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"ABSTRAKKuersetin merupakan senyawa flavonoid dari bahan alam memiliki aktivitas antiinflamasi. Pemberian kuersetin secara topikal diharapkan dapat meningkatkan kadar kuersetin pada situs target osteoartritis. Nanopartikel lesitin-kitosan terbukti menjadi pembawa yang menjanjikan pada sistem penghantaran obat secara topikal pada senyawa kuersetin. Selanjutnya, nanopartikel diformulasi ke dalam sediaan gel. Terhadap sediaan gel dilakukan uji stabilitas fisik serta uji farmakodinamik pada tikus model osteoartritis dengan induksi monoiodoasetat. Tujuan dari penelitian ini adalah mendapatkan dan mengevaluasi sistem pembawa nanopartikel lesitin kitosan dalam meningkatkan efikasi kuersetin pada situs target pengobatan osteoartritis. Tikus Sprague Dawley 2-3 bulan dibagi menjadi 7 kelompok dengan 5 tikus per kelompok. Injeksi secara intraartikular dilakukan pada lutut kanan tikus pada hari ke-0. Dosis gel nanopartikel kuersetin yang digunakan pada penelitian ini adalah 0,84, 1,68, dan 3,37 mg/g gel. Kuersetin dengan pembawa berupa nanopartikel lesitin-kitosan mampu menghantarkan kuersetin hingga situs target dimana gel nanopartikel kuersetin dosis 3 menunjukan efikasi terbaik pada hewan model osteoartritis. Gel nanopartikel kuersetin mampu menghambat proses inflamasi dengan menurunkan volume udem dan menghambat IL-1 yang merupakan sitokin pro inflamasi serta mampu menghambat degradasi proteoglikan dengan menurunkan kadar serum ADAMTS-5, MMP-9 dan MMP-13 yang berperan pada degradasi proteoglikan serta meningkatkan intensitas warna proteoglikan pada gambar histopatologi lutut tikus model osteoartritis.

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ABSTRACTQuercetin is a flavonoid substance which has antiinflammatory activity. Quercetin in topical application may enhance quercetin level on target site of osteoarthritis. Lecithin Chitosan Nanoparticle proven to be a good vehicle for quercetin drug delivery on skin. Furthermore, quercetin nanoparticle formulated into gel. The gel was tested for its phamacodynamic effects on osteoarthritis model rat with monoiodoacetate induction. The purpose of this research was to evaluated lecithin chitosan nanoparticle vehicle for quercetin efficacy on the target sites of osteoarthritis therapy. Sprague Dawley rat 2 3 months old divided into 7 groups. The rats were given intraarticularly injection of monoiodoacetate on day 0 in the right knee of the rat. The amount dosage of quercetin nanoparticles used in this study was 0.84, 1.68, and 3.37 mg g gel. Normal control was given clear gel without quercetin nanoparticle, the positive group was given sodium diclofenac gel Voltaren , and 3 dose variation of quercetin nanoparticle gel, and babandotan group were given 160 mg g babandotan gel on day 29 until 70. Quercetin with nanoparticle lecithin chitosan vehicle could reduced inflammation process by reduced edema volume and inhibited IL 1 as proinflammation cytokine and could inhibited proteoglycan degradation by reduced ADAMTS 5, MMP 9, and MMP 13 and increased the proteoglycan color intensity on histopatology image of osteosrthritis model rats. "

"[ABSTRAKLatar Belakang: Kardiomiopati uremikum adalah kelainan jantung yang didasari oleh kelainan pada ginjal dan merupakan penyebab kematian tertinggi pada pasien penyakit ginjal kronik (PGK). Overload cairan dan stres oksidatif berperan dalam patogenesis penyakit ini. Kuersetin adalah antioksidan yang bersifat kardioprotektif, namun belum ada data tentang efeknya pada kardiomiopati uremikum. Penelitian ini bertujuan untuk mengetahui efek kuersetin pada kardiomiopati uremikum menggunakan model nefrektomi 5/6 pada tikus.Metode: Uremia diinduksi pada 3 kelompok tikus jantan Sprague-Dawley dengan nefrektomi 5/6, satu kelompok kontrol tanpa nefrektomi 5/6, masing-masing 6 ekor/kelompok dan diamati selama 8 minggu. Kelompok SNX tidak diberi pengobatan. Kelompok SNX+Q mendapat quersetin per oral dengan dosis 100 mg/kgBB/hari dan kelompok SNX+Cap mendapat kaptopril 10 mg/kgBB/hari. Hewan uji dikorbankan untuk diukur kadar malondialdehid (MDA) plasma dan jantung, aktivitas glutation peroksidase (GPX) jantung, NT-proBNP plasma, dan fibrosis jantung. Data dianalisis dengan uji ANOVA.Hasil: Nefrektomi 5/6 menimbulkan sedikit fibrosis jantung, tidak mempengaruhi NT-proBNP, tidak mempengaruhi MDA jantung dan plasma dan meningkatkan secara bermakna aktivitas GPX jantung (p<0.05) sedangkan pemberian kuersetin dan kaptopril tidak mempengaruhi fibrosis jantung, tidak mempengaruhi NT-proBNP (p>0.05), tidak mempengaruhi MDA jantung dan plasma (p>0.05) dan tidak mempengaruhi aktivitas GPX jantung pada tikus uremia yang diinduksi dengan nefrektomi 5/6 (p>0.05).Kesimpulan: Kuersetin tidak mempengaruhi fibrosis jantung dan fungsi jantung tikus uremia pasca nefrektomi 5/6. Peningkatan secara bermakna aktivitas GPX jantung pada semua kelompok pasca nefrektomi 5/6 (p<0.05) dibandingkan kelompok kontrol normal menunjukkan bahwa jantung tikus uremia masih berada pada fase kompensasi, yaitu mekanisme adaptasi jantung dan fungsi jantung belum terganggu meskipun terjadi sedikit fibrosis jantung.

