Antimicrobial Activity Of Compounds Research Articles

New Route to the Synthesis of Novel Pyrazolo[1,5-a]pyrimidines and Evaluation of their Antimicrobial Activity as RNA Polymerase Inhibitors.

The current study aimed to synthesize novel pyrazolo[1,5-a]pyrimidines based on 5- aminopyrazoles 3, evaluate their antimicrobial activity, and study the minimum inhibitory concentration (MIC) for the most active compounds. In addition, molecular docking studies and RNA polymerase inhibitory activity were determined. Starting with our previously reported 5-aminopyrazoles 3, a number of novel pyrazolo[1,5- a]pyrimidines were synthesized. Due to the similarity of pyrazolopyrimidine derivatives with the purine systems, pyrazolopyrimidines are important in many different biological applications, most notably as anti-tumor, antibacterial, and hepatitis C virus inhibitors. The pharmaceutical applications of the pyrazolopyrimidine derivatives were explained in several approved drugs like Indiplon, Zaloplan, and Ocinaplon. To prepare a novel antimicrobial agent, namely pyrazolo[1,5-a]pyrimidine, reveal their structures using different spectral data, the minimum inhibitory concentration (MIC) for the most active compounds was evaluated, and both the molecular docking and the RNA polymerase inhibitory activity were determined. A number of different pyrazolopyrimidines namely 2-(phenylamino)-6,11-dihydrobenzo[g]pyrazolo [1,5-a]quinazoline-3-carboxamides (5a-c), (E)-5,7-dimethyl-2-(phenylamino)-6-(phenyldiazenyl)pyrazolo-[1,5- a]pyrimidine-3-carboxamides (7a-c), 7-amino-2-(phenylamino) pyrazolo[1,5-a]pyrimidine-3-carboxamides (11af), 7-amino-2-(phenylamino)-5-(2-thienyl)pyrazolo[1,5-a]pyrimidine-3-carboxamides (14-f) and ethyl 7-amino-3- carbamoyl-2-(phenylamino)-5-(4-pyridyl)pyrazolo[1,5-a]pyrimidine-6-carboxylate derivatives (14g-i) were synthesized through the reaction of 5-aminopyrazoles 3 with a variety of chemical reagents. On the other hand, the evaluation of the antimicrobial activity for all the prepared compounds was screened through different strains as Gram-positive bacteria, such as staphylococcus aureus and Streptococcus mutans, and Gram-negative bacteria, such as Escherichia coli, Pseudomonas aeruginosa, and klebsiella. The antifungal activity was determined by Candids Albicans fungal strain, and the MIC of the most active compounds was measured. The molecular docking was recorded, and the RNA polymerase inhibitory activity was estimated for the high docking score compounds. Compounds 5a, 5b, 5c, 7a, 7b, 7c, 11d, 14b, and 14h were the most active compounds against some of the bacterial and fungal tested strains. MIC was determined for the most active tested compounds. As an antimicrobial agent, compound 7b was the most potent, with a high docking score and RNA polymerase inhibitory activity (IC50= 0.213 μg/ml) compared to Rifampicin (IC50= 0.244 μg/ml). The reactivity of the latter compound was attributed to the presence of 4-Br-C6H4 moiety. The results demonstrated that docking studies on the most active compounds in the RNA polymerase active site were consistent with in vitro assays. The resultant novel bioactive pyrazolo[1,5-a]pyrimidine derivatives were synthesized based on 5- aminopyrazole derivatives 3. The current study evaluated the antimicrobial activity for all the prepared compounds, followed by the determination of the MIC for the most potent active compounds. The molecular docking study was performed, and it was appropriate with the in vitro activity. The RNA polymerase inhibitory activity was assessed for the most active antimicrobial compounds with a high docking score (7b, 7c, 14a, 14b, 14e, 14i). Compound 7b was the most potent compound inhibiting RNA polymerase enzyme compared to the reference drug Rifampicin. Other: The novel prepared heterocyclic systems are extremely important in a variety of domains, especially biological and pharmacological ones.

