Hasil Pencarian  ::  Simpan CSV :: Kembali

"By focusing on general molecular mechanisms of antiviral drugs rather than therapies for individual viruses, this ready reference provides the critical knowledge needed to develop entirely novel therapeutics and to target new viruses.It begins with a general discussion of antiviral strategies, followed by a broad survey of known viral targets, such as reverse transcriptases, proteases, neuraminidases, RNA polymerases, helicases and primases, as well as their known inhibitors. The final section contains several cases studies of recent successful antiviral drug development.Edited by Erik de Clercq, the world authority on small molecule antiviral drugs, who has developed more new antivirals than anyone else."

"New strategies and techniques for today's fast-paced discovery process. Today, the pressure is on for high-throughput approaches to accelerate the generation, identification, and optimization of molecules with desirable drug properties. As traditional methods of analysis become antiquated, new analytical strategies and techniques are necessary to meet sample throughput requirements and manpower constraints. Among them, mass spectrometry has grown to be a front-line tool throughout drug discovery. Integrated Strategies for Drug Discovery Using Mass Spectrometry provides a thorough review of current analytical approaches, industry practices, and strategies in drug discovery. The topics represent current industry benchmarks in specific drug discovery activities that deal with proteomics, biomarker discovery, metabonomic approaches for toxicity screening, lead identification, compound libraries, quantitative bioanalytical support, biotransformation, reactive metabolite characterization, lead optimization, pharmaceutical property profiling, sample preparation strategies, and automation. THIS BOOK: Clearly explains how drug discovery and mass spectrometry are interconnected Discusses the uses and limitations of various types of mass spectrometry in various aspects of drug discovery Prominently features analytical applications that require trace-mixture analysis Provides industry applications and real-world examples Shares historical background information on various techniques to aid in the understanding of how and why new methods are now being employed to analyze samples."

"ABSTRAKDemam dengue masih memiliki angka insidensi tinggi terutama di Indonesia. Sampai saat ini, belum ditemukan terapi antivirus dengue. Penelitian untuk mendapatkan antivirus dengue dari sumber herbal sudah banyak dilakukan. Salah satu tanaman yang berpotensi sebagai antivirus dengue adalah Calophyllum nodosum yang diketahui memiliki aktivitas antimikroba. Penelitian ini menguji efek antiviral fraksi butanol Calophyllum nodosum terhadap aktivitas virus dengue tipe 2 dengan sel Huh-7-it sebagai sel host secara in vitro dan konsentrasi inhibisi minimal. Efek antiviral dinilai dengan nilai konsentrasi inhibitorik 50 IC50 dan konsentrasi sitotoksik 50 CC50 . Nilai IC50 menilai efek inhibisi ekstrak dan didapatkan dari hasil focus assay dengan menggunakan konsentrasi ekstrak 80, 40, 20, 10, 5, dan 2,5 g/mL Nilai CC50 menunjukkan efek sitotoksik ekstrak dan dihasilkan dari MTT assay dengan menggunakan konsentrasi 640, 320, 160, 80, 40, 20, dan 10 g/mL Perbandingan IC50 dan CC50 menghasilkan indeks selektivitas SI . Hasil IC50 adalah 5.6 g/mL dan hasil CC50 adalah 1181 g/mL sehingga didapatkan SI 210.9. Konsentrasi inhibisi minimal adalah 2.5 g/mL. Analisis statistic menunjukkan perbedaan bermakna antara kelompok control dengan kelompok perlakuan pada focus assay dan MTT assay. Dapat disimpulkan bahwa fraksi butanol Calophyllum nodosum memiliki efek antiviral tinggi dibandingkan efek sitotoksiknya.

