Nobre da Silva Francisco Alcione, de Farias Freire Sônia Maria, da Rocha Borges Marilene Oliveira, Vidal Barros Francisco Erivaldo, da de Sousa Maria, de Sousa Ribeiro Maria Nilce, Pinheiro Guilhon Giselle Maria Skelding, Müller Adolfo Henrique, Romão Borges Antonio Carlos
Department of Physiological Sciences, Federal University of Maranhão, University City, Bacanga, São Luís, Maranhão, Brazil.
Department of Pharmacy, Federal University of Maranhão, University City, Bacanga, São Luís, Maranhão, Brazil.
Pharmacognosy Res. 2017 Dec;9(Suppl 1):S1-S4. doi: 10.4103/pr.pr_51_17.
DC. (Asteraceae), a medicinal plant known as "quitoco," "caculucage," "tabacarana" and "madre-cravo," is indicated for inflammatory conditions such as bronchitis, arthritis, and inflammation in the uterus and digestive system.
This study evaluated the analgesic and anti-inflammatory activities of the triterpenes compounds obtained from aerial parts.
The triterpenes compounds β-amyrin, taraxasterol and pseudo-taraxasterol in a mixture (T); β-amyrin, taraxasterol and pseudo-taraxasterol acetates in a mixture (Ta); β-amyrin, taraxasterol, pseudo-taraxasterol acetates in a mixture with β-amyrin, taraxasterol and pseudo-taraxasterol myristates (Tafe) were analyzed in the models of nociception and inflammation. The evaluation of antinociceptive activity was carried out by the acetic acid-induced writhing and tail-flick tests while leukocyte migration to the peritoneal cavity was used for anti-inflammatory profile.
The oral administration of T or Tafe (40 mg/kg and 70 mg/kg) and Ta (70 mg/kg) to mice reduced acetic acid-induced writhing. The tail-flick response of mice was not affected by T or Tafe (40 mg/kg). T or Tafe (40 mg/kg) and Ta (70 mg/kg) also inhibited peritoneal leukocyte infiltration following the injection of carrageenan.
The results demonstrate the anti-inflammatory and peripheral antinociceptive activity of the triterpenes β-amyrin, taraxasterol, and pseudo-taraxasterol that were decreased when these were acetylated; while the acetylated triterpenes in mixture with myristyloxy triterpenes improved this activity. These compounds seem, at least in part, to be related to the plant's reported activity.
The mixtures of hydroxylated, acetylated, and myristate triterpenes isolated from hexanic extracts of DC. were analyzed in the models of nociception and inflammation in mice. The results demonstrate the anti-inflammatory and peripheral antinociceptive activity of the triterpenes β-amyrin, taraxasterol, and pseudo-taraxasterol. This study showed too that the activity of triterpenes may be decreased by their being acetylated, while the acetylated triterpenes in mixture with myristate triterpenes improved this activity. T: Triterpenes compounds β-amyrin, taraxasterol, and pseudo-taraxasterol in a mixture, Ta: Triterpenes compounds β-amyrin, taraxasterol and pseudo-taraxasterol acetates in a mixture, Tafe: Triterpenes compounds β-amyrin, taraxasterol, pseudo-taraxasterol acetates in a mixture with β-amyrin, taraxasterol and pseudo-taraxasterol myristates, Ctrl: Control, Indo: Indomethacin, Dexa: Dexamethasone, EtOAc: Ethyl acetate, MeOH: Methanol.
菊科植物DC.，一种被称为“quitoco”“caculucage”“tabacarana”和“madre - cravo”的药用植物，适用于治疗如支气管炎、关节炎以及子宫和消化系统炎症等病症。
本研究评估了从地上部分提取的三萜类化合物的镇痛和抗炎活性。
在伤害感受和炎症模型中分析了混合物（T）中的三萜类化合物β - 香树脂醇、蒲公英甾醇和伪蒲公英甾醇；混合物（Ta）中的β - 香树脂醇、蒲公英甾醇和伪蒲公英甾醇乙酸酯；混合物（Tafe）中的β - 香树脂醇、蒲公英甾醇、伪蒲公英甾醇乙酸酯与β - 香树脂醇、蒲公英甾醇和伪蒲公英甾醇肉豆蔻酸酯。通过醋酸诱导扭体试验和甩尾试验评估抗伤害感受活性，而采用白细胞向腹腔的迁移来评估抗炎情况。
给小鼠口服T或Tafe（40mg/kg和70mg/kg）以及Ta（70mg/kg）可减少醋酸诱导的扭体反应。T或Tafe（40mg/kg）对小鼠的甩尾反应无影响。T或Tafe（40mg/kg）以及Ta（70mg/kg）在注射角叉菜胶后也抑制了腹腔白细胞浸润。
结果表明三萜类化合物β - 香树脂醇、蒲公英甾醇和伪蒲公英甾醇具有抗炎和外周抗伤害感受活性，乙酰化后活性降低；而乙酰化三萜类化合物与肉豆蔻酰氧基三萜类化合物混合可提高该活性。这些化合物似乎至少部分与该植物所报道的活性相关。
从DC.的己烷提取物中分离出的羟基化、乙酰化和肉豆蔻酸酯三萜类化合物混合物，在小鼠的伤害感受和炎症模型中进行了分析。结果表明三萜类化合物β - 香树脂醇、蒲公英甾醇和伪蒲公英甾醇具有抗炎和外周抗伤害感受活性。本研究还表明，三萜类化合物的活性可能因其乙酰化而降低，而乙酰化三萜类化合物与肉豆蔻酸酯三萜类化合物混合可提高该活性。T：混合物中的三萜类化合物β - 香树脂醇、蒲公英甾醇和伪蒲公英甾醇，Ta：混合物中的三萜类化合物β - 香树脂醇、蒲公英甾醇和伪蒲公英甾醇乙酸酯，Tafe：混合物中的β - 香树脂醇、蒲公英甾醇、伪蒲公英甾醇乙酸酯与β - 香树脂醇、蒲公英甾醇和伪蒲公英甾醇肉豆蔻酸酯，Ctrl：对照组，Indo：吲哚美辛，Dexa：地塞米松，EtOAc：乙酸乙酯，MeOH：甲醇。
