Methyl-Cantharidimide (MCA) Has Anticancer Efficacy in ABCB1- and ABCG2-Overexpressing and Cisplatin Resistant Cancer Cells
Copyright © 2020 Li, Mao, Dong, Lei, Yang, Lin, Ashby, Yang, Fan and Chen..
In this study, we investigated the efficacy of methyl-cantharidimide (MCA), a cantharidin (CTD) analog, as an anticancer drug, in cancer cells overexpressing either ABCB1 or ABCG2 transporters and in cisplatin-resistant cancer cells. The results indicated that: (i) MCA was efficacious in the ABCB1-overexpressing cell line, KB-C2, and the ABCB1-gene-transfected cell line, HEK293/ABCB1 (IC50 from 6.37 to 8.44 mM); (ii) MCA was also efficacious in the ABCG2-overexpressing cell line, NCI-H460/MX20, and the ABCG2-gene-transfected cell lines, HEK293/ABCG2-482-R2, HEK293/ABCG2-482-G2, and the HEK293/ABCG2-482-T7 cell lines (IC50 from 6.37 to 9.70 mM); (iii) MCA was efficacious in the cisplatin resistant cancer cell lines, KCP-4 and BEL-7404/CP20 (IC50 values from 7.05 to 8.16 mM); (iv) MCA (up to 16 mM) induced apoptosis in both BEL-7404 and BEL-7404/CP20 cancer cells; (v) MCA arrested both BEL-7404 and BEL-7404/CP20 cancer cells in the G0/G1 phase of the cell cycle; (vi) MCA (8 mM) upregulated the expression level of the protein, unc-5 netrin receptor B (UNC5B) in HepG2 and BEL-7404 cancer cells. Overall, our results indicated that MCA's efficacy in ABCB1- and ABCG2-overexpressing and cisplatin resistant cancer cells is due to the induction of apoptosis and cell cycle arrest in the G0/G1 phase.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:10 |
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| Enthalten in: |
Frontiers in oncology - 10(2020) vom: 03., Seite 932 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Li, Yi-Dong [VerfasserIn] |
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| Links: |
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| Themen: |
ABCB1 |
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| Anmerkungen: |
Date Revised 28.09.2020 published: Electronic-eCollection Citation Status PubMed-not-MEDLINE |
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| doi: |
10.3389/fonc.2020.00932 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Copyright © 2020 Li, Mao, Dong, Lei, Yang, Lin, Ashby, Yang, Fan and Chen. | ||
| 520 | |a In this study, we investigated the efficacy of methyl-cantharidimide (MCA), a cantharidin (CTD) analog, as an anticancer drug, in cancer cells overexpressing either ABCB1 or ABCG2 transporters and in cisplatin-resistant cancer cells. The results indicated that: (i) MCA was efficacious in the ABCB1-overexpressing cell line, KB-C2, and the ABCB1-gene-transfected cell line, HEK293/ABCB1 (IC50 from 6.37 to 8.44 mM); (ii) MCA was also efficacious in the ABCG2-overexpressing cell line, NCI-H460/MX20, and the ABCG2-gene-transfected cell lines, HEK293/ABCG2-482-R2, HEK293/ABCG2-482-G2, and the HEK293/ABCG2-482-T7 cell lines (IC50 from 6.37 to 9.70 mM); (iii) MCA was efficacious in the cisplatin resistant cancer cell lines, KCP-4 and BEL-7404/CP20 (IC50 values from 7.05 to 8.16 mM); (iv) MCA (up to 16 mM) induced apoptosis in both BEL-7404 and BEL-7404/CP20 cancer cells; (v) MCA arrested both BEL-7404 and BEL-7404/CP20 cancer cells in the G0/G1 phase of the cell cycle; (vi) MCA (8 mM) upregulated the expression level of the protein, unc-5 netrin receptor B (UNC5B) in HepG2 and BEL-7404 cancer cells. Overall, our results indicated that MCA's efficacy in ABCB1- and ABCG2-overexpressing and cisplatin resistant cancer cells is due to the induction of apoptosis and cell cycle arrest in the G0/G1 phase | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a ABCB1 | |
| 650 | 4 | |a ABCG2 | |
| 650 | 4 | |a cell apoptosis | |
| 650 | 4 | |a cisplatin resistance | |
| 650 | 4 | |a methyl-cantharidimide (MCA) | |
| 650 | 4 | |a multidrug resistance (MDR) | |
| 650 | 4 | |a unc-5 netrin receptor B (UNC5B) | |
| 700 | 1 | |a Mao, Yong |e verfasserin |4 aut | |
| 700 | 1 | |a Dong, Xing-Duo |e verfasserin |4 aut | |
| 700 | 1 | |a Lei, Zi-Ning |e verfasserin |4 aut | |
| 700 | 1 | |a Yang, Yuqi |e verfasserin |4 aut | |
| 700 | 1 | |a Lin, Lizhu |e verfasserin |4 aut | |
| 700 | 1 | |a Ashby, Charles R |c Jr |e verfasserin |4 aut | |
| 700 | 1 | |a Yang, Dong-Hua |e verfasserin |4 aut | |
| 700 | 1 | |a Fan, Ying-Fang |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Zhe-Sheng |e verfasserin |4 aut | |
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