Antagonism of Marmin on 5-hydroxytriptamine and Histamine Receptors in Guinea-Pig Ileum Smooth Muscle
The exploration of several active compounds of medicinal plants Aegle marmelos Correa (Rutaceae) have found marmin that strongly inhibit the histamine release from mast cells. The present study investigated the antagonism phenomena of marmin on 5-hydroxy triptamine and histamine receptors in guinea-pig ileum smooth muscle. The study was performed using isolated-organ technique in Tyrode buffer medium. The agonists used to sensitize the receptors were histamine and 5-hydroxy triptamine. The type of antagonism was identified by considering: 1). the decrease of pD2 or Emax values of agonists due to pretreatment of marmin, and 2) Schild regression method. In the study, marmin (10 and 100 mM) decreased the maximum contraction effect of 5-HT by 40% and 60%, respectively. However, marmin did not influence the pD2 value of 5-HT . On the other side, marmin did not influence the maximum contraction effect of histamine, however, decreased the pD2 value of histamine. Based on Schild regression method, the pA2 value of marmin was 0.8016. In conclusion, marmin non-competitively antagonized 5-HT 4 receptor, and competitively antagonized histamine receptor in ileum smooth muscle.
2. Rang HP, Dale MM, and Ritter JM. Pharmacology, 4th Ed., Melbourne: Churchill Livingstone; 2003. 7-20, Metcalfe DD , Baram D, Mekori YA. Mast cells. Physiological Reviews, 1997. 77(4): 1033-1064.
4. Riyanto S. Phytochemical Studies and Bioactivity Tests of Murraya paniculata Jack, Aegle marmelos Correa, and Zingiber amaricans Blume [Dissertation]. Universiti Putra Malaysia; 2003. 58-67, 179-188.
5. Nugroho AE, Riyanto S, Sukari MA, Maeyama K. The Effects of Compounds Isolated from Aegle marmelos Correa, on The Histamine Release from Mast Cells, 81th Annual Meeting of The Japanese Pharmacological Society, Yokohama March 17-18th; 2008. 189P.
6. Nugroho AE, Sahid NA, Riysanto S, Maeyama K, Ikawati I. Effects of Marmin, isolated from Aegle marmelos Correa, on the L-histidine decarboxylase (HDC ) enzyme in RBL -2H3 cells, Thai J. Pharm Sci, 2011. 35: 1-7.
7. Vogel GH . Drug Discovery and Evaluation Pharmacological Assays, 2nd Eds. New York : Springer- Verlag; 2002. 873-884.
8. Assem ES and Chong EK. Profiles of Different antiallergiy effects of a new histamine antagonist, BM 15,100, Br J Pharmacol. 1976. 57(3): 437P-438P.
9. Takase H, Yamamoto K, Hirano H, Saito Y, Yamashita A. Pharmacological profile of gastric mucosal protection by marmin and nobiletin from a traditional herbal medicine, Aurantii fructus immaturus, Jpn J Pharmacol. 1994. 66(1): 139-147.
10. Gonsior E, Schultze-Werninghaus G and Wuthrich B. Protective Antiallergic Effects of a New Coumarin Compound (BM 15.100) in Experimental Asthma, Int J Clin Pharmacol Biopharm, 1979. 17(7): 283-289.
Copyright @2017. This is an open-access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License (http://creativecommons.org/licenses/by-nc-sa/4.0/) which permits unrestricted non-commercial used, distribution and reproduction in any medium
This work is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License.