Therapeutic Potential of Diosgenin and Its Major Derivatives against Neurological Diseases: Recent Advances

Abstract

Diosgenin (DG), a well-known steroidal sapogenin, is present abundantly in medicinal herbs such as Dioscorea rhizome, Dioscorea villosa, Trigonella foenum-graecum, Smilax China, and Rhizoma polgonati. DG is utilized as a major starting material for the production of steroidal drugs in the pharmaceutical industry. Due to its wide range of pharmacological activities and medicinal properties, it has been used in the treatment of cancers, hyperlipidemia, inflammation, and infections. Numerous studies have reported that DG is useful in the prevention and treatment of neurological diseases. Its therapeutic mechanisms are based on the mediation of different signaling pathways, and targeting these pathways might lead to the development of effective therapeutic agents for neurological diseases. The present review mainly summarizes recent progress using DG and its derivatives as therapeutic agents for multiple neurological disorders along with their various mechanisms in the central nervous system. In particular, those related to therapeutic efficacy for Parkinson’s disease, Alzheimer’s disease, brain injury, neuroinflammation, and ischemia are discussed. This review article also critically evaluates existing limitations associated with the solubility and bioavailability of DG and discusses imperatives for translational clinical research. It briefly recapitulates recent advances in structural modification and novel formulations to increase the therapeutic efficacy and brain levels of DG. In the present review, databases of PubMed, Web of Science, and Scopus were used for studies of DG and its derivatives in the treatment of central nervous system diseases published in English until December 10, 2019. Three independent researchers examined articles for eligibility. A total of 150 articles were screened from the above scientific literature databases. Finally, a total of 46 articles were extracted and included in this review. Keywords related to glioma, ischemia, memory, aging, cognitive impairment, Alzheimer, Parkinson, and neurodegenerative disorders were searched in the databases based on DG and its derivatives.

Evaluation of diosgenin content from eleven different Indian varieties of fenugreek and fenugreek leaf powder fortified bread

“…Many researchers reported the medicinal importance of diosgenin on many diseases such as pathologies, including diabetes, hyperlipidemia, cancer, cardiovascular disease, oxidative stress, and inflammation etc. (Pari et al 2012;Deshpande and Bhalsing 2014;Dangi et al 2014;Cai et al 2020).…”

“…Diosgenin used extensively as an essential compound for the production of sex hormones, oral contraceptives pills and steroidal drugs due to its extensive pharmaceutical applications (Deshpande and Bhalsing 2014). Diosgenin found to be effective against disorders like diabetes, hyperlipidemia, different types of cancer, osteoporosis, cardiovascular diseases, skin diseases, oxidative stress, inflammation and neurological diseases (Deshpande and Bhalsing 2014;Dangi et al 2014;Cai et al 2020). However, due to its low solubility in water and poor bioavailability, it is hard to explore the medicinal property of diosgenin (Cai et al 2020).…”

“…Diosgenin found to be effective against disorders like diabetes, hyperlipidemia, different types of cancer, osteoporosis, cardiovascular diseases, skin diseases, oxidative stress, inflammation and neurological diseases (Deshpande and Bhalsing 2014;Dangi et al 2014;Cai et al 2020). However, due to its low solubility in water and poor bioavailability, it is hard to explore the medicinal property of diosgenin (Cai et al 2020). Therefore, food formulation may be an excellent alternative to provide diosgenin to the layman in a cost-effective manner.…”

The Dioscorea Genus (Yam)—An Appraisal of Nutritional and Therapeutic Potentials

“…Members of the Dioscorea genus mostly contain spirostane and furostane steroid glycosides; however, studies have reported the possible presence of other steroidal saponins [ 136 , 137 ]. Predominantly, yams contain a spirostane steroidal sapogenin known as diosgenin with a structure of 25R-spirost-5-en-3b-ol consisting of a hydrophilic sugar moiety linked to a hydrophobic steroid aglycone with a molecular formula C 27 H 42 O 3 [ 138 , 139 ].…”

“…The underlying mechanism of action of diosgenin may vary depending on the disease and has been reviewed by Cai et al [ 139 ], Chen et al [ 143 ] and Raju and Rao [ 138 ]. Although diosgenin has been reported in several yam species, its content varies considerably within the Dioscorea genus with D. barbasco (Mexican wild yam) and D. zingiberensis (Chinese yam) being very important sources for diosgenin [ 146 , 147 ].…”