Search results for: Antibacterial drugs
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 199

Search results for: Antibacterial drugs

199 An Antibacterial Dental Restorative Containing 3,4-Dichlorocrotonolactone: Synthesis, Formulation and Evaluation

Authors: Dong Xie, Leah Howard, Yiming Weng

Abstract:

The objective of this study was to synthesize and characterize 5-acryloyloxy-3,4-dichlorocrotonolactone (a furanone derivative), use this derivative to modify a dental restorative, and study the effect of the derivative on the antibacterial activity and compressive strength of the formed restorative. In this study, a furanone derivative was synthesized, characterized, and used to formulate a dental restorative. Compressive strength (CS) and S. mutans viability were used to evaluate the mechanical strength and antibacterial activity of the formed restorative. The fabricated restorative specimens were photocured and conditioned in distilled water at 37oC for 24 h, followed by direct testing for CS or/and incubating with S. mutans for 48 h for antibacterial testing. The results show that the modified dental restorative showed a significant antibacterial activity without substantially decreasing the mechanical strengths. With addition of the antibacterial derivative up to 30%, the restorative kept its original CS nearly unchanged but showed a significant antibacterial activity with 68% reduction in the S. mutans viability. Furthermore, the antibacterial function of the modified restorative was not affected by human saliva. The aging study also indicates that the modified restorative may have a long-lasting antibacterial function. It is concluded that this experimental antibacterial restorative may potentially be developed into a clinically attractive dental filling restorative due to its high mechanical strength and antibacterial function.

Keywords: Antibacterial, dental filling restorative, compressive strength, S. mutans viability.

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198 Antibacterial and Antifungal Activity Assesment of Nigella Sativa Essential Oils

Authors: Entela Haloci, Stefano Manfredini, Vilma Toska, Silvia Vertuani, Paola Ziosi, Irma Topi, Henri Kolani

Abstract:

Antifungal activities of ether and methanolic extracts of volatiles oils of Nigella Sativa seeds were tested against pathogenic bacterias and fungies strains.The volatile oil were found to have significant antifungal and antibacterial activities compare to tetracycline, cefuroxime and ciprofloxacin positive controls.The ether and methanolic esxtracts were compared to each other for antifungal and antibacterial activities and ether extracts showed stonger activity than methanolic one.

Keywords: Antifungal, antibacterial, essential oils, extraction, Nigella Sativa.

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197 Antibacterial Activity of Ethanol Extract from Some Thai Medicinal Plants against Campylobacter Jejuni

Authors: Achara Dholvitayakhun, Nathanon Trachoo

Abstract:

In this study, the forty Thai medicinal plants were used to screen the antibacterial activity against Campylobacter jejuni. Crude 95% ethanolic extracts of each plant were prepared. Antibacterial activity was investigated by the disc diffusion assay, and MICs and MBCs were determined by broth microdilution. The results of antibacterial screening showed that five plants have activity against C.jejuni including Adenanthera pavonina L., Moringa oleifera Lam., Annona squamosa L., Hibiscus sabdariffa L. and Eupotorium odortum L. The extraction of A. pavonina L. and A. squamosa L. produced an outstanding against C. jejuni, inhibiting growth at 62.5-125 and 250-500 μg/mL, respectively. The MBCs of two extracts were just 4-fold higher than MICs against C. jejuni, suggesting the extracts are bactericidal against this species. These results indicate that A. pavonina and A. squamosa could potentially be used in modern applications aimed at treatment or prevention of foodborne disease from C. jejuni.

Keywords: Antibacterial activity, Thai medicinal plants, Campylobacter jejuni

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196 Comparison of the Use of Vaccines or Drugs against Parasitic Diseases

Authors: H. Al-Khalaifa, A. Al-Nasser

Abstract:

The viewpoint towards the use of drugs or vaccines against avian parasitic diseases is one of the most striking challenges in avian medical parasitology. This includes many difficulties associated with drug resistance and in developing prophylactic vaccines. In many instances, the potential success of a vaccination in controlling parasitic diseases in poultry is well-documented. However, some medical, technical and financial limitations are still paramount. On the other hand, chemotherapy is not very well-recommended due to a number of medical limitations. But in the absence of an effective vaccine, drugs are used against parasitic diseases. This paper sheds light on some the advantages and disadvantages of using vaccination and drugs in controlling parasitic diseases in poultry species. The usage of chemotherapeutic drugs is discussed with some examples. Then, more light will be shed on using vaccines as a potentially effective and promising control tool.

Keywords: Drugs, parasitology, poultry, vaccines.

