Anti-Adipogenic Polyacetylene Glycosides from the Florets of Safflower ( Carthamus tinctorius )

Safflower ( ) is an annual herb belonging to the Compositae family; it has a history of use as a food colorant, dye, and medicine in oriental countries. LC-MS-UV-based chemical analysis of extract of the florets of led to the isolation of two new C -polyacetylene glycosides, (8 )-decaene-4,6-diyne-1,10-diol-1- - -d-glucopyranoside ( ) and (8 )-deca-4,6-diyne-1,8-diol-1- - -d-glucopyranoside ( ), together with five known analogs ( - ). The structures of the new compounds were determined by using 1D and 2D NMR spectroscopic data and HR-MS data, as well as chemical transformations. Of compounds - , compounds , , and inhibited the adipogenesis of 3T3-L1 preadipocytes, whereas compounds and promoted adipogenesis. Compounds , , and also prevented lipid accumulation through the suppression of the expression of lipogenic genes and the increase of the expression of lipolytic genes. Moreover, compounds and activated AMPK, which is known to facilitate lipid metabolism. Our findings provide a mechanistic rationale for the use of safflower-derived polyacetylene glycosides as potential therapeutic agents against obesity.