2016 Fiscal Year Final Research Report
Development of extraction techniques for natural products and discovery of hyaluronan-degrading enzyme inhibitors from natural products
| Project/Area Number |
26870217
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
General internal medicine(including psychosomatic medicine)
Natural medicines
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| Research Institution | University of Toyama |
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Principal Investigator |
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| Project Period (FY) |
2014-04-01 – 2017-03-31
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| Keywords | 生薬 / 多成分の分子変換 / アミノ酸誘導体 / ヒダントイン / ヒアルロニダーゼ / 化学的摂動効果 / ジメチルスルホキシド / 非特異的分子間相互作用 |
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| Outline of Final Research Achievements |
We have achieved direct chemical derivatization of natural plant extracts, where electrophilic ketones in the extracts could be selectively converted into the corresponding hydantoins (imidazolidine-2,4-dione) under the Bucherer-Bergs reaction conditions. The derivatization proceeded with enough chemoselectivity, minimizing the complication of the reaction system, and thus realizing the facile identification of unnatural hydantoins from the derivatized extracts.
We have also developed new methodology to highlight promiscuous non-specific binding inhibitors of enzymes by interpreting the behavior of concentration-response curves under in vitro DMSO-perturbing assay conditions. Furthermore, we have discovered novel inhibitors of hyaluronan-degrading enzyme from natural plant extracts.
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| Free Research Field |
創薬化学
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