C-Geranylated flavonoids from Paulownia tomentosa fruits with antimicrobial potential and synergistic activity with antibiotics

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F16%3A00463702" target="_blank" >RIV/61388963:_____/16:00463702 - isvavai.cz</a>

Alternative codes found

RIV/62157124:16170/16:43874123 RIV/62157124:16370/16:43874123 RIV/62157124:16810/16:43874123 RIV/75010330:_____/16:00011406

Result on the web

<a href="http://dx.doi.org/10.3109/13880209.2015.1103755" target="_blank" >http://dx.doi.org/10.3109/13880209.2015.1103755</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3109/13880209.2015.1103755" target="_blank" >10.3109/13880209.2015.1103755</a>

Result language

angličtina

Original language name

C-Geranylated flavonoids from Paulownia tomentosa fruits with antimicrobial potential and synergistic activity with antibiotics

Original language description

C-6-Geranylated flavonoids possess promising biological activities. These substances could be a source of lead compounds for the development of therapeutics. The study was designed to evaluate their antibacterial and antileishmanial activity. 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. 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. 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.

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

FR - Pharmacology and apothecary chemistry

OECD FORD branch

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Project

<a href="/en/project/ED1.1.00%2F02.0068" target="_blank" >ED1.1.00/02.0068: Central european institute of technology</a><br>

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2016

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Pharmaceutical Biology

ISSN

1388-0209

e-ISSN

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Volume of the periodical

54

Issue of the periodical within the volume

8

Country of publishing house

GB - UNITED KINGDOM

Number of pages

10

Pages from-to

1398-1407

UT code for WoS article

000381024800011

EID of the result in the Scopus database

2-s2.0-84955119969