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195 Essential Oils of Polygonum L. Plants Growing in Kazakhstan and Their Antibacterial and Antifungal Activity

Authors: Dmitriy Yu. Korulkin, Raissa A. Muzychkina

Abstract:

The article represents the results of isolation and component chromatographic analysis of essential oils of Polygonum L. plants growing in Kazakhstan in commercial reserves at the territory of Kazakhstan. The results of research of antibacterial and antifungal activity of isolated compounds have been represented.

Keywords: Antibacterial, antifungal, bioactive substances, essential oils, isolation, Polygonum L.

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194 User Satisfaction and Acceptability of Dialogue Systems for Detecting Counterfeit Drugs

Authors: Oyelami M. Olufemi

Abstract:

The menace of counterfeiting pharmaceuticals/drugs has become a major threat to consumers, healthcare providers, drug manufacturers and governments. It is a source of public health concern both in the developed and developing nations. Several solutions for detecting and authenticating counterfeit drugs have been adopted by different nations of the world. In this article, a dialogue system-based drug counterfeiting detection system was developed and the results of the user satisfaction and acceptability of the system are presented. The results show that the users were satisfied with the system and the system was widely accepted as a means of fighting counterfeited drugs.

Keywords: Counterfeiting, dialogue system, drugs, voice application.

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193 Biosynthesis of Titanium Dioxide Nanoparticles and Their Antibacterial Property

Authors: Prachi Singh

Abstract:

This paper presents a low-cost, eco-friendly and reproducible microbe mediated biosynthesis of TiO2 nanoparticles. TiO2 nanoparticles synthesized using the bacterium, Bacillus subtilis, from titanium as a precursor, were confirmed by TEM analysis. The morphological characteristics state spherical shape, with the size of individual or aggregate nanoparticles, around 30-40 nm. Microbial resistance represents a challenge for the scientific community to develop new bioactive compounds. Here, the antibacterial effect of TiO2 nanoparticles on Escherichia coli was investigated, which was confirmed by CFU (Colony-forming unit). Further, growth curve study of E. coli Hb101 in the presence and absence of TiO2 nanoparticles was done. Optical density decrease was observed with the increase in the concentration of TiO2. It could be attributed to the inactivation of cellular enzymes and DNA by binding to electron-donating groups such as carboxylates, amides, indoles, hydroxyls, thiols, etc. which cause little pores in bacterial cell walls, leading to increased permeability and cell death. This justifies that TiO2 nanoparticles have efficient antibacterial effect and have potential to be used as an antibacterial agent for different purposes.

Keywords: Antibacterial effect, CFU, Escherichia coli Hb101, growth curve, TEM, TiO2 nanoparticle, toxicity, UV-Vis.

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192 Fatty Acid Extracts of Sea Pen (Virgularia gustaviana) and Their Potential Applications as Antibacterial, Antifungal, and Anti-Inflammatory Agents

Authors: Sharareh Sharifi

Abstract:

In this study, the crude extracts of Virgularia gustavina were examined as antibacterial, antifungal and anti-inflammatory agent. To assess inflammation, Xylene was applied to the ear of mice. The mice of the experimental group were fed with doses of 10 mg/kg, 20 mg/kg, and 40 mg/kg of lipid extract of chloroform and hexane as a separate group and then statistical analysis was performed on the results. Chloroform and hexane extracts of sea pen have strong anti-inflammatory effects even at low doses which is probably due to 54% arachidonic acid. Antibacterial and antifungal effects of hexane and chloroform extracts were measured with MIC and MBC methods and it is shown that chloroform extract has best activity against Staphylococcus aureus on 125 µg/ml doze in MIC method.

Keywords: Sea pen (Virgularia gustaviana), lipid extract, anti-inflammatory, antibacterial activity.

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191 Drug Use Knowledge and Antimicrobial Drug Use Behavior

Authors: Pimporn Thongmuang

Abstract:

The import value of Antimicrobial drugs reached approximately fifteen million Baht in 2010, considered as the highest import value of all modern drugs, and this value is rising every year. Antimicrobials are considered the hazardous drugs by the Ministry of Public Health (No. 10). This research was conducted in order to investigate the past knowledge of drug use and Antimicrobial drug use behavior. A total of 757 students were selected as the samples out of a population of 1,800 students. This selected students had the experience of Antimicrobial drugs use a year ago. A questionnaire was utilized in this research. The findings put on the view that knowledge gained by the students about proper use of Antimicrobials drugs was not brought into practice. This suggests that the education procedure regarding drug use needs adjustment. And therefore the findings of this research are expected to be utilized as guidelines for educating people about the proper use of Antimicrobials drugs. At a broader perspective, correct drug use behavior of the public may potentially reduce drug cost of the Ministry of Public Health of Thailand.

Keywords: Drug Use Knowledge, Antimicrobial Drugs, Drug Use Behavior.

