Phloroglucinol derivatives from Hypericum species trigger mitochondrial dysfunction in Leishmania amazonensis

Parasitology
Ana Paula DagninoPedro Roosevelt Torres Romão

Abstract

Bioactive molecules isolated from plants are promising sources for the development of new therapies against leishmaniasis. We investigated the leishmanicidal activity of cariphenone A (1), isouliginosin B (2) and uliginosin B (3) isolated from Hypericum species. Promastigotes and amastigotes of Leishmania amazonensis were incubated with compounds 1-3 at concentrations 1-100 µm for 48 h. The anti-promastigote effect of compounds was also tested in combinations. The cytotoxicity against macrophages and human erythrocytes were determined using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) method and hemolysis assay, respectively. The compounds 1-3 showed high leishmanicidal activity against promastigotes, IC50 values of 10.5, 17.5 and 11.3 µm, respectively. Synergistic interactions were found to the associations of compounds 1 and 2 [Σ fractional inhibitory concentration (FIC) = 0.41], and 2 and 3 (ΣFIC = 0.28) on promastigotes. All Hypericum compounds induced mitochondrial hyperpolarization and reactive oxygen species production in promastigotes. The compounds showed low cytotoxicity toward mammalian cells, high selectivity index and killed intracellular amastigotes probably mediated by oxidative stress. ...Continue Reading

References

Mar 1, 1997·Molecular and Biochemical Parasitology·J J Van Hellemond, A G Tielens
May 22, 2001·Archives of Biochemistry and Biophysics·L Gille, H Nohl
Jun 16, 2001·Antimicrobial Agents and Chemotherapy·D SerenoJ L Lemesre
Nov 19, 2002·Antimicrobial Agents and Chemotherapy·Mireille BasselinMichael P Barrett
Apr 16, 2005·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·R FennerS Zacchino
Jun 1, 2005·Journal of Natural Products·Ana Paula M BernardiGilsane Lino von Poser
Sep 6, 2005·Experimental Parasitology·Brice RotureauBernard Carme
Oct 13, 2005·Molecular and Biochemical Parasitology·Angana MukherjeeRentala Madhubala
Dec 27, 2005·Antimicrobial Agents and Chemotherapy·Karin Seifert, Simon L Croft
Feb 25, 2006·Artificial Intelligence in Medicine·Stefan WagenpfeilAntonie Lehmer
Aug 28, 2007·Journal of Ethnopharmacology·Daniela FritzGilsane Lino von Poser
Dec 15, 2007·Nature Protocols·Cristiano Ferlini, Giovanni Scambia
Aug 3, 2010·Bioorganic & Medicinal Chemistry·Carlos Nava-ZuazoGabriel Navarrete-Vazquez
Jun 15, 2011·Bioorganic & Medicinal Chemistry Letters·Sandip B Bharate, Inder Pal Singh
Aug 2, 2011·Fitoterapia·Jasmeen SidanaInder Pal Singh
Jan 31, 2012·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·M A BrenzanD A G Cortez
Jun 20, 2012·Natural Product Research·Joaquim S Costa JúniorRivelilson M Freitas
Apr 30, 2013·Bioorganic & Medicinal Chemistry·Claudia Mara Maciel-RezendeMarcelo Henrique dos Santos
Sep 30, 2014·Journal of Natural Products·Gari V Ccana-CcapatintaGilsane L von Poser
Feb 1, 2015·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Ana Paula DagninoPedro R T Romão
Jul 25, 2015·BMC Complementary and Alternative Medicine·Raquel Raick P da SilvaEdilene O Silva
Oct 16, 2015·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Letícia de AlmeidaMarcos José Marques
Dec 23, 2015·Journal of Natural Products·Cecilia SocolskyAlicia Bardón

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Citations

May 1, 2018·Journal of Enzyme Inhibition and Medicinal Chemistry·Verônica da Silva CardosoClaudiu T Supuran
Feb 16, 2021·Frontiers in Microbiology·Patrícia de Almeida MachadoHerbert Leonel de Matos Guedes
Jun 15, 2021·Frontiers in Molecular Biosciences·Lakshika SharmaM M Sharma

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