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Chemical Compound Review

Esculatin     6,7-dihydroxychromen-2-one

Synonyms: Esculetin, Esculetol, Aesculetin, Asculetine, Cichorigenin, ...
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Disease relevance of Esculatin


High impact information on Esculatin

  • Bile salt-induced increases in chemiluminescence were abolished by CuDIPS, phenidone, and esculetin, but not by indomethacin [6].
  • Cells that received 4-BPB, IB, or NS398, but not esculetin showed a significant reduction in the levels of proMMP-2, MMP-9, and proMMP-9 in the culture medium [7].
  • We also tested the effect of 4-BPB, IB, NS398, and esculetin on the secretion of matrix metalloproteinases (MMPs) and tissue inhibitors of metalloproteinases (TIMPs), as key enzymes in the proteolysis of Matrigel during invasion, using gelatin zymograms and Western blots [7].
  • Esculetin, a specific inhibitor of 12-lipoxygenase, prevented the effect of AA, but cyclooxygenase inhibitor did not [8].
  • Further, esculetin (10(-6)M) increased renin release in renal slices from 150 +/- 10 to 310 +/- 20 ng/ml.h (P < 0.05) and this rise was entirely blocked in the presence of 12HETE (10(-7)M; 130 +/- 40 ng/ml.h) [9].

