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DEVELOPMENT OF MEDICINAL DRUGS FROM SOUTHERN HEMISPHERIC TASTY BRYOPHYTES AND FERNS AND THEIR CHEMOSYSTEMATICS

南半球美味苔藓植物和蕨类药物的开发及其化学体系

基本信息

批准号：
14403014
负责人：
ASAKAWA Yoshinori
金额：
$ 5.38万
依托单位：
FACULTY OF PHARMACEUTICAL SCIENCES, TOKUSHIMA BUNRI UNIVERSITY
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (B)
财政年份：
2002
资助国家：
日本
起止时间：
2002 至 2005
项目状态：
已结题

项目摘要

In the southern hemisphere, there are a great number of endemic bryophyte (liverworts, mosses and hornworts) and pteridophyte (ferns) species many of which contain pungent, bitter or sweet taste. Since the crude extracts of these tasty species showed potent antimicrobial and antifungal, insect and killing, antitumor, and muscle relaxing activity, we collected the New Zealand, Argentinean, Malgasy and Malaysian bryophytes and ferns and extracted with ether. 1.New Zealand liverworts : From Jungermannia species 12 new and 4 known ent-kaurane-type diterpenoids of which ent-11α-hydroxy-16-kauren-15-one and jugermannenone D showed strong cytotoxicity and apoptosis against HL-60. Lepidozia spinosissima contained a new gorgonae-type sesquiterpene the similar compound to which was isolated from some marine gorgonanian species. Balantiopsis rosea produced quite interesting 1-cyclohexy1-2-phenyl ethane derivatives which were suggested to be the biosynthetic precursors of the typical bibenzyls and … More bisbibinzyls which were peculiar secondary metabolites of liverworts. 2.Argentinean liverworts and fern : Frullania brasiliensis contained eremophilanolides which caused potent allergy. Porella swartziana elaborated africane-type and its related sesquiterpenoids which resembled those of Japanese species. The strong pungency of the fern, Thelypteris hispidula was responsible for polygodial which was also found in the liverwort Porella vernicosa complex as well as the New Zeland fern, Brechnum species. Such a chemical identity is very important to understand that some ferns might originate from the some genera of liverworts. 3.Malgasy liverworts : Several Bazzania, Plagiochila and Marchantia species produced many sesquiterpenes and bisbibenzyls, however, the new compounds were not isolated. 4.Malaysian liverworts : Two Marchantia species contained a large amount of marchanin A which showed NO production inhibitory activity. Riccardin C, which is a macrocyclic bisbibenzyl found in some New Zealand and Japanese liverwort, such as Reboulia hemisphaerica functioned as a liver X captor (LXR)α agonist and an LXRβ antagonist, thus this compound is now recognized as one of the most important potential antichorestemic drug. The present results were reported in the international and domestic symposia for1 and 35 times, respectively and 40 papers (7 are in press), four reviews and one book were published. The representative of this research project obtained the 35^<th> International Award of ISEO (International symposium on Essential Oils) and Tucman University award (Argentina) during this research project. Less

在南半球，分布着大量的特有苔藓植物(地衣、苔藓和金鱼草)和蕨类植物(蕨类)，其中许多都有辛辣、苦味或甜味。由于这些美味物种的粗提物具有很强的抗菌、抗真菌、杀虫、抗肿瘤和肌肉松弛活性，我们收集了新西兰、阿根廷、马尔加西和马来西亚的苔藓植物和蕨类植物，并用乙醚提取。1.新西兰地钱：12个新的和4个已知的龙胆烷型二萜化合物，其中Et-11α-羟基-16-角叉烯-15-酮和朱古兰酮D对HL-60细胞具有较强的细胞毒和细胞凋亡作用。棘鳞毛虫中含有一种新的柳珊瑚类倍半萜类化合物，类似于从一些海洋柳珊瑚物种中分离得到的化合物。玫瑰香产生了非常有趣的1-环己基-2-苯基乙烷衍生物，这些衍生物被认为是典型的联苯和…的生物合成前体。地衣特有的次生代谢物--联苯双酯较多。2.阿根廷地钱和蕨类植物：Frullania brasiliensis含有能引起强烈过敏的嗜热菌内酯类化合物。Swartziana阐述了类似日本种的非洲烷型及其相关的倍半萜类化合物。该蕨类植物的强烈刺激性导致了多聚果糖的产生，在地钱属植物Porella vernicosa复合体和新泽兰蕨类植物Brechnum中也存在。这种化学特性对于理解一些蕨类植物可能起源于一些苔类植物是非常重要的。3.地钱：几种地钱属植物产生了大量的倍半萜和联苯类化合物，但未分离到新化合物。4.马来西亚地钱：两种地钱草含有大量的马钱子素A，没有表现出生产抑制活性。Riccardin C是一种在新西兰和日本地钱中发现的大环联苯基化合物，具有肝X受体α激动剂和肝X受体β拮抗剂的作用，是目前公认的最重要的潜在抗舞蹈病药物之一。本研究结果分别在国际和国内研讨会上发表了1次和35次，发表了40篇论文(7篇在印中)，4篇综述和1本书。本研究项目的代表在本研究项目期间获得了第35届国际精油研讨会奖和阿根廷图克曼大学奖。较少