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

Agung Endro Nugroho; Ritmaleni Ritmaleni; Novrizal Abdi Sahid; Kazutaka Maeyama

doi:10.14499/indonesianjpharm0iss0pp242-249

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

Agung Endro Nugroho, Ritmaleni Ritmaleni, Novrizal Abdi Sahid, Kazutaka Maeyama

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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References

Barsumian, E. L., Isersky, C., Petrino, M. G., and Siraganian, R. P., 1981, IgE-induced histamine release from rat basophilic leukemia cell lines, Eur. J. Immunol., 11(4): 317-323.

Di Bello, M. G., Masini, E., Ioannides, C., Ndisang, J. F., Raspanti, S., Sacchi, T. B., and Mannaioni, P. F., 1998, Histamine release from rat mast cells induced by the metabolic activation of drugs of abuse into free radicals, Inflamm. Res., 47(3):122-130.

Kodak, 1961, Film-forming photosensitive polymers, Chem. Abstrs., 55 : 11154h.

Kustaniah, 2001, Profil Kadar Senyawa 2,5-Bis-(4’-Hidroksi-3’-Metoksi Benzilidin)-Siklopentanon (Pentagamavunon-0) dalam darah setelah pemberian secara Intraperitoneal pada tikus jantan Wistar, Skripsi, Fakultas Farmasi, Universitas Gadjah Mada, Yogyakarta.

Liu, F. T., Bohn, J. W., Ferry, E. L., Yamamoto, H., Molinaro, C. A., Sherman, L. A., Klinman, N. R., and Katz, D. H., 1980, Monoclonal dinitrophenyl-specific murine IgE antibody: preparation, isolation, and characterization, J Immunol., 124(6), 2728-2737.

Mannaioni, P. F., Bello, M. G. D., Raspanti, S., Mugnai, L., Romano, V., and Masini, E., 1996, Free radical mediated release of histamine from rat mast cells induced by drugs of abuse, Inflamm. Res., 45(suppl.1):S25-S26.

Metcalfe, D. D., Baram, D., and Mekori, YA., 1997, Mast Cells, Physiol Rev., 77(4): 1033-1064.

Nugroho, A. E., 2006, Pharmacological aspects of the main metabolite of curcumin, tetrahydrocurcumin (a review), Scientific Journal of Pharmacy, 3(1) : 37-47.

Nugroho, A. E., Ikawati, Z., Sardjiman, and Maeyama, K., 2009, Effects of benzylidenecyclopentanone analogues of curcumin on histamine release from mast cells, Bio. Pharm. Bull., 32(5) : 842-849.

Nugroho, A. E., Prasetyo, H., Suhardjono, D., Mulyono, Bei, Z., Liu, S., Supardjan, A. M., and Maeyama, K., 2010b, Effects of PGV-0 on histamine-mediated hyperresponsive airway in asthmatic models : in vitro and in vivo studies, Majalah Farmasi Indonesia, 21(2) : 90-99.

Nugroho, A. E., Sardjiman, and Maeyama, K., 2010a, Inhibitory effect of 2,5-bis(4-hydroxy-3-methoxy benzylidene) cyclopentanone on mast cell histamine mediated-rat paw edema, Thai. J. Pharm. Sci., 34 : 107-116

Nugroho, A. E., Sardjiman, and Maeyama, K., 2010c, Comparison of Cytotoxic and Antiproliferative Effects of Benzylidenecyclopentanone Analogues of Curcumin on RBL-2H3 Cells, Indonesian Journal of Biotechnology, In Press.

Nurshanti, N. L .P, 2001, Profil Kadar Senyawa 2,5-Bis-(4’-Hidroksi-3’-Metoksi Benzilidin)-Siklopentanon dalam darah setelah pemberian secara Intravena pada tikus betina Sprague Dawley, Skripsi, Fakultas Farmasi, Universitas Gadjah Mada, Yogyakarta.

Pan, M. H., Huang, T. M., and Lin, J. K., 1999, Biotransformation of curcumin through reduction and glucuronidation in mice, Drug Metab. Dispos., 21 : 486-494.

Patkar S.A., Rasmussen, U., Diamant, B.. 1979, On the mechanism of histamine release induced by thapsigargin from Thapsia garganica L., Agents Actions, 9(1):53-57.

Priyadarsini, K. I., Maity, D.K., Naik, G.H., Kumar, M.S., Unnikrishnan, M.K., Satav, J.G., and Mohan, H.. 2003, Role of phenolic O-H and methylene hydrogen on the free radical reactions and antioxidant activity of curcumin, Free Radic Biol Med., 35(5):475-484.

Rang, H.P., Dale, M.M., Ritter, J. M., and Moore, PK. 2003., Pharmacology, 5th Ed., Churchill Livingstone, Sydney.

Ritmaleni, and Simbara, A., 2010, Sintesis Tetrahidro Pentagamavunon-0 (THPGV-0), Majalah Farmasi Indonesia, 21(2) : 100-105.

Simbari, A., 2009, Sintesis dan uji antioksidan senyawa tetrahidropentagavunon-0 (THPGV-0), Thesis, Program Pascasarjana, Fakultas Farmasi Universitas Gadjah Mada, Jogjakarta.

Sugiyama, Y., Kawakishi, S. and Osawa, T., 1996, Involvement of The Beta-diketone Moiety in The Antioxidative Mechanism of Tetrahydrocurcumin, Biochem. Pharmacol., 52 : 519-525.

Sugiyanto, Oetari, and Nugroho, A.E., 2003, Biotransformation of Pentagamavunon-0 (PGV-0) : In Vitro and In Vivo Studies, Majalah Farmasi Indonesia, 14(2) : 290-298.

Suzuki, M., Nakamura, T., Iyoki, S., Fujiwara, A., Watanabe, Y., Mohri, K., Isobe, K., Ono, K., and Yano, S., 2005, Elucidation of anti-allergic activities of curcumin-related compounds with a special reference to their anti-oxidative activities, Biol Pharm Bull., 28(8) : 1438-1443.

Yamatodani, A., Fukuda, H., Wada, H., Iwaeda, T., and Watanabe, T., 1985, High-performance liquid chromatographic determination of plasma and brain histamine without previous purification of biological samples : cation-exchange chromatography coupled with post-column derivatization fluorometry, J Chromatogr., 344 : 115-123

DOI: http://dx.doi.org/10.14499/indonesianjpharm0iss0pp242-249