A Model In Vitro Study Using Hypericin: Tumor-Versus Necrosis-Targeting Property and Possible Mechanisms
Hypericin (Hyp) had been explored as a tumor-seeking agent for years; however, more recent studies showed its necrosis-avidity rather than cancer-seeking property. To further look into this discrepancy, we conducted an in vitro study on Hyp retention in vital and dead cancerous HepG2 and normal LO2...
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MDPI AG
2020-01-01
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| Online Access: | https://www.mdpi.com/2079-7737/9/1/13 |
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| author | Yue Li Shuncong Wang Yuanyu Zhao Hexige Saiyin Xiaoyan He Juanzhi Zhao Ling Li Ali Talebi Gang Huang Yicheng Ni |
| author_facet | Yue Li Shuncong Wang Yuanyu Zhao Hexige Saiyin Xiaoyan He Juanzhi Zhao Ling Li Ali Talebi Gang Huang Yicheng Ni |
| author_sort | Yue Li |
| collection | DOAJ |
| description | Hypericin (Hyp) had been explored as a tumor-seeking agent for years; however, more recent studies showed its necrosis-avidity rather than cancer-seeking property. To further look into this discrepancy, we conducted an in vitro study on Hyp retention in vital and dead cancerous HepG2 and normal LO2 cell lines by measuring the fluorescence intensity and concentration of Hyp in cells. To question the DNA binding theory for its necrosis-avidity, the subcellular distribution of Hyp was also investigated to explore the possible mechanisms of the necrosis avidity. The fluorescence intensity and concentration are significantly higher in dead cells than those in vital cells, and this difference did not differ between HepG2 and LO2 cell lines. Hyp was taken up in vital cells in the early phase and excreted within hours, whereas it was retained in dead cells for more than two days. Confocal microscopy showed that Hyp selectively accumulated in lysosomes rather than cell membrane or nuclei. Hyp showed a necrosis-avid property rather than cancer-targetability. The long-lasting retention of Hyp in dead cells may be associated with halted energy metabolism and/or binding with certain degraded cellular substrates. Necrosis-avidity of Hyp was confirmed, which may be associated with halted energy metabolism in dead LO2 or HepG2 cells. |
| first_indexed | 2024-03-12T08:14:00Z |
| format | Article |
| id | doaj.art-8b3b7b07366f4e07b3b243a724eb2cc8 |
| institution | Directory Open Access Journal |
| issn | 2079-7737 |
| language | English |
| last_indexed | 2024-03-12T08:14:00Z |
| publishDate | 2020-01-01 |
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| series | Biology |
| spelling | doaj.art-8b3b7b07366f4e07b3b243a724eb2cc82023-09-02T19:03:00ZengMDPI AGBiology2079-77372020-01-01911310.3390/biology9010013biology9010013A Model In Vitro Study Using Hypericin: Tumor-Versus Necrosis-Targeting Property and Possible MechanismsYue Li0Shuncong Wang1Yuanyu Zhao2Hexige Saiyin3Xiaoyan He4Juanzhi Zhao5Ling Li6Ali Talebi7Gang Huang8Yicheng Ni9Shanghai Key Laboratory of Molecular Imaging, Shanghai University of Medicine and Health Sciences, Shanghai 201318, ChinaKU Leuven, Campus Gasthuisberg, Faculty of Medicine, 3000 Leuven, BelgiumTechnology Center of Chongqing Entry-Exit Inspection and Quarantine Bureau, Chongqing 401147, ChinaState Key Laboratory of Genetic Engineering, School of Life Sciences, Fudan University, Shanghai 200433, ChinaShanghai Key Laboratory of Molecular Imaging, Shanghai University of Medicine and Health Sciences, Shanghai 201318, ChinaLaboratory of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, ChinaLaboratory of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, ChinaKU Leuven, Campus Gasthuisberg, Faculty of Medicine, 3000 Leuven, BelgiumShanghai Key Laboratory of Molecular Imaging, Shanghai University of Medicine and Health Sciences, Shanghai 201318, ChinaKU Leuven, Campus Gasthuisberg, Faculty of Medicine, 3000 Leuven, BelgiumHypericin (Hyp) had been explored as a tumor-seeking agent for years; however, more recent studies showed its necrosis-avidity rather than cancer-seeking property. To further look into this discrepancy, we conducted an in vitro study on Hyp retention in vital and dead cancerous HepG2 and normal LO2 cell lines by measuring the fluorescence intensity and concentration of Hyp in cells. To question the DNA binding theory for its necrosis-avidity, the subcellular distribution of Hyp was also investigated to explore the possible mechanisms of the necrosis avidity. The fluorescence intensity and concentration are significantly higher in dead cells than those in vital cells, and this difference did not differ between HepG2 and LO2 cell lines. Hyp was taken up in vital cells in the early phase and excreted within hours, whereas it was retained in dead cells for more than two days. Confocal microscopy showed that Hyp selectively accumulated in lysosomes rather than cell membrane or nuclei. Hyp showed a necrosis-avid property rather than cancer-targetability. The long-lasting retention of Hyp in dead cells may be associated with halted energy metabolism and/or binding with certain degraded cellular substrates. Necrosis-avidity of Hyp was confirmed, which may be associated with halted energy metabolism in dead LO2 or HepG2 cells.https://www.mdpi.com/2079-7737/9/1/13hypericinnecrosis-avidityliver cancerfluorescenceconfocal microscopy and mechanism |
| spellingShingle | Yue Li Shuncong Wang Yuanyu Zhao Hexige Saiyin Xiaoyan He Juanzhi Zhao Ling Li Ali Talebi Gang Huang Yicheng Ni A Model In Vitro Study Using Hypericin: Tumor-Versus Necrosis-Targeting Property and Possible Mechanisms Biology hypericin necrosis-avidity liver cancer fluorescence confocal microscopy and mechanism |
| title | A Model In Vitro Study Using Hypericin: Tumor-Versus Necrosis-Targeting Property and Possible Mechanisms |
| title_full | A Model In Vitro Study Using Hypericin: Tumor-Versus Necrosis-Targeting Property and Possible Mechanisms |
| title_fullStr | A Model In Vitro Study Using Hypericin: Tumor-Versus Necrosis-Targeting Property and Possible Mechanisms |
| title_full_unstemmed | A Model In Vitro Study Using Hypericin: Tumor-Versus Necrosis-Targeting Property and Possible Mechanisms |
| title_short | A Model In Vitro Study Using Hypericin: Tumor-Versus Necrosis-Targeting Property and Possible Mechanisms |
| title_sort | model in vitro study using hypericin tumor versus necrosis targeting property and possible mechanisms |
| topic | hypericin necrosis-avidity liver cancer fluorescence confocal microscopy and mechanism |
| url | https://www.mdpi.com/2079-7737/9/1/13 |
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