Open Journal Systems
Not a member yet
442 research outputs found
Sort by
MACARANGIN, A GERANYLATED FLAVONOID AND ANTICANCER ACTIVE COMPOUND ISOLATED FROM ETHYL ACETAT FRACTION OF Macaranga gigantifolia LEAVES
Get PDFMacaranga known locally as mahang-mahangan has uniquely ecological function, and also became a part of traditional medicine in Indonesia. Macaranga genus also known as a sources of terpenoid and phenolic (flavonoid) compounds which have biological activity as antioxidant and anticancer (cytotoxicity).There are few phytochemical investigations have been done on M. gigantifolia species. As a part of our continuing research of isolation anticancer compound from natural product, a geranylated flavonoid compound (macarangin) has been isolated from ethyl acetate fraction of Macaranga gigantifolia leaves using chromatography methods. The isolated compund (isolat MG) was elucidated to gain the chemical structure based on spectroscopic data (LC-MS and FT-NMR). Cytotoxicity test of this compound was tested against MCF 7 cell lines, showed that macarangin has a potential activity with IC50 value 119.12μg/mL. Key words: Macarangin, geranylated flavonoid, Macaranga gigantifolia, MCF 7 cell lines
Antiseptic activity evaluation of piper leave from Piper betle Linn extract in hand gel antiseptic preparation
Get PDFIt is known that piper leaves (sirih) from Piper betle Linn has been used traditionally as medicine, for example for mouthwash and wound curing. The usage of hand gels antiseptic preparation was getting increased in the current time as the incidence of desease caused by virus and bacteria like SARS appears.This research was aimed to develop preparation of hand gels from piper leaves extract obtained from extraction with hot water. The formulation of gels were made using 5%, 10%, 15%, 20% and 25% of piper leaves extract in Carbopol gel base. The evaluation of antiseptics activity was carried out using the Replica method. A series of test was done by pouring the gels at hand palm and slightly tap the thumb fingerprint to nutrient agar media. The media was incubated at 37°C for 24 hours,and the number of colonies of microorganism was counted. The antiseptic activity of the gels also compared with two hand gels antiseptic preparation containing ethanol and triclosan as antiseptic agentThe result showed that the piper leaves extract gels had a transparent pale yellow performance. The gel preparation with concentration of 15% extract had activity to reduce the microorganism of skin normal flora up to 50%. Yet the 25% concentration of piper leave extract could eliminate all the microorganism. It was also known that the 15% piper leaves extract gel had no significance different with the ethanol preparation, since the 20% and 25% piper leaves extract gels had similar antiseptic activity to the triclosan preparation.Key words: piper leaves extract, gel, antiseptic activity, replica method
SOLUBLE EXPRESSION OF SYNTHETIC CSF3syn GENE FUSED WITH THIOREDOXIN IN Escherichia coli BL21(DE3) THROUGH AUTOINDUCTION METHOD AND PURIFICATION
Get PDFA synthetic human gene of CSF3 (CSF3syn.Ec3), coding for hG-CSF was succesfully subcloned into pET32a(+) expression vector and fused with thioredoxin (Trx) at its N-terminal as fusion partner. The obtained fusion gene of Trx-CSF3syn within the recombinant plasmid pET32a(+)_CSF3yn.Ec3 was verified by PCR, plasmid restriction, and DNA sequencing analysis. In order to investigate the fusion gene expression, we transformed Escherichia coli BL21(DE3) as the host with the recombinant plasmid. The gene was succesfully expressed within the cytosol as fusion protein of Trx·tag, His·tag, S·tag, EK-site, and hG-CSF moities. By the autoinduction method, it was obtained 49% from the soluble fraction and 51% from the insoluble fraction. The soluble fraction was subsequently purified by IMAC method (Ni-NTA) and characterized.Key words : hG-CSF, thioredoxin, autoinduction, IMAC, E.coli
ANTIPROLIFERATIVE ACTIVITY OF RECOMBINANT HUMAN INTERFERON ALPHA2B ON ESTROGEN POSITIVE HUMAN BREAST CANCER MCF-7 CELL LINE
Get PDFIndonesia is the top three countries with hepatitis and moreover has 40.000 cancer mortalities per year. Interferon alpha 2b (IFNα-2b) is a therapeutic standard for cancer and hepatitis B/C treatments. We developed recombinant human interferon alpha 2b (rhIFNα-2b) in methilotropic yeast Pichia pastoris X-33. The protein was produced as extracellular protein with 24 kDa in size. This research was aimed to characterize the protein based on its amino acid sequence and to study its antiproliferative activity on MCF-7 cell line. Amino acid sequencing by using MALDI TOF TOF mass spectrometry with trypsin as proteolytic enzyme identified protein as hIFNα-2b with 33% of amino acid coverage. The antiproliferative activity was determined by 3-[4.5-dimethyltiazol-2il]-2.5-diphenylltetrazolium bromide (MTT) assay. Based on several studies about the synergistic activity of rhIFNα-2b with other anticancer drugs, we combined our rhIFNα-2b with tamoxifen (tmx). The growth percentage of the cells after being treated with 1µM of tmx at various concentrations of rhIFNα-2b was compared with that of untreated cell. This study showed that the antiproliferative activity was dose-dependently. Cell viability assay with calcein and ethidium bromide-based staining by fluorescence microscope confirmed that the rhIFNα-2b had ability to inhibit proliferation of human breast cancer cell line MCF-7. Keywords: human interferon alpha 2b, Pichia pastoris, antiproliferative and MCF-