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ABSTRACTBackground: Uremic cardiomyopathy is a heart disease because of abnormalities in the kidneys that is the leading cause of death in patients with chronic kidney disease (CKD). Fluid overload and oxidative stress play an important role in its pathogenesis. Quercetin, as an antioxidant, has cardioprotective effect. To the best of our knowledge, its effect on uremic cardiomyopathy has not been investigated yet. This study aims to determine the effect of quercetin on uremic cardiomyopathy using 5/6 nephrectomy model in rats. Methods: Uraemia was induced surgically in male Sprague-Dawley rats via 5/6 nephrectomy (SNX). Quercetin was administered per orally at a dose of 100 mg/kgBW/day for 8 weeks prior to sacrifice. Meanwhile captopril was administered per orally at a dose of 10 mg/kgBW/day. Oxidative stress was assessed using tiobarbituric acid reactive substances reaction then glutathione peroxidase (GPX) activity was determined to study on antioxidant mechanism. Myocardial fibrosis was analyzed using Massons? Trichrome staining and NTproBNP was measured as a marker of cardiac function. Data was analyzed using ANOVA. Results: Nephrectomy 5/6 had no effects on plasma NT - proBNP, cardiac and plasma MDA, but induced mild myocardial fibrosis and increased cardiac GPX activity significantly (p<0.05). However, administration of quercetin and captopril had no effects on plasma NT - proBNP, cardiac and plasma MDA, myocardial fibrosis and GPX activity in uremic rats? heart induced by 5/6 nephrectomy.Conclusion: Uremic rats? heart induced by 5/6 nephrectomy demonstrated mild myocardial fibrosis but preserved in vivo cardiac function. Increased GPX activity in uremic rats? heart compared to normal control (p<0.05) suggests induction of antioxidant defense mechanisms that might not be exhausted yet highlighting a compensatory phase which was unchanged following chronic either quercetin or captopril administration, Background: Uremic cardiomyopathy is a heart disease because of abnormalities in the kidneys that is the leading cause of death in patients with chronic kidney disease (CKD). Fluid overload and oxidative stress play an important role in its pathogenesis. Quercetin, as an antioxidant, has cardioprotective effect. To the best of our knowledge, its effect on uremic cardiomyopathy has not been investigated yet. This study aims to determine the effect of quercetin on uremic cardiomyopathy using 5/6 nephrectomy model in rats. Methods: Uraemia was induced surgically in male Sprague-Dawley rats via 5/6 nephrectomy (SNX). Quercetin was administered per orally at a dose of 100 mg/kgBW/day for 8 weeks prior to sacrifice. Meanwhile captopril was administered per orally at a dose of 10 mg/kgBW/day. Oxidative stress was assessed using tiobarbituric acid reactive substances reaction then glutathione peroxidase (GPX) activity was determined to study on antioxidant mechanism. Myocardial fibrosis was analyzed using Massons’ Trichrome staining and NTproBNP was measured as a marker of cardiac function. Data was analyzed using ANOVA. Results: Nephrectomy 5/6 had no effects on plasma NT - proBNP, cardiac and plasma MDA, but induced mild myocardial fibrosis and increased cardiac GPX activity significantly (p<0.05). However, administration of quercetin and captopril had no effects on plasma NT - proBNP, cardiac and plasma MDA, myocardial fibrosis and GPX activity in uremic rats’ heart induced by 5/6 nephrectomy.Conclusion: Uremic rats’ heart induced by 5/6 nephrectomy demonstrated mild myocardial fibrosis but preserved in vivo cardiac function. Increased GPX activity in uremic rats’ heart compared to normal control (p<0.05) suggests induction of antioxidant defense mechanisms that might not be exhausted yet highlighting a compensatory phase which was unchanged following chronic either quercetin or captopril administration]"

"[ABSTRAKLatar Belakang: Penyakit ginjal kronik (PGK) merupakan penyakit progresif dan ireversibel yang mempunyai berbagai komplikasi serius serta belum ada terapi yang dapat memperbaiki kerusakan ginjal yang telah terjadi. Beberapa studi menunjukkan stres oksidatif berperan dalam patogenesis penyakit ini. Stres oksidatif terjadi akibat ketidakseimbangan produksi ROS dan pertahanan antioksidan. Nrf2 merupakan faktor transkripsi yang terlibat dalam mekanisme pertahanan sel dalam mengatasi stres oksidatif. Penelitian ini bertujuan untuk mengetahui aktivitas kuersetin sebagai aktivator Nrf2 dalam menghambat progresivitas penyakit ginjal yang diinduksi nefrektomi 5/6.Metode: Tikus Sprague-Dawley jantan dikelompokkan secara acak dalam kelompok kontrol normal (C), kontrol nefrektomi 5/6 (Nx), nefrektomi 5/6 yang diberi kuersetin dengan dosis 100 mg/kgbb/hari/p.o. (NxQ), nefrektomi 5/6 dan diberi kaptopril dengan dosis 10 mg/kgbb/hari/p.o. (NxK). Hewan coba diterminasi diakhir perlakuan untuk diambil darah, urin, dan organ ginjalnya. Pemeriksaan yang dilakukan adalah pemeriksaan proteinuria, kreatinin urin dan plasma, ureum plasma, kadar MDA plasma dan jaringan, aktivitas glutation peroksidase (GPx), kerusakan jaringan (histopatologi) dan ekspresi Nrf2 (imunohistokimia).Hasil: Hasil penelitian menunjukkan bahwa nefrektomi 5/6 dapat menimbulkan peningkatan proteinuria, ureum plasma, dan derajat fibrosis ginjal secara signifikan. Nefrektomi 5/6 cenderung meningkatkan kreatinin plasma, kadar MDA ginjal, aktivitas GPx, dan menurunkan MDA plasma serta ekspresi Nrf2. Kuersetin tidak mempengaruhi proteinuria, ureum dan kreatinin plasma, dan derajat fibrosis ginjal. Kuersetin cenderung menurunkan kadar MDA dan meningkatkan aktivitas enzim GPx serta ekspresi Nrf2.Kesimpulan: Kuersetin tidak mempengaruhi proteinuria, ureum dan kreatinin plasma serta kerusakan struktur jaringan atau fibrosis ginjal. Kuersetin cenderung menurunkan kadar MDA dan meningkatkan aktivitas enzim GPx serta cenderung meningkatkan ekspresi Nrf2.

