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SINTESIS ANALOG UK-3A : 6-HIDROKSI-N-FENILNIKOTINAMIDA DAN 6-HIDROKSI-N- FENILPIKOLINAMIDA DAN UJI SITOTOKSISITAS SECARA IN VITRO TERHADAPSEL KANKER MURINE LEUKEMIA P388 Febriyanti, Lilis; Hanafi, Muhammad; Hayun, Hayun
Jurnal Farmasi Indonesia Vol 10, No 1 (2018)
Publisher : Indonesian Research Gateway

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.35617/jfi.v10i1.583

The Novel compound of analog UK-3A defined as HF-1 (6-hydroxy-N-phenylnicotinamide) and HF-2 (6-hydroxy-N-phenylpicolinamide)was successfully synthesized by amidation reaction of aromatic carboxilyc acids and primary amine by adding the activator of DCC (dicyclohexylcarbodiimide), catalyst DMAP (4-dimethyl aminopyridine, and DMSO (dimethyl sulfoxide) as the solvent. Reaction run for 24 hours in 55oC. Result shows yield of HF-1 as much as 52%, and for HF-2 is 16%. The analogue compounds structure of UK-3A were characterized by spectrophotometer FT-IR, LCMS, and NMR. Citotoxicity assay against Murine Leukemia cells of HF-1 and HF-2 by MTT (3-(4,5-dimethylltiazo-2-yl-) 2,5-diphenyltetrazolium bromide) assay. The result of bioassay showed IC50(inhibitory concentration)value 71 µg/mL and 63 µg/mL for HF-1 and HF-2 respectively. It informed that the analogue compounds have lower activity than UK-3A compound which has IC50 value 38 µg/mL.

SINTESIS ANALOG UK-3A : 6-HIDROKSI-N-FENILNIKOTINAMIDA DAN 6-HIDROKSI-N- FENILPIKOLINAMIDA DAN UJI SITOTOKSISITAS SECARA IN VITRO TERHADAPSEL KANKER MURINE LEUKEMIA P388 Febriyanti, Lilis; Hanafi, Muhammad; Hayun, Hayun
Jurnal Farmasi Indonesia Vol 10, No 1 (2018)
Publisher : Jurnal Farmasi Indonesia

The Novel compound of analog UK-3A defined as HF-1 (6-hydroxy-N-phenylnicotinamide) and HF-2 (6-hydroxy-N-phenylpicolinamide)was successfully synthesized by amidation reaction of aromatic carboxilyc acids and primary amine by adding the activator of DCC (dicyclohexylcarbodiimide), catalyst DMAP (4-dimethyl aminopyridine, and DMSO (dimethyl sulfoxide) as the solvent. Reaction run for 24 hours in 55oC. Result shows yield of HF-1 as much as 52%, and for HF-2 is 16%. The analogue compounds structure of UK-3A were characterized by spectrophotometer FT-IR, LCMS, and NMR. Citotoxicity assay against Murine Leukemia cells of HF-1 and HF-2 by MTT (3-(4,5-dimethylltiazo-2-yl-) 2,5-diphenyltetrazolium bromide) assay. The result of bioassay showed IC50(inhibitory concentration)value 71 Âµg/mL and 63 Âµg/mL for HF-1 and HF-2 respectively. It informed that the analogue compounds have lower activity than UK-3A compound which has IC50 value 38 Âµg/mL.

Penetapan Kadar Triprolidina Hidroklorida dan Pseudoefedrina Hidroklorida Dalam Tablet Anti Influenza Secara Spektrofotometri Derivatif Hayun, Hayun; Harianto, Harianto; Yenti, Yenti
Majalah Ilmu Kefarmasian Vol. 3, No. 2
Publisher : UI Scholars Hub

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The determination of triprolidine hydrochloride and pseudoephedrine hydrochloride in anti influenza tablet has been performed using derivative spectrophotometry method. Triprolidine hydrochloride and pseudoephedrine hydrochloride were determined by measuring the first derivative ratio amplitudes, at 227,6 nm (zero crossing for pseudoephedrine hydrochloride) and at 230,0 nm (zero crossing for triprolidine hydrochloride) respectively. The linear calibration graphs were obtained for 5-50 ppm of triprolidine hydrochloride and for 100-800 ppm of pseudoephedrine hydrochloride. The results showed that the method is rapid, simple and can be applied successfully to assay simultaneously of two components in tablet preparation.

