Comparative Hepatoprotective Effects of Esculetin and Its Derivatives Against Oxidative Stress
In this study, we evaluated the antioxidant activities of esculetin and four synthesized derivatives (E1, 2-oxo-2H-1-benzopyran-6,7-diyl diacetate; E2, 7-hydroxy-2-oxo-2H-1-benzopyran-6-yl acetate; E3, 7-(methoxymethoxy)-2-oxo-2H-1-benzopyran-6-yl acetate; E4, 7-hydroxy-2-oxo-2H-1-benzopyran-6-yl 2,...
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MDPI AG
2025-06-01
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| Series: | Antioxidants |
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| author | Yoonjeong Kim Jihyun Kwon Jae-Hwan Kwak In-hwan Baek Younghwa Kim |
| author_facet | Yoonjeong Kim Jihyun Kwon Jae-Hwan Kwak In-hwan Baek Younghwa Kim |
| author_sort | Yoonjeong Kim |
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| description | In this study, we evaluated the antioxidant activities of esculetin and four synthesized derivatives (E1, 2-oxo-2H-1-benzopyran-6,7-diyl diacetate; E2, 7-hydroxy-2-oxo-2H-1-benzopyran-6-yl acetate; E3, 7-(methoxymethoxy)-2-oxo-2H-1-benzopyran-6-yl acetate; E4, 7-hydroxy-2-oxo-2H-1-benzopyran-6-yl 2,4-dinitrobenzene-1-sulfonate) against oxidative stress in hepatocytes. In HepG2 cells, treatment with 1 mM <i>tert</i>-butyl hydroperoxide (TBHP) reduced cell viability to 40%, while co-treatment with esculetin restored cell viability. Among the esculetin derivatives, E2 exhibited the most significant cytoprotective effect, while E4 showed the lowest. Furthermore, E2 at 25 µM concentration showed the similar effects to esculetin in reducing ROS generation and preventing glutathione depletion. The treatment of E2 also enhanced the expression of HO-1 and GCLC proteins against oxidative stress. On the other hand, TBHP-induced oxidative stress decreased antioxidant activities including glutathione reductase, glutathione peroxidase, and catalase; however, E2 significantly increased these antioxidant activities. These findings suggest that the esculetin derivative, particularly E2, possesses potential as an antioxidant aimed at enhancing physiological functions. |
| format | Article |
| id | doaj-art-e514580a31d24f4784d9a7d8f28486cb |
| institution | Matheson Library |
| issn | 2076-3921 |
| language | English |
| publishDate | 2025-06-01 |
| publisher | MDPI AG |
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| series | Antioxidants |
| spelling | doaj-art-e514580a31d24f4784d9a7d8f28486cb2025-07-25T13:11:35ZengMDPI AGAntioxidants2076-39212025-06-0114778710.3390/antiox14070787Comparative Hepatoprotective Effects of Esculetin and Its Derivatives Against Oxidative StressYoonjeong Kim0Jihyun Kwon1Jae-Hwan Kwak2In-hwan Baek3Younghwa Kim4Department of Food Science and Biotechnology, Kyungsung University, Busan 48434, Republic of KoreaDepartment of Food Science and Biotechnology, Kyungsung University, Busan 48434, Republic of KoreaCollege of Pharmacy, Chungbuk National University, Cheongju 28160, Republic of KoreaCollege of Pharmacy, Kyungsung University, Busan 48434, Republic of KoreaDepartment of Food Science and Biotechnology, Kyungsung University, Busan 48434, Republic of KoreaIn this study, we evaluated the antioxidant activities of esculetin and four synthesized derivatives (E1, 2-oxo-2H-1-benzopyran-6,7-diyl diacetate; E2, 7-hydroxy-2-oxo-2H-1-benzopyran-6-yl acetate; E3, 7-(methoxymethoxy)-2-oxo-2H-1-benzopyran-6-yl acetate; E4, 7-hydroxy-2-oxo-2H-1-benzopyran-6-yl 2,4-dinitrobenzene-1-sulfonate) against oxidative stress in hepatocytes. In HepG2 cells, treatment with 1 mM <i>tert</i>-butyl hydroperoxide (TBHP) reduced cell viability to 40%, while co-treatment with esculetin restored cell viability. Among the esculetin derivatives, E2 exhibited the most significant cytoprotective effect, while E4 showed the lowest. Furthermore, E2 at 25 µM concentration showed the similar effects to esculetin in reducing ROS generation and preventing glutathione depletion. The treatment of E2 also enhanced the expression of HO-1 and GCLC proteins against oxidative stress. On the other hand, TBHP-induced oxidative stress decreased antioxidant activities including glutathione reductase, glutathione peroxidase, and catalase; however, E2 significantly increased these antioxidant activities. These findings suggest that the esculetin derivative, particularly E2, possesses potential as an antioxidant aimed at enhancing physiological functions.https://www.mdpi.com/2076-3921/14/7/787esculetinderivativesantioxidant activityROSHepG2 cells |
| spellingShingle | Yoonjeong Kim Jihyun Kwon Jae-Hwan Kwak In-hwan Baek Younghwa Kim Comparative Hepatoprotective Effects of Esculetin and Its Derivatives Against Oxidative Stress Antioxidants esculetin derivatives antioxidant activity ROS HepG2 cells |
| title | Comparative Hepatoprotective Effects of Esculetin and Its Derivatives Against Oxidative Stress |
| title_full | Comparative Hepatoprotective Effects of Esculetin and Its Derivatives Against Oxidative Stress |
| title_fullStr | Comparative Hepatoprotective Effects of Esculetin and Its Derivatives Against Oxidative Stress |
| title_full_unstemmed | Comparative Hepatoprotective Effects of Esculetin and Its Derivatives Against Oxidative Stress |
| title_short | Comparative Hepatoprotective Effects of Esculetin and Its Derivatives Against Oxidative Stress |
| title_sort | comparative hepatoprotective effects of esculetin and its derivatives against oxidative stress |
| topic | esculetin derivatives antioxidant activity ROS HepG2 cells |
| url | https://www.mdpi.com/2076-3921/14/7/787 |
| work_keys_str_mv | AT yoonjeongkim comparativehepatoprotectiveeffectsofesculetinanditsderivativesagainstoxidativestress AT jihyunkwon comparativehepatoprotectiveeffectsofesculetinanditsderivativesagainstoxidativestress AT jaehwankwak comparativehepatoprotectiveeffectsofesculetinanditsderivativesagainstoxidativestress AT inhwanbaek comparativehepatoprotectiveeffectsofesculetinanditsderivativesagainstoxidativestress AT younghwakim comparativehepatoprotectiveeffectsofesculetinanditsderivativesagainstoxidativestress |