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"ABSTRACTThree types of cyclopentanone derivatives have been synthesized from aromatic aldehyde and ketone derivatives undera base condition through aldol condensation. These cyclopentanone products were 2,5-dibenzylidene-cyclopentanone (a), 2,5-bis-(4-hydroxy-benzylidene)-cyclopentanone (b),and 2,5-bis-(4-hydroxy-benzylidene)-cyclopentanone (c)which has a yield of 63-99%. The chemical structure of these compounds were determined using UV, IR and NMRspectroscopy. In order to clarify the role of hydroxyl and amine moieties, toxic, antioxidant and anti-inflammatoryactivities were carried out. The toxic test indicated that thecompounds showed strong toxicity. In addition, the presenceof hydroxyl and amine groups on both rings of curcumin increased the antioxidant and anti-inflammatory activities."

"Tumor necrosis factor alpha (TNF-alpha) adalah salah satu sitokin proinflamasi yang berperan pada timbulnya cedera iskemia-reperfusi pasien infark miokard akut yang menjalani tindakan intervensi koroner perkutan primer (IKPP). Kolkisin merupakan salah satu obat antiinflamasi yang diduga memiliki pengaruh terhadap TNF-alpha. Penelitian ini bertujuan untuk mengetahui peran kolkisin terhadap kadar TNF-alpha serum pasien infark miokard akut dengan tindakan intervensi koroner perkutan primer. Desain penelitian uji klinis acak tersamar ganda menggunakan sampel sisa serum penelitian dari subjek pasien infark miokard akut Rumah Sakit dr. Cipto Mangunkusumo. Subjek penelitian dibagi menjadi dua kelompok. Kelompok studi diberikan loading dose kolkisin 2 mg, kemudian dilanjutkan 2 x 0,5 mg per hari secara oral selama 48 jam, sementara kelompok kontrol diberikan plasebo. Analisis kadar TNF-alpha menggunakan metode ELISA yang diperiksa sebelum dan 48 jam pasca-IKPP untuk mendapatkan delta perubahan kadar TNF-alpha. Terdapat 64 subjek yang dianalisis terdiri dari 30 kelompok kontrol dan 34 kelompok studi. Delta kadar TNF-alpha pasca-IKPP kelompok kontrol (2,2) terhadap delta kadar TNF-alpha kelompok studi (0,7). Penelitian ini merupakan penelitian pertama tentang pengaruh kolkisin terhadap kadar TNF-alpha pada pasien infark miokard akut dengan tindakan intervensi koroner perkutan primer di Indonesia. Pengukuran TNF-alpha perlu dilakukan lebih dari dua kali untuk melihat dinamika kadar TNF-alpha pada pasien infark miokard akut yang menjalani tindakan intervensi koroner perkutan primer dan penelitian lanjutan diperlukan untuk menilai peran kolkisin sebagai obat antiinflamasi dengan pemeriksaan menggunakan metoda ELISA dengan reagen high-sensitive.

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Tumor necrosis factor alpha (TNF-alpha) is a proinflammatory cytokine that plays a role in the emergence of ischemia-reperfusion injury in patients with acute myocardial infarction undergoing primary percutaneous coronary intervention (PCI). Colchicine is an anti-inflammatory drug believed to affect TNF-alpha. This study aimed to determine the role of colchicine on serum TNF-alpha levels in acute myocardial infarct patients undergoing primary percutaneous coronary intervention. The research design was a double-blind, randomized clinical trial using residual research serum samples from patients with acute myocardial infarction at Dr. Hospital. Cipto Mangunkusumo. The research subjects were divided into two groups. The study group was given a loading dose of 2 mg colchicine and then continued at 2 x 0.5 mg per day orally for 48 hours, whereas the control group was given a placebo. Analysis of TNF-alpha levels using the ELISA method was performed before and 48 hours after primary percutaneous coronary intervention to obtain the delta of changes in TNF-alpha levels. There were 64 subjects analyzed, comprising 30 control groups and 34 study groups. The delta of TNF-alpha levels post-PCI in the control group (2.2) compared with the delta of TNF-alpha levels in the study group (0.7). This is the first study on the effect of colchicine on TNF-alpha levels in acute myocardial infarction patients with primary percutaneous coronary intervention in Indonesia. TNF-alpha measurements need to be carried out more than twice to determine the dynamics of TNF-alpha levels in patients with acute myocardial infarction undergoing primary percutaneous coronary intervention, and further research is needed to assess the role of colchicine as an anti-inflammatory drug by ELISA with high-sensitive reagents."

