瑞香素

瑞香素用途

Daphnetin (7,8-dihydroxycoumarin) 是从 Genus Daphne 中分离得到的一种香豆素衍生物,是一种蛋白酶 (protein kinase) 抑制剂,对 EGFR、PKA 和 PKC 的 IC50 值分别为 7.67 μM、9.33 μM 和 25.01 μM。Daphnetin (7,8-dihydroxycoumarin) 是用于抗炎、抗过敏疾病的植物次生代谢产物药物,也已被临床用于治疗凝血功能障碍、类风湿性关节炎等疾病,具有抗疟疾、解热等特性。

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瑞香素名称

[ CAS 号 ]:
486-35-1

[ 中文名 ]:
瑞香素

[ 英文名 ]:
Daphnetin

[中文别名 ]:

[英文别名 ]:

Daphnetin
7,8-Dihydroxychromen-2-one
7,8-Dihydroxycoumarin
7,8-dihydroxy-coumarin
2H-1-Benzopyran-2-one, 7,8-dihydroxy-
EINECS 207-632-8
7,8-Dihydroxy-2H-chromen-2-one
7,8-Dihydroxy-2H-1-benzopyran-2-one
MFCD00016977
TCMDC-125839

瑞香素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

信号通路 >> JAK/STAT信号通路 >> EGFR

信号通路 >> 蛋白酪氨酸激酶 >> PKA

信号通路 >> 蛋白酪氨酸激酶 >> EGFR

信号通路 >> 干细胞及 Wnt 通路 >> PKA

研究领域 >> 炎症/免疫

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

[ 靶点 ]

EGFR:7.67 μM (IC50)

PKA:9.33 μM (IC50)

PKC:25.01 μM (IC50)

[参考文献]

[1]. Yang EB, et al. Daphnetin, one of coumarin derivatives, is a protein kinase inhibitor. Biochem Biophys Res Commun. 1999 Jul 14;260(3):682-5.

[2]. Lv H, et al. Daphnetin-mediated Nrf2 antioxidant signaling pathways ameliorate tert-butyl hydroperoxide (t-BHP)-induced mitochondrial dysfunction and cell death. Free Radic Biol Med. 2017 May;106:38-52.

[3]. Jiménez-Orozco FA, et al. Differential effects of esculetin and daphnetin on in vitro cell proliferation and in vivo estrogenicity. Eur J Pharmacol. 2011 Oct 1;668(1-2):35-41.

瑞香素物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
430.4±45.0 °C at 760 mmHg

[ 熔点 ]:
265-268°C (dec.)

[ 分子式 ]:
C₉H₆O₄

[ 分子量 ]:
178.14

[ 闪点 ]:
184.5±22.2 °C

[ 精确质量 ]:
178.026611

[ PSA ]:
70.67000

[ LogP ]:
0.77

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.689

[ 储存条件 ]:
2~8°C，密封

[ 水溶解性 ]:
可溶于：甲醇；极微溶：苯,乙醚,氯仿

瑞香素MSDS

详细MSDS(安全技术说明书)

瑞香素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GN6382600

CHEMICAL NAME :: Coumarin, 7,8-dihydroxy-

CAS REGISTRY NUMBER :: 486-35-1

BEILSTEIN REFERENCE NO. :: 0009372

LAST UPDATED :: 199612

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C9-H6-O4

MOLECULAR WEIGHT :: 178.15

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5370 mg/kg

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

REFERENCE :: YHTPAD Yaoxue Tongbao. Bulletin of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.13-23, 1978-88. For publisher information, see ZYZAEU. Volume(issue)/page/year: 22,87,1987

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 429 mg/kg

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

REFERENCE :: YHTPAD Yaoxue Tongbao. Bulletin of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.13-23, 1978-88. For publisher information, see ZYZAEU. Volume(issue)/page/year: 22,87,1987

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 375 mg/kg

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

REFERENCE :: YHTPAD Yaoxue Tongbao. Bulletin of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.13-23, 1978-88. For publisher information, see ZYZAEU. Volume(issue)/page/year: 22,87,1987

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瑞香素安全信息

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

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
S22-S24/25

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

[ WGK德国 ]:
2

[ RTECS号 ]:
GN6382600

[ 海关编码 ]:
2942000000

瑞香素合成路线

详细合成路线

瑞香素上下游产品

瑞香素上游产品

瑞香素下游产品

瑞香素海关

[ 海关编码 ]: 2932209090

[ 中文概述 ]:
2932209090. 其他内酯. 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 ]:
2932209090. other lactones. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

瑞香素文献

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

Nat. Chem. Biol. 5 , 765-71, (2009)

Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened...

Thousands of chemical starting points for antimalarial lead identification.

Nature 465 , 305-10, (2010)

Malaria is a devastating infection caused by protozoa of the genus Plasmodium. Drug resistance is widespread, no new chemical class of antimalarials has been introduced into clinical practice since 19...

更多文献

瑞香素相关知识

瑞香素的生物活性和实验方法

2018-10-19 12:04:32

瑞香素是一种天然香豆素衍生物，是一种抑制EGFR（IC50：7.67μM），PKA（IC50：9.33μM）和PKC（IC50：25.01μM）的蛋白激酶抑制剂，也具有抗氧化和抗炎活性。它的靶点活性为EGFR,7.67μM；PKA,9.33μM；PKC,25.01μM。一、瑞香素的生物活性详解：1...

瑞香素