KMID : 0811720220260010015
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Korean Journal of Physiology & Pharmacology 2022 Volume.26 No. 1 p.15 ~ p.24
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Gallic acid-mitochondria targeting sequence-H3R9 induces mitochondria-targeted cytoprotection
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Bae Yoon-Hee
Kim Goo-Young Jessa Flores Ko Kyung-Soo Han Jin
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Abstract
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The development of selective targeting of drug molecules towards the mitochondria is an important issue related to therapy efficacy. In this study, we report that gallic acid (GA)-mitochondria targeting sequence (MTS)-H3R9 exhibits a dual role as a mitochondria-targeting vehicle with antioxidant activity for disease therapy. In viability assays, GA-MTS-H3R9 showed a better rescue action compared to that of MTS-H3R9. GA-MTS-H3R9 dramatically exhibited cell penetration and intercellular uptake compared to MTS and fit escape from lysosome release to the cytosol. We demonstrated the useful targeting of GA-MTS-H3R9 towards mitochondria in AC16 cells. Also, we observed that the antioxidant properties of mitochondrial-accrued GA-MTSH3R9 alleviated cell damage by reactive oxygen species production and disrupted mitochondrial membrane potential. GA-MTS-H3R9 showed a very increased cytoprotective effect against anticancer activity compared to that of MTS-H3R9. We showed that GA-MTS-H3R9 can act as a vehicle for mitochondria-targeting and as a reagent for therapeutic applications intended for cardiovascular disease treatment.
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KEYWORD
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Antioxidant activity, Gallic acid, Mitochondria
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