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ABSTRACTBackground: Chronic Kidney Disease (CKD) is a progressive and irreversible condition that has several serious complications and currently there has no single therapy that can repair kidney damage was occurred. Some studies suggest a role of oxidative stress in the pathogenesis of this disease. Oxidative stress is caused by an imbalance of ROS production and antioxidant defenses. Nrf2 is a transcription factor involved in cell defense mechanisms againts oxidative stress. This study was aimed to determine the quercetin activity as Nrf2 activator in inhibit the progression of 5/6 nephrectomy induced CKD in male rats.Method: Sprague-Dawley rats were randomly divided into normal control group (C), untreated 5/6 nephrectomy (Nx), quercetin-treated 5/6 nephrectomy, NxQ (100 mg / kg / day orally), captopril-treated 5/6 nephrectomy, NxK (10 mg / kg / day orally). Animal models was sacrificed at the end of intervention to take blood to measure creatinine, urea, and MDA, urine to measure protein and creatinine, and kidney organ to measure levels of MDA, glutathione peroxidase (GPx) activity, and renal damage (histopathology) and Nrf2 expression (immunohistochemistry).Results: The results showed that 5/6 nephrectomy may cause an increased of proteinuria, plasma urea, and grade of renal fibrosis significantly. 5/6 nephrectomy has trend to increased plasma creatinine, renal MDA levels, GPx activity, and decreased plasma MDA and Nrf2 expression. Quercetin did not decrease proteinuria, plasma urea and creatinine, and renal fibrosis grading. Quercetin tend to reduced levels of MDA, increased GPx enzyme activity, and expression of Nrf2.Conclusion: Quercetin does not affect proteinuria, plasma urea,plasma creatinine, and tissue damage or kidney fibrosis. Quercetin tend to reduced levels of MDA and increased the activity of GPx and Nrf2 expression.;Background: Chronic Kidney Disease (CKD) is a progressive and irreversible condition that has several serious complications and currently there has no single therapy that can repair kidney damage was occurred. Some studies suggest a role of oxidative stress in the pathogenesis of this disease. Oxidative stress is caused by an imbalance of ROS production and antioxidant defenses. Nrf2 is a transcription factor involved in cell defense mechanisms againts oxidative stress. This study was aimed to determine the quercetin activity as Nrf2 activator in inhibit the progression of 5/6 nephrectomy induced CKD in male rats.Method: Sprague-Dawley rats were randomly divided into normal control group (C), untreated 5/6 nephrectomy (Nx), quercetin-treated 5/6 nephrectomy, NxQ (100 mg / kg / day orally), captopril-treated 5/6 nephrectomy, NxK (10 mg / kg / day orally). Animal models was sacrificed at the end of intervention to take blood to measure creatinine, urea, and MDA, urine to measure protein and creatinine, and kidney organ to measure levels of MDA, glutathione peroxidase (GPx) activity, and renal damage (histopathology) and Nrf2 expression (immunohistochemistry).Results: The results showed that 5/6 nephrectomy may cause an increased of proteinuria, plasma urea, and grade of renal fibrosis significantly. 5/6 nephrectomy has trend to increased plasma creatinine, renal MDA levels, GPx activity, and decreased plasma MDA and Nrf2 expression. Quercetin did not decrease proteinuria, plasma urea and creatinine, and renal fibrosis grading. Quercetin tend to reduced levels of MDA, increased GPx enzyme activity, and expression of Nrf2.Conclusion: Quercetin does not affect proteinuria, plasma urea,plasma creatinine, and tissue damage or kidney fibrosis. Quercetin tend to reduced levels of MDA and increased the activity of GPx and Nrf2 expression., Background: Chronic Kidney Disease (CKD) is a progressive and irreversible condition that has several serious complications and currently there has no single therapy that can repair kidney damage was occurred. Some studies suggest a role of oxidative stress in the pathogenesis of this disease. Oxidative stress is caused by an imbalance of ROS production and antioxidant defenses. Nrf2 is a transcription factor involved in cell defense mechanisms againts oxidative stress. This study was aimed to determine the quercetin activity as Nrf2 activator in inhibit the progression of 5/6 nephrectomy induced CKD in male rats.Method: Sprague-Dawley rats were randomly divided into normal control group (C), untreated 5/6 nephrectomy (Nx), quercetin-treated 5/6 nephrectomy, NxQ (100 mg / kg / day orally), captopril-treated 5/6 nephrectomy, NxK (10 mg / kg / day orally). Animal models was sacrificed at the end of intervention to take blood to measure creatinine, urea, and MDA, urine to measure protein and creatinine, and kidney organ to measure levels of MDA, glutathione peroxidase (GPx) activity, and renal damage (histopathology) and Nrf2 expression (immunohistochemistry).Results: The results showed that 5/6 nephrectomy may cause an increased of proteinuria, plasma urea, and grade of renal fibrosis significantly. 5/6 nephrectomy has trend to increased plasma creatinine, renal MDA levels, GPx activity, and decreased plasma MDA and Nrf2 expression. Quercetin did not decrease proteinuria, plasma urea and creatinine, and renal fibrosis grading. Quercetin tend to reduced levels of MDA, increased GPx enzyme activity, and expression of Nrf2.Conclusion: Quercetin does not affect proteinuria, plasma urea,plasma creatinine, and tissue damage or kidney fibrosis. Quercetin tend to reduced levels of MDA and increased the activity of GPx and Nrf2 expression.]"

