ABSTRACT
Objective: To identify the active compounds from the barks of Betula platyphylla for inhibitory on diacylglycerol acyltransferase (DGAT1). Methods: Bioassay-guided fractionation resulted in the isolation of DGAT1 inhibitory activity of lupane triterpenes. Results: Ten compounds were identified as lupenone (1), lupeol (2), betulinic acid (3), betulinaldehyde (4), betulin (5), 3-deoxybetulonic acid (6), glochidonol (7), lup-20/29-ene-1β/3β-diol (8), 3α-hydroxy-lup-20(29)-en-23,28-dioic acid (9), and 3α,11α-dihydroxy-23-oxo-lup-20(29)-en-28-oic acid (10). Compounds 3-6, 9, and 10 inhibited DGAT1 with IC50 values ranging from (11.2 ± 0.3) to (38.6 ± 1.2) μmol/L. Conclusion: Compounds 6, 9, and 10 are first isolated from the barks of B. platyphylla., and compounds 3-6, 9, and 10 from the barks of B. platyphylla are responsible for the inhibition on DGAT1. © 2014 Tianjin Press of Chinese Herbal Medicines.