Gallic acid-mitochondria targeting sequence-H3R9 induces mitochondria-targeted cytoprotection
10.4196/kjpp.2022.26.1.15
- Author:
Yoonhee BAE
1
;
Goo-Young KIM
;
Flores JESSA
;
Kyung Soo KO
;
Jin HAN
Author Information
1. Department of Physiology, Cardiovascular and Metabolic Disease Center, Smart Marine Therapeutic Center, Inje University College of Medicine, Busan 47392, Korea
- Publication Type:Original Article
- From:The Korean Journal of Physiology and Pharmacology
2022;26(1):15-24
- CountryRepublic of Korea
- Language:English
-
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.