"Latar Belakang: Penyakit Ginjal Kronik PGK merupakan masalah kesehatan di seluruh penjuru dunia. PGK menjadi penyebab menurunnya kualitas hidup penderitanya sekaligus meningkatkan risiko kematian. Penyakit Ginjal Kronik ditandai dengan terjadinya kerusakan ginjal dalam waktu lama dan progresif. Gangguan pada PGK berkaitan dengan kejadian stres oksidatif, yaitu keadaan di mana Reactive Oxygen Species ROS terbentuk melebihi pertahanan antioksidan. Kuersetin sebagai bagian keluarga flavonoid diketahui memiliki aktivitas antioksidan. Penelitian sebelumnya mendapatkan bahwa pemberian kuersetin mampu meningkatkan ekspresi protein Nuclear factor related erythroid factor 2 Nrf2 di dalam nukleus pada tikus yang mengalami PGK. Penelitian ini merupakan penelitian lanjutan untuk mengkonfirmasi apakah peningkatan ekspresi protein Nrf2 di dalam nukleus terjadi pada tahap transkripsi.Metode: Jaringan ginjal tikus Sprague-Dawley dari penelitian terdahulu yang tersimpan pada suhu -80oC, diukur ekspresi mRNA Nrf2, Keap1dan HO1menggunakan qRT PCR. Terdapat 4 kelompok penelitian yaitu kelompok kontrol normal, kelompok dengan nefrektomi 5/6 berturut-turut diberi CMC 0,5 , kaptopril 10 mg/kgBB, dan kuersetin 100 mg/kgBB. Ekspresi mRNA Nrf2, Keap1 dan HO1dianalisis statistik menggunakan uji ANOVA yang dilanjutkan dengan multiple comparison post hoc dengan LSD, Kruskal-Wallis untuk data yang tidak memenuhi syarat uji ANOVA dimana perbedaan dianggap bermakna secara statistik bila p.

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Background Chronic Kidney Disease CKD has been a problem all around the world as it causes the decrease of life quality and also raises the risk of death. Chronic kidney disease characterized with long time and progressively kidney failure. The alteration of CKD correlated to oxidative stress, a condition when Reactive oxygen species ROS produced more than antioxidant defense. Quercetin as a part of flavonoid, has been known to have an antioxidant activity. It has been showed in the previous study that quercetin increased intra nuclear Nuclear factor related erythroid factor 2 Nrf2 . This study proposed to confirm whether the increase of nuclear NRF2 is happened in transcription event.Method Kidney tissue of Sprague Dawley rat from previous study which had been saved in 80oC had measured the expression of Nrf2, Keap1 and HO1 mRNA by qRT PCR. There were 4 groups as the previous study, normal control group, 5 6 nephrectomy plus consecutively 0,5 CMC, 10 mg kgBW captopril, and 100 mg kgBW quercetin. Expression of Nrf2, Keap1 and HO1 mRNA had been analyzed statistically with ANOVA test and LSD multiple comparison post hoc. For data that are not fit to analyzed with ANOVA would be analyzed with Kruskal Wallis and Mann Whitney. The data considered as significantly different by p."

"Saat ini, pengembangan sediaan fitofarmaka perlu dilakukan suatu uji quality control (QC) untuk menjamin mutu dan keamanan dari sediaan tersebut. Oleh karena itu, standardisasi dan metode analisis yang valid baik pada bahan baku maupun produk jadi merupakan faktor penting dalam pengembangan sediaan fitofarmaka. Sediaan fitofarmaka yang digunakan untuk mengobati diare banyak mengandung ekstrak daun jambu biji (Psidium guajava Linn) dan rimpang kunyit (Curcuma domestica Val). Biomarker dari ekstrak daun jambu biji yaitu kuersetin, sedangkan biomarker dari ekstrak rimpang kunyit yaitu kurkuminoid. Kadar dari kurkuminoid dan kuersetin dapat dipengaruhi oleh umur tanaman, jenis tanah dan tempat tumbuh.Tujuan penelitian ini untuk mendapatkan kondisi optimum analisis kurkuminoid dan kuersetin serta mengetahui kadarnya dalam tablet obat diare yang mengandung ekstrak daun jambu biji dan rimpang kunyit dengan menggunakan metode Kromatografi Lapis Tipis Kinerja Tinggi (KLTKT) densitometri. Hasil penelitian menunjukkan fase gerak terbaik adalah toluenaseton-metanol-asam format (46:8:5:1) pada panjang gelombang 426 nm untuk kurkuminoid dan 303 nm untuk kuersetin. Kurva kalibrasi kurkuminoid antara 612-1632 ppm, dan kuersetin antara 81,12-405,6 ppm. Batas deteksi dan kuantitasi kurkuminoid berturut-turut sebesar 100,65 ppm dan 335,49 ppm, sedangkan batas deteksi dan kuantitasi kuersetin berturut-turut sebesar 17,92 ppm dan 59,72 ppm. Kadar rata-rata kurkuminoid sebelum dikoreksi sebesar 2541,59 μg/g dan kadar rata kuersetin sebelum dikoreksi sebesar 306,55 μg/g. Perolehan kembali kurkuminoid adalah 71,02 % dan kuersetin adalah 94,57 %. Kadar rata-rata kurkuminoid setelah dikoreksi sebesar 3578,70 μg/g dan kadar rata kuersetin setelah dikoreksi sebesar 324,16 μg/g.

