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Sintesis 1-(4-metoksibenzoiloksimetil)-5-fluorourasil sebagai Agen Antikanker . Ifada; Ayik Rosita Puspaningtyas1; Ika Oktavianawati; Yuni Retnaningtyas; Nia Kristiningrum
Pustaka Kesehatan Vol 1 No 1 (2013)
Publisher : UPT Percetakan dan Penerbitan Universitas Jember

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Abstract

A new compound from 5-fluorouracil (5-FU) derivatives, 1-(4-methoxybenzoyloxymethyl)-5-fluorouracil has been synthesized in a two steps reaction, alkylation (5-FU and formaldehyde to form 1-hydroxymethyl-5-fluorouracil) and esterification (1-hydroxymethyl-5-fluorouracil and 4-methoxybenzoylchloride to form 1-(4-methoxybenzoyloxymethyl)-5-fluorouracil). Reaction product purified by chromatography column, the product has been characteryzed for physical apperance is a yellowish white, crystal and melting range 168-169OC. Based on the FTIR and 1H-NMR spectra, it showed that the purified product does not contain a single compound. This fact is supported by Thin Layer Chromatography (TLC) result showing two spots for the pressure of 1-(4-methoxybenzoyloxymethyl)-5-fluorouracil and 4-methoxybenzoate acid. Keywords: 5-fluorouracil derivates, anticancer, 1-(4-methoxybenzoyloxymethyl)-5-fluorouracil, benzoylation.
SINTESIS DAN UJI AKTIVITAS ANTIBAKTERI SENYAWA TURUNAN KALKON PADA STRAIN BAKTERI Bacillus subtilis DAN Escherichia coli Ayik Rosita Puspaningtyas
STOMATOGNATIC - Jurnal Kedokteran Gigi Vol 8 No 3 (2011)
Publisher : Fakultas Kedokteran Gigi Universitas Jember

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Abstract

Disease caused by bacteria still have a high prevalence in Indonesia, both in urban and rural areas. Currently the treatment of diseases caused by bacteria carried by many antibiotics, whereas in reality antibacterial drugs like antibiotics are now causing a lot of resistance in some people. Because of this we effort to develop antimicrobial agents, a series of chalcones were 1-(4-Bromo-phenyl) -3-(4-methoxy-phenyl)-2-propen-1-on and 1-(4- Bromo-phenyl)-3-(3,4-dimethoxy-phenyl)-2-propen-1-on compounds.These compounds are synthesized on the basis of QSAR (Quantitative Structure Activity Relationships) using lipophilic, steric, and electronic parameters. Compound 1-(4-Bromo-fenill)-3-(4-methoxy-phenyl)-2-propen-1-on and 1-(4-Bromo-phenyl)-3-(3,4-dimethoxy-phenyl)-2-propen-1-on is made from raw materials 4-bromo-asetophenone and 4-Methoxy benzaldehide/3,4-dimethoxy benzaldehide usual Claisen-Schmidt condensation method of mixing for overnight 24 hours then be recrystallized to obtain a pure crystalline chalcones analog compounds. After the synthesis, compounds were characterized by organoleptic and melting point test. The results showed that a white color, smells aromatic, and needle crystals. The synthesized compounds were characterized by means of their 1H-NMR spectral data. All the compounds were tested for their antibacterial activities by the hole plate method.
MOLEKULAR DOCKING DENGAN METODE MOLEGRO VIRTUAL DOCKER TURUNAN KALKON SEBAGAI ANTIMIKROBA Ayik Rosita Puspaningtyas
STOMATOGNATIC - Jurnal Kedokteran Gigi Vol 9 No 1 (2012)
Publisher : Fakultas Kedokteran Gigi Universitas Jember

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Abstract

We have done docking molecule on chalcones derivatives that bind to antibacterial gram-positive (Bacillus subtilis ) and negative (Escherichia coli) compared with chalcones derivatives and chloramphenicol antibiotic. Chalcone derivatives compounds have been synthesized by varying the methoxy groups in chalcone structure. The results showed that chalcone derivatives have antibacterial activity in inhibition of Bacillus subtilis and Escherichia coli that were better than lead compound (chalcone) and chloramphenicol. The results can be viewed from Moldock and Rerank score that has lower energy. The results differ from in vitro study in 1 - (4-Bromo-phenyl) -3 - (4-phenyl-methoxy)-2-propen-1-on and 1-(4-Bromo-phenyl)-3-(3.4-dimethoxy-phenyl)-2-propen-1-on compounds as antibacterial activity in gram-negative bacteria (E. coli) and gram-positive bacteria (Bacillus subtilis) were smaller activity than chloramphenicol. Because of derivatives chalcones was very large lipophylic value (log P>2), these will decrease the activity. In addition, if these were viewed hydrogen bonds on Molegro Virtual Docker between chalcone derivatives and binding of bacterial amino acids, ie Lys 411, Ser 299, Ser 52, and Thr 412 in Bacillus subtilis and Tyr 136 and Tyr 52 in Escherichia coli provide less harmonious interaction within complex binding than that of chloramphenicol.
STUDI FITOKIMIA IRVINGIA MALAYANA SEBAGAI ANTIMALARIA DARI HUTAN MERU BETIRI DALAM RANGKA DRUG DISCOVERY Ayik Rosita Puspaningtyas
Jurnal Ilmiah Farmasi Farmasyifa Vol 1, No 2 (2018)
Publisher : Universitas Islam Bandung

