Isofraxidin, a natural product isolated and purified from the herbs of Sarcandra glabra (Thunb.) Nakai, possesses significant analgesic and anti-inflammatory activities that may be mediated through the regulation of pro-inflammatory cytokines, TNF-α and the phosphorylation of p38 and ERK1/2.
Isofraxidin/异嗪皮啶 细胞实验
Cell Line
Concentration
Treated Time
Description
References
RAW 264.7 macrophages
0.03, 0.06, and 0.06 mmol
24 hours
To investigate the effect of C + R + I on LPS-induced inflammatory factors and oxidative stress in RAW 264.7 macrophages. Results showed that C + R + I significantly suppressed the levels of nitric oxide (NO), pro-inflammatory cytokines, and inhibited iNOS and COX-2 expression.
Front Pharmacol. 2021 Jan 11;11:580064
Bone marrow-derived macrophages (BMMs)
12.5 µM
8 hours
To evaluate the effect of isofraxidin on RANKL-induced NFATc1 transcriptional activity, results showed that isofraxidin inhibited NFATc1 activation.
Cell Transplant. 2021 Jan-Dec;30:963689721990321
Bone marrow-derived macrophages (BMMs)
6.25 and 12.5 µM
4 days
To evaluate the effect of isofraxidin on RANKL-induced osteoclast formation in BMMs, results showed that isofraxidin inhibited TRAP activity and osteoclast formation.
Cell Transplant. 2021 Jan-Dec;30:963689721990321
Bone marrow-derived macrophages (BMMs)
6.25 and 12.5 µM
24 hours
To evaluate the effect of isofraxidin on BMMs cell viability, results showed that 6.25 and 12.5 µM concentrations did not affect cell viability.
Cell Transplant. 2021 Jan-Dec;30:963689721990321
Isofraxidin/异嗪皮啶 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c mice
Chronic unpredictable mild stress (CUMS)-induced depressive model
Oral gavage
3, 10, 30 mg/kg
Once daily for 4 weeks
Isofraxidin significantly reversed CUMS-induced decrease in body weight gain, sucrose preference, locomotor activity, and increased immobility time in the forced swimming test (FST) and tail suspension test (TST). Additionally, isofraxidin decreased serum levels of corticosterone (CORT), adrenocorticotropic hormone (ACTH), and hypothalamic corticotropin-releasing hormone (CRH), suppressed the expression of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6 in the hippocampus, and inhibited CUMS-induced activation of nuclear factor kappa B (NF-κB) and NOD-like receptor protein 3 (NLRP3) inflammasomes in the hippocampus.
Brain Sci. 2022 Oct 11;12(10):1376
BALB/c mice
LPS-induced acute lung injury model
Intraperitoneal injection
High dose (50, 20, and 20 mg/kg), middle dose (25, 10, and 10 mg/kg), low dose (12.5, 5, and 5 mg/kg)
Once daily for three days
To investigate the protective effect of C + R + I on LPS-induced acute lung injury in mice. Results showed that C + R + I significantly alleviated lung histopathological damage, reduced inflammatory cell infiltration, and inhibited the activation of the MAPK-NF-κB signaling pathway.
Front Pharmacol. 2021 Jan 11;11:580064
Swiss albino mice
LPS-induced cytokine release syndrome
Intraperitoneal
15 mg/kg
Once daily for 3 days
Isofraxidin alone or in combination with methylprednisolone ameliorates LPS-induced inflammatory and oxidative stress damage in mice, reduces inflammatory and oxidative stress markers, and prevents LPS-induced liver and lung tissue damage.
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