Isoorientin (or homoorientin) is a flavone, which is a chemical flavonoid-like compound, and a 6-C-glucoside of luteolin. In PC (pancreatic cancer), isoorientin strongly inhibited the survival of the cells, induced cell apoptosis, and decreased its malignancy by reversing the expression of epithelial-mesenchymal transition and matrix metalloproteinase and decreased vascular endothelial growth factor expression[3]. Isoorientin was found to be a potent inhibitor of COX-2with an IC50 value of 39 μM[4]. Isoorientin reduced inflammation in RAW 264.7 cell line in vitro and carrageenan induced inflammatory animal model systems in vivo. Isoorientin, a selective inhibitor of COX-2, not only exerts anti-inflammatory effects in LPS induced RAW cells and carrageenan induced inflammatory model systems but also exhibits potent antioxidant properties[5]. Isoorientin can inhibit GSK3β by increasing p-GSK3β and regulate the downstream signal molecules to inhibit inflammation and protect the integrity of the blood-brain barrier and the homeostasis in the brain[6].
Isoorientin/异荭草素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Plasmodium falciparum W2
0.8-100 μg/mL
48 h
Evaluate anti-plasmodial activity, results showed no activity at concentrations of 50 μg/mL or below
Aerial Parts. Antioxidants (Basel).
Plasmodium falciparum 3D7
0.8-100 μg/mL
48 h
Evaluate anti-plasmodial activity, results showed no activity at concentrations of 50 μg/mL or below
Aerial Parts. Antioxidants (Basel).
WI-38
2-100 μg/mL
48 h
Evaluate cytotoxicity, results showed no cellular toxicity at concentrations of 100 μg/mL or below
Aerial Parts. Antioxidants (Basel).
A549
2-100 μg/mL
48 h
Evaluate cytotoxicity, results showed no cellular toxicity at concentrations of 100 μg/mL or below
Aerial Parts. Antioxidants (Basel).
HeLa
2-100 μg/mL
48 h
Evaluate cytotoxicity, results showed no cellular toxicity at concentrations of 100 μg/mL or below
Aerial Parts. Antioxidants (Basel).
Human hepatocyte HL-7702 cells
25, 50, 100, 200 μg/mL
12 h
To evaluate cell viability and antioxidant capacity, results showed that Zein/GA-Iso nanoparticles significantly increased the survival rate of HL-7702 cells.
Food Chem X. 2024 Jul 1;23:101604.
Human colorectal adenocarcinoma Caco-2 cells
25, 50, 100, 200 μg/mL
12 h
To evaluate cell viability and antioxidant capacity, results showed that Zein/GA-Iso nanoparticles significantly increased the survival rate of Caco-2 cells.
Food Chem X. 2024 Jul 1;23:101604.
T lymphocytes
40 μM
96 h
Inhibited T lymphocyte proliferation, reducing CD4+ T cell proliferation to 57.07±6.4%, but no significant effect on CD8+ T cells
Antioxidants (Basel). 2022 Jul 30;11(8):1503.
HL-7702 liver cells
5 μM
24 h
Isoorientin attenuated BaP-induced pyroptotic hepatocyte damage by inhibiting the ROS/NF-κB/NLRP3/Caspase-1 signaling pathway
Antioxidants (Basel). 2021 Aug 11;10(8):1275.
primary colon epithelial cells
10 μM
48 h
To compare the effects of four main BLF components on inflammatory cytokines and oxidative markers in primary colon epithelial cells of AD mice, Isoorientin showed the strongest bioactivity.
CNS Neurosci Ther. 2024 Feb;30(2):e14620.
primary neuronal cells
10 μM
48 h
To compare the effects of four main BLF components on inflammatory cytokines and oxidative markers in primary neuronal cells of AD mice, Isoorientin showed the strongest bioactivity.
CNS Neurosci Ther. 2024 Feb;30(2):e14620.
Isoorientin/异荭草素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Zebrafish
Zebrafish larvae
Water solution
0.1-100 μg/mL
Once daily for 72 hours
Evaluate whole organism toxicity, results showed no toxicity at tested concentrations
Aerial Parts. Antioxidants (Basel).
ICR male mice
Acetic acid-writhing, hot plate and formalin-induced nociception models
Intraperitoneal injection
7.5, 15, 30 mg/kg
Single administration, evaluated 1 hour later
Assessed the antinociceptive and anti-inflammatory activities of isoorientin. Results showed that isoorientin at 30 mg/kg significantly inhibited acetic acid-induced writhing (86.2% inhibition) and formalin-induced licking time (73.9% in the first phase and 48.3% in the second phase), with effects superior to clinical drugs like rotundine and aspirin. Additionally, isoorientin suppressed TRPV1 and GluN2B protein expression in the spinal dorsal horn and modulated inflammatory cytokines (TNF-α, IL-1β, IL-10) and oxidative stress markers (GSH, MDA, SOD, VC).
Commun Biol. 2020 Mar 6;3(1):110
APP/PS1 transgenic mice
Alzheimer's disease (AD) mouse model
Oral gavage
2 mg/kg
Once daily for 4 weeks
To evaluate the therapeutic effects of BLF on ulcerative colitis in AD mice, BLF significantly alleviated colitis injury and possessed neuroprotective properties.
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