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.29313/jiff.v1i2.3340

Abstract

Meru Betiri forest in Jember contains a lot of medicinal plants. Irvingia malayana (Pauh Kijang), which is one of the medicinal plants found, has been proven as an antimalarial. However, phytochemical and antimalarial studies of Irvingia malayana have never been carried out. This study was conducted for an antimalarial Drug Discovery through phytochemical study by isolating the roots, stems, and leaves of Irvingia malayana. From the analysis using FTIR, H-NMR, and GC-MS, it was concluded that the compound in the ethyl acetate extract of Irvingia malayana stem was terpenoids that was included in silymarin group as well as other plants in the genus Irvingia. The melting point of Irvingia malayana isolate was 120-121oC with white crystals. Statistical result of in vivo study showed that each group was significantly different. On day 4 after administration, IC50 showed was 11,827 mg/kgBW and day 3 was 6,927 mg/kgBW. Therefore, 3 days is the maximum duration of administration in reducing plasmodium and shows the most excellent activity as antimalarial. In in vitro study, IC50 of Irvingia malayana (62.855 ug/ml) has weak activity of antiplasmodium compared to chloroquine positive controls containing IC50 (1,114x10-3 ug/ml). Based on the data of in vivo and in vitro antimalarial activities, the compound had no antimalarial activity because the extract consisted of many components that possessed many possible synergetic mechanisms of antimalarial if compared to single compound.Keywords: 
DOCKING MOLEKUL DENGAN METODA MOLEGRO VIRTUAL DOCKER DARI EKSTRAK AIR Psidium guajava, Linn DAN Citrus sinensis, Peels SEBAGAI INHIBITOR PADA TIROSINASE UNTUK PEMUTIH KULIT Ayik Rosita Puspaningtyas
Jurnal Kimia Terapan Indonesia Vol 15, No 1 (2013)
Publisher : Research Center for Chemistry - LIPI

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (6980.057 KB) | DOI: 10.14203/jkti.v15i1.102

Abstract

We have been molecular docking using MolegroVirtual Docker (MVD) on water extract of guava fruit(Psidiumguajava, Linn) and sweet orange (Citrussinensis,Peels) as inhibitor on enzyme tyrosinase withascorbic acid (vitamin C) as positive control to studywhitening agent. Based on the previous studies, the maincontent of the water extract of guava fruit (Psidiumguajava)are 2,6-dihydroxy-3,5-dimethyl-4-0--D-glucopyranosilbenzophenone, 3-hydroxy-2-butanone, and vitamin C, whilethe extract juice of sweet oranges (Citrus sinensis) arelimonene, linalol, and vitamin C. In this study the resultsshowed that the main content of the water extract of Psidiumguajava fruit have better bond as inhibitor on tyrosinase thanCitrus sinensis and vitamin C which can be seen fromMoldock score of Psidiumguajava (-107.806) and Citrussinensis (-76,9593); it meanslower the energyand morestable binding. The IC50 on water extract of guava fruit(psidiumguajava) and sweet orange (Citrus sinensis) were0.26 mM and 31.07 mM, respectively. The hydrogen bonds of2, 6-dihydroxy-3, 5-dimethyl-4-0--D- glucopyranosilbenzophenone with 5amino acid of tyrosinase were Gly 200,Pro 201 , Gly 196, Phe 197, and Asn 205, while limonen,linalool binding 3 amino acids were Gly 200, Phe 197, andAsn 205. Finally, 3D MVD visualization between maincontent of guava and sweet orange water extract can beconcluded that interaction of guava fruit (psidiumguajava)water extract against tyrosinase was more harmonious andstabil than vitamin C and main content of sweet orange(Citrus sinensis) water extract.Keywords: Psidium guajava, Citrus sinensis, tyrosinase, vitamin Cand docking molecule
Pengembangan Edible Sensor Berbasis Antosianin Kubis Merah (Brassica oleracea var capitata L.) untuk Monitoring Kesegaran Fillet Ikan Nila (Oreochromis niloticus) Hadiyatun Nuroniyah; Bambang Kuswandi; Ayik Rosita Puspaningtyas
Pustaka Kesehatan Vol 10 No 2 (2022): Volume 10 No.2, 2022
Publisher : UPT Percetakan dan Penerbitan Universitas Jember

