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The effect of acteoside on histamine release and arachidonic acid release in RBL-2H3 mast cells

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The effect of acteoside, a phenylpropanoid glycoside isolated fromClerodendron trichotomum Thunberg, on histamine and arachidonic acid release was investigated in RBL 2H3 cells. Histamine was dose-dependently released from RBL 2H3 cells by melittin, arachidonic acid and thapsigargin. In extracellular Ca2+-free solution, basal secretion of histamine increased by two fold. The response of histamine release to melittin and thapsigargin in Ca2+-free solution was significantly decreased, whereas the response to arachidonic acid was significantly increased as compared with those in normal solution. Acteoside inhibited histamine release induced by melittin, arachidonic acid and thapsigargin in a dose-dependent manner in the presence or absence of extracellular Ca2+. However, the inhibitory activity of acteoside was more potent in normal solution than that in Ca2+-free solution. These data suggest that inhibitory mechanism of acteoside on histamine release may be related to extracellular Ca2+. On the other hand, acteoside significantly inhibited arachidonic acid release and prostaglandin E2 production induced by 0.5 μM melittin. It is possible that acteoside may be developed as an anti-inflammatory agent.

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  1. Attur, M. G., Patel, R., Thakker, G., Vyas, P., Levartovsky, D., Patel, P., Naqvi, S., Raza, R., Patel, K., Abramson, D., Bruno, G., Abramson, S. B., and Amin, A. R., Differential anti-inflammatory effects of immunosuppressive drugs: cyclosporin, rapamycin and FK-506 on inducible nitric oxide synthase, nitric oxide, cyclooxygenase-2 and PGE2 production.Inflamm. Res., 49, 20–26 (2000).

  2. Battistella, A., Boarato, E., Bruni, A., Mietto, L., Palatini, P., and Toffano, G., Apomorphine-induced inhibition of histamine release in rat peritoneal mast cells.Br. J. Pharmacol., 88, 457–462 (1986).

  3. Choi, J. H., Whang, W. K., and Kim, H. J., Studies on the anti-inflammatory effects of Clerodendron trichotomum Thunberg leaves.Arch. Pharm. Res., 27, 189–193 (2004).

  4. Da Silva, A., Amrani, Y., Trifilieff, A., and Landry, Y., Involvement of B2 receptors in the bradykinin-induced relaxation of guinea-pig isolated trachea.Br. J. Pharmacol., 114, 103–108 (1995).

  5. Diaz, A. M., Abad, M. J., Fernandez, L., Silvan, A. M., De Santos, J., and Bermejo, P., Phenylpropanoid glycosides from Scrophularia scorodonia:in vitro anti-inflammatory activity.Life Sci., 74, 2515–2526 (2004).

  6. Gueck, T., Seidel, A., and Fuhrmann, H., Consequences of eicosapentaenoic acid (n-3) and arachidonic acid (n-6) supplementation on mast cell mediators.J. Anim. Physiol. Anim. Nutr. (Berl.), 88, 259–265 (2004).

  7. Jesus, B., Suzanne, E. B., Ismael, D. B., and Edward, A. D., Arachidonic acid mobilization in P388D1 macrophages is controlled by two distinct Ca2+-dependent phospholipase A2 enzymes.Proc. Natl. Acad. Sci. U.S.A., 91, 11060–11064 (1994).

  8. Kitsukawa, Y., Felley, C., Metz, D. C., and Jensen, R. T., Thapsigargin defines roles of Ca2+ in initial, sustained, and potentiated stimulation of pepsinogen secretion.Am. J. Physiol., 266, 613–623 (1994).

  9. Lau, C. W., Chen, Z. Y., Wong, C. M., Yao, X., He, Z., Xu, H., and Huang, Y., Attenuated endothelium-mediated relaxation by acteoside in rat aorta: Role of endothelial [Ca2+]i and nitric oxide/cyclic GMP pathway,Life Sci., 75, 1149–1157 (2004).

  10. Morita, Y., Aida, N., and Miyamoto, T., Role of phospholipase A2 activation in histamine release from human basophils.Allergy, 38, 413–418 (1983).

  11. Nakatani, N., Uozumi, N., Kume, K., Murakami, M., Kudo, I., and Shimizu, T., Role of cytosolic phospholipase A2 in the production of lipid mediators and histamine release in mouse bone-marrow-derived mast cells.Biochem J., 352, 311–317 (2000).

  12. Petrone, W. F., English, D. K., Wong, K., and McCord, J. M., Free radicals and inflammation: superoxide-dependent activation of a neutrophil chemotactic factor in plasma.Proc. Natl. Acad. Sci. U.S.A., 77, 1159–1163 (1980).

  13. Radvanyi, F., Jordan, L., Russo-Marie, F., and Bon, C., A sensitive and continuous fluorometric assay for phospholipase A2 using pyrene-labeled phospholipids in the presence of serum albumin.Anal. Biochem., 177, 103–109 (1989).

  14. Sahpaz, S., Garbacki, N., Tits, M., and Bailleul, F., Isolation and pharmacological activity of phenylpropanoid esters fromMarrubium vulgare.J. Ethnophamacol., 79, 389–392 (2002).

  15. Shore, P. A., Burkhalter, A., and Cohn, V. H., A method for the fluorometric assay of histamine in tissues.J. Phamacol. Exp. Ther., 127, 182–186 (1959).

  16. Smith, P. K., Krohn, R. I., Hermanson, G. T., Mallia, A. K., Gartner, F. H., Provenzano, M. D., Fujimoto, E. K., Goeke, N. M., Olson, B. J., and Klenk, D. C., Measurement of protein using bicinchoninic acid.Anal. Biochem., 150, 76–85 (1985).

  17. Woerdenbag, H. J., Merfort, I., Passreiter, C. M., Schmidt, T. J., Willuhn, G., van Uden, W., Pras, N., Kampinga, H. H., and Konings, A. W., Cytotoxicity of flavonoids and sesquiterpene lactones from Arnica species against the GLC4 and the COLO 320 cell lines.Planta Med., 60, 434–437 (1994).

  18. Wong, I. Y., Huang, Y., He, Z. D., Lau, C. W., and Chen, Z. Y., Relaxing effects of Ligstrum purpurascens extract and purified acteoside in rat aortic rings.Planta Med., 67, 317–321 (2001).

  19. Xiong, Q., Tezuka, Y., Kaneko, T., Li, H., Tran, L. Q., Hase, K., Namba, T., and Kadota, S., Inhibition of nitric oxide by phenylethanoids in activated macrophages.Eur. J. Pharmacol., 14, 137–144 (2000).

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Correspondence to Sang Soo Sim.

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Lee, J.H., Lee, J.Y., Kang, H.S. et al. The effect of acteoside on histamine release and arachidonic acid release in RBL-2H3 mast cells. Arch Pharm Res 29, 508 (2006). https://doi.org/10.1007/BF02969425

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Key words

  • Acteoside
  • Histamine
  • Arachidonic acid
  • Prostaglandin E2