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PREPARASI 4-ASETAMIDOFENIL BENZOAT DAN UJI AKTIFITAS ANALGESIK PADA MENCIT (Mus musculus) Muchlisin, M Artabah; Purwanto, Bambang Tri; Astuti, Engrid Juni
Media Farmasi: Jurnal Ilmu Farmasi Vol 10, No 2: September 2013
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (385.1 KB) | DOI: 10.12928/mf.v10i2.1165

Abstract

> Untuk mengembangkan senyawa turunan acetaminophen baru, dilakukan preparasi 4-acetamidofenil benzoat senyawa. Senyawa ini disintesis dengan mereaksikan dari acetamidofenil dengan benzoil klorida dengan metode Schotten Baumann. Kemurnian senyawa dibuktikan dengan kromatografi lapis tipis (KLT) dan titik lebur. Pada hasil KLT, senyawa yang disintesis memiliki 1 spot dengan tiga eluen yang berbeda dan memiliki rentang titik lebur 171,67-172,67 ºC. Sehingga dapat disimpulkan senyawa hasil sintesis murni. Karakterisasi struktur senyawa hasil sintesis dianalisis dengan spektrofotometer UV-VIS, spektrofotometer IR, NMR. Hasil analisis struktural menunjukkan bahwa senyawa hasil sintesis adalah 4 - acetamidofenil benzoat. Uji aktivitas analgesik dilakukan pada tikus menggunakan metode penghambatan nyeri dengan asam asetat glasial 0,6 % sebagai agen penginduksi nyeri. Hasil sintesis 4 - acetamidofenil benzoat memiliki ED50 73,48 mg / kg dan acetaminofen memiliki ED50 68,30 mg / kg. Secara statistik, potensi analgesik 4 - acetamidofenil benzoat sebanding dengan acetaminofen .Kata Kunci : 4 - acetamidofenil benzoat, acetaminophen, analgesik, mencit
Pengaruh Proses Fermentasi pada Daun Centella asiatica oleh Acetobacter tropicalis Terhadap Aktivitas Trombolitik Lailatul Nuraini; Bambang Tri Purwanto; Achmad Syahrani; Riesta Primaharinastiti; Achmad Toto Poernomo
Majalah Farmasetika Vol. 6, Supl. 1, Tahun 2021
Publisher : Universitas Padjadjaran

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.24198/mfarmasetika.v6i0.36665

Abstract

Agen trombolitik merupakan plasminogen activator yang dapat memecah fibrin menjadi fibrin degradation product (FDP) dan dapat digunakan pada terapi penyakit kardiovaskular. Agen trombolitik dapat diperoleh dari mikroorganisme seperti Acetobacter tropicalis InaCC B374 dan dari tanaman seperti Centella asiatica. Kedua sumber agen trombolitik tersebut dapat dilakukan kombinasi melalui proses fermentasi untuk meningkatkan efek terapetiknya. Proses fermentasi sendiri dipengaruhi oleh beberapa faktor termasuk media fermentasi dan waktu fermentasi. Penelitian ini bertujuan untuk mengetahui pengaruh proses fermentasi terhadap peningkatan aktivitas trombolitik dari hasil fermentasi Centella asiatica oleh Acetobacter tropicalis InaCC B374 pada berbagai variasi waktu fermentasi. Preparasi dilakukan dengan memfermentasi Centella asiatica selama 24, 48, dan 72 jam pada suhu 30°±1°C dengan kecepatan pengocokan 100 rpm kemudian ditentukan aktivitas trombolitiknya dengan metode clot lysis yang dilakukan inkubasi pada suhu 37°±1°C selama 60 menit. Hasil pengujian aktivitas trombolitik menunjukkan bahwa terjadi peningkatan aktivitas trombolitik setelah dilakukan proses fermentasi selama 24, 48 dan 72 jam dan aktivitas trombolitik maksimum tercapai pada hasil fermentasi 72 jam. Centella asiatica yang difermentasi selama 72 jam menunjukkan nilai indeks trombolitik yang paling besar (82,03) jika dibandingkan dengan infusa Centella asiatica tanpa fermentasi (37,39) dan Acetobacter tropicalis InaCC B374 (37,68). Disimpulkan bahwa proses fermentasi Centella asiatica oleh Acetobacter tropicalis InaCC B374 secara signifikan dapat meningkatkan aktivitas trombolitik keduanya
Metode RPTLC dan Optimasi Fase Gerak Dalam Penetapan Harga Rm Sebagai Salah Satu Parameter Lipofilisitas Dalam Rancangan Obat Gunardi Gunardi; Ratna Asmah S.; Bambang Tri Purwanto; Edy Sulistyowati; Siti Musinah
MEDIA MEDIKA INDONESIANA 2009:MMI VOLUME 43 ISSUE 5 YEAR 2009
Publisher : MEDIA MEDIKA INDONESIANA