"ABSTRAKAterosklerosis merupakan proses terjadinya penyempitan dan pengerasan pembuluh darah yang disebabkan oleh penimbunan lemak, terutama dalam pembuluh darah arteri. Pada tahun 2016, tercatat bahwa 35% kematian di Indonesia disebabkan oleh penyakit yang terjadi karena aterosklerosis. Beberapa alternatif penyembuhan aterosklerosis adalah dengan mengkonsumsi obat antiaterosklerosis. Namun, obat anti-aterosklerosis yang telah beredar di masyrakat luas saat ini memiliki efek samping yang cukup mengganggu saat dikonsumsi. Kombinasi herbal yang terdiri dari daun tanjung, daun belimbing manis dan temulawak dipercaya secara empirik berperan sebagai jamu antiaterosklerosis yang mengandung senyawa fenolik dan flavonoid yang berpotensi sebagai antioksidan, antihiperglikemik, dan antiinflamasi serta meningkatkan aktivitas imunomodulator dalam tubuh. Pengujian aktivitas antihiperglikemik, antiinflamasi dan aktivitas imunomodulator dilakukan masing-masing terhadap 5 kelompok perlakuan tikus putih jantan yaitu kelompok normal (tanpa perlakuan), kontrol positif (diberikan obat antihiperglikemik/antiinflamasi/imboost), dosis 1 ekstrak jamu (13,5 mg/g BB), dosis 2 ekstrak jamu (18 mg/g BB), dan dosis 3 esktrak jamu (22,5 mg/g BB). Melalui pengujian yang dilakukan, dosis jamu anti-aterosklerosis yang menghasilkan aktivitas imunomodulator yang optimum bervariasi antara dosis 2 dan 3. Dapat disimpulkan bahwa formulasi ekstrak jamu anti-aterosklerosis dapat digunakan sebagai imunomodulator yang mampu untuk meningkatkan dan meregulasi sistem kekebalan tubuh karena diketahui adanya aktivitas antihiperglikemik dan antiinflamasi dari jamu antiaterosklerosis.

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ABSTRACT

Atherosclerosis is a process of narrowing and hardening of the arteries caused by accumulation of fat, especially in arteries. In 2016, it was recorded that 35% of deaths in Indonesia were caused by diseases that occur due to atherosclerosis. Some alternatives to cure atherosclerosis are by taking antiaterosclerosis drugs. However, anti-atherosclerosis drugs that have been circulating in the wider community now have side effects that are quite disturbing when consumed. The combination of herbs consisting of tanjung leaves, sweet starfruit leaves and ginger is empirically believed to act as an antiaterosclerosis herbal medicine containing phenolic and flavonoid compounds that have the potential to be antioxidants, antihyperglycemic, and anti-inflammatory and to increase immunomodulatory activity in the body. Testing of antihyperglycemic, anti-inflammatory and immunomodulatory activities was carried out on each of the 5 treatment groups of male white rats namely normal group (without treatment), positive control (given antihyperglycemic/anti-inflammatory / imboost drug), dose 1 of herbal extract (13.5 mg/g BW), dose 2 of herbal extract (18 mg/g BW), and dose 3 of herbal extracts (22.5 mg/g BW). Through testing, the dosage of anti-atherosclerosis herbs that produce optimum immunomodulatory activity varies between doses 2 and 3. It can be concluded that the formulation of anti-atherosclerosis herbal extract can be used as an immunomodulator that is able to enhance and regulate the immune system because of the known antihyperglycemic and anti-inflammatory activity of anti-atherosclerosis herbs."

