Peimine is a natural compound with good anti-inflammatory effects in vivo. Peimine (0-25 mg/L) significantly inhibited tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-1β, and increased IL-10 production. Furthermore, peimine significantly inhibited the phosphorylation of p38, ERK and c-jun N-terminal kinase (JNK) as well as decreased p65 and IκB[3]. Moreover, peimine reduced MAPKs (Mitogen-activated protein kinases) phosphorylation and the nuclear NF-κB expression in PMACI-induced HMC-1(human mast cell). Peimine decreased PCA (Passive cutaneous anaphylaxis) reactions in rats as well[4]. Peimine increased the systemic exposure of paeoniflorin through inhibiting the activity of CYP3A4 and P-gp[5]. The intestinal absorption of peimine across Caco-2 cell monolayers involves active transport and that peimine is a substrate of P-gp[6].
Peimine/贝母素甲 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Caco-2 cells
10, 20, 50, 100, 200 µM
150 minutes
To investigate the intestinal absorption mechanism of Peimine in Caco-2 cell monolayers. The results show that Peimine transport is concentration-dependent and involves active transport.
Acta Pharm Sin B. 2016 Mar;6(2):125-31
293T/hACE2 cells
10 µM
2 hours
Evaluating the efficacy of peimine in inhibiting SARS-CoV-2 pseudovirus entry in 293T/hACE2 cells, peimine was found to significantly inhibit viral entry.
J Food Biochem. 2022 Oct;46(10):e14354
BV-2 microglia
7.5 μg/ml, 15 μg/ml, 30 μg/ml
24 hours
To investigate the effects of Peimine on M1/M2 polarization in LPS-stimulated BV-2 microglia. Results showed that Peimine dose-dependently decreased the levels of M1 markers CD16 and IL-6, and increased the levels of M2 markers CD206 and IL-10.
Heliyon. 2024 Jul 20;10(15):e34987
MH-S cells
12.5, 25, 50, 100 μg/ml
3 hours
Peimine significantly reduced the mRNA expression of Arg-1 and Fizz-1 in IL-4-induced MH-S cells and decreased the protein levels of Arg-1 and CD206.
Biosci Rep. 2022 Oct 28;42(10):BSR20220986
Peimine/贝母素甲 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague–Dawley rats
BLM-induced pulmonary fibrosis model
Oral
0.24 mg/kg
Daily administration from day 29 to day 42
Peimine significantly ameliorated BLM-induced pulmonary fibrosis by suppressing histological changes and collagen deposition, reducing the number of M2 macrophages and the expression of profibrotic factors.
Biosci Rep. 2022 Oct 28;42(10):BSR20220986
Male albino Swiss mice
Chronic constriction injury (CCI) model of the sciatic nerve
Intrathecal injection
10, 20, 60 µg/5 µL
Single administration on day 7 post-CCI
To evaluate the effect of Peimine on tactile and thermal hypersensitivity in a neuropathic pain model. Results showed that Peimine dose-dependently attenuated CCI-induced tactile and thermal hypersensitivity.
Int J Mol Sci. 2023 May 19;24(10):9000
Sprague Dawley (SD) rats
Drug-resistant epilepsy (DRE) rat model
Oral gavage
2.5 mg/kg, 5 mg/kg, 10 mg/kg
Once daily for 30 days
To investigate the effects of Peimine on epileptic behaviors and hippocampal neuron injury in DRE rats. Results showed that Peimine dose-dependently alleviated epileptic behaviors, reduced hippocampal neuron injury, and promoted a shift from M1 to M2 microglial phenotype.
Heliyon. 2024 Jul 20;10(15):e34987
Sprague-Dawley rats
Drug interaction model
Oral
5 mg/kg
Once daily for 10 days
To investigate the effect of Peimine on the pharmacokinetics of Paeoniflorin, results showed that Peimine significantly increased the Cmax and AUC of Paeoniflorin, prolonged t1/2, and decreased clearance.
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