Synthesis of cytotoxic amino acid derivatives from natural product
| Project/Area Number |
15K08004
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Natural medicines
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| Research Institution | Nihon University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
深津 誠 日本大学短期大学部, その他部局等, 教授 (80181238)
鈴木 孝 日本大学, 薬学部, 教授 (40318457)
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2017: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2016: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2015: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Keywords | テルペノイド / 腫瘍細胞傷害活性 / アミノ酸 / がん細胞 / 選択性 / 抗がん剤 / 天然物 / LAT1 / 抗がん活性 / アミノ酸誘導体 |
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| Outline of Final Research Achievements |
In this study, we prepared amino acid conjugates and amino acid derivatives from natural triterpenoid; faradiol, and diterpenoid; isosteviol. Faradiol-amino acid conjugate showed potent cytotoxicities against the four human cancer cell lines (HL60, A549, AZ521, and SK-BR-3) and the mode of action was though to be apoptosis inducing effects which was analyzed by flowcytometory using Annexin V and propidium iodide. Furthermore, isosteviol-amino acid conjugates are also prepared. These showed potent cytotoxicities against the four human cancer cell lines. The mode of action of the compound was determined as activation of some apoptosis related protein, caspase-3 and caspase-8 by Western-Blotting analysis. In addition, seco-type ent-beyerane α-amino acid was prepared from isosteviol and the stereochemistry was determined by spectroscopic method.
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Report
(4 results)
Research Products
(5 results)