Antimicrobial compounds and Antimicrobial Activity of Extracts of Thespesia garckeana F. Hoffm. on Candida albicans, Staphylococcus aureus and Escherichia coli

Herbal medicines form a significant role in African ethnomedicine. Thespesia garckeana F. Hoffm. is an important herbal medicinal plant used to treat or manage human diseases and ailments. However, its antimicrobial compounds and activity analysis has not been evaluated. This study aimed at evaluating the phytochemical and antimicrobial activities of compounds in Thespesia garckeana leaves and bark extracts on growth of C. albicans, S. aureus and E. coli. Plant materials were collected from Mwingi, Kenya. Crude plant extraction was done using soxhlet method with methanol and water solvents. Thin layer chromatography was used to purify the extracts and Phytochemical screening was done using standard methods. Thin layer chromatography plate surface was coated with silica gel, and n-Hexane and Ethyl acetate used as solvent systems in the ratio 2:3 and 3:7 respectively. Antimicrobial activity was performed on test microorganisms using plant extracts; 0 (distilled water), 90, 180, 270 and 360 mg/ml of the extract using paper disc method. Diameter of inhibition zones was dmeasured. The data on growth inhibition was subjected to analysis of variance (ANOVA). The extracts of Thespesia garckean revealed the presence of Tannins, Saponins, Cardiac glycosides, and Alkaloids. TLC using n-Hexane and Ethyl acetate ratio of 2:3 methanol leaves extracts produced 9 spots and The bark extracts produced 4 spots. Leaf methanol extracts using n-Hexane and Ethyl acetate in the ratio of 3:7 produced 8 spots and Bark methanol extracts produced 2 spots. Increase in extracts concentration of the leaves and bark of Thespesia garckeana, significantly inhibited the growth of Candida albicans, Staphylococcus aureus and E. coli. Methanol leaf and bark extracts had more inhibitory activity compared to the water extracts. The results from this study confirm the use of Thespesia garckeana in herbal medicine by traditional herbalists.

Evaluation of Antimicrobial Activity of a Pyrimidine Derivative Against <i>Staphylococcus Aureus</i>

The aim of this study was to evaluate the in vitro and in vivo antimicrobial activity of a new pyrimidine derivative against Staphylococcus aureus . The assessment of the antimicrobial activity of pyrimidine compound 3 3-(2-Phenyl-2- oxoethyl)quinazoline-4(3H)-one was performed in vitro using a test culture of the S. aureus strain isolated from patients’ sputum by serial dilutions in meat-peptone broth, followed by the formation of sequences with a concentration of pyrimidine derivative 128 mcg/ml; 64 mcg/ml; 32 mcg/ml; 16 mcg/ml; 8 mcg/ml; 4 mcg/ml; 2 mcg/ml; 1 mcg/ml. During the study, the minimum inhibitory concentration of 3-(2-Phenyl-2-oxoethyl)quinazoline-4(3H)-one against S. aureus was determined. The antimicrobial activity of the compound under examination was studied in vivo using a model of generalized staphylococcal infection. The infectious process was modeled via intraperitoneal administration of S. aureus at a dose of ×10 8 microbial bodies to 7-week-old mice. All laboratory mice were divided into 4 groups: control I — animals receiving an equivalent volume of water for injection; control II — animals infected with S. aureus ; comparison group — a group of animals treated with the comparison drug ceftriaxone at a dose of 50 mg/kg; experimental group – animals treated with the studied compound at a dose of 1/10 of the molecular weight of 26 mg/ kg, for 7 days starting from the day of infection. The survival rate of mice during the experiment was evaluated. At the end of the experiment, blood, spleen, liver, and lung contamination indices were calculated. The study established the antibacterial activity of the pyrimidine derivative 3-(2-Phenyl-2-oxoethyl)quinazoline-4(3H)-one under in vitro conditions against S. aureus : the compound showed bacteriostatic activity in the dilution of 16 mcg/kg and bactericidal activity in dilution of 64 mcg/kg. The results of the assessment of antimicrobial activity in vivo showed that the studied compound contributes to the survival of laboratory animals, as well as to a decrease in the index of bacterial contamination of internal organs and blood in conditions of generalized staphylococcal infection, which indicates the ability to form antimicrobial immunity.

Polymeric Packaging Applications for Seafood Products: Packaging-Deterioration Relevance, Technology and Trends.

