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Gallic acid-mitochondria targeting sequence-H3R9 induces mitochondria-targeted cytoprotection.


ABSTRACT: 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.

SUBMITTER: Bae Y 

PROVIDER: S-EPMC8723982 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature

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Gallic acid-mitochondria targeting sequence-H<sub>3</sub>R<sub>9</sub> induces mitochondria-targeted cytoprotection.

Bae Yoonhee Y   Kim Goo-Young GY   Jessa Flores F   Ko Kyung Soo KS   Han Jin J  

The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology 20220101 1


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)-H<sub>3</sub>R<sub>9</sub> exhibits a dual role as a mitochondria-targeting vehicle with antioxidant activity for disease therapy. In viability assays, GA-MTS-H<sub>3</sub>R<sub>9</sub> showed a better rescue action compared to that of MTS-H<sub>3</sub>R<sub>9</sub>. GA-MTS-H<sub>3  ...[more]

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