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维生素E醋酸酯

维生素E醋酸酯用途

Puromycin aminonucleoside 是一种氨基核苷类抗生素,为嘌呤霉素类似物,但并不影响蛋白质合成或诱导凋亡。

维生素E醋酸酯名称

[ CAS 号 ]:
58-60-6

[ 中文名 ]:
氨基核苷嘌呤霉素

[ 英文名 ]:
Stylomycin aminonucleoside

[中文别名 ]:

[英文别名 ]:

3'-amino-3'-deoxy-N(6),N(6)-dimethyladenosine
EINECS 200-388-3
MFCD00063462
Adenosine, 3'-amino-3'-deoxy-N,N-dimethyl-
3'-Amino-3'-deoxy-N,N-dimethyladenosine
PUROMYCIN AMINONUCLEOSIDE

维生素E醋酸酯生物活性

[ 描述 ]:

Puromycin aminonucleoside 是一种氨基核苷类抗生素,为嘌呤霉素类似物,但并不影响蛋白质合成或诱导凋亡。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> MDM-2/p53

研究领域 >> 癌症

[体外研究]

嘌呤霉素氨基核苷(30μg/ mL)显着增加足细胞中的p53蛋白水平。嘌呤霉素氨基核苷诱导的足细胞凋亡是p53依赖性的,并且支持地塞米松通过p53的下调对暴露于嘌呤霉素氨基核苷的细胞发挥抗细胞凋亡作用的观点。嘌呤霉素氨基核苷以时间依赖的方式诱导足细胞凋亡[1]。表达PMAT和载体转染的细胞的IC 50值分别为48.9和122.1μM,表明PMAT增强的细胞对嘌呤霉素氨基核苷的敏感性表达。嘌呤霉素氨基核苷(250μM)对表达PMAT和载体转染的细胞均有毒性。表达PMAT的细胞中的嘌呤霉素氨基核苷摄取在pH6.6时比pH7.4时高4倍[2]。

[体内研究]

对照大鼠中每个肾小球的足细胞数量为95.5±17.6,第4天为90.7,在嘌呤霉素氨基核苷(8mg/100g,iv)处理的肾病大鼠中。对照组大鼠肾小球nephrin含量为1.02±0.11 fmol,第4天和第7天嘌呤霉素氨基核苷肾病大鼠nephrin含量降至0.46±0.06 fmol和0.35±0.04 fmol。与足细胞相关的nephrin含量显着降低。嘌呤霉素氨基核苷肾病大鼠蛋白尿的发生[3]。给予嘌呤霉素氨基核苷(100 mg/kg,sc)的大鼠体重增加较少,血清肌酐水平高于对照组大鼠,表明imPuromycin氨基核苷酸肾功能[4]。

[细胞实验]

将细胞以5,000个细胞/孔的密度接种在96孔板上的含有10％FBS的MEM中。在孵育48小时后（约40-50％汇合），将细胞更换为含有不同浓度的嘌呤霉素氨基核苷的新鲜生长培养基。对于保护实验，将细胞在含有250μM嘌呤霉素氨基核苷的培养基中培养，有或没有PMAT抑制剂癸-22（2μM）。在37℃的95％O 2培养箱中孵育总共72小时后，洗涤细胞和平板。通过使用非线性回归（WinNonLin版本3.2）将细胞生长数据拟合到以下模型来确定IC 50值：S = Smax - [Smax-S0]×[Cγ/（Cγ+IC50γ）]，其中S是细胞存活表示为未处理对照细胞的光密度百分比，Smax是最大细胞存活率，S0是高药物浓度下的最低残留细胞存活率，C是嘌呤霉素氨基核苷浓度，γ是希尔系数，IC50是嘌呤霉素氨基核苷浓度导致半数最大细胞存活。在每个实验中进行五至六次测定，并进行四次独立实验。

[动物实验]

11周龄的雄性F344大鼠购自JaPuromycin氨基核苷SLC。在本研究中使用正常大鼠和嘌呤霉素氨基核苷肾病模型。通过在盐水中以8mg / 100g体重的剂量单次静脉内注射嘌呤霉素氨基核苷，在大鼠中诱导嘌呤霉素氨基核苷肾病。对照动物接受相同体积的盐水。在嘌呤霉素氨基核苷注射后第4天和第7天研究肾病大鼠（每组n = 6）。

[参考文献]

[1]. Wada T, et al. Dexamethasone prevents podocyte apoptosis induced by puromycin aminonucleoside: role of p53 and Bcl-2-related family proteins. J Am Soc Nephrol. 2005 Sep;16(9):2615-25.

[2]. Xia L, et al. Podocyte-specific expression of organic cation transporter PMAT: implication in puromycin aminonucleosidenephrotoxicity. Am J Physiol Renal Physiol. 2009 Jun;296(6):F1307-13.

[3]. Kawakami H, et al. Dynamics of absolute amount of nephrin in a single podocyte in puromycin aminonucleoside nephrosis rats calculated by quantitative glomerular proteomics approach with selected reaction monitoring mode. Nephrol Dial Transplant. 2012 Apr;

[4]. Nosaka K, et al. An adenosine deaminase inhibitor prevents puromycin aminonucleoside nephrotoxicity. Free Radic Biol Med 1997 ;22 (4): 597-605.

[相关活性小分子]

维生素E醋酸酯物理化学性质

[ 密度 ]:
1.7±0.1 g/cm3

[ 沸点 ]:
595.6±60.0 °C at 760 mmHg

[ 熔点 ]:
235℃ (Decomposition)

[ 分子式 ]:
C₁₂H₁₈N₆O₃

[ 分子量 ]:
294.310

[ 闪点 ]:
314.0±32.9 °C

[ 精确质量 ]:
294.144043

[ PSA ]:
122.55000

[ LogP ]:
0.02

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.776

[ 储存条件 ]:
库房通风低温干燥

[ 水溶解性 ]:
H2O: 50 mg/mL, clear, slightly yellow | Soluble in water at 50mg/ml. May require heating

维生素E醋酸酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AU7337000

CHEMICAL NAME :: Adenosine, 3'-amino-3'-deoxy-N,N-dimethyl-

CAS REGISTRY NUMBER :: 58-60-6

BEILSTEIN REFERENCE NO. :: 0093902

LAST UPDATED :: 199709

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C12-H18-N6-O3

MOLECULAR WEIGHT :: 294.36

WISWESSER LINE NOTATION :: T56 BN DN FN HNJ IN1&1 D- BT5OTJ CQ DZ E1Q

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 105 ug/kg

SEX/DURATION :: female 5-11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 45 mg/kg

SEX/DURATION :: female 8-10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - urogenital system

TYPE OF TEST :: DNA inhibition

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 83 mg/kg

REFERENCE :: JCLBA3 Journal of Cell Biology. (Rockefeller Univ. Press, 1230 York Ave., New York, NY 10003) V.12- 1962- Volume(issue)/page/year: 30,13,1966

维生素E醋酸酯安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H373

[ 靶器官 ]:
Kidney

[ 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) ]:
48/22

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

[ WGK德国 ]:
3

[ RTECS号 ]:
AU7337000

维生素E醋酸酯合成路线

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维生素E醋酸酯文献

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