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
粗糠柴苦素化学百科
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
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。
| 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 |
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. |
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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