---

ABSTRACTDengue fever still has a high incidence rate especially in Indonesia. Until now, there is no dengue antiviral therapy found. Researches to develop dengue antiviral from herbal sources had been done. One of the potential plants as dengue antiviral is Calophyllum nodosum which is known to have antimicrobial activity. This research evaluated the antiviral effects of butanol fraction of Calophyllum nodosum on DENV 2 activity with Huh 7 it cells as host cells in vitro and also evaluated minimal inhibitory concentration. Antiviral effects were assessed with 50 inhibitory concentration IC50 and 50 cytotoxic concentration CC50 values. The value of IC50 showed the effect of extract inhibition and is obtained from the focus assay results using the extract concentrations of 80, 40, 20, 10, 5, and 2.5 g mL. The CC50 value showed the effect of cytotoxic extract and resulted from MTT assay using concentrations of 640, 320 , 160, 80, 40, 20, and 10 g mL. Ratio of CC50 and IC50 is the selectivity index SI . The value of IC50 is 5.6 g mL and the value of CC50 is 1181 g mL and resulted in SI 210.9. The minimum inhibitory concentration is 2.5 g mL. Statistical analysis showed significant differences between control group and treatment group on focus assay and MTT assay. It can be concluded that the butanol fraction of Calophyllum nodosum has a high antiviral effect compared to its cytotoxic effects"

"ABSTRACTVirus Dengue (DENV) adalah salah satu penyakit virus dengan transmisi oleh nyamuk dan telah menyebar ke negara negara yang sebelumnya tidak pernah ada kejadian infeksi DENV. Walaupun demikian, belum ada obat antivirus berlisensi yang efektif. Salah satu agen alami yang diduga memiliki sifat anti virus terhadapDENV adalah asam galat yang telah terbukti memiliki sifat antivirus terhadap Herpes Simplex Virus 1 (HSV 1). Tujuan dari penelitian ini adalah untuk mempelajari toksisitas dan efektifitas amyl galat sebagai antivirus untuk DENV secara in vitro. Huh 7it-1 sel diinfeksikan dengan DENV 2 NGC strain yang telah diberi perlakuan dengan amyl galat pada konsentrasi 80 μg/ mL, 40 μg/ mL, 20 μg/mL, 10 μg/ mL, 5 μg/ mL, dan 2.5 μg/ mL. Viabilitas sel setelah diberi perlakuan dengan amyl galat kemudian diukur dengan MTT assay menggunakan spektrofotometer, sementara inhibisi virus oleh amyl galat diukur dengan menggunakan focus assay. Untuk menguji validitas dan perbedaan yang signifikan data uji statistik Kruskal Wallis dilakukan kepada setiap variabel dan uji Mann- Whitney juga digunakan untuk membandingkan hasil dengan kontrol negatif. Nilai CC50, IC50, dan SI dari penelitian adalah >80 ug/mL, 6 ug/mL, dan >13.333. Viabilitas sel setelah diberi amyl galat dengan konsentrasi 2.5 mg/mL tidak berbeda secara bermakna dengan control (P>0.05) akan tetapi pada konsentrasi ≥ 5 ug/mL ada perbedaan yang bermakna dengan kontrol (P<0.05). Hambatan infektivitas pada perlakuan amyl galat dengan konsentrasi 2.5 ug/mL, 5 ug/mL tidak berbeda secara bermakna dengan kontrol (P>0.05) namun pada konsentrasi ≥ 10 ug/mL ada perbedaan bermakna dengan control (P<0.05). Amyl galat mempunyai selektivitas yang signifikan terhadap sel yang terinfeksi DENV (SI>10) dan dapat disimpulkan bahwa amyl galat mempunyai potensi untuk dipakai sebagai obat anti virus melawan DENV, namun kajian dan percobaan lebih lanjut masih diperlukan.

---

ABSTRACTDengue virus (DENV) is a viral disease transmitted by mosquitoes and has spread to countries where there has never been a DENV infection. However, there are no effective antiviral drugs available. One of the natural agents suspected of having anti-virus properties is against DENV is gallic acid which has been proven to have antiviral properties against Herpes Simplex Virus 1 (HSV 1). The aim of this research is to study the toxicity and effectiveness of amyl galat as an antiviral for DENV in vitro. Huh 7it-1 cells were infected with DENV 2 NGC strains that had been treated with amyl error at concentrations of 80 μg / mL, 40 μg / mL, 20 μg /mL, 10 μg / mL, 5 μg / mL, and 2.5 μg / mL. Cell viability after being treated with amyl error was then measured by MTT assay using a spectrophotometer, while viral inhibition by amyl error was measured using focus assay. To test the validity and significant differences Kruskal Wallis statistical test data was performed on each variable and the Mann-Whitney test was also used to compare results with negative controls. Score CC50, IC50, and SI of the study were > 80 μg / mL, 6 μg / mL, and > 13,333. Cell viability after being given amyl error with a concentration of 2.5 mg / mL was not significantly different from control (P > 0.05) but at a concentration of ≥ 5 ug / mL there was a significant difference with control (P < 0.05). Barriers to infectivity in the treatment of amyl galat with a concentration of 2.5 μg / mL, 5 μg / mL did not differ significantly with control (P > 0.05) but at concentrations ≥ 10 ug / mL there were significant differences with control (P < 0.05). Amyl error has a significant selectivity to cells infected with DENV (SI > 10) and can be concludedthat amyl error has the potential to be used as an antiviral drug against DENV, but further studies and trials are still needed."

