Effects of lupene-ol and lupene-on from Aegle marmelos Correa on histamine release: In vitro and in silico studies
Penulis/Author
Prof. Dr. apt. Agung Endro Nugroho, S.Si., M.Si. (1); apt. Navista Sri Octa Ujiantari, S.Farm., M.Sc., Ph.D. (3); Prof. Dr. apt. Sugeng Riyanto, MS. (4)
Tanggal/Date
2015
Kata Kunci/Keyword
Abstrak/Abstract
Aegle marmelos is a tree native to India, and also present in Southeast Asia including Indonesia. Traditionally, A. marmelos is used as anti-inflammatory and anti-allergy. Exploration of its active compounds have been isolated and investigated for their pharmacological activities. Previous study reported that 20(29)-lupene-3a-ol and 20(29)-lupene-3-on can be isolated from the leaves and stem barks. In the study, these lupane-type triterpenes were evaluated for their inhibitory effect on histamine release from basophilic leukemia (RBL-2H3) cell line, a tumor analog of mast cells. The release of histamine from this mast cell was immunologically and non-immunologically stimulated by DNP24-BSA and thapsigargin, respectively. The histamine release was determined by using HPLC with fluorometric detector. In the study, these lupane-type triterpenes obviously exhibited inhibitory activity on histamine release from mast cell induced by DNP24-BSA. However, these compounds did not alter the histamine release from mast cells induced by thapsigargin. In silico study was carried out to examine the interaction between lupene-ol and lupene-on on Sarcoplasmic Reticulum Ca2+-ATPase. Both of the compounds blockade the sarcoplasmic reticulum Ca2+-ATPase and inhibite the Ca2+ uptake from intracellular cytosolic. Based on the results, the inhibitory effect of lupene-ol and lupene-on might be unrelated to intracellular Ca2+ concentration
