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Abstrak :
[Asam galat merupakan zat polifenol dengan kemampuan sitotoksik. Studi sebelumnya menunjukkan turunan asam galat mampu menghambat pertumbuhan sel kanker. Sampai saat ini, belum banyak studi yang mempelajari turunan alkil ester galat dan turunan metoksi galat terhadap pertumbuhan kanker kolon. Tujuan dari penelitian ini adalah untuk mengetahui aktivitas sitotoksik turunan alkil ester galat dan metoksi galat pada sel kanker kolon. Penelitian ini dilakukan dengan desain eksperimental secara in vitro. Kemampuan sitotoksik asam galat dan turunannya 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 setiap senyawa. Hasil penelitian menunjukkan modifikasi asam galat menjadi senyawa metil galat, propil galat, butil galat, t-butil galat, amil galat, oktil galat dan ketiga turunan metoksi galat tidak menunjukkan peningkatan aktivitas sitotoksik dengan peningkatan konsentrasi yang diuji. Dari semua senyawa yang memiliki kecenderungan menghambat, heptil galat memiliki aktivitas yang paling baik. Disimpulkan, metil galat, propil galat, butil galat, t-butil galat, amil galat, dan oktil galat merupakan turunan alkil galat yang tidak aktif. Etil galat, isobutil galat, isoamil galat, dan heptil galat merupakan turunan alkil galat yang memiliki aktivitas sitotoksik pada sel kanker kolon. Ketiga tur;Gallic acid is a polyphenol with anticancer activity. Previous studies had shown that the derivatives of gallic acid had cytotoxic activity in cancer cell. To date, few studies evaluated the activity of alkyl ester derivatives of gallic acid and methoxy derivatives of gallic acid in colon cancer cell. The objective of this study was to examine the cytotoxic activity of alkyl ester derivatives and methoxy derivatives of gallic acid in colon cancer cell. This study was conducted in in-vitro study in HCT116 colon cancer cell. Cytotoxic activity of gallic acid and its derivatives were evaluated in HCT116 colon cancer cell using MTS (3-(4,5-dimethylthiazol-2-yl)- 5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Data from this experiment was analyzed to obtain IC50 of each compound. The result showed that modification of gallic acid to methyl gallate, propyl gallate, butyl gallat, t-butyl gallate, pentyl gallate, octyl gallate and three methoxy derivatives of gallic acid did not increase cytotoxic activity in all concentrations tested. Among all derivatives of gallic acid, heptyl gallate has the best cytotoxic activity. In conclusion, methyl gallate, propyl gallate, butyl gallate, t-butyl gallate, pentyl gallate, and octyl gallate are alkyl ester derivatives of gallic acid with no cytotoxic activity. Ethyl gallate, isobutyl gallate, isopentyl gallate, and heptyl gallate are active derivatives of gallic acid. All methoxy derivatives of gallic acid do not show any cytotoxic activity in colon cancer cell.;Gallic acid is a polyphenol with anticancer activity. Previous studies had shown that the derivatives of gallic acid had cytotoxic activity in cancer cell. To date, few studies evaluated the activity of alkyl ester derivatives of gallic acid and methoxy derivatives of gallic acid in colon cancer cell. The objective of this study was to examine the cytotoxic activity of alkyl ester derivatives and methoxy derivatives of gallic acid in colon cancer cell. This study was conducted in in-vitro study in HCT116 colon cancer cell. Cytotoxic activity of gallic acid and its derivatives were evaluated in HCT116 colon cancer cell using MTS (3-(4,5-dimethylthiazol-2-yl)- 5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Data from this experiment was analyzed to obtain IC50 of each compound. The result showed that modification of gallic acid to methyl gallate, propyl gallate, butyl gallat, t-butyl gallate, pentyl gallate, octyl gallate and three methoxy derivatives of gallic acid did not increase cytotoxic activity in all concentrations tested. Among all derivatives of gallic acid, heptyl gallate has the best cytotoxic activity. In conclusion, methyl gallate, propyl gallate, butyl gallate, t-butyl gallate, pentyl gallate, and octyl gallate are alkyl ester derivatives of gallic acid with no cytotoxic activity. Ethyl gallate, isobutyl gallate, isopentyl gallate, and heptyl gallate are active derivatives of gallic acid. All methoxy derivatives of gallic acid do not show any cytotoxic activity in colon cancer cell., Gallic acid is a polyphenol with anticancer activity. Previous studies had shown that the derivatives of gallic acid had cytotoxic activity in cancer cell. To date, few studies evaluated the activity of alkyl ester derivatives of gallic acid and methoxy derivatives of gallic acid in colon cancer cell. The objective of this study was to examine the cytotoxic activity of alkyl ester derivatives and methoxy derivatives of gallic acid in colon cancer cell. This study was conducted in in-vitro study in HCT116 colon cancer cell. Cytotoxic activity of gallic acid and its derivatives were evaluated in HCT116 colon cancer cell using MTS (3-(4,5-dimethylthiazol-2-yl)- 5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Data from this experiment was analyzed to obtain IC50 of each compound. The result showed that modification of gallic acid to methyl gallate, propyl gallate, butyl gallat, t-butyl gallate, pentyl gallate, octyl gallate and three methoxy derivatives of gallic acid did not increase cytotoxic activity in all concentrations tested. Among all derivatives of gallic acid, heptyl gallate has the best cytotoxic activity. In conclusion, methyl gallate, propyl gallate, butyl gallate, t-butyl gallate, pentyl gallate, and octyl gallate are alkyl ester derivatives of gallic acid with no cytotoxic activity. Ethyl gallate, isobutyl gallate, isopentyl gallate, and heptyl gallate are active derivatives of gallic acid. All methoxy derivatives of gallic acid do not show any cytotoxic activity in colon cancer cell.]

