1989 Fiscal Year Final Research Report Summary
Systematic Search for New Pharmacologically Active Metabolites of Ascomycetes and Basidiomycetes
| Project/Area Number |
63570981
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| Research Category |
Grant-in-Aid for General Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Research Field |
Chemical pharmacy
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| Research Institution | Chiba University |
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Principal Investigator |
FUJIMOTO Haruhiro Chiba University, Faculty of Pharmaceutical Sciences, Associate Professor, 薬学部, 助教授 (50089603)
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| Project Period (FY) |
1988 – 1989
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| Keywords | Ascomycetes / Basidiomycetes / Pharmacologically active metabolites / Systematic search / Lethal toxicity / Monoamine oxidase inhibitory activity / Anti-acetylcholine effect / Cellular immunity |
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| Research Abstract |
1. Toxicity of the crude extracts of more than fifty strains in Ascomycetes belonging to the genera, Talaromyces, Eupenicillium, Neosartorya, Hamigera and Eurotium was investigated by monitoring whether any extraordinariness occurs or no in mice by administration of the extract. On this bioassay, Eupenicillium hirayamae and Neosartorya fischeri were newly discovered to be toxic to mice. The toxic principles of E. hirayamae and N. fischeri were disclosed to be a known azaphilone compound and a new 1-hydroxy-2-pyridone compound, respectively. On a systematic monitoring monoamine oxidase inhibitory (HAOI) activity, the crude extract of Talaromyces luteus afforded MAOI effect. The MAOI principles of the fungus, tentatively named TL-1 and -2, were clarified to be new azaphilme compounds being isomeric each other. Investigation of any possibility to apply TL-1 and -2 to Parkinson disease is now remained to be our next project.
2. Toxicity of the crude extracts of some species in Basidiomycete
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s collected in Chiba, Yamanashi and Nagano was investigated in the same way as for the assay of Ascomycetes. On this bioassay, Hebeloma spoliatum was newly discovered to be lethally toxic to mice. Among three toxic principles, tentatively named HS-A, -B and -C, of the fungus, HS-A was identical with a known cytotoxic triterpene compound already isolated from the closely related species and other two were new compounds having the related structures to that of HS-A. The main lethal toxicity of these compounds may be originated from any disorder occurred in the central nervous system, but these compounds seem to be also effective to the digestive organs. They showed an anti-acetylcholine effect on a Magnus assay with a mouse small intestine preparation. Their biological activity will be further studied in near future.
3. Some methods to search systematically for imunologically active metabolites in Asco- and Basidiomycetes were studied. It was revealed to be a good method to search for any fungal metabolites being effective to the cellular immunity system to adopt firstly lymphs, cyte transformation test in vitro and then delayed type hypersensitization test in vivo. Less
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Research Products
(9 results)
