Cytotoxic and Antitumor Potentialities of Aporphinoid Alkaloids

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Cytotoxic and Antitumor Potentialities of Aporphinoid Alkaloids

Anti-Cancer Agents in Medicinal Chemistry, 5(2): 173-182.

Author(s): C. Stevigny, C. Bailly and J Quetin-Leclercq.

Affiliation: Laboratoire de Pharmacognosie, Unite d;Analyse Chimique et Physico-Chimique des Medicaments, Universite Catholique de Louvain, UCL 72.30-CHAM, Av. E. Mounier 72, 1200 Bruxelles, Belgium.


Aporphinoids form an important group of plant secondary metabolites. Some of these compounds are used for a long time in traditional medicine for the treatment of various diseases, from benign syndromes to more severe illnesses. More than 500 aporphine alkaloids have been isolated from various plant families and many of these compounds display potent cytotoxic activities which may be exploited for the design of anticancer agents. Here we review the origin, biosynthesis, structure and cytotoxic properties of the prominent members of this class of compounds. Simple aporphinoids (boldine, dicentrine) as well as oxo-, pro- and dehydro-aporphines, and dimeric forms such as thalicarpine, are discussed here. Their mechanisms of action are not well known but DNA-manipulating enzymes such as polymerases and topoisomerases are among the most frequently cited targets for these benzylisoquinoline compounds. This review presents an updated view of the cytotoxic properties of the aporphinoids and their potential contribution to the development of anticancer agents.


aporphine alkaloids, aporphinoids, anticancer agents, natural products, cytotoxicity.

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Article Details

Volume: 5
Issue Number: 2
First Page: 173
Last Page: 182
Page Count: 10
DOI: 10.2174/1568011053174864
Price: $58
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