Abstrak :
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. ...... 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.

Abstrak :
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. ...... 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.

Abstrak :
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. ...... 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

Abstrak :
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.

Abstrak :
Kanker kolorektal merupakan salah satu jenis kanker dengan tingkat prevalensi tinggi. Terapi saat ini berupa tindak bedah, radioterapi dan kemoterapi masih memiliki kelemahan yaitu kekambuhan, metastasis, resistensi, serta beberapa efek samping, sehingga diperlukan penelitian alternatif pengobatan baru. Asam galat telah dikenal memiliki sifat sitotoksik terhadap berbagai sel kanker meskipun belum optimal. Perubahan struktur asam galat diketahui dapat merubah beberapa sifat fisiko kimia sehingga diharapkan dapet meningkatkan sifat sitotoksiknya terhadap kanker kolorektal. Penelitian ini bertujuan untuk menilai sitotoksisitas asam galat dan beberapa turunan alkil ester dan alkil eter terhadap sel kanker kolorektal HCT-116 secara in vitro. Penelitian dilakukan secara eksperimental dengan memberikan perlakuan kultur sel HCT-116 dengan asam galat dan turunannya dengan varian konsentrasi 1,6mg/mL ppm hingga 51,2 mg/mL. Viabilitas kemudian dihitung dengan mengukur nilai absorbansi yang selanjutnya dianalisis untuk memperoleh nilai IC50. Hasil analisis menunjukkan etil galat, salisil galat, propil galat, dialil-galat, amil galat, isoamil galat, sekunder amil galat, dan trans-2-heksinil-galat memiliki nilai IC50 lebih baik dari asam galat. Hal ini menunjukkan bahwa terdapat perbedaan sitotoksisitas asam galat dibandingkan dengan derivat alkil ester dan alkil eter, dimana modifikasi gugus karboksil secara umum dapat memperbaiki sitotoksisitas derivat asam galat terhadap kultur sel HCT-116 secara pada kondisi in-vitro. ...... Colorectal cancer is one of the most prevalent cancer worldwide. Current therapy of colorectal cancer are surgical procedure, radiotherapy, and chemotherapy depends on morbidity of the case. Those therapy still have some limitations such as relapse, metastasis, resistance, and some mild to serious side effects. Gallic acid have been known as cytotoxic agent against various of cancer cells although its effects is not yet optimal. This study aims to measure the in vitro cytotoxicity of alkyl ester derivatives and alkyl eter derivatives compared with gallic acid to colorectal cancer cell HCT 116. This study is an experimental study conducted by treating HCT 116 cells culture with gallic acids and its derivatives at various concentration ranged from 1,6 mg mL to 51,2 mg mL. The viability of cells measured was calculated from absorbance measurement then analyzed to find IC50 values. The results shows etyl gallate, salicyl gallate, propyl gallate, dialyl gallate, amyl gallate, isoamyl gallate, 1 metyl butyl gallate, and trans 2 hexinyl gallate have better IC50 value compared to gallic acid. This results shows that there are difference of cytotoxicity of gallic acid derivatives compared to gallic acid. The modifications of carboxyl groups generally improve cytotoxicity of gallic acids on culture of colorectal cancer cells HCT 116.

