Hasil Pencarian

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Hasil Pencarian

Ditemukan 4 dokumen yang sesuai dengan query
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Inas Priasti Siwi
"Obat antiinflamasi non-steroid (OAINS) adalah salah satu obat antiinflamasi yang paling sering digunakan. Namun, OAINS menghambat enzim COX-1 dan COX-2 sekaligus sehingga memiliki efek samping yang cukup serius jika digunakan jangka panjang, seperti gastrointestinal dan gangguan ginjal. Studi melaporkan benzimidazol dan vanilin memiliki aktivitas antioksidan dan antiinflamasi namun potensi dari kedua senyawa ini masih rendah. Modifikasi struktur benzimidazol pada posisi 2 dan substitusi basa C-Mannich diharapkan dapat memberikan peningkatan aktivitas antioksidan dan antiinflamasi serta bioavailibiltas yang lebih baik. Dengan demikian, dilakukan sintesis, uji in vitro antioksidan dan antiinflamasi serta studi penambatan molekuler senyawa turunan basa Mannich dari benzimidazolvanilin. Sintesis dilakukan dalam dua tahapan, yaitu sintesis benzimidazolvanilin melalui reaksi siklokondensasi antara o-fenilendiamin dengan vanilin. Dilanjutkan dengan sintesis tahap 2, yaitu reaksi basa Mannich yang terdiri dari reaksi kondensasi, dehidrasi, dan adisi nukelofilik antara senyawa benzimidazolvanilin dengan formaldehid dan amina sekunder. Telah berhasil disintesis 4 senyawa turunan benzimidazolvanilin yang merupakan senyawa benzimidazol tersubstitusi vanilin pada posisi 2 dan tersubstitusi basa C-Mannich pada posisi orto pada fenolik yaitu; benzimidazolvanilin-morfolin (2a), benzimidazolvanilin-pirolidin (2b), benzimidazolvanilin-dietilamina (2c), danbenzimidazolvanilin-dimetilamina (2d) dengan persen rendemen sebesar (%) 82,51 (2a); 43,74 (2b); 47,78 (2c); 51,12 (2d). Senyawa yang terbentuk dikarakterisasi strukturnya menggunakan FTIR, 1H-NMR, dan 13C-NMR. Senyawa-senyawa tersebut dilakukan uji aktivitas antioksidan dengan metode DPPH, hasil menunjukkan IC50 (μM) sebesar 59,63 (2a); 76,33 (2b); 70,00 (2c); 76,24 (2d). Selanjutnya dilakukan uji aktivitas antiinflamasi dengan metode penghambatan denaturasi protein, menunjukkan IC50 (μM) sebesar 231,06 (2a); 210,43 (2b); 229,55 (2c) dan 243,74 (2d). Pengujian in-silico dilakukan dengan penambatan molekuler antara senyawa 2a-2d terhadap protein COX-2 dan COX-1 menggunakan program Autodock. Hasil penambatan molekuler didapatkan senyawa 2b merupakan senyawa dengan indeks selektivitas terbaik sebesar 23,32 dan binding affinity sebesar -9,09 kkal/mol. Dari data tersebut menunjukkan senyawa hasil sintesis bukan merupakan inhibitor COX-2 selektif.

Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most commonly used anti-inflammatory drugs. However, NSAIDs inhibit COX-1 and COX-2 enzymes at the same time and have serious side effects if used long-term, such as gastrointestinal and renal disorders. Studies report benzimidazole and vanillin have antioxidant and anti-inflammatory activities but the potency of these two compounds is still low. Modification of the benzimidazole structure at position 2 and C-Mannich base substitution are expected to provide increased antioxidant and anti-inflammatory activity and better bioavailability. Thus, the synthesis, antioxidant and anti-inflammatory in vitro tests and molecular tethering studies of Mannich base derivative compounds of benzimidazolvaniline were carried out. The synthesis was carried out in two stages, namely the synthesis of benzimidazolvaniline through a cyclocondensation reaction between o-phenylenediamine and vanillin. Followed by stage 2 synthesis, which is a Mannich base reaction consisting of condensation, dehydration, and nucleophilic addition reactions between benzimidazolvaniline compounds with formaldehyde and secondary amines. Four benzimidazolvanillin-derived compounds have been successfully synthesized which are vanillin-substituted benzimidazole compounds at position 2 and C-Mannich base substituted at the ortho position on phenolics, namely; benzimidazolvanillin-morpholine (2a), benzimidazolvaniline-pyrrolidine (2b), benzimidazolvaniline-diethylamine (2c), and benzimidazolvaniline-dimethylamine (2d) with percent yields of (%) 82.51 (2a); 43.74 (2b); 47.78 (2c); 51.12 (2d). The formed compounds were characterized using FTIR, 1H-NMR, and 13C-NMR. The compounds were tested for antioxidant activity using the DPPH method, the results showed IC50 (μM) of 59.63 (2a); 76.33 (2b); 70.00 (2c); 76.24 (2d). Furthermore, the anti-inflammatory activity was tested using protein denaturation inhibition method, showing IC50 (μM) of 231.06 (2a); 210.43 (2b); 229.55 (2c) and 243.74 (2d). In-silico testing was carried out by molecular docking between compounds 2a-2d against COX-2 and COX-1 proteins using the Autodock program. The results of molecular docking showed that compound 2b is the compound with the best selectivity index of 23.32 and binding affinity of -9.09 kcal/mol. The data shows that the synthesized compound is not a selective COX-2 inhibitor."
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Depok: Fakultas Farmasi Universitas Indonesia, 2024
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UI - Tesis Membership  Universitas Indonesia Library
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Eva Risalia
"ABSTRAK
Obat anti-inflamasi nonsteroid (OAINS) nonselektif banyak digunakan oleh lansia. OAINS nonselektif oral memiliki efek samping terhadap gastrointestinal baik lokal maupun sistemik. Oleh karena itu, diperlukan rute untuk menghantarkan OAINS nonselektif yang nyaman dan efek samping yang minimal. Salah satunya rute alternatif yaitu penghantaran melalui kulit yang disebut rute transdermal. Stratum korneum menjadi tantangan utama dalam rute transdermal. Hal ini dapat dibantu dengan adanya peningkat penetrasi agar jumlah obat dapat mencapai efek terapeutiknya. Peningkat penetrasi sintesis menyebabkan berbagai masalah. Terpen, minyak atsiri, dan asam lemak dapat diperoleh dari alam. Minyak atsiri daun zodia (Evodia suaveolens) memiliki kandungan terpen yaitu linalool, alfa-pinen, dan limonen. Tinjauan ini membahas mengenai hubungan antara OAINS nonselektif dengan sistem penghantaran transdermal, pengaruh peningkat penetrasi dari alam terhadap OAINS nonselektif, serta potensi minyak atsiri daun zodia sebagai peningkat penetrasi pada OAINS nonselektif. Sistem penghantaran transdermal dapat mengurangi efek samping lokal yang terdapat pada gastrointestinal, selain itu sistem transdermal nyaman dan mudah digunakan. Peningkat penetrasi dapat menjadi alternatif untuk peningkat penetrasi sintesis OAINS nonselektif. Dari beberapa penelitian menunjukkan bahwa peningkat penetrasi dari alam mampu meningkatkan penetrasi obat melalui kulit. Kandungan minyak atsiri daun zodia mengandung linalool, alfa-pinen, dan limonen yang dapat berpotensi untuk menjadi peningkat penetrasi OAINS nonselektif. Untuk memperbaiki dari penelitian-penelitian sebelumnya, maka disarankan penelitian dilengkapi dengan membandingkan pengaruh dari kontrol, peningkat penetrasi sintesis (sebagai standar), serta peningkat penetrasi uji; uji kompatibilitas; penggunaan membran hewan (tikus/kelinci) pada uji in vitro; serta uji mekanisme kerja dari peningkat penetrasi

