Literature DB >> 17234416

In vitro antimalarial activity of hyperforin, a prenylated acylphloroglucinol. A structure-activity study.

Luisella Verotta1, Giovanni Appendino, Ezio Bombardelli, Reto Brun.   

Abstract

The antimalarial activity of hyperforin, a phenol-like compound that can be easily absorbed orally, and a series of derivatives variously modified on the cyclohexatrienone system was investigated. Hyperforin was active against Plasmodium falciparum with an IC(50) value in the micromolar range, and the activity was not critically dependent on either its phenol-like sensitivity to autooxidation or the presence of unsaturation on the prenyl residues. Related phloroglucinols like the hop beta-acids and the enantiomers of usnic acid showed only marginal activity, suggesting that hyperforin is a new antimalarial chemotype.

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Year:  2007        PMID: 17234416     DOI: 10.1016/j.bmcl.2006.12.100

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

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Journal:  Angew Chem Int Ed Engl       Date:  2013-12-18       Impact factor: 15.336

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Authors:  Ina L Lauinger; Livia Vivas; Remo Perozzo; Christopher Stairiker; Alice Tarun; Mire Zloh; Xujie Zhang; Hua Xu; Peter J Tonge; Scott G Franzblau; Duc-Hung Pham; Camila V Esguerra; Alexander D Crawford; Louis Maes; Deniz Tasdemir
Journal:  J Nat Prod       Date:  2013-06-19       Impact factor: 4.050

3.  Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin.

Authors:  Koushi Hidaka; Tooru Kimura; Adam J Ruben; Tsuyoshi Uemura; Mami Kamiya; Aiko Kiso; Tetsuya Okamoto; Yumi Tsuchiya; Yoshio Hayashi; Ernesto Freire; Yoshiaki Kiso
Journal:  Bioorg Med Chem       Date:  2008-10-10       Impact factor: 3.641

4.  Tetrahydrohyperforin and octahydrohyperforin are two new potent inhibitors of angiogenesis.

Authors:  Beatriz Martínez-Poveda; Luisella Verotta; Ezio Bombardelli; Ana R Quesada; Miguel Angel Medina
Journal:  PLoS One       Date:  2010-03-09       Impact factor: 3.240

5.  Synthesis of a potent antimalarial agent through natural products conjugation.

Authors:  Michela Bruno; Beatrice Trucchi; Diego Monti; Sergio Romeo; Marcel Kaiser; Luisella Verotta
Journal:  ChemMedChem       Date:  2013-01-10       Impact factor: 3.466

6.  One-pot Diels-Alder cycloaddition/gold(I)-catalyzed 6-endo-dig cyclization for the synthesis of the complex bicyclo[3.3.1]alkenone framework.

Authors:  Boubacar Sow; Gabriel Bellavance; Francis Barabé; Louis Barriault
Journal:  Beilstein J Org Chem       Date:  2011-07-22       Impact factor: 2.883

7.  Protonophore properties of hyperforin are essential for its pharmacological activity.

Authors:  Thomas S Sell; Thabet Belkacemi; Veit Flockerzi; Andreas Beck
Journal:  Sci Rep       Date:  2014-12-16       Impact factor: 4.379

8.  Synthesis and Antimalarial Activity of Mallatojaponin C and Related Compounds.

Authors:  Alexander L Eaton; Seema Dalal; M Belen Cassera; Shuqi Zhao; David G I Kingston
Journal:  J Nat Prod       Date:  2016-05-26       Impact factor: 4.050

  8 in total

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