Related Experiment Video
Updated: Jul 14, 2026
09:22
Amikacin Protection Assay for Quantification and Visualization of Escherichia coli Cell Invasion
Published on: July 3, 2026
Bacampicillin uptake is shared with thiamine in Caco-2 cells
Masako Oda1, Kaori Fujimoto, Michiya Kobayashi
1Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Ishikari-Tobetsu, Hokkaido, Japan.
Biological & Pharmaceutical Bulletin
|July 3, 2007
Summary
Bacampicillin, a prodrug for ampicillin, is transported via a saturable system in Caco-2 cells. This transport system appears to share a carrier with thiamine, a cationic vitamin.
Area of Science:
- Pharmacology
- Cell Biology
- Drug Transport
Background:
- Bacampicillin is a prodrug designed to enhance ampicillin's intestinal absorption.
- Understanding the transport mechanisms of bacampicillin is crucial for optimizing its delivery and efficacy.
Purpose of the Study:
- To characterize the transport of bacampicillin in Caco-2 cells.
- To investigate potential carrier-mediated transport systems involved in bacampicillin uptake.
Main Methods:
- Caco-2 cell monolayers were used to study bacampicillin uptake kinetics.
- Inhibition and trans-stimulation studies were performed using various organic cations and thiamine.
- Apical-to-basolateral transport was assessed across cell monolayers.
Main Results:
- Bacampicillin uptake was significantly higher than ampicillin and pivampicillin, indicating saturable transport (Km = 3.6 mM, Vmax = 23.9 nmol/mg protein/min).
- Thiamine, diphenhydramine, and procainamide inhibited bacampicillin uptake, while thiamine preloading enhanced it, suggesting carrier involvement.
- Bacampicillin transport shared characteristics with thiamine transport, including pH dependence and inhibition by amiloride and oxythiamine, but not with pivampicillin.
Conclusions:
- Bacampicillin is transported by a saturable, carrier-mediated system in Caco-2 cells.
- This system appears to involve shared carriers with thiamine, suggesting a potential interaction.
- These findings provide insights into the intestinal absorption mechanisms of bacampicillin.
More Related Videos
Related Concept Videos
01:23Drug Absorption Mechanism: Passive Membrane Transport
Passive transport is a method of drug absorption where small, lipid-soluble drugs can move across the cell membrane. This movement happens along the concentration gradient, which is a natural flow from higher to lower concentration areas. The speed at which the drug moves is directly related to its lipid–water partition coefficient. This means that the more a drug dissolves in lipids, the faster it diffuses or spreads throughout the body. It is important to note that most drugs are either weak...
01:27ABC Transporters: Importer
ATP-binding cassette or ABC transporters are a class of ATP-driven pumps that hydrolyze ATP to move solutes across the membrane. They can be grouped into importers and exporters. While exporters are present in all domains of life, importers exist only in bacteria and some plants.
In bacteria, based on the number of transmembrane helices and the chemical nature of their substrates, the ABC importers can be divided into three types:
In bacteria, based on the number of transmembrane helices and the chemical nature of their substrates, the ABC importers can be divided into three types:
01:19Drug Absorption Mechanism: Carrier-Mediated Membrane Transport
Certain large, lipid-insoluble drug molecules that resemble amino acids, peptides, or glucose, require specialized carrier proteins to facilitate their diffusion across cell membranes. This transport can occur through either facilitated diffusion, which does not require energy input, or active transport, which does require energy input.
Facilitated diffusion is a passive process that utilizes human Solute Carrier (SLC) transporters. These transporters bind to the drug, undergo structural...
Facilitated diffusion is a passive process that utilizes human Solute Carrier (SLC) transporters. These transporters bind to the drug, undergo structural...
01:15Drug Elimination by Renal Route: Tubular Secretion
Once the process of glomerular filtration is completed, blood carrying unfiltered drug molecules traverses through efferent arterioles and makes its way into the peritubular capillaries in the proximal tubule. A variety of carriers play a pivotal role in actively secreting drugs from these peritubular capillaries into the tubular fluid. The organic anion transporter transfers acidic drugs, against an electrochemical gradient, from the peritubular capillaries into the renal tubule cells and...
01:16Facilitated Diffusion
The plasma membrane, a critical structure in cellular biology, houses an array of transporters, or carrier proteins, interspersed within its lipid bilayer. These proteins play a crucial role in solute transport through facilitated diffusion, a form of passive diffusion that uses transporters to move the molecules across the membrane.
In this process, substrates such as organic compounds and ions interact with a transporter on one side, triggering conformational changes in proteins that enable...
In this process, substrates such as organic compounds and ions interact with a transporter on one side, triggering conformational changes in proteins that enable...
01:06Carrier-Mediated Transport
Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...