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扁塑藤素

扁塑藤素用途

Pristimerin是高效可逆的单酰基甘油脂肪酶(MGL)抑制剂,IC50值为93 nM。

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扁塑藤素名称

[ CAS 号 ]:
1258-84-0

[ 中文名 ]:
扁塑藤素

[ 英文名 ]:
Pristimerin

[中文别名 ]:

扁蒴藤素

[英文别名 ]:

Celastrol-methylether
pristimerine

扁塑藤素生物活性

[ 描述 ]:

Pristimerin是高效可逆的单酰基甘油脂肪酶(MGL)抑制剂,IC50值为93 nM。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

天然产物 >> 萜类化合物和糖苷

研究领域 >> 癌症

[ 靶点 ]

IC50: 93 nM (MGL)[1]

[体外研究]

Pristimerin抑制纯化的MGL的活性,IC50为93±8nM,未纯化的MGL(MGL转染的HeLa细胞的细胞裂解物)的IC50为398±68nM。 Pristimerin通过快速,可逆和非竞争性的机制抑制MGL。可以通过与调节性半胱氨酸(可能是Cys208)形成极性相互作用来加强pristimerin与MGL的结合[1]。 Pristimerin以剂量和时间依赖性方式抑制HFLS-RA和HUVEC细胞活力。 Pristimerin降低VEGF诱导的VEGFR2自身磷酸化,并减弱VEGF诱导的VEGFR2介导的信号通路的激活[2]。

[体内研究]

Pristimerin抑制炎症和肿瘤血管生成。 Pristimerin显着降低发炎关节滑膜组织中的血管密度,并降低血清中促血管生成因子的表达,包括TNF-α,Ang-1和MMP-9 [2]。

[细胞实验]

将HFLS-RA（5×103细胞/ mL）或HUVEC（1×10 4细胞/孔）接种在96孔板中并在正常生长培养基中培养24小时。然后将细胞与不同的Pristimerin浓度（0,0.125,0.25,0.5μM）一起温育。在VEGF诱导的条件下测定Pristimerin对HUVEC活力的影响。通过MTT测定定量细胞活力。在培养期结束前4小时，向每个孔中加入30μLMTT溶液（5.0mg / mL）。没有Pristimerin或VEGF的细胞作为载体对照[2]。

[动物实验]

大鼠：将Pristimerin溶解于DMSO（0.4％）中，并在实验组中每天腹膜内注射给雄性Sprague-Dawley大鼠（低剂量组，0.40mg / kg体重;高剂量组，0.80mg / kg体重）从免疫接种的第11天到第24天，体重）。模型组接受载体（DMSO，0.4％），正常对照组接受生理盐水（NS）。甲氨蝶呤（阳性对照）悬浮于NS中，并在自身免疫期以5天的间隔口服给药[2]。

[参考文献]

[1]. King AR, et al. Discovery of potent and reversible monoacylglycerol lipase inhibitors. Chem Biol. 2009 Oct 30;16(10):1045-52.

[2]. Deng Q, et al. Pristimerin inhibits angiogenesis in adjuvant-induced arthritic rats by suppressing VEGFR2 signaling pathways. Int Immunopharmacol. 2015 Dec;29(2):302-13.

[相关活性小分子]

扁塑藤素物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
607.7±55.0 °C at 760 mmHg

[ 熔点 ]:
219.5°C

[ 分子式 ]:
C₃₀H₄₀O₄

[ 分子量 ]:
464.636

[ 闪点 ]:
195.1±25.0 °C

[ 精确质量 ]:
464.292664

[ PSA ]:
63.60000

[ LogP ]:
7.54

[ 外观性状 ]:
orange

[ 蒸汽压 ]:
0.0±3.9 mmHg at 25°C

[ 折射率 ]:
1.582

[ 储存条件 ]:
Store at -20°C

[ 水溶解性 ]:
DMSO: ≥5mg/mL

扁塑藤素MSDS

详细MSDS(安全技术说明书)

扁塑藤素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RC4905000

CAS REGISTRY NUMBER :: 1258-84-0

LAST UPDATED :: 199309

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C30-H40-O4

MOLECULAR WEIGHT :: 464.70

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 :: 8 gm/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: 8(1),90,1982

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

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 :: 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 8(1),90,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 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: 8(1),90,1982

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扁塑藤素安全信息

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

扁塑藤素合成路线

详细合成路线

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扁塑藤素文献

Pristimerin, a naturally occurring triterpenoid, protects against autoimmune arthritis by modulating the cellular and soluble immune mediators of inflammation and tissue damage.

Clin. Immunol. 155(2) , 220-30, (2014)

Rheumatoid arthritis (RA) is a chronic autoimmune disorder affecting the synovial joints. The currently available drugs for RA are effective only in a proportion of patients and their prolonged use is...

Targeting tumor proteasome with traditional Chinese medicine.

Curr. Drug Discov. Technol. 7(1) , 46-53, (2010)

The proteasome is a multicatalytic protease complex whose activity is required for the growth of normal or tumor cells. It has been shown that human cancer cells are more sensitive to proteasome inhib...

Biomimetic synthesis of xuxuarines Ealpha and Ebeta: structure revision of Rzedowskia bistriterpenoids.

Bioorg. Med. Chem. 16(4) , 1884-9, (2008)

Reaction of pristimerin with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) resulted in a biomimetic-type coupling leading to xuxuarines Ealpha and Ebeta and not the previously reported Rzedowskia bi...

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