Establishment of a SPR system to screen for plant-based seed compounds for drugs against lifestyle diseases

2016 Fiscal Year Final Research Report

• Project/Area Number: 26460131
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Natural medicines
• Research Institution: Tokyo University of Pharmacy and Life Science
• Principal Investigator: KURODA Minpei 東京薬科大学, 薬学部, 准教授 (80266890)
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: 表面プラズモン共鳴 / 抗生活習慣病薬 / スクリーニング / aldose reductase

Outline of Final Research Achievements

Using a SPR system, we analyzed the interaction between aldose reductase (AR), which plays a role in diabetic complications, placed on the chip and a plant extract with AR inhibitory activity as determined by a conventional method. The resulting sensorgram showed no interaction. Then, we prepared four different plant extracts with AR inhibitory activity and isolated 49 compounds, including four new compounds, from the extracts. Among the compounds, dicaffeoylquinic acid (DCQA) derivatives exhibited strong inhibitory activity toward AR, and the activity decreased when the carboxylic acid of the DCQA was converted to a methyl ester. Our findings also revealed that the activity of the DCQA was affected by the binding site and number of caffeoyl groups.

Free Research Field

天然物化学