The transport mechanism of monocarboxylate transporter on spinosin in Caco-2 cells
Objectives: The aim of this study was to determine the uptake mechanism of spinosin (SPI) by the monocarboxylic acid transporters (MCTs) in Caco-2 cells. Methods: The Caco-2 cells were pretreated with various monocarboxylic acids, and the uptake of spinosin from Caco-2 cells was measured by High Per...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2016-05-01
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| Series: | Saudi Pharmaceutical Journal |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319016416300226 |
| _version_ | 1819098393950027776 |
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| author | Xiang Le Meng Yan Li Guo Hai Ying Huang |
| author_facet | Xiang Le Meng Yan Li Guo Hai Ying Huang |
| author_sort | Xiang Le Meng |
| collection | DOAJ |
| description | Objectives: The aim of this study was to determine the uptake mechanism of spinosin (SPI) by the monocarboxylic acid transporters (MCTs) in Caco-2 cells. Methods: The Caco-2 cells were pretreated with various monocarboxylic acids, and the uptake of spinosin from Caco-2 cells was measured by High Performance Liquid Chromatography (HPLC). Key findings: Preloading of various monocarboxylic acids enhanced the uptake of SPI, especially salicylic acid (a substrate of MCTs) had a 23.4 times increase in SPI uptake, indicating that the monocarboxylic acid transporters had an efflux effect on SPI uptake and salicylic acid had a strong inhibition on SPI efflux in Caco-2 cells. At the same time, the uptake of SPI through Caco-2 cells was Na+- and temperature-dependent, pretreatment without Na+ significantly increased the uptake of SPI by 1.85 times and incubated at low temperature (4 °C) SPI uptake increased 20% than that of 37 °C. Furthermore, SPI was transported mainly via a carrier-mediated transport: [Vmax = 5.364 μg/mg protein, Km = 657.0 μg/mL]. Conclusion: The uptake of spinosin (SPI) in Caco-2 cells was mainly regulated by the monocarboxylic acid transporters along with Salicylic acid. |
| first_indexed | 2024-12-22T00:30:17Z |
| format | Article |
| id | doaj.art-f834f2401bb24076a56829a1a819ea41 |
| institution | Directory Open Access Journal |
| issn | 1319-0164 |
| language | English |
| last_indexed | 2024-12-22T00:30:17Z |
| publishDate | 2016-05-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Saudi Pharmaceutical Journal |
| spelling | doaj.art-f834f2401bb24076a56829a1a819ea412022-12-21T18:44:57ZengElsevierSaudi Pharmaceutical Journal1319-01642016-05-0124328629110.1016/j.jsps.2016.04.021The transport mechanism of monocarboxylate transporter on spinosin in Caco-2 cellsXiang Le Meng0Yan Li Guo1Hai Ying Huang2The First Affiliated Hospital of Henan University of Traditional Chinese Medicine, Zhengzhou, ChinaDiscipline of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou, ChinaDiscipline of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou, ChinaObjectives: The aim of this study was to determine the uptake mechanism of spinosin (SPI) by the monocarboxylic acid transporters (MCTs) in Caco-2 cells. Methods: The Caco-2 cells were pretreated with various monocarboxylic acids, and the uptake of spinosin from Caco-2 cells was measured by High Performance Liquid Chromatography (HPLC). Key findings: Preloading of various monocarboxylic acids enhanced the uptake of SPI, especially salicylic acid (a substrate of MCTs) had a 23.4 times increase in SPI uptake, indicating that the monocarboxylic acid transporters had an efflux effect on SPI uptake and salicylic acid had a strong inhibition on SPI efflux in Caco-2 cells. At the same time, the uptake of SPI through Caco-2 cells was Na+- and temperature-dependent, pretreatment without Na+ significantly increased the uptake of SPI by 1.85 times and incubated at low temperature (4 °C) SPI uptake increased 20% than that of 37 °C. Furthermore, SPI was transported mainly via a carrier-mediated transport: [Vmax = 5.364 μg/mg protein, Km = 657.0 μg/mL]. Conclusion: The uptake of spinosin (SPI) in Caco-2 cells was mainly regulated by the monocarboxylic acid transporters along with Salicylic acid.http://www.sciencedirect.com/science/article/pii/S1319016416300226Spinosin (SPI)Monocarboxylic acid transporters (MCTs)Salicylic acidCaco-2 cells |
| spellingShingle | Xiang Le Meng Yan Li Guo Hai Ying Huang The transport mechanism of monocarboxylate transporter on spinosin in Caco-2 cells Saudi Pharmaceutical Journal Spinosin (SPI) Monocarboxylic acid transporters (MCTs) Salicylic acid Caco-2 cells |
| title | The transport mechanism of monocarboxylate transporter on spinosin in Caco-2 cells |
| title_full | The transport mechanism of monocarboxylate transporter on spinosin in Caco-2 cells |
| title_fullStr | The transport mechanism of monocarboxylate transporter on spinosin in Caco-2 cells |
| title_full_unstemmed | The transport mechanism of monocarboxylate transporter on spinosin in Caco-2 cells |
| title_short | The transport mechanism of monocarboxylate transporter on spinosin in Caco-2 cells |
| title_sort | transport mechanism of monocarboxylate transporter on spinosin in caco 2 cells |
| topic | Spinosin (SPI) Monocarboxylic acid transporters (MCTs) Salicylic acid Caco-2 cells |
| url | http://www.sciencedirect.com/science/article/pii/S1319016416300226 |
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