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (229.154 KB)

Abstract

RPTLC and optimizing mobile phase methods in Rm value determination as one of lipophylicity parameters in drug designBackground: The early process to successfully achieve its target is drug penetration or absorption. Of the three physicochemical parameters i.e, lipophyllicity, electronic and steric parameters, the lipophyllicity parameter is the most reponsible in drug absorption process. The research was aimed to determine retention modified (Rm) value of barbituric acid compound derivatives using RPTLC metod and mobile phase optimizing.Methods: This study was conducted on barbituric acid compound derivatives by using reverse phase thin layer chromatography (RPTLC). Silica Gel GF 254 that had been submerget in the mixture of liquid paraffin and petroleum eter (95:5) was used as a stationary phase. The mixture of polar to non polar solvent was used as mobile phase.Results: Research showed that in this method the most optimum of mobile phase was indicated by methanol and acetic acid mixture in the ratio of (1:9). The resulted Rm values of 5,5-diethylbarbituric acid, 5,5-diallylbarbituric acid, 5-allyl-5-isopropylbarbituric acid, 5-allyl-5-isobuthylbarbituric acid, 5-etil-5-(1-methylbutyl) barbituric acid, 5-(1-cyclohexene-1-yl)-1,5-dimethylbarbituric acid and 5-ethyl-5-phenylbarbituric acid were as follow 0.116; 0.144; 0.162; 0.221; 0.262; 0.187 and 0.199.Conclusions: The most optimum mobile phase in this method was the mixed solvents that had lower polarity, i.e, the mix of methanol and acetic acid in the ratio of (1:9). The H1 , H2 and H3 substituens in barbituric acid nuclei showed, the longer carbon chain, the higher the Rm values, howover the existing of double bond in such substituents will decrease the Rm value.Keywords: RPTLC, mobile phase, Rm value ABSTRAK Latar belakang: Proses awal keberhasilan obat dalam mencapai target adalah penetrasi atau absorpsi. Parameter lipofilisitas paling bertanggung jawab terhadap proses absorpsi obat dibanding parameter elektronik dan stearik. Tujuan penelitian ini adalah penggunaan metode RPTLC dan optimasi fase gerak dalam penentuan harga retention modified (Rm) senyawa turunan asam barbiturat.Metode: Penelitian dilakukan terhadap senyawa turunan asam barbiturat, dengan metoda kromatografi lapis tipis fase terbalik. Digunakan fase diam silika gel GF 254 yang telah dibacem dengan campuran parafin cair dan petroleum eter dengan perbandingan (95:5). Fase gerak yang digunakan dipilih campuran pelarut dari yang sangat polar sampai yang kurang polar.Hasil: Fase gerak yang paling optimum digunakan dalam metode ini adalah campuran metanol dan asam asetat dengan perbandingan (1:9). Harga Rm yang diperoleh secara berturutan, asam 5,5-dietilbarbiturat, asam 5,5-dialilbarbiturat, asam 5-alil-5- isopropilbarbiturat, asam 5-alil-5-isobutilbarbiturat, asam 5-etil-5-(1-metilbutil) barbiturat, asam 5-(1-sikloheksen-1-il) 1,5- dimetilbarbiturat dan asam 5-etil-5-fenilbarbiturat adalah: 0,116; 0,144; 0,162; 0,221; 0,262; 0,187 dan 0,199.Simpulan: Fase gerak yang paling optimum dalam metoda ini adalah bukan fase berair, tetapi berupa campuran pelarut yang mempunyai polaritas rendah, yakni campuran metanol dan asam asetat dengan perbandingan (1:9). Substituen atom H1 , H2 dan H3 pada inti asam barbiturat, menunjukkan makin panjang rantai karbon, makin tinggi harga Rm-nya. Adanya ikatan rangkap pada substituen menurunkan harga Rmnya.
PREPARASI 4-ASETAMIDOFENIL BENZOAT DAN UJI AKTIFITAS ANALGESIK PADA MENCIT (Mus musculus) M Artabah Muchlisin; Bambang Tri Purwanto; Engrid Juni Astuti
Media Farmasi: Jurnal Ilmu Farmasi Vol 10, No 2: September 2013
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (385.1 KB) | DOI: 10.12928/mf.v10i2.1165

