Effects of perfluoroalkyl carboxylic acids on the uptake of sulfobromophthalein via organic anion transporting polypeptides in human intestinal Caco-2 cells
We performed a detailed investigation of the uptake of sulfobromophthalein (BSP) from the apical membrane of Caco-2 cells, which is a substrate for organic anion transporting polypeptides (OATPs), and calculated the kinetic parameters of BSP uptake as follows: Km = 13.9 ± 1.3 μM, Vmax = 1.15 ± 0.07 ...
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Elsevier
2020-12-01
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| Series: | Biochemistry and Biophysics Reports |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2405580820301175 |
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| author | Osamu Kimura Yukiko Fujii Koichi Haraguchi Yoshihisa Kato Chiho Ohta Nobuyuki Koga Tetsuya Endo |
| author_facet | Osamu Kimura Yukiko Fujii Koichi Haraguchi Yoshihisa Kato Chiho Ohta Nobuyuki Koga Tetsuya Endo |
| author_sort | Osamu Kimura |
| collection | DOAJ |
| description | We performed a detailed investigation of the uptake of sulfobromophthalein (BSP) from the apical membrane of Caco-2 cells, which is a substrate for organic anion transporting polypeptides (OATPs), and calculated the kinetic parameters of BSP uptake as follows: Km = 13.9 ± 1.3 μM, Vmax = 1.15 ± 0.07 nmol (mg protein)−1 (5 min)−1, and kd = 38.2 ± 0.53 μL (mg protein)−1 (5 min)−1. Coincubation with medium-chain (C7–C11) perfluoroalkyl carboxylic acids (PFCAs), such as perfluoroheptanoic acid (PFHpA, C7), perfluorooctanoic acid (PFOA, C8), perfluorononanoic acid (PFNA, C9), perfluorodecanoic acid (PFDA, C10) and perfluoroundecanoic acid (PFUnDA, C11), significantly decreased BSP uptake by 27–55%, while coincubation with short- (C3–C6) and long-chain (C12–C14) PFCAs decreased the uptake only slightly. Dixon plotting suggested that PFOA, PFNA and PFDA competitively inhibited the BSP uptake with inhibition constant (Ki) values of 62.2 ± 1.3 μM, 35.3 ± 0.1 μM and 43.2 ± 0.3 μM, respectively. PFCAs with medium-chains could be substrates for OATPs, probably OATP2B1, which is the most abundantly expressed OATP isoform in Caco-2 cells. |
| first_indexed | 2024-12-14T20:44:40Z |
| format | Article |
| id | doaj.art-facffe5b81eb4298b941facf76816c5a |
| institution | Directory Open Access Journal |
| issn | 2405-5808 |
| language | English |
| last_indexed | 2024-12-14T20:44:40Z |
| publishDate | 2020-12-01 |
| publisher | Elsevier |
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| series | Biochemistry and Biophysics Reports |
| spelling | doaj.art-facffe5b81eb4298b941facf76816c5a2022-12-21T22:48:07ZengElsevierBiochemistry and Biophysics Reports2405-58082020-12-0124100807Effects of perfluoroalkyl carboxylic acids on the uptake of sulfobromophthalein via organic anion transporting polypeptides in human intestinal Caco-2 cellsOsamu Kimura0Yukiko Fujii1Koichi Haraguchi2Yoshihisa Kato3Chiho Ohta4Nobuyuki Koga5Tetsuya Endo6School of Pharmaceutical Sciences, Health Sciences University of Hokkaido, 1757 Kanazawa, Ishikari-Tobetsu, Hokkaido, 061-0293, Japan; Corresponding author.Daiichi University of Pharmacy, Tamagawa-cho, Minami-ku, Fukuoka, 815-8511, JapanDaiichi University of Pharmacy, Tamagawa-cho, Minami-ku, Fukuoka, 815-8511, JapanKagawa School of Pharmaceutical Sciences, Tokushima Bunri University, Sanuki, Kagawa, 769-2193, JapanFaculty of Nutritional