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190 Risk of Occupational Exposure to Cytotoxic Drugs: The Role of Handling Procedures of Hospital Workers

Authors: J. Silva, P. Arezes, R. Schierl, N. Costa

Abstract:

In order to study environmental contamination by cytostatic drugs in Portugal hospitals, sampling campaigns were conducted in three hospitals in 2015 (112 samples). Platinum containing drugs and fluorouracil were chosen because both were administered in high amounts. The detection limit was 0.01 pg/cm² for platinum and 0.1 pg/cm² for fluorouracil. The results show that spills occur mainly on the patient`s chair, while the most referenced occurrence is due to an inadequately closed wrapper. Day hospitals facilities were detected as having the largest number of contaminated samples and with higher levels of contamination.

Keywords: Antineoplastic, drugs, exposure, surface.

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189 Antibacterial Activity of Some Medicinal Plant Extracts

Authors: Hayam M. Ibrahim, Ferial M. Abu-Salem

Abstract:

Medicinal plants are now gaining attractiveness in treatment of bacterial infections and food preservation. The objective of this study was to assess antibacterial activity of some medicinal plants on pathogenic bacteria. Screening of antibacterial activity of aqueous and methanol extracts of some plants: Jojoba, Ginger, Sage, Thyme and Clove against Bacillus cereus, Salmonella typhimurium, Staphylococcus aureus, Clostridium perfringens and Escherichia coli were investigated. Antibacterial activity was performed by agar diffusion and disc diffusion method. Jatropha, Jojoba, Clove and Ginger extracts showed notable bacterial activity in the first screening step then selected to be tested against Bacillus cereus (Gram+), Staphylococcus aureus (Gram+) and Salmonella typhimurium (Gram−) and their effect was compared using antibiotics as control. Screening results showed potential antibacterial activity of the tested plant extracts against the screened bacterial strains. It was found that methanol extracts exhibited higher antibacterial activity than aqueous extracts. Methanol extract of Jatropha showed the highest inhibition zone against Staphylococcus aureus (Gram+) with 24.00 mm diameter, compared to the other plant extracts followed by clove. Meanwhile, the inhibition zones of methanol extracts of Jojoba and Ginger were the same (12mm).The Gram-positive bacteria were found to be more sensitive to aqueous and methanol extracts than Gram-negative bacteria.

Keywords: Antibacterial activity, Food-borne pathogenic bacteria, Medicinal plants, Plant extracts.

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188 Comparison between Antibacterial Effects of Ethanolic and Isopropyl: Hexan (7:3) Extracts of Zingiber officinale Rose

Authors: Tahereh Naji, Mahsa Jassemi

Abstract:

In this investigation, the antibacterial effects of ethanolic and 7:3 isopropyl –hexane mixture extracts of Zingiber officinale were evaluated against three Gram positive bacteria, B. cereus, S.epidermidis, S. aureus and three Gram negative bacteria, E. coli, K.pneumonia and P.areuginosa. Utilizing paper disk diffusion and well methods in-vitro, MIC and MBC were determined by macrodilution. The results showed that ethanolic rhizome extract of ginger had significantly active than Isopropyl –hexan extract. Further work needs to be done in these extracts including fractionation to isolate active constituents and subsequent pharmacological evaluation.

Keywords: Antibacterial, Medicinal plant extract, Zingiberofficinale.

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187 Antioxydant and Antibacterial Activity of Alkaloids and Terpenes Extracts from Euphorbia granulata

Authors: Bousselessela H., Yahia M., Mahboubi A., Benbia S., Yahia Massinissa

Abstract:

In order to enhance the knowledge of certain phytochemical Algerian plants that are widely used in traditional medicine and to exploit their therapeutic potential in modern medicine, we have done a specific extraction of terpenes and alkaloids from the leaves of Euphorbia granulata to evaluate the antioxidant and antibacterial activity of this extracts. After the extraction it was found that the terpene extract gave the highest yield 59.72% compared with alkaloids extracts. The disc diffusion method was used to determine the antibacterial activity against different bacterial strains: Escherichia coli (ATCC25922), Pseudomonas aeruginosa (ATCC27853) and Staphylococcus aureus (ATCC25923). All extracts have shown inhibition of growth bacteria. The different zones of inhibition have varied from (7 -10 mm) according to the concentrations of extract used. Testing the antiradical activity on DPPH-TLC plates indicated the presence of substances that have potent anti-free radical. As against, the BC-TLC revealed that only terpenes extract which was reacted positively. These results can validate the importance of Euphorbia granulata in traditional medicine.

Keywords: Euphorbia granulata, Euphorbiaceae, alkaloids, terpenoids, antioxidant activity, antibacterial activity.

