Elofsson, Mikael

Genina, Natalja

Gylfe, Åsa

Hanski, Leena

Hirvonen, Jouni

Kolakovic, Ruzica

Laaksonen, Timo

Malinovskaja, Kristina

Mäkilä, Ermei

Salonen, Jarno

Sandler, Niklas

Uvell, Hanna

Vuorela, Pia M.

PLoS ONE

PubMed

Given the established role of Chlamydia spp. as causative agents of both acute and chronic diseases, search for new antimicrobial agents against these intracellular bacteria is required to promote human health. Isoflavones are naturally occurring phytoestrogens, antioxidants and efflux pump inhibitors, but their therapeutic use is limited by poor water-solubility and intense first-pass metabolism. Here, we report on effects of isoflavones against C. pneumoniae and C. trachomatis and describe buccal permeability and initial formulation development for biochanin A. Biochanin A was the most potent Chlamydia growth inhibitor among the studied isoflavones, with an IC50 = 12 µM on C. pneumoniae inclusion counts and 6.5 µM on infectious progeny production, both determined by immunofluorescent staining of infected epithelial cell cultures. Encouraged by the permeation of biochanin A across porcine buccal mucosa without detectable metabolism, oromucosal film formulations were designed and prepared by a solvent casting method. The film formulations showed improved dissolution rate of biochanin A compared to powder or a physical mixture, presumably due to the solubilizing effect of hydrophilic additives and presence of biochanin A in amorphous state. In summary, biochanin A is a potent inhibitor of Chlamydia spp., and the in vitro dissolution results support the use of a buccal formulation to potentially improve its bioavailability in antichlamydial or other pharmaceutical applications

Leena Hanski

Natalja Genina

Hanna Uvell

Kristina Malinovskaja

Åsa Gylfe

Timo Laaksonen

Ruzica Kolakovic

Ermei Mäkilä

Jarno Salonen

Jouni Hirvonen

Mikael Elofsson

Niklas Sandler

Pia M Vuorela

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Inhibitory activity of the isoflavone biochanin A on intracellular bacteria of genus Chlamydia and initial development of a buccal formulation.

Given the established role of Chlamydia spp. as causative agents of both acute and chronic diseases, search for new antimicrobial agents against these intracellular bacteria is required to promote human health. Isoflavones are naturally occurring phytoestrogens, antioxidants and efflux pump inhibitors, but their therapeutic use is limited by poor water-solubility and intense first-pass metabolism. Here, we report on effects of isoflavones against C. pneumoniae and C. trachomatis and describe buccal permeability and initial formulation development for biochanin A. Biochanin A was the most potent Chlamydia growth inhibitor among the studied isoflavones, ;with an IC50=12 mu M on C. pneumoniae inclusion counts and 6.5 mu M on infectious progeny production, both determined by immunofluorescent staining of infected epithelial cell cultures. Encouraged by the permeation of biochanin A across porcine buccal mucosa without detectable metabolism, oromucosal film formulations were designed and prepared by a solvent casting method. The film formulations showed improved dissolution rate of biochanin A compared to powder or a physical mixture, presumably due to the solubilizing effect of hydrophilic additives and presence of biochanin A in amorphous state. In summary, biochanin A is a potent inhibitor of Chlamydia spp., and the in vitro dissolution results support the use of a buccal formulation to potentially improve its bioavailability in antichlamydial or other pharmaceutical applications

Gylfe, Asa

Makila, Ermei

Publikationer från Umeå universitet

Inhibitory Activity of the Isoflavone Biochanin A on Intracellular Bacteria of Genus Chlamydia and Initial Development of a Buccal Formulation

Digitala Vetenskapliga Arkivet - Academic Archive On-line

Vuorela, Pia M

Copenhagen University Research Information System

Inhibitory activity of the isoflavone biochanin a on intracellular bacteria of genus Chlamydia and initial development of a buccal formulation.

<div>Given the established role of Chlamydia spp. as causative agents of both acute and chronic diseases, search for new antimicrobial agents against these intracellular bacteria is required to promote human health. Isoflavones are naturally occurring phytoestrogens, antioxidants and efflux pump inhibitors, but their therapeutic use is limited by poor water-solubility and intense first-pass metabolism. Here, we report on effects of isoflavones against C. pneumoniae and C. trachomatis and describe buccal permeability and initial formulation development for biochanin A. Biochanin A was the most potent Chlamydia growth inhibitor among the studied isoflavones, with an IC50 = 12 µM on C. pneumoniae inclusion counts and 6.5 µM on infectious progeny production, both determined by immunofluorescent staining of infected epithelial cell cultures. Encouraged by the permeation of biochanin A across porcine buccal mucosa without detectable metabolism, oromucosal film formulations were designed and prepared by a solvent casting method. The film formulations showed improved dissolution rate of biochanin A compared to powder or a physical mixture, presumably due to the solubilizing effect of hydrophilic additives and presence of biochanin A in amorphous state. In summary, biochanin A is a potent inhibitor of Chlamydia spp., and the in vitro dissolution results support the use of a buccal formulation to potentially improve its bioavailability in antichlamydial or other pharmaceutical applications.</div

Leena Hanski (675511)

Natalja Genina (675512)

Hanna Uvell (449402)

Kristina Malinovskaja (675513)

Åsa Gylfe (675514)

Timo Laaksonen (675515)

Ruzica Kolakovic (675516)

Ermei Mäkilä (675517)

Jarno Salonen (675518)

Jouni Hirvonen (675519)

Mikael Elofsson (182229)

Niklas Sandler (675520)

Pia M. Vuorela (494458)

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Inhibitory Activity of the Isoflavone Biochanin A on Intracellular Bacteria of Genus Chlamydia and Initial Development of a Buccal Formulation

Pia M. Vuorela

Crossref

Helsingin yliopiston digitaalinen arkisto

Inhibitory activity of the isoflavone Biochanin A on intracellular bacteria of genus Chlamydia and initial development of a buccal formulation

Academic Archive On-line (Umeå University, Sweden)

http://dx.doi.org/10.1371/journal.pone.0115115

Inhibitory activity of the isoflavone Biochanin A on intracellular bacteria of genus Chlamydia and initial development of a buccal formulation

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