Enhanced Water Solubility and Anti-Tumor Activity of Oleanolic Acid through Chemical Structure Modification

Cancer has been a major health problem in the world in the past decades. It is urgent to develop new, effective and safe drugs for the treatment of cancer. There are many pentacyclic triterpenoids with positive anti-tumor activity and safety in nature. Oleanolic acid (OA), as one of the pentacyclic...

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Bibliographic Details
Published in:International journal of molecular sciences 2022-11, Vol.23 (21), p.13291
Main Authors: Gu, Zhicheng, Lin, Shuxian, Yan, Wanli, Chen, Di, Zeng, Ziwei, Chen, Lei, Li, Yan, He, Bin
Format: Article
Language:English
Subjects:
Angiogenesis
anti-tumor
Antiviral agents
Apoptosis
Autophagy
Breast cancer
Cancer therapies
Cell cycle
Cell growth
Chemotherapy
Colorectal cancer
Cytochrome
Cytotoxicity
Drugs
Hepatocytes
Inflammation
Liver
Natural products
Oleanolic acid
Pentacyclic triterpenoids
Phosphorylation
Proteins
Review
Signal transduction
Solubility
Triterpenoids
Tumors
water solubility
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Summary:Cancer has been a major health problem in the world in the past decades. It is urgent to develop new, effective and safe drugs for the treatment of cancer. There are many pentacyclic triterpenoids with positive anti-tumor activity and safety in nature. Oleanolic acid (OA), as one of the pentacyclic triterpenoids, also has broad biological activities including liver protection, anti-inflammatory, hypoglycemic, antiviral and anti-tumor. Therefore, to investigate its anti-tumor activity and mechanism, many OA derivatives have been developed. Some derivatives are less toxic to normal hepatocytes, which may be due to the strong liver protection ability of OA. However, the poor water solubility of OA is one of the main reasons for the weak anti-tumor activity. It is reported that some OA derivatives could enhance solubility by chemically linking some hydrophilic groups to improve anti-tumor activity. This review not only summarizes the highly water-soluble OA derivatives that can improve anti-tumor activity reported in recent years, but also introduces their possible anti-tumor mechanisms.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms232113291