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Recently, developing of phytopharmaca needs quality control (QC) test to ensure the quality and safety. Thus, standardization and validation analysis methods of raw materials and product are an important factor in developing of phytopharmaca. The phytopharmaca for diarrhoea treatment contains extract of guava leaves and turmeric rhizome. Biomarker from extract of guava leave is quercetin, while biomarker from turmeric rhizome is curcuminoid. Curcuminoid and quercetin contents are influenced by the age of plants themselves, cultivate type and place of growth.The purpose of this research was to get the analysis method for curcuminoid and quercetin contents in diarrhoea tablet contains extract of guava leaves and turmeric rhizome with using High Performance Thin Layer Chromatography (HPTLC) method densitometry. The result shows toluene-acetone-methanol-formic acid (46:8:5:1) is the best mobile phase at 426 nm for curcuminoid and 303 nm for quercetin. The calibration curve of curcuminoid between 612-1632 ppm, and quercetin between 81,12-405,6 ppm. Limit of Detection (LOD) and Limit of Quantitation (LOQ) of curcuminoid is 100,65 ppm and 335,49 ppm respectively, while Limit of Detection (LOD) and Limit of Quantitation (LOQ) of quercetin is 17,92 ppm and 59,72 ppm respectively. The average content of curcuminoid before corrected is about 2541,59 μg/g and quercetin is 306,55 μg/g. The recovery of curcuminoid is 71,02 % and quercetin 94,57 %."

"Kanker kolorektal merupakan masalah kesehatan masyarakat global dengan prevalensi tinggi yang pengobatannya masih memiliki keterbatasan. Senyawa flavonoid terutama kuersetin dinilai memiliki aktivitas biologis sebagai antikanker, sehingga beberapa senyawa flavonoid lainnya diharapkan juga memiliki aktivitas serupa. Tujuan dari studi ini adalah melakukan analisis secara in-silico dan in-vitro terhadap beberapa senyawa flavonoid terutama kuersetin dan turunannya sebagai agen apoptosis sel kanker kolorektal HT-29. Metode yang dilakukan secara in-silico meliputi jejaring farmakologi dan simulasi molekuler. Senyawa terbaik berdasarkan analisis in-silico diuji secara in-vitro dengan menilai aktivitas sitotoksisitasnya pada sel HT-29 menggunakan metode MTT Assay dan apoptosisnya dianalisis menggunakan flow cytometry. Protein target yang memiliki interaksi dengan kuersetin dan senyawa turunannya yaitu AKT1, APAF1, BCL2, CASP3, MAPK1 dan CASP9. Berdasarkan analisis prediksi ADMET, kuersetin dan turunannya masuk dalam kategori aman sebagai kandidat obat. Dua senyawa terbaik berdasarkan analisis in-silico yakni isoramnetin dan isokuersitrin dipilih untuk diuji secara in-vitro. Aktivitas sitotoksik kuersetin, isoramnetin dan isokuersitrin terhadap sel HT-29 dinyatakan dengan nilai CC50 berturut-turut 158,92mm + 5,4, 65,52mm + 5,0 dan 47,59mm + 2,5. Aktivitas apoptosis mencapai 16,7% hingga 62,4% jika dibandingkan dengan kontrol sel. Isoramnetin dan Isokuersitrin sebagai senyawa flavonoid turunan kuersetin berpotensi sebagai agen apoptosis sel kanker kolorektal HT-29.Kanker kolorektal merupakan masalah kesehatan masyarakat global dengan prevalensi tinggi yang pengobatannya masih memiliki keterbatasan. Senyawa flavonoid terutama kuersetin dinilai memiliki aktivitas biologis sebagai antikanker, sehingga beberapa senyawa flavonoid lainnya diharapkan juga memiliki aktivitas serupa. Tujuan dari studi ini adalah melakukan analisis secara in-silico dan in-vitro terhadap beberapa senyawa flavonoid terutama kuersetin dan turunannya sebagai agen apoptosis sel kanker kolorektal HT-29. Metode yang dilakukan secara in-silico meliputi jejaring farmakologi dan simulasi molekuler. Senyawa terbaik berdasarkan analisis in-silico diuji secara in-vitro dengan menilai aktivitas sitotoksisitasnya pada sel HT-29 menggunakan metode MTT Assay dan apoptosisnya dianalisis menggunakan flow cytometry. Protein target yang memiliki interaksi dengan kuersetin dan senyawa turunannya yaitu AKT1, APAF1, BCL2, CASP3, MAPK1 dan CASP9. Berdasarkan analisis prediksi ADMET, kuersetin dan turunannya masuk dalam kategori aman sebagai kandidat obat. Dua senyawa terbaik berdasarkan analisis in-silico yakni isoramnetin dan isokuersitrin dipilih untuk diuji secara in-vitro. Aktivitas sitotoksik kuersetin, isoramnetin dan isokuersitrin terhadap sel HT-29 dinyatakan dengan nilai CC50 berturut-turut 158,92mm + 5,4, 65,52mm + 5,0 dan 47,59mm + 2,5. Aktivitas apoptosis mencapai 16,7% hingga 62,4% jika dibandingkan dengan kontrol sel. Isoramnetin dan Isokuersitrin sebagai senyawa flavonoid turunan kuersetin berpotensi sebagai agen apoptosis sel kanker kolorektal HT-29.......Colorectal cancer is a global public health problem with a high prevalence, and its treatment still has limitations. Flavonoid compounds, especially quercetin, are considered to have biological activity as an anticancer, so several other flavonoid compounds are also expected to have similar activity. This study aimed to perform in-silico and in-vitro analysis of several flavonoid compounds, especially quercetin and its derivatives as apoptotic agents for colorectal cancer cells HT-29. The in silico method includes network pharmacology and molecular simulations. The best compounds based on in silico analysis were tested in-vitro by assessing their cytotoxic activity in HT-29 cells using the MTT Assay method. Their apoptosis was analyzed using flow cytometry. Target proteins interacting with quercetin and its derivatives are AKT1, APAF1, BCL2, CASP3, MAPK1 and CASP9. Based on ADMET prediction analysis, quercetin and its derivatives are included in the safe category as drug candidates. The best compounds based on in-silico analysis, isorhamnetin and isoquercitrin, were selected to be tested in-vitro. The cytotoxic activity of quercetin, isorhamnetin and isoquercitrin against HT-29 cells was expressed by CC50 values of 158.92 mm + 5.4, 65.52 mm + 5.0 and 47.59 mm + 2.5, respectively. Apoptotic activity reached 16.7% to 62.4% when compared to control cells. Isoramnetin and isoquercitrin, flavonoid compounds derived from quercetin, have potential apoptotic agents for HT-29 colorectal cancer cells."

