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All Journal Jurnal Teknosains INDONESIAN JOURNAL OF PHARMACY JPSCR : Journal of Pharmaceutical Science and Clinical Research Molekul: Jurnal Ilmiah Kimia
Aguslina Kirtishanti
Faculty Of Pharmacy Universitas Surabaya, Surabaya
Biochemistry, Genetics & Molecular Biology Chemical Engineering, Chemistry & Bioengineering Chemistry Civil Engineering, Building, Construction & Architecture Environmental Science Industrial & Manufacturing Engineering Mechanical Engineering Medicine & Pharmacology Public Health

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IDENTIFIKASI EFEK DEPRESAN SSP (SUSUNAN SARAF PUSAT) ANTIKEJANG DAN NEUROTOKSISITAS SENYAWA 4-KLOROBENZOILTIOUREA PADA MENCIT PUTIH JANTAN Aguslina kirtishanti dan Dini Kesuma
Jurnal Teknosains Vol 2, No 1 (2012): December
Publisher : Universitas Gadjah Mada

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.22146/teknosains.5980

Abstract

The study on the development of benzoylthiourea derivatives as central nervous system (CNS) depressants was based on their structure, which contains acyclic ureide, an isosteric group of CNS depressant drugs common structure. The study was carried out by modifying the structure of benzoylthiourea using the Topliss model based on the enhancement of its lipophilic and electronic properties. It is predicted that the product will give higher activity than the parent compound. In this study, identification of CNS depressant, anticonvulsant and neurotoxicity effects of the compound synthesized, i.e. 4-chlorobenzoylthiourea, was conducted. The identification of CNS depressant effects was done using Barbiturate Sleeping Time, the identification of anticonvulsant effects was done using Maximum Electroshock Seizure and the identification of neurotoxicity effect was done using rotarod in mice (Mus musculus). This study used five groups of mice: a control group, a standard group (Phenobarbital Na) and 3 treatment groups with doses of 15 mg/kg, 45 mg/kg and 75 mg/kg respectively. From the results, it can be concluded that 4-chlorobenzoylthiourea gives the best CNS depressant, anticonvulsant and neurotoxicity effects at the doses of 75 mg/kg, 15 mg/kg and 45 mg/kg respectively. 
The effect of mengkudu fruit methanolic extract and methanolic residual fraction on GLUT-4 protein elevation Aguslina Kirtishanti
Indonesian Journal of Pharmacy Vol 20 No 4, 2009
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (189.458 KB) | DOI: 10.14499/indonesianjpharm0iss0pp170-177

Abstract

Investigating in the Diabetes Mellitus drug which one having good activity and tolerance to patients are still in researchers’ concern. One of the main topics now days is the use of mengkudu plants as a traditional medicine of Diabetes Mellitus. This research was aimed to determine the increase of GLUT-4 protein in type 2 Diabetes Mellitus rats after given methanolic extract and methanolic residual of mengkudu fruit. The male rats were diabetic induced with exogenous i.p. insulin for 10 days. After showing hyperglycemic effect, the rats were given orally methanolic extract and methanolic residual fraction of mengkudu fruit for 4 days. On the fifth day, fasting blood glucose was measured and the rats were sacrificed to take the thigh muscle tissue for immunohistochemical calculation.The result showed that methanolic extract and methanolic residual of mengkudu fruit increase the amount of GLUT-4 protein, but can not reduce fasting blood glucose levels of male white rats.Key words : mengkudu fruit (Morinda citrifolia L.), methanolic extract and methanolic residual, type 2 Diabetes Mellitus, GLUT-4 protein
Reverse Docking, Molecular Docking, Absorption, Distribution, and Toxicity Prediction of Artemisinin as an Anti-diabetic Candidate Ruswanto Ruswanto; Richa Mardianingrum; Siswandono Siswandono; Dini Kesuma
Molekul Vol 15, No 2 (2020)
Publisher : Universitas Jenderal Soedirman

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (465.792 KB) | DOI: 10.20884/1.jm.2020.15.2.579

Abstract

Aldose reductase is an enzyme that catalyzes one of the steps in the sorbitol (polyol) pathway that is responsible for fructose formation from glucose. In diabetes, aldose reductase activity increases as the glucose concentration increases. The purpose of this research was to identify and develop the use of artemisinin as an anti-diabetic candidate through in silico studies, including reverse docking, receptor analysis, molecular docking, drug scan, absorption, and distributions and toxicity prediction of artemisinin. Based on the results, we conclude that artemisinin can be used as an anti-diabetic candidate through inhibition of aldose reductase
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.
Co-Authors Amelia Lorensia Ananta Yudiarso Bambang Tri Purwanto Lidia Junita Linggani Linggani Richa Mardianingrum Ruswanto, Ruswanto Selvia Agustina Siswandono, Siswandono Suko Hardjono