Cefaclor is an orally active cephalosporin antibiotic that is well absorbed. It specifically targets penicillin-binding protein 3 (PBP3) and is used for the treatment and research of various bacterial infections such as respiratory tract infections, bacterial bronchitis, pharyngitis, and skin infections. It also has potential implications for studying depression[1].[2].[3].[4].
体内研究
When administered orally at a dosage of 200 mg/kg/day for five consecutive days, Cefaclor can disturb the intestinal flora balance in mice, leading to anxiety and depression-like behaviors. These effects are alleviated with treatments like Fluoxetine or vagotomy[1].
体外研究
In laboratory tests, Cefaclor demonstrates significant antibacterial activity against 556 Gram-positive and Gram-negative bacterial isolates. It typically exhibits low minimum inhibitory concentrations (MIC), with most strains showing MIC values below 3.1 μg/mL, and specifically, Staphylococcus aureus has an MIC of 1 μg/mL[4].
Cefaclor is primarily transported by hPepT2 and hPepT1 transporters in an MDCK cell line stably transduced to overexpress hOAT1, hPepT1, and hPepT2. This interaction was observed at concentrations of 60/500 μM over a period of 30 minutes[2].
At a concentration of 0.16 mg/mL over 30 minutes, Cefaclor can induce allergic reactions by directly activating basophils and mast cells[3].
Cefaclor monohydrate/头孢克洛一水合物 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Haemophilus parasuis clinical strain C7
0.015625 - 256 μg/mL
24-48 h
To screen for cefaclor-resistant strains and determine their resistance mechanisms.
Front Microbiol. 2024 Mar 15;15:1364339
STC-1 cells
1–20 mM
Cefaclor stimulates CCK release from STC-1 cells, involving pertussis toxin-sensitive G protein(s) and Ca2+ availability.
Br J Pharmacol. 2000 Oct;131(3):399-404
Cefaclor monohydrate/头孢克洛一水合物 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Anxiety- and depression-like behavior model
Oral
200 mg/kg
Once a day for 5 days
To investigate the effect of cefaclor on anxiety- and depression-like behaviors in mice. Results showed that cefaclor induced anxiety- and depression-like behaviors and altered gut microbiota and neurotransmitter levels.
Sci Rep. 2023 Sep 19;13(1):15529
Sprague-Dawley rats
Delayed gastric emptying model
Intragastric instillation
3, 10, 30, 100 μM
Single dose, measured 5 minutes after administration
Cefaclor delays gastric emptying via a CCK-A receptor-mediated mechanism, and this effect is reversed by the CCK-A antagonist SR-27897B. Additionally, cefaclor acts through capsaicin-sensitive afferent pathways.
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