2000 Fiscal Year Final Research Report Summary
SERCHING FOR DISCOVERY OF RHEUMATOID ARTHRITIS DRUG FROM TRIPTERYGIUM WILFORDII.
| Project/Area Number |
10557209
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| Research Category |
Grant-in-Aid for Scientific Research (B).
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| Allocation Type | Single-year Grants |
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| Section | 展開研究 |
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| Research Field |
Chemical pharmacy
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| Research Institution | University of Tokushima |
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Principal Investigator |
TAKAISHI Yoshihisa University of Tokushima, Faculty of Pharmaceutical Sciences, Professor, 薬学部, 教授 (60035558)
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| Co-Investigator(Kenkyū-buntansha) |
ONO Yukihisa Otsuka Pharmaceutical Company, Researcher, 医薬第3研究所, 研究員
MURAKAMI Koutarou University of Tokushima, Faculty of Pharmaceutical Sciences, Assistnt Prof., 薬学部, 助手 (10035553)
KAWAZOE Kazuyoshi University of Tokushima, Faculty of Pharmaceutical Sciences, Lecture, 薬学部, 講師 (00248296)
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| Project Period (FY) |
1998 – 2000
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| Keywords | RHEUMATOID ARTHRITIS / CYTOKINE / Tripterygium wilfordii / Triterpene / Diterpene / Interleukin-1 / Natural Product |
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| Research Abstract |
In recently years, a refined extract from the root xylem of Tripterygium wilfordii (TII) has been used in the clinical treatment of rheumatoid arthrits, and for other inflammatory and autoimmune diseases, including systermic lupus erythemasus etc. However, the precise mechanism of the therapeutic effect of TII has not been completely delineated. We has started work on the isolation of T.hypoglaucum and T.wildfordii and the TII extract to discover new drug for Rheumatoid Arthrits desease. We isolated five new triterpenes, two new diterpenes, and twelve new sesquiterpene pyridine alkaloids, as well as thirty-three known compounds from the root outer barks of T.hypoglaucum. From the TII extract of T.wilfordii, seven new triterpenes, four new diterpenes, twenty new sesquiterpene pyridine alkaloids, as well as fifty-six known compounds. In the bioactive screening experiment for isolated compoinds, the auther examined inhibitory effect on cytokine production and anti-HIV activity. Three compounds showed extreamely potent inhibitory effect on cytokine production from LPS stimulated human peripheral mononuclea cellscompared with reference compound. and sesquiterpene alkaloid inhibited HIV replication in H9 lymphocytes with therapeutic index value of>1000, this compound is a new class of potent anti-HIV agents from natural source.
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