Comparison of Antibacterial and Antifungal Activities of Lapachol and β-Lapachone

Guiraud, Pascal; Steiman, R.; Campos-Takaki, Galba Maria de; Seigle‐Murandi, F.; Buochberg, M. Simeon De

doi:10.1055/s-2006-959504

Cited by 152 publications

(90 citation statements)

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“…1) is one of the most studied. Lapachol is endowed with anticancer and antimicrobial properties [7,8]. Because of its antiproliferative activity, lapachol has been employed as a prototype for the design and synthesis of new anticancer and antimicrobial agents.…”

Section: Introductionmentioning

confidence: 99%

Antiparasitic activities of novel ruthenium/lapachol complexes

Barbosa

Corrêa

Oliveira

et al. 2014

Journal of Inorganic Biochemistry

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The present study describes the synthesis, characterization, antileishmanial and antiplasmodial activities of novel diimine/(2,2′-bipyridine (bipy), 1,10-phenanthroline (phen), 4,4′-methylbipyridine (Me-bipy) and 4,4′-methoxybipyridine (MeO-bipy)/phosphine/ruthenium(II) complexes containing lapachol (Lap, 2-hydroxy-3- The Ru(III) complex, [RuCl 2 (Lap)(dppb)], was also characterized by the EPR technique. The structure of the complexes [Ru(Lap)(PPh 3 ) 2 (bipy)]PF 6 and [RuCl 2 (Lap)(dppb)] was elucidated by X-ray diffraction. The evaluation of the antiparasitic activities of the complexes against Leishmania amazonensis and Plasmodium falciparum demonstrated that lapachol-ruthenium complexes are more potent than the free lapachol. The [RuCl 2 (Lap)(dppb)] complex is the most potent and selective antiparasitic compound among the five new ruthenium complexes studied in this work, exhibiting an activity comparable to the reference drugs.

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Section: Introductionmentioning

confidence: 99%

Antiparasitic activities of novel ruthenium/lapachol complexes

Barbosa

Corrêa

Oliveira

et al. 2014

Journal of Inorganic Biochemistry

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“…Chemically related compounds were also effective against staphylococci, presenting similar MIC values (3,10,39). Particularly, isoxazolylnaphthoquinones show MIC ranging from 16 to 64 µg/ml against different clinical isolates of S. aureus, suggesting their potential application as antimicrobial agents (10).…”

Section: Discussionmentioning

confidence: 99%

In vitro antimicrobial activity of a new series of 1,4-naphthoquinones

Riffel

Medina

Stéfani

et al. 2002

Braz J Med Biol Res

124

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The antibacterial activity of a series of 1,4-naphthoquinones was demonstrated. Disk diffusion tests were carried out against several Gram-positive and Gram-negative bacteria. The compound 5-amino-8-hydroxy-1,4-naphthoquinone was the most effective, presenting inhibition zones measuring 20 mm against staphylococci, streptococci and bacilli at 50 µg/ml. Methicillin-resistant Staphylococcus aureus and several clinical isolates of this bacterium were also inhibited. Naphthazarin, 5-acetamido-8-hydroxy-1,4-naphthoquinone, and 2,3-diamino-1,4-naphthoquinone were the next most active compounds. The minimal inhibitory concentration of the active compounds was determined against S. aureus, ranging from 30 to 125 µg/ml. All compounds presented a minimal bactericidal concentration higher than 500 µg/ml, indicating that their effect was bacteriostatic. The EC 50 , defined as the drug concentration that produces 50% of maximal effect, was 8 µg/ml for 5-amino-8-hydroxy-1,4-naphthoquinone against S. aureus, S. intermedius, and S. epidermidis. These results indicate an effective in vitro activity of 5-amino-8-hydroxy-1,4-naphthoquinone and encourage further studies for its application in antibiotic therapy.

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“…Previous studies showing antifungal activity of lapachol and beta-lapachone against C. neoformans are to some extent contradictory because of the different experimental protocols used (10). Nevertheless, these data indicate that new studies are necessary before proposing antifungal tests on humans.…”

Section: Received May 23 2009 Acceptedmentioning

confidence: 99%