INDONESIAN JOURNAL OF PHARMACY
Vol 21 No 4, 2010

Inhibitory effect of THPGV-0 on the histamine release from antigen-induced RBL-2H3 cells

Agung Endro Nugroho (Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Gadjah Mada University, Sekip Utara Yogyakarta)
Ritmaleni Ritmaleni (Pharmaceutical Chemistry, Faculty of Pharmacy, Universitas Gadjah Mada, Jogjakarta, Indonesia)
Novrizal Abdi Sahid (Pharmacology, Informational Biomedicine, Ehime University Graduate School of Medicine, Shitsugawa, Japan)
Kazutaka Maeyama (Pharmacology, Informational Biomedicine, Ehime University Graduate School of Medicine, Shitsugawa, Japan)



Article Info

Publish Date
01 Oct 2010

Abstract

Tetrahydropentagamavunon-0  (THPGV-0)  is  assumed  to  be  main metabolite  product  of  biotransformation  process  of  PGV-0.  THPGV-0  was synthesized  by  converting  PGV-0  to  the  compound  by  hydrogenation  with  Pd/C as a catalyst. PGV-0 potently inhibited the histamine release from  rat mast cells in  vitro  and  in  vivo,  however,  ironically  only  traces  amount  of  compound  was found in the blood. THPGV-0 is assumed to have important roles in the biological effects of PGV-0 in vivo. In present study, we investigated the antiallergy effect of  THPGV-0  in  compare  to  this  of  PGV-0  in  vitro.  The  study  was  performed  by using  rat  basophilic  leukemia  (RBL-2H3)  cell  line,  a  tumor  analog  of  mucosal mast  cells.  DNP-BSA,  an  antigen,  was  used  as  an  inducer  for  stimulating  the histamine  release  from  mast  cells.  In  present  study,  THPGV-0  at  low concentration  did  not  succeed  to  inhibit  the  histamine  release,  but  at  higher concentration (30 and 100  M) showed strong effects. THPGV-0 at concentration of  100  M  depleted  the  histamine  release  by  96.10  0.51%.  In  compare  to PGV-0,  THPGV-0  has  higher  efficacy  but  less  potent.  In  the  study,  the possibilities  of  the  spontaneous  release  from  RBL-2H3  cells  by  the  compounds were also observed. All concentrations of THPGV-0 as well as PGV-0 showed low spontaneous histamine release, less than 10 % of the total histamine contained in RBL-2H3 cells.Key words: tetrahydropentagamavunon-0, allergy, histamine, RBL-2H3 cells

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Journal Info

Abbrev

3

Publisher

Subject

Medicine & Pharmacology

Description

Indonesian Journal of Pharmacy (ISSN-e: 2338-9486, ISSN-p: 2338-9427), formerly Majalah Farmasi Indonesia (ISSN: 0126-1037). The journal had been established in 1972, and online publication was begun in 2008. Since 2012, the journal has been published in English by Faculty of Pharmacy Universitas ...