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首页> 外文期刊>Photodiagnosis and Photodynamic Therapy >Antifungal photosensitive activity of Porophyllum obscurum (Spreng.) DC.: Correlation of the chemical composition of the hexane extract with the bioactivity
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Antifungal photosensitive activity of Porophyllum obscurum (Spreng.) DC.: Correlation of the chemical composition of the hexane extract with the bioactivity

机译：鬼臼根（Porophyllum obscurum，DC）的抗真菌光敏活性：己烷提取物的化学组成与生物活性的相关性

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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.
机译：我们报告黑鬼臼作为新型光敏剂的来源，具有潜在的光动力疗法潜力，可作为口咽念珠菌病的替代疗法。通过使用微稀释和生物自显影试验评估了暗黑假单胞菌不同提取物的抗真菌光敏活性。 UV-A照射下己酮提取物的最小杀真菌浓度为0.98μg / mL，但在未经照射的实验中无活性。该提取物的生物测定指导分馏导致分离出四种负责光敏活性的噻吩：2,2'：5'2''对噻吩，5-（3-丁烯-1-炔基）-2,2'-联噻吩，5-（4-乙酰氧基-1-丁烯基）-2,2'-联噻吩和5-（4-羟基-1-丁烯基）-2,2'-联噻吩，最小杀真菌浓度为0.24-7.81微克/ mL在UV-A照射下。针对25种念珠菌临床菌株评估了己酸提取物的活性。分离物作为口咽念珠菌病的病原体。在对常规抗真菌药物具有抗药性和敏感性的菌株中未观察到敏感性差异。对在四个不同物候期收集到的七个黑曜石样品进行了定性和定量化学分析，结果表明完全开花期噻吩含量最高。根据二阶多项式模型，这些数据还使我们能够建立不同提取物的噻吩成分与其抗真菌光敏活性之间的相关性：y = 11.2603-0.6831 * x + 0.0108 * x（2）。分离出的噻吩是抗真菌光敏活性的原因，可用于提取物的未来标准化。结果表明，暗黑假单胞菌己酸提取物有可能被开发为一种草药，并将其用作光动力疗法中的光敏剂。

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