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All Journal INDONESIAN JOURNAL OF PHARMACY
Agung Endro Nugroho
Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy Universitas Gadjah Mada Yogyakarta
Medicine & Pharmacology

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Active cutaneous anaphylaxis-inhibitory activity of Gamavuton-0 potassium (K-GVT-0) Agung Endro Nugroho; Nunung Yuniarti; Enade Perdana Istyastono; Supardjan .; Lukman Hakim
Indonesian Journal of Pharmacy Vol 18 No 2, 2007
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (277.154 KB) | DOI: 10.14499/indonesianjpharm0iss0pp63-70

Abstract

Potassium Gamavuton-0 is a salt form of 1,5-bis(4’-hydroxy-3’-methoxyphenyl)-1,6-heptadiene-3,5 dione or gamavuton-0. Structure modification to a salt form is expected to result in a soluble compound which should have a better bioavailability. The purpose of this experimental study was to evaluate the inhibitory effects of potassium gamavuton-0 on active cutaneous anaphylaxis reaction induced by ovalbumin as an antigen.The study was performed using an active cutaneous anaphylaxis method followed by histopathological observation. The rats were subcutaneously sensitised by ovalbumin (OVA) and Al(OH)3 twice on the days of 0 and 7, and finally were challenged by ovalbumin on the day of 14 to induce active cutaneous anaphylaxis reaction. In order to determine the mast cells on the inflammation tissues, the specimens were stained with 0.1 % Alcian Blue (pH 0.3) and nuclear fast red. Under light microscopy, mast cells were identified as blue granules against a pale red backgound.The results showed that potassium gamavuton-0 at the doses of 20 and 40 mg/kg BW could inhibit the pigmentation area of vascular permeability on rats dorsal skin. It indicated that this compound has the inhibitory effect on active cutaneous anaphylaxis reaction with ED30 value of 28.26 mg/kg BW. Nevertheless, inhibitory effect of potassium gamavuton-0 was still lower than that of cromolyn sodium, a mast cell degranulation inhibitory drug. Histopathologically, the mechanism of inhibitory effect of potassium gamavuton-0 on active cutaneous anaphylaxis reaction is suggested through the inhibition on mast cell degranulation process responsible for releasing inflammation mediators such as histamine, serotonin.Key words: Gamavuton-0 potassium, anaphylaxis, mast cell, ovalbumin
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

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (219.677 KB) | DOI: 10.14499/indonesianjpharm0iss0pp84-90

Abstract

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,
Profile of sulphacetamide pharmacokinetics on uranyl nitrate-induced renal failure rats Djoko Wahyono; Arief Rahman Hakim; Agung Endro Nugroho
Indonesian Journal of Pharmacy Vol 18 No 3, 2007
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (180.141 KB) | DOI: 10.14499/indonesianjpharm0iss0pp117-123

Abstract

Kidney is a vital organ which has main function to maintain the body homeostasis. The role of kidney is the excretion (elimination) of waste product, and if there is pathologically a renal failure so will change the drug pharmacokinetics and in turn change it’s potency. The present study evaluated the effect of uranyl nitrate-induced renal failure on the pharmacokinetics profiles of sulphacetamide in rats.The study was conducted by employing a completely randomized design in male Wistar in bred rat (aged 2-2.5 months, 150-250 g). The animals in group I were given sulphacetamide sodium with an oral single dose 100.0 mg/kg BW (control group) and in group II were given pretreatment with uranyl nitrate at 3 days before sulphacetamide administration.After collected at some certain times, the drug concentrations on bloods were analyzed by an ultraviolet spectrophometer. The results have shown that uranyl nitrate-induced renal failure decreased the primer pharmacokinetics parameter i.e. total clearance (ClT) and volume of distribution in steady state (Vdss), significantly (P<0.05). The decreasing of these parameter could cause alteration of the secondary pharmacokinetics parameters of sulphacetamide and these derivates i.e. Cmax, tmax, AUC0-240, AUC0-inf, MRT, K and t1/2 elimination significantly (P<0.05). According from the results, it is concluded that uranyl nitrate-induced renal failure affected the pharmacokinetics of sulphacetamide or could increase the sulphacetamide concentration in blood.Key words : sulphacetamide, pharmacokinetics, renal failure, uranyl nitrate
Determination of antioxidant activity of dehydrozingerone through hydroxy radical scavengers using deoxyribosa method Agung Endro Nugroho; Nunung Yuniarti; Enade Perdana Estyastono; Supardjan .; Lukman Hakim
Indonesian Journal of Pharmacy Vol 17 No 3, 2006
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (192.727 KB) | DOI: 10.14499/indonesianjpharm0iss0pp116-122

Abstract

Dehydrozingerone (4-(4-hydroxy-3-methoxyphenyl)-3-buten-2-one) is an analog of curcumin which is termed as half-curcumin. The compound is isolated from ginger (Zingiber officinale). Nevertheless, this compound still has a phenolic hydroxy moiety responsible for antioxidant activity. The research was performed to obtain information on the antioxidant activity of dehydrozingerone through hydroxy radical scavengers.The study was performed according to a hydroxy radical scavenging procedur. In this method, reaction between hydroxy radical, resulted from phenton reaction, and deoxyribosa produces malonedealdehyde. Incubation in thiobarbituric acid at low pH produced violet-coloured solution (complex MDA-TBA).The results showed that dehydrozingerone has antioxidant activity through hydroxy radical scavengers with ES15 value of 48.36 μM. The antioxidant activity of dehydrozingerone was lower than curcumin, with ES15 value of 25.01 μM. Besides, exchange of phenolic hydroxy moiety by salting with potassium could deplete its antioxidant activity. Based on these facts, it can be concluded that phenolic hydroxy moiety of dehydrozingerone was important for its antioxidant activity through hydroxy radical scavengers.Key words : dehydrozingerone, curcumin, antioxidant, radical hydroxy, Zingiber
Co-Authors Arief Rahman Hakim Djoko Wahyono Enade Perdana Estyastono Enade Perdana Istyastono Kazutaka Maeyama Lukman Hakim Nunung Yuniarti Sardjiman . Supardjan . Supardjan .