Abstract

> Untuk mengembangkan senyawa turunan acetaminophen baru, dilakukan preparasi 4-acetamidofenil benzoat senyawa. Senyawa ini disintesis dengan mereaksikan dari acetamidofenil dengan benzoil klorida dengan metode Schotten Baumann. Kemurnian senyawa dibuktikan dengan kromatografi lapis tipis (KLT) dan titik lebur. Pada hasil KLT, senyawa yang disintesis memiliki 1 spot dengan tiga eluen yang berbeda dan memiliki rentang titik lebur 171,67-172,67ºC. Sehingga dapat disimpulkan senyawa hasil sintesis murni. Karakterisasi struktur senyawa hasil sintesis dianalisis dengan spektrofotometer UV-VIS, spektrofotometer IR, NMR. Hasil analisis struktural menunjukkan bahwa senyawa hasil sintesis adalah 4 - acetamidofenil benzoat. Uji aktivitas analgesik dilakukan pada tikus menggunakan metode penghambatan nyeri dengan asam asetat glasial 0,6 % sebagai agen penginduksi nyeri. Hasil sintesis 4 - acetamidofenil benzoat memiliki ED50 73,48 mg / kg dan acetaminofen memiliki ED50 68,30 mg / kg. Secara statistik, potensi analgesik 4 - acetamidofenil benzoat sebanding dengan acetaminofen .
Rational Design, Synthesis and Cytotoxic Activity of N-(Phenylcarbamoyl)Benzamide on HeLa Cell Lines Bambang Tri Purwanto; Siswandono Siswandono; Suko Hardjono; Dian Triwidiandany
Journal of Mathematical and Fundamental Sciences Vol. 52 No. 2 (2020)
Publisher : Institute for Research and Community Services (LPPM) ITB

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.5614/j.math.fund.sci.2020.52.2.3

Abstract

Urea derivatives are extensively used in the pharmaceutical industry. However, the unsatisfactory level of their membrane penetration requires further modification of the structures with stronger lipophillic properties. Phenylurea has a phenyl group that enables easier membrane penetration as a result of stronger pharmacological activity. Activity prediction was conducted by docking experiments and molecular dynamics, performed with Molegro Virtual Docker 5.5 using checkpoint kinase 1 (CHK1) enzyme with ID PDB: 2YWP. ADMET prediction was applied to collect data using the pkCSM tool. N-(phenyl carbamyol)benzamide compounds, modified by the Schotten Baumann method, were synthesized from benzoil chloride reacting with N-phenylurea. For evaluating anticancer activity, the MTT assay method on HeLa cells was used. Derived from the docking experiments, the compound rerank score of the N-(phenylcarbamoyl)benzamide was 72.0603 kcal/mol, lower than that of hydroxyurea, -32.1514 kcal/mol, causing better inhibitory activities against HeLA cell lines due to higher cytotoxic effects. ADMET Predictor was employed, indicating satisfactory compound distribution with a low, favorable metabolism, possessing good excretion and non-toxicity. The synthesized compound was 82% N-(phenyl carbamoyl)benzamide with 0.8 mM IC80, higher than that of hydroxyurea, 4.3 mM. In conclusion, successfully synthesized N-(phenylcarbamoyl)benzamide was proved to have higher cytotoxic effects. The satisfactory values of these compounds indicate that they are promising anticancer drug candidates.
Analgesic Activity of Acyl-Salicylic Acid Derivatives And In Silico Docking Study For Their Potency As Cyclooxygenase-2 Inhibitors Nuzul Wahyuning Diyah; Anindi Lupita Nasyanska; Bambang Tri Purwanto; Siswandono Siswandono
Berkala Ilmiah Kimia Farmasi Vol. 7 No. 2 (2020): DESEMBER
Publisher : Universitas Airlangga