Sciences, Nakamura Gakuen University, Johnan-ku, Fukuoka, 814-0198, JapanFaculty of Nutritional Sciences, Nakamura Gakuen University, Johnan-ku, Fukuoka, 814-0198, JapanSchool of Pharmaceutical Sciences, Health Sciences University of Hokkaido, 1757 Kanazawa, Ishikari-Tobetsu, Hokkaido, 061-0293, JapanWe performed a detailed investigation of the uptake of sulfobromophthalein (BSP) from the apical membrane of Caco-2 cells, which is a substrate for organic anion transporting polypeptides (OATPs), and calculated the kinetic parameters of BSP uptake as follows: Km = 13.9 ± 1.3 μM, Vmax = 1.15 ± 0.07 nmol (mg protein)−1 (5 min)−1, and kd = 38.2 ± 0.53 μL (mg protein)−1 (5 min)−1. Coincubation with medium-chain (C7–C11) perfluoroalkyl carboxylic acids (PFCAs), such as perfluoroheptanoic acid (PFHpA, C7), perfluorooctanoic acid (PFOA, C8), perfluorononanoic acid (PFNA, C9), perfluorodecanoic acid (PFDA, C10) and perfluoroundecanoic acid (PFUnDA, C11), significantly decreased BSP uptake by 27–55%, while coincubation with short- (C3–C6) and long-chain (C12–C14) PFCAs decreased the uptake only slightly. Dixon plotting suggested that PFOA, PFNA and PFDA competitively inhibited the BSP uptake with inhibition constant (Ki) values of 62.2 ± 1.3 μM, 35.3 ± 0.1 μM and 43.2 ± 0.3 μM, respectively. PFCAs with medium-chains could be substrates for OATPs, probably OATP2B1, which is the most abundantly expressed OATP isoform in Caco-2 cells.http://www.sciencedirect.com/science/article/pii/S2405580820301175Perfluoroalkyl carboxylic acids (PFCAs)Sulfobromophthalein (BSP)Intestinal absorptionOrganic anion transport polypeptides (OATPs)Caco-2 cells |
| spellingShingle | Osamu Kimura Yukiko Fujii Koichi Haraguchi Yoshihisa Kato Chiho Ohta Nobuyuki Koga Tetsuya Endo Effects of perfluoroalkyl carboxylic acids on the uptake of sulfobromophthalein via organic anion transporting polypeptides in human intestinal Caco-2 cells Biochemistry and Biophysics Reports Perfluoroalkyl carboxylic acids (PFCAs) Sulfobromophthalein (BSP) Intestinal absorption Organic anion transport polypeptides (OATPs) Caco-2 cells |
| title | Effects of perfluoroalkyl carboxylic acids on the uptake of sulfobromophthalein via organic anion transporting polypeptides in human intestinal Caco-2 cells |
| title_full | Effects of perfluoroalkyl carboxylic acids on the uptake of sulfobromophthalein via organic anion transporting polypeptides in human intestinal Caco-2 cells |
| title_fullStr | Effects of perfluoroalkyl carboxylic acids on the uptake of sulfobromophthalein via organic anion transporting polypeptides in human intestinal Caco-2 cells |
| title_full_unstemmed | Effects of perfluoroalkyl carboxylic acids on the uptake of sulfobromophthalein via organic anion transporting polypeptides in human intestinal Caco-2 cells |
| title_short | Effects of perfluoroalkyl carboxylic acids on the uptake of sulfobromophthalein via organic anion transporting polypeptides in human intestinal Caco-2 cells |
| title_sort | effects of perfluoroalkyl carboxylic acids on the uptake of sulfobromophthalein via organic anion transporting polypeptides in human intestinal caco 2 cells |
| topic | Perfluoroalkyl carboxylic acids (PFCAs) Sulfobromophthalein (BSP) Intestinal absorption Organic anion transport polypeptides (OATPs) Caco-2 cells |
| url | http://www.sciencedirect.com/science/article/pii/S2405580820301175 |
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