Search results for: Illegal drug

Authors: S. S. Pati, L. Herojit Singh, A. C. Oliveira, V. K. Garg

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Chitosan functionalized Fe3O4-Au core shell nanoparticles have been prepared using a two-step wet chemical approach using NaBH4 as reducing agent for formation of Au in ethylene glycol. X-ray diffraction studies shows individual phases of Fe3O4 and Au in the as prepared samples with crystallite size of 5.9 and 11.4 nm respectively. The functionalization of the core-shell nanostructure with Chitosan has been confirmed using Fourier transform infrared spectroscopy along with signatures of octahedral and tetrahedral sites of Fe3O4 below 600cm-1. Mössbauer spectroscopy shows decrease in particle-particle interaction in presence of Au shell (72% sextet) than pure oleic coated Fe3O4 nanoparticles (88% sextet) at room temperature. At 80K, oleic acid coated Fe3O4 shows only sextets whereas the Chitosan functionalized Fe3O4 and Chitosan functionalized Fe3O4@Au core shell show presence of 5 and 11% doublet, respectively.

Keywords: Magnetic nanoparticles, Fe3O4@Au core shell, iron oxide, Au nanoparticles.

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Authors: Ren-Jy Ben, Jo-Chi Jao, Chiu-Ya Liao, Ya-Ru Tsai, Lain-Chyr Hwang, Po-Chou Chen

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Cancer is still one of the serious diseases threatening the lives of human beings. How to have an early diagnosis and effective treatment for tumors is a very important issue. The animal carcinoma model can provide a simulation tool for the studies of pathogenesis, biological characteristics, and therapeutic effects. Recently, drug delivery systems have been rapidly developed to effectively improve the therapeutic effects. Liposome plays an increasingly important role in clinical diagnosis and therapy for delivering a pharmaceutic or contrast agent to the targeted sites. Liposome can be absorbed and excreted by the human body, and is well known that no harm to the human body. This study aimed to compare the therapeutic effects between encapsulated (doxorubicin liposomal, Lipodox) and un-encapsulated (doxorubicin, Dox) anti-tumor drugs using magnetic resonance imaging (MRI). Twenty-four New Zealand rabbits implanted with VX2 carcinoma at left thighs were classified into three groups: control group (untreated), Dox-treated group, and LipoDox-treated group, 8 rabbits for each group. MRI scans were performed three days after tumor implantation. A 1.5T GE Signa HDxt whole body MRI scanner with a high resolution knee coil was used in this study. After a 3-plane localizer scan was performed, three-dimensional (3D) fast spin echo (FSE) T2-weighted Images (T2WI) was used for tumor volumetric quantification. Afterwards, two-dimensional (2D) spoiled gradient recalled echo (SPGR) dynamic contrast-enhanced (DCE) MRI was used for tumor perfusion evaluation. DCE-MRI was designed to acquire four baseline images, followed by contrast agent Gd-DOTA injection through the ear vein of rabbit. A series of 32 images were acquired to observe the signals change over time in the tumor and muscle. The MRI scanning was scheduled on a weekly basis for a period of four weeks to observe the tumor progression longitudinally. The Dox and LipoDox treatments were prescribed 3 times in the first week immediately after the first MRI scan; i.e. 3 days after VX2 tumor implantation. ImageJ was used to quantitate tumor volume and time course signal enhancement on DCE images. The changes of tumor size showed that the growth of VX2 tumors was effectively inhibited for both LipoDox-treated and Dox-treated groups. Furthermore, the tumor volume of LipoDox-treated group was significantly lower than that of Dox-treated group, which implies that LipoDox has better therapeutic effect than Dox. The signal intensity of LipoDox-treated group is significantly lower than that of the other two groups, which implies that targeted therapeutic drug remained in the tumor tissue. This study provides a radiation-free and non-invasive MRI method for therapeutic monitoring of targeted liposome on an animal tumor model.

Keywords: Doxorubicin, dynamic contrast-enhanced MRI, lipodox, magnetic resonance imaging, VX2 tumor model.