"Bawang dayak mengandung naphtoquinon sedangkan herba ceplukan mengandung quersetin dan physalin yang memiliki efek antihipertensi. Penelitian ini bertujuan untuk menguji efektivitas antihipertensi kombinasi ekstrak bawang dayak dan herba ceplukan. Deksametason 0,02mg dan larutan NaCl 2,5% digunakan sebagai penginduksi hipertensi. Kelompok normal: akuades, kontrol negatif: CMC-Na 1%, kontrol positif: kaptopril 0,45mg, ekstrak bawang dayak 121,5mg, ekstrak herba ceplukan 232,5mg, dosis kombinasi 1 (BD 40.5mg + HC 77,5mg), dosis kombinasi 2 (BD 81mg + HC 155mg), dan  dosis kombinasi 3 (BD 121,5 mg + HC 232,5mg). Tekanan darah dan berat badan diukur setiap minggu selama 49 hari. Hasil uji antihipertensi menunjukan bahwa, dosis kombinasi 1, 2, dan 3 efektif menurunkan hipertensi dengan p<0,05 dibandingkan dengan tekanan darah pada hari 28. Dosis kombinasi 1 menurunkan tekanan sistolik 32 mmHg (27%), diastolik 29 mmHg (37%), dan MAP 30 mmHg (33%). Dosis kombinasi 1 sudah  cukup untuk menurunkan tekanan darah, kadar angiotensin 2, malondialdehid, VEGF, dan kaveolin-1 dalam plasma serta mengurangi penebalan dinding aorta. ......Dayak onions contain naphtoquinone while herba ceplukan  contain quercetin and physalin which have antihypertensive effects. This study aimed to test the antihypertensive effectiveness of a combination of dayak onion extract and herba ceplukan. Dexamethasone 0.02mg and 2.5% NaCl solution are used as inducers of hypertension. Normal group: aquades, negative control: CMC-Na 1%, positive control: captopril 0.45mg, dayak onion extract 121.5 mg, herba ceplukan  extract 232.5 mg, combination dose 1 (BD 40.5mg + HC 77.5mg), combination dose 2 (BD 81 mg + HC 155 mg), and combination dose 3 (BD 121.5 mg + HC 232.5mg). Blood pressure and weight were measured weekly for 49 days. The results of the antihypertensive test showed that the combined dose of 1, 2, and 3 was effective in reducing hypertension by p<0.05 compared to blood pressure on day 28. The combination dose 1 lowered systolic pressure by 32 mmHg (27%), diastolic by 29 mmHg (37%), and MAP by 30 mmHg (33%). A combination dose of 1 is sufficient to lower blood pressure, levels of angiotensin 2, malondialdehyde, VEGF, and kaveolin-1 in plasma and reduce thickening of the aortic wall. "

