粗糠柴苦素 ROTTLERIN CAS#:82-08-6

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粗糠柴苦素

产品纠错

CAS号：82-08-6 | 英文名称：ROTTLERIN

分子式 C₃₀H₂₈O₈

分子量 517

EINECS号 201-395-4

MDL MFCD00017361

Smiles

InChIKey

乙二醇化学百科

基本信息

中文名称	粗糠柴苦素
英文名称	ROTTLERIN
CAS号	82-08-6
分子式	C30H28O8
分子量	516.54
EINECS号	201-395-4

物化性质

熔点	200 °C
沸点	521.39°C (rough estimate)
密度	1.2051 (rough estimate)
折射率	1.4900 (estimate)
LogP	8.660 (est)
溶解度	溶于DMSO（高达50mg/ml）。
形态	粉末
酸度系数(pKa)	6.92±0.40(Predicted)
颜色	橙色至棕色
稳定性	DMSO中的溶液可在-20°下稳定储存1个月。

安全信息

危险品标志	Xn
危险类别码	20/21/22-22
安全说明	36/37-24/25
WGK Germany	3
RTECS号	AM6913800
海关编码	29329990

生产及用途

生物活性

Rottlerin (Mallotoxin, NSC 56346, NSC 94525)是一种从 Mallotus Philippinensis 纯化出来的天然化合物，一种特效的 Protein kinase 的抑制剂，对PKCδ(来自杆状病毒感染的Sf9昆虫细胞)、PKCδ(来自猪脾)和CaM kinase III的IC50值分别为3 μM、6 μM和5.3 μM。Rottlerin 还可以抑制PKCα、PKCγ、PKCβ、PKCη、CKII和PKA，其IC50值分别为30 μM、40 μM、42 μM、82 μM、30 μM和78 μM。

靶点

Target	Value
PKCδ (Cell-free assay)	3 μM
CKIII (Cell-free assay)	5.3 μM
PKCα (Cell-free assay)	30 μM
CKII (Cell-free assay)	30 μM
PKCγ (Cell-free assay)	40 μM

体外研究

Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner in primary HMVEC.
Rottlerin (20 μM) exhibits cell proliferation in HMVEC.

Western Blot Analysis

Cell Line:	Primary HMVEC (Human Microvascular Endothelial Cell).
Concentration:	20 μM.
Incubation Time:	2, 6, 24 hours.
Result:	Dramatically decreased the cyclin D-1 mRNA levels in a time-dependent manner. After 2 h of treatment, the mRNA level was reduced to 50% of the control, to circa 40% after 6 h, and to 20% after 24 h. Consistently, a similar trend was observed in the protein levels, where the decrease was circa 50% after 2 h, 80% after 6 h, and to almost undetectable levels after 24 h.

Cell Proliferation Assay

Cell Line:	Primary HMVEC (Human Microvascular Endothelial Cell).
Concentration:	20 μM.
Incubation Time:	24/48 hours.
Result:	Exhibited a strong growth inhibition, with a reduction in thymidine incorporation respect to the control cells (DMSO 0.1%) of circa 75% and 80%, respectively.

体内研究

Rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth in Balb C nude mice with no toxicity.
Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP).

Animal Model:	Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2×10 ⁶ cells mixed with Matrigel, 50:50 ratio) injection.
Dosage:	0 or 20 mg/kg.
Administration:	Gavage 5 days per week, once daily, for 6 weeks.
Result:	Inhibited AsPC-1 pancreatic tumor growth in Balb C nude mice and had no effect on the body weight of AsPC-1 tumor-bearing mice.

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