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186 Antibacterial Capacity of Plumeria alba Petals

Authors: M. H. Syakira, L. Brenda

Abstract:

Antibacterial activity of Plumeria alba (Frangipani) petals methanolic extracts were evaluated against Escherichia coli, Proteus vulgaris,Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus saprophyticus, Enterococcus faecalis and Serratia marcescens by using disk diffusion method. Concentration extracts (80 %) showed the highest inhibition zone towards Escherichia coli (14.3 mm). Frangipani extract also showed high antibacterial activity against Staphylococcus saprophyticus, Proteus vulgaris and Serratia marcescens, but not more than the zones of the positive control used. Comparison between two broad specrum antibiotics to frangipani extracts showed that the 80 % concentration extracts produce the same zone of inhibition as Streptomycin. Frangipani extracts showed no bacterial activity towards Klebsiella pneumoniae, Pseudomonas aeruginosa and Enterococcus faecalis. There are differences in the sensitivity of different bacteria to frangipani extracts, suggesting that frangipani-s potency varies between these bacteria. The present results indicate that frangipani showed significant antibacterial activity especially to Escherichia coli.

Keywords: Frangipani, Plumeria alba, anti microbial, Escherichia coli

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185 The Antibacterial and Anticancer Activity of Marine Actinomycete Strain HP411 Isolated in the Northern Coast of Vietnam

Authors: Huyen T. Pham, Nhue P. Nguyen, Tien Q. Phi, Phuong T. Dang, Hy G. Le

Abstract:

Since the marine environmental conditions are extremely different from the other ones, marine actinomycetes might produce novel bioactive compounds. Therefore, actinomycete strains were screened from marine water and sediment samples collected from the coastal areas of Northern Vietnam. Ninety-nine actinomycete strains were obtained on starch-casein agar media by dilution technique, only seven strains, named HP112, HP12, HP411, HPN11, HP 11, HPT13 and HPX12, showed significant antibacterial activity against both gram-positive and gram-negative bacteria (Bacillus subtilis ATCC 6633, Staphylococcus epidemidis ATCC 12228, Escherichia coli ATCC 11105). Further studies were carried out with the most active HP411 strain against Candida albicans ATCC 10231. This strain could grow rapidly on starch casein agar and other media with high salt containing 7-10% NaCl at 28-30oC. Spore-chain of HP411 showed an elongated and circular shape with 10 to 30 spores/chain. Identification of the strain was carried out by employing the taxonomical studies including the 16S rRNA sequence. Based on phylogenetic and phenotypic evidence it is proposed that HP411 to be belongs to species Streptomyces variabilis. The potent of the crude extract of fermentation broth of HP411 that are effective against wide range of pathogens: both grampositive, gram-negative and fungi. Further studies revealed that the crude extract HP411 could obtain the anticancer activity for cancer cell lines: Hep-G2 (liver cancer cell line); RD (cardiac and skeletal muscle letters cell line); FL (membrane of the uterus cancer cell line). However, the actinomycetes from marine ecosystem will be useful for the discovery of new drugs in the future.

Keywords: Marine actinomycetes, antibacterial, anticancer, Streptomyces variabilis.

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184 The Effects of Media Campaigns on Different Cultures

Authors: B. Al-Jenaibi

Abstract:

The paper examines the Most public relations spots and advertisements dealing with drugs. For this reason, public service advertisements show Americans in activities with drugs and alcohol. The way that the advertisements are produced, viewers from the Middle East say these ads are not for them. They recognize the ads as strictly for Americans trying to overcome their problems with drugs and alcohol. Also, this paper explores the development of the advertisements which are ineffective in other cultures like the Islamic because the limited scope of the message does not have a major effect on the Islamic beliefs and practices.

Keywords: Arab media campaign, Middle easy Advertisements, Islamic culture and American campaigns.

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183 Counterfeit Drugs Prevention in Pharmaceutical Industry with RFID: A Framework Based On Literature Review

Authors: Zeeshan Hamid, Asher Ramish

Abstract:

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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182 Computer Aided Docking Studies on Antiviral Drugs for SARS

Authors: Virupakshaiah DBM, Chandrakanth Kelmani, Rachanagouda Patil, Prasad Hegade

Abstract:

