Thomet Olivier A R, Schapowal Andreas, Heinisch Isabelle V W M, Wiesmann Ulrich N, Simon Hans-Uwe
Department of Pharmacology University of Bern, Switzerland.
Int Immunopharmacol. 2002 Jun;2(7):997-1006. doi: 10.1016/s1567-5769(02)00046-2.
Previous studies have suggested that histamine and leukotrienes (LTs) play an important pathobiological role in IgE-mediated allergic diseases. In vitro studies suggested that an extract of Petasites hybridus (Ze339) blocks LT synthesis in monocytes and granulocytes. Petasins are considered to be the pharmacologically active fraction within Ze339. Patients suffering from allergic rhinitis received three times a day two tablets of Ze339 standardized to 8 mg petasins within a time period of 1 week. After 5 days of treatment, Ze339 significantly improved primary end points, which were day- and nighttime nasal symptoms. Nasal resistance, which was measured by rhinomanometry, gradually decreased as a consequence of Ze339 treatment reaching normal levels after 5 days (rhinomanometry: from 403.5+/-62.0 to 844.8+/-38.8 ml). Levels of inflammatory mediators in nasal fluids and serum were measured 90 min after drug administration every day in the morning. After 5 days of treatment, a significant reduction of histamine (from 153.7+/-32.1 to 53.0+/-8.4 pg/ml) and LT levels (LTB4: from 313.1+/-46.5 to 180.6+/-32.2 pg/ml; cysteinyl-LT: from 137.0+/-42.2 to 70.1+/-16.5 pg/ml) could be observed. Moreover, quality-of-life scores significantly improved. The drug had no effect on the distribution of lymphocyte subpopulations in the blood as well as on the capacity of blood leukocytes to generate cytokines and lipid mediators. These results suggest that Ze339 is effective in treating allergic rhinitis patients by decreasing levels of nasal inflammatory mediators.
先前的研究表明,组胺和白三烯(LTs)在IgE介导的过敏性疾病中发挥重要的病理生物学作用。体外研究表明,蜂斗菜(Petasites hybridus,Ze339)提取物可阻断单核细胞和粒细胞中的LT合成。蜂斗菜素被认为是Ze339中的药理活性成分。患有过敏性鼻炎的患者在1周的时间段内每天服用3次两片标准化为8毫克蜂斗菜素的Ze339。治疗5天后,Ze339显著改善了主要终点指标,即白天和夜间的鼻部症状。通过鼻阻力计测量的鼻阻力由于Ze339治疗而逐渐降低,在5天后达到正常水平(鼻阻力计测量:从403.5±62.0降至844.8±38.8毫升)。每天早晨给药90分钟后测量鼻液和血清中的炎症介质水平。治疗5天后,可观察到组胺水平显著降低(从153.7±32.1降至53.0±8.4皮克/毫升)以及LT水平降低(白三烯B4:从313.1±46.5降至180.6±32.2皮克/毫升;半胱氨酰白三烯:从137.0±42.2降至70.1±16.5皮克/毫升)。此外,生活质量评分显著改善。该药物对血液中淋巴细胞亚群的分布以及血液白细胞产生细胞因子和脂质介质的能力没有影响。这些结果表明,Ze339通过降低鼻炎症介质水平对治疗过敏性鼻炎患者有效。