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CAS	No.491-70-3
中文名称	木犀草素
英文名称	Luteolin
别名	Digitoflavone;Luteoline;Luteolol;Flacitran
分子式	C₁₅H₁₀O₆
分子量	286.24
溶解性	Soluble in DMSO ≥25mg/mL
纯度	HPLC≥98%
外观(性状)	Light yellow to yellow Solid
储存条件	Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
EC	EINECS 207-741-0
MDL	MFCD00017309
SMILES	O=C1C=C(C2=CC=C(O)C(O)=C2)OC3=CC(O)=CC(O)=C13
InChIKey	IQPNAANSBPBGFQ-UHFFFAOYSA-N
InChI	InChI=1S/C15H10O6/c16-8-4-11(19)15-12(20)6-13(21-14(15)5-8)7-1-2-9(17)10(18)3-7/h1-6,16-19H
PubChem CID	5280445
靶点	PDE;Nrf2
通路	Metabolic Enzyme&Protease；NF-κB
背景说明	Luteolin是一种黄酮类化合物,是一种有效的 Nrf2 抑制剂和一种非选择性的PDE抑制剂,具有抗炎和抗癌活性。
生物活性	Luteolin is a potent PDE and Nrf2 inhibitor.Luteolin can protect against non-alcoholic steatohepatitis through targeting the pro-inflammatory IL-1 and Il-18 pathways in addition to an antioxidant effect.[1-3]
In Vitro	According to the Lineweaver-Burk analysis，luteolin(3-30 microM)competitively inhibited PDE1-5 activities，with K(i)values of 15.0，6.4，13.9，11.1，and 9.5 microM，respectively，which did not significantly differ from each other. [1] In non-small-cell lung cancer A549 cells，which possess constitutively active Nrf2，luteolin elicited a dramatic reduction in Nrf2 at both the mRNA and the protein levels，leading to decreased Nrf2 binding to AREs，down-regulation of ARE-driven genes，and depletion of reduced glutathione. After transcription was blocked with actinomycin D，1μM luteolin decreased the Nrf2 mRNA level by 34% in 30 min，indicating its role in accelerating Nrf2 mRNA turnover. At physiological concentrations，luteolin significantly sensitized A549 cells to the anticancer drugs oxaliplatin，bleomycin，and doxorubicin. [3]
In Vivo	Both luteolin(10-30 micromol/kg，s.c.)and Ro 20-1724(0.1-1 micromol/kg，s.c.)significantly reversed the xylazine/ketamine-induced anesthesia in mice. [1]Luteolin to reduce activity of ALT and AST and to decrease levels of bilirubin，hyaluronic acid and malondialdehyde significantly(p < 0.05). Also，luteolin showed an anti-oxidant activity as indicated by the significant(p < 0.05)increase in reduced glutathione. Finally，a significant(p < 0.05)decrease in IFN-γ，TNF-α，IL-1α and IL-18 levels was observed most notably in groups that received high doses of luteolin(50 and 100 mg/kg).[2]
动物实验	Adult male Wistar rats(200-220 g; n = 60)were used. Rats were fed a high carbohydrate/high fat diet( 30% carbohydrate and 42% fat)daily for 12 weeks to induce NASH. Luteolin(10，25，50 or 100 mg/kg/day)was administered as a suspension(10% w/v in 0.9% NaCl)using an oral gavage. Histopathological changes(necrosis，inflammation and steatosis)were evaluated. Biomarkers for liver function，lipid peroxidation，extracellular matrix deposition and anti-oxidant activity were measured. Levels of IFN-γ，TNF-α and IL-1α and IL-18 were measured.[2]
数据来源文献	[1]. Yu MC， Chen JH， Lai CY， Han CY， Ko WC. Luteolin， a non-selective competitive inhibitor of phosphodiesterases 1-5， displaced [3H]-rolipram from high-affinity rolipram binding sites and reversed xylazine/ketamine-induced anesthesia. Eur J Pharmacol. 2010 Feb 10;627(1-3):269-75. [2].Abu-Elsaad N， El-Karef A. Protection against nonalcoholic steatohepatitis through targeting IL-18 and IL-1alpha by luteolin. Pharmacol Rep. 2019 Aug;71(4):688-694. [3].Tang X， Wang H， Fan L， Wu X， Xin A， Ren H， Wang XJ. Luteolin inhibits Nrf2 leading to negative regulation of the Nrf2/ARE pathway and sensitization of human lung carcinoma A549 cells to therapeutic drugs. Free Radic Biol Med. 2011 Jun 1;50(11):1599-609.
规格	5mg 10mg 10mM*1mL in DMSO 25mg 50mg 100mg 500mg
单位	瓶