"Virus dengue (DENV) adalah patogen yang dapat disebarkan oleh vektor nyamuk Aedes aegypti. Infeksi dengue adalah masalah global dan endemik di Indonesia. Hingga saat ini pengobatan untuk infeksi dengue hanya sesuai gejala. Studi ini akan mengeksplorasi potensial ekstrak Curcuma longa (Curcuma longa) yang didapatkan dari Universitas Sebelas Maret sebagai antivirus DENV melalui observasi half inhibitory concentration (IC50) dan half cytotoxic concentration (CC50). Sel Huh 7it-1 yang telah ditumbuhkan pada plat 96 sumuran dan 48 sumuran diinfeksi DENV yang telah diberi perlakuan dengan ekstrak Curcuma longa. MTT assay dan Focus assay digunakan untuk mendapatkan nilai CC50 dab IC50, sehingga didapatkan nilai Selectivity index (SI). Hasil penelitianinimenunjukkanbahwanilaiCC50,IC50 danSIdariCurcumalongaadalah 118,417μg/ml, 2,424 μg/ml, dan 48,852 secara berurutan. Ekstrak Curcuma longa memiliki IC50 rendah dan CC50 tinggi Ketika dibandingkan dengan berbagai ekstrak tanaman dari riset lain, sehingga berpotensial sebagai antivirus DENV. Riset lebih lanjut mungkin dibutuhkan untuk memahami lebih lanjut mekanisme inhibisi DENV oleh ekstrak Curcuma longa.

---

Dengue virus (DENV) is a vector born pathogen spread by Aedes aegypti mosquito. Dengue infection is a worldwide problem and is endemic in Indonesia. Until now the treatment for dengue infection is limited to symptomatic. The current study aims to explore the potential of Curcuma longa (Curcuma longa) extract obtained from Universitas Sebelas Maret as DENV antivirus through observation of the half inhibitory concentration (IC50) and half cytotoxic concentration (CC50). Huh 7it-1 cell grown in 96 well plate and 48 well plate infected by DENV that was treated with Curcuma longa extract. MTT assay and Focus assay is used to obtain CC50 and IC50 value, so Selectivity index (SI) can be counted. The result showed that the CC50, IC50 and SI of Curcuma longa is 118.417μg/ml, 2.424 μg/ml, dan 48.852. Curcuma longa extract has low IC50 and high CC50 when compared to various plant extract from other research that has been done, so it has potential as DENV antivirus. Further research may be needed to understand more about the mechanism of DENV inhibition by Curcuma longa extract."

"ABSTRAKInfeksi dengue memiliki prevalensi yang tinggi di dunia, dengan spektrum penyakit yang luas yaitu Demam Dengue, Demam Berdarah Dengue, dan Sindrom Syok Dengue. Namun, tatalaksana yang ada tidak bersifat spesifik. Sudah banyak penelitian yang dilakukan untuk mencari vaksin dan antivirus dengue. Salah satu yang sudah terbukti memiliki efek antivirus dengue adalah senyawa turunan asam galat yaitu propil galat dan etil galat. Penelitian eksperimental ini bertujuan untuk mengetahui efek antivirus campuran propil galat dan etil galat terhadap virus dengue serotipe 2 pada sel Huh7it-1. Efek sitotoksisitas senyawa terhadap sel diuji dengan metode 3- 4,5-dimethylthiazol-2-yl -2,5-diphenyltetrazolium bromide assay. Nilai yang didapat digunakan untuk mencari nilai konsentrasi toksik 50 . Efek inhibisi senyawa terhadap replikasi virus diuji dengan metode focus assay. Nilai yang didapat digunakan untuk mencari nilai konsentrasi hambat 50 . Dari hasil penelitian didapatkan nilai CC50 = 117.942 mg/ml, IC50 = 4.455 mg/ml, dan SI = 26.474. Campuran propil galat dan etil galat memiliki efek antivirus terhadap DENV-2 dan cukup selektif.