Abstrak :
Prevalensi kanker payudara pada tahun 2020 menduduki peringkat pertama di dunia maupun di Indonesia. Pencarian obat antikanker menggunakan metode komputasi dinilai lebih efektif dan selektif. Asam galat dan turunannya (ester dan amida) merupakan senyawa yang memiliki aktivitas biologis seperti antikanker. Tujuan dari studi ini adalah melakukan analisis secara in-siliko dan in-vitro terhadap senyawa turunan asam galat (N-Alkil galamida) sebagai agen apoptosis sel kanker payudara MCF7. Sebelas senyawa N-Alkil galamida yang telah disintesis dilakukan studi in-siliko meliputi, interaksi protein-protein, interaksi obat-protein, analisis ADMET dan pemodelan molekuler. Tiga senyawa terbaik berdasarkan studi in-siliko diuji aktivitas sitotoksisitasnya pada sel MCF7 menggunakan metode MTT dan analisis apoptosis menggunakan annexin V-FITC/PI dengan flow cytometry. Protein target terpilih, yaitu JUN, AKT1, CASP3 dan CASP7. Senyawa N-Oktil galamida, N-Ters-Butil galamida dan N-Isoamil galamida merupakan tiga senyawa terbaik. Senyawa asam galat dan turunannya, secara analisis prediksi ADMET termasuk dalam kategori aman sebagai kandidat obat. Aktivitas sitotoksik ketiga senyawa tersebut dinyatakan dengan nilai IC50 berturut-turut adalah 205.2 ± 0,44 μM, 372.6 ± 4,09 μM, dan 441.7 ± 1,41 μM. Aktivitas apoptosis mencapai 55 hingga 56% dibandingkan dengan kontrol sel. Senyawa N-Oktil galamida, N-Ters-Butil galamida dan N-Isoamil galamida berpotensi sebagai agen apoptosis pada sel kanker payudara MCF7. ......The prevalence of breast cancer in 2020 is ranked first in the world and in Indonesia. Searching for anticancer drugs using computational methods is considered more effective and selective. Gallic acid and its derivatives (esters and amides) are compounds that have biological activities such as anticancer. In this study, N-Alkyl gallamides were analyzed in-vitro and in-silico for their potential to act as apoptotic agents for MCF7 breast cancer cells. In-silico investigations on eleven N-alkyl gallamide compounds, including protein-protein interactions, drug-protein interactions, ADMET analysis, and molecular modelling, have been conducted. The three best compounds based on in-silico studies were tested for cytotoxicity activity on MCF7 cells using the MTT assay and apoptosis analysis using annexin V-FITC/PI with flow cytometry. Selected target proteins, namely JUN, AKT1, CASP3 and CASP7. According to ADMET study, gallic acid and their derivatives are safe as therapeutic candidates. The cytotoxic activities of the three compounds were expressed by IC50 values of 205.2 ± 0.44 μM, 372.6 ± 4.09 μM, and 441.7 ± 1.41 μM, respectively. Apoptotic activity reached 55 to 56% compared to control cells. The N-Octyl gallamide, N-Ters-Butyl gallamide and N-Isoamil gallamide compounds have the potential as apoptotic agents in MCF7 cells.

