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Background   Calotropis gigantea  (Asclepiadaceae) ( Niu jiao gua ) has been used as a poultice in Chinese medicine for treating inflammatory skin diseases, e.g., neurodermatitis. This study aims to isolate the epidioxysterols from the flowers of  C. gigantea , elucidate their structures and evaluate their possible inhibitory effects on the NF- κ B pathway.    Methods  The two epidioxysterols 9,11-dehydroergosterol peroxide ( 1 ) and ergosterol peroxide ( 2 ) were isolated from the powdered flowers of  C. gigantea  by ultrasonic-assisted extraction, followed by the purification of the crude extract by column chromatography (i.e., silica gel and MCI-gel CHP 20P open columns). The chemical structures of these compounds were identified through a comparison of their HRMS,  1 H and  13 C NMR data with those in the literature. The in vitro IKK- β  inhibitory activities of compounds  1  and  2  (1–100 µM) were evaluated using an IKK  α  and  β  Assay/Inhibitor Screening Kit, which is a single-site, semi-quantitative immunoassay. Berberine was used as a positive control. The IKK- β  inhibitory activities between compounds  1  and  2  were compared by a two-tailed Student’s  t  test to summarize the structure activity relationship.    Results  Compounds  1  and  2  exhibited a dose-dependent inhibitory activity towards IKK- β  in a similar manner to that of berberine. The IKK- β  inhibitory activities of these two epidioxysterols were significantly stronger ( P  = 0.001 for compound  1  and  P  = 0.028 for compound  2 ) than that of berberine at the concentration of 100 µM. Furthermore, at the same concentration the suppressive effect of compound  1  towards IKK- β  was greater than that of compound  2  ( P  = 0.041), while their activities at 10 and 50 µM were comparable. The difference in the results at 100 µM therefore suggested that the double bond between C-9 and C-11 in compound  1  could be responsible for its higher inhibitory activity towards IKK- β  at this concentration.    Conclusions  9,11-dehydroergosterol peroxide ( 1 ) and ergosterol peroxide ( 2 ) were isolated from the flowers of  C. gigantea  and exhibited in vitro inhibitory activities towards IKK- β .    Electronic supplementary material  The online version of this article (doi:10.1186/s13020-016-0081-1) contains supplementary material, which is available to authorized users.

Inhibition of IKK-β by epidioxysterols from the flowers of Calotropis gigantea (Niu jiao gua)