Penetapan Kadar Triprolidina Hidroklorida dan Pseudoefedrina Hidroklorida Dalam Sediaan Sirup Obat Influenza Secara Kromatografi Lapis Tipis Densitometri Hayun, Hayun; Leswara, Nelly D.; Masrijal, Camelia D.P.
Majalah Ilmu Kefarmasian
Publisher : UI Scholars Hub

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The determination of pseudoephedrine hydrochloride and triprolidine hydro-chloride in influenza syrup medicine has been performed using TLC densitometric method. Pseudoephedrine hydrochloride and triprolidine hydrochloride were extracted using chloroform at pH 12 from the syrup, and separated using HPTLC silica Kie-selguhr glass plates 60 F 254, 20x10 cm2 as stationary phase, and a mixture of methanol, ammonia and chloroform (40:2:30) as mobile phase. The plates were ana-lyzed using Camag TLC Scanner 3 with UV-detector at 257 nm for pseudoephe-drine hydrochloride and at 290 nm for triprolidine hydrochloride. The results showed that the linearity, limit of detection, and limit of quantitation of the method for pseudoephedrine hydrochloride were 0.9999, 0.0064 µg, and 0.2124 µg respectively; while for triprolidine hydrochloride were 0.9999, 0.0076 µg, and 0.0254 µg respec-tively. The coefficient of variance (CV) of repeatability for the two substances were less than 2.0%; and the recovery values for pseudoepherine hydrochloride and triprolidine hydrochloride were 99.98 + 1.05% and 99.73 + 1,54% respectively. The result showed that the samples analysed contained pseudoephedrine hydrochloride 94.36% of the labeled ammount, and triprolidine hydrochloride 94.44% of the la-beled ammount.

Sintesis dan Uji Aktivitas Antibakteri N,N'-Divanilidenaetilendiamina Hayun, Hayun; Munim, Abdul; Hariria, Dini; Aunillah, Ulfah
Majalah Ilmu Kefarmasian
Publisher : UI Scholars Hub

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The study of synthesis and antibacterial activity test of N,N'-divanilidene-ethylendiamine was performed. N,N'-divanilidene-ethylendiamine was synthesized by reacting vaniline with ethylendiamine in ethanol pH 1, and the structure was elucidated based on IR and 1H-NMR spectra data. Antibacterial activity test was performed using minimum inhibition concentration method (MIC) against Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 25922. The results showed that N,N'-divanilidene-ethylendiamine has antibacterial activity with MIC of 2 mg/mL against the the bacteria.

Penetapan Kadar Sakarin, Asam Benzoat, Asam Sorbat, Kofeina, Dan Aspartam Di Dalam Beberapa Minuman Ringan Bersoda Secara Kromatografi Cair Kinerja Tinggi Hayun, Hayun; Harahap, Yahdiana; Azizah, Citra Nur
Majalah Ilmu Kefarmasian Vol. 1, No. 3
Publisher : UI Scholars Hub