---

ABSTRACTDengue infection have a serious prevalence in worldwide with a broad spectrum of disease from dengue fever, dengue hemorrhagic fever, and dengue shock syndrome. Otherwise, the nowadays treatment seems not specific for the dengue itself. There were a lot of study to search for the vaccine and the antivirus. One of the successful study that contained a significant effect of dengue antivirus is a chemical compound from gallate acid named propyl gallate and ethyl gallate. This experimental study aim to know the antivirus effect from the mixture of propyl gallate and ethyl gallate to the dengue virus serotype 2 in Huh7it 1 cells. Cytotoxicity effect of the mixture to the cells tested by 3 4,5 dimethylthiazol 2 yl 2,5 diphenyltetrazolium bromide assay technique. Obtained results can be used to search for the half cytotoxic concentration. The inhibition effect from this mixture to the viral replication processes tested by focus assay technique. Obtained results can be used to search for the half inhibitory concentration. From this study, the value of CC50 is 117.942 g mL, meanwhile the value of IC50 is 4.455 g mL with the SI value is 26.474. The mixture of propyl gallate and ethyl gallate have an antivirus effect to DENV 2 strain which are quite selective."

"Hepatitis B merupakan penyakit endemik di Indonesia. Pengobatan hepatitis B yang sedang dikembangkan adalah pengobatan herbal menggunakan senyawa aktif. Salah satu zat yang telah diteliti dan dapat menghentikan perkembangan virus Hepatitis B adalah zat andrografolida yang terdapat dalam tanaman sambiloto. Penelitian ini mengekstraksi zat andrografolida tersebut dari daun sambiloto dengan metode sonikasi. Dilakukan juga nanoenkapsulasi ekstrak dengan nanoenkapsulator kitosan-STPP sodium tripolifosfat menggunakan metode gelasi ionik dengan memvariasikan berat molekul kitosan dan jenis surfaktan. Kapasitas penjerapan tertinggi dihasilkan oleh kitosan HW sebesar 89,1 dan oleh surfaktan TWEEN 80 sebesar 88,2 . Efisiensi enkapsulasi terbaik dihasilkan oleh kitosan MW dan TWEEN 80 sebesar 96,6 . Ukuran partikel terkecil yang diperoleh dihasilkan kitosan MW sebesar 979,5 nm dan kombinasi surfaktan TWEEN 80 dan PEG 6000 sebesar 1128,2 nm. Profil rilis yang dihasilkan berupa slow release pada kondisi lambung kemudian burst release pada kondisi usus halus.

---

Hepatitis B is an endemic disease in Indonesia. One of the developments of hepatitis B treatment is herbal treatment using active compounds from plants, one of which is andrographolide that is found in abundance in sambiloto Andrographis paniculata . This research will extract andrographolide from sambiloto leaf by sonication and encapsulate the extract. Encapsulation is done using chitosan STPP sodium tripholiphosphate by ionic gelation with variations of chitosan molecular weight and surfactant type. The highest loading capacities are obtained by high molecular weight chitosan chitosan HW and TWEEN 80 as a surfactant with the values of 89,1 and 88,2 respectively. The optimum encapsulation efficiency with the value of 96,6 is obtained by medium molecular weight chitosan chitosan MW . Encapsulation using chitosan MW resulted in an optimum particle size of 979,5 nm, and the combined use of TWEEN 80 and PEG 6000 resulted in an optimum particle size of 1128,2 nm. The surfactant combination of TWEEN 80 and PEG 6000 led to a release profile of initial slow release in the stomach condition and burst release when in the small intesines. "

