| Summary: | Safflower (<i>Carthamus tinctorius</i>) 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 <i>C. tinctorius</i> led to the isolation of two new C<sub>10</sub>-polyacetylene glycosides, (8<i>Z</i>)-decaene-4,6-diyne-1,10-diol-1-<i>O</i>-<i>β</i>-<span style="font-variant: small-caps;">d</span>-glucopyranoside (<b>1</b>) and (8<i>S</i>)-deca-4,6-diyne-1,8-diol-1-<i>O</i>-<i>β</i>-<span style="font-variant: small-caps;">d</span>-glucopyranoside (<b>2</b>), together with five known analogs (<b>3</b>–<b>7</b>). 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 <b>1</b>–<b>7</b>, compounds <b>2</b>, <b>3</b>, and <b>4</b> inhibited the adipogenesis of 3T3-L1 preadipocytes, whereas compounds <b>1</b> and <b>6</b> promoted adipogenesis. Compounds <b>2</b>, <b>3</b>, and <b>4</b> also prevented lipid accumulation through the suppression of the expression of lipogenic genes and the increase of the expression of lipolytic genes. Moreover, compounds <b>3</b> and <b>4</b> 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.
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