IN VITRO ANTIDIABETIC AND IN VIVO ANTIDIARRHEAL ACTIVITY OF Oncoba Spinosa ROOTS
Get PDFThe different extracts of O.spinosa (Flacourtiaceae) were screened for in-vitro antidiabetic activity. Of all the extracts tested, ethanolic extract showed highest alpha amylase inhibition ranging from 8.64+0.66% to 79.94+0.65% and alpha glucosidase inhibition ranging from 14.12+0.51% to 78.68+0.36% when studied at concentrations 62.5-1000μg/mL. The ethanolic extract was subjected to antidiarrheal activity and diarrheal severity was reduced significantly by 15.81% in 100mg/kg group, 30.45% in 200mg/kg group and 74.37% in 400mg/kg group in castor oil induced diarrhea model. In castor oil induced enteropooling, the extract at doses 200mg/kg and 400mg/kg showed 33.46% and 42.44% inhibition of intestinal accumulation. In the charcoal meal test, the distance travelled by charcoal meal was significantly reduced by the extract at doses 200mg/kg and 400mg/kg (P<0.01). The overall results tend to suggest the antidiabetic and antidiarrheal activities of O. spinosa.Key word : in vivo, in vitro, antidiabetic, antidiarrheal, O.spinosa, root
SYNTHESIS AND PHARMACOLOGICAL EVALUATION: ANTIMICROBIAL, ANTI-INFLAMMATORY, ANALGESIC, ULCEROGENIC PROPERTIES OF SEVERAL BIS-HETEROCYCLIC DERIVATIVES
Get PDFIn Medicinal chemistry, heterocyclic derivatives contributed the largest classical division of organic chemistry. Thiadiazole compounds have been know many biological activities such as hypoglycemic, anticancer, anti-inflammatory, anti-asthmatic, antihypertensive and etc. On this research, several 1,1-Bis [2-{2-(5-(arylidene)imino-1,3,4-thiadiazol-2-yl) methyl amino}- 1,3,4-thiadiazo-5-yl] cyclopropane 5(a-h) have been synthesized from cyclopropane dicarboxylic acid comprising thiadiazole moieties. All the synthesized compounds have been characterized by elemental (C,H,N) and spectral (I.R., 1H- NMR, Mass) analysis. Furthermore, all synthesized compounds were screened for their antifungal, antimicrobial, anti-inflammatory, analgesic, ulcerogenic and toxic activities. The Compound 5f, 3-chlorophenyl substituted was found the most potent in antimicrobial spectrum against all the used microbes. On the other hand, compound 5g, 4-hydroxy-3-methoxy phenyl substituted was found the most potent in anti-inflammatory, analgesic, and ulcerogenic activities which further evaluated for lesser toxicity test.Key words: Bis-phenylarylidinylthiadiazolidinone cyclopropane, anti-microbial, anti-inflammatory, analgesic, ulcerogenic and toxicity studie
MUTATION INDUCTION FOR IMPROVING OF ARTEMISININ CONTENT IN EACH PART OF ARTEMISIA CINA MUTAN LINES
No full textMutation induction on Artemisia cina herbal medicine by gamma rays with the doses of 10, 20 and 40 Gy have been conducted at PAIR – BATAN. The purpose of mutation for improving of plant traits which were mutant lines more artemisinin content than control plant. The mutant lines interest were collected based on morphological characters (flowers, leaves, roots and stems). Artemisinin contents so far are only found in the leaves, the improvement are expected not only to increase artemisinin content in leaves but also in the roots, stems and flowers of A.cina mutant lines by mutation induction using gamma rays by the doses of 10, 20 and 40 Gy, every dose was selected 8 mutant lines for analysis artemisinin content.To obtain artemisinin from all selected mutant lines, flowers, leaves, roots and stems were extracted by using n-hexan, and then fractionation by ethyl acetate. Artemisinin content were analyzed by High Pressure Liquid Chromatography (HPLC), and pure artemisinin used as standard. Mutation induction by the dose of 40 Gy have been improving dry weight of roots from 38.85 to 76.19g, dry weight of leaves of mutant lines from 10 Gy irradiation was two times higher than leaves of parent plant, and three times by the dose of 40 Gy compared to dry weight of leaves parent plant, and no different by the dose of 20 Gy. The highest artemisinin content is 73.13mg/g in leaves of A26a3 mutant line and 36.68mg/g in flowers of A17.1 A.cina mutant lines, both of mutant lines from mutation induction by the dose of 10 Gy. Mutation induction by the dose of 20 Gy could improve artemisinin content in stems part of B12.1 mutant line from non detection in parent plant to 0.83mg/g. Mutation induction by the dose of 40 Gy improved artemisinin content to 1.90mg/g in roots and 1.50mg/g in stems of C27b1 and C8.3 mutant lines respectively. Artemisia cina un-irradiated as parent plant only contain artemisinin in flowers, leaves and roots were 0.13; 0.45 and 0.05mg/g respectively. Dose of 40 Gy is the best dose for enhancement of artemisinin content in each part of A.cina mutant lines.Key word : mutation, production of artemisinin, roots, stems, flower
