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茴香霉素

茴香霉素用途

Anisomycin是一种有效的蛋白质合成抑制剂,它通过抑制肽基转移酶或80S核糖体系统干扰蛋白质和DNA合成。

茴香霉素名称

[ CAS 号 ]:
22862-76-6

[ 中文名 ]:
茴香霉素

[ 英文名 ]:
Anisomycin

[英文别名 ]:

antibioticpa-106
ANISOMYCIN,STREPTOMYCES GRISEOLUS
EINECS 245-269-7
MFCD00077650
Anisomycin
FLAGECIDIN
Anisomycin from Streptomyces griseolus

茴香霉素生物活性

[ 描述 ]:

Anisomycin是一种有效的蛋白质合成抑制剂,它通过抑制肽基转移酶或80S核糖体系统干扰蛋白质和DNA合成。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

研究领域 >> 癌症

[ 靶点 ]

DNA synthesis[1]

[体外研究]

为了检查JNK是否在PC-12细胞中的粘菌素诱导的神经毒性中具有核心作用,在该研究中使用SP600125(JNK的高选择性抑制剂)和Anisomycin(强效激活剂)。为了选择合适的浓度,分别用一系列SP600125(0-80μM)和Anisomycin(0-20μM)处理PC-12细胞24小时。结果显示,SP600125处理以浓度依赖性方式显着降低细胞存活率,在大于20μM的浓度下观察到(p <0.01)。类似地,通过Anisomycin处理(≥8μM)抑制细胞活力(p <0.05)[1]。

[体内研究]

TNFRp55/p75的破坏减弱了Anisomycin诱导的心室功能改善。 Anisomycin导致左心室发展压力(LVDP)的改善,其在TNFR p55/p75破坏的动物中消失。此外,通过删除TNFR p55/p75消除了野生型动物中的Anisomycin诱导的LVEDP改善。同样地,TNFR p55/p75的破坏消除了通过预处理Anisomycin引起的速率压力产物(RPP)的回收。与对照野生型小鼠相比,没有使用Anisomycin处理的TNFR p55/p75 -/-小鼠在心脏功能恢复方面没有显示出差异。野生型和TNFR p55/p75缺陷小鼠的心率没有显着差异。为了观察Nox2是否参与Anisomycin诱导的心肌保护,用Anisomycin处理Nox2缺陷型小鼠。与野生型小鼠相比,在Nox2 -/-小鼠中消除了在Anisomycin处理的小鼠中LVEDP的改善。此外,在Nox2 -/-小鼠中减轻了用Anisomycin处理的野生型小鼠中RPP的恢复。与野生型对照小鼠相比,没有使用Anisomycin处理的Nox2 -/-小鼠在心脏功能恢复方面没有显示出差异[2]。

[细胞实验]

将PC-12细胞以1×10 4个细胞/孔的浓度接种于96孔板中，并在37℃，5％CO 2的培养箱中培养至少12小时，然后暴露于不同浓度的SP600125（0- 80μM）或Anisomycin（0-20μM）24小时。随后，将培养基加入20μL5mg/ mL MTT工作溶液中，并将板在37℃下温育2小时。除去培养上清液，将甲crystals晶体溶于150μLDMSO中。最后，通过酶标仪在490nm处测量每个孔的吸光度。细胞活力表示为对照组的百分比，设定为100％[1]。

[动物实验]

小鼠[2]在该研究中使用成年雄性TNFRp55 / p75小鼠，成年雄性野生型C57 / BL和纯合型Nox2 - / - 小鼠。将小鼠随机分成六个实验组，进行以下治疗。将动物分为六组：第1组：对照缺血/再灌注，向野生型小鼠注射DMSO（0.1mL）;第2组：Anisomycin +野生型小鼠，野生型小鼠注射Anisomycin（0.1 mg / kg ip）;组3：Anisomycin + TNFR p55 / p75 - / - 小鼠，TNFR p55 / 75 - / - 小鼠注射Anisomycin（0.1mg / kg ip）;第4组：TNFR p55 / p75 - / - 小鼠，TNFR p55 / 75 - / - 小鼠未注射Anisomycin;组5：Anisomycin + Nox2 - / - 小鼠，Nox2 - / - 小鼠注射Anisomycin（0.1mg / kg ip）;和第6组：Nox2 - / - 小鼠，Nox2 - / - 小鼠未注射Anisomycin。后来（24小时），心脏缺血30分钟，再灌注30分钟[2]。