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Authors: Athirah Nur Amirulhusni, Navindra Kumari Palanisamy, Zaini Mohd-Zain, Liew Jian Ping, R.Durairaj

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Multidrug resistant organisms have been taunting the medical world for the last few decades. Even with new antibiotics developed, resistant strains have emerged soon after. With the advancement of nanotechnology, we investigated colloidal silver nanoparticles for its antimicrobial activity against Pseudomonas aeruginosa. This organism is a multidrug resistant which contributes to the high morbidity and mortality in immunocompromised patients. Five multidrug resistant strains were used in this study. The antimicrobial effect was studied using the disc diffusion and broth dilution techniques. An inhibition zone of 11 mm was observed with 10 μg dose of the nanoparticles. The nanoparticles exhibited MIC of 50 μg/ml when added at the lag phase and the subinhibitory concentration was measured as 100 μg/ml. The MIC50 value showed to be 15 μg/ml. This study suggests that silver nanoparticles can be further developed as an antimicrobial agent, hence decreasing the burden of the multidrug resistance phenomena.

Keywords: Antimirobial activity, Multidrug resistance, Pseudomonas aeruginosa, Silver nanoparticles

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Authors: Iman I. Salama, Samia M. Sami, Somaia I. Salama, Zeinab N. Said, Thanaa M. Rabah, Aida M. Abdel-Mohsin

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This is a national community based project to evaluate effectiveness of HBV vaccination program in prevention of infection. HBV markers were tested in the sera of 3600 vaccinated children. Infected children were followed up for 1 year. Prevalence of HBV infection was 0.39 % (0.28% positive for anti-HBc, 0.03% positive for HBsAg and 0.08% positive for both). One year later, 50% of positive anti-HBc children turned negative with sustained positivity for positive HBsAg cases. HBV infection was significantly higher at age above 9 years (0.6%) compared to 0.2% at age 3-9 years and 0% at younger age (P<0.05). Logistic analysis revealed that predictors for HBV infection were history of blood transfusion, regular medical injection, and family history of either HBV infection or drug abuse (adjusted odds ratios 6.2, 5.6, 7.6 & 19.1 respectively). HBV vaccination program produced adequate protection. Adherence to infection control measures and safe blood transfusion are recommended.

Keywords: Children, Egypt, HBV Infection, HBV Vaccine.

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Authors: S. Gupta, R. Chadha

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Five crystal modifications of water insoluble artesunate were generated by recrystallizing it from various solvents with improved physicochemical properties. These generated crystal forms were characterized to select the most potent and soluble form. SEM of all the forms showed changes in external shape leading them to be different morphologically. DSC thermograms of Form III and Form V showed broad endotherm peaks at 83.04oC and 76.96oC prior to melting fusion of drug respectively. Calculated weight loss in TGA revealed that Form III and Form V are methanol and acetone solvates respectively. However, few additional peaks were appeared in XRPD pattern in these two solvate forms. All forms exhibit exothermic behavior in buffer and two solvates display maximum ease of molecular release from the lattice. Methanol and acetone solvates were found to be most soluble forms and exhibited higher antimalarial efficacy showing higher survival rate (83.3%) after 30 days.

Keywords: Artesunate, Crystal modifications, in vivo studies, Recrystallization.

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Authors: Alesya Ya. Maruk, Olga E. Klementyeva, Ekaterina I. Lesik, Anton A. Larenkov, Alexander B. Bruskin

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Alpfa-fetoprotein and its fragments may be an important vehicle for targeted delivery of radionuclides to the tumor. We investigated the effect of conditions on the labeling of biologically active synthetic peptide based on the (F-afp) with technetium-99m. The influence of the nature of the buffer solution, pH, concentration of reductant, concentration of the peptide and the reaction temperature on the yield of labeling was examined. As a result, the following optimal conditions for labeling of (F-afp) are found: pH 8.5 (phosphate and bicarbonate buffers) and pH from 1.7 to 7.0 (citrate buffer). The reaction proceeds with sufficient yield at room temperature for 30 min at the concentration of SnCl2 and (Fafp) (F-afp) is to be less than 10 mkg/ml and 25 mkg/ml, respectively. Investigations of the test drug accumulation in the tumor cells of human breast cancer were carried out. Results can be assumed that the in vivo study of the (F-afp) in experimental tumor lesions will show concentrations sufficient for imaging these lesions by SPECT.

Keywords: peptide, technetium-99m, tumor, SPECT.

