Letter to the editor

An update on the biological and pharmacological activities of diosgenin

Jae Kwang Kim1, Sang Un Park2[*]

1Division of Life Sciences and Convergence Research Center for Insect Vectors, Incheon National University, Incheon 22012, Korea

2Department of Crop Science, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon, 34134, Korea

EXCLI J 2018;17:Doc24


Dear Editor,

Diosgenin, a phytosteroid saponin, is found at high levels in several plant species, including Costus speciosus, Smilax menispermoidea, Trigonella foenum, species of Paris, Aletris, Trigonella, and Trillium, and many species of Dioscorea (Patel et al., 2013[25]; Chen et al., 2011[4]).

Fujii and Matsukawa first discovered diosgenin within Dioscorea tokoro Makino in 1935 (Djerassi et al., 1952[7]). The biosynthesis of steroidal saponins such as diosgenin in plants has not yet been reported in detail, although cholesterol was found to be a precursor of this compound. Cholesterol is formed from lanosterol and some of the reactions involved are catalyzed by cytochrome P450 systems. Vaidya et al. (2013[29]) suggested that diosgenin might be formed from squalene-2,3-oxide in two ways: from lanosterol via cholesterol, and from cycloartenol via the formation of sitosterol (Ciura et al., 2017[6]).

In the pharmaceutical industry, diosgenin is the principal precursor compound in the manufacture of several synthetic steroidal drugs (Chen et al., 2015[5]). It also represents a promising bioactive biomolecule that exhibits various biological properties; these include hypolipidemic, hypoglycemic, antioxidant, anti-inflammatory, and antiproliferative activities (Jesus et al., 2016[14]). Diosgenin has therefore attracted considerable attention in recent years within the pharmaceutical, functional food, and cosmetic industries. Here, we summarize recent studies performed to evaluate the biological and pharmacological activities of diosgenin (Table 1(Tab. 1); References in Table 1: Badalzadeh et al., 2015[1]; Bhuvanalakshmi et al., 2017[2]; Chen et al., 2016[3]; Fang et al., 2015[8]; Folwarczna et al., 2016[9]; Hao et al., 2015[10]; Haratake A et al., 2017[11]; Hua et al., 2016[12]; Huang et al., 2017[13]; Jiang et al., 2016[15]; Junchao et al., 2017[16]; Kim et al., 2016[17]; Liu et al., 2016[19]; Liu et al., 2017[18]; Lv et al., 2015[20]; Masood-Ur-Rahman et al., 2017[21]; Mischitelli et al., 2016[22]; Naidu et al., 2015[23]; Nie et al., 2016[24]; Pi et al., 2017[26]; Selim and Al Jaouni, 2015[27]; Tikhonova et al., 2015[28]; Wang et al., 2015[30]; Wang et al., 2017[31]; Xie et al., 2015[32]; Zhang et al., 2016[33]; Zhao et al., 2016[34]; Zheng et al., 2016[35]; Zhou et al., 2017[36]).


This work was supported by Korea Institute of Planning and Evaluation for Technology in Food, Agriculture, Forestry and Fisheries(IPET) through Advanced Production Technology Development Program, funded by Ministry of Agriculture, Food and Rural Affairs (MAFRA) (116115-03-1-CG000). This research was supported by the Bio & Medical Technology Development Program of the National Research Foundation (NRF) funded by the Ministry of Science, ICT & Future Planning (2016M3A9A5919548).

Conflict of interest

The authors declare no conflict of interest.