Abstrak :
Penyakit akibat infeksi bakteri masih menjadi masalah di masyarakat. Salah satu cara untuk mengatasi infeksi tersebut dengan menggunakan antibiotika. Namun, beberapa penelitian melaporkan banyak bakteri telah resisten terhadap antibiotika tertentu. Penelitian ini dilakukan untuk memodifikasi asam risinoleat dan mereaksikannya dengan asam galat untuk menghasilkan produk yang memiliki aktivitas antibakteri. Esterifikasi dilakukan dengan mereaksikan asam risinoleat dan oleat dengan metanol serta adanya penambahan katalis asam sulfat. Metil ester yang terbentuk selanjutnya dioksidasi menggunakan H2O2 30%. Tahap berikutnya adalah reaksi esterifikasi Steglich dengan asam galat. Tahapan reaksi dipantau menggunakan KLT. Produk hasil reaksi dikarakterisasi menggunakan FTIR, NMR dan UV, setelah dilakukan pemurnian dengan kromatografi kolom. Dari tahapan sintesis fenolipid didapatkan produk berupa fenolipid metil risinoleat, fenolipid oksida risinoleat, dan fenolipid oksida metil oleat. Hasil karakterisasi FTIR produk fenolipid didapatkan peningkatan intensitas pita serapan gugus -OH pada rentang bilangan gelombang 3500 cm-1 sampai 3200 cm-1 yang menunjukkan adanya pertambahan gugus -OH. Ciri khas serapan lainnya terdapat serapan -C-O ester aromatik pada bilangan gelombang 1300 cm-1 sampai 1000 cm-1. Selain itu, terdeteksi serapan infra merah gugus C=C aromatik pada bilangan gelombang 1625 cm-1 samapai 1500 cm-1. Produk fenolipid yang diperoleh diuji tosisitasnya terhadap Daphnia magna. Hasil uji menunjukkan bahwa senyawa fenolipid memiliki toksisitas yang sangat tinggi dengan nilai LC50 <100 ppm. Produk hasil sintesis jugdiuji aktivitas antibakterinya terhadap Escherichia coli dan Staphylococcus aureus. Hasil uji tersebut menunjukkan bahwa produk fenolipid mengalami sedikit peningkatan aktivitas dibandingkan senyawa prekursor yang ditunjukkan pada nilai zona inhibisin namun masih tergolong memiliki aktivitas lemah ......Diseases caused by bacterial infections are still a problem in society. One way to treat the infection is to use antibiotics. However, some studies report that many bacteria have become resistant to certain antibiotics. This research was conducted to modify ricinoleic acid and react with gallic acid to produce a product that has antibacterial activity. Esterification was carried out by reacting ricinoleic and oleic acids with methanol with the addition of sulfuric acid as a catalyst. The methyl ester formed was then oxidized using 30% H2O2. The Steglich esterification reaction with gallic acid. The reaction steps were monitored using TLC. The reaction products were characterized using FTIR, NMR, and UV after purification by column chromatography. From the phenolipid synthesis stage, the products obtained were phenolipid methyl ricinoleate, phenolipid ricinoleic oxide, and phenolipid oxide methyl oleate. The results of FTIR characterization of phenolipid products showed an increase in the intensity of the absorption band of the-OH group in the range of wave numbers from 3500 cm-1 to 3200 cm-1, which indicated an increase in the-OH group. Another characteristic of absorption is the absorption of-C-O aromatic esters at wave numbers of 1300 cm-1 to 1000 cm-1. In addition, infrared absorption of the aromatic C=C group was detected at wave numbers from 1625 cm1 to 1500 cm-1. The phenolipid products obtained weres examined for their toxicity against Daphnia magna. The results showed that all phenolipid compounds were categorized as very strong toxicity with an LC50 value of <100 ppm. The synthesized products were also tested for their antibacterial activity against Escherichia coli and Staphylococcus aureus. The test results showed that the phenolipid product experienced a slight increase in activity compared to the precursor compound, indicated by the inhibitory zone value, but was still classified as having weak activity.

Abstrak :
Kanker payudara merupakan salah satu penyakit dengan prevalensi dan mortalitas yang tinggi di Indonesia. Asam galat merupakan senyawa alami yang dapat dikembangkan sebagai agen antikanker, terutama setelah dilakukan modifikasi struktur. Penelitian ini menggunakan asam galat dan 14 senyawa derivat alkil ester dan eter galat masing-masing sebanyak 20 L yang dimasukkan ke lini sel MCF-7 yang sudah ditambahkan 100 L DMEM dan diinkubasi selama 24 jam. Sampel diberikan dalam 8 variasi konsentrasi, yaitu 0,067; 0,133; 0,267; 0,533; 1,067; 2,133; 4,267; dan 8,533 g/mL. Setelah diinkubasi selama 24 jam, dilakukan uji MTT Assay dengan panjang gelombang 490 nm. Data yang diperoleh dianalisis sehingga didapatkan nilai IC50 untuk 15 senyawa yang diujikan. Hasil menunjukkan bahwa trans -2-heksenil galat, asam 4 trans -2-heksenil-oksi galat, cis -2-heksenil galat, amil galat, dan asam 4 cis -2-heksenil-oxy galat memilki nilai IC50 yang lebih rendah daripada asam galat. Dapat disimpulkan bah.wa derivat asam galat yang dimodifikasi dengan gugus alkil ester lima karbon rantai lurus, yaitu amil galat, dan derivat asam galat yang memiliki gugus alkil ester berikatan rangkap dengan konfigurasi cis atau trans, yaitu asam 4 trans -2-heksenil-oksi galat, trans -2-heksenil galat, cis -2-heksenil galat, dan asam 4 cis -2-heksenil-oxy galat, menunjukkan peningkatan aktivitas antikanker terhadap lini sel MCF-7 dibandingkan asam galat, sehingga berpotensi dikembangkan sebagai agen antikanker payudara.