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Authors: Sperisa Distantina, Rieke Ulfha Noviyanti, Sri Sutriyani, Fadilah Fadilah, Mujtahid Kaavessina

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In this research, carrageenan extracted from seaweed Eucheuma cottonii was mixed with polyvinyl alcohol (PVA) and then crosslinked using glutaraldehyde (GA). The obtained hydrogel films were applied to control the drug release rate of paracetamol. The aim of this research was to develop a mathematical model that can be used to describe the mass transfer rate of paracetamol from the hydrogel film into buffer solution. The effect of weight ratio carrageenan-PVA (5: 0, 1: 0.5, 1: 1, 1: 2, 0: 5) on the parameters of the mathematical model was investigated also. Based on the experimental data, the proposed mathematical model could describe the mass transfer rate of paracetamol. The weight ratio of carrageenan-PVA greatly affected the amount of paracetamol absorbed in the hydrogel film and the mass transfer rate of paracetamol.

Keywords: Carrageenan-PVA, crosslinking, hydrogel, glutaraldehyde, paracetamol, mass transfer.

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Authors: Farid A., Ismail A., Rabee I., Zalat R. El Amir A.

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This study was designed for assessment of 3 types of Cysteine protease inhibitors (CPIs) fluromethylketone (FMK), vinyl sulfone (VS) and sodium nitro prussid (SNP), to define which of them is the best for curing S. mansoni infection in mice? In vitro, treated S. mansoni adult worms recorded a mortality rate after 1 hr of exposure to 500 ppm of FMK, VS and SNP as 75, 70 and 60%, respectively. FMK+PZQ treatment recorded the maximum reduction in worm burden (97.2% at 5 wk PI). VS treatment alone or combined with PZQ increases IgM, total IgG, IgG2 and IgG4 levels. In EM study, the completely implanted spines were reported in the degenerated tegument of adult worms in all groups treated with CPIs. VS+PZQ Treatment increased Igs levels but, its effect was different on worm reduction. So, it is not enough to eliminate the infection and FMK+PZQ considered the antischistosomicidal drug of choice.

Keywords: Praziquantel, fluromethylketone, vinyl sulfone, sodium nitro prussid.

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Authors: Guilan Huang

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In 2013 and 2014, the U.S. Food and Drug Administration (FDA) collected data from selected fast food restaurants and full service restaurants for tracking changes in the occurrence of foodborne illness risk factors. This paper discussed how we customized spatial random sampling method by considering financial position and availability of FDA resources, and how we enriched restaurants data with location. Location information of restaurants provides opportunity for quantitatively determining random sampling within non-government units (e.g.: 240 kilometers around each data-collector). Spatial analysis also could optimize data-collectors’ work plans and resource allocation. Spatial analytic and processing platform helped us handling the spatial random sampling challenges. Our method fits in FDA’s ability to pinpoint features of foodservice establishments, and reduced both time and expense on data collection.

Keywords: Geospatial technology, restaurant, retail food risk factors study, spatial random sampling.

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Authors: Rezvan Najafi, Korosh Heydari, Massoud Saidijam

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5-FU is a chemotherapeutic agent that has been used in colorectal cancer (CRC) treatment. However, it is usually associated with the acquired resistance, which decreases the therapeutic effects of 5-FU. miR-200c is involved in chemotherapeutic drug resistance, but its mechanism is not fully understood. In this study, the effect of inhibition of miR-200c in sensitivity of HCT-116 CRC cells to 5-FU was evaluated. HCT-116 cells were transfected with LNA-anti- miR-200c for 48 h. mRNA expression of miR-200c was evaluated using quantitative real- time PCR. The protein expression of phosphatase and tensin homolog (PTEN) and E-cadherin were analyzed by western blotting. Annexin V and propidium iodide staining assay were applied for apoptosis detection. The caspase-3 activation was evaluated by an enzymatic assay. The results showed LNA-anti-miR-200c inhibited the expression of PTEN and E-cadherin protein, apoptosis and activation of caspase 3 compared with control cells. In conclusion, these results suggest that miR-200c as a prognostic marker can overcome to 5-FU chemoresistance in CRC.

Keywords: Colorectal cancer, miR-200c, 5-FU resistance, E-cadherin, PTEN.