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2. Bhuvanalakshmi G, Basappa, Rangappa KS, Dharmarajan A, Sethi G, Kumar AP, et al. Breast cancer stem-like cells are inhibited by diosgenin, a steroidal saponin, by the attenuation of the Wnt β-catenin signaling via the Wnt antagonist secreted frizzled related protein-4. Front Pharmacol. 2017;8:124.
3. Chen J, Zhang HF, Xiong CM, Ruan JL. Inhibitory effect of diosgenin on experimentally induced benign prostatic hyperplasia in rats. J Huazhong Univ Sci Technol Med Sci. 2016;36:806-10.
4. Chen PS, Shih YW, Huang HC, Cheng HW. Diosgenin, a steroidal saponin, inhibits migration and invasion of human prostate cancer PC-3 cells by reducing matrix metalloproteinases expression. PLoS One. 2011;6(5):e20164.
5. Chen Y, Tang YM, Yu SL, Han YW, Kou JP, Liu BL, et al. Advances in the pharmacological activities and mechanisms of diosgenin. Chin J Nat Med. 2015;13:578-87.
6. Ciura J, Szeliga M, Grzesik M, Tyrka M. Next-generation sequencing of representational difference analysis products for identification of genes involved in diosgenin biosynthesis in fenugreek (Trigonella foenum-graecum). Planta. 2017;245:977-91.
7. Djerassi C, Rosenkranz G, Pataki J, Kaufmann S. Steroids, XXVII. Synthesis of allopregnane-3beta, 11beta, 17alpha-, 20beta, 21-pentol from cortisone and diosgenin. J Biol Chem. 1952;194:115-8.
8. Fang K, Dong H, Jiang S, Li F, Wang D, Yang D, et al. Diosgenin and 5-methoxypsoralen ameliorate insulin resistance through ER-α/PI3K/Akt-signaling pathways in HepG2 cells. Evid Based Complement Alternat Med. 2016;2016:7493694.
9. Folwarczna J, Zych M, Nowińska B, Pytlik M, Bialik M, Jagusiak A, et al. Effect of diosgenin, a steroidal sapogenin, on the rat skeletal system. Acta Biochim Pol. 2016;63:287-95.
10. Hao S, Xu R, Li D, Zhu Z, Wang T, Liu K. Attenuation of Streptozotocin-Induced Lipid Profile Anomalies in the Heart, Brain, and mRNA Expression of HMG-CoA Reductase by Diosgenin in Rats. Cell Biochem Biophys. 2015;72:741-9.
11. Haratake A, Watase D, Setoguchi S, Nagata-Akaho N, Matsunaga K, Takata J. Effect of orally ingested diosgenin into diet on skin collagen content in a low collagen skin mouse model and its mechanism of action. Life Sci. 2017;174:77-82.
12. Hua S, Li Y, Su L, Liu X. Diosgenin ameliorates gestational diabetes through inhibition of sterol regulatory element-binding protein-1. Biomed Pharmacother. 2016;84:1460-5.
13. Huang CH, Wang CC, Lin YC, Hori M, Jan TR. Oral administration with diosgenin enhances the induction of intestinal T helper 1-like regulatory T cells in a murine model of food allergy. Int Immunopharmacol. 2017;42:59-66.
14. Jesus M, Martins AP, Gallardo E, Silvestre S. Diosgenin: recent highlights on pharmacology and analytical methodology. J Anal Methods Chem. 2016;2016:4156293.
15. Jiang S, Fan J, Wang Q, Ju D, Feng M, Li J, et al. Diosgenin induces ROS-dependent autophagy and cytotoxicity via mTOR signaling pathway in chronic myeloid leukemia cells. Phytomedicine. 2016;23:243-52.
16. Junchao Y, Zhen W, Yuan W, Liying X, Libin J, Yuanhong Z, et al. Anti- trachea inflammatory effects of diosgenin from Dioscorea nipponica through interactions with glucocorticoid receptor α. J Int Med Res. 2017;45:101-13.
17. Kim JE, Go J, Koh EK, Song SH, Sung JE, Lee HA, et al. Diosgenin effectively suppresses skin inflammation induced by phthalic anhydride in IL-4/Luc/CNS-1 transgenic mice. Biosci Biotechnol Biochem. 2016;80:891-901.
18. Liu J, He X, Zhen P, Chen H, Zhou S, Tian Q, et al. Sirtuin type 1 signaling pathway mediates the effect of diosgenin on chondrocyte metabolisms in osteoarthritis. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2017;422:121-7.
