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Costunolide

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Chemical Structure| 553-21-9 同义名 : Costus lactone;Melampolide;CCRIS 6754;NSC 106404;(+)-Costunolide
CAS号 : 553-21-9
货号 : A496529
分子式 : C15H20O2
纯度 : 98%
分子量 : 232.318
MDL号 : -
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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

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].
实验方案
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
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.