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.19184/pk.v10i2.28183

Abstract

Tilapia is actually the most popular source of protein in the world market in the form of fillets, because it has several advantages, such as being able to be processed into various new processed products, easy to distribute and marketable in attractive forms. It is necessary to monitor the freshness quality of tilapia fish fillets. This study aims to develop an edible sensor for monitoring the freshness of tilapia (Oreochromis niloticus) fillets that are safe for consumption and also environmentally friendly with a pH indicator of the anthocyanin of red cabbage (Brassica Oleracea Var. Capitata L.). The edible sensor was applied to the tilapia fillet package. The characterization of edible sensors includes observation of surface morphology with SEM and functional group analysis with FTIR. Tests for freshness parameters of tilapia fish fillets included pH value test, total microbial count test, TVBN level test, and organoleptic test. The color change of the edible sensor was observed visually and using ImageJ software to determine the mean red value. The results show that the color of the edible sensor is dark purple when it indicates fresh tilapia fillet, the light purple color is still fresh, and the grayish-purple color of rotten tilapia fillet is not safe for consumption. Red cabbage anthocyanin-based edible sensors can be applied as smart labels for monitoring the freshness of tilapia fillets.
Development and Validation of RP-HPLC Analysis Method for Determination of Total Alkaloid Content of Soursop (Annona muricata L.) Leaf Extract Lindawati Setyaningrum; Dyah Purwaningtyas; Ayik Rosita Puspaningtyas; Dyan Wigati; Mohammad Rofik Usman; Maasyitoh Sari Latifah
EKSAKTA: Berkala Ilmiah Bidang MIPA Vol. 23 No. 03 (2022): Eksakta: Berkala Ilmiah Bidang MIPA (E-ISSN : 2549-7464)
Publisher : Faculty of Mathematics and Natural Sciences (FMIPA), Universitas Negeri Padang, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (1166.627 KB) | DOI: 10.24036/eksakta/vol23-iss03/325

Abstract

Soursop leaves contain alkaloids that have pharmacological effects. This study aims determine the total alkaloid content of soursop leaf ethanol extract using a validated HPLC method. Extraction was carried out by soxhletation followed by liquid-liquid extraction using chloroform. Optimizing HPLC conditions on the mobile phase, flow rate, concentration, and wavelength, further testing the validation of the analytical method. Optimizing HPLC conditions obtained optimal results at concentration of 500 ppm with a flow rate of 1.0 mL/min using acetonitrile: methanol: water (80:5:15) at wavelength of 272 nm. These results have met the validation requirements of analytical methods including System Suitability Test (UKS), selectivity, linearity with y = 2.01914x –219,97226, correlation coefficient value (r) = 0.9995, and Vx0 value 0.11201%. The limit of detection and quantization were 8,78525 ppm and 29,28418 ppm, respectively. The RSD percentage of the precision test is 1.0453%, and the accuracy test is obtained from the recovery of 98-102%. The result of determining the total alkaloid content  sample was 0.0862 ± 0.004 % (%w/w) of the entire alkaloid content (TALC) triple replication. This research concludes that the analytical method using the HPLC system for determining the total alkaloid content of the ethanolic extract of soursop leaves is validate
SKRINING FITOKIMIA DAN POTENSI DAYA HAMBAT EKSTRAK METANOL KULIT BATANG MERBAU PANTAI (Intsia bijuga) TERHADAP ENZIM α-GLUKOSIDASE Estu Wilujeng; Ayik Rosita Puspaningtyas; Indah Purnama Sary
Jurnal Ilmiah Farmasi Farmasyifa Vol 6, No 1 (2023)
Publisher : Universitas Islam Bandung

