Synthesis, Physicochemical Characterization and Study of the Antimicrobial Activity of Chlorobutanol

Introduction and objectives: Chlorobutanol is a raw material, mainly used as an antiseptic and antimicrobial preservative in injectable and ophthalmic preparations. The main objective of our study was the synthesis and evaluation of the antimicrobial activity of chlorobutanol hemihydrates. Material and methods: Chlorobutanol was synthesized according to the nucleophilic addition reaction of chloroform to acetone, identified by an infrared absorption using Spectrum One FTIR spectrometer, melting point, Scanning electron microscopy and colorimetric reactions. The dosage of carvedilol active substance was carried out by assaying the degradation products of chlorobutanol in a basic solution. The chlorobutanol obtained was subjected to bacteriological tests in order to study its antimicrobial activity. The antibacterial activity was evaluated against strains such as Escherichia coli (ATCC 25 922), Staphylococcus aureus (ATCC 25 923) and Pseudomonas aeroginosa (ATCC = American type culture collection). The antifungal activity was evaluated against human pathogenic fungal strains, such as Candida albicans and Aspergillus niger provided by the parasitology laboratory of the Hospital of Tizi-Ouzou, Algeria. Results and discussion: Chlorobutanol was obtained in an acceptable yield. The characterization tests of the product obtained showed a white and crystalline appearance (confirmed by scanning electron microscopy), solubilities (in water, ethanol and glycerol), and a melting temperature in accordance with the requirements of the European pharmacopoeia. The colorimetric reactions were directed towards the presence of a trihalogenated carbon and an alcohol function. The spectral identification (IR) showed the presence of characteristic chlorobutanol peaks and confirmed the structure of the latter. The microbiological study revealed an antimicrobial effect on all strains tested (Sataphylococcus aureus (MIC = 1250 µg/ml), E. coli (MIC = 1250 µg/ml), Pseudomonas aeroginosa (MIC = 1250 µg/ml), Candida albicans (MIC =2500 µg/ml), Aspergillus niger (MIC =2500 µg/ml)) with MIC values close to literature data. Conclusion: Thus, on the whole, the synthesized chlorobutanol satisfied the requirements of the European Pharmacopoeia, and possesses antibacterial and antifungal activity; nevertheless, it is necessary to insist on the purification step of the product in order to eliminate the maximum impurities.

Synthesis, Physicochemical Characterization and Study of the Antimicrobial Activity of Chlorobutanol

Introduction and objectives: Chlorobutanol is a raw material, mainly used as an antiseptic and antimicrobial preservative in injectable and ophthalmic preparations. The main objective of our study was the synthesis and evaluation of the antimicrobial activity of chlorobutanol hemihydrates. Material and methods: Chlorobutanol was synthesized according to the nucleophilic addition reaction of chloroform to acetone, identified by an infrared absorption using Spectrum One FTIR spectrometer, melting point, Scanning electron microscopy and colorimetric reactions. The dosage of Carvedilol active substance was carried out by assaying the degradation products of chlorobutanol in a basic solution. The chlorobutanol obtained was subjected to bacteriological tests in order to study its antimicrobial activity. The antibacterial activity was evaluated against strains such as Escherichia coli (ATCC 25 922), Staphylococcus aureus (ATCC 25 923) and Pseudomonas aeroginosa (ATCC = American type culture collection). The antifungal activity was evaluated against human pathogenic fungal strains, such as Candida albicans and Aspergillus niger provided by the parasitology laboratory of the Hospital of Tizi-Ouzou, Algeria. Results and discussion: Chlorobutanol was obtained in an acceptable yield. The characterization tests of the product obtained showed a white and crystalline appearance (confirmed by scanning electron microscopy), solubilities (in water, ethanol and glycerol), and a melting temperature in accordance with the requirements of the European pharmacopoeia. The colorimetric reactions were directed towards the presence of a trihalogenated carbon and an alcohol function. The spectral identification (IR) showed the presence of characteristic chlorobutanol peaks and confirmed the structure of the latter. The microbiological study revealed an antimicrobial effect on all strains tested (Sataphylococcus aureus (MIC = 1250 µg/ml), E. coli (MIC = 1250 µg/ml), Pseudomonas aeroginosa (MIC = 1250 µg/ml), Candida albicans (MIC =2500 µg/ml), Aspergillus niger (MIC =2500 µg/ml)) with MIC values close to literature data. Conclusion: Thus, on the whole, the synthesized chlorobutanol satisfied the requirements of the European Pharmacopoeia, and possesses antibacterial and antifungal activity; nevertheless it is necessary to insist on the purification step of the product in order to eliminate the maximum impurities.

