Pectolinarigenin is a dual inhibitor of COX-2/5-LOX with anti-inflammatory activity[3]. Pectolinarigenin has potent inhibitory activities on melanogenesis. Pectolinarigenin treatment resulted in growth inhibition and apoptosis induction in melanoma cells, and the potential of pectolinarigenin to impair the migration and invasion of melanoma cells in accordance with the changes in the expression of the associated proteins[4]. Intraperitoneal administrations of pectolinarigenin significantly inhibited breast cancer metastasis to lungs without affecting the tumor growth of incubated 4T1 breast cancer cells. Pectolinarigenin could also recruit CD8+ T cells to mediate tumor immune response. Furthermore, pectolinarigenin markedly impaired cancer cell migration and invasion by down-regulating phosphorylated-Stat3, and expression of matrix metalloproteinase (MMP)-2, MMP-9, while up-regulating the expression of TIMP2[5]. Treatment of pectolinarigenin inhibited cell viability and cell migration of NPC C666-1 cells in concentration- and time-dependent manner. The in vivo experiment of subcutaneous xenograft mice model also indicated that the administration of pectolinarigenin could decrease the tumor growth of NPC (Nasopharyngeal cancer) and no severe toxicity was observed[6].
Pectolinarigenin/柳穿鱼黄素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Osteosarcoma cell lines
0, 10, 20, 50 µM
24 hours
Inhibits STAT3 activity
Cell Death Dis. 2018 Sep 5;9(9):902
143B cells
0, 5, 10, 20, 50 µM
24 hours
Inhibits STAT3 activity
Cell Death Dis. 2018 Sep 5;9(9):902
MKN-28 cells
0, 25, 50, 75, 100, 150, and 200 µM
24 hours
PEC significantly reduced the viability of MKN-28 cells with an IC50 of approximately 96.88 μM.
Nutrients. 2018 Oct 30;10(11):1596
AGS cells
0, 25, 50, 75, 100, 150, and 200 µM
24 hours
PEC significantly reduced the viability of AGS cells with an IC50 of approximately 124.79 μM.
Nutrients. 2018 Oct 30;10(11):1596
TCMK-1 cells
25, 50, 100, 150, 300 µM
24 hours
To evaluate the effect of PEC on uric acid-induced inflammation and fibrosis in TCMK-1 cells. Results showed that PEC significantly suppressed the expression of IL-6, TNF-α, and FABP4, and reduced the fibrotic expression of α-SMA, FN, and Col I.
Front Pharmacol. 2022 Jan 27;12:792139
HepG2 cells
0.1, 1.0, 10 µM
24 hours
PG significantly increased the expression of HO-1, NQO-1, and AKR1B10, inducing antioxidant enzymes via the Nrf2/ARE pathway
Antioxidants (Basel). 2022 Mar 30;11(4):675
Mouse NSC-34 motor neuron cell lines
2.5 and 5 µM
24 hours
PLG treatment significantly increased the viability of PR50-expressing cells, reduced ROS production and apoptosis, and restored mitochondrial membrane potential.
Antioxidants (Basel). 2023 Nov 16;12(11):2008
MKN28 cells
25, 50, 75, 100, 125, 150 µM
24 hours
PEC significantly inhibited MKN28 cell growth in a dose-dependent manner with an IC50 of 96.88 μM.
Nutrients. 2018 Aug 8;10(8):1043
AGS cells
25, 50, 75, 100, 125, 150 µM
24 hours
PEC significantly inhibited AGS cell growth in a dose-dependent manner with an IC50 of 124.79 μM.
Nutrients. 2018 Aug 8;10(8):1043
MCF-7
0–40 µM
24, 48, 72 hours
Pectolinarigenin significantly inhibited the proliferation and migration of MCF-7 cells and impaired cell invasion by down-regulating phosphorylated-Stat3, MMP-2, and MMP-9 while up-regulating the expression of TIMP2.
Front Pharmacol. 2019 Oct 10;10:1195
MDA-MB-231
0–40 µM
24, 48, 72 hours
Pectolinarigenin significantly inhibited the proliferation and migration of MDA-MB-231 cells and impaired cell invasion by down-regulating phosphorylated-Stat3, MMP-2, and MMP-9 while up-regulating the expression of TIMP2.
Front Pharmacol. 2019 Oct 10;10:1195
4T1
0–40 µM
24, 48, 72 hours
Pectolinarigenin significantly inhibited the proliferation and migration of 4T1 cells and impaired cell invasion by down-regulating phosphorylated-Stat3, MMP-2, and MMP-9 while up-regulating the expression of TIMP2.
Front Pharmacol. 2019 Oct 10;10:1195
Pectolinarigenin/柳穿鱼黄素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
Hyperuricemic nephropathy model
Oral
25 and 50 mg/kg
Daily administration for 4 weeks
To evaluate the nephroprotective effects of PEC in hyperuricemic nephropathy mice. Results showed that PEC significantly lowered serum uric acid levels, improved kidney function, alleviated renal inflammation and fibrosis, and inhibited the activation of TGF-β/SMAD3 and JAK2/STAT3 signaling pathways.
Front Pharmacol. 2022 Jan 27;12:792139
Balb/c mice
4T1 breast cancer model
Intraperitoneal injection
25 mg/kg, 50 mg/kg
Once daily for 10 days
Pectolinarigenin significantly inhibited breast cancer metastasis to lungs without affecting the tumor growth of incubated 4T1 breast cancer cells. Additionally, Pectolinarigenin could recruit CD8+ T cells to mediate tumor immune response.
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