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Authors: Nhien-An Le-Khac, Sammer Markos, M-Tahar Kechadi

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Today, money laundering (ML) poses a serious threat not only to financial institutions but also to the nation. This criminal activity is becoming more and more sophisticated and seems to have moved from the cliché of drug trafficking to financing terrorism and surely not forgetting personal gain. Most international financial institutions have been implementing anti-money laundering solutions (AML) to fight investment fraud. However, traditional investigative techniques consume numerous man-hours. Recently, data mining approaches have been developed and are considered as well-suited techniques for detecting ML activities. Within the scope of a collaboration project for the purpose of developing a new solution for the AML Units in an international investment bank, we proposed a data mining-based solution for AML. In this paper, we present a heuristics approach to improve the performance for this solution. We also show some preliminary results associated with this method on analysing transaction datasets.

Keywords: data mining, anti money laundering, clustering, heuristics.

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Authors: Virupakshaiah DBM, Madiha Ahmed, Smita T. Patil, Chandrakanth Kelmani

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Tuberculosis (TB) is a bacterial infectious disease caused by the obligate human pathogen, Mycobacterium tuberculosis. Multidrug-resistant tuberculosis (MDR-TB) is a global reality that threatens tuberculosis control. Resistance to antibiotic Rifampicin, occurs in 95% of cases through nucleotide substitutions in an 81-bp core region of the rpoB i.e; beta subunit of DNA dependant RNA polymerase. In this paper, we studied the Rifampicin-rpoB receptor interactions In silico. First, homology modeling was performed to obtain the three dimensional structure of Mycobacterium rpoB. Sixty analogs of Rifampicin were prepared using Marvin sketch software. Both original Rifampicin and the analogs were docked with rpoB and energy values were obtained. Out of sixty analogs, 43 analogs had lesser energy values than conventional Rifampicin and hence are predicted to have greater binding affinity to rpoB. Thus, this study offers a route for the development of Rifampicin analogs against multi drug resistant Mycobacterium rpoB.

Keywords: Marvin Sketch, Mycobacterium tuberculosis, Rifampicin, rpoB.

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Authors: Rungsinee Phongpradist, Sawitree Chiampanichayakul, Singkome Tima, Teruna J. Siahaan, Cory J. Berkland, Songyot Anuchapreeda, Chadarat Ampasavate

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The expression of LFA-1 diverges from the physiological condition, thus active targeting carrier can provide the benefits from difference into LFA-1 expression in various conditions. Here, the selectivity of cIBR-conjugated nanoparticles (cIBR-NPs), in terms of uptake, was investigated using PBMCs, Mixed PBMCMolt- 3 cells and Molt-3 cells. The expressions of LFA-1 on Molt-3 cells, from flow cytometry and Western blot, possessed the highest level whereas PBMCs showed the lowest level. The kinetic uptake profiles of cIBR-NPs were obtained by flow cytometry, which the degree of cellular uptake presented a similar trend with the level of LFA-1 indicating the influence of LFA-1 expression on the cellular uptake of cIBR-NPs. The conformation of LFA-1 had a slight effect on the cellular uptake of cIBR-NPs. Overall we demonstrated that cIBR-NPs enhanced cellular uptake and improved the selectivity of drug carriers to LFA-1 on the leukemia cells, which related with the order of LFA-1 expression.

Keywords: cIBR, LFA-1, Molt-3, PBMCs

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Authors: Nafisur Rahman, Habibur Rahman, Syed Najmul Hejaz Azmi

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This paper presents a simple and sensitive kinetic spectrophotometric method for the determination of ramipril in commercial dosage forms. The method is based on the reaction of the drug with 1-chloro-2,4-dinitrobenzene (CDNB) in dimethylsulfoxide (DMSO) at 100 ± 1ºC. The reaction is followed spectrophotometrically by measuring the rate of change of the absorbance at 420 nm. Fixed-time (ΔA) and equilibrium methods are adopted for constructing the calibration curves. Both the calibration curves were found to be linear over the concentration ranges 20 - 220 μg/ml. The regression analysis of calibration data yielded the linear equations: Δ A = 6.30 × 10-4 + 1.54 × 10-3 C and A = 3.62 × 10-4 + 6.35 × 10-3 C for fixed time (Δ A) and equilibrium methods, respectively. The limits of detection (LOD) for fixed time and equilibrium methods are 1.47 and 1.05 μg/ml, respectively. The method has been successfully applied to the determination of ramipril in commercial dosage forms. Statistical comparison of the results shows that there is no significant difference between the proposed methods and Abdellatef-s spectrophotometric method.

