In Vitro and In Vivo Antibacterial Activities of the Tricyclic Ketolide TE-802 and Its Analogs

Ono, Takeo; Kashimura, Masato; Suzuki, Keiko; Oyauchi, Rika; Miyachi, Junko; Ikuta, Hiroshi; Kawauchi, Hiroyuki; Akashi, Toshi; Asaka, Toshifumi; Morimoto, Shigeo

doi:10.7164/antibiotics.57.518

Cited by 22 publications

(9 citation statements)

References 6 publications

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“…The macrocyclic templates we have chosen were derived from the medically successful antibiotics azithromycin (AZ) and clarithromycin (CL) (Figure 11), as well as a triketolide (TE-802) that has demonstrated superior efficacy in mice model of respiratory tract infection [35,131,132]. Our choice of these macrocyclic compounds was informed by their extraordinary tissue distribution profiles in data presented to the FDA and subsequently confirmed by various independent laboratories [133,134].…”

Section: Targeting Cap Groups For Tissue–cell-selective Drug Accumulamentioning

confidence: 99%

Targeted Cancer Therapy: Giving Histone Deacetylase Inhibitors All They Need To Succeed

2012

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Histone deacetylase inhibitors (HDACis) have now emerged as a powerful new class of small-molecule therapeutics acting through the regulation of the acetylation states of histone proteins (a form of epigenetic modulation) and other non-histone protein targets. Over 490 clinical trials have been initiated in the last 10 years, culminating in the approval of two structurally distinct HDACis – SAHA (vorinostat, Zolinza™) and FK228 (romidepsin, Istodax™). However, the current HDACis have serious limitations, including ineffectively low concentrations in solid tumors and cardiac toxicity, which is hindering their progress in the clinic. Herein, we review the primary paradigms being pursued to overcome these hindrances, including HDAC isoform selectivity, localized administration, and targeting cap groups to achieve selective tissue and cell type distribution.

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Section: Targeting Cap Groups For Tissue–cell-selective Drug Accumulamentioning

confidence: 99%

Targeted Cancer Therapy: Giving Histone Deacetylase Inhibitors All They Need To Succeed

2012

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“…The differences in susceptibility may be explained by the differences in cell wall composition and/or in genetic content of plasmids that can be easily transferred among microbial strains (Karaman et al 2003). It may also be explained by differences in the mechanism by which the active principles of the plant extracts exert their effect (Takeo et al 2004). It was also observed that the ratios MBC/MIC found for the tested substances were generally less than or equal to 4 (Table 2), on the corresponding microbial species, suggesting that the killing effects of the extract/fractions could be expected on most of the tested micro-organisms (Tene et al 2008; Tamokou et al 2009).…”

Section: Resultsmentioning

confidence: 99%

Phytochemical analysis, antimicrobial and radical-scavenging properties of Acalypha manniana leaves

et al. 2013

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Acalypha manniana (Euphorbiaceae) is a plant popularly used in Cameroon and in several parts of Africa for the treatment of various microbial diseases like diarrhea and skin infections.The present study was designed to evaluate the phytochemical composition, antimicrobial and radical-scavenging activities of A. manniana methanol leaf extract and its fractions.The methanol extract was partitioned into hexane, ethyl acetate and residual fractions and phytochemical analysis was conducted using standard methods. The broth microdilution method was used to evaluate the antimicrobial activity against nine bacterial species and four dermatophyte species. The free radical scavenging activities of the methanol extract and its fractions were evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay.The results obtained showed that A. manniana contains alkaloids, tannins, anthocyanins, flavonoids, phenols and steroids. The methanol extract as well as the hexane, ethyl acetate and residual fractions exhibited both antibacterial and antidermatophytic activities that varied between the microbial species (MIC = 0.12 – 2.04 mg/mL). These tested samples also showed high radical-scavenging activities (RaS50 = 3.34 – 4.80 μg/mL) when compared with vitamin C used as reference antioxidant (RaS50 = 1.74 μg/mL).These findings provide evidence that the studied plant possesses antimicrobial and antioxidant properties and may act as potential antioxidant for biological systems susceptible to free radical-mediated reactions.

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“…Several compounds from the investigated classes of phytochemicals were reported for their antibacterial activities [50,51], and their presence in the tested extracts could explain their antibacterial effects. The differences in bacterial susceptibility to the extracts may be either due to the differences in cell wall composition and/or genetic content of their plasmids [52] or to the differences in the composition and the mechanism of action of the bioactive compounds [53]. As shown in Table 3, the three most active plants ( P. nigrum, T. occidentalis and V. amygdalina ) possess more classes of phytochemicals than the extract from S. aromaticum .…”

Section: Discussionmentioning

confidence: 99%

In Vitro antibacterial and antibiotic-potentiation activities of four edible plants against multidrug-resistant gram-negative species

Noumedem

Mihășan

Kuiaté

et al. 2013

BMC Complement Altern Med

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BackgroundThe present study was designed to investigate the antibacterial activities of the methanol extracts of four Cameroonian edible plants, locally used to treat microbial infections, and their synergistic effects with antibiotics against a panel of twenty nine Gram-negative bacteria including Multi-drug resistant (MDR) phenotypes expressing active efflux pumps.MethodsThe broth microdilution method was used to determine the minimum inhibitory concentrations (MICs) of the extracts [alone and in the presence of the efflux pumps inhibitor (EPI) Phenylalanine-Arginine β-Naphtylamide (PAβN)], and those of antibiotics in association with the two of the most active ones, Piper nigrum and Telfairia occidentalis. The preliminary phytochemical screening of the extracts was conducted according to the standard phytochemical methods.ResultsPhytochemical analysis showed the presence of alkaloids and flavonoids in all studied extracts. Other chemical classes of secondary metabolites were selectively present in the extracts. The results of the MIC determination indicated that the crude extracts from P. nigrum and V. amygdalina were able to inhibit the growth of all the twenty nine studied bacteria within a concentration range of 32 to 1024 μg/mL. At a similar concentration range (32 to 1024 μg/mL) the extract from T. occidentalis inhibited the growth of 93.1% of the tested microorganisms. At MIC/2 and MIC/5, synergistic effects were noted between the extracts from P. nigrum and T. occidentalis and seven of the tested antibiotics on more than 70% of the tested bacteria.ConclusionThe overall results of the present study provide information for the possible use of the studied edible plants extracts in the control of bacterial infections including MDR phenotypes.

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In Vitro and In Vivo Antibacterial Activities of the Tricyclic Ketolide TE-802 and Its Analogs

Cited by 22 publications

References 6 publications

Targeted Cancer Therapy: Giving Histone Deacetylase Inhibitors All They Need To Succeed

Targeted Cancer Therapy: Giving Histone Deacetylase Inhibitors All They Need To Succeed

Phytochemical analysis, antimicrobial and radical-scavenging properties of Acalypha manniana leaves

In Vitro antibacterial and antibiotic-potentiation activities of four edible plants against multidrug-resistant gram-negative species

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