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@article{1726800,
author = {Sychrová, Alice and Nesuta, O. and Vancatova, I. and Cizek, A. and Varela, R.E. and LopezandAban, J. and VillaandPulgarin, J.A. and Mollinedo, F. and Muro, A. and Zemlickova, H and Kadlecova, D. and Šmejkal, Karel},
article_location = {NETHERLANDS},
article_number = {8},
doi = {http://dx.doi.org/10.3109/13880209.2015.1103755},
keywords = {Flavonoid; geranyl; Leishmania; MRSA; synergy},
language = {eng},
issn = {1388-0209},
journal = {Pharmaceutical Biology},
title = {C-Geranylated flavonoids from Paulownia tomentosa fruits with antimicrobial potential and synergistic activity with antibiotics},
volume = {54},
year = {2016}
}
TY - JOUR
ID - 1726800
AU - Sychrová, Alice - Nesuta, O. - Vancatova, I. - Cizek, A. - Varela, R.E. - Lopez-Aban, J. - Villa-Pulgarin, J.A. - Mollinedo, F. - Muro, A. - Zemlickova, H - Kadlecova, D. - Šmejkal, Karel
PY - 2016
TI - C-Geranylated flavonoids from Paulownia tomentosa fruits with antimicrobial potential and synergistic activity with antibiotics
JF - Pharmaceutical Biology
VL - 54
IS - 8
SP - 1398-1407
EP - 1398-1407
PB - TAYLOR & FRANCIS INC
SN - 13880209
KW - Flavonoid
KW - geranyl
KW - Leishmania
KW - MRSA
KW - synergy
N2 - Context C-6-Geranylated flavonoids possess promising biological activities. These substances could be a source of lead compounds for the development of therapeutics.Objective The study was designed to evaluate their antibacterial and antileishmanial activity.Materials and methods C-6-Geranylated flavanones were tested in micromolar concentrations against promastigote forms of Leishmaniabrazilensis, L. donovani, L. infantum, and L. panamensis against methicillin-resistant Staphylococcus aureus (MRSA); and synergistic potential with antibiotics was analyzed. IC50 values (after 72h) were calculated and compared with that of miltefosine. Flow cytometry and DNA fragmentation analysis were used the mechanism of the effect. Geranylated flavanones or epigallocatechin gallate were combined with oxacillin, tetracycline, and ciprofloxacin, and the effects of these two-component combinations were evaluated. Minimal inhibitory concentrations (MICs) and minimal bactericidal concentrations (MBCs) were established (after 24h), the synergy was measured by the checkerboard titration technique, and the sums of the fractional inhibitory concentrations (Sigma FICs) were computed.Results 3-O-Methyl-5-O-methyldiplacone and 3-O-methyldiplacone showed good antileishmanial activities (IC50 8-42M). 3-O-Methyl-5-hydroxydiplacone activates the apoptotic death at leishmanias, the effect of 3-O-methyl-5-O-methyldiplacone has another mechanism. The test of the antibacterial activity showed good effects of 3-O-methyldiplacol and mimulone against MRSA (MIC 2-16g/mL), and in six cases, the results showed synergistic effects when combined with oxacillin. Synergistic effects were also found for the combination of epigallocatechin gallate with tetracycline or oxacillin.Conclusion This work demonstrates anti-MRSA and antileishmanial potential of geranylated flavanones and uncovers their promising synergistic activities with antibiotics. In addition, the mechanism of antileishmanial effect is proposed.
ER -
SYCHROVÁ, Alice, O. NESUTA, I. VANCATOVA, A. CIZEK, R.E. VARELA, J. LOPEZ-ABAN, J.A. VILLA-PULGARIN, F. MOLLINEDO, A. MURO, H ZEMLICKOVA, D. KADLECOVA a Karel ŠMEJKAL. C-Geranylated flavonoids from Paulownia tomentosa fruits with antimicrobial potential and synergistic activity with antibiotics. \textit{Pharmaceutical Biology}. NETHERLANDS: TAYLOR \&{} FRANCIS INC, 2016, roč.~54, č.~8, s.~1398-1407. ISSN~1388-0209. Dostupné z: https://dx.doi.org/10.3109/13880209.2015.1103755.
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