Seafood is a highly economical product worldwide. Primary modes of deterioration include autolysis, oxidation of protein and lipids, formation of biogenic amines and melanosis, and microbial deterioration. These post-harvest losses can be properly handled if the appropriate packaging technology has been applied. Therefore, it is necessary for packaging deterioration relevance to be clearly understood. This review demonstrates recent polymeric packaging technology for seafood products. Relationship between packaging and quality deterioration, including microbial growth and chemical and biochemical reactions, are discussed. Recent technology and trends in the development of seafood packaging are demonstrated by recent research articles and patents. Development of functional polymers for active packaging is the largest area for seafood applications. Intelligent packaging, modified atmosphere packaging, thermal insulator cartons, as well as the method of removing a fishy aroma have been widely developed and patented to solve the specific and comprehensive quality issues in seafood products. Many active antioxidant and antimicrobial compounds have been found and successfully incorporated with polymers to preserve the quality and monitor the fish freshness. A thermal insulator has also been developed for seafood packaging to preserve its freshness and avoid deterioration by microbial growth and enzymatic activity. Moreover, the enhanced biodegradable tray is also innovative as a single or bulk fish container for marketing and distribution. Accordingly, this review shows emerging polymeric packaging technology for seafood products and the relevance between packaging and seafood qualities.

Antibacterial Activity and GC–MS Based Metabolite Profiles of Indonesian Marine Bacillus

Investigating Indonesian marine bacteria producing active compounds is key to finding a cultivable source of marine drugs. Screening the potential strain as well as profiling the active compounds are important steps to identifying the targeted substances. Methods used in this study were isolated some Bacillus strains from several marine environments in Indonesia, evaluated the antibacterial activity, and characterized the secondary metabolite using GC-MS spectroscopy. Several active antimicrobial compounds derived from marine microorganisms were identified using GC-MS such as pyrrolo [1,2-a] pyrazine-1,4-dione, octatriacontyl pentafluoropropionate. We found that some marine bacillus showed antimicrobial activity, such as B. flexus, B. tequilensis, B subtilis, and Bacillus sp. Profiling of metabolites on GC-MS showed the presence of several bioactive compounds in the ethyl acetate extract, which were identified to be nitrogen compounds such as pyrrolo[1,2-a]pyrazine-1,4-dione, phthalates compounds (butyl isohexyl ester and 1,2 benzendicarboxilate bis (2-etilhexyl) ester), and dibutyl phthalate. Some phenolic compounds also were found, such as tris (2,4-di-ter-butilfenil) fosfat, phenol, 2,4-bis (1,1-dimethyl ethyl), and phenol 3,5-bis (1,1-dimethyl ethyl). Finally, fatty acid derivatives such as n-hexadecanoic acid, cis-vaccenic acid, 7-hexadecene, farnesol isomer A, and stigmastan-3,5-diene were also identified in several marine bacillus.

Uji Toksisitas Ekstrak Daun Sirih (Piper betle) Terhadap Benih Ikan Kakap Putih (Lates calcarifer)

White snapper (Lates calcarifer) is a type of seawater fish that is in great demand by the public. This study aims to determine the 48-hour LC50 value and the effect of using betel leaf extract on the health status of white snapper. This research was conducted in July 2020 which took place at the Sekotong Coastal Aquaculture Development Center (BPBPP), West Lombok Regency, West Nusa Tenggara. This research was conducted using experimental methods. This study used 5 treatments and three replications, to obtain 15 experimental units with doses of 0 ppm, 80 ppm, 90 ppm, 100 ppm and 200 ppm. Data analysis was performed using a linear regression test, namely probit analysis by testing the mortality of tested animals and calculated through statistical data using Microsoft Excel. The higher the betel leaf extract concentration, the higher the number of white snapper seed deaths. This happens because the betel leaf extract contains active antimicrobial compounds, but at high concentrations, it can poison the white snapper seeds. For further research, it is recommended to test the toxicity of betel leaf extract on the mortality of white snapper with variations in water quality.

Biological Activities of Seven Medicinal Plants Used in Chiapas, Mexico.

