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"ABSTRAKKanker payudara adalah kanker kedua terbanyak diderita di dunia, sedangkan di Indonesia kanker payudara menempati peringkat kedua jenis kanker yang paling sering terdiagnosis setelah kanker serviks di Indonesia. Terdapat beberapa pilihan terapi untuk kanker payudara seperti operasi, kemoterapi, dan radiasi yang memiliki efektivitas rendah pada stadium lanjut dan kerap menimbulkan efek samping. Oleh karena itu dibutuhkan pilihan terapi lain dengan efek terapetik yang optimal dan efek samping yang minimal. Salah satu senyawa alami yang berpotensi dikembangkan sebagai antikanker adalah asam galat. Penelitian ini dilakukan untuk mengetahui aktivitas sitotoksik senyawa asam galat dan derivatnya dengan menggunakan 8 variasi konsentrasi, yaitu 0,07; 0,13; 0,27; 0,53; 1,07; 2,13; 4,27 dan 8,53 g/ml pada lini sel kanker payudara T47-D. Dengan metode MTT assay, didapatkan nilai absorbansi dan viabilitas sel yang kemudian diolah dengan menggunakan GraphPad Prism untuk mendapatkan nilai IC50 dari tiap senyawa uji. Hasil menunjukkan alil galat, amil galat, trans-heksinil galat, benzil galat, sekunder amil galat, propil galat, dan isoamil galat memiliki IC50 yang rendah, yaitu 1,25 g/mL, 2,78 g/mL, 3,17 g/mL, 4,82 g/mL, 5,32 g/mL, 7,84 g/mL, dan 8,02 g/mL. Hasil penelitian menunjukkan bahwa modifikasi asam galat melalui penambahan rantai samping alkil ester, penambahan gugus aromatis, dan konfigurasi cis-trans dapat meningkatkan aktivitas sitotoksik senyawa asam galat.

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ABSTRAKBreast cancer is the second most suffered cancer in the world, whereas in Indonesia is the second most suffered after cervix cancer. There are several treatments for breast cancer such as surgery, chemotherapy, and radiation, however these treatments have low effectiveness at advanced stage and often cause side effects. Therefore, there are significant need of treatment with the optimal therapeutic effect and minimal side effects. Gallic acid is a natural compound which could be developed as anticancer agent. This study was conducted to determine the cytotoxic activity of gallic acid and its derivatives by using 8 variety of concentrations, namely 0,07 0,13 0,27 0,53 1,07 2,13 4,27 and 8,53 g ml against breast cancer cell line T47 D. Anticancer activity of the tested samples were evaluated by MTT assay, the absorbance and cell viability values are obtained and processed using GraphPad Prism application to get the IC50 value of each compound. The result showed that allyl gallate, amyl gallate, trans hexynyl gallate, benzyl gallate, sec amyl gallate, propyl gallate, and isoamyl gallate have anticancer activity higher than gallic acid with IC50 value 1,25 g mL, 2,78 g mL, 3,17 g mL, 4,82 g mL, 5,32 g mL, 7,84 g mL, and 8,02 g mL, respectively. It could be concluded that the structure modification of gallic acid through the addition of a side chain alkyl ester, the addition of aromatic groups, and cis trans configuration in gallic acid derivatives could increase its cytotoxic activity."

