1. Anti-inflammatory
It is currently believed that the anti-inflammatory activity of luteolin can inhibit the production of nitric oxide (NO) and other inflammatory cytokines such as tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6), and inhibit protein Tyrosine phosphorylation is related to gene expression mediated by nuclear transcription factor KB (NF-KB).
2. Anti-tumor
The anti-tumor mechanism of action is more and more complicated. Studies have shown that luteolin can selectively inhibit the fatty acid synthase activity of prostate cancer and breast cancer cells, which is related to its anti-tumor cell growth and apoptosis; luteolin can significantly Reduce the incidence of colon cancer and tumor size caused by dimethylhydrazine, which is related to its ability to regulate lipid peroxidation, anti-oxidation and anti-proliferation; luteolin can inhibit the invasion and movement ability of ovarian cancer cell HO8910PM in a dose-dependent manner in vitro It is related to its inhibition of the secretion of matrix metalloproteinase-9 (MMP-9) and down-regulation of the expression of extracellular signal-regulated kinase 2 (ERK2).
3. Anti-allergic
Luteolin can inhibit immunoglobulin E (IgE)-mediated allergy transmitters produced by human mast cells, including histamine, leukotrienes, prostaglandin D2, and the release of monocyte-macrophage colony stimulating factor. The effect may be related to the inhibition of Ca2+ influx and protein kinase C (PKC) translocation activation.
4. Anti-inflammatory demyelinating diseases
Luteolin can protect oligodendrocytes against oxidative damage induced by hydrogen peroxide in a dose-dependent manner in vitro, strongly inhibit the phagocytosis of myelin by macrophages, significantly reduce the production of cellular reactive oxygen species, and reduce the expression of iNOS protein. At low doses, the level of NO produced by macrophages was significantly reduced.
5. Anti-fibrosis
Luteolin can reduce the degree of liver fibrosis, reduce the content of hydroxyproline (HYP), malondialdehyde (MDA) and the expression of type I procollagen mRNA in liver tissues, and can inhibit hepatic stellate cells (HSC) in vitro Proliferation and collagen synthesis. It can also improve the histopathological changes of pulmonary fibrosis caused by bleomycin, reduce lung mass index, significantly reduce the increase of MDA and HYP, and inhibit the expression of transforming growth factor-β1 (TGF-β1) mRNA in lung tissue , In vitro can inhibit the proliferation of human embryonic lung fibroblasts and promote their apoptosis.
6. Anti-fertility and hormone effects
Luteolin has significant dose-dependent anti-implantation activity. After oral administration, it can significantly increase the weight and diameter of the uterus, the thickness of the endometrium, and the height of its epithelial cells. When used alone, it has an estrogen-like effect, but it is compatible with ethinyl estradiol. When alcohol is used in combination, it has an anti-estrogen effect.
7. The effect on blood vessels
Luteolin can inhibit vascular endothelial growth factor (VEGF)-induced rabbit corneal angiogenesis in vivo; inhibit tumor growth and angiogenesis in murine xenograft tumor models; inhibit VEGF-induced human umbilical vein endothelial cells (HUVECs) in vitro Survival and proliferation. It can significantly inhibit the proliferation and DNA synthesis of vascular smooth muscle cells induced by platelet-derived growth factor-BB (PDGF-BB), and can block the cell cycle in the G1 phase. It can concentration-dependently reduce the tension of phenylephrine pre-constricted blood vessels, antagonize the vasoconstriction caused by high potassium, have arterial relaxation, and its vasodilation effect is not endothelial-dependent, and its mechanism of action is directly related to the direct inhibition of voltage-dependent calcium channels, Receptor-operated calcium channels, intracellular calcium release, and activation of potassium channels are related, but have nothing to do with α and β receptors.
8. Other
Luteolin can inhibit a variety of bacteria and viruses, such as Staphylococcus aureus, Escherichia coli, herpes simplex virus, polio virus, Coxsackie B3 virus and so on. It can inhibit the activity of HIV-1 integrase of HIV, and has a potential anti-HIV effect. Luteolin can bind to the s2 protein of the severe acute respiratory syndrome (SARS) coronavirus, thereby inhibiting the virus from entering the host cell. Luteolin also has the effect of resisting Leishmania donovani, and inhibits its growth by inhibiting the effects of Leishmania donovani topoisomerase I and topoisomerase II. In addition, luteolin also has immunomodulatory effects.