Quassinoids: From traditional drugs to new cancer therapeutics

Fiaschetti, G; Grotzer, M A; Shalaby, T; Castelletti, D; Arcaro, A (2011). Quassinoids: From traditional drugs to new cancer therapeutics. Current medicinal chemistry, 18(3), pp. 316-28. Schiphol: Bentham 10.2174/092986711794839205

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Quassinoids are a group of compounds extracted from plants of the Simaroubaceae family, which have been used for many years in folk medicine. These molecules gained notoriety after the initial discovery of the anti-leukemic activity of one member, bruceantin, in 1975. Currently over 150 quassinoids have been isolated and classified based on their chemical structures and biological properties investigated in vitro and in vivo. Many molecules display a wide range of inhibitory effects, including anti-inflammatory, anti-viral, anti-malarial and anti-proliferative effects on various tumor cell types. Although often the exact mechanism of action of the single agents remains unclear, some agents have been shown to affect protein synthesis in general, or specifically HIF-1α and MYC, membrane polarization and the apoptotic machinery. Considering that future research into chemical modifications is likely to generate more active and less toxic derivatives of natural quassinoids, this family represents a powerful source of promising small molecules targeting key prosurvival signaling pathways relevant for diverse pathologies. Here, we review available knowledge of functionality and possible applications of quassinoids and quassinoid derivatives, spanning traditional use to the potential impact on modern medicine as cancer therapeutics.

Item Type:

Journal Article (Further Contribution)

Division/Institute:

04 Faculty of Medicine > Department of Gynaecology, Paediatrics and Endocrinology (DFKE) > Clinic of Paediatric Medicine

UniBE Contributor:

Arcaro, Alexandre

ISSN:

0929-8673

Publisher:

Bentham

Language:

English

Submitter:

Factscience Import

Date Deposited:

04 Oct 2013 14:24

Last Modified:

06 Dec 2013 13:29

Publisher DOI:

10.2174/092986711794839205

PubMed ID:

21143123

Web of Science ID:

000286587600001

URI:

https://boris.unibe.ch/id/eprint/8330 (FactScience: 213851)

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