[参考文献]

[1]. Lu Z, et al. Colistin-induced autophagy and apoptosis involves the JNK-Bcl2-Bax signaling pathway and JNK-p53-ROS positive feedback loop in PC-12 cells.

[2]. Zhao TC, et al. Disruption of Nox2 and TNFRp55/p75 eliminates cardioprotection induced by Anisomycin. Am J Physiol Heart Circ Physiol. 2012 Nov 15;303(10):H1263-72.

[相关活性小分子]

放线菌酮 | 放线菌素D | Alpha-毒伞肽 | SCR7 | CX-5461 | 布拉扑兰 | COH29 | 曲西立滨 | 叶酸 | 氢溴酸常山酮 | RG7800 | N-[4-氟-3-(三氟甲基)苯基]-N'-[5-(4-吡啶基)-1,3,4-噻二唑-2-基]脲 | 腺嘌呤 | 奈达铂 | 2-[(3-氨基吡啶-2-基)亚甲基]氨基硫脲

茴香霉素物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
398.7±42.0 °C at 760 mmHg

[ 熔点 ]:
140-141ºC

[ 分子式 ]:
C₁₄H₁₉NO₄

[ 分子量 ]:
265.305

[ 闪点 ]:
194.9±27.9 °C

[ 精确质量 ]:
265.131409

[ PSA ]:
67.79000

[ LogP ]:
0.42

[ 外观性状 ]:
白色结晶固体

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.558

[ 储存条件 ]:
库房通风低温干燥,与食品原料分开存放

茴香霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: BZ9800000

CHEMICAL NAME :: Anisomycin

CAS REGISTRY NUMBER :: 22862-76-6

BEILSTEIN REFERENCE NO. :: 0020705

LAST UPDATED :: 199612

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C14-H19-N-O4

MOLECULAR WEIGHT :: 265.34

WISWESSER LINE NOTATION :: T5MTJ B1R DO1& COV1 DQ

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 :: 72 mg/kg

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

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 345 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 230 mg/kg

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

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 167 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 148 mg/kg

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

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 600 mg/kg

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

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 10 mg/kg

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

REFERENCE :: 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 5,77,1981

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >300 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >100 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >100 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >300 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >50 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: >200 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >200 mg/kg

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

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 300 mg/kg

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

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 5,490,1955 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5265 No. of Facilities: 63 (estimated) No. of Industries: 1 No. of Occupations: 4 No. of Employees: 504 (estimated) No. of Female Employees: 420 (estimated)

茴香霉素安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 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

[ 安全声明 (欧洲) ]:
45-36-26

[ 危险品运输编码 ]:
UN 3462 6

[ WGK德国 ]:
3

[ RTECS号 ]:
BZ9800000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933990090

茴香霉素合成路线

详细合成路线

茴香霉素上下游产品

茴香霉素上游产品

茴香霉素下游产品

茴香霉素制备

茴香霉素海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

茴香霉素文献

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...

Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.

Eur. J. Med. Chem. 45 , 4813-26, (2010)

In this study, we have explored the structure activity relationships of substrates of two major, promiscuous, multidrug transporters of an opportunistic human pathogen Candida albicans namely, CaCdr1p...

Trophic factor-induced activity 'signature' regulates the functional expression of postsynaptic excitatory acetylcholine receptors required for synaptogenesis.

Sci. Rep. 5 , 9523, (2015)

Highly coordinated and coincidental patterns of activity-dependent mechanisms ("fire together wire together") are thought to serve as inductive signals during synaptogenesis, enabling neuronal pairing...

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