Isorhamnetin, a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L., is well known for its anti-inflammatory, anti-oxidative, anti-adipogenic, anti-proliferative, and anti-tumor activities. Isorhamnetin could inhibit cardiac hypertrophy and fibrosis 8 weeks after aortic banding. In vitro studies performed in neonatal rat cardiomyocytes confirmed that isorhamnetin could attenuate cardiomyocyte hypertrophy induced by angiotensin II, which was associated with phosphatidylinositol 3-kinase-AKT signaling pathway[3]. Isorhamnetin inhibited epidermal growth factor (EGF)-induced neoplastic cell transformation. Isorhamnetin attenuated EGF-induced COX-2 expression in JB6 and A431 cells. In an in vivo mouse xenograft using A431 cells, isorhamnetin reduced tumor growth and COX-2 expression[4]. Isorhamnetin inhibits the proliferation of numerous breast cancer cells (IC50, ~10 µM), including MCF7, T47D, BT474, BT-549, MDA-MB-231 and MDA-MB-468, whereas less inhibitory activity is observed in the MCF10A normal breast epithelial cell line (IC50, 38 µM) [5]. Isorhamnetin inhibits the TGF-β/Smad signaling pathway and relieves oxidative stress, thus inhibiting HSC (hepatic stellate cells) activation and preventing liver fibrosis[6].
Isorhamnetin/异鼠李素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human amniotic epithelial stem cells
20 µM
10 days
Investigate the gene expression profile of ISO in hAESCs, showing significant suppression of TGF-β, collagen-related functions, and inflammatory processes
Front Cell Dev Biol. 2020 Sep 29;8:578197.
Human amnion epithelial cells (hAECs)
20 mM
10 days
Induced hepatic-lineage specific differentiation in hAECs, activating essential biological processes, molecular functions, and signaling pathways for hepatic differentiation.
Front Cell Dev Biol. 2020 Nov 5;8:578036.
Porcine ovarian granulosa cells
20 µM
24 hours
To investigate the therapeutic effect of isorhamnetin on ZEA-induced damage in porcine ovarian granulosa cells and elucidate its molecular mechanism. Results showed that isorhamnetin suppressed ZEA-induced apoptosis, endoplasmic reticulum stress, and oxidative stress via the PI3K/Akt signaling pathway, promoting cell proliferation and hormone secretion.
Anim Nutr. 2022 Aug 8;11:381-390.
Bovine endometrial epithelial cells (bEECs)
2.5 µM
24 hours
To evaluate the protective effect of isorhamnetin on NEFA-induced cell damage. Results showed that isorhamnetin significantly improved cell viability, reduced apoptosis, and decreased the expression of BAX and cleaved caspase-3.
Antioxidants (Basel). 2025 Jan 28;14(2):156.
BV2 microglial cells
0, 50, 100, 200 µM
24 hours
To evaluate the effect of isorhamnetin on LPS-induced inflammatory responses, results showed that isorhamnetin significantly suppressed LPS-induced secretion of NO and PGE2 without significant cytotoxicity.
Int J Mol Med. 2019 Feb;43(2):682-692.
NOZ cells
0, 40, 60, 80, 100 µM
24, 48, 72 hours
Isorhamnetin significantly inhibited the proliferation of NOZ cells in a time- and dose-dependent manner
Front Pharmacol. 2021 Feb 17;12:628621.
GBC-SD cells
0, 40, 60, 80, 100 µM
24, 48, 72 hours
Isorhamnetin significantly inhibited the proliferation of GBC-SD cells in a time- and dose-dependent manner
Front Pharmacol. 2021 Feb 17;12:628621.
Porcine oocytes
5, 10, 20, 30 µM
44 hours
To investigate the protective effect of isorhamnetin on ZEA-induced damage in porcine oocytes. Results showed that isorhamnetin significantly increased the polar body extrusion rate of ZEA-exposed oocytes and inhibited ZEA-induced early apoptosis.
J Anim Sci Biotechnol. 2023 Feb 3;14(1):22.
Corneal epithelial cells (CorE) and conjunctival epithelial cells (ConjE)
30 µM
48 hours
The cytotoxic effect of isorhamnetin was evaluated, showing that isorhamnetin at 30 μM did not affect cell viability.
Int J Mol Sci. 2021 Apr 12;22(8):3954.
CD274-knockout U27 cells (U27−/−)
10, 20, 40 µM
48 hours
Reduced sensitivity to ISO, weaker inhibition of migration and invasion
Int J Mol Sci. 2024 Jan 4;25(1):670.
