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Ionone alkaloid 9-( N , N -dimethyl)-4,7-megastigmedien-3-one (compound 1 ) is a new anti-metastatic natural product. However, it was previously reported as optical isomers mixture. Herein, the optical isomers ( 6a-6d ) of compound 1 were synthesized. The absolute configurations of 6a-6d were determined by ECD experiments and calculated spectra with time-dependent density functional theory (TDDFT). The anti-metastatic effects of the optical isomers were examined by transwell assay. These results revealed that compound 6a had potential anti-metastatic activity with an IC 50 value of 0.512 ± 0.093 μM. [ABSTRACT FROM AUTHOR]

3-O-[(E)-4-(4-cyanophenyl)-2-oxobut-3-en-1-yl] kaempferol is a novel lead compound to discover anti-diabetic and anti-obesity drugs. The present study reported the scaffold hopping of the lead compound to obtain a new isoxazole derivative, C45 , which has improved glucose consumption at the nanomolar level (EC 50 = 0.8 nM) in insulin resistant (IR) HepG2 cells. Western blotting showed that C45 markedly enhanced the phosphorylation of AMPK (AMP-activated protein kinase) and reduced the levels of the gluconeogenesis key enzymes PEPCK (phosphoenolpyruvate carboxykinase) and G6Pase (glucose 6-phosphatase) in HepG2 cells. The potential molecular mechanism of C45 may be activation of the AMPK/PEPCK/G6Pase pathways. We concluded that C45 might be a valuable candidate to discover anti-diabetic drugs. Unlabelled Image [ABSTRACT FROM AUTHOR]