Abstract

Novel and alternative options are being adopted to combat the initiation and progression of human cancers. One of the approaches is the use of molecules isolated from traditional medicinal herbs, edible dietary plants and seeds that play a pivotal role in the prevention/treatment of cancer, either alone or in combination with existing chemotherapeutic agents. Compounds that modulate these oncogenic processes are potential candidates for cancer therapy and may eventually make it to clinical applications. Diosgenin is a naturally occurring steroidal sapogenin and is one of the major bioactive compounds found in dietary fenugreek (Trigonella foenum-graecum) seeds. In addition to being a lactation aid, diosgenin has been shown to be hypocholesterolemic, gastro- and hepato-protective, anti-oxidant, anti-inflammatory, anti-diabetic, and anti-cancer. Diosgenin has a unique structural similarity to estrogen. Several preclinical studies have reported on the pro-apoptotic and anti-cancer properties of diosgenin against a variety of cancers, both in in vitro and in vivo. Diosgenin has also been reported to reverse multi-drug resistance in cancer cells and sensitize cancer cells to standard chemotherapy. Remarkably, diosgenin has also been reported to be used by pharmaceutical companies to synthesize steroidal drugs. Several novel diosgenin analogs and nano-formulations have been synthesized with improved anti-cancer efficacy and pharmacokinetic profile. In this review we discuss in detail the multifaceted anti-cancer properties of diosgenin that have found application in pharmaceutical, functional food, and cosmetic industries; and the various intracellular molecular targets modulated by diosgenin that abrogate the oncogenic process.

Highlights

  • Cancer is a complex and heterogeneous disease that afflicts men and women worldwide; it is expected to increase due to human lifestyle changes and a rapidly aging population [1]

  • In this review we provide an in-depth evaluation of literature on diosgenin and its and its pharmacodynamics and pharmacokinetics, discuss several novel derivatives derivatives and pharmacodynamics and pharmacokinetics, and and discuss several of ofitsitsnovel and pharmacodynamics and pharmacokinetics, and discuss several of its novel derivatives and nanoformulations nanoformulationsthat that increase increaseits its bioavailability bioavailability and and therapeutic therapeutic efficacy

  • In a recent article by Ghosh et al, they reported the synthesis of diosgenin functionalized iron oxide nanoparticles that exhibited anti-breast cancer activity by inhibiting proliferation and migration, and by inducing apoptosis [89]

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Summary

Introduction

Cancer is a complex and heterogeneous disease that afflicts men and women worldwide; it is expected to increase due to human lifestyle changes and a rapidly aging population [1]. The mainstream of United States Food and Drug Administration (US FDA)-approved compounds divulge that natural products and their derivatives occupy one-third of all novel drugs [22,23,24,31] These natural compounds, in general, show multi-targeted effects and can modulate several oncogenic transcription factors that block the tumor microenvironment targets that usually sustain tumor growth [22,27,32]. Diosgenin is a phytosteroidal saponin and a major bioactive compound found in the seeds of T. foenum-graecum, commonly known as fenugreek, and in the roots of wild yam (Dioscorea villosa) [36,40, 41,47,48].

Fenugreek
In Vitro Anti-Cancer Effects of Diosgenin
In Vivo Anti-Cancer Effects of Diosgenin
Semisynthetic Derivatives of Diosgenin That Exhibit Anti-Cancer Activity
Findings
Conclusions and Future Perspectives

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