19. Liu J, He X, Zhen P, Zhou S, Li X. Protective effect of diosgenin on chondrocytes mediated by JAK2/STAT3 signaling pathway in mice with osteoarthritis. Zhejiang Da Xue Xue Bao Yi Xue Ban. 2016;45:453-60.
20. Lv YC, Yang J, Yao F, Xie W, Tang YY, Ouyang XP, et al. Diosgenin inhibits atherosclerosis via suppressing the MiR-19b-induced downregulation of ATP-binding cassette transporter A1. Atherosclerosis. 2015;240:80-9.
21. Masood-Ur-Rahman, Mohammad Y, Fazili KM, Bhat KA, Ara T. Synthesis and biological evaluation of novel 3-O-tethered triazoles of diosgenin as potent antiproliferative agents. Steroids. 2017;118:1-8.
22. Mischitelli M, Jemaà M, Almasry M, Faggio C, Lang F. Ca2+ entry, oxidative stress, ceramide and suicidal erythrocyte death following diosgenin treatment. Cell Physiol Biochem. 2016;39:1626-37.
23. Naidu PB, Ponmurugan P, Begum MS, Mohan K, Meriga B, RavindarNaik R, et al. Diosgenin reorganises hyperglycaemia and distorted tissue lipid profile in high-fat diet-streptozotocin-induced diabetic rats. J Sci Food Agric. 2015;95:3177-82.
24. Nie C, Zhou J, Qin X, Shi X, Zeng Q, Liu J, et al. Diosgenin‑induced autophagy and apoptosis in a human prostate cancer cell line. Mol Med Rep. 2016;14:4349-59.
25. Patel K, Gadewar M, Tahilyani V, Patel DK. A review on pharmacological and analytical aspects of diosmetin: a concise report. Chin J Integr Med. 2013;19:792-800.
26. Pi WX, Feng XP, Ye LH, Cai BC. Combination of morroniside and diosgenin prevents high glucose-induced cardiomyocytes apoptosis. molecules. 2017;22 (1):163.
27. Selim S, Al Jaouni S. Anticancer and apoptotic effects on cell proliferation of diosgenin isolated from Costus speciosus (Koen.) Sm. BMC Complement Altern Med. 2015;15:301.
28. Tikhonova MA, Ting CH, Kolosova NG, Hsu CY, Chen JH, Huang CW, et al. Improving bone microarchitecture in aging with diosgenin treatment: a study in senescence-accelerated OXYS rats. Chin J Physiol. 2015;58:322-31.
29. Vaidya K, Ghosh A, Kumar V, Chaudhary S, Srivastava N, Katudia K, et al. De novo transcriptome sequencing in Trigonella foenum-graecum L. to identify genes involved in the biosynthesis of diosgenin. Plant Genome. 2013;6:1–11.
30. Wang L, Ma T, Zheng Y, Lv S, Li Y, Liu S. Diosgenin inhibits IL-1β-induced expression of inflammatory mediators in human osteoarthritis chondrocytes. Int J Clin Exp Pathol. 2015;8:4830-6.
31. Wang S, Wang F, Yang H, Li R, Guo H, Hu L. Diosgenin glucoside provides neuroprotection by regulating microglial M1 polarization. Int Immunopharmacol. 2017;50:22-9.
32. Xie WL, Jiang R, Shen XL, Chen ZY, Deng XM. Diosgenin attenuates hepatic stellate cell activation through transforming growth factor-β/Smad signaling pathway. Int J Clin Exp Med. 2015;8:20323-9.
33. Zhang X, Xue X, Zhao J, Qian C, Guo Z, Ito Y, et al. Diosgenin attenuates the brain injury induced by transient focal cerebral ischemia-reperfusion in rats. Steroids. 2016;113:103-12.
34. Zhao S, Niu F, Xu CY, Liu Y, Ye L, Bi GB, et al. Diosgenin prevents bone loss on retinoic acid-induced osteoporosis in rats. Ir J Med Sci. 2016;185:581-7.
35. Zheng H, Wei Z, Xin G, Ji C, Wen L, Xia Q, et al. Preventive effect of a novel diosgenin derivative on arterial and venous thrombosis in vivo. Bioorg Med Chem Lett. 2016;26:3364-9.
36. Zhou HT, Yu XF, Zhou GM. Diosgenin inhibits angiotensin II-induced extracellular matrix remodeling in cardiac fibroblasts through regulating the TGF‑β1/ Smad3 signaling pathway. Mol Med Rep. 2017;15:2823-8.

Table 1: Recent studies of the biological and pharmacological activities of diosgenin

[*] Corresponding Author:

Sang Un Park, Department of Crop Science, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon, 34134, Korea; Tel.: +82-42-821-5730, Fax: +82-42-822-2631, eMail: supark@cnu.ac.kr