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Breast cancer is one of the diseases which has high prevalence and mortality in Indonesia. Gallic acid is a natural compound which can be developed as an anticancer agent, especially after undergone structural modification. The experiment was done by adding 20 L gallic acid and 14 of its derivates alkyl ester and eter of gallic acid samples to MCF 7 breast cancer cell mixed with 100 L DMEM and then incubated for 24 hours. The samples was given in 8 concentration 0,067 0,133 0,267 0,533 1,067 2,133 4,267 and 8,533 g mL. After incubated for another 24 hours, MTT Assay 490 nm was executed. The data was then analyzed to get IC50 values for each compound. The result showed that asam 4 trans 2 heksenil oksi galat, trans 2 heksenil galat, cis 2 heksenil galat, amil galat, and asam 4 cis 2 heksenil oxy galat each had lower IC50 than gallic acid. It can be concluded that gallic acid derivates modificated by 5 carbon straight chain alkyl ester amil galat and have double bond with cis trans configuration asam 4 trans 2 heksenil oksi galat, trans 2 heksenil galat, cis 2 heksenil galat, and asam 4 cis 2 heksenil oxy galat shows higher anticancer activity to MCF 7 breast cancer cell compared to gallic acid, so they can be developed as anticancer agent for breast cancer.

Abstrak :
ABSTRAK
Infeksi dengue (DENV) merupakan salah satu penyakit endemik di daerah tropis dan subtropis yang disebabkan oleh virus dengue melalui vektor nyamuk dari genus Aedes, khususnya oleh Aedes aegypti dan Aedes albopictus. Hingga saat ini belum ada pengobatan yang efektif untuk mengatasi infeksi dengue. Salah satu pengobatan baru yang dibutuhkan bersifat antivirus yang dapat menghambat aktivitas enzim yang berperan dalam replikasi di dalam tubuh. Pada penelitian ini dilakukan pengujian dari senyawa asam galat dan enam turunannya (benzil-, propil, dialil-, alil-, etil-, dan salisil galat) secara in vitro pada sel Huh7it-1 dengan DENV2 dan secara in silico dengan docking protein-ligan terhadap strain NGC dan 251 sekuens NS5 pada GenBank (NS5 konsensus). Salisil galat merupakan kandidat paling potensial secara in vitro (IC50: 12,18 μg/ mL, CC50: 259,35 μg/ mL, SI: 21,30) dan in silico (S: -16,793 kkal/ mol, pKi 3,344 μM). Propil galat dan etil galat ditemukan potensial secara in vitro (untuk propil galat, IC50: 13,19 μg/ mL, CC50: 241,85 μg/ mL, SI: 18,33; untuk etil galat, IC50: 14,39 μg/ mL, CC50: 185,60 μg/ mL, SI: 7,24), namun secara in silico paling rendah nilainya (untuk propil galat, nilai S: -11,908 kkal/mol, pKi 5,771 μM; untuk etil galat, nilai S: -5,513 kkal/mol, pKi 4,974 μM). Melalui docking pada sekuens konsesus NS5 diketahui, setiap jenis asam galat potensial tersebut dapat berikatan dengan masing-masing GLU715, LYS668, ASN701, THR584; ARG472, ASP663, ARG207; dan LYS139, ARG207. Secara keseluruhan, turunan asam galat hasil modifikasi memberikan hasil lebih baik dibandingkan dengan senyawa aslinya

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ABSTRACT
Dengue infection (DENV) is an endemic disease in tropical and subtropical regions caused by dengue virus that is transmitted by mosquitos of Aedes aegypti and Aedes albopictus. Currently, there is no effective treatment to overcome dengue infection. As alternative, a new approach of drug is needed by targeting inhibition of enzyme activity that responsible for viral replication. In this research examined synthetic gallic acid and its six derivatives (benzyl-, propyl, diallyl-, allyl-, ethyl-, and salicyl gallate) through in vitro in Huh7it-1 with DENV2 and in silico with protein-ligand docking against 251 sequences NS5 in GenBank. Salicyl gallate was the best candidate in in vitro analysis (IC50: 12,18 μg/ mL, CC50: 259,35 μg/ mL, SI: 21,30) and in in silico analysis (S: -16,739 kkal/ mol, pKi 3,344 μM). Propyl- and ethyl gallate were showed potential in in vitro (for propyl gallate, IC50: 13,19 μg/ mL, CC50: 241,85 μg/ mL, SI: 18,33; for ethyl gallate, IC50: 14,39 μg/ mL, CC50: 185,60 μg/ mL, SI: 7,24), however showed lowest scoring in in silico (for propyl gallate, S score: -11,908 kkal/mol, pKi 5,771μM; for ethyl gallate, S score: -5,513 kkal/mol, pKi 4,974μM). Using docking, each of potential gallic acid types above was able to bind to GLU715, LYS668, ASN701, THR584; ARG472, ASP663, ARG207; dan LYS139, ARG207. Overall, derivatives gallic acid modified was showed better result rather than original compound