Severe acute respiratory syndrome (SARS) is a respiratory disease in humans which is caused by the SARS coronavirus. The treatment of coronavirus-associated SARS has been evolving and so far there is no consensus on an optimal regimen. The mainstream therapeutic interventions for SARS involve broad-spectrum antibiotics and supportive care, as well as antiviral agents and immunomodulatory therapy. The Protein- Ligand interaction plays a significant role in structural based drug designing. In the present work we have taken the receptor Angiotensin converting enzyme 2 and identified the drugs that are commonly used against SARS. They are Lopinavir, Ritonavir, Ribavirin, and Oseltamivir. The receptor Angiotensin converting enzyme 2 (ACE-2) was docked with above said drugs and the energy value obtained are as follows, Lopinavir (-292.3), Ritonavir (-325.6), Oseltamivir (- 229.1), Ribavirin (-208.8). Depending on the least energy value we have chosen the best two drugs out of the four conventional drugs. We tried to improve the binding efficiency and steric compatibility of the two drugs namely Ritonavir and Lopinavir. Several modifications were made to the probable functional groups (phenylic, ketonic groups in case of Ritonavir and carboxylic groups in case of Lopinavir respectively) which were interacting with the receptor molecule. Analogs were prepared by Marvin Sketch software and were docked using HEX docking software. Lopinavir analog 8 and Ritonavir analog 11 were detected with significant energy values and are probable lead molecule. It infers that some of the modified drugs are better than the original drugs. Further work can be carried out to improve the steric compatibility of the drug based upon the work done above for a more energy efficient binding of the drugs to the receptor.

Keywords: Protein data bank, Rasmol, Marvin sketch, Hexdocking.

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181 Probiotics’ Antibacterial Activity on Beef and Camel Minced Meat at Altered Ranges of Temperature

Authors: Rania Samir Zaki

Abstract:

Because of their inhibitory effects, selected probiotic Lactobacilli may be used as antimicrobial against some hazardous microorganisms responsible for spoilage of fresh minced beef (cattle) minced meat and camel minced meat. Lactic acid bacteria were isolated from camel meat. These included 10 isolates; 1 Lactobacillus fermenti, 4 Lactobacillus plantarum, 4 Lactobacillus pulgaricus, 3 Lactobacillus acidophilus and 1 Lactobacillus brevis. The most efficient inhibitory organism was Lactobacillus plantarum which can be used as a propiotic with antibacterial activity. All microbiological analyses were made at the time 0, first day and the second day at altered ranges of temperature [4±2 ⁰C (chilling temperature), 25±2 ⁰C, and 38±2 ⁰C]. Results showed a significant decrease of pH 6.2 to 5.1 within variant types of meat, in addition to reduction of Total Bacterial Count, Enterococci, Bacillus cereus and Escherichia coli together with the stability of Coliforms and absence of Staphylococcus aureus.

Keywords: Antibacterial, camel meat, inhibition, probiotics.

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180 Synthesis and in vitro Characterization of a Gel-Derived SiO2-CaO-P2O5-SrO-Li2O Bioactive Glass

Authors: Mehrnaz Aminitabar, Moghan Amirhosseinian, Morteza Elsa

Abstract:

Bioactive glasses (BGs) are a group of surface-reactive biomaterials used in clinical applications as implants or filler materials in the human body to repair and replace diseased or damaged bone. Sol-gel technique was employed to prepare a SiO2-CaO-P2O5 glass with nominal composition of 58S BG with the addition of Sr and Li modifiers which imparts special properties to the BG. The effect of simultaneous addition of Sr and Li on bioactivity and biocompatibility, proliferation, alkaline phosphatase (ALP) activity of osteoblast cell line MC3T3-E1 and antibacterial property against methicillin-resistant Staphylococcus aureus (MRSA) bacteria were examined. BGs were characterized by X-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy before and after soaking the samples in the simulated body fluid (SBF) for different time intervals to characterize the formation of hydroxyapatite (HA) formed on the surface of BGs. Structural characterization indicated that the simultaneous presence of 5% Sr and 5% Li in 58S-BG composition not only did not retard HA formation because of opposite effect of Sr and Li of the dissolution of BG in the SBF but also, stimulated the differentiation and proliferation of MC3T3-E1s. Moreover, the presence of Sr and Li on dissolution of the ions resulted in an increase in the mean number of DAPI-labeled nuclei which was in good agreement with live/dead assay. The result of antibacterial tests revealed that Sr and Li-substituted 58S BG exhibited a potential antibacterial effect against MRSA bacteria. Because of optimal proliferation and ALP activity of MC3T3-E1cells, proper bioactivity and high antibacterial potential against MRSA, BG-5/5 is suggested as a multifunctional candidate for bone tissue engineering.

Keywords: Antibacterial activity, bioactive glass, sol-gel, strontium.

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179 Antimicrobial Activity of Girardinia heterophylla

Authors: P. S. Bedi, Neayti Thakur, Balvinder Singh

Abstract:

In the present study an attempt has been made to prepare the crude extracts of leaves and stem of ‘Girardinia heterophylla’ by using various solvents like petroleum ether, ethanol and double distilled water. The samples were given the code NGLS 1, NGLS 2, NGLS 3 and NGSS 1, NGSS 2 and NGSS 3 respectively. All the extracts were used to study their antimicrobial activity against gram positive bacteria e.g. Bacillus subtilis, gram negative bacteria e.g. E. coli and K. pneumonia and antifungal activity against Aspergillus niger. The results of the antimicrobial activity showed that all the crude extracts of the plant possesses antibacterial activity. Maximum antibacterial activity was shown by NGLS 2, NGLS 3 and NGSS 3 against K. pneumonia. The growth of fungus A. niger was also inhibited by all the crude extracts. Maximum inhibition was shown by NGSS 2 followed by NGSS 1.

