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浅蓝菌素

浅蓝菌素用途

Cerulenin 是一种广泛使用的天然脂肪酸合成酶 (FAS) 抑制剂。Cerulenin 是由真菌 Cephalosporium caeruleus 产生的。

浅蓝菌素名称

[ CAS 号 ]:
17397-89-6

[ 中文名 ]:
浅蓝菌素

[ 英文名 ]:
Cerulenin

[中文别名 ]:

[英文别名 ]:

2,3-Epoxy-4-oxo-7,10-dodecadienamide
trans-dodecadienamide)
3S)-2,3-epoxy-4-oxo-7,10-trans
caerulein A
EINECS 241-424-8
Helicocerin
MFCD00077686
Cerulenin

浅蓝菌素生物活性

[ 描述 ]:

Cerulenin 是一种广泛使用的天然脂肪酸合成酶 (FAS) 抑制剂。Cerulenin 是由真菌 Cephalosporium caeruleus 产生的。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 脂肪酸合成酶(FAS)

研究领域 >> 代谢疾病

[ 靶点 ]

Fatty acid synthase (FAS)[1]

[体外研究]

Cerulenin共价结合FAS的催化位点并破坏乙酰-CoA和丙二酰-CoA的缩合反应,抑制酵母中脂肪酸和甾醇的生物合成。黄酮类化合物槲皮素和反式查耳酮对红色毛癣菌有效,野生型菌株(MYA3108)的MIC为125和7.5μg/ mL,ABC转运突变株(ΔTruMDR2)的MIC为63和1.9μg/ mL,分别。 Fluconazole和Cerulenin对照的MIC分别为野生型菌株63和125μg/ mL,突变菌株30和15μg/ mL [1]。为了探讨类固醇激素急性调节蛋白(StAR)对内皮功能障碍模型的保护作用的潜在机制,在棕榈酸之前使用脂肪酸合成酶抑制剂和HMG-CoA还原酶,Cerulenin(5μg/ mL)和洛伐他汀( PA)补充说。通过抑制剂处理,IL-1β,TNFα,VCAM-1和IL-6的mRNA表达降低,而NO产生恢复[2]。

[体内研究]

Cerulenin治疗ob/ob小鼠对体重有明显影响。经过2天的治疗,与对照组的5.7％体重增加相比,治疗小鼠的体重降低。经过长时间(7天)治疗,未观察到体重减轻,但体重增加减慢。在所有组中,60mg/kg的Cerulenin在抑制体重增加方面比30mg/kg更有效。如果每天或每隔一天给药,通过7天60mg/kg蓝绿素的治疗,ATP含量分别增加58.1％和61.5％。用60mg/kg青霉素处理仅2天也观察到显着的ATP升高。相比之下,给予2天或7天的30 mg/kg Cerulenin对细胞ATP含量没有任何显着影响[3]。

[细胞实验]

分离大鼠主动脉内皮细胞（RAEC）并进行少量修改。简言之，从雄性Wistar大鼠（150-180g）切除胸主动脉的片段，并立即置于含有100U / mL青霉素和100mg / mL链霉素的冷PBS中。去除外膜脂肪后，将主动脉切成1毫米宽的环。转移至T-25cm 2烧瓶后，将环在含有20％胎牛血清，2.5ng / mL碱性成纤维细胞生长因子，100U / mL青霉素和100mg / mL链霉素的培养基199中培养。将主动脉环置于37℃，5％CO 2的潮湿气氛中72-80小时，不移动。当细胞迁移时，所有主动脉环都被移除。通过CD31和vWF染色证实其微血管细胞学特征。在涉及PA处理的实验中，使用补充有1％牛血清白蛋白的M199培养基。所有实验均使用RAEC进行至第4代。在使用抑制剂的实验中，在培养物中加入5μg/ mL Cerulenin（在ethonal中）或5μM洛伐他汀（在DMSO中）或3.3μg/ mL Cerulenin加3.3μM洛伐他汀PA处理前24小时培养基。与对照[2]同时添加相同体积的溶剂。

[动物实验]

