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"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."

"[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.]"

"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."

"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."

"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."

"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 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."

"Latar belakang: Imunotoksin adalah salah satu bentuk terapi target pada kanker berupa konjugasi antara antibodi monoklonal dengan molekul toksin Antibodi menghantarkan toksin ke sel kanker dan menyebabkan kematian sel. Pada penelitian ini, toksin mitokondria asam bongkrek dikonjugasikan dengan antibodi anti-CD3 menjadi senyawa konjugat asam bongkrek-antibodi anti-CD3, dan digunakan SMDT sebagai model uji spesifisitas. Tujuan: Penelitian ini bertujuan untuk mensintesis senyawa konjugat antara asam bongkrek dengan antibodi monoklonal anti-CD3 dan uji spesifisitas secara in-vitro pada SMDT. Metode: Uji in-silico dilakukan untuk memprediksi situs konjugasi. Sintesis imunotoksin asam bongkrek-antibodi anti-CD3 dilakukan secara kimiawi menggunakan penaut EDC.HCl/Sulfo-NHS. SMDT digunakan sebagai model uji spesifisitas. Hasil: Molecular docking menunjukkan bahwa asam amino lisin, asparagin dan glutamin dari Fc IgG2a berinteraksi secara kovalen dengan gugus karboksilat dari asam bongkrek. Serapan senyawa konjugat pada panjang gelombang 280 nm dan 260 nm menunjukkan adanya serapan protein dan asam bongkrek. Inkubasi SMDT dengan senyawa konjugat menunjukkan jumlah sel hidup yang lebih tinggi dibandingkan dengan inkubasi asam bongkrek (p<0.05) ataupun dengan antibodi anti-CD3 (p<0.05). Kesimpulan: Uji in-silico menunjukkan adanya interaksi antara gugus karboksilat dari asam bongkrek dengan gugus amina primer dari imunoglobulin. Uji in-vitro senyawa konjugat menunjukkan efek sitotoksik lebih rendah dibandingkan dengan asam bongkrek maupun antibodi anti-CD3.

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Background: Immunotoxin is a form of targeted therapy in cancer in the form of conjugation between monoclonal antibodies and toxins. Antibodies will deliver toxins to cancer cells and cause cell death. In this study, mitochondrial toxin bongkrekic acid was conjugated with anti-CD3 monoclonal antibodies into anti-CD3 monoclonal antibody-bongkrekic acid conjugate, and PBMC was used as a specificity test model.

Objective: This study aims to synthesize conjugate between bongkrekic acid with anti-CD3 monoclonal antibodies and in-vitro specificity tests on PBMC. Method: An in-silico test was performed to predict the conjugation site. The synthesis of anti-CD3 monoclonal antibody-bongkrekic acid was carried out chemically using EDC.HCl/Sulfo-NHS crosslinker. PBMC was used as a specificity test model.

Results: Molecular docking showed that the amino acids lysine, asparagine, and glutamine from Fc IgG2a interact covalently with the carboxylic group of bongkrekic acid. The spectroscopy measurement of conjugate compounds at wavelengths of 280 nm and 260 nm indicates the absorption of proteins and bongkrekic acid. PBMC incubation with conjugate compounds showed a higher number of living cells compared to bongkrekic acid (p<0.05) or with anti-CD3 antibodies (p < 0.05).

Conclusion: In-silico studies show an interaction between the carboxylic group of bongkrekic acid and the primary amine group of immunoglobulin. In-vitro assays of conjugate compounds showed lower cytotoxic effects compared to bongkrekic acid and anti-CD3 antibodies."

"ABSTRAKEucheuma cottonii memiliki aktivitas antikanker yang cukup aktif. Nilai IC50 terendah dimiliki oleh ekstrak etil asetat dari Eucheuma spinosum. Sebagai kesimpulan, ekstrak etil asetat dari Eucheuma spinosum memiliki potensi sebagai agen antikanker yang paling poten.