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.29313/jiff.v6i1.10133

Abstract

Diabetes mellitus (DM) merupakan penyakit yang ditandai dengan terjadinya kenaikan kadar glukosa darah dan gangguan metabolisme yang berkaitan dengan sekresi insulin. Potensi kulit batang merbau pantai sebagai antidiabetes hanya dilakukan berdasarkan survey etnobotani saja sehingga diperlukan penelitian experimental laboratories untuk mengetahui manfaatnya dari segi kesehatan sebagai antidiabetes. Penelitian ini bertujuan untuk mengetahui golongan senyawa yang terkandung dalam ekstrak metanol kulit batang merbau pantai, melakukan analisis profil kurva Lineweaver-Burk dan menentukan nilai presentase penghambatan untuk mengetahui jenis pola dan potensi hambatan yang dihasilkan senyawa yang terkandung dalam ekstrak metanol kulit batang merbau pantai tehadap reaksi enzimatik α-glukosidase yang mana digunakan akarbosa sebagai kontrol positif. Penelitian ini menunjukkan bahwa ekstrak metanol mengandung golongan senyawa flavonoid, tanin dan alkaloid. Pada konsentrasi 25-500 µg/mL menghasilkan presentrase penghambatan yang cukup rendah jika dibandingkan dengan akarbosa yaitu 13-22%. Selain itu, diketahui pola penghambatan terhadap enzim α-glukosidase bekerja uncompetitive.
PENGEMBANGAN VALIDASI METODE DAN PENETAPAN KADAR AKRILAMIDA PADA UBI JALAR GORENG SECARA KROMATOGRAFI LAPIS TIPIS-DENSITOMETRI Ayik Rosita P
JOURNAL OF PHARMACY SCIENCE AND TECHNOLOGY Volume 2 No. 2: Desember 2021
Publisher : Prodi Farmasi Fakultas Kedokteran Universitas Hang Tuah

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.30649/pst.v3i1.107

Abstract

A thin-layer chromatography (TLC) Densitometric method for analyzing acrylamide in fried sweet potatoes is not reported before. The research aims to determine the development of acrylamide validation and acrylamide concentration in fried sweet potatoes. The retardation factor for evaluating acrylamide uses silica gel column 254 with range 0.4-0.5 and eluate by methanol: benzene (2:1) was analyzed in a maximum wavelength of 200 nm. Linear response of acrylamide standard was tested within a 120-300 ppm concentration range, and the correlation coefficient (r) more remarkable than 0,99, detection limit 17.45 ppm and quantitative limit 52.36 ppm. Sample preparation was performed by ethanol 70%. The precision resulted from 2,67%, and this result was less than 16% (literature). Percentage of recoveries 98,18 %, and in the literature, 98%-102%. The TLC densitometric method is selective, precise, and accurate. Finally, the research showed that fried sweet potatoes contain acrylamide less than 230,32 ng samples, so the selection is very safe to consume.
Synthesis of Novel Ester-Based 5-Fluorouracil Derivatives Ayik Rosita Puspaningtyas; Ika Oktavianawati
Jurnal Kimia Sains dan Aplikasi Vol 27, No 8 (2024): Volume 27 Issue 8 Year 2024
Publisher : Chemistry Department, Faculty of Sciences and Mathematics, Diponegoro University

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.14710/jksa.27.8.354-362

Abstract

Fluorouracil (5-Fu, 1) is an antimetabolite cancer drug and the first-line drug of anticancer administration by WHO that has been widely used worldwide for more than 50 years. The development of 5-fluorouracil is an effort to obtain higher activity, decrease side effects, and create a specific target receptor compared to 5-fluorouracil. In this research, a series of novel 5-Fluorouracil (5-Fu) derivatives has been synthesized based on a benzoylation reaction (Schotten-Baumann reaction) of N1-hydroxylated 5-Fu called compound 2, 5-fluoro-1-(hydroxymethyl)-uracil. The benzoyl chloride substituents used in this research, including 3-chlorobenzoyl (4a), 2-chlorobenzoyl (4b), 3-nitrobenzoyl (4c), 4-methoxy benzoyl (4d), 4-trifluoromethylbenzoyl (4e), 3,4-dichlorobenzoyl (4f), and 4-nitrobenzoyl (4g) chloride become (4a-4f)-5Fu. This research meticulously examined the conditions (time and reaction temperature) at the second step of the synthesis reaction (esterification), ensuring the reliability of the results. The best synthesis conditions for 4a, 4b, 4c, 4d, and 4g compounds were found to be reflux at 40°C for 6 hours, whereas 4e and 4f compounds reactions were performed in an ice bath for 11 and 17 hours, respectively. All product syntheses, 4a-4g compound, were purified using column chromatography and eluted using eluent hexane: acetone (6:4), and the yields of 4a-4g compounds were around 61-79%. The pure compounds were characterized using FTIR and 1HNMR spectrometer, further validating the research. Based on these findings, it can be concluded that all 5-Fu derivatives can be synthesized using the Schotten-Baumann reaction method.