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木香烃内酯 /Costunolide {[allProObj[0].p_purity_real_show]}

货号:A496529 同义名: Costus lactone;Melampolide

Costunolide shows anti-inflammatory and anti-oxidant activities and also induces apoptosis. It is a sesquiterpene lactone isolated from stem bark of Magnolia sieboldii,

Costunolide 化学结构 CAS号:553-21-9
Costunolide 化学结构
CAS号:553-21-9
Costunolide 3D分子结构
CAS号:553-21-9
Costunolide 化学结构 CAS号:553-21-9
Costunolide 3D分子结构 CAS号:553-21-9
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Costunolide 纯度/质量文件 产品仅供科研

货号:A496529 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Telomerase 其他靶点 纯度
4',7-Dimethoxyisoflavone 97%
BIBR 1532 +++

Telomerase, IC50: 100 nM

99%+
Costunolide ++

Telomerase (MCF-7), IC50: 90 μM

Telomerase (MDA-MB-231), IC50: 65 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Costunolide 生物活性

靶点
  • Telomerase

    Telomerase (MCF-7), IC50:90 μM

    Telomerase (MDA-MB-231), IC50:65 μM

描述 Costunolide, a natural sesquiterpene lactone, is found commonly in many species such as Saussurea lappa and Artemisia balchanorum. Besides, it has a variety of biological activities, such as chemopreventive and antitumor activity, anti-inflammatory, antibiotic, anti-fungal and anti-viral activity of costunolide[3]. Costunolide caused inhibition of cell growth of human breast carcinoma cell lines MCF-7 cells and MDA-MB-231 cells with IC50 of 90 mM and 50 mM, respectively, and this effect was mediated at least in part by costunolide-induced significant reduction in telomerase activity[4]. Costunolide treatment at 40 mg/kg on acute liver injury (ALI) mice significantly improved the pathological changes of hepatic tissue, and reduced the LPS and D-galactosamine-induced increases of alanine aminotransferase (from 887.24 ± 21.72 to 121.67 ± 6.56 IU/L) and aspartate aminotransferase (from 891.01 ± 45.24 to 199.94 ± 11.53 IU/L) activities in serum, remarkably reduced malondialdehyde content (from 24.56 ± 1.39 to 9.17 ± 0.25 nmol/ml) and reactive oxygen species (from 203.34 ± 7.68 to 144.23 ± 7.12%), increased the activity of anti-oxidant enzymes superoxide dismutase (from 153.74 ± 10.33 to 262.27 ± 8.39 U/ml), catalase (from 6.12 ± 0.30 to 12.44 ± 0.57 U/ml), and total anti-oxidant capacity (from 0.64 ± 0.06 to 6.29 ± 0.11 U/ml) in hepatic tissues[5]. CHO cells treated with 5.01 μM Costunolide showed slightly higher micronuclei compared to the untreated cells, and Costunolide at 5.01, 7.56, and 10.12 μM concentrations significantly inhibited tubulin polymerization by 64.89, 50.86, and 41.63%, respectively, in comparison to the control[6].

Costunolide 参考文献

[1]Choi SH, Im E, et al. Inhibitory effects of costunolide on the telomerase activity in human breast carcinoma cells. Cancer Lett. 2005 Sep 28;227(2):153-62.

[2]Park SH, Choi SU, et al. Costunolide, a sesquiterpene from the stem bark of Magnolia sieboldii, inhibits the RAS-farnesyl-proteintransferase. Planta Med. 2001 Jun;67(4):358-9.

[3]Park SH, Choi SU, Lee CO, Yoo SE, Yoon SK, Kim YK, Ryu SY. Costunolide, a sesquiterpene from the stem bark of Magnolia sieboldii, inhibits the RAS-farnesyl-proteintransferase. Planta Med. 2001 Jun;67(4):358-9. doi: 10.1055/s-2001-14315. PMID: 11458455.

[4]Choi SH, Im E, Kang HK, Lee JH, Kwak HS, Bae YT, Park HJ, Kim ND. Inhibitory effects of costunolide on the telomerase activity in human breast carcinoma cells. Cancer Lett. 2005 Sep 28;227(2):153-62. doi: 10.1016/j.canlet.2005.01.011. PMID: 16112418.

[5]Mao J, Yi M, Wang R, Huang Y, Chen M. Protective Effects of Costunolide Against D-Galactosamine and Lipopolysaccharide-Induced Acute Liver Injury in Mice. Front Pharmacol. 2018 Dec 20;9:1469. doi: 10.3389/fphar.2018.01469. PMID: 30618760; PMCID: PMC6307542.

[6]Singireesu SSNR, Misra S, Mondal SK, Yerramsetty S, Sahu N, K SB. Costunolide induces micronuclei formation, chromosomal aberrations, cytostasis, and mitochondrial-mediated apoptosis in Chinese hamster ovary cells. Cell Biol Toxicol. 2018 Apr;34(2):125-142. doi: 10.1007/s10565-017-9411-z. Epub 2017 Sep 15. PMID: 28914393.

Costunolide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.30mL

0.86mL

0.43mL

21.52mL

4.30mL

2.15mL

43.04mL

8.61mL

4.30mL

Costunolide 技术信息

CAS号553-21-9
分子式C15H20O2
分子量 232.318
别名 Costus lactone;Melampolide;CCRIS 6754;NSC 106404;(+)-Costunolide
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 50 mg/mL(215.22 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 25 mg/mL(107.61 mM),配合低频超声,并水浴加热至45℃助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 3.4 mg/mL clear

PO 0.5% CMC-Na 66 mg/mL suspension

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