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Chemical Compound Review

Costunlide     (1R,4E,8E,10S)-4,8-dimethyl- 13-methylidene...

Synonyms: Costunolid, Costunolide, melampolide, PubChem6258, AC1NQYGR, ...
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Disease relevance of Costunolide


High impact information on Costunolide


Biological context of Costunolide


Anatomical context of Costunolide

  • In this report, we investigated the effect of costunolide on cellular differentiation in the human promyelocytic leukemia HL-60 cell culture system [5].
  • These results suggest that PCA and costunolide inhibited hamster buccal pouch carcinogenesis and such inhibition may be related to suppression of cell proliferation in the buccal mucosa [7].
  • Compound 4d showed around 2-fold better cytotoxicity against SW-620 (colon) cell line with improved safety index than costunolide (1) [10].
  • Our data suggest an interaction of costunolide with microtubules, which may represent a new intracellular target for this drug [2].
  • While compounds 4e, 4g, and 4p have shown around 2- to 3-fold better cytotoxicity against MIAPaCa2 (pancreas), K-562 (leukemia) and PA-1 (ovary) cell lines as well as better safety index in comparison to costunolide (1) [10].

Associations of Costunolide with other chemical compounds


Gene context of Costunolide


Analytical, diagnostic and therapeutic context of Costunolide


  1. Active compounds from Saussurea lappa Clarks that suppress hepatitis B virus surface antigen gene expression in human hepatoma cells. Chen, H.C., Chou, C.K., Lee, S.D., Wang, J.C., Yeh, S.F. Antiviral Res. (1995) [Pubmed]
  2. A sesquiterpene lactone, costunolide, interacts with microtubule protein and inhibits the growth of MCF-7 cells. Bocca, C., Gabriel, L., Bozzo, F., Miglietta, A. Chem. Biol. Interact. (2004) [Pubmed]
  3. Antimycobacterial evaluation of germacranolides. Fischer, N.H., Lu, T., Cantrell, C.L., Castañeda-Acosta, J., Quijano, L., Franzblau, S.G. Phytochemistry (1998) [Pubmed]
  4. Modifying effects of naturally occurring products on the development of colonic aberrant crypt foci induced by azoxymethane in F344 rats. Kawamori, T., Tanaka, T., Hara, A., Yamahara, J., Mori, H. Cancer Res. (1995) [Pubmed]
  5. Potentiation of 1,25-dihydroxyvitamin D(3)-induced differentiation of human promyelocytic leukemia cells into monocytes by costunolide, a germacranolide sesquiterpene lactone. Kim, S.H., Kang, S.N., Kim, H.J., Kim, T.S. Biochem. Pharmacol. (2002) [Pubmed]
  6. Costunolide inhibits interleukin-1beta expression by down-regulation of AP-1 and MAPK activity in LPS-stimulated RAW 264.7 cells. Kang, J.S., Yoon, Y.D., Lee, K.H., Park, S.K., Kim, H.M. Biochem. Biophys. Res. Commun. (2004) [Pubmed]
  7. Inhibitory effects of dietary protocatechuic acid and costunolide on 7,12-dimethylbenz[a]anthracene-induced hamster cheek pouch carcinogenesis. Ohnishi, M., Yoshimi, N., Kawamori, T., Ino, N., Hirose, Y., Tanaka, T., Yamahara, J., Miyata, H., Mori, H. Jpn. J. Cancer Res. (1997) [Pubmed]
  8. Costunolide triggers apoptosis in human leukemia U937 cells by depleting intracellular thiols. Choi, J.H., Ha, J., Park, J.H., Lee, J.Y., Lee, Y.S., Park, H.J., Choi, J.W., Masuda, Y., Nakaya, K., Lee, K.T. Jpn. J. Cancer Res. (2002) [Pubmed]
  9. A sesquiterpene lactone, costunolide, from Magnolia grandiflora inhibits NF-kappa B by targeting I kappa B phosphorylation. Koo, T.H., Lee, J.H., Park, Y.J., Hong, Y.S., Kim, H.S., Kim, K.W., Lee, J.J. Planta Med. (2001) [Pubmed]
  10. Synthesis of 13-amino costunolide derivatives as anticancer agents. Srivastava, S.K., Abraham, A., Bhat, B., Jaggi, M., Singh, A.T., Sanna, V.K., Singh, G., Agarwal, S.K., Mukherjee, R., Burman, A.C. Bioorg. Med. Chem. Lett. (2006) [Pubmed]
  11. Chemopreventive effect of costunolide, a constituent of oriental medicine, on azoxymethane-induced intestinal carcinogenesis in rats. Mori, H., Kawamori, T., Tanaka, T., Ohnishi, M., Yamahara, J. Cancer Lett. (1994) [Pubmed]
  12. Inhibitory mechanism of costunolide, a sesquiterpene lactone isolated from Laurus nobilis, on blood-ethanol elevation in rats: involvement of inhibition of gastric emptying and increase in gastric juice secretion. Matsuda, H., Shimoda, H., Ninomiya, K., Yoshikawa, M. Alcohol Alcohol. (2002) [Pubmed]
  13. Costunolide and dehydrocostus lactone as inhibitors of killing function of cytotoxic T lymphocytes. Taniguchi, M., Kataoka, T., Suzuki, H., Uramoto, M., Ando, M., Arao, K., Magae, J., Nishimura, T., Otake, N., Nagai, K. Biosci. Biotechnol. Biochem. (1995) [Pubmed]
  14. (1)H, (13)C NMR and X-ray crystallographic studies of highly polyhalogenated derivatives of costunolide lactone. Corona, D., Díaz, E., Nava, J.L., Guzmán, A., Barrios, H., Fuentes, A., Hernandez-Plata, S.A., Allard, J., Jankowski, C.K. Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy. (2005) [Pubmed]
  15. Inhibitory effects of costunolide on the telomerase activity in human breast carcinoma cells. Choi, S.H., Im, E., Kang, H.K., Lee, J.H., Kwak, H.S., Bae, Y.T., Park, H.J., Kim, N.D. Cancer Lett. (2005) [Pubmed]
  16. Costunolide, a sesquiterpene lactone from Saussurea lappa, inhibits the VEGFR KDR/Flk-1 signaling pathway. Jeong, S.J., Itokawa, T., Shibuya, M., Kuwano, M., Ono, M., Higuchi, R., Miyamoto, T. Cancer Lett. (2002) [Pubmed]
  17. Costunolide induces apoptosis by ROS-mediated mitochondrial permeability transition and cytochrome C release. Lee, M.G., Lee, K.T., Chi, S.G., Park, J.H. Biol. Pharm. Bull. (2001) [Pubmed]
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