(-)-土曲霉酸

(-)-土曲霉酸用途

苯甲酸是一种醌类环氧化物抗生素,是一种有效的Btk抑制剂。土甲酸阻断PKC和Btk的pleckstrin同源结构域之间的相互作用。在IC50约为100μM的HMC-1人类肥大细胞的裂解物中,稀土酸抑制GST-BtkPH与PKC的结合[1]。

(-)-土曲霉酸名称

[ CAS 号 ]:
121-40-4

[ 中文名 ]:
(-)-土曲霉酸

[ 英文名 ]:
(-)-Terreic acid

[英文别名 ]:

(-)-土曲霉酸生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

研究领域 >> 炎症/免疫

信号通路 >> 蛋白酪氨酸激酶 >> BTK

[ 靶点 ]

Btk; Antibiotic[1]

[体外研究]

在较低浓度下,土甲酸抑制小鼠肥大细胞中Btk与PKCβII的结合(IC50≈30μM)。稀土酸抑制Btk的催化活性,但不抑制PKC[1]。土来酸(在抗原刺激3分钟之前预处理30分钟)抑制Btk自身磷酸化活性的基础水平和激活水平,IC50分别为10μM和3μM[1]。土甲酸以剂量依赖性方式抑制部分从重组杆状病毒感染的Sf9昆虫细胞中纯化的Btk的自磷酸化活性[1]。Western Blot分析[1]细胞系：小鼠骨髓来源的肥大细胞浓度：0,5,10,20μM培养时间：预处理30分钟结果：以剂量依赖性方式抑制Btk自身磷酸化活性的基础水平和激活水平。

[体内研究]

土油酸抑制体内过敏性皮肤反应的后期反应[1]。动物模型：BALB/c小鼠[1]剂量：0、0.15、1.5和15 mg/kg给药：抗原激发前1小时腹腔注射。在1小时和24小时测量耳厚结果：抗原激发后1小时检测的早期反应不受TA影响。相比之下,TA以剂量依赖性的方式抑制晚期(24小时)反应。

[参考文献]

[1]. Y Kawakami, et al. Terreic acid, a quinone epoxide inhibitor of Bruton's tyrosine kinase. Proc Natl Acad Sci U S A. 1999 Mar 2;96(5):2227-32.

(-)-土曲霉酸物理化学性质

[ 密度 ]:
1.613 g/cm3

[ 沸点 ]:
333.6ºC at 760 mmHg

[ 分子式 ]:
C₇H₆O₄

[ 分子量 ]:
154.12000

[ 精确质量 ]:
154.02700

[ PSA ]:
66.90000

[ 蒸汽压 ]:
9.63E-06mmHg at 25°C

[ 折射率 ]:
1.618

[ 储存条件 ]:
2-8°C，避光，干燥，密封

(-)-土曲霉酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RN8925000

CHEMICAL NAME :: 7-Oxabicyclo(4.1.0)hept-3-ene-2,5-dione, 3-hydroxy-4-methyl-, (1R)-

CAS REGISTRY NUMBER :: 121-40-4

LAST UPDATED :: 199409

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C7-H6-O4

MOLECULAR WEIGHT :: 154.13

WISWESSER LINE NOTATION :: T36 BO DV GV EUTJ E1 FQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 75 mg/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

TYPE OF TEST :: DNA adduct

MUTATION DATA

TYPE OF TEST :: DNA adduct

TEST SYSTEM :: Rodent - mouse Liver

DOSE/DURATION :: 200 mg/L

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: 10,249,1982

(-)-土曲霉酸安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302 + H312

[ 警示性声明 ]:
P280

[ 危害码 (欧洲) ]:
Xi

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

(-)-土曲霉酸文献

Studies on terreic acid.

Jpn. J. Antibiot. 33(3) , 320-8, (1980)

It was found that Aspergillus sp. No. Y-8980 which was isolated from a soil sample collected at Yoron Island in Kagoshima Prefecture belonged to Aspergillus terreus group by morphological observation....

An improved mouse model of atopic dermatitis and suppression of skin lesions by an inhibitor of Tec family kinases.

Allergol. Int. 56(4) , 403-9, (2007)

Atopic dermatitis is a chronic or chronically relapsing, pruritic inflammatory skin disease. The incidence of atopic dermatitis has dramatically increased during the past three decades in industrializ...

Characterization of versilin-sensitive sites in self-sensitive producer and sensitive non-producer or unrelated organism.

J. Appl. Bacteriol. 67(2) , 191-200, (1989)

Studies on self-sensitivity of producer mutant vs. sensitivity of non-producer parent and unrelated organism showed that versilin inhibited spore germination and sporulation in the self-sensitive prod...

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