"[Asam galat merupakan zat polifenol dengan kemampuan sitotoksik. Studisebelumnya menunjukkan turunan asam galat mampu menghambat pertumbuhansel kanker. Sampai saat ini, belum banyak studi yang mempelajari turunan alkilester galat dan turunan metoksi galat terhadap pertumbuhan kanker kolon. Tujuandari penelitian ini adalah untuk mengetahui aktivitas sitotoksik turunan alkil estergalat dan metoksi galat pada sel kanker kolon. Penelitian ini dilakukan dengandesain eksperimental secara in vitro. Kemampuan sitotoksik asam galat danturunannya diuji pada sel HCT116 (sel kanker kolon) dengan menggunakan MTS(3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2Htetrazolium)assay. Data yang diperoleh dianalisis untuk mendapatkan IC50 setiapsenyawa. Hasil penelitian menunjukkan modifikasi asam galat menjadi senyawametil galat, propil galat, butil galat, t-butil galat, amil galat, oktil galat dan ketigaturunan metoksi galat tidak menunjukkan peningkatan aktivitas sitotoksik denganpeningkatan konsentrasi yang diuji. Dari semua senyawa yang memilikikecenderungan menghambat, heptil galat memiliki aktivitas yang paling baik.Disimpulkan, metil galat, propil galat, butil galat, t-butil galat, amil galat, dan oktilgalat merupakan turunan alkil galat yang tidak aktif. Etil galat, isobutil galat,isoamil galat, dan heptil galat merupakan turunan alkil galat yang memiliki aktivitassitotoksik pada sel kanker kolon. Ketiga tur;Gallic acid is a polyphenol with anticancer activity. Previous studies had shown thatthe derivatives of gallic acid had cytotoxic activity in cancer cell. To date, fewstudies evaluated the activity of alkyl ester derivatives of gallic acid and methoxyderivatives of gallic acid in colon cancer cell. The objective of this study was toexamine the cytotoxic activity of alkyl ester derivatives and methoxy derivatives ofgallic acid in colon cancer cell. This study was conducted in in-vitro study inHCT116 colon cancer cell. Cytotoxic activity of gallic acid and its derivatives wereevaluated in HCT116 colon cancer cell using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Data fromthis experiment was analyzed to obtain IC50 of each compound. The result showedthat modification of gallic acid to methyl gallate, propyl gallate, butyl gallat, t-butylgallate, pentyl gallate, octyl gallate and three methoxy derivatives of gallic acid didnot increase cytotoxic activity in all concentrations tested. Among all derivatives ofgallic acid, heptyl gallate has the best cytotoxic activity. In conclusion, methylgallate, propyl gallate, butyl gallate, t-butyl gallate, pentyl gallate, and octyl gallateare alkyl ester derivatives of gallic acid with no cytotoxic activity. Ethyl gallate,isobutyl gallate, isopentyl gallate, and heptyl gallate are active derivatives of gallicacid. All methoxy derivatives of gallic acid do not show any cytotoxic activity incolon cancer cell.;Gallic acid is a polyphenol with anticancer activity. Previous studies had shown thatthe derivatives of gallic acid had cytotoxic activity in cancer cell. To date, fewstudies evaluated the activity of alkyl ester derivatives of gallic acid and methoxyderivatives of gallic acid in colon cancer cell. The objective of this study was toexamine the cytotoxic activity of alkyl ester derivatives and methoxy derivatives ofgallic acid in colon cancer cell. This study was conducted in in-vitro study inHCT116 colon cancer cell. Cytotoxic activity of gallic acid and its derivatives wereevaluated in HCT116 colon cancer cell using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Data fromthis experiment was analyzed to obtain IC50 of each compound. The result showedthat modification of gallic acid to methyl gallate, propyl gallate, butyl gallat, t-butylgallate, pentyl gallate, octyl gallate and three methoxy derivatives of gallic acid didnot increase cytotoxic activity in all concentrations tested. Among all derivatives ofgallic acid, heptyl gallate has the best cytotoxic activity. In conclusion, methylgallate, propyl gallate, butyl gallate, t-butyl gallate, pentyl gallate, and octyl gallateare alkyl ester derivatives of gallic acid with no cytotoxic activity. Ethyl gallate,isobutyl gallate, isopentyl gallate, and heptyl gallate are active derivatives of gallicacid. All methoxy derivatives of gallic acid do not show any cytotoxic activity incolon cancer cell., Gallic acid is a polyphenol with anticancer activity. Previous studies had shown thatthe derivatives of gallic acid had cytotoxic activity in cancer cell. To date, fewstudies evaluated the activity of alkyl ester derivatives of gallic acid and methoxyderivatives of gallic acid in colon cancer cell. The objective of this study was toexamine the cytotoxic activity of alkyl ester derivatives and methoxy derivatives ofgallic acid in colon cancer cell. This study was conducted in in-vitro study inHCT116 colon cancer cell. Cytotoxic activity of gallic acid and its derivatives wereevaluated in HCT116 colon cancer cell using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Data fromthis experiment was analyzed to obtain IC50 of each compound. The result showedthat modification of gallic acid to methyl gallate, propyl gallate, butyl gallat, t-butylgallate, pentyl gallate, octyl gallate and three methoxy derivatives of gallic acid didnot increase cytotoxic activity in all concentrations tested. Among all derivatives ofgallic acid, heptyl gallate has the best cytotoxic activity. In conclusion, methylgallate, propyl gallate, butyl gallate, t-butyl gallate, pentyl gallate, and octyl gallateare alkyl ester derivatives of gallic acid with no cytotoxic activity. Ethyl gallate,isobutyl gallate, isopentyl gallate, and heptyl gallate are active derivatives of gallicacid. All methoxy derivatives of gallic acid do not show any cytotoxic activity incolon cancer cell.]"