Antifungal Activity of Medicinal Plants Used Traditionally for the Treatment of Fungal Infections and Related Ailments in South Africa

The current study investigates the antifungal properties of crude plant extracts from selected medicinal plant species. Eight plant species used by the traditional healers and local people to treat fungal infections were selected for further phytochemical analysis and biological assay. The selected plant species were extracted with solvent of various polarities such as acetone, methanol, ethanol, hexane, dichloromethane, ethyl acetate and water. Leaf, roots and bark extracts of Maerua juncea Pax, Albuca seineri (Engl & K. Krause) J.C Manning & Goldblatt, Senna italica Mill., Elephantorrhiza elephantina (Burch.) Skeels, Indigofera circinata Benth., Schinus molle L., Asparagus buchananii Bak., were screened for antifungal activity against three animal fungal pathogens (Candida albicans, Aspergillus fumigatus and Cryptococcus neoformans). All plant extracts were active against the tested microorganisms. Acetone, dichloromethane, hexane and ethanol extracts of Senna italica and Elephantorrhiza elephantine had excellent activity against Candida albicans and A. fumigatus with the lowest MIC value of 0.02 mg/ml. Bioautography assay was used to determine the number of antifungal compounds presence in the plant extracts. No active compounds were observed in plant extracts of Indigofera circinnata, Schinus molle and Pentarrhinum insipidum with good antifungal activity against C. albicans and A. fumigatus indicating possible synergism between separated metabolites.

Encapsulation of Satureja khuzestanica Essential Oil in Chitosan Nanoparticles with Enhanced Antifungal Activity

During the recent years the six-fold growth of cancer in Iran has led the production of healthy products to become a challenge in the food industry. Due to the young population in the country, the consumption of fast foods is growing. The chemical cancer-causing preservatives are used to produce these products more than the standard; so using an appropriate alternative seems to be important. On the one hand, the plant essential oils show the high antimicrobial potential against pathogenic and spoilage microorganisms and on the other hand they are highly volatile and decomposed under the processing conditions. The study aims to produce the loaded chitosan nanoparticles with different concentrations of savory essential oil to improve the anti-microbial property and increase the resistance of essential oil to oxygen and heat. The encapsulation efficiency was obtained in the range of 32.07% to 39.93% and the particle size distribution of the samples was observed in the range of 159 to 210 nm. The range of Zeta potential was obtained between -11.9 to -23.1 mV. The essential oil loaded in chitosan showed stronger antifungal activity against Rhizopus stolonifer. The results showed that the antioxidant property is directly related to the concentration of loaded essential oil so that the antioxidant property increases by increasing the concentration of essential oil. In general, it seems that the savory essential oil loaded in chitosan particles can be used as a food processor.

Quantitative Structure Activity Relationship and Insilco Docking of Substituted 1,3,4-Oxadiazole Derivatives as Potential Glucosamine-6-Phosphate Synthase Inhibitors

Quantitative Structure Activity Relationship (QSAR) analysis has been developed to relate antifungal activity of novel substituted 1,3,4-oxadiazole against Candida albicans and Aspergillus niger using computer assisted multiple regression analysis. The study has shown the better relationship between antifungal activities with respect to various descriptors established by multiple regression analysis. The analysis has shown statistically significant correlation with R2 values 0.932 and 0.782 against Candida albicans and Aspergillus niger respectively. These derivatives were further subjected to molecular docking studies to investigate the interactions between the target compounds and amino acid residues present in the active site of glucosamine-6-phosphate synthase. All the synthesized compounds have better docking score as compared to standard fluconazole. Our results could be used for the further design as well as development of optimal and potential antifungal agents.

In vitro Susceptibility of Madurella mycetomatis to the Extracts of Anogeissus leiocarpus Leaves

Anogeissus leiocarpus (Combretaceae) is well known for its medicinal uses in African traditional medicine, for treating many human diseases mainly skin diseases and infections. Mycetoma disease is a fungal and/ or bacterial skininfection, mainly cause by Madurella mycetomatis fungus. This study was carried out in vitro to investigate the antifungal activity of Anogeissus leiocarpus leaf extracts against the isolated pathogenic Madurella mycetomatis, by using the NCCLS modified method compared to Ketoconazole standard drug, and MTT assay. The bioactive fraction was subjected to chemical analysis implementing different chromatographic analytical methods (TLC, HPLC, and LC-MS/MS). The results showed significance antifungal activity of A. leiocarpus leaf extracts against the isolated pathogenic M. mycetomatis, compared to negative and positive controls. The chloroform fraction showed the highest antifungal activity. The chromatographic analysis of the chloroform fraction with the highest activity showed the presence of important bioactive compounds such as ellagic and flavellagic acids derivatives, flavonoids and stilbenoid, which are well known for their antifungal activity.

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

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.

