Brown A M, Edwards C M, Davey M R, Power J B, Lowe K C
Department of Life Science, University of Nottingham, University Park, UK.
J Pharm Pharmacol. 1997 May;49(5):558-61. doi: 10.1111/j.2042-7158.1997.tb06841.x.
The bioactivity of feverfew (Tanacetum parthenium) leaf extracts has been analysed, by use of a human polymorphonuclear leukocyte (PMNL) bioassay, to assess the relative contributions of solvent extraction and parthenolide content to the biological potency of the extract. Extracts prepared in acetone-ethanol (system 1) contained significantly more parthenolide (mean +/- s.d. 1.3 +/- 0.2% dry leaf weight) than extracts in chloroform-PBS (phosphate-buffered saline; system 2; 0.1 +/- 0.04% dry leaf weight) or PBS alone (system 3; 0.5 +/- 0.1% dry leaf weight). Extract bioactivity, measured as inhibition of phorbol 12-myristate 13-acetate-induced, 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol)-enhanced PMNL, chemiluminescence, followed a similar trend. Extracts inhibited phorbol 12-myristate 13-acetate-induced oxidative burst by amounts which, if solely attributable to parthenolide, indicated parthenolide concentrations for the respective solvent systems of 2.2 +/- 0.6%, 0.2 +/- 0.1% and 0.9 +/- 0.1% dry leaf weight. The mean ratio of parthenolide concentration to the parthenolide equivalent/PMNL-bioactivity value, for acetone-ethanol and PBS extracts were both 1:1.7. Parthenolide, although a key determinant of biological activity for T. parthenium leaf extracts based on the PMNL-bioassay, seems not to be the sole pharmacologically-active constituent. The identical and elevated bioactivity-parthenolide ratios for both organic and aqueons-phase leaf extracts suggest that a proportion of the other bioactive compounds have solubilities similar to that of parthenolide.
通过使用人多形核白细胞（PMNL）生物测定法，分析了小白菊（Tanacetum parthenium）叶提取物的生物活性，以评估溶剂萃取和小白菊内酯含量对提取物生物效力的相对贡献。丙酮 - 乙醇体系（体系1）制备的提取物中所含小白菊内酯（平均±标准差，1.3±0.2%干叶重）显著多于氯仿 - PBS（磷酸盐缓冲盐水；体系2；0.1±0.04%干叶重）或单独的PBS（体系3；0.5±0.1%干叶重）制备的提取物。以佛波醇12 - 肉豆蔻酸酯13 - 乙酸酯诱导的、5 - 氨基 - 2,3 - 二氢 - 1,4 - 酞嗪二酮（鲁米诺）增强的PMNL化学发光抑制作用来衡量，提取物的生物活性呈现类似趋势。提取物抑制佛波醇12 - 肉豆蔻酸酯13 - 乙酸酯诱导的氧化爆发的量，如果仅归因于小白菊内酯，则表明各溶剂体系中，小白菊内酯浓度分别为2.2±0.6%、0.2±0.1%和0.9±0.1%干叶重。丙酮 - 乙醇提取物和PBS提取物中，小白菊内酯浓度与小白菊内酯当量/PMNL生物活性值的平均比值均为1:1.7。基于PMNL生物测定法，小白菊内酯虽然是小白菊叶提取物生物活性的关键决定因素，但似乎不是唯一的药理活性成分。有机相和水相叶提取物相同且升高的生物活性 - 小白菊内酯比值表明，其他一些生物活性化合物的溶解度与小白菊内酯相似。