"Asam galat adalah salah satu senyawa yang berpotensi menjadi obat baru bagi kanker. Banyak penelitian yang telah menguji aktivitas asam galat sebagai antikanker, tetapi asam galat bersifat sangat hidrofilik sehingga sulit untuk menembus membran sel. Untuk meningkatkan aktivitas sitotoksisitas dan hidrofobisitas, dibuat senyawa turunan asam galat yaitu alkil galat dan metoksi galat. Aktivitas diuji pada sel MCF-7 menggunakan MTS (3-(4,5-dimethylthiazol- 2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay dengan inkubasi selama 48 jam. Aktivitas setiap senyawa ditentukan dengan menggunakan nilai IC50. Dari seluruh senyawa yang diuji, isoamil galat, heptil galat dan oktil galat, merupakan senyawa yang aktif sebagai antikanker MCF-7 dengan nilai IC50 58,11; 25,94 dan 42,34. Berdasarkan ekstrapolasi garis, isobutil galat dan juga dapat menurunkan persentase viabilitas sel, meskipun nilai IC50-nya belum dapat ditentukan dari penelitian ini. Metoksi galat tidak memiliki efek penghambatan pada sel kanker payudara MCF-7. Oleh karena itu, dapat disimpulkan bahwa isobutil, isoamil, heptil dan oktil galat merupakan senyawa turunan asam galat yang memiliki aktivitas sitotoksik sedangkan metoksi galat tidak memiliki aktivitas sitotoksik terhadap MCF-7.

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Gallic acid is a potential chemotherapeutic agent. Many studies have proven the anti cancer activity of gallic acid, including in breast cancer. However, gallic acid is a hydrophilic molecule, which restrict the substance from passing the cell membrane. To increase the potential cytotoxicity and its hydrophobicity, two groups of gallic acid derivatives, alkyl gallates and methoxy gallates, were developed. The activity of these derivatives were tested in MCF-7 cell lines, using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4- sulfophenyl)-2H-tetrazolium) assay, and then incubated for 48 hours. Percentage of cell viability over control were assessed. Cytotoxic activities of gallic acid and its derivatives were determined using IC50 values. Among all of the gallic acid derivatives, isoamyl gallate, heptyl gallate and octyl gallate were the most potential drugs to treat MCF-7 breast cancer with IC50 values of 58,11; 25,94 and 42,34 μg/ml, respectively. Based on the trendline prediction, isobutyl gallate also showed cytotoxic activity towards MCF-7, although the IC50 values cannot be determined in this research. Methoxy gallates do not have any inhibitory activity towards breast cancer MCF-7. In conclusion, isobutyl, isoamyl, heptyl and octyl gallate are gallic acid derivatives with cytotoxic activity, while methoxy gallates do not have any cytotoxic activity towards MCF-7."

