Effect of Some Compounds on Tubercle Bacilli &lt;i&gt;in vitro&lt;/i&gt;. VII

Naito, Masukazu; Watanabe, Reika; Fujikawa, Fukujiro; Nakajima, Kunio; Tokuoka, Akimasa; Hitosa, Yuhei

doi:10.1248/yakushi1947.73.9_911

Cited by 1 publication

(2 citation statements)

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“…21,42,43 The low efficacy of 3 against M. tuberculosis 44 and S. aureus 45 is in agreement with the results obtained in this study. The antimycobacterial potential of 2 reported half a century ago 46 could not be confirmed in this work; and although several reports over the last 60 years described the antibacterial activity of 1 , 2 and 4 against S. aureus . 20,47,48 2 was the only compound inhibiting S. aureus with an IC 50 of 32 μ M, which is lower than that previously reported.…”

Section: Resultscontrasting

confidence: 82%

“…Reported antimycobacterial activity of (+)-usnic acid ( 4 ) ranges from similar to 10 times lower potency. ,, The low efficacy of 3 against M. tuberculosis and S. aureus is in agreement with the results obtained in this study. The antimycobacterial potential of 2 reported half a century ago could not be confirmed in this work, although several reports over the last 60 years described the antibacterial activity of 1 , 2 , and 4 against S. aureus . ,, 2 was the only compound inhibiting S. aureus , with an IC 50 of 32 μM, which is lower than that previously reported . These discrepancies may stem from the use of different test systems and incompletely solubilized samples in biological assays.…”

Section: Resultscontrasting

confidence: 78%

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Potential of Lichen Secondary Metabolites against Plasmodium Liver Stage Parasites with FAS-II as the Potential Target

et al. 2013

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Chemicals targeting the liver stage (LS) of the malaria parasite are useful for causal prophylaxis of malaria. In this study, four lichen metabolites, evernic acid (1), vulpic acid (2), psoromic acid (3) and (+)-usnic acid (4) were evaluated against LS parasites of Plasmodium berghei. Inhibition of P. falciparum blood stage (BS) parasites was also assessed to determine stage specificity. Compound 4 displayed the highest LS activity and stage specificity (LS IC50 value 2.3 μM, BS IC50 value 47.3 μM). The compounds 1-3 inhibited one or more enzymes (PfFabI, PfFabG and PfFabZ) from the plasmodial fatty acid biosynthesis (FAS-II) pathway, a potential drug target for LS activity. To determine species specificity and to clarify the mechanism of reported antibacterial effects, 1-4 were also evaluated against FabI homologues and whole cells of various pathogens (S. aureus, E. coli, M. tuberculosis). Molecular modelling studies suggest that lichen acids act indirectly via binding to allosteric sites on the protein surface of the FAS-II enzymes. Potential toxicity of compounds was assessed in human hepatocyte and cancer cells (in vitro) as well as in a zebrafish model (in vivo). This study indicates the therapeutic and prophylactic potential of lichen metabolites as antibacterial and antiplasmodial agents.

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