Anti-Inflammatory Activity of Chlorogenic Acid on Macrophages: A Simplified Simulation of Pharmacokinetics Following Ingestion Using a Windup Syringe Pump
Cell-culture-based drug tests are usually performed in an instantaneous delivery manner. However, in vivo pharmacokinetic studies have shown a steady increase in the concentration of bioactive compounds in the plasma following oral administration, with the maximum concentration observed after severa...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-01-01
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| Series: | Applied Sciences |
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| Online Access: | https://www.mdpi.com/2076-3417/13/1/627 |
| _version_ | 1797626225013817344 |
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| author | Lei Cao Won Han Sang Gil Lee Joong Ho Shin |
| author_facet | Lei Cao Won Han Sang Gil Lee Joong Ho Shin |
| author_sort | Lei Cao |
| collection | DOAJ |
| description | Cell-culture-based drug tests are usually performed in an instantaneous delivery manner. However, in vivo pharmacokinetic studies have shown a steady increase in the concentration of bioactive compounds in the plasma following oral administration, with the maximum concentration observed after several hours. Here, a novel palm-sized syringe pump powered by the manual winding of a spring was utilized for sustained delivery of chlorogenic acid (CHA) to lipopolysaccharide (LPS)-challenged RAW 264.7 macrophages over 2 h. When delivered in a sustained manner and simulating the in vivo pharmacokinetics following oral administration, CHA showed a stronger inhibitory effect on LPS-induced expression of inducible nitric oxide synthase and the transcription and secretion of pro-inflammatory cytokines, such as tumor necrosis factor-α. It also enhanced the mRNA expression of the gene encoding heme oxygenase 1. The suppression of phosphorylation of p38 but not the nuclear translocation of nuclear factor-κB was affected by the sustained delivery of CHA. High-performance liquid chromatography analysis indicated that the sustained delivery model showed a higher concentration of CHA in the conditioned medium two hours after starting the delivery. A stronger anti-inflammatory effect of CHA was observed upon sustained delivery to the cell medium, simulating an in vivo pharmacokinetic release profile following oral administration. |
| first_indexed | 2024-03-11T10:07:23Z |
| format | Article |
| id | doaj.art-ed7f7afe3ebd4984b9c572d39774814f |
| institution | Directory Open Access Journal |
| issn | 2076-3417 |
| language | English |
| last_indexed | 2024-03-11T10:07:23Z |
| publishDate | 2023-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Applied Sciences |
| spelling | doaj.art-ed7f7afe3ebd4984b9c572d39774814f2023-11-16T14:59:35ZengMDPI AGApplied Sciences2076-34172023-01-0113162710.3390/app13010627Anti-Inflammatory Activity of Chlorogenic Acid on Macrophages: A Simplified Simulation of Pharmacokinetics Following Ingestion Using a Windup Syringe PumpLei Cao0Won Han1Sang Gil Lee2Joong Ho Shin3Department of Biomedical Engineering, Pukyong National University, Busan 48513, Republic of KoreaIndustry 4.0 Convergence Bionics Engineering, Pukyong National University, Busan 48513, Republic of KoreaDepartment of Food Science and Nutrition, Pukyong National University, Busan 48513, Republic of KoreaDepartment of Biomedical Engineering, Pukyong National University, Busan 48513, Republic of KoreaCell-culture-based drug tests are usually performed in an instantaneous delivery manner. However, in vivo pharmacokinetic studies have shown a steady increase in the concentration of bioactive compounds in the plasma following oral administration, with the maximum concentration observed after several hours. Here, a novel palm-sized syringe pump powered by the manual winding of a spring was utilized for sustained delivery of chlorogenic acid (CHA) to lipopolysaccharide (LPS)-challenged RAW 264.7 macrophages over 2 h. When delivered in a sustained manner and simulating the in vivo pharmacokinetics following oral administration, CHA showed a stronger inhibitory effect on LPS-induced expression of inducible nitric oxide synthase and the transcription and secretion of pro-inflammatory cytokines, such as tumor necrosis factor-α. It also enhanced the mRNA expression of the gene encoding heme oxygenase 1. The suppression of phosphorylation of p38 but not the nuclear translocation of nuclear factor-κB was affected by the sustained delivery of CHA. High-performance liquid chromatography analysis indicated that the sustained delivery model showed a higher concentration of CHA in the conditioned medium two hours after starting the delivery. A stronger anti-inflammatory effect of CHA was observed upon sustained delivery to the cell medium, simulating an in vivo pharmacokinetic release profile following oral administration.https://www.mdpi.com/2076-3417/13/1/627pharmacokineticsingestionoral administrationchlorogenic acidanti-inflammationantioxidant |
| spellingShingle | Lei Cao Won Han Sang Gil Lee Joong Ho Shin Anti-Inflammatory Activity of Chlorogenic Acid on Macrophages: A Simplified Simulation of Pharmacokinetics Following Ingestion Using a Windup Syringe Pump Applied Sciences pharmacokinetics ingestion oral administration chlorogenic acid anti-inflammation antioxidant |
| title | Anti-Inflammatory Activity of Chlorogenic Acid on Macrophages: A Simplified Simulation of Pharmacokinetics Following Ingestion Using a Windup Syringe Pump |
| title_full | Anti-Inflammatory Activity of Chlorogenic Acid on Macrophages: A Simplified Simulation of Pharmacokinetics Following Ingestion Using a Windup Syringe Pump |
| title_fullStr | Anti-Inflammatory Activity of Chlorogenic Acid on Macrophages: A Simplified Simulation of Pharmacokinetics Following Ingestion Using a Windup Syringe Pump |
| title_full_unstemmed | Anti-Inflammatory Activity of Chlorogenic Acid on Macrophages: A Simplified Simulation of Pharmacokinetics Following Ingestion Using a Windup Syringe Pump |
| title_short | Anti-Inflammatory Activity of Chlorogenic Acid on Macrophages: A Simplified Simulation of Pharmacokinetics Following Ingestion Using a Windup Syringe Pump |
| title_sort | anti inflammatory activity of chlorogenic acid on macrophages a simplified simulation of pharmacokinetics following ingestion using a windup syringe pump |
| topic | pharmacokinetics ingestion oral administration chlorogenic acid anti-inflammation antioxidant |
| url | https://www.mdpi.com/2076-3417/13/1/627 |
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