Keywords: Girardinia heterophylla, leaves and stem extracts, antibacterial activity, antifungal activity.

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178 Novel Inhibitor of E. coli DNA Adenine Methyltransferase (Ecodam)

Authors: H. Elsawy, A. Jeltsch

Abstract:

EcoDam is an adenine-N6 DNA methyltransferase that methylates the GATC sites in the Escherichia coli genome. DNA-adenine methylation is not present in higher eukaryotes including humans. These observations raise the possibility that dam inhibitors may be used as anti-microbial agents. Polyphosphate (Poly(P)) is an important metabolite and signaling molecule in prokaryotes and eukaryotes. Here, by using gel retardation experiments to investigate the competition of DNA binding by EcoDam in the presence of polyphosphate, we found that Poly (P) strongly interferes with DNA binding by EcoDam, while same concentration of monophosphate does not. In addition, we demonstrated that Poly (P) binding inhibits the activity of EcoDam and our results suggest that Poly (P) led to strong inhibition of the EcoDam catalytic activity, while monophosphate had only moderate effect.

Keywords: Antibacterial drugs, EcoDam inhibitors, Polyphosphate.

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177 Combining Similarity and Dissimilarity Measurements for the Development of QSAR Models Applied to the Prediction of Antiobesity Activity of Drugs

Authors: Irene Luque Ruiz, Manuel Urbano Cuadrado, Miguel Ángel Gómez-Nieto

Abstract:

In this paper we study different similarity based approaches for the development of QSAR model devoted to the prediction of activity of antiobesity drugs. Classical similarity approaches are compared regarding to dissimilarity models based on the consideration of the calculation of Euclidean distances between the nonisomorphic fragments extracted in the matching process. Combining the classical similarity and dissimilarity approaches into a new similarity measure, the Approximate Similarity was also studied, and better results were obtained. The application of the proposed method to the development of quantitative structure-activity relationships (QSAR) has provided reliable tools for predicting of inhibitory activity of drugs. Acceptable results were obtained for the models presented here.

Keywords: Graph similarity, Nonisomorphic dissimilarity, Approximate similarity, Drugs activity prediction.

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176 Synthesis, Characterization and Antibacterial Screening of 3-Hydroxy-2-[3-(2/3/4-Methoxybenzoyl)Thioureido]Butyric Acid

Authors: M. S. M. Yusof, R. Ramli, S. K. C. Soh, N. Ismail, N. Ngah

Abstract:

This study presents the synthesis of a series of methoxybenzoylthiourea amino acid derivatives. The compounds were obtained from the reactions between 2/3/4-methoxybenzoyl isothiocyanate with threonine. All of the compounds were characterized via mass spectrometry, 1H and 13C NMR spectrometry, UV-Vis spectrophotometer and FT-IR spectroscopy. Mass spectra for all of the compounds showed the presence of molecular ion [M]+ peaks at m/z 312, which are in agreement to the calculated molecular weight. For 1H NMR spectra, the presence of OCH3, C=S-NH and C=O-NH protons were observed within range of δH 3.8-4.0 ppm, 11.1-11.5 ppm and 10.0-11.5 ppm, respectively. 13C NMR spectra in all compounds displayed the presence of OCH3, C=O-NH, C=O-OH and C=S carbon resonances within range of δC 55.0-57.0 ppm, 165.0-168.0 ppm, 170.0-171.0 ppm and 180.0-182.0 ppm, respectively. In UV spectra, two absorption bands have been observed and both were assigned to the n-π* and π-π* transitions. Six vibrational modes of v(N-H), v(O-H), v(C=O-OH), v(C=O-NH), v(C=C) aromatic and v(C=S) appeared in the FT-IR spectra within the range of 3241-3467 cm-1, 2976-3302 cm-1, 1720-1768 cm-1, 1655-1672 cm-1, 1519-1525 cm-1 and 754-763 cm-1, respectively. The antibacterial activity for all of the compounds was screened against Staphylococcus aureus, Staphylococcus epidermidis, Salmonella typhimurium and Escherichia coli. However, no activity was observed.

Keywords: Methoxybenzoyl isothiocyanate, amino acid, threonine, antibacterial.