"Objective: Garcinia xanthochymus extract has been reported to have several pharmacological properties. This study was conducted to evaluate cytotoxic and anti-inflammatory activities of G. xanthochymus extracts on cell lines. Methods: The roots and stem barks of plant were extracted using maceration method with n-hexane, dichloromethane and methanol, successively. Cytotoxic activity of the extracts was tested against MCF-7 breast adenocarcinoma using MTT assay. Anti-inflammatory study was evaluated using RAW 264.7 mouse macrophage cells. The nitric oxide production in LPS-stimulated cells was measured using Griess reagent. Results: The results of cytotoxic and anti- inflammatory study showed that dichloromethane and n-hexane extracts of root and stem bark exhibited cytotoxic activity in dose-dependent manner. Meanwhile, for anti-inflammatory study, all root extracts together with stem bark dichloromethane and n-hexane extracts reduce NO production in LPS-stimulated cells in dose dependent manner. Conclusions: This finding indicated that G. xanthochymus extracts might become interesting candidate for treatment of cancer and inflammation.;"

"Objective: Garcinia xanthochymus extract has been reported to have several pharmacological properties. This studywas conducted to evaluate cytotoxic and anti-inflammatory activities of G. xanthochymus extracts on cell lines.Methods: The roots and stem barks of plant were extracted using maceration method with n-hexane, dichloromethaneand methanol, successively. Cytotoxic activity of the extracts was tested against MCF-7 breast adenocarcinoma usingMTT assay. Anti-inflammatory study was evaluated using RAW 264.7 mouse macrophage cells. The nitric oxideproduction in LPS-stimulated cells was measured using Griess reagent. Results: The results of cytotoxic and antiinflammatorystudy showed that dichloromethane and n-hexane extracts of root and stem bark exhibited cytotoxicactivity in dose-dependent manner. Meanwhile, for anti-inflammatory study, all root extracts together with stem barkdichloromethane and n-hexane extracts reduce NO production in LPS-stimulated cells in dose dependent manner.Conclusions: This finding indicated that G. xanthochymus extracts might become interesting candidate for treatment ofcancer and inflammation."

"Dehidrozingeron adalah analog kurkumin hasil isolasi dari jahe Zingiber officinale yang diketahui memiliki berbagai aktivitas farmakologis. Walaupun begitu, dehidrozingeron masih belum diakui sebagai obat karena efeknya yang belum optimal. Oleh karena itu, dilakukan modifikasi struktur melalui reaksi Mannich yang diketahui dapat meningkatkan aktivitas farmakologis senyawa. Sintesis dilaksanakan dengan dua metode. Metode pertama dilakukan melalui reaksi kondensasi aldol antara vanilin dan aseton, dilanjutkan dengan reaksi Mannich menggunakan morfolin dan formaldehid. Rendemen crude dan rendemen murni yang dihasilkan pada masing-masing tahap adalah 76,94 dan 32,48 serta 51,83 dan 19,71. Metode kedua dilakukan dengan mensintesis vanilin morfolin dengan reaksi Mannich, dilanjutkan dengan kondensasi aldol menggunakan aseton. Rendemen crude yang dihasilkan adalah 51,19 dan 35,99. Hasil sintesis metode 1 diuji kemurniannya melalui uji KLT dan pengujian jarak lebur. Senyawa dielusidasi dengan spektrofotometri FT-IR, spektrofotometri UV-Vis, spektrometri 1H-NMR, spektrometri 13C-NMR serta MS. Setelah itu, dilaksanakan studi aktivitas antiinflamasi secara in vitro dan in silico. Uji in vitro dilakukan dengan teknik denaturasi albumin. Hasil IC50 yang diperoleh untuk senyawa uji adalah 12.261 M yang menunjukkan aktivitasnya lebih rendah 0,65 kali daripada natrium diklofenak. Nilai ?G yang diperoleh melalui AutoDock lebih rendah daripada dehidrozingeron, yakni sebesar -6,94 kkal/mol dan -6,78 kkal/mol untuk target COX-1 dan COX-2.

