Hecogenin

Hecogenin is a natural steroid sapogenin with diverse biological activities that was originally isolated from A. sisalana and has been used in the synthesis of steroids.¹ It has antioxidant, anti-inflammatory, antiproliferative, and neuroprotective properties.^2,3,4,5 Hecogenin (10 μM) decreases superoxide anion formation induced by N-Formyl-Met-Leu-Phe in rat neutrophils by 23.6%.² It also inhibits myeloperoxidase (MPO) release from human neutrophils activated by phorbol 12-myristate 13-acetate when used at a concentration of 1 μg/ml.³ Hecogenin inhibits proliferation of the breast cancer cell lines MDA-MB-231, MDA-MB-468, MCF-10A, MCF-7, T47D, BT474, and SK-BR-3 (IC₅₀s = 28.7-38.2 μM).⁴ It decreases the number of glutamate-induced TUNEL-positive primary rat spinal motor neurons by 11% when used at a concentration of 1 μM.⁵ In vivo, hecogenin (15 mg/kg) decreases the mucosal lesion area of ethanol-induced gastric ulceration in mice.³ It also decreases tumor volume in an MDA-MB-231 human breast cancer mouse xenograft model when administered at a dose of 10 mg/kg three times per week.⁴

1.Cripps, A.L., and Blunden, G.A quantitative gas-liquid chromatographic method for the estimation of hecogenin and tigogenin in the leaves, juice and sapogenin concentrates of Agave sisalanaSteroids31(5)661-669(1978) 2.Tsai, P.L., Wang, J.P., Chang, C.W., et al.Constituents and bioactive principles of Polygonum chinensisPhytochemistry49(6)1663-1666(1998) 3.Santos Cerqueira, G., dos Santos e Silva, G., Rios Vasconcelos, E., et al.Effects of hecogenin and its possible mechanism of action on experimental models of gastric ulcer in miceEur. J. Pharmacol.683(1-3)260-269(2012) 4.Elsayed, H.E., Ebrahim, H.Y., Haggag, E.G., et al.Rationally designed hecogenin thiosemicarbazone analogs as novel MEK inhibitors for the control of breast malignanciesBioorg. Med. Chem.25(24)6297-6312(2017) 5.Vincent, A.M., Backus, C., Taubman, A.A., et al.Identification of candidate drugs for the treatment of ALSAmyotroph. Lateral Scler. Other Motor Neuron Disord.6(1)29-36(2005)