Sarsasapogenin

Sarsasapogenin is a steroid sapogenin originally isolated from Smilax that has antiproliferative, pro-apoptotic, anti-inflammatory, neuroprotective, and antidepressant-like properties.^1,2,3,4,5,6 Sarsasapogenin inhibits proliferation of HeLa cervical, MCF-7 breast, HepG2 liver, A549 lung, A375.S2 melanoma, and HT-1080 fibrosarcoma cells (IC₅₀s = 31.36-48.79 μM) and dose-dependently induces apoptosis of HeLa cells.^2,3 It also protects human SH-SY5Y neuroblastoma cells from hydrogen peroxide-induced death with a neuroprotective ratio of 27.3% when used at a concentration of 100 μM.⁵ In vivo, sarsasapogenin (10 mg/kg) reduces 2,3,4-trinitrobenzene sulfonic acid-induced colon shortening, myeloperoxidase activity, NF-κB activation, and IL-1β, TNF-α, and IL-6 levels in mice.⁴ It also increases the percentage of correct responses in the Y-maze test in aged rats when administered at a dose of 3.6 mg/kg per day.⁷ Sarsasapogenin (12.5 mg/kg per day) reduces the amount of time mice spend immobile in the forced swim test, indicating antidepressant-like behavior.⁶

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1. Power, F.B., and Salway, A.H. XXV-Chemical examination of sarsaparilla root. J. Chem. Soc. 105, 201-219 (1914).

2. Yin, Y., Zhao, X.-C., Wang, S.-J., et al. Synthesis and biological evaluation of novel sarsasapogenin derivatives as potential anti-tumor agents. Steroids 93, 25-31 (2015).

3. Shen, S., Zhang, Y., Zhang, R., et al. Sarsasapogenin induces apoptosis via the reactive oxygen species-mediated mitochondrial pathway and ER stress pathway in HeLa cells. Biochem. Biophys. Res. Commun. 441(2), 519-524 (2013).

4. Lim, S.M., Jeong, J.J., Kang, G.D., et al. Timosaponin AIII and its metabolite sarsasapogenin ameliorate colitis in mice by inhibiting NF-κB and MAPK activation and restoring Th17/Treg cell balance. Int. Immunopharmacol. 25(2), 493-503 (2015).

5. Wang, Z.-D., Yao, G.-D., Wang, W., et al. Synthesis and evaluation of 26-amino acid methyl ester substituted sarsasapogenin derivatives as neuroprotective agents for Alzheimer’s disease. Steroids 125, 93-106 (2017).

6. Ren, L.-X., Luo, Y.-F., Li, X., et al. Antidepressant-like effects of sarsasapogenin from Anemarrhena asphodeloides BUNGE (Liliaceae). Biol. Pharm. Bull. 29(11), 2304-2306 (2006).

7. Hu, Y., Xia, Z., Sun, Q., et al. A new approach to the pharmacological regulation of memory: Sarsasapogenin improves memory by elevating the low muscarinic acetylcholine receptor density in brains of memory-deficit rat models. Brain Res. 1060(1-2), 26-39 (2005).