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175 Preparation and Characterization of Chitosan / Polyacrylic Acid / Ag-Nanoparticles Composite Membranes

Authors: Abdel-Mohdy, A. Abou-Okeil, S. El-Sabagh, S. M. El-Sawy

Abstract:

Chitosan polyacrylic acid composite membranes were prepared by a bulk polymerization method in presence of N, N'- methylene bisacrylamide (crosslinker) and ammonium persulphate as initiator. Membranes prepared from this copolymer in presence and absence of Ag nanoparticles were characterized by measuring mechanical and physical properties, water up-take and antibacterial properties. The results obtained indicated that the prepared membranes have antibacterial properties which increase with adding Ag nanoparticles.

Keywords: Ag nanoparticles, antimicrobial, composites, Membrane, physical properties.

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174 Surfactant-Free O/W-Emulsion as Drug Delivery System

Authors: M. Kumpugdee-Vollrath, J.-P. Krause, S. Bürk

Abstract:

Most of the drugs used for pharmaceutical purposes are poorly water-soluble drugs. About 40% of all newly discovered drugs are lipophilic and the numbers of lipophilic drugs seem to increase more and more. Drug delivery systems such as nanoparticles, micelles or liposomes are applied to improve their solubility and thus their bioavailability. Besides various techniques of solubilization, oil-in-water emulsions are often used to incorporate lipophilic drugs into the oil phase. To stabilize emulsions surface active substances (surfactants) are generally used. An alternative method to avoid the application of surfactants was of great interest. One possibility is to develop O/W-emulsion without any addition of surface active agents or the so called “surfactant-free emulsion or SFE”. The aim of this study was to develop and characterize SFE as a drug carrier by varying the production conditions. Lidocaine base was used as a model drug. The injection method was developed. Effects of ultrasound as well as of temperature on the properties of the emulsion were studied. Particle sizes and release were determined. The long-term stability up to 30 days was performed. The results showed that the surfactant-free O/W emulsions with pharmaceutical oil as drug carrier can be produced.

Keywords: Emulsion, lidocaine, Miglyol, size, surfactant, light scattering, release, injection, ultrasound, stability.

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173 Comparative Study of Calcium Content on in vitro Biological and Antibacterial Properties of Silicon-Based Bioglass

Authors: Morteza Elsa, Amirhossein Moghanian

Abstract:

The major aim of this study was to evaluate the effect of CaO content on in vitro hydroxyapatite formation, MC3T3 cells cytotoxicity and proliferation as well as antibacterial efficiency of sol-gel derived SiO2–CaO–P2O5 ternary system. For this purpose, first two grades of bioactive glass (BG); BG-58s (mol%: 60%SiO2–36%CaO–4%P2O5) and BG-68s (mol%: 70%SiO2–26%CaO–4%P2O5)) were synthesized by sol-gel method. Second, the effect of CaO content in their composition on in vitro bioactivity was investigated by soaking the BG-58s and BG-68s powders in simulated body fluid (SBF) for time periods up to 14 days and followed by characterization inductively coupled plasma atomic emission spectrometry (ICP-AES), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and scanning electron microscopy (SEM) techniques. Additionally, live/dead staining, 3-(4,5dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), and alkaline phosphatase (ALP) activity assays were conducted respectively, as qualitatively and quantitatively assess for cell viability, proliferation and differentiations of MC3T3 cells in presence of 58s and 68s BGs. Results showed that BG-58s with higher CaO content showed higher in vitro bioactivity with respect to BG-68s. Moreover, the dissolution rate was inversely proportional to oxygen density of the BG. Live/dead assay revealed that both 58s and 68s increased the mean number live cells which were in good accordance with MTT assay. Furthermore, BG-58s showed more potential antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) bacteria. Taken together, BG-58s with enhanced MC3T3 cells proliferation and ALP activity, acceptable bioactivity and significant high antibacterial effect against MRSA bacteria is suggested as a suitable candidate in order to further functionalizing for delivery of therapeutic ions and growth factors in bone tissue engineering.

Keywords: Antibacterial, bioactive glass, hydroxyapatite, proliferation, sol-gel processes.