"Kanker serviks merupakan kanker ketiga tersering pada perempuan dan kelima tersering di dunia. Hingga saat ini, terapi kanker serviks masih memiliki efek samping dan komplikasi masih tinggi, serta efektivitas pada stadium lanjut masih rendah sehingga menyebabkan perlunya pengembangan terapi yang lain. Asam galat diketahui sebagai antikanker yang potensial. Modifikasi struktur gugus alkil akan mengubah sifat farmakokinetik dan farmakodinamik senyawa. Studi ini menilai aktivitas sitotoksik derivat asam galat. Inhibition concentration (IC50) derivat asam galat dinilai pada sel HeLa. Sel diberikan asam galat atau derivatna dengan jumlah minimal 1x104 sel/ well dengan konsentrasi berkisar antara 0.4 ? 51,2 μg/ml selama 48 jam. Setelah itu, viabilitas sel dinilai menggunakan MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Hasil menunjukkan heptil galat dan oktil galat memiliki IC50 terendah, yaitu 4,00 μg/ml dan 7,47 μg/ml berturut-turut. Penambahan rantai cabang menunjukkan peningkatkan inhibisi sel HeLa. Akan tetapi, derivat metoksi galat tidak menunjukkan perbaikan aktivitas sitotoksik terhadap HeLa. Dengan demikian, modifikasi struktur alkil galat berupa penambahan rantai utama dan cabang derivat asam galat memiliki aktivitas sitotoksik yang lebih baik terhadap HeLa.

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Cervical cancer is the third most common cancer in women and the fifth most common cancer in the world. Nowadays, the treatments for cervical cancer still have high rate of complications and side effects and low effectiveness in advanced stage led to the need for the development of other therapies. Gallic acid is known as potential anticancer. Structure modifications of alkyl gallic acid is predicted to change the pharmacokinetics and pharmacodynamics of the substance. The aim of this study was to observed cytotoxicity activity of gallic acid derivatives. We assessed inhibition concentration (IC50) of gallic acid derivatives in HeLa cells. The cells were given gallic acid or its derivatives with a minimal amount of 1x104 cells/ well at concentration ranged from 0.4 ? 51.2 μg/ml for 48 hours. Afterwards, the cells were subjected for viability assessment using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. The results showed that IC50 of heptyl and octyl gallate were the lowest, which is 4.00 μg/ml and 7.47 μg/ml, respectively. Addition of chain branch was shown to improve the inhibition of HeLa. However, methoxy gallate derivatives did not improve the cytotoxic activity of the substance to HeLa. In conclusion, structure modification of alkyl gallate by adding the main chain and branch gallic acid derivatives increase the cytotoxic activity against HeLa"

"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."

"Kanker serviks merupakan jenis kanker yang paling banyak dialami oleh wanita di Indonesia. Gangguan pada proses apoptosis merupakan tahapan yang penting dalam perkembangan tumor dan menyebabkan sel tumor lebih resisten terhadap terapi sitotoksik konvensional. Protein antiapoptosis Bcl-2 merupakan protein yang berperan penting dalam proses apoptosis yang bisa dijadikan molekul target obat antikanker. Asam galat merupakan senyawa penuntun yang telah terbukti secara in vitro memiliki aktivitas sebagai anti kanker. Penelitian ini bertujuan untuk mendesain, mensintesis dan menguji aktivitas sitotoksik turunan asam galat terhadap sel HeLa. Desain turunan asam galat dilakukan dengan metode structure based drug design untuk mendapatkan senyawa turunan yang menghambat protein anti apoptosis Bcl-2 dengan lebih baik. Lima senyawa turunan asam galat yang memberikan nilai ΔG terkecil dipilih untuk disintesis. Tiga senyawa turunan asam galat disintesis dengan reaksi kondensai dengan alkil halida, sedangkan dua turunan yang lain disintesis dengan reaksi esterifikasi menggunakan katalis DIC dan DMAP. Senyawa hasil sintesis diidentifikasi dengan menggunakan spektrofotometer FT-IR, Spektrometer massa, 1H-NMR dan 13C-NMR. Senyawa hasil sintesis dilakukan uji sitotoksisitas dengan metode MTT. Hasil pengujian sitotoksisitas menunjukkan bahwa tiga turunan ester asam galat memiliki aktivitas penghambatan yang lebih besar pada sel HeLa dibandingkan dengan asam galat dengan IC50 berkisar antara 30,20-34,43 μM.