"Zat besi merupakan salah satu mineral penting dalam darah. Di dalam tubuh, zat besi disimpan dalam suatu protein penyimpan yang disebut dengan feritin, sehingga feritin merupakan salah satu indikator penting kadar zat besi dalam darah. Teknik deteksi senyawa feritin yang sederhana seperti metode elektrokimia memiliki keunggulan berupa batas deteksi rendah serta preparasi sampel sederhana. Salah satu senyawa yang dapat digunakan adalah kuersetin, senyawa elektroaktif yang memiliki interaksi kuat dengan feritin. Penelitian ini memanfaatkan metode elektrokimia berbasis senyawa kuersetin untuk diaplikasikan sebagai sensor feritin. Studi elektrokimia senyawa kuersetin menggunakan metode differential pulse voltammetry (DPV) pada elektroda cetak karbon menunjukkan bahwa interaksi antara kuersetin dan ferritin menyebabkan terjadinya penurunan puncak arus oksidasi kuersetin pada potensial +0,09 V (vs. A /AgCl). Penurunan puncak arus ini linier terhadap peningkatan konsentrasi kuersetin, dengan rentang linear dinamis pada konsentrasi 0-10 dan 10-1000 ng/mL. Sensor ini memiliki nilai LOD 1,96 ng/mL, LOQ 6,54 ng/mL, dan sensitivitas 7,79 µA/(ng/mL)/cm2 pada rentang 1-10 ng/mL serta LOD 145,5 ng/mL, LOQ 483,9 ng/mL, dan sensitivitas 0,03 µA/(ng/mL)/cm2 pada rentang 10-1000 ng/mL. Kemampuan keberulangan sensor ini cukup baik dengan RSD sebesar 2,06% untuk sepuluh kali pengukuran. Selain itu, sensor ini bersifat selektif terhadap beberapa interferen meliputi asam urat, asam askorbat, dan glukosa terlihat dari respon yang tidak jauh berbeda antara pengukuran dengan dan tanpa interferen (98-99%). Secara keseluruhan sensor feritin berbasis senyawa kuersetin ini memiliki performa yang baik.......Iron is one of the most important minerals in the blood. In our body, iron is stored in a storage protein called ferritin. Thus, ferritin is an important indicator of serum iron level. One of ferritin detection methods is electrochemical method that has lower detection limit and require less preparations. Quercetin can be employed as recognition element since it is an electroactive compound that interacts strongly with ferritin. In this study, electrochemical method based on quercetin is used as ferritin sensor. Electrochemical study of quercetin using Differential Pulse Voltammery (DPV) on screen-printed carbon electrode shows that interaction between quercetin and ferritin cause significant decrease in quercetin oxidation peak potential at +0.09 V (vs. Ag/AgCl). The increase of ferritin concentration is directly proportional to the decrease of quercetin oxidation peak potential, showing dynamic linear range at 0-10 and 10-1000 ng/mL of ferritin. This sensor has LOD of 1.96 ng/mL, LOQ of 6.54 ng/mL, and sensitvity of 7.79 µA/(ng/mL)/cm2 in 1-10 ng/mL range and LOD of 145.5 ng/mL, LOQ of 483.8 ng/mL, and sensitivity of 0.03 µA/(ng/mL)/cm2 in 10-1000 ng/mL range. This sensor shows great repeatibility over ten repeated measurements showing %RSD of 2.06%. Interference test shows that this sensor is selective towards several interferents such as uric acid, ascorbic acid, and glucose, showing similar response (98-99%) than that of the solution with no interference. Overall, this ferritin sensor based on quercetin exhibits a good performance."

"Kuersetin memiliki banyak aktivitas farmakologi tetapi bioavailabilitas dan absorpsi kuersetin rendah. Tujuan dari penelitian ini adalah mendapatkan formula mikrosfer fitosom kuersetin untuk pemberian secara oral mengevaluasi formulasi tersebut pada uji ketersediaan hayati menggunakan tikus Sprague Dawley. Optimasi formula fitosom telah dilakukan pada penelitian ini, yaitu F1, F2, F3 dengan konsentrasi kuersetin berturut-turut adalah 1%, 1,5%, dan 2%.Hasil menunjukkan bahwa F1 adalah formula terbaik dengan morfologi vesikel sferis, efisiensi penjerapan 96,57 ± 5,61%, ukuran partikel rata-rata 266,6 ± 1,37 nm, indeks polidispersitas 0,388 ± 0,01 dan potensial zeta -29,43 ± 0,75 mV sehingga digunakan pada formulasi mikrosfer. Mikrosfer yang dibuat terdiri dari dua formula, yaitu mikrosfer fitosom (MF) dan mikrosfer non fitosom (MNF).Pembuatan mikrosfer dilakukan dengan proses enkapsulasi menggunakan metode semprot kering. Formula MF yang dihasilkan berbentuk sferis, dengan ukuran partikel 1154,67 ± 69,10 nm dan efisiensi penjerapan 98,56 ± 0,05 %. Uji ketersediaan hayati dilakukan terhadap kedua formula dan suspensi oral kuersetin sebagai pembanding. Konsentrasi maksimum (Cmax) untuk MF, MNF, dan suspensi oral berturut-turut adalah 213,33 ± 73,51 ng/mL, 92,79 ± 16,88 ng/mL, 95,01 ± 2,66 ng/mL. Hasil uji ketersediaan hayati formula mikrosfer fitosom kuersetin memberikan profil farmakokinetik yang lebih baik dibandingkan mikrosfer non fitosom dan suspensi oral.

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Quercetin has many pharmacological activities but it has low bioavailability and absorption. The purpose of this research is to get quercetin phytosome microspheres formula for oral administration and evaluate it in the bioavailability study using Sprague Dawley rats. Phytosome formula optimization has been done in this study, namely F1, F2, F3 with concentration of quercetin in a row is 1%, 1.5% and 2%.The results show that F1 is the best formula with spherical vesicle morphology, entrapment efficiency 96.57 ± 5.61%, average particle size 266.6 ± 1.37 nm, polydispersity index 0.01 ± 0.388 and zeta potential -29,43 ± 0.75 mV, so it was incorporated into microspheres formulation. Microspheres made comprised of two formulas, namely phytosome microspheres (MF) and non phytosome microspheres (MNF).Microspheres was made with the encapsulation process by spray drying method. MF formula produced has spherical morphology, with particle size 1154.67 ± 69.10 nm and the entrapment efficiency of 98.56 ± 0.05%. Bioavailability test conducted on both formula and oral suspension quercetin as a comparison. The maximum concentration (Cmax) for MF, MNF, and oral suspension respectively are 213.33 ± 73.51 ng/mL, 92.79 ± 16.88 ng/mL, 95.01 ± 2.66 ng/mL. The bioavailability study of quercetin phytosome microspheres formula provide a better pharmacokinetic profile than non phytosome microspheres and oral suspensions formula."

