期刊
PHOTODIAGNOSIS AND PHOTODYNAMIC THERAPY
卷 20, 期 -, 页码 263-272出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.pdpdt.2017.10.023
关键词
Oropharyngeal candidiasis; Photodynamic therapy; Candida; Porophyllum obscurant; Tiophenes; Composition activity correlation
类别
资金
- Agencia Nacional de Promocion Cientifica y Tecnologica de Argentina (ANPCyT) [PICT 0608/2010]
- Consejo Nacional de Investigaciones Cientificas y Tecnicas (CONICET) [1170/2014, PIP 112-201201 00444 CO]
- National University of Rosario [BIO 1BIO381]
- ANPCyT
- CONICET
We report Porophyllum obscurum as a source of new photosensitizers with potential use in Photodynamic Therapy as an alternative for oropharyngeal candidiasis treatment. The antifungal photosensitive activity of different extracts from P. obscurum was evaluated by using microdilution and bioautographic assays. The Minimum Fungicidal Concentration for hexanic extract under UV-A irradiation was 0.98 mu g/mL, but it was inactive in experiments without irradiation. The bioassay-guided fractionation of this extract led to the isolation of four thiophenes responsible for the photosensitive activity: 2,2':5'2 '' terthiophene, 5-(3-buten-1-ynyl)-2,2'-bithiophene, 5-(4-acetoxy-1-butenyl)-2,2'- bithiophene and 5-(4-hydroxy-1-butenyl)-2,2'- bithiophene, with Minimum Fungicidal Concentrations ranging 0.24-7.81 mu g/mL under UV-A irradiation. The activity of the hexanic extract was evaluated against 25 clinical strains of Candida spp. isolates as etiological agents of oropharyngeal candidiasis. No differences in susceptibility were observed in strains resistant and susceptible to conventional anti fungal drugs. Qualitative and quantitative chemical analyses of seven samples of P. obscurum collected in four different phenological stages were carried out showing that full flowering stage possesses the highest thiophenes content. These data also allowed us to establish a correlation between the thiophene composition of the different extracts and their antifungal photosensitive activity, according to a second order polynomial model with the equation: y = 11.2603-0.6831*x + 0.0108*x(2). The thiophenes isolated were the responsible of antifungal photosensitive activity and can be used for the future standardization of the extract. Results showed that P. obscurum hexanic extract could be potentially developed as an Herbal Medicinal Product to be applied as a photosensitizer in Photodynamic Therapy.
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