| Project/Area Number |
60470144
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| Research Category |
Grant-in-Aid for General Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Chemical pharmacy
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| Research Institution | Faculty of Pharmaceutical Sciences, University of Tokyo |
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Principal Investigator |
YUTAKA EBIZUKA Faculty of Pharmaceutical Sciences, University of Tokyo, 薬学部, 助教授 (90107384)
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| Project Period (FY) |
1985 – 1986
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| Project Status |
Completed (Fiscal Year 1986)
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| Budget Amount *help |
¥3,300,000 (Direct Cost: ¥3,300,000)
Fiscal Year 1986: ¥900,000 (Direct Cost: ¥900,000)
Fiscal Year 1985: ¥2,400,000 (Direct Cost: ¥2,400,000)
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| Keywords | Anti-allergy / Medicinal Drugs / PCA; Histamine release / Magnolia salicifolia / Centipeda minima / 石胡すい / Melalenca lencadendron |
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| Research Abstract |
Some oriental medicinal drugs which are reputed in Chinese literatures to be effective to certain allergic disorders were selected and assayed for their inhibitory activities against in vivo rat passive cutaneous anaphylaxis (PCA) test, a common experimental model for Type- <I> allergy mediated by IgE. Hot aqueous extract of Magnolia salicifolia, Centipeda minima and Melaleuca leucadendron showed marked inhibition in this assay.
Isolation of the active constituents of these extracts were attempted using in vitro inhibition of histamine release from rat peritoneal mast cells as a monitor. Close co-relation between inhibition of PCA and histamine release has been demonstrated. Repeated chromatographies yielded coumarins, flavonoids and lignans as the active constituents of M. salicifolia, flavonoids and sesquiterpene lactones of C. minima and triterpenes and stilbenes of M. leucadendron. Some of them exhibited more potent activity in vitro than DSCG, one of the most popular clinical anti-allergy drugs. Structure-activity relationship among coumarins, lignans and stilbenes were conducted as well in vitro.
In vivo inhibition of some flavonoids and sesquiterpene lactones against PCA test revealed that they are indeed active even by oral administration.
In conclusion, the results obtained in this study provide not only scientific rationalization for the use of these traditional medicinal drugs but also lead compounds for the development of new clinical anti-allergy drugs.
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