Feltenstein M W, Schühly W, Warnick J E, Fischer N H, Sufka K J
Department of Psychology, University of Mississippi, University, MS 38677, USA.
Pharmacol Biochem Behav. 2004 Oct;79(2):299-302. doi: 10.1016/j.pbb.2004.08.008.
Sesquiterpene lactones possess a variety of biological activities, including anti-inflammatory activity. Two plants native to the southeastern United States, Magnolia grandiflora (L.) and Smallanthus uvedalius (L.) [syn Polymnia uvedalius (L.)], are novel sources of the sesquiterpene lactones parthenolide and enhydrin, respectively. In this study, the anti-inflammatory and anti-hyperalgesic effects of these isolated lactones from these two plant sources were evaluated in the rat carrageenan inflammation model. Rats received ip injections of either vehicle (propylene glycol), indomethacin (5 mg/kg), 11,13-dihydroparthenolide (20 mg/kg), parthenolide (5 or 20 mg/kg) or enhydrin (5 or 20 mg/kg). A 100-microl injection of 2.0% carrageenan was made into the plantar surface of the right hindpaw. Paw withdrawal latencies and paw volumes in both inflamed and non-inflamed paws were recorded at four test intervals: pre-inflammation baseline (0 time point), and 1, 2 and 4 h post-carrageenan injection. Vehicle-treated animals exhibited a significant time-dependent hyperalgesic and edema response that was greatest at the 4-h test interval. Indomethacin significantly blocked the hyperalgesic response and modestly attenuated the edema response. Parthenolide (20 mg/kg) and enhydrin (20 mg/kg) significantly blocked the hyperalgesic response and significantly attenuated the edema response; 11,13-dihydroparthenolide did not affect either inflammation or hyperalgesia. These findings suggest that parthenolide and enhydrin from these plant sources may be useful in the treatment of inflammatory pain.
倍半萜内酯具有多种生物活性,包括抗炎活性。原产于美国东南部的两种植物,即荷花玉兰(Magnolia grandiflora (L.))和乌檀叶小苦荬(Smallanthus uvedalius (L.))[同义词为多须公(Polymnia uvedalius (L.))],分别是倍半萜内酯小白菊内酯和泽兰内酯的新来源。在本研究中,在大鼠角叉菜胶炎症模型中评估了从这两种植物来源分离得到的这些内酯的抗炎和抗痛觉过敏作用。大鼠腹腔注射溶剂(丙二醇)、吲哚美辛(5毫克/千克)、11,13 - 二氢小白菊内酯(20毫克/千克)、小白菊内酯(5或20毫克/千克)或泽兰内酯(5或20毫克/千克)。将100微升2.0%的角叉菜胶注射到右后爪的足底表面。在四个测试时间点记录炎症和未炎症爪子的爪退缩潜伏期和爪体积:炎症前基线(0时间点)以及角叉菜胶注射后1、2和4小时。溶剂处理的动物表现出显著的时间依赖性痛觉过敏和水肿反应,在4小时测试时间点最为明显。吲哚美辛显著阻断痛觉过敏反应并适度减轻水肿反应。小白菊内酯(20毫克/千克)和泽兰内酯(20毫克/千克)显著阻断痛觉过敏反应并显著减轻水肿反应;11,13 - 二氢小白菊内酯对炎症或痛觉过敏均无影响。这些发现表明,来自这些植物来源的小白菊内酯和泽兰内酯可能对治疗炎性疼痛有用。