Improvement of Reaction Technology of Decalin Halogenation

In this research paper were investigated the main regularities of a radical bromination reaction of decalin. There had been studied the temperature effect, durations of reaction, frequency rate of process, a ratio of initial components, type and number of the initiator on decalin bromination degree. There were specified optimum conditions of synthesis of a perbromodecalin by the method of a decalin bromination. There are developed the technological flowchart of receiving a perbromodecalin and the mass balance of process on the first and the subsequent loadings of components. The results of research of antibacterial and antifungal activity of synthesized bromoderivatives have been represented.

Antibacterial and Antifungal Activity of Essential Oil of Eucalyptus camendulensis on a Few Bacteria and Fungi

Red River Gum (Eucalyptus camaldulensis) is a tree of the genus Eucalyptus widely distributed in Algeria and in the world. The value of its aromatic secondary metabolites offers new perspectives in the pharmaceutical industry. This strategy can contribute to the sustainable development of our country. Preliminary tests performed on the essential oil of Eucalyptus camendulensis showed that this oil has antibacterial activity vis-à-vis the bacterial strains (Enterococcus feacalis, Enterobacter cloaceai, Proteus microsilis, Escherichia coli, Klebsiella pneumonia, and Pseudomonas aeruginosa) and antifungic (Fusarium sporotrichioide and Fusarium graminearum). The culture medium used was nutrient broth Muller Hinton. The interaction between the bacteria and the essential oil is expressed by a zone of inhibition with diameters of MIC indirectly expression of. And we used the PDA medium to determine the fungal activity. The extraction of the aromatic fraction (essentially oilhydrolat) of the fresh aerian part of the Eucalyptus camendulensis was performed by hydrodistillation. The average essential oil yield is 0.99%. The antimicrobial and fungal study of the essential oil and hydrosol showed a high inhibitory effect on the growth of pathogens.

Levels of Some Antinutritional Factors in Tempeh Produced From Some Legumes and Jojobas Seeds

Three legumes i.e. soybean, kidney bean and mung bean, and jojoba seed as an oil seed were processed into tempeh, a fermented food. Changes in phytic acid, total phenols and trypsin inhibitor were monitored during the pretreatments (soaking, soaking– dehulling, washing and cooking) and fermentation with Rhizopus oligosporus. Soaking was found to reduce total phenol and trypsin inhibitor levels in soybean, kidney bean and mung bean. However, phytic acid was reduced by soaking in kidney bean and mung bean. Cooking was the most effective in reducing the activity of trypsin inhibitor. During fermentation, a slight increase in the level of trypsin inhibitor was noticed in soybean. Phytic acid and total phenols were decreased during fermentation in soybean, kidney bean but mung bean faild to form tempeh because the antifungal activity of herein a protein in mung bean, which exerts both chitinase activity and antifungal activity against a variety of fungal species. On the other hand, solid- state fermentation of jojoba seeds was not effective in reducing their content from cyanogenic glycosides (simmondsin).

Antimicrobial Activity of Girardinia heterophylla

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.

Antibacterial and Antifungal Activity Assesment of Nigella Sativa Essential Oils

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.

Evaluation of Antifungal Potential of Cenchrus pennisetiformis for the Management of Macrophomina phaseolina

Macrophomina phaseolina is a devastating soil-borne fungal plant pathogen that causes charcoal rot disease in many economically important crops worldwide. So far, no registered fungicide is available against this plant pathogen. This study was planned to examine the antifungal activity of an allelopathic grass Cenchrus pennisetiformis (Hochst. & Steud.) Wipff. for the management of M. phaseolina isolated from cowpea [Vigna unguiculata (L.) Walp.] plants suffering from charcoal rot disease. Different parts of the plants viz. inflorescence, shoot and root were extracted in methanol. Laboratory bioassays were carried out using different concentrations (0, 0.5, 1.0, …, 3.0 g mL-1) of methanolic extracts of the test allelopathic grass species to assess the antifungal activity against the pathogen. In general, extracts of all parts of the grass exhibited antifungal activity. All the concentrations of methanolic extracts of shoot and root significantly reduced fungal biomass by 20–73% and 40–80%, respectively. Methanolic shoot extract was fractionated using n-hexane, chloroform, ethyl acetate and n-butanol. Different concentrations of these fractions (3.125, 6.25, …, 200 mg mL-1) were analyzed for their antifungal activity. All the concentrations of n-hexane fraction significantly reduced fungal biomass by 15–96% over corresponding control treatments. Higher concentrations (12.5–200 mg mL-1) of chloroform, ethyl acetate and n-butanol also reduced the fungal biomass significantly by 29–100%, 46–100% and 24–100%, respectively.