SYNTHESIS OF TETRAHYDROHEXAGAMAVUNON-5 AND TETRAHYDROHEXAGAMAVUNON-7
Get PDFSynthesis of Tetrahydrohexagamavunon-5 (THHGV-5) and Tetrahydrohexagamavunone-7 (THHGV-7) were prepared by catalytic hydrogenation reaction on Hexagamvunon-5 (HGV-5) and Hexagamavunone-7 (HGV-7) by using gas H2 as source of hydrogen gas, Pd/C 10 % as metal catalyst and methanol as solvent at room temperature. The products were characterized by IR Spectroscopy, Gas Chromatography-Mass Spectroscopy (GCMS), 1D-NMR (1H-NMR and 13C-NMR) and 2D-NMR (1H-13C HMQC) Spectroscopy to determine the product structure molecules. According to the data of IR, GC-MS, 1H-NMR, 13C-NMR and 1H-13C HMQC spectra, the products are THHGV-5 and THHGV-7 as white crystalline powders. Key words:Tetrahydrohexagamavunon-5, Tetrahydrohexagamavunone-7, Hexagamvunon-5, Hexagamavunone-
CONSTRUCTION AND RETROSPECTIVE VALIDATION OF STRUCTURE-BASED VIRTUAL SCREENING PROTOCOLS TO IDENTIFY POTENT LIGANDS FOR HUMAN ADRENERGIC BETA-2 RECEPTOR
Get PDFAdrenergic Beta-2 Receptor (ADRB2) is a member of G-protein coupled receptors family, which has served as targets for more than 30% of top-selling drugs in the market. Recently, an enhanced dataset of ligands and decoys for ADRB2 has publicly available. However, the original retrospective structure-based virtual screening campaign accompanying the dataset showed relatively poor quality with enrichment factor of true positives at 1% false positives (EF1%)value of 3.9. In this article, the construction and retrospective validation of a structure-based virtual screening protocol by employing PLANTS1.2 as the molecular docking software and PyPLIF as an alternative post docking scoring functions are presented. The results show that the developed protocols have better quality compared the original structure-based virtual screening with EF1% values of 24.24 and 8.22 by using ChemPLP from PLANTS1.2 and by using Tc-PLIF from PyPLIF, respectively. Further investigation by performing systematic filtering resulted in the identification of D113, S203, and N293 as molecular determinants in ADRB2-ligand binding.Key words: Structure-based virtual screening, molecular docking, adrenergic beta-2 receptor, protein-ligand interaction fingerprinting, molecular determinant
EFFECT OF DIALYZER REUSE UPON UREA REDUCTION RATIO (URR), KT/V UREA AND SERUM ALBUMIN IN REGULAR HEMODIALYSIS PATIENT
Get PDFReuse of dialyzers for hemodialysis can help in bringing down the cost of hemodialysis. On the other hand reuse of dialyzer may change dialyzer integrity. This study was undertaken to determine dialyzer reuse effect on Urea Reduction Ratio (URR), Kt/V urea and serum albumin. This was prospective study in Sanglah Public General Hospital Denpasar. Inclusion criteria for this study were patients who receive hemodialysis more than 3 months on twice weekly hemodialysis. In the study we used hollow fiber or dialyzer Elisio type H-130H reprocessed with Renaline automatically by machine renatron. After each session blood urea, post dialysis weight and serum albumin were measured. Measurements was performed on the use new dialyzer, 1st reuse, 4th reuse and 7th reuse. The dialyzer was discarded, if TCV fell below 80% of baseline value. Kt/V and urea reduction ratio (URR) were calculated as measure of dialysis adequacy. A total of 23 people completed the study. There was a lack of uniformity duration of hemodialysis, so that we also performed an analysis using a uniform length hemodialysis duration (4.5 hours) with 15 samples. There were no significant difference between URR and Kt/V urea of new dialyzer and dialyzer reprocessed by renaline respectfully with p=0.131 and p=0.373. If we analyzed only using uniform time of dialysis (4.5 h) the value of URR and Kt/V urea between new and reused dialyzer not significantly different with p=0.520 and p=0.784. There was also not found significant differences between serum albumin of the use new dialyzer and reused dialyzer by the time of uniform or non-uniform, respectfully with p=0.271 and 0.073. Reuse dialyzer does not alter efficacy of hemodialysis.Key words : Dialyzer, Urea Reduction Ratio (URR), Kt/V Urea, Albumin, Total Cell Volume (TCV