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Inhibitor Effect of THPGV-0 on the Histamine Release From Antigen-Induced RBL-2H3 Cells (Efek THPGV-0 tehadap Pelepasan Histamin dari Kultur Sel RBL-2H3 dinduksi Antigen)
Tetrahydropentagamavunon-O (THPGV-O) is assumed to be main metabolite product of biotransformation process of PGV-O. THPGV-O was synthesized by converting PGV-O to the compound by hydrogenation with PdjC as a catalyst. PGV-O potently inhibited the histamine release from ~at mast cells in vitro and in vivo, however, ironically only traces amount of compound was found in the blood. THPGV-O is assumed to have important roles in the biological effects of PGV-O in vivo. In present study, we investigated the antiallergy effect of THPGV-O in compare to this of PGV-O 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-O at low concentration did not succeed to inhibit the histamine release, but at higher concentration (30 and 100 I'M) showed strong effects. THPGV-O at concentration of 100 I'M depleted the histamine release by 96.10 ±O.Sl %. In compare to PGV-O, THPGV-O 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-O as well as PGV-O showed low spontaneous histamine release, less than 10 % of the total histamine contained in RBL-2H3 cells.
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