Antifungal Activity of Silver Colloidal Nanoparticles against Phytopathogenic Fungus (Phomopsis sp.) in Soybean Seeds

Among the many promising nanomaterials with antifungal properties, metal nanoparticles (silver nanoparticles) stand out due to their high chemical activity. Therefore, the aim of this study was to evaluate the effect of silver nanoparticles (AgNPs) against Phomopsis sp. AgNPs were synthesized by silver nitrate reduction with sodium citrate and stabilized with ammonia. The synthesized AgNPs have further been characterized by UV/Visible spectroscopy, Biophysical techniques like Dynamic light scattering (DLS) and Scanning Electron Microscopy (SEM). The average diameter of the prepared silver colloidal nanoparticles was about 52 nm. Absolute inhibitions (100%) were observed on treated with a 270 and 540 µg ml-1 concentration of AgNPs. The results from the study of the AgNPs antifungal effect are significant and suggest that the synthesized silver nanoparticles may have an advantage compared with conventional fungicides.

Evaluation of the Inhibitory Effect of Some Plant Crude Extracts Against Albugo Candida, the Causal Agent of White Rust

White rust, caused by Albugo candida, is the most destructive foliar diseases of persian cress, Lepidium sativum in Iran. Application of fungicide is the most common method for the disease control. However, regarding the problems created by synthetic pesticides application, environmentally safe methods are needed to replace chemical pesticides. In this study, the antifungal activity of plant natural extracts was investigated for their ability to inhibit zoospore release from sporangia of A. candida. The crude extract of 46 plants was obtained using methanol. The inhibitory effect of the extracts was examined by mixing the plant extracts with a zoosporangial suspension of A. candida (1×106 spore/ml) at three concentrations, 250, 100 and 50 ppm. The experiments were conducted in a completely randomized design, with three replicates. The results of the experiment showed that three out of 46 plants species, including, Rhus coriaria, Anagallis arvensis and Mespilus germanica were completely inhibit zoospore release from zoosporangia of Albugo candida at concentration of 50 ppm.

Evaluation of the Antifungal and Antioxidant Activities of the Leaf Extract of Aloe vera(Aloe barbadensis Miller)

Aloe vera has been used worldwide both for pharmaceutical, food, and cosmetic industries due to the plethora of biological activities of some of its metabolites. The aim of this study was to evaluate the antifungal and antioxidant activities of the leaf extract. The antifungal activity was determined by the agar-well diffusion method against plant and human fungal pathogens. The methanol and ethanol portions of the extracts studied were more bioactive than ethyl acetate portion. It was also observed that the activity was more pronounced on plant pathogen than human pathogen except Candida albicans. This is an indication that the extract has the potential to treat plant fungal infections. The Aloe extract showed the significant antioxidant activity by the DPPH radical scavenging method. Therefore, the Aloe extract provided as natural antioxidant has been used in health foods for medical and preservative purposes.

Effect of Crude Extract from Bacillus Subtilis LB5 Cultivated Broth on Conidial Germination of Colletotrichum Gloeosporioides

Bacillus subtilis strain LB5 produced lipopeptide antibiotic iturin A-2 in liquid medium. Crude extract from cell-free supernatant of B. subtilis cultivated broth extracted with n-butanol showed antifungal activity to conidial germination of Colletotrichum gloeosporioides. The germination of conidia was completely inhibited by crude extract. The ultrastructure of conidia after treated with crude extract was found an accumulation of vesiclelike material between cell wall and plasma membrane while this accumulation was not observed in untreated and germinated conidia. Besides, the cell wall was not affected by crude extract.

In Vitro Antibacterial and Antifungal Effects of a 30 kDa D-Galactoside-Specific Lectin from the Demosponge, Halichondria okadai

The present study has been taken to explore the screening of in vitro antimicrobial activities of D-galactose-binding sponge lectin (HOL-30). HOL-30 was purified from the marine demosponge Halichondria okadai by affinity chromatography. The molecular mass of the lectin was determined to be 30 kDa with a single polypeptide by SDS-PAGE under non-reducing and reducing conditions. HOL-30 agglutinated trypsinized and glutaraldehydefixed rabbit and human erythrocytes with preference for type O erythrocytes. The lectin was subjected to evaluation for inhibition of microbial growth by the disc diffusion method against eleven human pathogenic gram-positive and gram-negative bacteria. The lectin exhibited strong antibacterial activity against gram-positive bacteria, such as Bacillus megaterium and Bacillus subtilis. However, it did not affect against gram-negative bacteria such as Salmonella typhi and Escherichia coli. The largest zone of inhibition was recorded of Bacillus megaterium (12 in diameter) and Bacillus subtilis (10 mm in diameter) at a concentration of the lectin (250 μg/disc). On the other hand, the antifungal activity of the lectin was investigated against six phytopathogenic fungi based on food poisoning technique. The lectin has shown maximum inhibition (22.83%) of mycelial growth of Botrydiplodia theobromae at a concentration of 100 μg/mL media. These findings indicate that the lectin may be of importance to clinical microbiology and have therapeutic applications.