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ABSTRACTSeaweed macroalgae, as marine natural products has showed a potent anticancer activity. Therefore, in this research, we analyse the phytochemical content of Eucheuma sp. that came from Labuhan Haji Beach, Nusa Tenggara Barat and its anticancer activity to further develop it as anticancer agent. Method. Hexane, ethyl acetate, ethanol, and chloroform extracts of seaweed were tested using Thin Layer Chromatography to the amount of metabolite content of the extract. Finally, the anticancer activity was tested using MTT Assay. The result of this test is expressed in percentage inhibition and IC50 value. Results. Phytochemical analysis showed almost all extracts of Eucheuma spinosum contain flavonoid and triterpenoid. Thin Layer Chromatography showed ethyl acetate and hexane extract have three similar Rf factors that can show that these extracts contain similar metabolites. MTT assays showed that Eucheuma sp. has moderately active anticancer activity. Conclusion. The results of this study show that Eucheuma sp. has moderately active anticancer activity. Ethyl acetate extract of Eucheuma spinosum has the smallest value of IC50. To sum up, ethyl acetate extract of Eucheuma spionosum showed the strongest antiproliferative activity, so this can be one of the most potential anticancer drug."

"Analog Kurkumin Indazol merupakan senyawa analog berpotensi dikembangkan sebagai antikanker. Penelitian ini bertujuan untuk memperoleh senyawa baru analog kurkumin tetrahidro-indazol yang mempunyai akivitas penghambatan antikanker yang selektif. Penelitian diawali skrining in silico 186 senyawa disain didasarkan pada penapisan model farmakofor dan terpilih 14 senyawa, dilanjutkan penambatan molekular menghasilkan 10 senyawa hit. Kemudian dilakukan sintesis dengan reaksi kondensasi Clasein-Schmidth, dihasilkan enam analog indazole baru dari kurkumin dan dievaluasi aktivitas sitotoksiknya menggunakan uji proliferasi metil tiazolil tetrazolium terhadap sel kanker MCF-7, HeLa, WiDr, dan Vero. Struktur senyawa dikarakterisasi dengan FTIR, NMR, dan spektral massa. Hasil penelitian menunjukkan bahwa senyawa yang disintesis lebih aktif terhadap sel WiDr dibandingkan dengan sel MCF-7 dan HeLa. Aktivitas sitotoksik senyawa 3b, 3c, 3d, 5a terhadap sel WiDr lebih aktif dibandingkan kurkumin dan tamoxifen. Evaluasi lebih lanjut terhadap sel Vero (sel normal) untuk menentukan selektivitasnya menunjukkan beberapa senyawa hasil sintesis lebih selektif (nilai IS > 2) dibandingkan tamoxifen dan doksorubisin (nilai SI < 2,00). Tiga senyawa (3a, 3b, dan 3c) menunjukkan IS tinggi terhadap sel WiDr yaitu 3,74, 5,27, dan 4,39. Di antara senyawa yang disintesis, 3b menunjukkan aktivitas sitotoksik tertinggi, terutama terhadap garis sel WiDr (IC50 = 27,20 M) dengan selektivitas yang sangat baik (SI = 5,27).

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Indazole Analogs of Curcumin is an analog compound that has the potential to be developed as an anticancer. This study aims to obtain a new compound analogue of curcumin tetrahydro-indole which has selective anticancer inhibitory activity. The research began with the design of the curcumin analog compound tetrahydro-indazole in silico based on a pharmacophore model and 14 compounds were selected, then continued molecular docking to produce 10 hit compounds. Then the synthesis was carried out using the Clasein-Schmidth condensation reaction and produced a series of six novel indazole analogs of curcumin and evaluated their cytotoxic activity against MCF-7, HeLa, WiDr, and Vero cells. The structure of the compound was characterized by FTIR, NMR, and mass spectral. The results showed that the synthesized compound was more active against WiDr cells than MCF-7 and HeLa cells. The cytotoxic activity of compounds 3b, 3c, 3d, 5a against WiDr cells was more active than curcumin and tamoxifen. Further evaluation of Vero cells to determine their selectivity showed that some of the compounds synthesized were more selective (SI value>2) than tamoxifen and doxorubicin. Three compounds (3a, 3b, and 3c) showed high SI against WiDr cells, namely 3.74, 5.27, and 4.39. Among the synthesized compounds, 3b showed the highest cytotoxic activity, especially against the WiDr cell line (IC50 = 27.20 M) with excellent selectivity (SI = 5.27)."