Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis |
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| Authors: | Duc Manh Hoang Tran Minh Ngoc Nguyen Tien Dat Do Thi Ha Young Ho Kim Hoang Van Luong Jong Seog Ahn KiHwan Bae |
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| Affiliation: | 1. College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea;2. Functional Metabolite Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), 52 Eoun-dong, Yuseong-gu, Daejeon 305-333, Republic of Korea;3. Institute of Natural Products Chemistry, Vietnamese Academic of Science and Technology, Hanoi, Viet Nam;4. Vietnam Military Medical University, Hanoi, Viet Nam |
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| Abstract: | Bioassay-guided fractionation of the chloroform-soluble fraction of Morus bombycis, using an in vitro PTP1B inhibitory assay led to the identification of three 2-arylbenzofurans, albafuran A (1), mulberrofuran W (2) and mulberrofuran D (6), along with three chalcone-derived Diels–Alder products, kuwanon J (3), kuwanon R (4), and kuwanon V (5). Compounds 1–6 showed remarkable inhibitory activity against PTP1B with IC50 values ranging from 2.7 to 13.8 μM. Inhibition kinetics were analyzed by Lineweaver–Burk plots, which suggested that compounds 1–6 inhibited PTP1B in a mixed-type manner. The present results indicate that the respective lipophilic and hydroxyl groups of 2-arylbenzofurans and chalcone-derived Diels–Alder products play an important role in inhibition of PTP1B. |
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