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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。

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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

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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。

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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...

更多文献

槲皮素

槲皮素用途

槲皮素名称

槲皮素生物活性

槲皮素物理化学性质

槲皮素MSDS

详细MSDS(安全技术说明书)

槲皮素毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

槲皮素安全信息

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

槲皮素海关

槲皮素文献

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