Strategies for reducing plasma cholesterol have been focused on reducing the absorption or synthesis of cholesterol. The aim of this study was to correlate the content of flavonoids and saponins in black bean (Phaseolus vulgaris L.) seed coats extracts with a potential effect in lowering cholesterol absorption by the inhibition of cholesterol micellar solubility. Extracts with different flavonoids and saponins concentration were obtained from a Box-Behnken design used to optimize extraction temperature, stirring time and solvent composition. Major flavonoids and saponins were quantified by HPLC-PDA-ELSD and confirmed through mass spectrometry. Contrary to the flavonoid content, saponins were correlated to the inhibitory effect of cholesterol micelle solubility as an approach to a potential reduction of cholesterol absorption. Extracts with the highest saponin content strongly inhibited cholesterol micellization with values of 55.4 ± 1.9 %, while stigmasterol used as control, only reached 12 ± 2.3 % at the same concentration (5 mg/ml). The optimal extracting conditions for saponins were 25 °C, during 3 h in 85 % aqueous-methanol. Correlations of inhibitory effect of cholesterol micellar solubility with the content of each identified saponin suggested that the reduction of cholesterol micellization depends on the C-22 substitution of saponins.