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As the food and beverages industry grows in Indonesia, there also has been an increase in the soft-drinks production in the society. There are elements often added into the drinks; such as caffeine, artifical sweetener and preservatives,which the content should be monitored. Because, if they are over-used, they will be hazardous to health. The purpose of this research is to obtain the optimum analysis condition for determining the content of saccharin, aspartame, benzoic acid, sorbic acid and caffeine, which are in the soft-drinks, using the reversed phase High-Performance- Liquid-Chromatography (HPLC). In this study, the condition used are Latek 18 column (15 cm x 4.0 mm), mobile phase as a mixture of acetonitrile and acetat buffer pH 5(5:95), flow rate 1,0 ml/minutes and detected by a 254 nm length-wave. The detection limit discovered by this method are for saccharin, benzoic acid, sorbic acid, caffeine and aspartame, respectively, are 0,2 ppm; 0,2 ppm; 0,007 ppm; 0,142 ppm; and 6,5 ppm. Whereas, the quantitative limit for saccharin, benzoic acid, sor- bic acid, caffeine and aspartame, respectively, are 0,689 ppm; 0,852 ppm; 0,027 ppm; 0,452 ppm; 25,2 ppm. The calibration curve ranged between 1-60 ppm for saccharin and benzoid acid, 1-40 ppm for caffeine, 0.05-2 ppm for sorbic acid, and 30-100 ppm for aspartame. The investigation has been done for five (5) brands od soft-drinks. The analysis results are sample A contains caffeine 96,66 ppm, sample B contains saccharin 112,13 ppm, benzoic acid 206,81 ppm, and caffeine 130,63 ppm. Sample C contains benzoic acid 10,83 ppm and caffeine 97,66 ppm. Sample D con- tains benzoic acid 163,78 ppm, caffeine 101,52 ppm, and aspartame 231,20 ppm. The amounts of saccharin, benzoic acid, caffeine, and aspartame which has been found in the sample, do not exceed the tolerance limit of usage, whereas the amount of benzoic acid which has been found in sample B exceed the tolerance limit of usage.

Percobaan Sintesis 4-(4-Metoksibenzilidena) 2-metiloksazol-5-on dari Asetilglisin dan 4-Metoksibenzaldehid Arrahman, Arif; Hayun, Hayun; Yanuar, Arry
Majalah Ilmu Kefarmasian Vol. 8, No. 2
Publisher : UI Scholars Hub

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Compound 4-(4-methoxybenzylidene)-2-methyloxazole-5-one was one of oxazolone moety derivative. Oxazolones had several different pharmacological activity depend on substituent which was bonded to oxazolone ring. Oxazolones was an important precursor for synthesizing several compounds which had pharmacological activity. For that reason, experiment to synthesize 4-(4-methoxybenzylidene)-2-methyloxazole-5-one from acetyl- glicine and 4-methoxybenzaldehyde as an oxazolone derivative become necessary. Com- pound 4-(4-methoxybenzylidene)-2-methyloxazole-5-one was synthesized over two step of reaction. First step was reacted glycine with acetic anhydride in acidic environment yielded acetylglycine. Second step was reacted acetylglycine with 4-methoxybenzaldehyde yielded 4-(4-methoxybenzylidene)-2-methyloxazole-5-one. The product, which was collected in every step, was purified by washing and recrystalization then the purification to be tested by examining melting range and thin layer chromatography. The compound was eluci- dated by using infrared spectrophotometry and 1H-NMR spectrophotometry. Synthesis of 4-(4-methoxybenzylidene)-2-methyloxazole-5-one yielded rendement over 0,54%. The interpretation of infrared spectrum indicated that the compound which synthesized was different from the former compound but the interpretation of 1H-NMR spectrum indicated that the compound could not be ascertained as 4-(4-methoxybenzylidene)-2-methyloxa- zole-5-one because of there were impurities.

Analisis Adduct DNA Setelah Pemberian Natrium Nitrit dan Dimetilamin Secara Berulang Pada Tikus Meilianti, Sherly; Harahap, Yahdiana; Hayun, Hayun
Majalah Ilmu Kefarmasian Vol. 8, No. 1
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Nitrosodimethylamine is a carcinogenic compound which can be formed from the reaction of nitrite and dimethylamine that is found in food. Nitrosodimethylamineis activated in liver and alkylates the DNA base and producing a DNA adductssuch as O6-methylguanine and N7-methylguanine that have a role incarcinogenesis. In this research, DNA was isolated from rat’s blood which waspreviously given nitrosodimethylamine’s precursor, sodium nitrite anddimethylamine. DNA adducts can be obtained from hydrolysis in hydrochloricacid 0.1 N for 30 minutes at 7000C. Then the adducts were analyzed using High Performance Liquid Chromatography (HPLC), with a strong cation exchangecolumn (Supelcosil LC-SCX, 5 μm, 250 x 4.6 mm), mobile phase consisting ofammonium phosphate with a final concentration of 40 mM, pH 3.00, flow rate 1.5mL/minute, column temperature 30oC and detected at exitation wavelength 286 nm and emission wavelength 366 nm. This method gave an acceptable validation result according to accuracy and precicion test results that fulfill the requirementand linear calibration curve with a quantitation limit of 22,5403 ng/mL. Rats were divided into six groups that two groups were given nitrosodimethylamine aspositive control, three groups were given prekursor, and the other was normalcontrol. Blood samples were collected in 1,2 and 4 hour after last induced. Aftergiving sodium nitrite 110 mg/kg bw and dimethylamine (1:5) orally for a week,N7-methylguanine and O6-methylguanine had not been detected in rat’s blood.

