Anti-inflammatory and analgesic activity of Baccharis trimera: Identification of its active constituents
Anti-inflammatory and analgesic activity of Baccharis trimera: Identification of its active constituents
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DOI：
10.1055/s-2006-957866
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发表时间：
1996-06-01
期刊：
影响因子：
2.7
通讯作者：
Canigueral, S
中科院分区：
文献类型：
--
作者：
Gene, RM;Cartana, C;Canigueral, S
从Baccharis trimera的地上部分制备来自水性粗提物的丁醇级分（BT-II），并在抗炎、镇痛和溃疡形成模型中进行评估。用冻干BT-II以40至100 mg/kg的剂量范围腹膜内预处理，显著抑制角叉菜胶和葡聚糖诱导的炎症（分别为70.4- 90.8%和25.7- 77.3%），并微弱地降低C-16-paf和花生四烯酸诱导的肿胀（分别为24.9-36.7%和0- 30.6%）。在相同剂量下，未观察到对酵母多糖诱导的水肿的影响。腹腔内检查表明，BT-II的抗炎作用不是由于注射部位的刺激作用。此外，BT-II减少注射乙酸后小鼠的腹部收缩：50 mg/kg时，抑制率为67.4%，100 mg/kg时为95.1%。致溃疡性试验显示，BT-II i. p.给药后，50 mg/kg组和100 mg/kg组的溃疡发生率分别为2/6和6/6。致溃疡指数分别为1.3 +/- 0.5和2.7 +/- 0.8。这些结果表明，B. Trimera显示出强的镇痛和止痛特性，这似乎至少部分是由于前列腺素生物合成的抑制。通过生物测定（小鼠角叉菜胶诱导的水肿试验）监测BT-II的色谱分离。活性成分主要为皂苷类和芦丁，其中刺囊酸（或其对映体）是主要的苷元。
The butanolic fraction (BT-II) derived from the aqueous crude extract was prepared from aerial parts of Baccharis trimera and assessed in anti-inflammatory, analgesia, and ulcerogenesis models. Intraperitoneal pretreatment with lyophilized BT-II, at doses ranging from 40 to 100 mg/kg, markedly inhibited carrageenan- and dextran-induced inflammation (70.4-90.8 % and 25.7-77.3%, respectively) and weakly decreased C-16-paf- and arachidonic acid-induced swelling (24.9-36.7% and 0-30.6%, respectively). No effect was observed, at the same doses, on zymosan-induced edema. The intraperitoneal examination indicates that the anti-phlogistic action of BT-II was not due to an irritating effect at the injection site. Besides, BT-II reduced abdominal constrictions in mice following injection of acetic acid: at 50 mg/kg, it gave 67.4 % inhibition and, at 100 mg/kg, 95.1 %. The ulcerogenic assay showed that the incidence of ulcers after BT-II i.p. treatment was 2/6 at 50 mg/kg and 6/6 at 100 mg/kg. Ulcerogenic indices were 1.3 +/- 0.5 and 2.7 +/- 0.8, respectively. These results indicate that B. trimera shows strong antiinflammatory and analgesic properties which seem to be due, at least partly, to the inhibition of prostaglandin biosynthesis. The chromatographic separation of BT-II monitored by bio-assay (carrageenan-induced edema test in mice) was carried out. The active constituents were found to be mainly saponins in which echinocystic acid (or its enantiomer) is the major aglycone, and also rutin.