Protein tyrosine phosphatase 1B inhibitors from a marine-derived fungal strain aspergillus sp. SF-5929 |
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Authors: | Dong-Cheol Kim Tran Minh Ha Jae Hak Sohn Joung Han Yim |
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Institution: | 1. College of Pharmacy, Wonkwang University, Iksan, Republic of Korea;2. College of Medical and Life Sciences, Silla University, Busan, Republic of Korea;3. Korea Polar Research Institute, KORDI, Incheon, Republic of Korea |
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Abstract: | AbstractIn the course of our continuing investigation of bioactive secondary metabolites from marine-derived fungal strains, a racemate of a novel diphenolic derivative named (±)-tylopilusin D (1) along with ten previously known secondary metabolites (2–11) were isolated from a marine-derived fungal strain Aspergillus sp. SF-5929. Their structures were elucidated mainly by analysis of NMR and MS data. In addition, the inhibitory effects of the isolated compounds against protein tyrosine phosphatase 1B (PTP1B) activity were evaluated, and compounds 1, 2, and 5–7 inhibited PTP1B activity with IC50 values ranging from 3.3 to 8.1?µM. Kinetics studies suggested that compounds 1, 2, and 5 had noncompetitive inhibitory effects against PTP1B. |
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Keywords: | Marine-derived fungus Aspergillus sp diphenolic derivative PTP1B inhibitors |
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