Yunnan Institute of Medical Material, Kunming, PR China.
J Ethnopharmacol. 2010 May 27;129(2):174-81. doi: 10.1016/j.jep.2010.02.011. Epub 2010 Feb 26.
Alstonia scholaris (Apocynaceae) has been historically used in "dai" ethnopharmacy to treat chronic respiratory diseases. The leaf extract, developed as a commercially available traditional Chinese medicine, used to release tracheitis and cold symptom, has also been prescribed in hospitals and sold over the counter in drug stores.
The investigation evaluated the anti-inflammatory and analgesic activities of the ethanolic extract, fractions and main alkaloids of Alstonia scholaris leaf to provide experimental evidence for its traditional and modern clinical use. Besides, to discover the active fraction and components for further better use in Chinese medicine is hopeful.
The leaf of Alstonia scholaris was extracted with ethanol and then separated into different fractions. Furthermore, alkaloids were isolated by phytochemical method. The analgesic activities were investigated using acetic acid-induced writhing, hot-plate and formalin tests in mice. The anti-inflammatory activities were carried out in vivo and in vitro, including xylene-induced ear edema and carrageenan-induced air pouch formation in mice, and COX-1, -2 and 5-LOX inhibition.
It has been exhibited that the EtOAc and alkaloid fractions reduced acetic acid-induced writhing response in mice, significantly. The ethanolic extract, EtOAc and alkaloid fractions remarkably inhibited xylene-induced ear edema. Further investigation was focused on the alkaloids fraction and three main alkaloids isolated from the alkaloids fraction, in different animal models. Alkaloids reduced acetic acid-induced writhing response, and xylene-induced ear edema in mice. In the hot-plate test, alkaloids did not increase the latency period of mice obviously. In the formalin test, alkaloids did not inhibit the licking time in first phase, but significantly inhibited the licking time in second phase of mice. Alkaloids increased significantly SOD activity and decreased levels of NO, PGE2 and MDA significantly, in air pouch mice model. Moreover, some alkaloids isolated from the leaf of Alstonia scholaris exhibited inhibition of COX-1, COX-2 and 5-LOX in vitro anti-inflammatory assay, which supported alkaloids as the bioactive fraction.
The alkaloids fraction of Alstonia scholaris leaf, three main alkaloids, picrinine, vallesamine and scholaricine, may produce the anti-inflammatory and analgesic effect peripherally based on several in vivo assays. In in vitro tests, alkaloids exhibited inhibition of inflammatory mediators (COX-1, COX-2 and 5-LOX), which is accordant with results on animal models. Besides, COX-2/5-LOX dual inhibitors found in the experiment, such as 16-formyl-5alpha-methoxystrictamine, picralinal, and tubotaiwine might be valuable for further attention.
夹竹桃科鸡骨常山（Alstonia scholaris）在“傣”民族药物学中一直被用于治疗慢性呼吸道疾病。作为一种商业化的传统中药，从其叶子中提取的用于缓解气管炎和感冒症状的提取物，也已在医院开具处方并在药店柜台出售。
本研究评估了鸡骨常山叶的乙醇提取物、馏分和主要生物碱的抗炎和镇痛活性，为其传统和现代临床应用提供实验依据。此外，希望发现活性馏分和成分，以便进一步更好地用于中药。
用乙醇提取鸡骨常山叶，然后用不同的方法将其分离成不同的馏分。此外，还通过植物化学方法分离出生物碱。在小鼠体内和体外进行镇痛活性试验，包括乙酸诱导的扭体反应、热板试验和福尔马林试验。采用二甲苯诱导的耳肿胀和角叉菜胶诱导的气囊形成以及 COX-1、-2 和 5-LOX 抑制来进行抗炎活性试验。
研究表明，EtOAc 和生物碱馏分可显著减少小鼠的乙酸诱导扭体反应。乙醇提取物、EtOAc 和生物碱馏分显著抑制二甲苯诱导的耳肿胀。进一步的研究集中在生物碱馏分和从生物碱馏分中分离出的三种主要生物碱上，在不同的动物模型中进行了研究。生物碱可减少乙酸诱导的扭体反应和二甲苯诱导的小鼠耳肿胀。在热板试验中，生物碱并未明显延长小鼠的潜伏期。在福尔马林试验中，生物碱并未抑制小鼠第一阶段的舔舐时间，但明显抑制了第二阶段的舔舐时间。生物碱显著增加了气囊小鼠模型中的 SOD 活性，并显著降低了 NO、PGE2 和 MDA 的水平。此外，从鸡骨常山叶中分离出的一些生物碱在体外抗炎试验中表现出对 COX-1、COX-2 和 5-LOX 的抑制作用，这支持生物碱是生物活性馏分。
鸡骨常山叶的生物碱馏分、三种主要生物碱（ picrinine、vallesamine 和 scholaricine）可能通过几种体内试验产生外周抗炎和镇痛作用。在体外试验中，生物碱抑制了炎症介质（COX-1、COX-2 和 5-LOX），这与动物模型的结果一致。此外，实验中发现的 COX-2/5-LOX 双重抑制剂，如 16-甲酰基-5alpha-甲氧基斯特里克胺、picralinal 和 tubotaiwine 可能具有进一步关注的价值。
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