Evaluasi Aktivitas Antioksidan Senyawa 4-[(E)-2-(4-okso-3-fenilkuinazolin-2-il)etenil]-benzensulfonamida dan Analognya Jatmika, Catur; Maggadani, Baitha Palanggatan; Hayun, Hayun
Pharmaceutical Sciences and Research
Publisher : UI Scholars Hub

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Quinazolinone derivative compounds exhibit a broad spectrum of biological activity, including antioxidant. Quinazolinone derivative compound 4-[(E)-2-(4-oxo-3-phenyl quinazolin-2-yl)ethenyl]-benzensulfonamida and its analogs (2a-f) have been synthesized and demonstrated its activity as a selective inhibitor of cyclooxygenase-2. The aim of this research was to evaluate the antioxidant activity of compound 4-[(E) -2-(4-oxo-3-fenilkuinazolin-2-yl)ethenyl]-benzensulfonamida and its analogs with DPPH radical scavenging method, ferric reducing activity potential (FRAP), and phosphomolybdenum method. The experiment revealed that the % inhibition and antioxidant capacity of compound 2c, 2e and 2f were higher compared to compound 2a, 2b and 2d. The DPPH radical scavenging analysis found that the % inhibition of compound 2c, 2e and 2f at high concentration of compound solution (1000 µg/mL) were 4.8 %, 3.46 %, and 3.68 %, respectively. While the total antioxidant capacity of compound 2c, 2e and 2f were recorded 37.93, 33.4, and 46.3 µg ascorbic acid equivalence/mg of compound, respectively. However the antioxidant activity of all synthesized compounds (2a-f) were lower than the standard ascorbic acid.

Penetapan Kadar Hidrokortison Asetat dalam Sediaan Krim Mengandung Pengawet Nipagin secara Spektrofotometri Derivatif Orde Pertama Hayun, Hayun; Leswara, Nelly D.; Zarkasih, Lutfhi
Pharmaceutical Sciences and Research
Publisher : UI Scholars Hub

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The simple and rapid spectrophotometric methods were developed for analysis of hydrocortisone acetate in cream pharmaceutical formulations containing nipagin as preservative. Concentration of hydrocortisone acetate was determined by measuring the first derivative absorption (ratio amplitudes) at 257.0 nm (zero crossing for nipagin). The calibration graphs were linear over the range of 4.0-40.0 ppm of hydrocortisone acetate (r= 0.9999). The limit of detection (LOD) and the limit of quantitation (LOQ) were found to be 0.9617 ppm and 3.2050 ppm, respectively. This method had good precision (repeatability and intermediate precision) with RSD < 2.0% where as the means of the recovery data (accuracy) were 102.03±0.14% and 100.23±0.69% for hydrocortisone acetate cream 1% and 2.5%, respectively. The proposed method was applied for the determination of hydrocortisone acetate in three out of four commercial cream formulations samples and the results of label claim were 102.93±0.22%, 108.48±0.19% and 106.67±0.35% for sample A, B and D, respectively. The result of brand C analysis showed to contain more than 110.0% of the labeled amount of hydrocortisone acetate, indicated there was additive other than nipagin in the cream basis to interfer with the hydrocortisone acetate measurements.

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