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粗糠柴苦素

粗糠柴苦素用途

Rottlerin 是 PKC 的一个特异性抑制剂,其对 PKCδ 的 IC50 值为 3-6 μM,PKCα,β,γ 的为 30-42 μM,PKCε,η,ζ 为 80-100 μM。

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粗糠柴苦素名称

[ CAS 号 ]:
82-08-6

[ 中文名 ]:
粗糠柴苦素

[ 英文名 ]:
Rottlerin

[中文别名 ]:

粗糠紫苦素

[英文别名 ]:

Kamalin
Mallotoxin
EINECS 201-395-4
MFCD00017361
Rottlerin

粗糠柴苦素生物活性

[ 描述 ]:

Rottlerin 是 PKC 的一个特异性抑制剂,其对 PKCδ 的 IC50 值为 3-6 μM,PKCα,β,γ 的为 30-42 μM,PKCε,η,ζ 为 80-100 μM。

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

研究领域 >> 感染

[ 靶点 ]

PKCδ:3 μM (IC50, Porcine spleen)

PKCα:30 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCγ:40 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCβ:42 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCη:82 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCζ:100 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCε:100 μM (IC50, baculovirus-infected Sf9 insect cells)

CaM kinase III:5.3 μM (IC50, EF-2 kinase activity in cytosol of murine pancreas)

CKII:30 μM (IC50, holoenzyme expressed in E.coli)

PKA:78 μM (IC50, catalytic subunit from porcine heart)

[体外研究]

Rottlerin是Ca2 +反应性PKCδ的强效抑制剂,来自猪脾的酶的IC50为3μM,来自杆状病毒感染的Sf9昆虫细胞的重组酶的IC50为6μM。其他PKC同工酶对Rottlerin的敏感性至少低一个数量级。不同PKC同工酶的IC50值按以下顺序增加：δ<α,β,γ<η,ζ,ε[1]。 Rottlerin以剂量依赖性方式抑制细胞增殖。两种抑制剂(索拉非尼和罗特林)的组合比单一药剂更有效,并且使神经胶质瘤细胞存活率显着降低。使用克隆形成试验进一步证实了Rottlerin和索拉非尼的细胞毒性作用。当Rottlerin和索拉非尼独立施用时,集落形成能力存在剂量依赖性降低,后者具有浓度高于5μM的活性。此外,当两种药物联合给药时,疗效显着增强[2]。

[细胞实验]

将细胞（5×103 /孔）置于96孔微量滴定板中的100μL生长培养基中，并在过夜附着后暴露3天至一系列浓度的索拉非尼和Rottlerin（0,0.1,0.2,0.4）单独和组合使用，0.8,1.5,3,6,12,25,50μM）。对照细胞单独接受载体（DMSO）。处理后，洗涤细胞，并使用比色细胞增殖试验测定活细胞数。为了进行测定，向每个孔中加入20μLMTS/吩嗪硫酸甲酯溶液，并且在37℃下在潮湿的5％CO 2气氛中孵育1小时后，在酶标仪中在490nm处测量吸光度。为了直接评估细胞毒性，将2.5×105个细胞接种在60-mm培养皿中，并用选定浓度的抑制剂或载体处理[2]。

[参考文献]

[1]. Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun. 1994 Feb 28;199(1):93-8.

[2]. Jane EP, et al. Coadministration of sorafenib with rottlerin potently inhibits cell proliferation and migration in human malignant glioma cells. J Pharmacol Exp Ther. 2006 Dec;319(3):1070-80.

[相关活性小分子]

粗糠柴苦素物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
800.4±65.0 °C at 760 mmHg

[ 熔点 ]:
200 °C

[ 分子式 ]:
C₃₀H₂₈O₈

[ 分子量 ]:
516.539

[ 闪点 ]:
266.0±27.8 °C

[ 精确质量 ]:
516.178406

[ PSA ]:
144.52000

[ LogP ]:
8.66

[ 蒸汽压 ]:
0.0±2.9 mmHg at 25°C

[ 折射率 ]:
1.682

[ 储存条件 ]:
2-8°C

粗糠柴苦素MSDS

详细MSDS(安全技术说明书)

粗糠柴苦素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AM6913800

CHEMICAL NAME :: Acetophenone, 3'-((8-cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2H-1-benz opyran-6-yl)methyl)- 2',4',6'-trihydroxy-5'-methyl-

CAS REGISTRY NUMBER :: 82-08-6

BEILSTEIN REFERENCE NO. :: 0070757

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C30-H28-O8

MOLECULAR WEIGHT :: 516.58

WISWESSER LINE NOTATION :: T66 BO CHJ C1 C1 GQ H1R BQ DQ FQ C1 EV1& IQ JV1U1R

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 750 mg/kg

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: IJPPAZ Indian Journal of Physiology and Pharmacology. (All India Institute of Medical Sciences, Dept. of Physiology, Ansari Nagar, New Delhi 110 029, India) V.1- 1957- Volume(issue)/page/year: 3,168,1959 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 150 mg/kg

SEX/DURATION :: female 6 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :: IJPPAZ Indian Journal of Physiology and Pharmacology. (All India Institute of Medical Sciences, Dept. of Physiology, Ansari Nagar, New Delhi 110 029, India) V.1- 1957- Volume(issue)/page/year: 3,168,1959

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 375 mg/kg

SEX/DURATION :: female 15 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

REFERENCE :: IJPPAZ Indian Journal of Physiology and Pharmacology. (All India Institute of Medical Sciences, Dept. of Physiology, Ansari Nagar, New Delhi 110 029, India) V.1- 1957- Volume(issue)/page/year: 3,168,1959

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 120 mg/kg

SEX/DURATION :: female 6 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - mating performance (e.g. # sperm positive females per # females mated; # copulations per # estrus cycles)

REFERENCE :: IJMRAQ Indian Journal of Medical Research. (Indian Council of Medical Research, Ansari Nagar, New Delhi 110 029, India) V.1- 1913- Volume(issue)/page/year: 48,52,1960

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粗糠柴苦素安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
20/21/22

[ 安全声明 (欧洲) ]:
S36/37

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

[ WGK德国 ]:
3

[ RTECS号 ]:
AM6913800

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粗糠柴苦素文献

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Two types of overcontraction are involved in intrarenal artery dysfunction in type II diabetic mouse.

J. Pharmacol. Exp. Ther. 351(1) , 77-86, (2014)

Contractile responses in small intrarenal arteries are associated with diabetic nephropathy. However, the mechanisms that induce and maintain altered small vessel contraction are not clearly understoo...

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