小鼠[3]在含有20％DMSO腹膜内（ip）的RPMI培养基中给予6-8周龄雄性ob / ob小鼠青霉素。仅用载体类似地注射对照。实验组（每组4只小鼠）如下：A：60mg / kg /天Cerulenin，每天注射7天; B：每隔一天60mg / kg，持续7天; C：30mg / kg /天，持续7天; D：每隔一天30mg / kg，持续7天; E：车辆，每天7天; F：60mg / kg /天Cerulenin 2天; G：30mg / kg /天Cerulenin 2天; H：车辆，每天2天;我：控制。在麻醉下在同一天处死所有动物。通过门静脉穿刺收集血液。将肝脏样品在液氮中快速冷冻并储存在-80℃直至分析，或多聚甲醛固定用于组织学分析。

[参考文献]

[1]. Bitencourt TA, et al. Trans-chalcone and quercetin down-regulate fatty acid synthase gene expression and reduce ergosterol content in the human pathogenic dermatophyte Trichophyton rubrum. BMC Complement Altern Med. 2013 Sep 17;13:229.

[2]. Tian D, et al. Overexpression of steroidogenic acute regulatory protein in rat aortic endothelial cells attenuates palmitic acid-induced inflammation and reduction in nitric oxide bioavailability. Cardiovasc Diabetol. 2012 Nov 21;11:144.

[3]. Cheng G, et al. Cerulenin blockade of fatty acid synthase reverses hepatic steatosis in ob/ob mice. PLoS One. 2013 Sep 27;8(9):e75980.

[相关活性小分子]

奥利司他 | C75 | 4-(1-(5-(3,4-Dimethyl-1H-pyrazol-5-yl)-2,4-dimethylbenzoyl)azetidin-3-yl)benzonitrile | HS79

浅蓝菌素物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
456.1±45.0 °C at 760 mmHg

[ 熔点 ]:
93.5℃

[ 分子式 ]:
C₁₂H₁₇NO₃

[ 分子量 ]:
223.268

[ 闪点 ]:
241.1±25.0 °C

[ 精确质量 ]:
223.120850

[ PSA ]:
72.69000

[ LogP ]:
0.94

[ 外观性状 ]:
白色至灰白色粉末

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.529

浅蓝菌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: JR1670000

CHEMICAL NAME :: 7,10-Dodecadienamide, 2,3-epoxy-4-oxo-

CAS REGISTRY NUMBER :: 17397-89-6

LAST UPDATED :: 199410

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C12-H17-N-O3

MOLECULAR WEIGHT :: 223.30

WISWESSER LINE NOTATION :: T3OTJ BVZ CV2U4U2

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 :: 547 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 211 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 245 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 154 mg/kg

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

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Microorganism - not otherwise specified

DOSE/DURATION :: 2 mg/L

REFERENCE :: JOBAAY Journal of Bacteriology. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1916- Volume(issue)/page/year: 133,472,1978

浅蓝菌素安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
24/25

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

[ WGK德国 ]:
3

[ RTECS号 ]:
JR1670000

浅蓝菌素文献

Purification and characterization of the Staphylococcus aureus bacillithiol transferase BstA.

Biochim. Biophys. Acta 1840(9) , 2851-61, (2014)

Gram-positive bacteria in the phylum Firmicutes synthesize the low molecular weight thiol bacillithiol rather than glutathione or mycothiol. The bacillithiol transferase YfiT from Bacillus subtilis wa...

Fatty acid synthase inhibitors induce apoptosis in non-tumorigenic melan-a cells associated with inhibition of mitochondrial respiration.

PLoS ONE 9(6) , e101060, (2014)

The metabolic enzyme fatty acid synthase (FASN) is responsible for the endogenous synthesis of palmitate, a saturated long-chain fatty acid. In contrast to most normal tissues, a variety of human canc...

A Duo of Potassium-Responsive Histidine Kinases Govern the Multicellular Destiny of Bacillus subtilis.

MBio 6 , e00581, (2015)

Multicellular biofilm formation and surface motility are bacterial behaviors considered mutually exclusive. However, the basic decision to move over or stay attached to a surface is poorly understood....

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