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Cervical cancer is the most common cancer among women in Indonesia. Impaired apoptosis is a central step in tumor development and renders the tumor cell more resistant to conventional cytotoxic therapy. Proteins Bcl-2, a protein that plays an important role in the process of apoptosis, could be used as an anticancer drugs target molecule. Gallic acid is a lead compound that has been proven have anticancer activity in vitro. The aims of this research are to design, synthesize, and evaluate the cytotoxic activity of gallic acid derivatives in HeLa cells. Gallic acid derivatives is designed by structure-based drug design as anti-apoptotic protein Bcl- 2. Five gallic acid derivatives with the smallest ΔG value are selected for synthesized. Three gallic acid derivatives synthesized by condensation reaction with an alkyl halide, while the other two derivatives were synthesized by esterification reaction using DIC and DMAP catalysts.The synthesized product identified by FT-IR, MS Spectrometer, 1H-NMR and 13C-NMR. Cytotoxicity evaluation are then done by MTT methode. It shows that three derivatives exhibited as a greater anticancer activity against HeLa Cell cells than the lead compound gallic acid with IC50 ranging of 30,20-34,43 μM."

"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.

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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."

"Asam galat merupakan senyawa polihidroksilfenolik yang mempunyai peran penting dalam berbagai aktivitas selektif terhadap banyak sel line. Desain senyawa dengan modifikasi struktur dan mekanisme aksi dari lead compound asam galat diharapkan dapat meningkatkan aktivitas baik lipofilisitas maupun aksi sitotoksiknya. Penelitian ini bertujuan untuk mendesain dan memodifikasi struktur asam galat, melakukan simulasi docking, mensintesis, serta melakukan uji aktivitas sitotoksik senyawa derivat asam galat terhadap sel line kanker kolon HCT-116. Simulasi docking dilakukan dengan beberapa software adalah is MarvinSketch 15.5.11, Chimera 1.10.2, Autodock 4.2, Pymol 1.7.4.5 dan LigPlot v.1.4.5.; sintesis senyawa derivat asam galat melibatkan beberapa reaksi yaitu esterifikasi, metilasi dan hidrolisis; serta melakukan uji sitotoksik terhadap sel kanker kolon HCT-116. Hasil simulasi docking menghasilkan empat senyawa derivat asam galat dengan nilai binding energy terkecil yaitu benzil galat -7,36 kkal/mol , 2-hidroksi benzil galat -7,63 kkal/mol , 4-metoksi- 2-hidroksi benzil galat -7,18 kkal/mol dan feniletil galat -7,47 kkal/mol . Selanjutnya senyawa derivat asam galat disintesis dan dikarakterisasi menggunakan FT-IR, spektrometer Massa, 1H NMR dan 13C NMR. Sintesis senyawa derivat asam galat menghasilkan rendemen masing-masing adalah 62,11 ; 53,25 ; 51,05 dan 58,87 . Uji sitotoksik keempat senyawa derivat asam galat memiliki aktivitas penghambatan yang baik terhadap sel line kanker kolon HCT-116 dengan nilai IC50 masing-masing adalah 24,79 g/mL; 21,82 g/mL; 26,98 g/mL; dan 19,93 g/mL. Senyawa terbaik yang memberikan aktivitas penghambatan terhadap sel kanker kolon HCT-116 adalah feniletil galat dengan IC50 sebesar 19,93 g/mL.

