| Budget Amount *help |
¥5,070,000 (Direct Cost: ¥3,900,000、Indirect Cost: ¥1,170,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2014: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
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| Outline of Final Research Achievements |
5-Aminolevulinic acid (ALA) is now widely used for photodynamic diagnosis and photodynamic therapy (ALA-PDT) of various cancers. In the heme biosynthesis pathway, ALA is converted to protoporphyrin IX (PpIX). Following excitation with blue light (405 nm), the accumulated PpIX emits a red fluorescence (635 nm). Thus, cancer tissue can be effectively visualized by the PpIX fluorescence. Furthermore, absorption of light beyond 630 nm by PpIX leads to the production of reactive oxygen species that can induce cell death in various cancer cells. Previously, we found that the Schiff base derivative TX-816 can significantly increase the effect of ALA-PDT by accelerating the intracellular PpIX accumulation. In this study, we synthesized TX-816 derivatives in which 2-chloro-4-nitroaniline was substituted with 4-alkyl aniline. These derivatives were chemically more stable than TX-816 was. The derivatives may become a potent lead compounds for the development of prodrug-type ALA-PDT sensitizers.
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