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Journal : INDONESIAN JOURNAL OF PHARMACY

PGV-1 decreases angiogenic factor (VEGF and COX-2) expression on T47D cell induced by estrogen Meiyanto, Edy; Melannisa, Rosita; Da'i, Muhammad
Indonesian Journal of Pharmacy Vol 17 No 1, 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 (326.278 KB) | DOI: 10.14499/indonesianjpharm0iss0pp1-6

Abstract

Breast cancer is the most common cancer occurring in women after cervix cancer in Indonesia. Tumor metastasis is the major cause of mortality in breast cancer. For a tumor cell to metastasize effectively, it must induce angiogenesis. 17 β-estradiol has been shown to stimulate the proliferation and angiogenesis of breast cancer cells which express estrogen receptor (ER), T47D (human breast cancer cell line). In the present study Pentagamavunon-1 or PGV-1 [2,5-bis-(4’-hydroxy-3’,5’-dimethylbenzylidene)-cyclopentanone], an analogue of curcumin [1,7-bis-(4’-hydroxy-3’-methoxyphenyl)-1,6-heptadiena-3,5-dion], were tested on their cytotoxicity and suppression effect on angiogenic factors (i.e. VEGF and COX-2) on the breast cancer cell lines (T47D) induced by 17 β-estradiol 10-8 M. The results showed that PGV-1 performed cytotoxicity effect againts T47D cells with IC50 values 3,16 μM. This was more potent than curcumin (IC50 = 19,05 μM). PGV-1 5 μM and curcumin 20 μM decrease VEGF and COX-2 expression. These results suggest both compounds possessed antiangio-genic potensial.Key words : PGV-1, curcumin, 17 β-estradiol, angiogenesis
Geometric Isomers and Cytotoxic Effect On T47D Cells of Curcumin Analogues PGV-0 and PGV-1 Edy Meiyanto; Muhammad Da'i; Supardjan A. M.; Umar Anggara Jenie
Indonesian Journal of Pharmacy Vol 18 No 1, 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 (343.101 KB) | DOI: 10.14499/indonesianjpharm0iss0pp40-47

Abstract

Curcumin analogues 2,5-bis-(4’-hidroxy-3’-methoxy)-benzilidinecylopentanone (PGV-0) and 2,5-bis-(4’hidroxy-3’,5’-dimethyl)-benzilidinecylopentanone (PGV-1) have a potency to be developed as cytotoxic agent. The aims of this research are to elucidate the geometric isomer and to study the cytotoxic effect on T47D cells of both compounds. To establish the geometric isomer these compounds, they were elucidated by LC-MS, 1H-NMR, 13C-NMR, HMBC, HMQC, NOESY. Their cytotoxic effect were evaluated by MTT assay method on T47D cells. The results concluded that the geometric isomer of PGV-1 is zusammen-zusammen (Z-Z) and PGV-0 is entgegen-entgegen (EE). The IC50 of both compounds are 1.74 and 9.39 μM respectively.Key words: PGV-0, PGV-1, Cytotoxicity
PGV-1 is a potent antimitotic agent Barinta Widaryanti; Edy Meiyanto; Muhammad Da'i; Masashi Kawaichi
Indonesian Journal of Pharmacy Vol 19 No 3, 2008
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (266.103 KB) | DOI: 10.14499/indonesianjpharm0iss0pp145-150

Abstract

Carcinogenesis can be involved in the malfunctioning of programmed cell death Most of the anticancer drug in current use induce apoptosis in susceptible cells. The fact that disparate agent interacting with different targets seem to induce cell death through some common mechanism suggest that anticancer activity is determined by the ability of inhibiting cell growth.Pentagamavunon-1 (PGV-1) is one of the curcumin analogue which showed to have potency in inhibiting proliferation of human breast carcinoma cell T47D. The effect on T47D growth is associated with cell cycle arrest in G2/M phase at the concentration of 2.5 mM, followed by hyperploidy. Our data on polymerization assay, indicate PGV-1 interact with tubulin in different manner from taxol. PGV-1 inhibit tubulin polymerization on cell culture while taxol stabilized tubulin polymerization. Immunostainning data on cell treated with PGV-1 showed slightly tubulin condensation, while cell treated with taxol showed tubulin condensation distinctly at 12 minutes after releasing from depolymerization agent.In conclusion, PGV-1 represent a new microtubule inhibitor and has the potential to be developed for anticancer drugKey words: Pentagamavunon-1, T47D, tubulin, antimitotik