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Dehydrozingerone is a curcumin analogue isolated from ginger which is known to have a variety of pharmacological activities. However, dehidrozingeron isn rsquo t acknowledged as a drug yet as the effect is not optimal. Therefore, structure modification via Mannich reaction that is known to increase the pharmacological activities is then performed.

Synthesis is done in two methods. The first method is done by reacting vanillin and acetone, followed by Mannich reaction using morpholine. Crude yield and pure yield obtained from each step is 76,94 and 32,48 , and 51,83 and 38 respectively. The second method is done by synthesizing vanillin morpholine first, followed by aldol condensation using acetone. Crude yield obtained from each step is 51.19 dan 39.95.

The compound is then evaluated for purity by TLC and melting point determination, elucidated with FT IR and UV Vis spectrophotometry, 1H NMR and 13C NMR spectrometry and MS. After that, antiinflammatory activity is studied by in vitro and in silico methods. In vitro assay is done using albumin denaturation technique.

The IC50 result is 12.261 M, showing the activity to be 0.63 times lower than diclofenac sodium. G value from AutoDock is lower than dehydrozingerone, which is 6,94 kkal mol and 6,78 kkal mol for the COX 1 and COX 2."

"ABSTRAKPeradangan adalah upaya tubuh untuk mengurangi aktivitas atau kerusakan organisme yang menyerang tubuh, menghilangkan iritasi, dan mengatur derajat perbaikan jaringan tubuh. Pengobatan peradangan dapat menggunakan berbagai obat obat anti inflamasi non steroid, namun penggunaan obat ini tetap memberikan efek pihak terhadap penggunanya. Di Indonesia, arthritis yang merupakan a kelompok penyakit sendi, prevalensinya mencapai 24,7%, peringkat kedua setelah tekanan darah tinggi. Dehidrozingeron memiliki aktivitas berbagai biologis seperti anti-inflamasi. Dalam penelitian ini, tujuannya adalah untuk mendapatkan 4- (4-hidroksi-3-metoksi-5 - [(4-metilpiperazin-1-Il) metil] senyawa fenil} tetapi-3-en-2-on (dehydrozingerone 1-methylpiperazine) melalui sintesis basa Mannich dengan aktivitas anti-inflamasi untuk diuji menggunakan metode penghambatan enzimlipoksigenase. Proses sintesis dilakukan dengan cara mensintesis vanilin secara kondensasi aldol menjadi dehydrozingerone kemudian disubstitusi menggunakan 1-methylpiperazine reaksi Mannich. Hasil uji anti inflamasi pada senyawa dehydrozingerone 1-methylpiperazin(IC50 = 236.5566 M) menunjukkan aktivitas anti-inflamasi 1,012 kali lebih tinggi dibandingkan dengan senyawa standar yaitu asam nordihidroguaiaric (IC50 = 239,4282 μM).ABSTRACTInflammation is the body's effort to reduce activity or damage to organisms that attack the body, eliminate irritation, and regulate the degree of repair of body tissues. Treatment of inflammation can use various non-steroidal anti-inflammatory drugs, but the use of these drugs still has side effects on the user. In Indonesia, arthritis, which is a group of joint diseases, has a prevalence of 24.7%, ranking second after high blood pressure. Dehidrozingerone has various biological activities such as anti-inflammatory. In this study, the aim was to obtain 4-(4-hydroxy-3-methoxy-5-[(4-methylpiperazine-1-Il)methyl]phenyl compounds} but-3-en-2-one (dehydrozingerone 1-methylpiperazine ) through the synthesis of Mannich bases with anti-inflammatory activity to be tested using the enzyme inhibition method lipoxygenase. The synthesis process was carried out by synthesizing vanillin by aldol condensation to dehydrozingerone then substituted using 1-methylpiperazine Mannich reaction. Anti-inflammatory test results on dehydrozingerone 1-methylpiperazin (IC50 = 236.5566 M) showed anti-inflammatory activity 1.012 times higher than the standard compound, namely nordihydroguaiaric acid (IC50 = 239.4282 M)"

