Luteolin (luteolin) is a natural flavonoid which exists in many plants. It has a variety of pharmacological activities, such as anti-inflammatory, anti allergic, uric acid, anti-tumor, antibiosis, antiviral and so on. It is mainly used in relieving cough, eliminating phlegm, reducing inflammation, reducing uric acid, treating cardiovascular disease, treating amyotrophic lateral sclerosis, SARS, hepatitis and so on.
Luteolin, mostly in the form of glycosides, exists in many plants. These plants are high in all Ye Qinglan, pepper, wild chrysanthemum, honeysuckle and perilla. It has the effect of antitussive and expectorant. According to the latest research, respiratory symptoms, cough, expectoration and wheezing are all associated with chronic airway inflammation. It has been shown that luteolin inhibits the phosphorylation of macrophages and inhibits the activity of transcription factor NF-kB, and inhibits the production of cytokines IL-6, TNF-a, in macrophages induced by lipopolysaccharide (LPS). The latter two cytokines play a very important role in the mechanism of inflammation, and are sensitive indicators to reflect the degree of inflammation. Luteolin can also enhance IFN- gamma, reduce specific Ig-E and reduce eosinophil infiltration. In addition, luteolin, in addition to anti-inflammatory and anti allergic effects, also has the characteristics of inhibiting PDE, anti SARS and HIV virus, which is the reason for inhibiting the activity of S protein before SARS virus, thus preventing its entry into the host cell. It is used to treat chronic cough caused by COPD, bronchial asthma, chronic pharyngitis, allergic rhinitis and so on.
Chemical name: 3', 4', 5,7- four hydroxyflavone
Alias: yellowish lutein, yellow indicator
Chemical formula: C15H10O6
Molecular weight: 286.23
Physical properties: yellow needle shaped crystal, melting point 328-330℃. Slightly soluble in water, weakly acidic, soluble in alkaline solution and stable under normal conditions.
Luteolin is widely distributed in the natural world. It was named from the leaves, stems and branches of Resedaceae herb (ResedaodorataL.), and it is mainly extracted from peanuts.
It is believed that the anti-inflammatory activity of luteolin is related to the inhibition of nitric oxide (NO) and other inflammatory cytokines such as tumor necrosis factor - alpha (TNF- alpha) and interleukin -6 (IL-6), the inhibition of the phosphorylation of protein arginine and the expression of nuclear factor KB (NF-KB) mediated gene expression.
The mechanism of anti-tumor action is more and more complex. The study shows that luteolin can selectively inhibit the activity of fatty acid synthetase in prostate cancer and breast cancer cells, which is related to the growth and apoptosis of tumor cells, and luteolin can significantly reduce the incidence of colon cancer and the size of cancer caused by two methyl hydrazine. It is related to the regulation of lipid peroxidation, antioxidation and anti proliferation; luteolin can inhibit the invasion and movement of ovarian cancer cell HO8910PM in a dose dependent manner, which is related to the inhibition of the secretion of matrix metalloproteinase -9 (MMP-9) and down regulation of extracellular signal regulated kinase 2 (ERK2).
3. Anti allergy
Luteolin can inhibit the hypersensitivity of human mast cells mediated by immunoglobulin E (IgE), including histamine, leukotrienes, prostaglandin D2, and the release of monocyte macrophage colony stimulating factor, which may be related to the inhibition of Ca2+ inflow and protein kinase C (PKC) translocation activation.
4. Anti inflammatory demyelinating disease
Luteolin can protect oligodendrocytes in a dose-dependent manner against oxidative damage induced by hydrogen peroxide, strongly inhibit macrophage phagocytosis of myelin sheath, significantly reduce the production of active oxygen clusters, reduce the expression of iNOS protein, and significantly reduce the NO level produced by macrophages at low doses.
5. Anti fibrosis
Luteolin can reduce the degree of liver fibrosis, reduce the content of hydroxyproline (HYP), malondialdehyde (MDA) in liver tissue and the expression of I type procollagen mRNA, which can inhibit the proliferation and collagen synthesis of hepatic stellate cells (HSC) in vitro. It can also improve the histopathological changes of pulmonary fibrosis induced by bleomycin, reduce the lung weight index, reduce the increase of MDA and HYP, and inhibit the expression of transforming growth factor - beta 1 (TGF- beta 1) mRNA in the lung tissue, which can inhibit the proliferation of human embryo lung fibroblasts in vitro and promote its apoptosis in vitro.
6, anti fertility and hormone effect
Luteolin has a significant dose dependent anti implantation activity. After oral administration, it can significantly increase the weight, diameter of the uterus, the thickness of the endometrium, and the height of the epithelial cells. It has the role of estrogen like when used alone, but it has anti estrin effect when used with estriol.
7. Effect on blood vessels
Luteolin can inhibit the formation of vascular endothelial growth factor (VEGF) induced rabbit corneal blood vessels, inhibit the growth of tumor and angiogenesis in rat xenograft tumor model, and inhibit the survival and proliferation of human umbilical vein endothelial cells (HUVECs) induced by VEGF in vitro. It can significantly inhibit the proliferation and DNA synthesis of vascular smooth muscle cells induced by platelet-derived growth factor -BB (PDGF-BB), and block the cell cycle in G1 phase. It can reduce the tension of the precontracted blood vessels of phenylephrine in a concentration dependent manner, antagonize the vasoconstriction caused by high potassium, and have the vasodilatation, and its vasodilatation is non endothelium-dependent, and its mechanism of action is to directly inhibit the voltage compliance calcium channel, the longitudinal calcium channel of gymnastics, the intracellular calcium release, and the activation of potassium. The channel is related, but it is not related to the alpha and beta receptor.
Luteolin can inhibit many kinds of bacteria and viruses, such as Staphylococcus aureus, Escherichia coli, herpes simplex virus, poliovirus, Coxsackie B3 virus and so on. It can inhibit the activity of HIV-1 integrase and has potential anti HIV effect. Luteolin can bind to the S2 protein of severe acute respiratory syndrome (SARS) coronavirus, thereby inhibiting the entry of virus into host cells. Luteolin also has the effect of resistance to DDL, and inhibits its growth by inhibiting the action of topoisomerase I and topoisomerase II. In addition, luteolin also has the function of immunomodulation.
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