Search for anti-allergic constituents in South-East Asian traditional medicine

对肥大细胞组胺释放抑制活性的生物测定方法进行了改进，使其能够一次快速测定多个样品。通过对几种菲律宾传统药用植物活性的测定，选择了以下活性较强的植物(甲醇提取物)进行进一步的研究：小叶杜鹃、菲律宾杜鹃、紫草科植物。这些植物在当地被用于抗过敏和抗炎目的。从第一和第二植物提取物中分离出迷迭香酸，并通过核磁共振分析对其进行了表征。从第一株植物中分离得到两个新的开环二萜葡萄糖苷和尿囊素，其化学结构经仪器分析，特别是核磁共振波谱确证，二萜葡萄糖苷是植物酚的同系物。最近从泰国药用植物中发现了一种类似的化合物，Plaunotol，现在正被用作抗溃疡药物。从结构的相似性来看，我们的糖苷需要测试这种活性。尿囊素是已知的外用弱点，用于皮肤溃疡治疗，因此它也可能是上述植物活性的贡献者。值得注意的是，迷迭香酸的含量很高，这两种植物是这种活性化合物的有希望的来源。从抗过敏植物拟象耳属植物中分离得到两个新的倍半萜类化合物，并确定了它们的化学结构。

Bioassay method of measuring inhibiting activity of histamine release from mast cells was improved to be able to measure many samples at a time rapidly.By measuring the activity of several Philippine traditional medicinal plants, the following plants (MeOH extract) which showed strong activity, were selected for further study: Ehretia microphylla, E. philippinensis, Cordia myxa (Boraginaceae). These plants were locally used for anti-allergic and anti-inflammatory purposes.From the first and the second plant extracts, rosmarinic acid was isolated and characterized by NMR analysis. This compound was known to have anti-inflammatory activity, and it may well be responsible for the effect of these herbal medicines.Again from the first plant, two novel acyclic diterpene glucosides and allantoin were isolated and the chemical structure were elucidated by instrumental analysis, especially NMR spectroscopy.The diterpene glucosides were phytol congeners. A similar compound, plaunotol was recently found from Thai medicinal plant and is now being used as an anti-ulcer medicine. From the similarity of the structure, our glucosides need to be tested for such activity. Allantoin is known to be topical vulnerary and is used for skin ulcer therapy, so it may also be a contributor to the activity of the said plant. It is to be noted that the high content of rosmarinic acid is remarkable and the two Ehretia plants are promising sources of this active compound. From an antiallergic plant, Pesudoelephantopus spicatus, two novel sesquiterpenes were isolated and the chemical structures were decided.