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Gallic acid is a polyhydroxyphenolic compound that has an important role in a variety of selective activity against many cell line. Design modifications of compounds with structures and mechanisms of action of lead compound gallic acid is expected to increase the activity of both lipophilicity and cytotoxic action. This research aims to design and modify the structure of gallic acid, docking simulation, synthesis, and test the cytotoxic activity of gallic acid derivative compounds against colon cancer cell line HCT 116. Docking simulation perfomed with some software is MarvinSketch 15.5.11, Chimera 1.10.2, Autodock 4.2, Pymol 1.7.4.5 and LigPlot v.1.4.5. Synthesis of compound gallic acid derivatives which involves several reaction that is esterification, methylation and hydrolysis. As well as to test the cytotoxic against colon cancer cell HCT 116. Docking simulation results produced four compounds gallic acid derivatives with a value of binding energy smallest that is benzyl gallate 7.36 kcal mol , 2 hydroxy benzyl gallate 7.63 kcal mol , 4 metoksi 2 hydroxy , benzyl gallate 7.18 kcal mol and phenylethyl gallate 7.47 kcal mol . Further synthesized compound gallic acid derivatives with yield respectively is 62.11 53.25 51.05 and 58.87 . Analysis of compound characterization using FT IR, mass spectrometry, 1H NMR and 13C NMR. Test fourth cytotoxic compound gallic acid derivatives have good inhibitory activity against colon cancer cell line HCT 116 with a value IC50 respectively is 24.79 g mL 21.82 g mL 26.98 g mL and 19.93 g L. Compounds that give the best inhibitory activity against colon cancer cells HCT 116 is phenylethyl gallate with IC50 of 19.93 g mL."

"Kanker serviks merupakan kanker dengan prevalensi tertinggi di Indonesia. Tatalaksana kanker serviks saat ini meliputi kemoterapi, radioterapi, dan pembedahan yang relatif mahal dan menimbulkan efek samping. Asam galat adalah senyawa alami yang berpotensi menjadi pengobatan alternatif kanker serviks. Penelitian ini bertujuan untuk mengetahui aktivitas penghambatan asam galat dan derivatnya pada pertumbuhan kultur sel HeLa, yang dinyatakan dengan nilai IC50. Asam galat dan derivatnya dilarutkan dalam phosphate buffered saline PBS , dibuat triplo dengan 8 variasi konsentrasi dalam rentang 0,067-8,533 g/mL. Kultur sel HeLa diencerkan dan ditambahkan 10 mL PBS serta 1 mL dulbecco 39;s modified eagle medium. Viabilitas sel diuji dengan MTT assay. Hasil yang diperoleh menunjukkan terdapat 9 senyawa derivat yang lebih poten sebagai antikanker serviks HeLa dibandingkan asam galat IC50: 3,606 g/mL , yaitu: propil galat IC50: 0,0000674 g/mL , trans-2-heksenil galat IC50: 0,09583 g/mL , cis-2-heksenil galat IC50: 0,19 g/mL , 2-hidroksi-benzil galat IC50: 0,40 g/mL , amil galat IC50: 0,62 g/mL , sekunder-amil galat IC50: 0,73 g/mL , asam 4-cis-2-heksenil-oksi galat IC50: 1,31 g/mL , asam-4-trans-2-heksenil-oksi galat IC50: 1,69 g/mL , dan benzil galat IC50: 2,98 g/mL . Secara umum, hasil penelitian menunjukkan bahwa penambahan rantai alkil ester pada asam galat dapat meningkatkan sitotoksisitasnya terhadap sel HeLa.

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Cervical cancer is a cancer with the highest prevalence in Indonesia. Currently, the treatments of cervical cancer chemotherapy, radiotherapy, and surgery still have side effects and limitations. Gallic acid is a natural compound that could be developed as alternative treatment of cervical cancer. This study aims to determine anticancer activity of gallic acid and its derivatives on the growth of HeLa cell cultures measured by IC50 value. Gallic acid and its derivatives dissolved in phosphate buffered saline PBS , and made into 8 concentrations 0.067 to 8.533 g mL . HeLa cells culture is diluted and added by 10 mL PBS and 1 mL dulbecco 39 s modified eagle medium. HeLa cells viability was tested by MTT assay. Results showed 9 gallic acid derivatives that have greater anticancer activity than gallic acid IC50 3,606 g mL , i.e. propyl gallate IC50 0,0000674 g mL , cis 2 hexenyl gallate IC50 0,19 g mL , 2 hydroxy benzyl gallate IC50 0,40 g mL , amyl gallate IC50 0,62 g mL , sec amyl gallate IC50 0,73 g mL , 4 cis 2 hexenyl oxy gallic acid IC50 1,31 g mL , 4 trans 2 hexenyl oxy gallic acid IC50 1,69 g mL , trans 2 hexenyl gallate IC50 2,79 g mL , and benzyl gallate IC50 2,98 g mL . In general, the results indicate that addition of alkyl ester chain on gallic acid can increase its cytotoxicity against HeLa cells. "