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (805.626 KB) | DOI: 10.20473/bikfar.v7i2.29302

Abstract

A series of acyl salicylic acid derivatives were screened to investigate their analgesic activities and their potency as cyclooxygenase-2 (COX-2) inhibitors. Fourteen compounds (BS1–14) were assayed by acetic acid induced writhing test. Their ability for interaction with COX-2 was studied through a docking simulation at the COX-2 active site (PDB. 5IKQ). The results of the analgesic activity test gave 3 compounds that produce ED50< 0.39 mmol/kg body weight, lower than aspirin as a positive control. The compounds BS3 and BS4 showed excellent analgesic activity and the tert-butyl substituted molecule BS3 (O-(4-tert-butylbenzoyl)-salicylic acid analog) showed the highest analgesic activity with ED50 of 0.26 mmol/kg. Based on in silico molecular docking, it is known that almost all of the tested ligands (12 compounds) showed a higher binding affinity for COX-2 than meclofenamic acid which is a COX-2 inhibitory NSAID. The results of in vivo analgesic activity were justified with the outcome of in silico investigation. Molecular docking of acyl-salicylates confirmed in vivo experiments and it was found that BS3 was the most active compound as an analgesic agent and the most potent as a COX-2 inhibitor among the evaluated compounds.a
Sintesis Senyawa N-(2-Klorobenzoil)-N’-Fenilurea dan Uji Aktivitas Anti Kanker Terhadap Sel HeLa Bambang Tri Purwanto
JURNAL ILMU KEFARMASIAN INDONESIA Vol 16 No 2 (2018): JIFI
Publisher : Fakultas Farmasi Universitas Pancasila

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (321.562 KB) | DOI: 10.35814/jifi.v16i2.548

Abstract

Research in the search for cancer drug compounds continue to be developed given the lack of specific anticancer compounds. Some urea derived compounds are also continuously being developed in search of potent anticancer compounds with minimal side effects. In relation to the above, we want to develop an urea derivative of N-phenylurea compound which will be reacted with benzoyl chloride derivative that is 2-chlorobenzoyl chloride so that N-(2-chlorobenzoyl) -N'phenylurea will be obtained. Synthesis of N- (2-chlorobenzoyl) -N'phenylurea was done by modified Schotten-Baumman method, then purity test was performed with thin layer chromatography using 3 different solvents. The next step is structural characterization using UV and IR spectrophotometry method, then 1H-NMR and MS spectrometry, so that the structure of N- (2-chlorobenzoyl) -N'phenylurea will be obtained. An anticancer activity test is performed on HeLa cells using MTT assay method and IC50 value will be obtained. Compounds that have been successfully synthesized are compound of N- (2-chlorobenzoyl) -N'phenylurea, with yield of 80.47% in the form of white needle crystal. The purity test of the N- (2-chlorobenzoyl) -N'phenylurea compound was performed by thin layer chromatography with 3 different solvents (hexan: ethyl acetate: methanol = 2: 3: 1; Hexan: acetone = 4: 2; Hexan: ethylacetate = 4: 2) a single stain is obtained which is different from the Rf value compared to the N-phenylurea origin compound. The Melting Point of the compound is 149oC so it is seen that the compound has been formed and different from the origin compound of N-phenylurea. The anticancer activity test after performed with MTT assay method using HeLa cells line, has an IC50 2100 mg / ml or 8,52 mM for the N- (2-chlorobenzoyl) -N'phenylurea and higher than hydroxy urea as standard compound which has the activity as 7537 mg / ml or 99,10 mM. Conclusion: N- (2-chlorobenzoyl) -N'phenylurea compound has been successfully synthesized and can be further developed as an anticancer compound. Keywords: Synthesis; N-(2-chlorobenzoyl)-N'phenylurea; anticancer activity; HeLa cells.
Uji in silico Aktivitas Sitotoksik dan Toksisitas Senyawa Turunan N-(Benzoil)-N’- feniltiourea Sebagai Calon Obat Antikanker Dini Kesuma; Siswandono Siswandono; Bambang Tri Purwanto; Suko Hardjono
JPSCR: Journal of Pharmaceutical Science and Clinical Research Vol 3, No 1 (2018)
Publisher : Universitas Sebelas Maret

