| Project/Area Number |
14572022
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Chemical pharmacy
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| Research Institution | KYOTO PHARAMCEUTICAL UNIVERSITY |
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Principal Investigator |
YOSHIKAWA Masayuki KYOTO PHARMACEUTICAL UNIVERSITY, PROFESSOR, 薬学部, 教授 (90116129)
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| Co-Investigator(Kenkyū-buntansha) |
MORIKAWA Toshio KYOTO PHARMACEUTICAL UNIVERSITY, ASSISTANT PROFESSOR, 薬学部, 助手 (10340449)
MATSUDA Hisashi KYOTO PHARMACEUTICAL UNIVERSITY, ASSOCIATE PROFESSOR, 薬学部, 助教授 (40288593)
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| Project Period (FY) |
2002 – 2003
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| Project Status |
Completed (Fiscal Year 2003)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,900,000)
Fiscal Year 2003: ¥1,300,000 (Direct Cost: ¥1,300,000)
Fiscal Year 2002: ¥2,600,000 (Direct Cost: ¥2,600,000)
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| Keywords | Salacia reticulata / Salacia chinensis / anti-obese activity / antidiabetogenic activity / α-glucosidase inhibitory activity / salacinol / mangiferin / artichoke / α-glucosidase阻害活性 / aldose reductase阻害活性 / AGEs産生抑制活性 / flavonoid / アルドース還元酵素阻害活性 / リパーセ阻害活性 |
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| Research Abstract |
The genus Salacia have been used as a specific remedy at the initial stages of diabetes in the Ayuruvedic system of Indian traditional medicine. The aqueous methanolic extract from the roots and stems of S.reticulata, S.oblonga, and S.chinensis were found to show hypoglycaemic activity in rats and α-glucosidase inhibitory activity. By bioassay-guided separation, salacinol and kotalanol, which having the unique thiosugar sulfonium sulfate inner salt structures, were isolated as the active constituents. Particularly, sucrase and maltase inhibitory activities (in vitro) and inhibitory effects on serum glucose levels in sucrose-and maltose-loaded rats (in vivo) of salacinol were more potent than those of commercial medicine as α-glucosidase inhibitor, acarbose. In addition, the water extract of S.reticulata and its polyphenolic constituents indcuding mangiferin found to show anti-obese activity. Furthermore, seven new triterpenes and two new sesquiterpenes were isolated from the stems of S.chinensis and its triterpene constirutens found to show inhibit aldose reductase inhibitory activity and radical scavenging activities.
The methanolic extract from artichoke exhibited anti-hyprelipidemic activity and several sesquiterpenes were isolated as the active components.
To clarify structural requirements for aldose reductase, AGEs formation, and radical scavenging activities, various flavonoid compounds were examined above-mentioned screening tests and suggested several structure-activity relationships.
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