Biochemical research of phenyclidine reseptor : Interaction to specific bonding to the lower affinity receptor

Fixed concentration of MK-801 molecule had been used as a specific ligand for differenciating two kinds of phencyclidine (PCP) and thienylphencyclidine (TCP) receptors. By using several drug molecules which have different pharmacological action, as well as such molecular affinity (IC50) to the rat brain, it was obtained that both of these interacting receptors had equal character for its higher or lower affinity sites. The MK-801 molecule inhibited much strongly (IC50 is about 10 nM) fixation of 3HTCP to its higher affinity receptor and much weakly (IC50 is about 10 μM) fixation of 3H-PCP to its lower affinity receptor. The MK-801 molecule could be used as well for differenciating two 3H-TCP receptors, the higher and the lower affinity.Key words : phencyclidine – thienylphencyclidine – MK-801 – higher affinity receptor– lower affinity receptor

BETWEEN ARTEMISININ AND DERIVATIVES WITH NEURAMINIDASE: A DOCKING STUDY INSIGHT

Objectives: This study aims to find the relationship between artemisinins and neuraminidase (NA) with molecular docking study and also to determine the most potent NA inhibitor from artemisinin and derivatives.Methods: All ligands were sketched and optimized using Gaussian 03W with Hartree-Fock method basis sets 6-311G. Molecular docking was performed using AutoDock 4.2.3 toward NA in complexes with oseltamivir as co-crystal ligand. The main parameters used were the free energy of binding (ΔG) and dissociation constant (Ki) as affinity marker.Results: Artesunate provided most negative free ΔG and lowest Ki toward NA with −9.55 kcal/mol and 100.66 nM, respectively. Artesunate shows higher affinity than oseltamivir with interactions between artesunate and amino acids at position 246 had important influences on artesunate affinity toward NA from H5N1.Conclusion: In silico molecular docking results indicated that artesunate could be considered as NA inhibitor and should be potential to be developed as anti-influenza particularly to H5N1 with oseltamivir resistance

Penentuan Kadar Resistin dan Korelasinya dengan Beberapa Parameter Klinik pada Kondisi Normal Dan Kurang Tidur

Resistin merupakan suatu molekul yang berperan penting dalam patofisiologi beberapa penyakit seperti obesitas, diabetes mellitus dan aterosklerosis yang merupakan faktor resiko penyakit kardiovaskuler. Kadar resistin di dalam serum berperan dalam menghubungkan obesitas dengan diabetes dan resistensi insulin. Penelitian ini bertujuan untuk menentukan kadar resistin dan korelasinya dengan beberapa parameter klinik pada subyek normal dan kurang tidur. Diperoleh profil yang terdistribusi normal untuk hasil pemeriksaan dengan nilai p> 0,05. Hasilnya tidak ada korelasi antara konsentrasi serum resistin dengan beberapa parameter klinik yang diperiksa tetapiterdapat perbedaan hasil pemeriksaan antara subyek tidur normal dengan kurang tidur pada semua parameter, namun yang berbeda signifikanhanya konsentrasi resistin dengan p=0,010.Kata kunci: resistin, subyek normal, kurang tidur.AbstractResistin is a molecule that plays an important role in several pathophysiological conditions such us obesitas, diabetes mellitus and aterosklerosis is a risk factor cardiovascular diseases. The level of resistin in serum plays a role in connecting obesity to diabetes and insulin resistance. The aims of this study was to determine serum resistin levels andtheir correlation to the several clinical parameters in normal subjects and sleep-deprived subject. A profil normal distribution was retrived for the result of examination, with a value of p> 0.05. The result showed that there was no significant correlation between serum resistin concentrations with several examined clinical parameters but there are differences in examination results between subjects with normal sleep and sleep deprivation on all parameters, but the significant difference was only parameter of resistin concentrations with p= 0.010.Keywords: resistin, normal subject,sleep deprivation

CORRELATION STUDY OF AGE, DISEASE DURATION, AND ERYTHROCYTE SEDIMENTATION RATE AMONG THE INDONESIAN RHEUMATOID ARTHRITIS PATIENTS

Objective: The present study aims to determine the correlation between age, disease duration, and erythrocyte sedimentation rate (ESR) among the Indonesian rheumatoid arthritis (RA) patients.Methods: The subject was the Indonesian RA patients and healthy control subjects. We were determined the correlation between age, disease duration, and ESR uses statistical analysis. The subjects who participated in the present study are patients who visit the Rheumatology clinic at one governmental hospital in Bandung City, Indonesia. ESR was determined by the modified Westergren's method. R software was conducted to data analysis.Results: The number of subjects was 16.17% of men and 83.33% of women with the range from 20 to 77 y old. All patients received the combination of disease-modifying antirheumatic drugs, analgesic, and corticosteroid. The average of disease duration was 8.08+5.73 y. The experimental ESR of the RA patients were 22.50+12.23 mm/h for men and 31.75+15.03 mm/h for women. This value is only slightly higher than the normal value. We suggested that treatment with combination therapy can maintain the ESR.Conclusion: Spearman's correlation showed that there is no correlation between age and disease duration (rho = 0.325), between age and ESR (rho =-0.285), and between disease duration and ESR (rho = 0.039).Â