ABSTRACT
Non-selective anti-inflammatory drugs (NSAIDs) are widely used by the elderly. Oral non-selective NSAIDs have side effects on both local and systemic gastrointestinal. Therefore, a route is needed to deliver convenient non-selective NSAIDs and minimal side effects. One alternative route is delivery through the skin called the transdermal route. The stratum corneum is the main challenge on the transdermal route. This can be helped by increasing penetration so that the amount of drug can reach its therapeutic effect. Synthesis penetration enhancers causes various problems. The terpenes, essensial oil, and fatty acid can be obtained from nature. Zodia (Evodia suaveolens) contain terpenes namely linalool, alpha-pinene, and limonene. This review discusses the relationship between non-selective NSAIDs and transdermal delivery systems, the effect of penetration enhancers from nature on non-selective NSAIDs, and the potential of Zodia as penetration enhancers in non-selective NSAIDs. The transdermal delivery system can reduce the local side effects in the gastrointestinal, besides that the transdermal system is comfortable and easy to use. Penetration enhancers can be an alternative to synthesis penetration enhancers nonselective NSAIDs. Several studies shown that natural penetration enhancers can increase drug penetration through the skin. The zodia leaf oil contains linalool, alpha-pinene, and limonene which can be potential to increase penetration of non-selective NSAIDs. To improve from previous studies, it is recommended that research should be completed by comparing the effects of controls, synthetic penetration enhancers (as a standard), and penetration enhancer test; compatibility test; use of animal membranes (mice/rabbits) for in vitro tests; and the mechanism action of penetration enhancers testing.
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Depok: Fakultas Farmasi Universitas Indonesia, 2020
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UI - Skripsi Membership  Universitas Indonesia Library
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"Dispepsia nonulseratif adalah suatu masalah gastrointestinal yang sering terjadi. Etiopatogenesisnya belum diketahui pasti. Tujuan penelitian ini adalah untuk mengetahui pengaruh faktor lingkungan seperti merokok, teh, alkohol, dan konsumsi NSAID terhadap dispepsia nonulseratif. Penelitian dilakukan di Bagian Gastroenterologi, Penyakit Dalam dan Radiologi IG Medical College, Shimla, India. Tiga ratus pasien dispepsia non ulseratif diteliti. Sebagai kelompok kontrol diambil dengan usia dan jenis kelamin yang sama. Riwayat merokok, teh, alkohol, dan konsumsi NSAID diteliti pada kedua kelompok. Konsumsi teh sebagai faktor lingkungan ternyata mempunyai pengaruh bermakna pada kelompok dispepsia nonulseratif, sedangkan faktor-faktor lain seperti merokok, alkohol, dan NSAID tidak mempunyai hubungan positif dengan dispepsia nonulseratif. (Med J Indones 2004; 14: 50-4)

Non ulcer dyspepsia is a common gastrointestinal problem, the etiopathogenesis of which is not well established. This study was planned to see the effect of environmental factors like smoking, tea, alcohol, and NSAIDs consumption with non-ulcer dyspepsia. This study was conducted in the department of Gastroenterology, Medicine and Radiology of I.G. Medical College, Shimla, India. Three hundred patients of non-ulcer dyspepsia were included in the study. Each case was matched with community control of same age and sex. A detailed history of smoking, tea, alcohol, and NSAIDs consumption was taken from the patients and controls. Consumption of tea as an environmental factor was found to be statistically significant in non-ulcer dyspepsia patients as compared to controls using multivariate regression. In the present study, environmental factors like smoking, alcohol, NSAIDs consumption did not show positive co-relation with non-ulcer dyspepsia. (Med J Indones 2004; 14: 50-4)
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Lengkap +
Medical Journal of Indonesia, 14 (1) January March 2005: 50-54, 2005
MJIN-14-1-JanMar2005-50
Artikel Jurnal  Universitas Indonesia Library
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Stella Ilone
"Non-steroidal anti-inflammatory drugs (NSAIDs) is a group of drugs used to treat pain, inflammation, and fever. High consumption of NSAIDs associated with high gastrointestinal side effects. Common complaint from patients, which ranging from mild heartburn to the onset of gastrointestinal bleeding, often complicates the adequate administration of NSAIDs. Various methods have been developed to reduce the likelihood of gastroenteropathy complication. Early diagnosis, appropriate prompt treatment, as well as adequate monitoring will reduce morbidity and mortality from complications due to NSAIDs. This paper will discuss the diagnosis and management of gastro-enteropathy NSAID through approaching the underlying pathophysiology."
Jakarta: Interna Publishing (Pusat Penerbitan Ilmu Penyakit Dalam), 2016
611 UI-IJGHE 17:2 (2016)
Artikel Jurnal  Universitas Indonesia Library