Keywords: Equilibrium method, Fixed-time (ΔA) method, Ramipril, Spectrophotometry.

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Authors: Deepak Mohan, Sushma Sharma

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Diclofenac sodium, a member of the acetic acid family of non-steroidal anti-inflammatory drugs, is used to retard inflammation, arthritis pain and ankylosing spondylitis. The drug is known to cause severe injury in different tissues due to formation of reactive oxygen species. The present study is focused on the effect of different doses of diclofenac (4 mg/kg/body weight and 14 mg/kg/body weight on histoarchitecture of the liver from 7-28 days of the investigation. Diclofenac administration resulted in distorted hepatic degeneration and formation of wide areas in the form of sinusoidal gaps. Hepatic fibrosis noticed in different stages of investigation could be attributed to chronic inflammation and reactive oxygen species which results in deposition of extracellular matrix proteins. The abrupt degenerative changes observed during later stages of the experiment showed maximum damage to the liver, and there was enlargement of sinusoidal gaps accompanied by maximum necrosis in the tissues.

Keywords: Arthritis, diclofenac, histoarchitecture, sinusoidal.

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Authors: N. K. Sharma, J. Nayak, D. K. Sehgal, R. K. Pandey

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Bone material is treated as heterogeneous and hierarchical in nature therefore appropriate size of bone specimen is required to analyze its tensile properties at a particular hierarchical level. Tensile properties of cortical bone are important to investigate the effect of drug treatment, disease and aging as well as for development of computational and analytical models. In the present study tensile properties of buffalo as well as goat femoral and tibiae cortical bone are analyzed using sub-size tensile specimens. Femoral cortical bone was found to be stronger in tension as compared to the tibiae cortical bone and the tensile properties obtained using sub-size specimens show close resemblance with the tensile properties of full-size cortical specimens. A two dimensional finite element (FE) modal was also applied to simulate the tensile behavior of sub-size specimens. Good agreement between experimental and FE model was obtained for sub-size tensile specimens of cortical bone.

Keywords: Cortical bone, sub-size specimen, full size specimen, finite element modeling.

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Authors: Diky Mudhakir, Satrialdi, Sukmadjaja Asyarie, Yeyet C. Sumirtapura

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Today, cancer remains one of the major diseases that lead to death. The main obstacle in chemotherapy as a main cancer treatment is the toxicity to normal cells due to Multidrug Resistance (MDR) after the use of anticancer drugs. Proposed solution to overcome this problem is the use of MDR efflux inhibitor of cinchona alkaloids which is delivered together with anticancer drugs encapsulated in the form of polymeric nanoparticles. The particles were prepared by the hydration method. The characterization of nanoparticles was particle size, zeta potential, entrapment efficiency and in vitro drug release. Combination nanoparticle size ranged 29-45 nm with a neutral surface charge. Entrapment efficiency was above 87% for the use quinine, quinidine or cinchonidine in combination with etoposide. The release test results exhibited that the cinchona alkaloids release released faster than that of etoposide. Collectively, cinchona alkaloids can be packaged along with etoposide in nanomicelles for better cancer therapy.

Keywords: Cinchona alkaloids, etoposide, MDR efflux inhitor, polymeric nanomicelles.

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Authors: Jong Ho Hwang, Dae Hwan Kang, Young-IL Jeong

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Since hyaluronic acid (HA) receptor such as CD44 is over-expressed at sites of cancer cells, HA can be used as a targeting vehicles for anti-cancer drugs. The aim of this study is to synthesize block copolymer composed of hyaluronic acid and poly(ε-caprolactone) (HAPCL) and to fabricate polymeric micelles for anticancer drug targeting against CD44 receptor of tumor cells. Chemical composition of HAPCL was confirmed using 1H NMR spectroscopy. Doxorubicin (DOX) was incorporated into polymeric micelles of HAPCL. The diameters of HAPHS polymeric micelles were changed around 80nm and have spherical shapes. Targeting potential was investigated using CD44-overexpressing. When DOX-incorporated polymeric micelles was added to KB cells, they revealed strong red fluorescence color while blocking of CD44 receptor by pretreatment of free HA resulted in reduced intensity, indicating that HAPCL polymeric micelles have targetability against CD44 receptor.

Keywords: Hyaluronic acid, CD44 receptor, biorecognizable nanoparticles, block copolymer.