"Latar Belakang: Kanker kolorektal merupakan salah satu kanker dengan prevalensi yang cukup tinggi dan penanganan yang tersedia dapat menyebabkan efek samping buruk. Oleh karena itu, pengobatan alternatif untuk kanker kolorektal perlu dikembangkan. Asam galat telah menunjukkan aksi menghambatan proliferasi sel di berbagai tipe sel kanker termasuk HCT 15 colon cancer cells. Penambahan grup hidrofobik ke asam galat diduga dapat meningkatkan efek anti kanker asam galat. Riset ini dilakukan untuk mengobservasi efek antikanker derivat asam galat, (enam senyawa alkil amida galat hasil sintesis) terhadap sel kolon karsinoma HCT 116. Metode: Menggunakan MTT, enam (6) senyawa alkil amida galat, yaitu: -metil, -etil, -butil, -sek-butil, -ters-butil dan heksil amida galat diuji efek antikankernya terhadap sel HCT 116. Penentuan nilai IC50 dilakukan dengan menggunakan metoda regresi linear untuk analisis data. Hasil uji efek antikanker senyawa turunan alkil amida galat dibandingkan dengan hasil uji efek antikanker asam galat sebagai senyawa awal dan doxorubicin sebagai kontrol positif. Jika dibandingkan dengan asam galat (IC50: 0.05 μg/mL) dan doxorubicin (IC50: 0.001 μg/mL), keenam senyawa turunan alkil amida galat memiliki aktivitas antikanker yang lebih rendah terhadap sel kanker kolon HCT 116. Diantara ke-enam senyawa alkil amida galat hasil sintesis, heksil amida galat dengan IC50 0,07 μg/mL memiliki aktivitas antikanker terbaik. Kesimpulan: Dari hasil studi yang telah dilakukan ini, dapat disimpulkan bahwa heksil amida galat memiliki potensi untuk dikembangkan menjadi agen antikanker kolon.

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Background: Colorectal cancer is one of the most prevalent cancers and its common managements still evoke undesirable side effects. Therefore, there needs to be a development of a safer alternative. Gallic acid has exhibited significant cell proliferation inhibition in a variety of cancer cell lines including HCT 15 colon cancer cells. Addition of hydrophobic groups to gallic acid has been postulated to increase the anti-cancer effects of gallic acid and henceforth this research is conducted to observe the derivatives of gallic acid (six derivative compounds of alkyl amide gallate) on HCT 116 cells. Methods: With the utilization of MTT assay, six synthesized compounds of alkyl amide gallate, namely methyl-, ethyl-, butyl-, sec-butyl-, tert-butyl-, and hexyl amide gallate were measured for their anticancer effect on HCT 116 cells. Determination of IC50 values was carried out by the linear regression method for data analysis. Lastly, results were compared with gallic acid as an original compound and doxorubicin as a positive control. Results: In comparison to gallic acid (IC50: 0.05 μg/mL) and doxorubicin (IC50: 0.001 μg/mL), a lower anticancer effect on colon HCT 116 cells was displayed by all the six- synthesized alkyl amide gallates. Hexyl amide gallate with IC50 value of 0.07 μg/mL shows the strongest anticancer and inhibitory effect on HCT 116 cells. Conclusion: Result of the study indicates that hexyl amide gallate has the potential to undergo further development as a promising anti- colon cancer agent."