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

改进了测量肥大细胞组胺释放抑制活性的生物测定方法，使其能够一次快速测量多个样品。通过对几种菲律宾传统药用植物的活性测定，筛选出活性较强的植物（MeOH提取物）：小叶Ehretia microphylla， E. philippinensis, Cordia myxa （Boraginaceae）。这些植物在当地用于抗过敏和抗炎。从第一和第二植物提取物中分离得到迷迭香酸，并通过核磁共振分析对其进行了表征。这种化合物已知具有抗炎活性，它很可能是这些草药效果的原因。从第一株植物中分离到两个新的无环二萜糖苷和尿囊素，并通过仪器分析特别是核磁共振光谱对其化学结构进行了鉴定。二萜糖苷是叶绿醇同系物。一种类似的化合物，普劳诺醇，最近从泰国药用植物中发现，现在被用作抗溃疡药。从结构的相似性来看，我们的糖苷需要进行这种活性的测试。众所周知，尿囊素是局部易感性的，用于皮肤溃疡治疗，因此它也可能是上述植物活性的一个贡献者。值得注意的是，迷迭香酸的高含量是显著的，这两种Ehretia植物是这种活性化合物的有希望的来源。从抗过敏植物假象皮（pseudoelephantopus spicatus）中分离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.