Chemical compound and disease context of Esculatin


Biological context of Esculatin


Anatomical context of Esculatin


Associations of Esculatin with other chemical compounds


Gene context of Esculatin


Analytical, diagnostic and therapeutic context of Esculatin


  1. Disruption of putative regulatory loci in Listeria monocytogenes demonstrates a significant role for Fur and PerR in virulence. Rea, R.B., Gahan, C.G., Hill, C. Infect. Immun. (2004) [Pubmed]
  2. Esculetin inhibits Ras-mediated cell proliferation and attenuates vascular restenosis following angioplasty in rats. Pan, S.L., Huang, Y.W., Guh, J.H., Chang, Y.L., Peng, C.Y., Teng, C.M. Biochem. Pharmacol. (2003) [Pubmed]
  3. Studies on coumarins and coumarin-related compounds to determine their therapeutic role in the treatment of cancer. Lacy, A., O'Kennedy, R. Curr. Pharm. Des. (2004) [Pubmed]
  4. Esculetin (dihydroxycoumarin) inhibits the production of matrix metalloproteinases in cartilage explants, and oral administration of its prodrug, CPA-926, suppresses cartilage destruction in rabbit experimental osteoarthritis. Yamada, H., Watanabe, K., Saito, T., Hayashi, H., Niitani, Y., Kikuchi, T., Ito, A., Fujikawa, K., Lohmander, L.S. J. Rheumatol. (1999) [Pubmed]
  5. Enhancement of esculetin on Taxol-induced apoptosis in human hepatoma HepG2 cells. Kuo, H.C., Lee, H.J., Hu, C.C., Shun, H.I., Tseng, T.H. Toxicol. Appl. Pharmacol. (2006) [Pubmed]
  6. Role of reactive oxygen in bile salt stimulation of colonic epithelial proliferation. Craven, P.A., Pfanstiel, J., DeRubertis, F.R. J. Clin. Invest. (1986) [Pubmed]
  7. Inhibitors of prostaglandin synthesis inhibit human prostate tumor cell invasiveness and reduce the release of matrix metalloproteinases. Attiga, F.A., Fernandez, P.M., Weeraratna, A.T., Manyak, M.J., Patierno, S.R. Cancer Res. (2000) [Pubmed]
  8. Stimulation of eicosapentaenoic acid metabolism in washed human platelets by 12-hydroperoxyeicosatetraenoic acid. Morita, I., Takahashi, R., Saito, Y., Murota, S. J. Biol. Chem. (1983) [Pubmed]
  9. Tonic inhibition of renin secretion by the 12 lipoxygenase pathway: augmentation by high salt intake. Stern, N., Nozawa, K., Kisch, E., Tuck, M.L., Golub, M., Eggena, P., Knoll, E. Endocrinology (1996) [Pubmed]
  10. Effects of esculin and esculetin on the survival of Escherichia coli O157 in human faecal slurries, continuous-flow simulations of the rumen and colon and in calves. Duncan, S.H., Leitch, E.C., Stanley, K.N., Richardson, A.J., Laven, R.A., Flint, H.J., Stewart, C.S. Br. J. Nutr. (2004) [Pubmed]
  11. Inhibitory activity of gut bacteria against Escherichia coli O157 mediated by dietary plant metabolites. Duncan, S.H., Flint, H.J., Stewart, C.S. FEMS Microbiol. Lett. (1998) [Pubmed]
  12. Schistosoma mansoni: cercarial eicosanoid production and penetration response inhibited by esculetin and ibuprofen. Salafsky, B., Fusco, A.C. Exp. Parasitol. (1985) [Pubmed]
  13. Lipoxygenase inhibitors suppress proliferation of G5:113 fibrosarcoma cells in vitro but they have no anticancer activity in vivo. Hoferová, Z., Fedorocko, P., Hofer, M., Hofmanová, J., Kozubík, A., Eliásová, V. Neoplasma (2003) [Pubmed]
  14. Rapid spot test for the determination of esculin hydrolysis. Edberg, S.C., Gam, K., Bottenbley, C.J., Singer, J.M. J. Clin. Microbiol. (1976) [Pubmed]
  15. Effects of eicosanoid synthesis inhibitors on the in vitro growth and prostaglandin E and leukotriene B secretion of a human breast cancer cell line. Earashi, M., Noguchi, M., Kinoshita, K., Tanaka, M. Oncology (1995) [Pubmed]
  16. The effect of nordihydroguaiaretic acid, an inhibitor of prostaglandin and leukotriene biosynthesis, on hematopoiesis of gamma-irradiated mice. Kozubík, A., Hofmanová, J., Holá, J., Netíková, J. Exp. Hematol. (1993) [Pubmed]
  17. A comparative study on the effects of inhibitors of the lipoxygenase pathway on neutrophil function. Inhibitory effects on neutrophil function may not be attributed to inhibition of the lipoxygenase pathway. Ozaki, Y., Ohashi, T., Niwa, Y. Biochem. Pharmacol. (1986) [Pubmed]
  18. Induction of apoptosis by esculetin in human leukemia cells. Chu, C.Y., Tsai, Y.Y., Wang, C.J., Lin, W.L., Tseng, T.H. Eur. J. Pharmacol. (2001) [Pubmed]
  19. Esculetin inhibits T cell activation without suppressing IL-2 production or IL-2 receptor expression. Kabelitz, D., Al-Gorany, K.H. Immunol. Lett. (1989) [Pubmed]
  20. Esculetin suppresses proteoglycan metabolism by inhibiting the production of matrix metalloproteinases in rabbit chondrocytes. Watanabe, K., Ito, A., Sato, T., Saito, T., Hayashi, H., Niitani, Y. Eur. J. Pharmacol. (1999) [Pubmed]
  21. Antiproliferative effect of esculetin on vascular smooth muscle cells: possible roles of signal transduction pathways. Huang, H.C., Lai, M.W., Wang, H.R., Chung, Y.L., Hsieh, L.M., Chen, C.C. Eur. J. Pharmacol. (1993) [Pubmed]
  22. Modulatory role of eicosanoids in vascular changes during the preovulatory period in the rat. Abisogun, A.O., Daphna-Iken, D., Reich, R., Kranzfelder, D., Tsafriri, A. Biol. Reprod. (1988) [Pubmed]
  23. Eicosanoid inhibitors enhance synergistically the effect of transforming growth factor beta 1 on CCL 64 cell proliferation. Kozubík, A., Hofmanová, J., Dusek, L. Eur. J. Pharmacol. (1996) [Pubmed]
  24. Synthesis of sterols and 5-lipoxygenase products are required for the G1-S phase transition of interleukin-2-dependent lymphocyte proliferation. Hata, S., Sugama, K., You-Li, Z., Hatanaka, M., Namba, Y., Hanaoka, M. Microbiol. Immunol. (1987) [Pubmed]
  25. Inhibition of cell cycle progression in human leukemia HL-60 cells by esculetin. Wang, C.J., Hsieh, Y.J., Chu, C.Y., Lin, Y.L., Tseng, T.H. Cancer Lett. (2002) [Pubmed]
  26. Comparative effects of piroxicam and esculetin on incidence, proliferation, and cell kinetics of mammary carcinomas induced by 7,12-dimethylbenz[a]anthracene in rats on high- and low-fat diets. Kitagawa, H., Noguchi, M. Oncology (1994) [Pubmed]
  27. Solid-phase extraction of esculetin from the ash bark of Chinese traditional medicine by using molecularly imprinted polymers. Hu, S.G., Li, L., He, X.W. Journal of chromatography. A. (2005) [Pubmed]
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