Betulinic Acid: Recent Advances in Chemical Modifications, Effective Delivery, and Molecular Mechanisms of a Promising Anticancer Therapy

Mohamed Ali-Seyed, Ibrahim Jantan, Kavitha Vijayaraghavan, Bukhari Syed Nasir Abbas

Research output: Contribution to journalArticle

46 Citations (Scopus)

Abstract

An important method of drug discovery is examination of diverse life forms, including medicinal plants and natural products or bioactive compounds isolated from these sources. In cancer research, lead structures of compounds from natural sources can be used to design novel chemotherapies with enhanced biological properties. Betulinic acid (3β-hydroxy-lup-20(29)-en-28-oic acid or BetA) is a naturally occurring pentacyclic triterpene with a wide variety of biological activities, including potent antitumor properties. Non-malignant cells and normal tissues are not affected by BetA. Because BetA exerts its effects directly on the mitochondrion and triggers death of cancerous cells, it is an important alternative when certain chemotherapy drugs fail. Mitochondrion-targeted agents such as BetA hold great promise to circumvent drug resistance in human cancers. BetA is being developed by a large network of clinical trial groups with the support of the U.S. National Cancer Institute. This article discusses recent advances in research into anticancer activity of BetA, relevant modes of delivery, and the agent's therapeutic efficacy, mechanism of action, and future perspective as a pipeline anticancer drug. BetA is a potentially important agent in cancer therapeutics.

Original languageEnglish
Pages (from-to)517-536
Number of pages20
JournalChemical Biology and Drug Design
Volume87
Issue number4
DOIs
Publication statusPublished - 1 Apr 2016

Fingerprint

Chemical modification
Mitochondria
Chemotherapy
Pentacyclic Triterpenes
Pharmaceutical Preparations
Drug Therapy
Neoplasms
National Cancer Institute (U.S.)
Drug Discovery
Medicinal Plants
Bioactivity
Biological Products
Research
Drug Resistance
Cell Death
Therapeutics
Pipelines
Cells
Clinical Trials
Tissue

Keywords

  • anticancer agents
  • apoptosis
  • BetA
  • betulin
  • betulinic acid
  • natural products
  • pipeline drugs
  • plant derivatives

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine

Cite this

Betulinic Acid : Recent Advances in Chemical Modifications, Effective Delivery, and Molecular Mechanisms of a Promising Anticancer Therapy. / Ali-Seyed, Mohamed; Jantan, Ibrahim; Vijayaraghavan, Kavitha; Syed Nasir Abbas, Bukhari.

In: Chemical Biology and Drug Design, Vol. 87, No. 4, 01.04.2016, p. 517-536.

Research output: Contribution to journalArticle

Ali-Seyed, Mohamed ; Jantan, Ibrahim ; Vijayaraghavan, Kavitha ; Syed Nasir Abbas, Bukhari. / Betulinic Acid : Recent Advances in Chemical Modifications, Effective Delivery, and Molecular Mechanisms of a Promising Anticancer Therapy. In: Chemical Biology and Drug Design. 2016 ; Vol. 87, No. 4. pp. 517-536.
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