Title:Biosynthesis and Anticancer Activity of Genistein Glycoside Derivatives
Volume: 24
Issue: 13
Author(s): Xing Zheng, Jun Zhang, Shun Liu, Yingzi Yu, Qingying Peng, Yaling Peng, Xu Yao*, Xingxing Peng*Jing Zhou*
Affiliation:
- Institute of Pharmacy and Pharmacology, Hengyang Medicinal School, University of South China, Hengyang,
Hunan, 421001, China
- Institute of Pharmacy and Pharmacology, Hengyang Medicinal School, University of South China, Hengyang,
Hunan, 421001, China
- Institute of Pharmacy and Pharmacology, Hengyang Medicinal School, University of South China, Hengyang,
Hunan, 421001, China
Keywords:
Genistein derivatives, glycoside, anti-cancer activity, synthesis, biosynthesis, genistin.
Abstract: As a beneficial natural flavonoid, genistein has demonstrated a wide range of biological functions
via regulating a number of targets and signaling pathways, such as anti-cancer, antioxidant, antibacterial, antiinflammatory,
antifungal, antiviral, iron chelation, anti-obesity, anti-diabetes, and anti-hypertension. Pub-
Med/Medline and Web of Science were searched using appropriate keywords until the end of December 2023.
Despite its many potential benefits, genistein’s clinical application is limited by low hydrophilicity, poor solubility,
and suboptimal bioavailability due to its structure. These challenges can be addressed through the conversion
of genistein into glycosides. Glycosylation of active small molecules may enhance their solubility,
stability, and biological activity. In recent years, extensive research has been conducted on the synthesis, properties,
and anticancer activity of glycoconjugates. Previous reviews were devoted to discussing the biological
activities of genistin, with a little summary of the biosynthesis and the structure-activity relationship for their
anticancer activity of genistein glycoside derivatives. Therefore, we summarized recent advances in the biosynthesis
of genistein glycosylation and discussed the antitumor activities of genistein glycoside derivatives in a
structure-activity relationship, which may provide important information for further development of genistein
derivatives.
