Development of the new molecular system which can control capture of drugs, a delivery and release
| Project/Area Number |
25410184
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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 |
Bio-related chemistry
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| Research Institution | Fukuoka University |
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Principal Investigator |
Ando Setsuko 福岡大学, 理学部, 教育嘱託 (20078562)
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| Project Period (FY) |
2013-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2015: ¥520,000 (Direct Cost: ¥400,000、Indirect Cost: ¥120,000)
Fiscal Year 2014: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2013: ¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
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| Keywords | ホストゲスト化学 / ペプチド化学 / アシルヒドラゾン結合 / ペプチド結合 / クラスター効果 / トリプシン / トリプシン基質 / ホストーゲスト / 水溶性シクロファン / ジペプチド / テトラペプチド / タンパク質分解酵素 |
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| Outline of Final Research Achievements |
Water-soluble cyclophane with tetrapeptide (host:CP-N3-LKLA-Fmoc) was synthesized and identified by HPLC,MALDI-TOF-MS,and 1H-NMR spectroscopy. Upon addition of the host to aqueous solutions containing of the guests (2,6-ANS), a fluorescence intensity originated from the guest molecules was subjected to increase,was suggested that the guest molecules are incorporated into the hydrophobic cavity provided by the host. The host-guest binding constant (K) of the host toward 2,6-ANS was calculated to be 16,000 M-1 on the basis of Benesi-Hildebrand relationship.
Tryptic digestion of the host afforded the peptide fragments (Fmoc-ALK-OH), which was confirmed by HPLC and MALDI-TOF-MS measurements. Upon addition of trypsin to a buffer solution containing host-guest complexes, the fluorescence intensity originated from the guest molecules decreased gradually.. The degradation of the present cyclophane and the slow guest-release under enzymatic conditions was thought to be useful for DDS systems.
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Report
(4 results)
Research Products
(7 results)
