Engeletin, a natural product isolated and purified from the leaves of Engelhardtia roxburghiana Wall., may serve as a potential anti-inflammatory agent. Engeletin possesses potent inhibition of PGE2 release with IC50 values of 19.6 μg/mL.
Engeletin/黄杞苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
RAW264.7 cells
5, 10, 20, 40 μM
5 days
To evaluate the effect of Engeletin on RANKL-induced differentiation of RAW264.7 cells into osteoclasts. Results showed that Engeletin dose-dependently inhibited the formation of TRAP-positive multinucleated osteoclasts.
J Inflamm Res. 2023 May 24;16:2255-2270.
NCI-N87 cells
5 μM
24 hours
Engeletin alleviated CDO1-induced oxidative stress and integrated stress response (ISR), restoring the proliferation ability of GC cells.
Cell Death Discov. 2022 Dec 16;8(1):493.
MKN45 cells
5 μM
24 hours
Engeletin alleviated CDO1-induced oxidative stress and integrated stress response (ISR), restoring the proliferation ability of GC cells.
Cell Death Discov. 2022 Dec 16;8(1):493.
Rat nucleus pulposus cells
80 µM
24 hours
To evaluate the anti-inflammatory effects of Engeletin on TNF-α-induced inflammation. Results showed that Engeletin effectively inhibited the up-regulation of inflammatory mediators (iNOS, IL-1β, IL-6, COX2, and TNF-α) at both mRNA and protein levels.
J Inflamm Res. 2022 Oct 10;15:5767-5783.
Rat chondrocytes
10 μM and 20 μM
24 hours
Engeletin pretreatment alleviated TNF-α-induced inhibition of ECM components (collagen II and aggrecan) and upregulation of matrix catabolic enzymes (MMP9 and MMP3).
J Inflamm Res. 2021 Mar 9;14:745-760.
Engeletin/黄杞苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
Ovariectomy-induced osteoporosis model
Intraperitoneal injection
5 mg/kg
Every other day for 8 weeks
To assess the protective effect of Engeletin on bone loss in ovariectomized mice. Results demonstrated that Engeletin significantly reduced bone loss induced by ovariectomy and increased trabecular number and thickness.
J Inflamm Res. 2023 May 24;16:2255-2270.
Sprague Dawley rats
Transient middle cerebral artery occlusion (tMCAO) model
Intravenous injection
15, 30, 60 mg/kg
Immediately administered, lasting for 22.5 hours
To evaluate the neuroprotective effects of Engeletin on cerebral ischemia-reperfusion injury, results showed that Engeletin significantly reduced neurological deficit scores, infarct volume, brain edema, and levels of inflammatory factors.
J Cell Mol Med. 2023 Jun;27(12):1653-1663
C57BL/6 mice
Chronic restraint stress (CRS) model
Intragastric administration
2.5, 5, 10, 20 mg/kg
Once daily for 28 days
To evaluate the antidepressant effects of Engeletin in the CRS model, results showed that Engeletin significantly reduced immobility time in FST and TST, and reversed CRS-induced weight loss and reduced sucrose preference.
J Cell Mol Med. 2023 Dec;27(23):3928-3938
Sprague-Dawley rats
Percutaneous needle puncture-induced intervertebral disc degeneration model
Intradiscal injection
80 µM
Once a week for 4 weeks
To evaluate the therapeutic effects of Engeletin on intervertebral disc degeneration in vivo. Results showed that Engeletin partially maintained disc height and T2WI signal intensity, inhibited the expression of inflammatory mediators and matrix-degrading enzymes, and alleviated nucleus pulposus cell apoptosis.
J Inflamm Res. 2022 Oct 10;15:5767-5783.
C57BL/6J mice
Chronic social defeat stress (CSDS) model
Intragastric administration
5, 10, 20 mg/kg
Once daily for 21 days
Engeletin significantly alleviated depressive-like behaviours in CSDS model mice by modulating the LCN2/CXCL10 signalling pathway and altering microglial polarization.
J Cell Mol Med. 2024 Apr;28(8):e18285
Sprague-Dawley rats
ACLT-induced osteoarthritis model
Intraarticular injection
50 μg per injection
Once a week for 4 or 8 weeks
Engeletin alleviated ACLT-induced knee OA in rats via intraarticular injection.
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