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Establishment of Hepatocarcinoma in BALB/c-nu Mice and Investigation of the Therapeutic Effect of the Sanleng Jiashen Formula
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An Update on Pentacyclic Triterpenoids Ursolic and Oleanolic Acids and Related Derivatives as Anticancer Candidates

Diana Similie1,2, Daliana Minda1,2, Larisa Bora1,2

  • 1Department of Pharmacognosy, Faculty of Pharmacy, "Victor Babeș" University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Romania.

Antioxidants (Basel, Switzerland)
|August 29, 2024
PubMed

Insights

Ursolic acid and oleanolic acid derivatives show promise for cancer treatment. Chemical modifications enhance their anticancer efficacy, solubility, and stability, offering new therapeutic strategies.

Area of Science:

  • Natural Product Chemistry
  • Medicinal Chemistry
  • Oncology

Background:

  • Cancer poses a significant global health challenge, with limited curative options.
  • Plant-derived compounds, particularly pentacyclic triterpenoids like ursolic acid (UA) and oleanolic acid (OA), exhibit anticancer potential.
  • Challenges with natural products include poor physicochemical properties, hindering clinical application.

Purpose of the Study:

  • To review recent advancements in the synthesis and evaluation of UA and OA derivatives for anticancer applications.
  • To highlight structural modifications that improve the therapeutic profile of these natural compounds.

Main Methods:

  • Literature review of studies synthesizing and testing UA and OA derivatives.
  • Analysis of structural modifications, focusing on positions C-3 and C-28.
  • Evaluation of derivative properties including solubility, absorption, stability, efficacy, and toxicity.

Main Results:

  • Derivatization of UA and OA significantly enhances their anticancer efficacy.
  • Modifications at C-3, C-28, or both positions are common strategies.
  • Conjugation with heterocycles, cinnamic acid, or formation of hydrazides, esters, and amides improved anticancer activity.

Conclusions:

  • UA and OA derivatives represent a promising avenue for developing novel anticancer agents.
  • Strategic chemical modifications can overcome limitations of natural products, leading to improved drug candidates.
  • Further research into these derivatives could yield more effective cancer chemotherapies.
Keywords:
antiproliferativecancerchemopreventiveclinical trialscytotoxicin vitroin vivooleanolic acidpentacyclic triterpenoidsproapoptoticursolic acid

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