"Dari sekian banyak obat yang diyakini dapat mencegah pertumbuhan virus SARS-CoV2, kombinasi penggunaan lopinavir/ritonavir yang dilakukan secara oral menjadi salah satu pilihan karena dapat mengurangi gejala dan memperpendek durasi pelepasan virus. Namun, penggunaan obat memberikan efek samping pada kesehatan pencernaan pasien yaitu munculnya keluhan penyakit baru yaitu diare akibat kemudahan degradasi ritonavir yang disebabkan oleh pH sistem gastrointestinal yang sangat asam. Telah dilakukan penelitian mengenai material MOF MIL-101 (Cr) terenkapsulasi material sensitif pH, CMC(Catboxymethyl Cellulose) sebagai material pembawa obat ritonavir dalam upaya mengurangi efek samping tersebut. Sintesis dilakukan dengan secara hidrotermal untuk membentuk kerangka MOF yang diinginkan. Untuk mengetahui kemampuan material sebagai pembawa obat, digunakan variasi penambahan asam asetat pada sintesis MOF MIL-101 (Cr) untuk mengetahui pengaruhnya terhadap bentuk, ukuran, dan morfologi MOF, serta jumlah rendemen yang dihasilkan. Hasil analisis dan karakterisasi menunjukkan bahwa penambahan asam akan mempengaruhi jumlah rendemen yang dihasilkan, serts ukuran partikel MOF, yang kemudian mempengaruhi kemampuannya sebagai material pembawa obat. Persen rendemen yang didapatkan adalah 30,833% untuk material hasil sintesis dengan penambahan asam, dan 40,5% untuk material hasil sintesis tanpa penambahan asam. Didapatkan pula ukuran partikel MOF Asam yang lebih kecil daripada MOF Non Asam, yang menyebabkan persentase pemuatan obat yang didapatkan juga lebih kecil. Persen pemuatan obat optimum berada pada angka 73,6% untuk MOF Non Asam dengan variasi konsentrasu obat ritonavir 500 ppm. Penelitian mengindikasikan bahwa MOF MIL-101 (Cr) terenkapsulasi CMC memiliki kemampuan dalam memuat obat.

---

Of the many drugs that are believed to prevent the growth of the SARS-CoV2 virus, the combination of lopinavir/ritonavir taken orally is an option because it can reduce symptoms and shorten the duration of viral shedding. However, the use of drugs has side effects on the patient's digestive system, which is the emergence of a new disease complaint, diarrhea due to the ease of degradation of ritonavir caused by the acidic pH of the gastrointestinal system. Research has been conducted on CMC (Catboxymethyl Cellulose) coated MOF MIL-101 (Cr) as a drug carrier material for ritonavir in an effort to reduce these side effects. Synthesis was carried out hydrothermally to form the MOF framework. To determine the material's ability as a drug carrier, variations in the addition of acetic acid were used in the synthesis of MOF MIL-101 (Cr) to determine its effect on the shape, size and morphology of MOF, as well as the amount of yield produced. The analysis and characterization results show that the addition of acid will affect the amount of yield produced, as well as the particle size, which then affects its ability as a drug carrier material. The yield percentage obtained was 30,833% for materials synthesized with the addition of acid, and 40,5% for synthesized materials without the addition of acid. It was also found that the particle size of Acid MOF was smaller than that of non-Acid MOF, which caused a smaller percentage of drug loading. The optimum percentage of drug loading was at 73,6% for non-Acid MOF with a variation of 500 ppm of ritonavir drug concentration. Research indicated that MOF MIL-101 (Cr) encapsulated CMC has its capability of the drug loading system."

"How are medicines transported intact through the body to their specific target sites without triggering side effects? The answer is "Drug targeting".This thoroughly application-oriented book gives comprehensive answers to this and many other questions that confront scientists daily in chemical, pharmaceutical and medical research. A concise overview of the most important basic theories, modern forms of therapy and molecular biological tools, it represents a comprehensible introduction to the topic. The book then goes on to deal with strategies for target applications, divided according to target site, for example brain, lungs, liver, blood vessels and tumor cells. The third part is devoted to special, modern techniques, from phage display methods, via the use of tissue slices right up to pharmacokinetic modeling. Throughout, the focus remains on the practical aspect and successful application of the method in question, although a glance at what the future holds is also included. "

"The focus of early drug development has been the submission of an Investigational New Drug application to regulatory agencies. Early drug development : strategies and routes to first-in-human trials guides drug development organizations in preparing and submitting an Investigational New Drug (IND) application. By explaining the nuts and bolts of preclinical development activities and their interplay in effectively identifying successful clinical candidates, the book helps pharmaceutical scientists determine what types of discovery and preclinical research studies are needed in order to support a submission to regulatory agencies.This book about provides an invaluable guide to the earliest and most critical stages of drug development, getting promising new chemicals into humans quickly, effectively, and safely, to provide information of maximum benefit for critical decision making."