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葛根素

葛根素用途

葛根素是从葛根中提取的异黄酮,是5-HT2C受体拮抗剂。

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葛根素名称

[ CAS 号 ]:
3681-99-0

[ 中文名 ]:
葛根素

[ 英文名 ]:
Puerarin

[中文别名 ]:

[英文别名 ]:

8-(β-D-Glucopyranosyl)-4',7-dihydroxyisoflavone
Puerarin std.
Puerqarin
Pueraria flavonoids
MFCD00076007
Puerain
Puerarine
Kakonein
daidzein-8-C-glucose
Purerarin

葛根素生物活性

[ 描述 ]:

葛根素是从葛根中提取的异黄酮,是5-HT2C受体拮抗剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

天然产物 >> 黄酮类化合物

研究领域 >> 炎症/免疫

[体外研究]

葛根素抑制LPS诱导的iNOS,COX-2和CRP蛋白的表达,并且还抑制其在RAW264.7细胞中的RT-PCR实验中的mRNA。 iNOS,COX-2和CRP表达的抑制是由于磷酸化和I-κB降解的剂量依赖性抑制,导致p65NF-κB核转位的减少。葛根素介导的抑制LPS诱导的iNOS,COX-2和CRP表达的作用归因于在转录水平上抑制NF-κB活化[1]。葛根素是一种新型的IK1开放通道阻滞剂,可能是葛根素抗心律失常作用的基础。葛根素与IK1的开放通道阻滞剂钡竞争抑制IK1电流[2]。

[体内研究]

金雀异黄素和葛根素均可通过潜在的抗氧化,抗炎或抗凋亡机制有效缓解慢性酒精引起的肝损伤。然而,金雀异黄素在降低丙二醛水平方面比葛根素更有效(1.05±0.0947对比1.28±0.213 nmol/mg pro,p <0.05),肿瘤坏死因子α(3.12±0.498对3.82±0.277 pg/mg pro, p <0.05),白细胞介素-6(1.46±0.223对1.88±0.309 pg/mg pro,p <0.05),而葛根素在改善血清活性或丙氨酸转氨酶水平方面比金雀异黄素更有效(35.8±3.95 vs. 42.6) ±6.56 U/L,p <0.05)和低密度脂蛋白胆固醇(1.12±0.160对1.55±0.150 mmol/L,p <0.05)[3]。葛根素可显着改善早期肾损害,可能通过抑制糖尿病大鼠肾脏中ICAM-1和TNF-α的表达[4]。

[细胞实验]

RAW264.7细胞在95％空气和5％CO 2湿润气氛中维持在37℃的亚汇合状态。用于常规传代培养的培养基是Dulbecco's Modified Eagle's培养基，其补充有10％胎牛血清，青霉素（100单位/ mL）和链霉素（100μg/ mL）。 MTT测定用于测量用葛根素处理后细胞的活力。除去上清液用于亚硝酸盐测定后，将细胞在37℃下与MTT（0.05mg / mL）一起温育4小时，并在540nm处测量光密度。葛根素的浓度分别为10,20,40和100μM[1]。

[动物实验]

大鼠：将一组健康雄性SD大鼠（7周龄）随机分为对照组，模型组和具有高（H），中度（M）和低（L）剂量的葛根素治疗组。将葛根素重悬于0.9％生理盐水中，通过不同浓度的胃内插管给予（L组为0.25 mg /（kg×d），M组为0.5 mg /（kg×d），1.0 mg /（）每天连续8天每公斤×d）。在同一时间段内给予等量的生理盐水来控制和模拟大鼠[4]。小鼠：40只雄性ICR小鼠（体重：20-22g）适应每日12小时光照：在22±2℃室温和55％±5％相对湿度下12小时黑暗循环。适应1周后，将小鼠随机分成4组，每组10只小鼠。金雀异黄素和葛根素用羧甲基纤维素钠溶液施用于小鼠，等摩尔浓度为0.1M（胃体积：3mL kg-1体重）[3]。

[参考文献]

[1]. Hu W, et al. Puerarin inhibits iNOS, COX-2 and CRP expression via suppression of NF-κB activation in LPS-induced RAW264.7 macrophage cells. Pharmacol Rep. 2011;63(3):781-9.

[2]. Zhang H, et al. Puerarin: a novel antagonist to inward rectifier potassium channel (IK1). Mol Cell Biochem. 2011 Jun;352(1-2):117-23.

[3]. Zhao L,et al. Protective Effects of Genistein and Puerarin against Chronic Alcohol-Induced Liver Injury in Mice via Antioxidant, Anti-inflammatory, and Anti-apoptotic Mechanisms.J Agric Food Chem. 2016 Sep 28;64(38):7291-7.

[4]. Pan X, et al. Effect of Puerarin on Expression of ICAM-1 and TNF-α in Kidneys of Diabetic Rats. Med Sci Monit. 2015 Jul 23;21:2134-40.

[相关活性小分子]

葛根素物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
791.2±60.0 °C at 760 mmHg

[ 熔点 ]:
187-189°C

[ 分子式 ]:
C₂₁H₂₀O₉

[ 分子量 ]:
416.38

[ 闪点 ]:
281.5±26.4 °C

[ PSA ]:
160.82000

[ LogP ]:
-0.67

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
0.0±2.9 mmHg at 25°C

[ 折射率 ]:
1.717

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
可溶于：甲醇

葛根素MSDS

详细MSDS(安全技术说明书)

葛根素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UO5216000

CHEMICAL NAME :: Puerarin

CAS REGISTRY NUMBER :: 3681-99-0

BEILSTEIN REFERENCE NO. :: 0064198

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C21-H20-O9

MOLECULAR WEIGHT :: 416.41

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 738 mg/kg

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

REFERENCE :: CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year: 6,166,1985

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葛根素安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
F,C

[ 风险声明 (欧洲) ]:
R11

[ 安全声明 (欧洲) ]:
22-24/25-45-36/37/39-26-16

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
UO5216000

[ 海关编码 ]:
2932999099

葛根素合成路线

详细合成路线

葛根素海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

葛根素文献

The transgenic Arabidopsis plant system, pER8-GFP, as a powerful tool in searching for natural product estrogen-agonists/antagonists.

J. Nat. Prod. 68 , 971-3, (2005)

The transgenic Arabidopsis plant system, pER8-GFP, may be used as a powerful tool in searching for natural estrogen-agonists/antagonists. Among selected plant extracts and natural products, the method...

UFLC-MS/MS method for simultaneous determination of luteolin-7-O-gentiobioside, luteolin-7-O-β-D-glucoside and luteolin-7-O-β-D-glucuronide in beagle dog plasma and its application to a pharmacokinetic study after administration of traditional Chinese medicinal preparation: Kudiezi injection.

J. Pharm. Biomed. Anal. 72 , 127-33, (2013)

A rapid, sensitive and selective ultra-fast liquid chromatography-tandem mass spectrometry (UFLC-MS/MS) method for the simultaneous determination of three active flavonoid glycosides: luteolin-7-O-gen...

Glucose uptake enhancing activity of puerarin and the role of C-glucoside suggested from activity of related compounds.

Bioorg. Med. Chem. Lett. 20 , 4333-6, (2010)

Chemical treatment of diabetes mellitus is widely studied and controlling of blood glucose level is the main course of therapy. In type 2 diabetes mellitus, insulin resistance is the major problem. An...

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葛根素