Uji Aktivitas Enzim Superoksida Dismutase dalam Ekstrak Mesokarp Buah Merah (Pandanus conoideus Lamarck) Menggunanakan Densitometri Citra Elektroforegram

Penelitian ini bertujuan menguji aktivitas super oksida dismutase (SOD) mesokarp buah merah (Pandanus conoideus Lamarck). Pengujian dilakukan dengan metode elektroforesis gel poliakrilamid dan densitometri citra terhadap ekstrak kasar buah merah dan ekstrak hasil pemurnian dengan dialisis setelah pengendapan dengan amonium sulfat konsentrasi 25, 50 dan 75% b/v. Aktivitas SOD ditunjukkan dengan terbentuknya pita transparan pada gel setelah dua tahap proses pewarnaan yaitu dengan nitro biru tetrazolium dan riboflavin, dan hasil pencitraan gel dianalisis dengan densitometer. Aktivitas SOD ditentukan dengan membandingkan terhadap SOD dari Escherichia coli dan diperoleh aktivitas SOD sebesar 420 U/mL atau setara dengan 836 U/gram buah merah.Kata kunci: Elektroforesis, Densitometer, Superoksida dismutase, Buah merahThe aim of this study was to test the activity of SOD buah merah (Pandanus conoideus Lamarck). Evaluation was done by polyacrylamide gel electrophoresis and image densitometry was performed to raw extract of buah merah, and the extract pure by dialysis after precipitation with ammonium sulfate concentrations of 25, 50 and 75% w/v. SOD activity was shown by the formation of transparent tape on the gel after the gel staining by nitro blue tetrazolium and riboflavin, then imaging results were analyzed by densitometer. SOD activity was determined by comparing the SOD from Escherichia coli and it was 420 U/mL.Keywords: Electrophoresis, Densitometer, Superoxide dismutase, red frui

Optimasi Isolasi dan Karakterisasi Jakalin dari Biji Nangka

Telah diisolasi jakalin dari biji nangka (Artocarpus heterophyllus) menggunakan metode kromatografi afinitas dengan matriks guar gum yang telah dipaut silang dengan epiklorohidrin, isolasi dilakukan dengan menggunakan pengelusi D-galaktosa. Hasil karakterisasi jakalin menggunakan SDS-PAGE menunjukkan bahwa jakalin memiliki dua pita dengan bobot molekul 14,1 dan 15,5 kDa, antar subunitnya tidak dihubungkan dengan ikatan disulfida. Jakalin yang diisolasi memiliki kemampuan mengaglutinasi eritrosit, kemampuan hemaglutinasi jakalin tidak berkurang setelah diinkubasi pada suhu 20oC dan 30oC, tetapi setelah inkubasi pada suhu 40oC, 50oC, 60oC, 70oC, aktivitasnya turun masing-masing 75%, 87,5%, 93,75% dan 98,4%. Kemampuan hemaglutinasi jakalin tidak berkurang setelah diinkubasi pada pH 5, 6, dan 7, tetapi aktivitasnya turun 75% setelah inkubasi pada pH 2, 3, 4, dan 8, serta turun 96,9% pada pH 9 dan 10. Kemampuan hemaglutinasi jakalin dihambat oleh D-galaktosa dengan kemampuan inhibisi hemaglutinasi sebesar 6,25 mM, aktivitas hemaglutinasi jakalin tidak dihambat oleh D-manosa, D-glukosa, fruktosa, laktosa, arabinosa, maltosa, dan manitol. Diperoleh jakalin dengan perolehan rata-rata sebesar 0,32% b/b dari serbuk kering biji nangka.Kata kunci: Jakalin, lektin, Artocarpus heterophyllus, D-galaktosa.Jacalin from jackfruit (Artocarpus heterophyllus) had been isolated using affinity chromatography method with epichlorohydrin crosslinked guar gum as the matrix, isolation carried out using D-galactose as the eluen. Characterizationjacalin using SDS-PAGE showed that jacalin has two bands with molecular weights 14.1 and 15.5 kDa, intersubunit not connected with disulfide bonds. Jacalin isolates have the ability to haemagglutination erythrocytes, haemagglutination activity of jacalin maintained after incubation at 20oC and 30oC, but the activity decreased at 40, 50, 60, and 70 oC of incubation, which were 75%, 87.5%, 93.75% and 98.4% , respectively. Jacalin hemagglutination ability is not reduced after incubation at pH 5, 6, and 7, but the activity down 75% after incubation at pH 2, 3, 4, and 8, and down 96.9% at pH 9 and 10. The haemagglutination activity of jacalin was inhibited by D-galactose with the capacity inhibition value was 6.25 mM, but it was not inhibited by D-manose, D-glucose, fructose, lactose, arabinose, maltose, and manitol. Average recovery of jacalin is 0.32% w/w of jackfruit dry powder.Keywords: Jacalin, lectin, Artocarpus heterophyllus, D-galactose

