Abstract

Diosgenin is a steroidal saponin isolated from dioscorea opposita, which has been proven to have anti-cancer, anti-inflammatory, anti-thrombotic and immune system modulating effects in a large number of pharmacological tests. Diosgenin is also one of the important raw materials for the synthesis of steroidal drugs, and structural modification of diosgenin to obtain diosgenin derivatives can not only improve the solubility and dissolution, but also enhance their pharmacological effects. This paper reviews the synthetic reactions, pharmacological effects of diosgenin and its derivatives, aiming to provide detailed information for the further development and application of diosgenin, which is important to improve the utilization value of diosgenin.

Highlights

  • Diosgenin (Dio) is a steroidal saponin isolated from Dioscorea nipponica Makino (Chinese Pharmacopoeia Commission, 2020), an endemic dioscorea plant in China, commonly known as dioscorea, which is known as (3β,25R)-spirost-5-en-3-ol in IUPAC, CAS No.:512-04-9, is a spirostanol glycosides, obtained by hydrolysis and extraction from raw material of Sichuan Dioscorea or Huang Jiang

  • Several studies have shown that diosgenin have a variety of biological activities, such as anti-bacterial (Cong et al, 2020), anti-inflammatory, anti-cardiovascular disease (Chen et al, 2015), hypoglycemic, and can be used as an effective antioxidant (Jesus et al, 2016); at the same time, diosgenin can act on cells to inhibit the proliferation and induce apoptosis of many cancer cells (Digbeu et al, 2013; Leonel et al.,2006), such as hepatocellular carcinoma, breast cancer, gastric cell carcinoma, and prostate cancer; in addition, it have the ability to delay aging, anti-pulmonary fibrosis (Sun et al, 2019), immunomodulation, anti-hyperthyroidism (Wang et al, 2016), anti-platelet aggregation and hypolipidemic effects

  • We review the progress of domestic and international research in recent years regarding the synthesis of steroidal drugs, pharmacological effects and related mechanisms in anti-tumor, immunomodulatory and anti-inflammatory and anti-thrombotic aspects

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Summary

Introduction

Diosgenin (Dio) is a steroidal saponin isolated from Dioscorea nipponica Makino (Chinese Pharmacopoeia Commission, 2020), an endemic dioscorea plant in China, commonly known as dioscorea, which is known as (3β,25R)-spirost-5-en-3-ol in IUPAC, CAS No.:512, is a spirostanol glycosides, obtained by hydrolysis and extraction from raw material of Sichuan Dioscorea or Huang Jiang. Diosgenin have a wide range of applications in pharmaceutical, functional food and skin care industries, especially the pharmaceutical industry uses diosgenin as the main precursor compounds to make steroid drugs (Chen et al, 2015). We review the progress of domestic and international research in recent years regarding the synthesis of steroidal drugs, pharmacological effects and related mechanisms in anti-tumor, immunomodulatory and anti-inflammatory and anti-thrombotic aspects

Synthesis of diosgenin derivatives
Glucocorticoids
Diosgenin derivatives
Pharmacological effects of diosgenin
Anti-tumor
Immunomodulation and anti-inflammation
Anti-thrombotic
Pharmacological effects of diosgenin derivatives
Anti-inflammatory and analgesic
Effects on tracheal smooth muscle
Discussion
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