"Hemoroid merupakan pembengkakan vena rektoanal yang menyebabkan peradangan, nyeri, dan pendarahan. Tanaman dengan senyawa fenolik diketahui memperbaiki tonus vena dan antiinflamasi. Daun sirsak mengandung senyawa fenolik, alkaloid, acetogenin dan megastigmanes. Penelitian ini bertujuan untuk memeriksa parameter spesifik, nonspesifik, kadar fenol total, flavonoid total dan antioksidan Ekstrak Etanol Daun Sirsak (EEDS), juga melihat efek EEDS terhadap gambaran histopatologi dan ekspresi COX-2 dan TNFα pada jaringan rektoanal mencit Swiss berusia 20 minggu yang diinduksi dengan kroton oil 12% melalui anus. EEDS dosis 100, 200, dan 400mg/KgBB diberikan peroral selama 7 hari. Hasilnya menunjukkan EEDS memenuhi standar mutu ekstrak spesifik dan nonspesifik, kadar total fenol 22,85% atau 228,5 mgGAE/g ekstrak, kadar total flavonoid 5,36% atau 53,6 mgQE/g ekstrak, dan memiliki aktivitas antioksidan sedang (IC50 123,325 μg/mL). Pemeriksaan histopatologi pada jaringan rektoanal mencit dinilai dengan menskor lesi nekrosis, inflamasi, vasodilatasi, dan oedema yang diwarnai Hematoksilin-Eosin. Pemberian EEDS pada semua dosis menunjukkan perbedaan pada jaringan inflamasi, nekrosis, vasodilatasi dan oedema P<0.00. Sel positif mengekspresikan COX-2 dan TNFα dihitung pada sel epitel terinflamasi. Hasil menunjukkan EEDS dosis 200, 400 mg/KgBB signifikan menurunkan COX-2 P<0,002 dibandingkan dengan kontrol negatif, dan EEDS dosis 100, 200, dan 400 mg/KgBB signifikan menurunkan TNFα P< 0,010 dibandingkan dengan kontrol negatif.

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Haemorrhoids are rectoanal swelling that causes inflammation, pain, and bleeding. Plants with phenolic compounds are known to improve venous tone and anti-inflammation. Soursop leaves contain phenolic compounds, alkaloids, acetogenin and megastigmanes. This study aims to examine specific, nonspecific parameters, and total phenol levels, total flavonoids and antioxidants of Soursop Leaf Ethanol Extract (SLEE), also see the effect of SLEE on the histopathological features and expression of COX-2 and TNFα in rectoanal tissue of 20-week Swiss mice that are induced with 12% croton oil through the anus. SLEE doses of 100, 200, and 400mg/Kg were given orally for 7 days.

The results show SLEE meets the quality standards of specific and nonspecific extracts, total phenol levels of 22.85% or 228.5 mgGAE/g extracts, total flavonoid levels of 5.36% or 53.6 mgQE/g extracts, and have moderate antioxidant activity (IC50 123,325 μg/mL). Histopathological examination of the rectoanal tissue of mice was assessed by scoring necrotizing, inflammatory, vasodilatation, and oedema lesions hematoxylin-eosin. Administration of SLEE at all doses showed differences in inflammatory tissue, necrosis, vasodilation and oedema P<0.00. Positive cells expressing COX-2 and TNFα were counted on inflammatory epithelial cells. The results showed SLEE dosages of 200, 400 mg/Kg significantly decreased COX-2 P<0.002 compared to negative controls, and SLEE doses of 100, 200, and 400 mg/Kg significantly reduced TNFα P<0.010 compared with negative controls."

"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)

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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)"