CORRELATION STUDY OF SERUM CALCIUM LEVELS AND SERUM CARTILAGE OLIGOMERIC MATRIX PROTEIN LEVELS IN RHEUMATOID ARTHRITIS PATIENTS IN BANDUNG, INDONESIA

  Objective: This study was designed is to determine the correlation between serum calcium level and serum cartilage oligomeric matrix protein (COMP) level in Indonesian patients with rheumatoid arthritis (RA).Subjects and Methods: The subjects are patients who visit the rheumatology clinic at a government hospital in Bandung, Indonesia. Serum calcium level was determined by a complexometric method, and the serum COMP level was determined by enzyme-linked immunosorbent assay. Statistical analysis was performed with R software.Results: The serum calcium level was 82.24±44.82 mg/mL in RA patients and 99.04±60.56 mg/mL in normal controls. The serum COMP level was 843.80±35.79 ng/ml in RA patients and 830.00±48.92 ng/ml in normal controls.Conclusion: There is no correlation between serum calcium level and serum COMP levels in RA patients (p=0.967 and rho=0.006)

Anti-inflammatory Activities and Gastric Ulcer-inducing Properties of Tetraacetylquercetin and Tetrapivaloylquercetin

Quercetin (3,3'4',5,7-pentahydroxyflavone) has been reported to show anti-inflammatory activity. However, its low oral bioavailability limits the application of quercetin in therapy. Ester derivatives of quercetin have been reported to have higher bioavailability than quercetin. This research aimed to study the anti-inflammatory activities and gastric ulcer-inducing properties of tetraacetylquercetinas well as tetrapivaloylquercetin. Synthesis of tetra-acyl derivatives of quercetin was conducted using acetic anhydride or pivaloyl chloride in the presence of pyridine and the structure was confirmed by 1H-NMR and 13C-NMR spectroscopy as well as elemental analysis. At a dose of 20 mg/kg bw, oral administration of quercetin only showed 20% inhibition activity on carragenan induced rat paw edema, while tetraacetyl and tetrapivaloyl derivatives at equimolar dose showed 11-33% and 5-15% inhibition activity respectively. Contrary to the gastric ulcer healing-promoting action of quercetin, tetraacetylquercetin caused mild gastric ulcers. However, no gastric ulcer was observed after administration of tetrapivaloylquercetin. It was concluded that acylation enhances the anti-inflammatory activity of quercetin but causes mild gastric ulcers in the case of tetraacetylation

FTIR Method for Peptide Content Estimation and Degradation Kinetic Study of Canarium Nut Protein

Quantitative analysis of bioactive peptide mostly conducted by measuring the activity. While the determination of peptide content in natural sources has been conducted using various instruments, vibrational spectroscopy remains underutilized. Here, we attempted new developed method in peptide quantification and degradation kinetic analysis using Fourier-Transform Infrared Spectroscopy. Bovine Serum Albumin was used as standard protein in method development and validation. Peptide content was estimated by converting peak area to concentration. The method was used to estimate peptide content in Canarium nut protein and its hydrolysates, which potentially hold biological activity. Kinetic study was conducted with microwave as an accelerator for hydrolysis, an apparatus rarely used in peptide study. Amide I band on wavenumber range of 1724.05-1619.91 cm-1 was selected for analysis, considering its selectivity and linearity. The method also met other validation requirement, including accuracy and precision. When applied in quantitative analysis, the method was able to calculate peptide content decrease in Canarium nut protein after hydrolysis using papain (38.24%), pepsin (33.67%) and alkaline reagent (28.53%). In kinetic study, microwave-assisted peptide degradation exhibited logarithmic profile with the equation of y=-0.148ln(x)+0.9591 and R² value of 0.963. Based on these results, FTIR is useful in estimating peptide content and in analyzing degradation kinetic profile.

CORRELATION STUDY OF DISEASE ACTIVITY SCORE AND SERUM CARTILAGE OLIGOMERIC MATRIX PROTEINLEVELS OF RHEUMATOID ARTHRITIS PATIENTS IN BANDUNG, INDONESIA

Objective: This study was designed to determine the correlation between Disease Activity Score (DAS 28) and the serum Cartilage Oligomeric Matrix Protein (COMP) levels in Indonesian Rheumatoid Arthritis (RA) patients.Methods: The subjects were patients who visit the rheumatology clinic at one governmental hospital in Bandung, Indonesia. DAS was determined by the QxMD Software based on erythrocyte sedimentation rate, and serum COMP levels were determined by enzyme-linked immunosorbent assay. Statistical analysis was conducted with IBM SPSS Statistics 23.Results: DAS 28 value was 3.36 ± 0.16 which indicates the moderate disease activity. Serum COMP levels were 843.80 ± 35.79 ng/ml in RA patients and 830.00 ± 48.92 ng/ml in normal controls.Conclusion: There is no correlation between DAS 28 and serum COMP levels in RA patients (p = 0.496 and rho = 0.129).Keywords: Autoimmune disease, Rheumatoid arthritis monitoring, Cartilage oligomeric matrix protein, Disease activity score 2