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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 :
ABSTRAK
Adenokarsinoma paru merupakan keganasan epitel paru yang paling seringdijumpai baik pada perokok aktif maupun pasif. Seiring bertambah majunyateknologi, sudah ditemukan beberapa terapi untuk adenokarsinoma paru, sepertikemoterapi dan farmakogenetik terhadap gen tertentu. Akan tetapi , efek sampingterapi tersebut cukup besar dan hanya ampuh untuk gen tertentu. Oleh karena itu,diperlukan penelitian baru untuk menemukan alternatif terapi adenokarsinoma paru.Asam galat telah lama dikenal memiliki aktivitas antikanker yang baik. Namun,kadar asam galat yang diperlukan untuk menghambat pertumbuhan sel A549 adenokarsinoma paru masih terhitung besar. Untuk memperbaiki farmakokinetikdan farmakodinamik asam galat, dibuatlah derivat-derivatnya melalui modifikasistruktur, dengan menambahkan gugus alkil ester dan alkil eter pada asam galat.Penelitian ini bertujuan untuk membandingkan dan menemukan IC50 asam galatbeserta derivatnya terhadap sel A549 berbasis konsentrasi. Peneliti menggunakandelapan variasi konsentrasi, berkisar antara 0,26 g/ml hingga 33,33 g/ml. Tiapsumur yang berisi sel A549 diinkubasi bersama asam galat dan derivatnya selama24 jam. Pembacaan absorbansi dilakukan menggunakan MTT assay. Hasilpengolahan data menunjukkan etil galat, isoamil galat, sekunder amil galat, heksilgalat, cis-2-heksenil galat, cis-2-oksi-heksenil galat, dan trans-heksenil galatmemiliki nilai IC50 yang lebih baik dari asam galat. Hasil tersebut menunjukkanbahwa modifikasi gugus karboksil pada asam galat dengan gugus alkil ester rantailurus, rantai bercabang, maupun alkil ester yang memiliki ikatan rangkap berisomergeomeri cis dan trans, dapat memperbaiki sitotoksisitas derivat asam galat terhadapsel adenokarsinoma paru A549.Kata kunci: Derivat asam galat, alkil galat, sel paru A549, sitotoksisitas.

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ABSTRAK
Lung adenocarcinoma is the most common lung epithelial malignancy found inboth active and passive smoker. Recently, chemotherapy and genetic therapy havebeen widely used to treat the lung cancer. Unfortunately, thechemotherapy has theside effects, and the gene therapy can be used only for certain gene involved in thepathogenesis. These facts indicated that the search for new anti lung cancer agentsis needed. Gallic acid has been known to have anticancer activities. However, ittakes a high concentration of gallic acid to inhibit lung adenocarcinoma A549 cells.Therefore, research and development of the new gallic acid derivatives that showhigher cytotoxicity in lower concentration is required. The purpose of this researchis to compare and to find the IC50 value of gallic acid and its derivatives againstlung A549 cells in eight variety of concentrations, ranging of 0,26 g ml to 33,33 g ml. Each lung A549 cells in well is incubated with gallic acid and its derivativesfor 24 hours. The absorbance was read by using MTT assay. The results showedthat ethyl gallate, isoamyl gallate, secondary amyl gallate, hexyl gallate, cis 2 hexenyl gallate, cis 2 oxy hexenyl gallate, and trans hexenyl gallate show lowerIC50 value than gallic acid. These results suggested Thar structure modification oncarboxyl group of gallic acid withalkyl ester group having linear chain andbranched chain, as well as having the double bond with cis or trans configuration,could improve the cytotoxicities of gallic acid derivatives against lung A549 cells.Keyword alkyl gallate, cytotoxicity, gallic acid derivatives, lung A549 cell.