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. 2013 Jan 16;18(1):1150-61.
doi: 10.3390/molecules18011150.

Bioassay-guided isolation of DPP-4 inhibitory fractions from extracts of submerged cultured of Inonotus obliquus

Yan Geng  1 , Zhen-Ming Lu, Wei Huang, Hong-Yu Xu, Jin-Song Shi, Zheng-Hong Xu
Affiliations

Bioassay-guided isolation of DPP-4 inhibitory fractions from extracts of submerged cultured of Inonotus obliquus

Yan Geng et al. Molecules. .

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.

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Figures

Figure 1
Figure 1
Activity-guided purification of the chloroform extract of mycelium powders. Gray represents active site. F: fraction. The results are expressed as the mean ± SD.
Figure 2
Figure 2
UPLC profile and compounds proposed from the active fractions.
Figure 3
Figure 3
TOF MS–MS spectra and proposed fragmentation (insets) of compound 1 (above) and compound 18 (below).
See this image and copyright information in PMC

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