title: Carboranyl-Chlorin e6 as a Potent Antimicrobial Photosensitizer.
abstract: Antimicrobial photodynamic inactivation is currently being widely considered as alternative to antibiotic chemotherapy of infective diseases, attracting much attention to design of novel effective photosensitizers. Carboranyl-chlorin-e6 (the conjugate of chlorin e6 with carborane), applied here for the first time for antimicrobial photodynamic inactivation, appeared to be much stronger than chlorin e6 against Gram-positive bacteria, such as Bacillus subtilis, Staphyllococcus aureus and Mycobacterium sp. Confocal fluorescence spectroscopy and membrane leakage experiments indicated that bacteria cell death upon photodynamic treatment with carboranyl-chlorin-e6 is caused by loss of cell membrane integrity. The enhanced photobactericidal activity was attributed to the increased accumulation of the conjugate by bacterial cells, as evaluated both by centrifugation and fluorescence correlation spectroscopy. Gram-negative bacteria were rather resistant to antimicrobial photodynamic inactivation mediated by carboranyl-chlorin-e6. Unlike chlorin e6, the conjugate showed higher (compared to the wild-type strain) dark toxicity with Escherichia coli ΔtolC mutant, deficient in TolC-requiring multidrug efflux transporters.
authors.affiliation: Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: Elena O
authors.initials: EO
authors.lastname: Omarova
authors.affiliation: Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: Pavel A
authors.initials: PA
authors.lastname: Nazarov
authors.affiliation: Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: Alexander M
authors.initials: AM
authors.lastname: Firsov
authors.affiliation: Biological Department, Lomonosov Moscow State University, Moscow, Russia.|Federal Scientific and Clinical Center for Specialized Medical Service and Medical Technologies, FMBA, Moscow, Russia.
authors.forename: Marina G
authors.initials: MG
authors.lastname: Strakhovskaya
authors.affiliation: Biological Department, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: Anastasia Yu
authors.initials: AY
authors.lastname: Arkhipova
authors.affiliation: Biological Department, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: Mikhail M
authors.initials: MM
authors.lastname: Moisenovich
authors.affiliation: Biological Department, Lomonosov Moscow State University, Moscow, Russia.|Shumakov Research Center of Transplantology and Artificial Organs, Moscow, Russia.
authors.forename: Igor I
authors.initials: II
authors.lastname: Agapov
authors.affiliation: Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Moscow, Russia.
authors.forename: Valentina A
authors.initials: VA
authors.lastname: Ol'shevskaya
authors.affiliation: Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Moscow, Russia.
authors.forename: Andrey V
authors.initials: AV
authors.lastname: Zaitsev
authors.affiliation: Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Moscow, Russia.
authors.forename: Valery N
authors.initials: VN
authors.lastname: Kalinin
authors.affiliation: Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: Elena A
authors.initials: EA
authors.lastname: Kotova
authors.affiliation: Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: Yuri N
authors.initials: YN
authors.lastname: Antonenko
mesh_terms: D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology*; D001425:Bacterial Outer Membrane Proteins / Q000235:genetics / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism*; D002735:Chlorophyllides; D004926:Escherichia coli / Q000378:metabolism; D029968:Escherichia coli Proteins / Q000235:genetics / Q000378:metabolism; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008081:Liposomes / Q000378:metabolism; D026901:Membrane Transport Proteins / Q000235:genetics / Q000378:metabolism; D017319:Photosensitizing Agents / Q000737:chemistry / Q000494:pharmacology*; D011166:Porphyrins / Q000737:chemistry / Q000494:pharmacology*; D013050:Spectrometry, Fluorescence
chemical_list: D000890:Anti-Infective Agents; D001425:Bacterial Outer Membrane Proteins; D002735:Chlorophyllides; D029968:Escherichia coli Proteins; D008081:Liposomes; D026901:Membrane Transport Proteins; D017319:Photosensitizing Agents; D011166:Porphyrins; C073126:tolC protein, E coli; C062985:phytochlorin