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Authors: U. Umadevi, T. Umakanthan

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Globally, mycotic dermatitis is very common but there is no single proven specific allopathic treatment regimen. In this study, domestic animals with skin diseases of different age and breed from geographically varied regions of Tamil Nadu state, India were employed. Most of them have had previous treatment with native and allopathic medicines without success. Clinically, the skin lesions were found to be mild to severe. The trial animals were treated with poly herbal formulation (ointment) prepared using the indigenous medicinal plants – viz Andrographis paniculata, Lawsonia inermis and Madhuca longifolia. Allopathic antifungal drugs and ointments, povidone iodine and curabless (Terbinafine HCl, Ofloxacin, Ornidazole, Clobetasol propionate) were used in control. Comparatively, trial animals were found to have lesser course of treatment time and higher recovery rate than control. In Ethnoveterinary, this combination was tried for the first time. This herbal formulation is economical and an alternative for skin diseases.

Keywords: Allopathic drugs, dermatitis, domestic animals, poly herbal formulation.

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Authors: W. P. Hu, J. V. Kumar, Jeffrey J. P. Tsai

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The inhibition of SH2 domain regulated protein-protein interactions is an attractive target for developing an effective chemotherapeutic approach in the treatment of disease. Molecular simulation is a useful tool for developing new drugs and for studying molecular recognition. In this study, we searched potential drug compounds for the inhibition of SH2 domain by performing structural similarity search in PubChem Compound Database. A total of 37 compounds were screened from the database, and then we used the LibDock docking program to evaluate the inhibition effect. The best three compounds (AP22408, CID 71463546 and CID 9917321) were chosen for MD simulations after the LibDock docking. Our results show that the compound CID 9917321 can produce a more stable protein-ligand complex compared to other two currently known inhibitors of Src SH2 domain. The compound CID 9917321 may be useful for the inhibition of SH2 domain based on these computational results. Subsequently experiments are needed to verify the effect of compound CID 9917321 on the SH2 domain in the future studies.

Keywords: Nonpeptide inhibitor, Src SH2 domain, LibDock, molecular dynamics simulation.

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Authors: Zeeshan Hamid, Asher Ramish

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The purpose of this paper is to focus on security and safety issues facing by pharmaceutical industry globally when counterfeit drugs are in question. Hence, there is an intense need to secure and authenticate pharmaceutical products in the emerging counterfeit product market. This paper will elaborate the application of radio frequency identification (RFID) in pharmaceutical industry and to identify its key benefits for patient’s care. The benefits are: help to co-ordinate the stream of supplies, accuracy in chains of supplies, maintaining trustworthy information, to manage the operations in appropriate and timely manners and finally deliver the genuine drug to patient. It is discussed that how RFID supported supply chain information sharing (SCIS) helps to combat against counterfeit drugs. And a solution how to tag pharmaceutical products; since, some products prevent RFID implementation in this industry. In this paper, a proposed model for pharma industry distribution suggested to combat against the counterfeit drugs when they are in supply chain.

Keywords: Supply chain, RFID, pharmaceutical industry, counterfeit drugs, patients care.

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Authors: Amudha Kadirvelu, Sunil Gurtu, Sivalal Sadasivan

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Pharmacology curriculum plays an integral role in medical education. Learning pharmacology to choose and prescribe drugs is a major challenge encountered by students. We developed pharmacology applied learning activities for first year medical students that included realistic clinical situations with escalating complications which required the students to analyze the situation and think critically to choose a safe drug. Tutor feedback was provided at the end of session. Evaluation was done to assess the students- level of interest and usefulness of the sessions in rational selection of drugs. Majority (98 %) of the students agreed that the session was an extremely useful learning exercise and agreed that similar sessions would help in rational selection of drugs. Applied learning sessions in the early years of medical program may promote deep learning and bridge the gap between pharmacology theory and clinical practice. Besides, it may also enhance safe prescribing skills.

Keywords: Medical education, pharmacology curriculum, applied learning, safe prescribing.

