF-MS; molecular docking 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. https://doi.org/10.3390/molecules18011150

AMA 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(1):1150-1161. https://doi.org/10.3390/molecules18011150

Chicago/Turabian Style

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. https://doi.org/10.3390/molecules18011150

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