Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 19, Pages 6116-6119Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.08.029
Keywords
Endangered plant; Rhododendron brachycarpum; Protein tyrosine phosphatase-1B; Rhododendric acid; LogP value
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Funding
- National Research Foundation of Korea (NRF)
- Ministry of Education, Science and Technology of Korea (MEST) [2011-0024389]
- Global R&D Center (GRDC) Program through the NRF
- KRIBB Research Initiative Program
- MEST
- National Research Foundation of Korea [과09B2106, 2011-0024389] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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In spite of the critical role of the natural products in drug discovery, surprising little attention has been placed on endangered and rare plant species that could play a pivotal role in pharmaceutical and fiber development. Protein tyrosine phosphatase-1B (PTP1B), which blocks insulin signaling, has been gaining interest to be a promising therapeutic target for the treatment of type 2 diabetes mellitus. Bioassay-guided fractionation on the leaves of Rhododendron brachycarpum G. Don (Ericaceae) yielded seven PTP1B inhibitory triterpenoids, including a new triterpene, rhododendric acid A (1). Their PTP1B inhibitory potency and their lipophilicity were investigated to provide a feasible scaffold that may overcome the innate limitation of the previously reported PTP1B inhibitors. (C) 2012 Elsevier Ltd. All rights reserved.
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