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Prodrugs of triterpenoids and their derivatives

2017; Elsevier BV; Volume: 131; Linguagem: Inglês

10.1016/j.ejmech.2017.03.005

1768-3254

Meng Zhou, Rong‐Hong Zhang, Min Wang, Guo‐Bo Xu, Shang‐Gao Liao,

Phytochemical compounds biological activities

Triterpenoids are structurally diverse organic compounds that exist widely as natural products. Triterpenoids and their derivatives possess a wide range of biological effects including hepatoprotective, hypoglycemic, immunomodulatory, anti-inflammatory, anti-oxidant, and antitumor activities. In particular, the lupane-, oleanane-, and ursane-type triterpenes have been reported to exhibit pharmacological effects without prominent toxicity even at higher concentrations. Whereas, the poor drug-like properties (e.g., low solubility and selectivity, poor bioavailability, and short half-life) severely limit their applications. This review summarized the advances in prodrug strategies for improving the drug-like properties of different types of triterpenoids, and the information indicated in the review will surely stimulate further efforts toward the development of these compounds for potential clinical uses.