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Authors: Francesco Maiorana

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In this paper a one-dimension Self Organizing Map algorithm (SOM) to perform feature selection is presented. The algorithm is based on a first classification of the input dataset on a similarity space. From this classification for each class a set of positive and negative features is computed. This set of features is selected as result of the procedure. The procedure is evaluated on an in-house dataset from a Knowledge Discovery from Text (KDT) application and on a set of publicly available datasets used in international feature selection competitions. These datasets come from KDT applications, drug discovery as well as other applications. The knowledge of the correct classification available for the training and validation datasets is used to optimize the parameters for positive and negative feature extractions. The process becomes feasible for large and sparse datasets, as the ones obtained in KDT applications, by using both compression techniques to store the similarity matrix and speed up techniques of the Kohonen algorithm that take advantage of the sparsity of the input matrix. These improvements make it feasible, by using the grid, the application of the methodology to massive datasets.

Keywords: Clustering algorithm, Data mining, Feature selection, Grid, Kohonen Self Organizing Map.

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Authors: N. A. Zainuddin, I. Norhuda, I. S. Adeib, A. N. Mustapa, S. H. Sarijo

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Recently, RESS (Rapid Expansion Supercritical Solution) method has been used by researchers to produce fine particles for pharmaceutical drug substances. Since RESS technology acknowledges a lot of benefits compare to conventional method of ginger extraction, it is suggested to use this method to explore particle formation of bioactive compound from powder ginger. The objective of this research is to produce direct solid oil particles formation from ginger rhizome which contains valuable compounds by using RESS-CO₂ process. RESS experiments were carried using extraction pressure of 3000, 4000, 5000, 6000 and 7000psi and at different extraction temperature of 40, 45, 50, 55, 60, 65 and 70°C for 40 minutes extraction time and contant flowrate (24ml/min). From the studies conducted, it was found that at extraction pressure 5000psi and temperature 40°C, the smallest particle size obtained was 2.22μm on 99 % reduction from the original size of 370μm.

Keywords: Particle size, RESS, solid oil particle, supercritical carbon dioxide.

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Authors: Deepak Mohan, Sushma Sharma

Abstract:

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are a group of widely used drugs for the treatment of rheumatoid diseases and to relieve pain and inflammation due to their analgesic anti-pyretic and anti-inflammatory properties. The therapeutic and many of the toxic effects of NSAIDs result from reversible inhibition of enzymes in the cyclooxygenase (COX) group. In the present investigation the effect of the drug on the concentration of lipids, and on the activity of the enzymes i.e. acid and alkaline phosphatase, GOT, GPT and lipid peroxidase were studied. There was a significant enhancement in the activities of both acid and alkaline phosphatase after 21 days of treatment. Proportionate increase in the MDA contents was observed after different days of diclofenac treatment. Cellular damage in the liver resulted in decrease in the activity of both GOT (Glutamate oxaloacetate transaminase) and GPT (Glutamate pyruvate transaminase) in both low and high dose groups. Significant decrease in the liver contents was also observed in both dose groups.

Keywords: Anti-inflammatory, cyclooxygenase, glutamate oxaloacetate transaminase, malondialdehyde.

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Authors: Jeff Clarine, Chang-Shyh Peng, Daisy Sang

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Bioassay is the measurement of the potency of a chemical substance by its effect on a living animal or plant tissue. Bioassay data and chemical structures from pharmacokinetic and drug metabolism screening are mined from and housed in multiple databases. Bioassay prediction is calculated accordingly to determine further advancement. This paper proposes a four-step preprocessing of datasets for improving the bioassay predictions. The first step is instance selection in which dataset is categorized into training, testing, and validation sets. The second step is discretization that partitions the data in consideration of accuracy vs. precision. The third step is normalization where data are normalized between 0 and 1 for subsequent machine learning processing. The fourth step is feature selection where key chemical properties and attributes are generated. The streamlined results are then analyzed for the prediction of effectiveness by various machine learning algorithms including Pipeline Pilot, R, Weka, and Excel. Experiments and evaluations reveal the effectiveness of various combination of preprocessing steps and machine learning algorithms in more consistent and accurate prediction.

Keywords: Bioassay, machine learning, preprocessing, virtual screen.

