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Int. J. Mol. Sci. 2010, 11(2), 562-594; doi:10.3390/ijms11020562
Review

Hypericins as Potential Leads for New Therapeutics

*  and
Received: 3 December 2009; in revised form: 27 January 2010 / Accepted: 28 January 2010 / Published: 4 February 2010
(This article belongs to the Special Issue Phenolics and Polyphenolics)
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Abstract: 70 years have passed since the first isolation of the naphthodianthrones hypericin and pseudohypericin from Hypericum perforatum L. Today, they continue to be one of the most promising group of polyphenols, as they fascinate with their physical, chemical and important biological properties which derive from their unique chemical structure. Hypericins and their derivatives have been extensively studied mainly for their antitumor, antiviral and antidepressant properties. Notably, hypericin is one of the most potent naturally occurring photodynamic agents. It is able to generate the superoxide anion and a high quantum yield of singlet oxygen that are considered to be primarily responsible for its biological effects. The prooxidant photodynamic properties of hypericin have been exploited for the photodynamic therapy of cancer (PDT), as hypericin, in combination with light, very effectively induces apoptosis and/or necrosis of cancer cells. The mechanism by which these activities are expressed continues to be a main topic of discussion, but according to scientific data, different modes of action (generation of ROS & singlet oxygen species, antiangiogenesis, immune responces) and multiple molecular pathways (intrinsic/extrinsic apoptotic pathway, ERK inhibition) possibly interrelating are implicated. The aim of this review is to analyse the most recent advances (from 2005 and thereof) in the chemistry and biological activities (in vitro and in vivo) of the pure naphthodianthrones, hypericin and pseudohypericin from H. perforatum. Extracts from H. perforatum were not considered, nor pharmakokinetic or clinical data. Computerised literature searches were performed using the Medline (PubMed), ChemSciFinder and Scirus Library databases. No language restrictions were imposed.
Keywords: Hypericum perforatum; naphthodianthrones; hypericin; pseudohypericin; photodynamic therapy; antiviral; antidepressant Hypericum perforatum; naphthodianthrones; hypericin; pseudohypericin; photodynamic therapy; antiviral; antidepressant
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Karioti, A.; Bilia, A.R. Hypericins as Potential Leads for New Therapeutics. Int. J. Mol. Sci. 2010, 11, 562-594.

AMA Style

Karioti A, Bilia AR. Hypericins as Potential Leads for New Therapeutics. International Journal of Molecular Sciences. 2010; 11(2):562-594.

Chicago/Turabian Style

Karioti, Anastasia; Bilia, Anna Rita. 2010. "Hypericins as Potential Leads for New Therapeutics." Int. J. Mol. Sci. 11, no. 2: 562-594.



Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert