82-08-6
中文名称
粗糠柴苦素
英文名称
ROTTLERIN
CAS
82-08-6
EINECS 编号
201-395-4
分子式
C30H28O8
MDL 编号
MFCD00017361
分子量
516.54
MOL 文件
82-08-6.mol
更新日期
2025/04/16 09:54:37
82-08-6 结构式
基本信息
中文别名
粗糠柴苦素咖马林/粗糠柴苦素
咖马林
英文别名
3'-[(8-CINNAMOYL-5,7-DIHYDROXY-2,2-DIMETHYL-2H-1-BENZOPYRAN-6-YL)METHYL]-2',4',6'-TRIHYDROXY-5'-METHYLACETOPHENONEMALLOTOXIN
ROTTLERIN
4’,6’-trihydroxy-5’-methyl-methyl)-2
acetophenone,3’-((8-cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2h-1-benzopyran-6-yl)
kamalin
(E)-1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one
2-Propen-1-one, 1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-, (2E)-
1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2h-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one
3'-[(8-Cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-6-yl)methyl]-2',4',6'-trihydroxy-5'-methylacetophenone
所属类别
生物化工：提取物物理化学性质
熔点200 °C
熔点200 °C
沸点521.39°C (rough estimate)
密度1.2051 (rough estimate)
折射率1.4900 (estimate)
储存条件2-8°C
储存条件2-8°C
溶解度溶于DMSO（高达50mg/ml）。
酸度系数(pKa)6.92±0.40(Predicted)
形态粉末
颜色橙色到棕色
生物来源plant (Mallotus philippinensis)
稳定性DMSO中的溶液可在-20°下稳定储存1个月。
LogP8.660 (est)
安全数据
危险品标志Xn
危险类别码20/21/22-22
危险类别码R20/21/22
安全说明36/37-24/25
安全说明S36/37
WGK Germany3
WGK Germany3
RTECS号AM6913800
海关编码29329990
粗糠柴苦素价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/02/08 | HY-18980 | 粗糠柴苦素 Rottlerin | 82-08-6 | 5 mg | 812元 |
| 2025/02/08 | HY-18980 | 粗糠柴苦素 Rottlerin | 82-08-6 | 10 mM * 1 mLin DMSO | 923元 |
| 2025/02/08 | HY-18980 | 粗糠柴苦素 Rottlerin | 82-08-6 | 10 mg | 1245元 |
常见问题列表
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. |