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172 Investigating the Formation of Nano-Hydroxyapatite on a Biocompatible and Antibacterial Cu/Mg-Substituted Bioglass

Authors: Elhamalsadat Ghaffari, Moghan Amirhosseinian, Amir Khaleghipour

Abstract:

Multifunctional bioactive glasses (BGs) are designed with a focus on the provision of bactericidal and biological properties desired for angiogenesis, osteogenesis, and ultimately potential applications in bone tissue engineering. To achieve these, six sol-gel copper/magnesium substituted derivatives of 58S-BG, i.e. a mol% series of 60SiO2-4P2O5-5CuO-(31-x) CaO/xMgO (where x=0, 1, 3, 5, 8, and 10), were synthesized. Afterwards, the effect of MgO/CaO substitution on the in vitro formation of nano-hydroxyapatite (HA), osteoblast-like cell responses and BGs antibacterial performance were studied. During the BGs synthesis, the elimination of nitrates was achieved at 700 °C that prevented the BGs crystallization and stabilized the obtained dried gels. The structural and morphological evaluations were performed with X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). These characterizations revealed that Cu-substituted 58S-BG consisting of 5 mol% MgO (BG-5/5) slightly had retarded the formation of HA. In addition, Cu-substituted 58S-BGs consisting 8 mol% and 10 mol% MgO (BG-5/8 and BG-5/10) displayed lower bioactivity probably due to the lower ion release rate of Ca–Si into the simulated body fluid (SBF). The determination of 3-(4, 5 dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) and alkaline phosphate (ALP) activities proved that the highest values of both differentiation and proliferation of MC3T3-E1 cells can be obtained from a 5 mol% MgO substituted BG, while the over addition of MgO (8 mol% and 10 mol%) decreased the bioactivity. Furthermore, these novel Cu/Mg-substituted 58S-BGs displayed antibacterial effect against methicillin-resistant Staphylococcus aureus bacteria. Taken together, the results suggest the equally-substituted BG-5/5 (i.e. the one consists of 5 mol% of both CuO and MgO) as a promising candidate for bone tissue engineering, among all newly designed BGs in this work, owing to its desirable cell proliferation, ALP activity and antibacterial properties.

Keywords: Apatite, bioactivity, biomedical applications sol-gel processes.

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171 Study on Phytochemical Properties, Antibacterial Activity and Cytotoxicity of Aloe vera L.

Authors: K. Thu, Yin Y. Mon, Tin A. Khaing, Ohn M. Tun

Abstract:

The aim of the study was to investigate phytochemical properties, antimicrobial activity and cytotoxicity of Aloe vera. The phytochemical screening of the extracts of leaves of A. vera revealed the presence of bioactive compounds such as alkaloids, tannins, flavonoids phenolic compounds, and etc. with absence of cyanogenic glycosides. Three different solvents such as methanol, ethanol and Di-Methyl sulfoxide were used to screen the antimicrobial activity of A. vera leaves against four human clinical pathogens by agar well diffusion method. The maximum antibacterial activities were observed in methanol extract followed by ethanol and Di-Methyl sulfoxide. It was also found that remarkable antibacterial activities with methanolic and ethanolic extracts of A. vera compared with the standard antibiotic, tetracycline that was not active against E. coli and S. boydii and supported the view that A. vera is a potent antimicrobial agent compared with the conventional antibiotic. Moreover, the brine shrimps (Artemia salina) toxicity test exhibited LC50 value was 569.52 ppm. The resulting data indicated that the A. vera plant have less toxic effects on brine shrimp. Hence, it is signified that Aloe vera plant extract is safe to be used as an antimicrobial agent.

Keywords: Aloe vera L., antimicrobial activity, brine shrimp, cytotoxicity, phytochemical properties.

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170 Anti-Diabetic Effect of Bryophyllum pinnatum Leaves

Authors: E. F. Aransiola, M.O. Daramola, E. O. Iwalewa, A. M. Seluwa, O. O. Olufowobi

Abstract:

Diabetes is a chronic metabolic disorder that affects the quality of life in terms of physical health, social and psychological well-being. In spite of the enormous progress in the treatment of diabetes using existing commercial drugs, such as, insulin and oral hypoglycemic agents, the quest and search for new drugs is imperative due to several limitations of the commercial drugs. In addition, the existing diabetic drugs are expensive and unaffordable by the rural populace in the developing countries. The present study demonstrates the anti-diabetic property of aqueous extract of Bryophyllum pinnatum (BP) leaves using diabetic rats (albino rats) as models. At the same time, the anti-diabetic effect of the aqueous extract was compared to that of a sample containing a mixture of the extract and a commercial diabetic medicine, glibenclamide. A specified dosage of aqueous extract of Bryophyllum pinnatum (BP) leaves was administered on the experimental diabetic rats, and their BGL was measured and recorded. The results showed a significant drop in the BGL of the diabetic rats to a value close to normal blood glucose level within 120 minutes when only aqueous extract from BP leaves was used. When a sample containing a mixture of the aqueous extract and glibenclamide was administered, a further drop in BGL was observed. Therefore, the results reveal that aqueous extract of Bryophyllum pinnatum leaves have significant anti-diabetic properties, and that the performance of the existing drugs (glibenclamide) could be enhanced with the use of the aqueous extract.

Keywords: Anti-diabetics, Bryophyllum pinnatum, Blood glucose level, albino rats.

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