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Authors: Diah Tri Widayati, Sunendar, Kresno Suharto, Pudji Asuti, Aris Junaid

Abstract:

Eight Etawah cross bred does were divided into two groups based on body condition score (BCS). Group I (BSC 2, body weight 25-30 kg; n = 4), and Group II (BSC 3, body weight, 35-40 kg, n=4). All does received intravaginal controlled internal drug release devices (CIDR) for 10 days, and a prostaglandin F2α at 48 h before CIDR removal. Estrus detection was carried out using vasectomized buck. Vaginal epithelium was taken to determine estrus cycle. Blood samples were taken every 3-6 hours, started from moment of CIDR removal until the end of estrus. The results showed vaginal histological indicated estrus occurred at the hours of 25 to 60 and 30 to 70 post CIDR removal in BCS 2 and 3, respectively. Progesterone peak of BCS 2 and BCS 3 were 0.18±0.31 and 0.48±0.31 ng/mL on the hour 0 post CIDR removal. Estradiol -17ß peak of each group was 53.25±35.08 and 89.91±92.84 pg/mL at 48 post CIDR removal. LH surge only occurred on BCS 3 groups, the LH concentrations were 9.9± 9.1; 4.5± 4.0; and 18.2± 9.1 ng/mL at 45, 48 and 51 hours post CIDR removal, respectively. It was concluded that the BCS had effects on vaginal histological changes and LH surge.

Keywords: Estrus synchronization, Vaginal histological changes, Progesterone, Estradiol -17ß , LH

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Authors: S. Nurashikin, E. Z. Rusley, A. Husaini

Abstract:

Kojic acid is an organic acid that is widely used as an ingredient for dermatological products, precursor for flavor enhancer and also as anti-inflammatory drug. The present study was undertaken to test the feasibility of pineapple residues as substrate for kojic acid production by Aspergillus flavus Link 44-1 via solid-state fermentation. The effect of initial moisture content, pH and incubation time on kojic acid fermentation was investigated. The best initial moisture content for kojic acid production from pineapple residues was observed at 70% (v/w) whereas initial culture pH 2.5 was identified to give high production of kojic acid. The optimal range of incubation time was identified between 8 and 14 days of incubation which corresponded to highest range of kojic acid produced. The results from this study pronounce the promising usability of pineapple residues as alternative substrate for kojic acid production by A. flavus Link 44-1.

Keywords: Aspergillus flavus, kojic acid, pineapple residues, solid state fermentation.

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Authors: Sang-Ho Baik

Abstract:

D-erythro-cyclohexylserine (D chiral unnatural β-hydroxy amino acid expected for the synthesis of drug for AIDS treatment. To develop a continuous bioconversion system with whole cell biocatalyst of D-threonine aldolase (D genes for the D-erythro-CHS production, D-threonine aldolase gene was amplified from Ensifer arboris 100383 by direct PCR amplication using two degenerated oligonucleotide primers designed based on genomic sequence of Shinorhizobium meliloti Sequence analysis of the cloned DNA fragment revealed one open-reading frame of 1059 bp and 386 amino acids. This putative D-TA gene was cloned into NdeI and EcoRI (pEnsi His-tag sequence or BamHI (pEnsi-DTA[2]) sequence of the pET21(a) vector. The expression level of the cloned gene was extremely overexpressed by E. coli BL21(DE3) transformed with pEnsi-DTA[1] compared to E. coli BL21(DE3) transformed with pEnsi-DTA[2]. When the cells expressing the wild used for D-TA enzyme activity, 12 mM glycine was successfully detected in HPLC analysis. Moreover, the whole cells harbouring the recombinant D-TA was able to synthesize D-erythro of 0.6 mg/ml in a batch reaction.

Keywords: About four key words or phrases in alphabetical order, separated by commas.

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Authors: Michaela Chovancova, Pavel Niedoba

Abstract:

For the treatment of acute and chronic lung diseases it is preferred to deliver medicaments by inhalation. The drug is delivered directly to tracheobronchial tree. This way allows the given medicament to get directly into the place of action and it makes rapid onset of action and maximum efficiency. The transport of aerosol particles in the particular part of the lung is influenced by their size, anatomy of the lungs, breathing pattern and airway resistance. This article deals with calculation of airway resistance in the lung model of Horsfield. It solves the problem of determination of the pressure losses in bifurcation and thus defines the pressure drop at a given location in the bronchial tree. The obtained data will be used as boundary conditions for transport of aerosol particles in a central part of bronchial tree realized by Computational Fluid Dynamics (CFD) approach. The results obtained from CFD simulation will allow us to provide information on the required particle size and optimal inhalation technique for particle transport into particular part of the lung.

Keywords: Human lungs, bronchial tree, pressure losses, airways resistance, flow, breathing.

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