Abstract
One new isopimarane diterpene (1), together with two known compounds, 11-deoxydiaporthein A (2) and iso-pimara-8(14),15-diene (3) were isolated from the culture of Epicoccum sp., which was associated with Apostichopus japonicus. Their structures were determined by the analysis of 1D and 2D NMR, as well as mass spectroscopic data. The absolute configuration of Compound 1 was deduced by a single-crystal X-ray diffraction experiment using CuKα radiation. In the bioactivity assay, both Compounds 1 and 2 exhibited α-glucosidase inhibitory activity with IC50 values of 4.6 ± 0.1 and 11.9 ± 0.4 μM, respectively. This was the first report on isopimarane diterpenes with α-glucosidase inhibitory activity.
Highlights
The incidence and prevalence of type 2 diabetes, representing over 90% of all case of diabetes, are increasing rapidly as time passes
Epicoccum sp. associated with Apostichopus japonicus was cultivated in liquid media, and a chemical investigation of cultures of this strain led to the isolation of one new isopimarane diterpene (1), together with two known compounds, 11-deoxydiaporthein A (2) and isopimara-8(14),15-diene (3)
The absolute configuration of Compound 1 was deduced as 5R, 6S, 10S, 11R, 13R and 14S by a single-crystal X-ray diffraction experiment with CuKα radiation
Summary
The incidence and prevalence of type 2 diabetes, representing over 90% of all case of diabetes, are increasing rapidly as time passes. In the course of our continuing search for biologically-active substances from fungi derived from mangrove and sea cucumber [7,8,9], we had screened extracts from a number of fungi, and those with interesting biological activities were routinely subjected to chemical exploration. HS-1, associated with Apostichopus japonicus, showed α-glucosidase inhibition activity. One new isopimarane diterpene (1), together with two known compounds, 11-deoxydiaporthein A (2) and isopimara-8(14),15-diene (3), were isolated from the extract. Biomedical and pharmaceutical studies of isopimarane diterpene have shown interesting activities, such as cytotoxicity [10,11], acetylcholinesterase inhibitory activity [12] and anti-HIV-1 bioactivity [13]. There have been no previous reports of the α-glucosidase inhibition activity of these. The details of the isolation, structural elucidation and the results of the α-glucosidase inhibition study of the isolated compounds are reported
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