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All Journal Majalah Obat Tradisional INDONESIAN JOURNAL OF PHARMACY
Hari Purnomo
Department Of Pharmaceutical Chemistry, Faculty Of Pharmacy, Universitas Gadjah Mada
Health Professions Medicine & Pharmacology Public Health

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INTERAKSI SENYAWA AKTIF DARI Aegle marmelos CORREA SEBAGAI ANTI INFLAMASI DENGAN RESEPTOR COX-1 DAN COX-2 Dani Dwi Agistia; Hari Purnomo; Maulana Tegar; Agung Endro Nugroho
Majalah Obat Tradisional Vol 18, No 2 (2013)
Publisher : Faculty of Pharmacy, Universitas Gadjah Mada

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (719.411 KB) | DOI: 10.22146/tradmedj.7983

Abstract

The compounds in Aegle marmelos have an activity as anti inflammation. The objective of this study is to evaluate six active compounds in Aegle marmelos Correa, (E,R)- Marmin, skimmianine, (S)-aegeline, aurapten, zeorin, and dustanin as anti inflammation to the COX-1 and COX-2 as target receptors. Method: Molecular docking was done with PLANTS. Ligand preparation used MarvinSketch, and protein preparation was done by using YASARA. The result was marmin, skimmianine, aegeline, aurapten, zeorin, and dustanin have interaction with Arg120, tyr 355, and Ile 523 in COX-1 and Ser353, Arg 513, and Ser 530 in COX-2. Based on the result of molecular docking, active compounds in Aegle marmelos Correa have potency as anti inflammation agent.
Econazole depleted calcium release-activated calcium (CRAC) current through blockade of voltage-dependent Ca 2+ channels Agung Endro Nugroho; Hari Purnomo; Kazutaka Maeyama
Indonesian Journal of Pharmacy Vol 22 No 2, 2011
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (349.21 KB) | DOI: 10.14499/indonesianjpharm0iss0pp128-136

Abstract

Econazole  is  an  azole  antifungal  agent  which  can  block  the  calcium release-activated  calcium  (CRAC)  current  in  human  leukaemic  T  cell  line.  The phenomenon  is  also  possible  to  occur  in  mast  cell  such  as  RBL-2H3  (rat basophilic  leukemia)  cells,  a  tumor  analog  of  mast  cells.  In  the  study,  we investigated  effect  of  econazole  on 45Ca2+ uptake  into  the  cells  in  response  to thapsigargin, an ATP-dependent Ca2+ (SERCA) inhibitor, by direct measurement of  radiolabelled  Ca2+ uptake  in  cells.  The  mechanism  underlying  this  effect  of econazole  was  studied  using  molecular  modelling.  In present  study,  econazole inhibited 45Ca2+ influx  into  mast  cells  in  absence  of  mast  cells  inducer, thapsigargin.  Moreover,  econazole  potently  suppressed  the 45Ca2+ influx induced  by  thapsigargin.  It  was  supported  that  econazole  also  inhibited  Ca2+-induced  tracheal  contraction.  The  increase  of  Ca2+ was  stimulated  by  the opening of voltage-dependent Ca2+ channels activated by KCl-induced membrane depolarization. Based on molecular docking study, score of interaction (equal to  energy  of  interaction)  of  3FGO,  a  main  protein  target  on  Ca2+ -ATPase,  with native ligan, thapsigargin and econazole were -76.941, -117.205, and -92.277, respectively.  The  interaction  of  thapsigargin  and  Ca2+ -ATPase  was  more  stable than  this  of  econazole  and  Ca2+ -ATPase.   It  suggests  that  it  would  be  difficult for  econazole  to  block  the  interaction  of  thapsigargin  with  Ca2+ -ATPase  to increase  intracellular  Ca2+.In  conclusion,  econazole  inhibited  the  increase  of intracellular Ca2+involving the blokade of voltage-dependent Ca2+ channels, but not involving the Ca2+ -ATPase pathway.Key words :econazole, Ca2+ -ATPase, CRAC current, thapsigargin 
Co-Authors Agung Endro Nugroho Agung Endro Nugroho Dani Dwi Agistia Kazutaka Maeyama Maulana Tegar AdityaNugraha