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Hadanu R.,Pattimura University | Syamsudin,Pancasila University
Asian Journal of Chemistry | Year: 2013

Quantitative electronic structure-activity relationship (QSAR) analysis of a series of mangostin derivatives as antiplasmodial compounds have been conducted using atomic net charges (q), dipole moment (?) ELUMO, EHOMO, polarizability (a), log P and massa molecular as the descriptors. The descriptors were obtained from computational chemistry method using semi-empirical PM3. Antiplasmodial activities were taken as the activity of the drugs against chloroquine-resistant plasmodiumfalciparum FCR3 strain and are presented as the value of ln (1/IC50) where IC50 is an effective concentration inhibiting 50 % of the parasite growth. The best model of QSAR model was determined by multiple linear regression method and giving equation of QSAR: ln 1/IC50 = -189.029-(752.054) qC5 + (1249.672)qO6 + (3134.359) qC9 + (1174.323) qC10 + (329.121)qC13 -(1.409)? + (75.214) ELUMO -(23.683) ELUMO -(2.156) a-(3.372) log P + (0.309) MM. The equation was significant on the 95 % level with statistical parameters: n = 15; r = 0.951; r2 = 0.905; SE = 1.326498; Fcalc/Ftable = 1.029 and gave the PRESS = 5.650972. Its means that there were only a relatively few deviations between the experimental and theoretical data of antimalarial activity. Source

Syamsudin,Pancasila University
Research Journal of Pharmacology | Year: 2011

The study aimed at determining the effects of the stem bark extracts of Garcinia parvifolia administered orally to P. berghei infected mice in varied dosages to observe Malondialdehyde (MDA) level, SGOT and SGPT and its relationship with liver cell damage and degree of parasitemia. Thirty mice of Swiss strain used in the experiment were assigned into 5 treatment groups: Group 1 (control group) consisted of P. bergheii infected mice reacted with physiological salt solution; group 2 (normal) consisted of uninfected mice; group 3 consisted infected mice treated with stem bark extracts of G. parvifolia with a dosage of 200 mg/kg BW/day; group 4 consisted of infected mice treated with stem bark extracts of G. parvifolia with a dosage of 400 mg/kg BW/day and group 5 consisted of infected mice treated with stem bark extracts of G. parvifolia with a dosage of 800 mg/kg BW/day. The test preparation was administered orally for 4 days. After 4 days of administration, MDA level was measured in the plasma using a spectrophotometer and three mice were killed to obtain the liver for histopathological purpose. The study found 400 mg kg -1 BW that during malaria infection, MDA production increased and liver damage tended to be milder. Administration of stem bark extract of G. parvifolia in oral way could reduce MDA, SGOT and SGPT level (p<0.05), particularly with a dosage of 400 mg and 800 mg/kg BW/day. © Medwell Journals, 2011. Source

Sarti F.,University of Innsbruck | Iqbal J.,University of Innsbruck | Iqbal J.,PCSIR Laboratories Complex | Muller C.,University of Innsbruck | And 4 more authors.
Analytical Biochemistry | Year: 2012

The aim of this study was to investigate the potential of poly(acrylic acid)-cysteine (PAA-cys) solution and microparticles to enhance the transport of vitamin B12 (VB 12) across Caco-2 cell monolayer and rat intestinal mucosa. Thiolated PAA was synthesized by covalent attachment of l-cysteine. Microparticles were prepared by spray-drying and characterized regarding their size, morphology, thiol group content, VB 12 payload and release, swelling behavior, mucoadhesion, permeation-enhancing effect, and cytotoxicity. Particles with a mean diameter of 2.452 ± 2.26 μm, a payload of 1.11 ± 0.72%, and 190.2 ± 8.85 μmol of free thiol groups per gram were prepared. Swelling behavior studies revealed that the stability of thiolated particles was improved compared with unmodified ones. Of the total VB 12 loaded, 95 ± 0.12% was released within 3 h from thiolated particles. PAA-cys particles exhibited 2.24-fold higher mucoadhesive properties compared with unmodified particles. Permeation experiments with Caco-2 cells proved that permeability of VB 12 with PAA-cys solution and particles was 3.8- and 3.6-fold higher than control, respectively, and with rat intestinal mucosa it was 4.8- and 4.4-fold higher than control, respectively. Negligible cytotoxicity was assessed. PAA-cys is a promising excipient for oral delivery of VB 12 as a solution and as microparticles. © 2011 Elsevier Inc. All rights reserved. Source

Syamsudin,Pancasila University
International Journal of Phytomedicine | Year: 2010

Extracts of Leucaena leucocephala (lmk) De Wit seeds were collected from different areas in Java; they include Jakarta, Cengkareng, Bogor and Bandung. Each extract was examined for water content, ash content, acid-insoluble ash content, and α- glycosidase inhibition assay. The results showed that ethanolic extracts of Leucaena leucocephala (lmk) De Wit seeds collected from Bandung were found to be most active in inhibiting the formation of α-glycosidase compounds with an IC50 value of 7,46 ± 0,21 μg/ml, which was confirmed with ash content of 5,58 ± 0,04, acid-insoluble ash content of 0,55 ± 1,33, and water content of 26,22 ± 0,90. ©arjournals.org. Source

Syamsudin,Pancasila University
Asian Journal of Chemistry | Year: 2010

In present work, a systematic study of the relative antioxidant activity of Indonesian propolis collected from different regions of Java have been reported. The total phenol varied from 136.2 ± 10.1 to 203.7 ± 9.8 mg g-1 in the extracts. Flavones and flavonols were determined using aluminium chloride and expressed as quercetine equivalent, while flavanones were determined using 2,4-dinitrophenylhydrazine and expressed as naringenin. Contents of flavones and flavonols were similar for most samples and ranged from 1.7-7.3%. The content of flavanones in propolis samples varies from 1.2-5.9%. 1,1-Diphenyl-2-picrylhydrazine (DPPH) radical scavenging effect of the extracts was determined spectrophotometrically. IC50 of the extracts and the standard compounds quercetine was 8.44, 130.35, 19.27, 91.03 and 2.58 μg mL -1. Source

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