Núcleo de Investigações Químico-Farmacêuticas (Niqfar), Program of Post-Graduation in Pharmaceutical Sciences, Universidade do Vale do Itajaí (UNIVALI), Caixa postal 360, CEP 88302-202 Itajaí, SC, Brazil.
Department of Pharmaceutical Sciences, Universidade Federal de Santa Catarina, Campus Universitário - Trindade, Florianópolis 88040-900, SC, Brazil.
Talanta. 2017 May 15;167:302-309. doi: 10.1016/j.talanta.2017.02.024. Epub 2017 Feb 10.
As the temperature of extraction and processing could impact the biological effects of herbal extracts, which have wide chemical diversity, the aim of this work were to investigate the thermostability of herbal derivatives of the aerial parts of Sphagneticola trilobata, a reputed medicinal plant; to biomonitor its oral anti-hyperalgesic effect; and to elucidate the degradation pathways of the major components by UHPLC-ESI-QTOF-MS. The lipophilic markers (kaurenoic acid-KA) and hydrophilic markers [chlorogenic acids; measured as total phenolic compounds (PC), expressed in caffeic acid] were also monitored through a validated HPLC-UV methodology, suitable for quality control and stability studies. The soft extract (drug:solvent ratio of 1:10, ethanol 60% v/v) was exposed to high temperatures (50-180°C). PC showed high thermolability (27.4% of degradation at 150°C), compared to KA (16.5%, at 180°C). These results suggest that the loss of oral anti-hyperalgesic activity observed in the spray-dried extracts (dried at 170°C), compared with the soft and the lyophilized extract may be related to degradation of the active components, especially the polar compounds, i.e. chlorogenic acid derivatives and the four oleanane type triterpenoid saponins. These latter degraded at temperatures above 150°C and vanished at 180°C, as demonstrated in the UHPLC-ESI-QTOF-MS analyses. These results provide a relevant guide for the extraction process of S. trilobata, aimed at preserving the antinociceptive effect.
由于提取和加工温度会影响植物提取物的生物效应,而植物提取物具有广泛的化学多样性,因此本研究旨在考察裂叶荆芥地上部分的草药衍生物的热稳定性,裂叶荆芥是一种公认的药用植物;通过生物监测其口服抗痛觉过敏作用;并通过 UHPLC-ESI-QTOF-MS 阐明主要成分的降解途径。还通过验证的 HPLC-UV 方法监测亲脂性标志物(贝壳杉烯酸-KA)和亲水性标志物[绿原酸;以咖啡酸表示的总酚类化合物(PC)],该方法适用于质量控制和稳定性研究。软提取物(药物:溶剂比为 1:10,60%乙醇 v/v)暴露于高温(50-180°C)下。与 KA(180°C 时 16.5%)相比,PC 的热不稳定性更高(150°C 时降解 27.4%)。这些结果表明,与软提取物和冻干提取物相比,喷雾干燥提取物(在 170°C 下干燥)中观察到的口服抗痛觉过敏活性丧失可能与活性成分的降解有关,特别是极性化合物,即绿原酸衍生物和四种齐墩果酸型三萜皂苷。这些化合物在 150°C 以上的温度下降解,并在 180°C 时消失,这在 UHPLC-ESI-QTOF-MS 分析中得到证实。这些结果为裂叶荆芥的提取过程提供了重要指导,旨在保留其镇痛作用。