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槲皮素

槲皮素用途

Quercetin是一种天然黄酮类化合物,可激活或抑制许多蛋白质的活性。槲皮素可激活SIRT1,也可抑制 PI3K,抑制PI3K γ,PI3K δ,PI3K β的 IC50 分别为2.4 μM, 3.0 μM, 5.4 μM。

槲皮素名称

[ CAS 号 ]:
117-39-5

[ 中文名 ]:
槲皮素

[ 英文名 ]:
Quercetin

[中文别名 ]:

[英文别名 ]:

EINECS 204-187-1
MELETIN
2',3,4',5,7-pentahydroxyflavone
MFCD00006828
QUERTINE
Sophretin
QUERCETOL
QUERCETINE
SOPHORETIN
3,3',4',5,7-Pentahydroxyflavone

槲皮素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> PI3K/Akt/mTOR 信号通路 >> PI3K

天然产物 >> 黄酮类化合物

研究领域 >> 癌症

[ 靶点 ]

PI3Kβ:5.4 μM (IC50)

PI3Kδ:2.4 μM (IC50)

PI3Kγ:3 μM (IC50)

Autophagy

Mitophagy

[体外研究]

槲皮素是一种基于植物的化学物质或植物化学物质,用作补充剂,饮料或食品中的成分。在一些研究中,它可能具有抗炎和抗氧化特性,并且正在研究其广泛的潜在健康益处。槲皮素是一种PI3K抑制剂,IC50为2.4-5.4μM。它强烈消除PI3K和Src激酶,轻度抑制Akt1/2,并轻微影响PKC,p38和ERK1/2 [1]。槲皮素抑制TNF诱导的LDH％释放,EC依赖性中性粒细胞与牛肺动脉内皮细胞(BPAEC)的粘附,以及BPAEC DNA合成和增殖[2]。

[体内研究]

槲皮素(75mg/kg)和2-甲氧基雌二醇的组合增强了对人前列腺癌LNCaP和PC-3细胞异种移植肿瘤生长的抑制[3]。

[动物实验]

小鼠皮下接种5×105个PC-3细胞，悬浮在100μLPBS中，2×108个LNCaP细胞悬浮于100μL基质胶和右侧背部的PBS混合物（1：1）中。当异种移植肿瘤达到约100mm 3的体积时，将小鼠随机分配至四组（每组n = 8）并腹膜内处理。基于我们的体外结果，初步实验和许多其他研究人员的研究的治疗方案如下：（1）媒介物对照组：第1天的槲皮素载体，第2天的2-ME载体，（2）槲皮素处理组：第1天槲皮素75mg / kg，第2天2-ME载体，（3）2-ME处理组：第1天槲皮素载体，第2天2-ME 150mg / kg，（4）组合治疗组：第1天槲皮素75 mg / kg，第2天2-ME 150 mg / kg。两天为治疗周期，整个治疗过程持续4周。使用卡尺每2天监测肿瘤大小，并根据下式计算肿瘤体积：L×S2×0.5，其中L代表最长直径，S代表肿瘤的最短直径。小鼠也称重。在治疗过程结束时，在第29天，用水合氯醛麻醉小鼠并通过颈椎脱位处死。异种移植肿瘤快速取出并称重。其中一部分立即投入液氮中进行生物标记物分析，另一部分固定在10％中性缓冲福尔马林中进行免疫组化分析。还检测到反映药物毒性的血清生化参数如ALT，AST，肌酸酐和尿素氮。

[参考文献]

[1]. Navarro-Nú?ez L, et al. Effect of quercetin on platelet spreading on collagen and fibrinogen and on multiple platelet kinases. Fitoterapia. 2010 Mar;81(2):75-80.

[2]. Yu XB, et al. Inhibitory effects of protein kinase C inhibitors on tumor necrosis factor induced bovine pulmonary artery endothelial cell injuries. Yao Xue Xue Bao. 1996;31(3):176-81.

[3]. Yang F, et al. Combination of Quercetin and 2-Methoxyestradiol Enhances Inhibition of Human Prostate Cancer LNCaP and PC-3 Cells Xenograft Tumor Growth. PLoS One. 2015 May 26;10(5):e0128277.

