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啶南平A

啶南平A用途

Pyripyropene A 是一种高效、选择性的 SOAT2/ACAT2 抑制剂,其 IC50 值为 0.07 µM。Pyripyropene A 在体内能减轻高胆固醇血症和动脉粥样硬化。

啶南平A名称

[ CAS 号 ]:
147444-03-9

[ 中文名 ]:
啶南平A

[ 英文名 ]:
Pyripyropene A

[英文别名 ]:

Homopurine
1,3,5,7-Tetraazanaphthalene
pyripropen A
Pyrimidopyrimidin

啶南平A生物活性

[ 描述 ]:

Pyripyropene A 是一种高效、选择性的 SOAT2/ACAT2 抑制剂,其 IC50 值为 0.07 µM。Pyripyropene A 在体内能减轻高胆固醇血症和动脉粥样硬化。

[ 相关类别 ]:

研究领域 >> 心血管疾病

研究领域 >> 感染

研究领域 >> 炎症/免疫

[ 靶点 ]

IC50: 0.07 µM (ACAT2)[1]

[体外研究]

吡咯烷酮A(0-100μM；72小时)对人脐静脉内皮细胞具有抗增殖活性,IC50值为1.8μM[1]。吡咯烷酮A(10μM；24小时)以剂量依赖的方式抑制VEGF(20 ng/ml)诱导的huvec迁移和管状形成[1]。吡咯烷酮A对KB3-1、K562和神经2a细胞无生长抑制作用[1]。细胞增殖试验[1]细胞系：HUVECs浓度：0-100μM培养时间：72小时结果：对HUVECs具有抗增殖活性,IC50值为1.8μM。

[体内研究]

吡咯烷酮A(10-50 mg/kg/天；p.o；12周)降低载脂蛋白E基因敲除小鼠血浆胆固醇、极低密度脂蛋白(VLDL)、低密度脂蛋白(LDL)和肝胆固醇含量。吡咯烷酮A治疗的小鼠显示主动脉和心脏的致动脉粥样硬化病变区域减少[3]。吡咯烷酮A抑制肝脏e酰基辅酶A:胆固醇酰基转移酶2(ACAT2)在体内的活性[3]。吡咯烷酮A的半衰期(t1/2)为0.693/λ,其中λ表示浓度-时间曲线对数线性部分的终端斜率[4]。动物模型：雄性C57BL/6小鼠[2]剂量：0 mg/kg、1 mg/kg、10 mg/kg、50 mg/kg、100 mg/kg；口服；每日；12周结果：主动脉和心脏动脉粥样硬化病变面积减少。动物模型：9周龄雄性ICR小鼠(药代动力学分析)[4]剂量：5mg/kg,10mg/kg给药：口服给药结果：t1/2=0.693/λ

[参考文献]

[1]. Hayashi A, et al. Pyripyropenes, fungal sesquiterpenes conjugated with alpha-pyrone and pyridine moieties, exhibits anti-angiogenic activity against human umbilical vein endothelial cells. Biol Pharm Bull. 2009 Jul;32(7):1261-5.

[2]. Ohtawa M, et al. Design and Synthesis of A-Ring Simplified Pyripyropene A Analogues as Potent and Selective Synthetic SOAT2 Inhibitors. ChemMedChem. 2018 Mar 6;13(5):411-421.

[3]. Ohshiro T, et al. Pyripyropene A, an acyl-coenzyme A:cholesterol acyltransferase 2-selective inhibitor, attenuates hypercholesterolemia and atherosclerosis in murine models of hyperlipidemia. Arterioscler Thromb Vasc Biol. 2011 May;31(5):1108-15.

[4]. Lee KR , et al. Determination of Penicillium griseofulvum-oriented pyripyropene A, a selective inhibitor of acyl-coenzyme A:cholesterol acyltransferase 2, in mouse plasma using liquid chromatography-tandem mass spectrometry and its application to pharmacokinetic studies. Biomed Chromatogr. 2019 Feb;33(2):e4388.

啶南平A物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
690.8±55.0 °C at 760 mmHg

[ 熔点 ]:
153-154°C (lit.)

[ 分子式 ]:
C₃₁H₃₇NO₁₀

[ 分子量 ]:
583.626

[ 闪点 ]:
371.6±31.5 °C

[ 精确质量 ]:
583.241760

[ PSA ]:
151.46000

[ LogP ]:
2.68

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0.0±2.3 mmHg at 25°C

[ 折射率 ]:
1.587

[ 储存条件 ]:
室温

啶南平A毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QL6289000

CHEMICAL NAME :: 2H,11H-Naphtho(2,1-b)pyrano(3,4-e)pyran-11-one, 1,3,4,4a,5,6a,12,12a,12b-decahydro-4- ((acetyloxy)methyl)-3,6-bis(acetyloxy)-12-hydroxy-9-( 3-pyridinyl)-4,6a,12b -trimethyl-

CAS REGISTRY NUMBER :: 147444-03-9

LAST UPDATED :: 199509

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C31-H37-N-O10

MOLECULAR WEIGHT :: 583.69

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >200 mg/kg

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

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 47,148,1994