Canine mammary tumor U27 cells
10, 20, 40 µM
48 hours
Inhibited cell migration and invasion, induced apoptosis
Int J Mol Sci. 2024 Jan 4;25(1):670.
Human bladder cancer T24 cells
127.86 µM (IC50)
48 hours
Isorhamnetin inhibited T24 cell proliferation via G2/M phase arrest and apoptosis, accompanied by decreased expression of Wee1 and cyclin B1, increased expression of p21WAF1/CIP1, and enhanced binding of p21 to Cdk1.
Cancers (Basel). 2019 Oct 4;11(10):1494.
Primary pancreatic acinar cells
10 µM
50 minutes
To evaluate the protective effect of isorhamnetin on STC-induced acinar cell necrosis, results showed that isorhamnetin significantly alleviated STC-induced acinar cell necrosis
Int J Mol Sci. 2024 Mar 28;25(7):3784.
FRT cells
30 µM
The effect of isorhamnetin on CFTR chloride channel activity was measured, showing that isorhamnetin fully activated CFTR at 30 μM.
Int J Mol Sci. 2021 Apr 12;22(8):3954.
Isorhamnetin/异鼠李素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
NOZ cell xenograft model
Intraperitoneal injection
1 or 5 mg/kg
Once daily for 14 days
Isorhamnetin significantly inhibited tumor growth in a dose-dependent manner
Front Pharmacol. 2021 Feb 17;12:628621.
C57 mice
Bleomycin-induced pulmonary fibrosis model
Intragastrically
10 and 30 mg/kg
Once a day for 28 days
To investigate the effect of Isor on bleomycin-induced pulmonary fibrosis. Results showed that Isor attenuated fibrotic changes, reduced collagen deposition and α-SMA expression, and alleviated EMT and ERS.
Int J Mol Med. 2019 Jan;43(1):117-126
C57BL/6 mice
STC or L-arginine-induced SAP model
Intraperitoneal injection
10 mg/kg or 30 mg/kg
24 hours or 72 hours after a single injection
To evaluate the protective effect of isorhamnetin on SAP, results showed that isorhamnetin significantly alleviated pancreatic damage and reduced serum lipase and amylase levels
Int J Mol Sci. 2024 Mar 28;25(7):3784.
Nude mice
Ishikawa cell xenograft model
Intraperitoneal injection
20 mg/kg
Once daily for 15 days
Isorhamnetin significantly inhibited the growth of Ishikawa xenografts with an inhibition rate up to 50.42%, and suppressed tumor growth by regulating key proteins of mitochondrial and endoplasmic reticulum-related pathways.
Foods. 2022 Oct 28;11(21):3415
CD-1 mice
Scopolamine-induced dry eye model
Topical ocular administration
30 μM
Three times a day for 10 days
The therapeutic effect of isorhamnetin on dry eye disease was evaluated, showing that isorhamnetin significantly reduced corneal damage and increased tear volume.
Int J Mol Sci. 2021 Apr 12;22(8):3954.
C57BL/6 mice
Angiotensin II-induced cardiac hypertrophy and fibrosis model
Intraperitoneal injection
5 mg/kg
Once daily for 3 weeks
Investigate the protective effect of ISO on Angiotensin II-induced cardiac hypertrophy and fibrosis, showing significant suppression of myocardial hypertrophy and fibrosis
Front Cell Dev Biol. 2020 Sep 29;8:578197.
BALB/SCID nude mice
U27 cell xenograft model
Intraperitoneal injection
50 mg/kg
Every 3 days for 9 days
Inhibited tumor growth, reduced tumor volume and mass
Int J Mol Sci. 2024 Jan 4;25(1):670.
Caenorhabditis elegans
Wild-type and mutant C. elegans
Liquid media
50-200 μM
2 days
Isorhamnetin reduced fat accumulation dependent on nhr-49, a functional homolog of PPARα, by upregulating an NHR-49 downstream target (ech-1.1) involved in fatty acid β-oxidation in C. elegans.
Curr Res Food Sci. 2019 Nov 21;2:70-76
C57BL/6 mice
Aspergillus fumigatus keratitis model
Topical administration
80 μg/mL
Four times per day for 1 to 5 days
To evaluate the antifungal and anti-inflammatory effects of isorhamnetin in a Mice model of A. fumigatus keratitis. Results showed that isorhamnetin treatment alleviated the severity of FK by reducing corneal fungal load and inhibiting neutrophil recruitment and inflammatory factor expression.
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