Pérez-García F, Marín E, Parella T, Adzet T, Cañigueral S
Unitat de Farmacologia i Farmacognòsia, Facultat de Farmàcia, Universitat de Barcelona, Av. Diagonal, 643, E-08028 Barcelona, Spain.
Phytomedicine. 2005 Apr;12(4):278-84. doi: 10.1016/j.phymed.2004.03.008.
Pluchea sagittalis whole plant dichloromethane extract showed inhibitory activity in several inflammatory models: rat hind paw-edema, mice ear edema, and air-pouch rat granuloma. The extract inhibited the production of reactive oxygen species (ROS) and reactive nitrogen species (RNS) in stimulated human neutrophils. It also showed inhibitory effect on heat shock protein 72 (hsp72) synthesis in stimulated neutrophils, while it had opposite effects on unstimulated cells. The triterpene taraxasteryl acetate was obtained from the dichloromethane extract by bioassay directed isolation, being active against induced ROS and RNS production in human neutrophils. In mice ear edema (induced by phorbol-12-mirystate-13-acetate, croton oil and arachidonic acid), taraxasteryl acetate showed a topical anti-inflammatory activity similar to the extract, but at 1/20 of the dose. The same ratio was observed for the inhibition of hsp72 production in stimulated human neutrophils. In unstimulated monocytes and neutrophils, taraxasteryl acetate showed a higher stimulating activity of hsp72 production than the extract, involving different mechanisms in each cell type. To our knowledge, taraxasteryl acetate is the first natural product for which a dual effect on the hsp response is reported.
大鼠后爪水肿、小鼠耳水肿和大鼠气囊肉芽肿。该提取物抑制了受刺激的人中性粒细胞中活性氧（ROS）和活性氮（RNS）的产生。它还对受刺激的中性粒细胞中热休克蛋白72（hsp72）的合成显示出抑制作用，而对未受刺激的细胞则有相反的作用。通过生物活性导向分离从二氯甲烷提取物中获得了三萜类化合物乙酸蒲公英甾醇酯，其对人中性粒细胞中诱导的ROS和RNS产生具有活性。在小鼠耳水肿（由佛波醇-12-肉豆蔻酸酯-13-乙酸酯、巴豆油和花生四烯酸诱导）模型中，乙酸蒲公英甾醇酯显示出与提取物相似的局部抗炎活性，但剂量仅为提取物的1/20。在抑制受刺激的人中性粒细胞中hsp72产生方面也观察到相同的比例。在未受刺激的单核细胞和中性粒细胞中，乙酸蒲公英甾醇酯显示出比提取物更高的hsp72产生刺激活性，且在每种细胞类型中涉及不同的机制。据我们所知，乙酸蒲公英甾醇酯是首个被报道对hsp反应具有双重作用的天然产物。
