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All Journal INDONESIAN JOURNAL OF PHARMACY

Kazutaka Maeyama

Department of Pharmacology, Informational Biomedicine, School of Medicine, Ehime University Japan

Author-ID : 3096839

Medicine & Pharmacology

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The effects of PGV-1 and PGV-2 on the b-hexosaminidase release from intraceluller calcium ion-induced mast cells Agung Endro Nugroho; Sardjiman .; Kazutaka Maeyama
Indonesian Journal of Pharmacy Vol 20 No 4, 2009
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

PGV-1 or 2,5-bis(4'-hydroxy-3',5'-dimethylbenzylidene)cyclopentanone and PGV-2 or 2,5-bis(4'-hydroxy-3',5' diethylbenzylidene)cyclopentanone are two benzylidene cyclopentanone analogues of curcumin. In our study, we investigated the effects of these compounds on the b-hexoaminidase enzyme release from mast cell culture (RBL-2H3 cell line). Thapsigargin and ionomycin were used as intracellular calcium ion stimulants for inducing b-hexoaminidase enzyme release from mast cells. The release of b-hexoaminidase enzyme was determined by colorimetric methods with substrate, p-nitrophenyl-2-acetamido-2-deoxy-b-D-glucopyranocide, and a microplate reader at 405 nm. In present study, treatment of 0.5 mM thapsigargin or 1 mM ionomycin could stimulate the release of b-hexoaminidase enzyme from RBL-2H3 cells by 43.91 ± 1.30 % and 52.93 ± 2.07 %, respectively. PGV-1 and PGV-2 showed inhibitory effects on the b-hexoaminidase enzyme release from RBL-2H3 cells induced by the increase of intraceluller calcium ion in dose dependent manner. At the dose of 100 mM, PGV-1 and PGV-2, respectively, inhibited the b-hexoaminidase enzyme release by 73.51 ± 8.69 % and 66.42 ± 8.63 % on thapsigargin experiments; and by 89.73 ± 3.23 % and 38.57 ± 5.32 % on ionomycin experiments. The IC50 values of their effects on the b-hexoaminidase enzyme release from RBL-2H3 cells, respectively, were 22.20 mM and 22.27 mM on thapsigargin experiment; and 22.77 mM and >100 mM on ionomycin experiment. Based on the results, the inhibitory effect of PGV-1 and PGV-2 on the b-hexoaminidase enzyme release from RBL-2H3 cells involving mechanisms related to the alteration on activation processes of intracellular calcium ion on mast cells.Key words : Curcumin, PGV-1, PGV-2, mast cells, b-hexoaminidase enzyme

The cytotoxic and antiproliferative effects of gamavuton-0 in rat basophilic Leukemia cells Agung Endro Nugroho; Sardjiman .; Kazutaka Maeyama
Indonesian Journal of Pharmacy Vol 20 No 2, 2009
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Gamavuton-0 (GVT-0), also named as 1,5-bis(4’-hydroxy-3’- methoxyphenyl)-1,4-pentadiene-3 one is a 1,5-diphenyl-1,4-pentadiene-3-one analog of curcumin by modifying the center site of curcumin leading to 1,4-pentadiene-3-ones to maintain the hydroxy moiety at aromatic rings which are responsible for its biological activities. Curcumin has been reported to have potent anticarcinogenic effects. Besides, curcumin was found to induce apoptosis in human Leukemia cells. In our study, we investigated the cytotoxic and antiproliferative effects of gamavuton-0 in rat basophilic leukemia cells. Cell viability was determined by WST-1 assay. In brief, tetrazolium salts were cleaved to formazan by cellular enzymes of viable cells, determined by colorimetric methods with a microplate (ELISA) reader at 450 nm.In the present study, we evaluated cytotoxic and proliferative effects of GVT-0 in rat basophilic leukemia cells. In the study, GVT-0 induced rat basophilic leukemia cells death in a dose dependent manner after overnight incubation. GVT-0 also impaired the content of histamine and b-hexoaminidase enzyme in cells. However, the cytotoxic effect of GVT-0 (IC50 : 43,67 mM) was less potent than this of curcumin (IC50 : 29,14 mM). GVT-0 (1 mM) also showed a significant inhibition of cell growth after 48 and 72 hr. Its fact indicates that GVT-0 could prolong the cells doubling time. These results provide useful information to guide the development of new synthetic compounds for the treatment of cancer diseases.Key words : gamavuton-0, curcumin, cancer, cytotoxic, antiproliferative,

Effects of pentagamavunon-0 on histaminemediated hyperresponsive airway in asthmatic models : in-vitro in-vivo Agung Endro Nugroho; Hemmy Prasetyo; Djoko Suhardjono; Mulyono Zhang Be; Shuang Liu; Supardjan A. Margono; Kazutaka Maeyama
Indonesian Journal of Pharmacy Vol 21 No 2, 2010
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Asthma is a chronic inflammatory airway disease involving reversible airway constriction and airway hyperresponsiveness (AHR) to allergens, airway edema, and increased mucus secretion tumor cells. To date, exploration of antiasthmatic drug is still being studied both from natural products or sinthetic processes. One of the sinthetic compound is pentagamavunon-0 (PGV-0) which possesses anti-inflammatory and inhibitory effects on histamine release from rat mast cells. The aim of the study is to look at the effects of PGV-0 on histaminemediated hyperresponsive airway in asthmatic models (in vitro and in vivo studies). In vitro study was conducted using isolated organ technique with isotonic transducer. The results have shown that PGV-0 could not inhibit the contraction of isolated guinea pig trachea induced by histamine. PGV-0 did not change the pD2 and Emax values of histamine on trachea smooth muscle. The finding indicates that PGV-0 does not have affinity and intrinsic activity on H-1 histaminergic receptor in trachea smooth muscle. In vivo study, we sensitized the rats with ovalbumin (OVA) to develop the airway hyperreactivity to histamine. Histamine level in bronchoalveolar lavage fluid (BALF) and airway tissue were determined using HPLC-fluorometry. Multiple exposures of ovalbumin significantly histamine level in BALF by 74.51±5.33 pmol/mL or 6-times higher than this of control saline group. Oral administration of PGV-0 (40 mg/kg BW) significantly decreased the histamine accumulation in BALF to 30 % of the value of control group in asthmatic rats. Besides, PGV-0 significantly prevented the histamine decrease in asthmatic rats to 37.8 % trachea, and 34.2 % in bronchus. However, PGV-0 did not succeed to prevent the histamine decrease in the lung of asthmatic rats. The result of the study may provide useful information for further discovering pharmacological synthetic compound for treatment of allergic inflammatory asthma.Key words: asthma, curcumin, pentamavunon-0, histamine, airway hyperresponsiveness

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

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 Agung Endro Nugroho Agung Endro Nugroho Djoko Suhardjono Hari Purnomo Hemmy Prasetyo Mulyono Zhang Be Sardjiman . Sardjiman . Shuang Liu Supardjan A. Margono

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