[相关活性小分子]

槲皮素物理化学性质

[ 密度 ]:
1.8±0.1 g/cm3

[ 沸点 ]:
642.4±55.0 °C at 760 mmHg

[ 熔点 ]:
314-317°C

[ 分子式 ]:
C₁₅H₁₀O₇

[ 分子量 ]:
302.236

[ 闪点 ]:
248.1±25.0 °C

[ 精确质量 ]:
302.042664

[ PSA ]:
131.36000

[ LogP ]:
2.08

[ 外观性状 ]:
黄色至绿色-黄色结晶粉末

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.823

[ 储存条件 ]:
Store at 0-5°C

[ 水溶解性 ]:
<0.1 g/100 mL at 21 ºC

槲皮素MSDS

详细MSDS(安全技术说明书)

槲皮素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: LK8750000

CHEMICAL NAME :: Flavone, 3,3',4',5,7-pentahydroxy-

CAS REGISTRY NUMBER :: 117-39-5

BEILSTEIN REFERENCE NO. :: 0317313

LAST UPDATED :: 199709

DATA ITEMS CITED :: 60

MOLECULAR FORMULA :: C15-H10-O7

MOLECULAR WEIGHT :: 302.25

WISWESSER LINE NOTATION :: T66 BO EVJ CR CQ DQ& DQ GQ IQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 161 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 159 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - muscle weakness Lungs, Thorax, or Respiration - respiratory depression

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3 gm/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 97 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - muscle weakness Lungs, Thorax, or Respiration - respiratory depression

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 18 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 33610 mg/kg/58W-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Gastrointestinal - tumors Kidney, Ureter, Bladder - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 966 gm/kg/23W-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Lungs, Thorax, or Respiration - tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 38235 mg/kg/58W-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Gastrointestinal - tumors Kidney, Ureter, Bladder - tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 243 gm/kg/3Y-C

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Liver - tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 487 gm/kg/3Y-C

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Liver - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 20 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 16 mg/kg

SEX/DURATION :: male 5 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Sperm Morphology

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Micronucleus test

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Mammal - cattle Cells - not otherwise specified

DOSE/DURATION :: 12 umol/L

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 44,882,1988 *** REVIEWS *** IARC Cancer Review:Animal Limited Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 31,213,1983 IARC Cancer Review:Human No Adequate Data IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 31,213,1983 IARC Cancer Review:Group 3 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,56,1987

槲皮素安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310 + P330

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic

[ 风险声明 (欧洲) ]:
R25;R40

[ 安全声明 (欧洲) ]:
S45

[ 危险品运输编码 ]:
2811

[ RTECS号 ]:
LK8750000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2932999099

槲皮素合成路线

详细合成路线

槲皮素上下游产品

槲皮素上游产品

槲皮素下游产品

槲皮素制备

1.栎皮酮及其衍生物广泛存在于各种蔬菜水果中，是黄酮的衍生物。可由百合科植物洋葱和其他植物提取物如芸香苷、檞苷、异檞苷、茴香苷、檞皮黄苷、腊梅苷中得到。

槲皮素海关

[ 海关编码 ]: 2914501900

[ 中文概述 ]:
2914501900 其他酮酚。监管条件:无。增值税率:17.0%。退税率:9.0%。最惠国关税:5.5%。普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 丙酮报明包装

[ Summary ]:
2914501900 other ketone-phenols。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:5.5%。General tariff:30.0%

槲皮素文献

Hesperetin inhibit adipocyte differentiation and enhance Bax- and p21-mediated adipolysis in human mesenchymal stem cell adipogenesis.

J. Biochem. Mol. Toxicol. 29(3) , 99-108, (2015)

We aimed to explore the antiadipogenic and adipolysis effect of hesperetin in human mesenchymal stem cells (hMSCs)-induced adipogenesis. IC50 value of hesperetin was higher for hMSCs such as 149.2 ± 1...

Quercetin promotes cell apoptosis and inhibits the expression of MMP-9 and fibronectin via the AKT and ERK signalling pathways in human glioma cells.

Neurochem. Int. 80 , 60-71, (2015)

Gliomas are the most common and malignant primary brain tumours and are associated with a poor prognosis despite the availability of multiple therapeutic options. Quercetin, a traditional Chinese medi...

The identification of a novel SIRT6 modulator from Trigonella foenum-graecum using ligand fishing with protein coated magnetic beads.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 968 , 105-11, (2014)

SIRT6 is a histone deacetylase that has been proposed as a potential therapeutic target for metabolic disorders and the prevention of age-associated diseases. Thus the identification of compounds that...

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槲皮素