Search for Bioactive Natural Products from Unexplored Medicinal Resources

在本研究中，我们使用未开发的药用资源如海藻、粘菌和热带植物构建了天然存在的小分子文库，并进行了筛选研究，以寻找有望作为药物开发主导分子的生物活性物质。在房总半岛采集了约100种海藻，并对其提取物进行了抗菌活性、卤虫毒性和胶原酶抑制活性的检测。其中，一种根皮单宁和一种抗菌质体醌分别从褐藻Ishige okamurae和Sargassum yamadae中分离得到。房总半岛还采集了约30种裸鳃亚目动物，并从皮鳃亚目动物的触角中获得了新的萜类成分。2）粘菌：我们研究了在日本野外采集的数百种粘菌的孢子萌发实验，并成功地在实验室培养了几种粘菌的原质团。 ...更多信息 天然产物化学研究的实用量表。结果，我们分别从培养的虹膜绒黏菌、硬绒泡菌和黑绒泡菌的疟原虫中分离出吡咯亚胺醌、多烯黄色素和肽内酯。还分别从野外采集的Cribraria purpurea、Fuligo candida、Tubifera casparyi和Tubifera dimorphotheca的子实体中分离出新的抗微生物萘醌、新的环邻氨基苯甲酰基脯氨酸、细胞周期抑制性双吲哚和细胞毒性三萜醛内酯。3）植物：我们研究了一个针对细胞毒性和细胞-利用从泰国孔敬地区收集的近300种热带植物提取物进行循环抑制活性的测定。其中，我们从菊科艾纳香中分离到一个具有细胞周期抑制活性的二萜，并对其绝对构型进行了修正。从龙舌兰（Agave faurcroydes）和姜黄（Curcuma parviflora）中分别分离得到一个新的甾体六萜内酯和一系列新的倍半萜二聚体。从夹竹桃中分离得到一种新的生物碱，对长春新碱耐药的小鼠白血病P388细胞具有细胞毒活性。少

In this study, we constructed a naturally-occurring small-molecule library using unexplored medicinal resources such as marine algae, myxomycetes, and tropical plants, and carried out a screening study searching for bioactive substances which may be expected as leading molecules for drug developments.1)Marine organisms : About 100 species of marine algae were collected at Boso Peninsula, and their extracts were examined against antimicrobial activity, Artemia salina toxicity, and collagenase inhibitory activity. Among them, a phlorotannin and an antimicrobial plastoquinone were isolated from brown algae Ishige okamurae and Sargassum yamadae, respectively. About 30 species of nudibranchs were also collected at Boso Peninsula, and new terpenoid constituents were obtained from Dermatobranchus otome.2)Myxomycetes : We studied spore germination experiments of hundreds of field-collected myxomycetes collected in Japan and succeeded in laboratory culture of plasmodia of several myxomycetes in … More a practical scale for natural products chemistry studies. As a result, we isolated pyrroloiminoquinones, polyene yellow pigments, and a peptide lactone from cultured plasmodia of Didymium iridis, Physarum rigidum, and P.melleum, respectively. A new antimicrobial naphthoquinone, new cycloanthranilylprolines, cell-cycle inhibitory bisindoles, and a cytotoxic triterpenoid aldehyde lactone were also isolated from field-collected fruit bodies of Cribraria purpurea, Fuligo candida, Tubifera casparyi, and Tubifera dimorphotheca, respectively.3)Plants : We investigated a screening program against cytotoxicity and cell-cycle inhibitory activity using almost 300 species of tropical plants extracts collected from Khon Kaen area of Thailand. Among them, we isolated a diterpene with cell-cycle inhibitory activity from Blumea glomerata (Compositae) and its absolute configuration was revised. A new cytotoxic steroidal hexasaccharaide and a series of new sesquiterpene dimers were obtained from Agave faurcroydes (Agavaceae) and Curcuma parviflora (Zingiberaceae), respectively. A new pregnane alkaloid with cytotoxic activity against vincristine-resistant murine leukemia P388 cells was isolated from Wrightia javanica (Apocynaceae). Less