"Di Indonesia, daun Babandotan (Ageratum conyzoides (L.) L.) (EAC) dan herba Rumput Mutiara (Oldenlandia corymbosa L.) (EOC) telah digunakan secara empiris turun-temurun untuk mengobati penyakit sendin dengan cara ditumbuk kemudian dioleskan. Kuersetin (KU) dan asam ursolat (AU) yang merupakan zat aktif di dalam ekstrak tersebut memiliki aktivitas antiinflamasi pada hewan model yang diinduksi osteoartritis. Di dalam penelitian ini, kombinasi ekstrak babandotan dan rumput mutiara serta kombinasi kuersetin dan asam ursolat diformulasikan dalam sistem pembawa nanoemulsi sehingga memiliki karakteristik fisik yang baik serta dapat menghambat proses inflamasi dan dapat digunakan sebagai obat osteoartritis. Sebanyak 50 (lima puluh) ekor tikus dibagi dalam 10 kelompok (n=5) yaitu: (1) kelompok kontrol normal (normal) (2) kelompok kontrol negatif (negatif) (3) kelompok kombinasi EAC-EOC (EAC-EOC) (4) kelompok EAC tunggal (EAC) (5) kelompok EOC tunggal (EOC) (6) kelompok kombinasi KU-AU (KU-AU) (7) kelompok KU tunggal (KU) (8) kelompok AU tunggal (9) kelompok kombinasi KU-AU non-nano (Emulgel KU-AU) (10) kelompok kontrol positif (positif). Pada hari ke-0, tikus diinduksi monoiodoasetat secara intraartikular 3,0mg/0.05 mL kecuali kelompok normal. Pemberian sediaan topikal sesuai dengan kelompok dosis dilakukan mulai hari ke-29. Dilakukan evaluasi terhadap volume udem (setiap 7 hari), analisis kadar sitokin serum dengan enzyme-linked immunoabsorbent assay (ELISA) dan histopatologi serta imunohistokimia pada hari ke-57. Volume udem lutut tikus tidak berbeda bermakna dengan kelompok normal sejak hari ke-42. Penurunan kadar sitokin serum terjadi pada biomarker Protein S100A8, Interleukin-1β, inducible nitric oxide synthase (iNOS), matrix metalloproteinase-13 (MMP-13), a disintegrin and metalloproteinase thrombospondin-like motifs-5 (ADAMTS-5), Kolagen Tipe 2 dan Aggrecan Core Protein. Perbedaan bermakna semua kelompok perlakuan dengan kelompok negatif terjadi pada biomarker penanda proses inflamasi yaitu Protein S100A8, Interleukin-1ß dan iNOS (#P<0,05). Hasil evaluasi histopatologi dan imunohistokimia menunjukkan bahwa terjadi penghambatan degradasi proteoglikan. Sediaan nanoemulgel yang dikembangkan baik komposisi tunggal maupun kombinasi dapat memperbaiki kerusakan kartilago yang bermanfaat sebagai obat osteoartritis.

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In Indonesia, babandotan leaves (ageratum conyzoides (L.) L.) (ACE) and pearl grass herbs (Oldenlandia corymbosa L.) (OCE) have been used empirically as topical preparation for traditional medicine in the treatment of joint disease. Their active compound namely quercetin (QU) and ursolic (UA) acid has appearance anti-inflammatory activity in osteoarthritis (OA) animal model. We investigated nanoemulgel of combination QU and UA as well as the combination ACE and OCE from nanoemulsion carrier systems as the new drug focused on plant-based natural products with a good physical characteristic that inhibit inflammatory process and applied in managing osteoarthritis (OA). Fifty animals were randomly designated to the 10 groups (n=5) as follows: (1) normal control group (Normal), (2) negative control groups (negative), (3) combination ACE-OCE, (4) single ACE, (5) single OCE, (6) combination QU-UA, (7) single QU, (8) single UA, (9) combination QU-UA non-nano formula (emulgel QU-UA), (10) positive control group (positive). Rats were receiving intraartikular monoiodoacetate injection 3.0mg/0.05 mL on day 0 exluding for normal control group. All groups were administered topical preparations allow to each dose group on day 29. We evaluated knee edema profile (every 7 days), serum cytokine level (on day 57) with enzyme-linked immunoabsorbent assay (ELISA) and histopatological and immunhostochemistry evaluation. Since day 42, knee edema profile of all group treatment has been similar with normal control group (p>0.05). Serum cytokines level for some biomarkers, such as S100A8 Protein, Interleukin-1β, inducible nitric oxide synthase (iNOS), matrix metalloproteinase-13 (MMP-13), a disintegrin and metalloproteinase thrombospondin-like motifs-5 (ADAMTS-5), Collagen Type II and Aggrecan Core Protein were decrease. A significant difference compared with negative group showed for all groups treatment on measurement of inflammation process biomarker of S100A8 Protein, IL-1β, and iNOS (#P<0.05). Based on histological and immunohistochemistry evaluation showed that there was inhibition of proteoglycan degradation. The developed nanoemulgel ACE-OCE and QU-UA either combination or not has good physical characteristic and promising effect to enhance MIA induced cartilage damage as potential therapeutic agent for OA and encouraging to conduct further study as clinical trials. "