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (359.352 KB) | DOI: 10.20961/jpscr.v3i1.16266

Abstract

Senyawa N-(benzoil)-N’-feniltiourea mempunyai gugus farmakofor yang sama dengan turunan urea yang mempunyai aktivitas antikanker, sepertihidroksiurea, sehinggalayakdijadikansenyawaindukuntukdikembangkanlebihlanjutmelaluimodifikasistruktur.  Penelitianinibertujuanuntukmemprediksiaktivitas sitotoksik dan toksisitas dari duapuluh tiga senyawa turunanN-(benzoil)-N’-feniltiourea sebagaicalonobatantikanker. Salah satumekanismekerjaturunanN-(benzoil)-N’-feniltiourea sebagaiantikanker adalah menghambat VEGFR2,regulatorpentinguntuk proses angiogenesis, sertasangatberperanuntukpertumbuhan tumor dan metastasis. Aktivitas biologis dapat diprediksi melalui pemodelan molekul yang disebut uji in silico, menggunakan program MVD (Molegro Virtual Docker),sedang toksisitas dapat diprediksi menggunakan program pkCSMdanProtoxonline tool. Uji in silico dilakukan dengan melakukan docking senyawa yang akan diprediksi aktivitasnya dengan target reseptor, VEGFR2, PDB ID. 3WZE.Hasildockingberupaenergiikatandigambarkandengannilai Rerank Score (RS).Senyawa dengan nilai RS kecil berarti mempunyai ikatan ligan-reseptor yang stabil dan diprediksi mempunyai aktivitas yang besar. Dari hasilujiin silicodisimpulkanbahwasemuaturunanN-(benzoil)-N’-feniltiourea diprediksimenimbulkantoksisitas relatifrendah, danmempunyai aktivitas sitotoksik lebihbesardibandinghidroksiurea, tetapimasihlebihrendahdibandingsorafenib.N-(4-propoksibenzoil)-N’-feniltioureadanN-(3,5-di-trifluorometilbenzoil)-N’-feniltioureadiprediksi mempunyai aktivitas sitotoksik paling besar tetapi menimbulkan hepatotoksik, sehingga sebagai senyawa terpilih untuk disintesis dan dikembangkan lebih lanjut adalah N-(3,4-dimetilbenzoil)-N’-feniltiourea.
SINTESIS, UJI AKTIVITAS SITOTOKSIK IN VITRO DAN MOLECULAR DOCKING SENYAWA 1-(4-KLOROBENZOIL)-1,3-DIMETILUREA Dian Agung Pangaribowo; Siswandono Siswandono; Bambang Tri Purwanto
Jurnal Kimia Terapan Indonesia Vol 16, No 1 (2014)
Publisher : Research Center for Chemistry - LIPI

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (1134.674 KB) | DOI: 10.14203/jkti.v16i1.6

