1102 癌細胞選択的なアミノレブリン酸取り込み評価(OS13-(5)オーガナイズドセッション《生体医工学及びバイオマテリアル》)

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  • 1102 Evaluation of 5-aminolevulinic acid as a cancer-targeting ligand

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Side-effects of anticancer drugs are the serious problem in cancer chemotherapy because anticancer drugs affect not only cancer cells but also normal cells. As the preferential ligand for targeting tumor cells, we focused on 5-aminolevulinic acid (5ALA), which is known as the heme precursor. In this study, the ligand potency of ALA was investigated by comparing the amount of cellular uptake of ALA into the normal cell and that into cancer cell. To evaluate the amount of cellular uptake, ALA was labeled with fluorescent compound. ALA was conjugated with 4-aminofluorescein in three steps. RGM cell which is a cell line derived from normal gastric mucosa of rat and RGK cell which is rat gastric carcinoma mucosal cells were seeded into 24 well plate at a density 1x1O^5 cells/well for 12h. The cells were exposed to each of labelled ALA (ALAFL) or 4-aminofluorescein (FL). The cellular uptakes of each compound were measured using flow cytometer, at 488 nm excitation and 510〜540 nm emission wavelength at time course. The ability to target cancer cell was also evaluated by the comparison between the amount of cellular uptake by RGK and that by RGM. It is clearly shown that the uptake of ALAFL by RGK was amazingly higher than by RGM. Actually, in contrast to FL which was taken up 2.5 times higher by RGK than by RGM, the amount of ALA-FL uptake by RGK was 14 times higher than that by RGM. On the basis of this experiment, it is confirmed that preferential ALA-FL uptake into carcinoma cell indeed took place. ALA-FL is thus, a promising compound, which improve preferential uptake of versatile compounds such as peptide, and drug vehicles to cancerous cells.

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