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Abstrak :
Asam galat adalah senyawa yang memiliki efek anti kanker termasuk pada kanker paru. Diduga, efektivitas asam galat sebagai agen sitotoksik dapat ditingkatkan dengan perubahan gugus samping. Penelitian ini bertujuan untuk menguji aktivitas sitotoksik asam galat dan turunan asam galat (alkil ester galat dan asam metoksi galat). Pada penelitian ini, sel A549 diberikan asam galat dan turunannya lalu diinkubasi selama 48 jam lalu akan diukur persentase viabilitas sel terhadap kontrol menggunakan MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Data kemudian dianalisis menggunakan GraphPad Prism untuk mendapatkan inhibitory concentration (IC50).
Hasil penelitian menunjukkan bahwa asam galat, metil galat, etil galat, propil galat, butil galat, isobutil galat, t-butil galat, dan amil galat tidak memiliki aktivitas sitotoksik. Sedangkan isoamil galat menunjukkan aktivitas sitotoksik namun IC50 dari isoamil galat kemungkinan >51,2 μg/ml. Heptil galat dan oktil galat adalah dua senyawa yang memiliki efek sitotoksik pada sel A549 dengan nilai IC50 <51,2 μg/ml yaitu 19,11 μg/ml dan 41,23 μg/ml secara berurutan. Disimpulkan bahwa heptil galat dan oktil galat memiliki aktivitas sitotoksik yang lebih baik dari asam galat pada sel A549, sedangkan asam metoksi galat tidak memiliki aktivitas sitotoksik pada sel A549.

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Gallic acid is a substance with anti-cancer activity including lung cancer. The potency of gallic acid as a cytotoxic agent can be improved by modifying its side chains. This study was aimed to examine the cytotoxic activity of gallic acid and its derivates in lung cancer cells, A549. In this study, cells were treated with gallic acid and its derivates and were incubated for 48 hour. After incubation period, percentage of cell viability over control were tested using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulophenyl)-2Htetrazolium) assay. Afterwards, data were analysed using GraphPad Prism to obtain inhibitory concentration (IC50).

The result showed gallic acid, methyl gallate, ethyl gallate, propyl gallate, butyl gallate, isobutyl gallate, t-butyl gallate, and amyl gallate did not have cytotoxic activity. Isoamyl gallate showed cytotoxic activity, but the IC50 value was probably >51,2 μg/ml. That gallic acid derivatives with cytotoxic activities and IC50 <51,2 μg/ml were heptyl gallate and octyl gallate with IC50 values of 19,11 μg/ml and 41,23 μg/ml, respectively. However, methoxy gallate (monometohoxy gallate, dimethoxy gallate, and trimethoxy gallate) did not show any cytotoxic activity. We conclude that heptyl gallate and octyl gallate have better cytotoxic activity in A549 cells compared to gallic acid, while methoxy gallates do not have cytotoxic activity in cell A549.

Abstrak :
Marine-derived fungi have proven to be a rich source of cytotoxic compounds for the development of new anti cancer drugs. The aims of this research were to: 1) screen cytotoxic activity of marine fungi from Indonesian waters, 2) indentify marine fungus that produced that produced the most active cytotoxic compound and 3) investigate inhibition concentration 50 (IC50) value of cytotoxic compound. The fungi were isolated from marine organism collected from Wakatobi Marine National Park-South East Sulawesi, Binuangeun Beach-Banten, Manado watersNorth Sulawesi and Kepulauan Seribu Marine National Park-Jakarta. Liquid cultures of the fungi were carried out in Malt Extract Broth and Soluble Starch Soytone medium for 4 weeks at 27?28oC without shaking. Molecular identification of fungus was conducted through PCR amplificatin using primers of ITS1 and ITS4 primer. Cytotoxic activity of the extract was tested by using MTT (3-(4.4-dimethylthiazol-2-yl)-2.5-diphenyl-tetrazolium bromide) method. The MTT test showed that MFW39 strain exhibited the strongest cytotoxic activity. Molecular identification revealed that MFW39 marine fungus was similar to Emericella nidulans with precent identity of 99%. Mycelium and broth extract of MFW39 fungus inhibited the growth of T47D cell with IC 50 values of 21.9 and 169.3 µg/mL, respectively. Further research will be focus on to the strain of MFW39 marine fungi.

Abstrak :
Pendahuluan: Asam galat adalah salah satu senyawa aktif yang dapat menyebabkan apoptosis pada sel kanker paru manusia. Aktivitas antikanker paru yang mengesankan dari asam galat mendorong dilakukannya penelitian untuk menguji aktivitas sitotoksik senyawa turunan asam galat (alkil amida galat) terhadap sel kanker paru A549. Metode: Enam senyawa alkil amida galat hasil sintesis, yaitu Senyawa metil amida galat, etil amida galat, butil amida galat, sek-butil amida galat, ters-butil amida galat, dan heksil amida galat diuji aktivitas sitotoksiknya terhadap sel kanker paru A549 dengan metode MTT Proliferation assay. Data yang dihasilkan dianalisa menggunakan analisis regresi linear untuk mendapatkan nilai IC50. Hasil uji aktivitas sitotoksik senyawa alkil amida galat hasil sintesis dibandingkan dengan hasil uji aktivitas sitotoksik asam galat sebagai senyawa asli dan doxorubicin selaku kontrol positif. Hasil: Jika dibandingkan dengan asam galat (IC50: 23.2 μM) dan doxorubicin (IC50: 31.1 μM), keenam senyawa alkil amida galat, yaitu metil amida galat, etil amida galat, butil amida galat, sek-butil amida galat, ters-butil amida galat, dan heksil amida galat memperlihatkan sitotoksisitas yang lebih kuat terhadap sel kanker paru A549 dengan nilai IC50 berkisar dari 5.4 μM hingga 30.0 μM. Kesimpulan: Enam senyawa alkil amida galat berpotensi dikembangkan lebih lanjut sebagai agen antikanker paru. ......Objective: Gallic acid has shown its potential to induce apoptosis in lung cancer cells. Its impressive anti-lung cancer agent prompted us to conduct research that is aimed to evaluate six alkyl amide derivatives of gallic acid against lung cancer A549 cells. Methods: six synthesized compounds of alkyl amide gallate, which are methyl amide gallate, ethyl amide gallate, butyl amide gallate, sec-butyl gallate, ters-butyl gallate and hexyl amide gallate, will be evaluated their cytotoxicities agains lung A549 cells by MTT Proliferation assay. Linear regression analysis is used to analyzed the data to generate IC50 value. Cytotoxicity results of alkyl amide gallates will be compared with cytotoxicity result of gallic acid as an original compound and with doxorubicin as positive control. Results: Compared with gallic acid (IC50 23.2 μM) and doxorubicin (IC50 31.1 μM), six derivatives of aklyl amide gallates (methyl-, butyl-, sec-butyl-, ters- butyl, and hexyl amide gallate) shows better cytotoxic activity against lung A549 cells, with IC50 value range from 5.4 μM to 30.0 μM. Conclusion: Six compounds of Alkyl amide gallate could be further developed as anti-lung cancer agent.