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Leelamine is a diterpene amine that has been found in gum resin and has diverse biological activities.1,2,3 It inhibits pyruvate dehydrogenase kinase (PDHK; IC50 = 9.5 µM).1 Leelamine is active against the plant pathogenic fungus B. cinerea (EC50 = 70 µM).2 It induces apoptosis in UACC-903 and 1205Lu melanoma cell lines when used at a concentration of 3 µM.3 Leelamine (100 and 300 µmol/kg per day) reduces blood glucose levels in an ob/ob mouse model of type II diabetes.1
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1. Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK). Bioorg. Med. Chem. Lett. 9(15), 2223-2228 (1999).
2. Detection of the effects of fungicides on the cell membrane by proton nuclear magnetic resonance spectroscopy. Pest. Biochem. Phys. 38(2), 172-177 (1990).
3. Leelamine mediates cancer cell death through inhibition of intracellular cholesterol transport. Mol. Cancer Ther. 13(7), 1690-1703 (2014).