Abstract

Senyawa 1-(4-klorobenzoil)-1,3-dimetilurea telah dirancang, disintesis, diidentifikasi struktur, dan diuji aktivitas sitotoksik secara in vitro. Simulasi docking dilakukan dengan memposisikan senyawa ke dalam sisi aktif reseptor Checkpoint kinase 1 (Chk1) untuk menentukan model pengikatan ligan reseptor. Sintesis 1-(4-klorobenzoil)-1,3-dimetilurea dilakukan lewat reaksi asilasi antara 1,3-dimetilurea dan 4-klorobenzoil klorida. Kemurnian produk hasil sintesis ditentukan dengan metode Kromatografi Lapis Tipis (KLT).Identifikasi struktur dilakukan dengan spektrofotometer UV, FT-IR dan spektrometer NMR. Hasil uji antiproliferatif menunjukkan bahwa senyawa 1-(4-klorobenzoil)-1,3-dimetilurea memiliki aktivitas sitotoksik terhadap sel HeLa yang lebih baik dibandingkan dengan kontrol positif yaitu hidroksiurea. Senyawa 1-(4-klorobenzoil)-1,3-dimetilurea dengan potensi aktivitas sitotoksik ini dapat menjadi agen antikanker yang potensial. Kata kunci: 1-(4-klorobenzoil)-1,3-dimetilurea, molecular docking, sintesis, aktivitas sitotoksik, hidroksiurea A novel 1-(4-chlorobenzoyl)-1,3-dimethylurea has been designed, synthesized, structurally determined, and the in vitro cytotoxic activity was evaluated. Docking simulation was performed to position this compound into the Checkpoint kinase 1 (Chk1) active site to determine the probable binding model. Synthesis of 1-(4-chlorobenzoyl)-1,3-dimethylurea was completed by acylation reaction between 1,3-dimethylurea and 4-chlorobenzoyl chloride. The purity of synthesized product was determined by Thin Layer Chromatography. Structure identification was performed by UV spectrophotometer, FT-IR and NMR spectrometer. Antiproliferative assay result demonstrated that this compound possessed good cytotoxic activity against HeLa cells, which is comparable to the positive control, hydroxyurea. This compound with potent cytotoxic activity might be a potential anticancer agent. Keywords: 1-(4-chlorobenzoyl)-1,3-dimethylurea, molecular docking, synthesis, cytotoxic activity
Peningkatan Pemahaman Pengelolaan Obat Keluarga dan Pangan Sehat untuk Anak sebagai Implementasi SDGS 3 di Bojonegoro: Increased Understanding of Family Medicine Management and Healthy Food for Children as Implementation of SDGS 3 in Bojonegoro Suzana Suzana; Juni Ekowati; I Nyoman Wijaya; Rosita Handayani; Siti Rahmah; Bambang Tri Purwanto; Dewi Melani Hariyadi
PengabdianMu: Jurnal Ilmiah Pengabdian kepada Masyarakat Vol. 8 No. 4 (2023): PengabdianMu: Jurnal Ilmiah Pengabdian kepada Masyarakat
Publisher : Institute for Research and Community Services Universitas Muhammadiyah Palangkaraya

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.33084/pengabdianmu.v8i4.4719

Abstract

This service activity is motivated by efforts to maintain health after the Covid-19 pandemic. The community carries out preventive efforts by providing stocks of their medicines at home. The culture of storing medicines in the household requires proper drug management to prevent drug damage due to improper storage, drug use errors, and environmental pollution due to errors in handling damaged or expired drugs. The pharmacist's role is vital in providing drug management education to the community. Another preventive effort undertaken by the community is to maintain a healthy body by applying a diet where fast food currently contains a lot of Food Additives (BTP), which can threaten long-term public health. For this reason, people need to get an education directly, so they are wise in using BTP. The solution is to educate the public regarding managing household medicines and healthy food for parents and guardians of RA Al Manshur Play Group (KB) students in Bojonegoro. Activities are packaged in counseling methods and training/practice activities. The expected outcome of the activity is an increase in the understanding of guardian parents, as indicated by an average post-test score of >65 with an increase in score of >10% compared to the pretest. By increasing the understanding of parents and teachers about managing medicines and healthy food in the family, it is hoped that conditions of good health and well-being in society will be achieved.