Seven medicinal plants from Chiapas, Mexico, used by Native Americans were analyzed, aiming to improve the understanding of their medicinal properties through the evaluation of various biological activities, i.e., bactericidal, antioxidant, α-glucosidase inhibition, and toxicity, to provide a scientific basis for the management of infectious and hyperglycemic diseases in the Mexican southeast. Plant extracts were obtained from Cordia dodecandra, Gaultheria odorata, Heliotropium angiospermum, Justicia spicigera, Leucaena collinsii spp. collinsii, Tagetes nelsonii, and Talisia oliviformis through maceration techniques using methanol and chloroform (1:1). Minimum Inhibitory Concentration (MIC) was employed to determine the antibacterial activity against Staphylococcus aureus, Enterobacter faecalis, Escherichia coli, Enterobacter aerogenes, Enterobacter cloacae, Klebsiella pneumoniae, and Pseudomonas aeuroginosa. The antiradical/antioxidant activity was determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays and antihemolytic activity using the 2,2’-Azobis(2-amidinopropane) dihydrochloride radical (APPH). The anti-α-glucosidase activity was evaluated in vitro through the chromogenic PNPG assay. The toxicity was assessed using the brine shrimp lethality assay. The highest antimicrobial activity was displayed by T. nelsonii, mainly against E. faecalis and P. aeuroginosa. The extracts of L. collinsii, J. spicigera, and T. nelsonii possess antioxidant properties with EC50 < 50 μg/mL. J. spicigera and T. nelsonii extracts showed the highest antihemolytic activity with IC50 < 14 μg/mL. T. nelsonii exhibited a remarkable inhibitor effect on the α-glucosidase enzyme and the greatest toxic effect on Artemia salina with IC50 = 193 ± 20 μg/mL and LD50 = 14 ± 1 μg/mL, respectively. According to our results, G. odorata, J. spicigera, T. nelsonii, and T. oliviformis extracts contained active antimicrobial compounds. At the same time, T. nelsonii stands to be a possible source of effective antineoplastic and antihyperglycemic compounds.

Antioxidant, Antimicrobial, and Molecular Docking Studies of Novel Chalcones and Schiff Bases Bearing 1, 4-naphthoquinone Moiety

Background: The 1,4-naphthoquinone ring has attracted prominent interest in the field of medicinal chemistry due to its potent pharmacological activities such as antioxidant, antibacterial, antifungal, and anticancer. Objective: Herein, a series of new Schiff bases (4-6) and chalcones (8a-c &amp; 9a-d) bearing 1,4- naphthoquinone moiety were synthesized in good yields and were subjected to in-vitro antimicrobial, antioxidant, and molecular docking testing. Methods: A facile protocol has been described in this study for the synthesis of new derivatives (4-7, 8ac, and 9a-d) bearing 1,4-naphthoquinone moiety. The chemical structures of all the synthesized compounds were identified by 1H-NMR, 13C-NMR, MS, and elemental analyses. Moreover, these derivatives were assessed for their in-vitro antimicrobial activity against gram-positive, gram-negative bacteria, and fungal strains. Further studies were conducted to test their antioxidant activity using DPPH (2,2-diphenyl- 1-picrylhydrazyl) scavenging assay. Molecular docking studies were realized to identify the most likely interactions of the novel compounds within the protein receptor. Results: The antimicrobial results showed that most of the compounds displayed good efficacy against both bacterial and fungal strains. The antioxidant study revealed that compounds 9d, 9a, 9b, 8c, and 6 exhibited the highest radical scavenging activity. Docking studies of the most active antimicrobial compounds within GLN- 6-P, recorded good scores with several binding interactions with the active sites. Conclusion: Based on the obtained results, it was found that compounds 8b, 9b, and 9c displayed the highest activity against both bacterial and fungal strains. The obtained findings from the DPPH radical scavenging method revealed that compounds 9d and 9a exhibited the strongest scavenging potential. The molecular docking studies proved that the most active antimicrobial compounds 8b, 9b and 9c displayed the highest energy binding scores within the glucosamine-6-phosphate synthase (GlcN-6-P) active site.

Antimicrobial Evaluation, Molecular Docking and ADME Properties of Indole Amide Derivatives

Background: Besides the viral infections, bacterial infections can cause serious and lifethreatening complications and drug resistance is an important problem to fight bacterial infections. Therefore, it is important to discover novel antimicrobial agents to fight such infections. Objective: Several indole containing antimicrobial drug development studies have been reported in literature that provided strong evidence for good antimicrobial activities against a variety of microorganisms. Taken into consideration from these findings, antimicrobial properties of previously synthesized 16 indole amide derivatives were evaluated by in vitro tests against 14 different microorganisms, and also molecular docking and in silico prediction studies were used to identify structure-activity relationship of compounds. Methods: Antimicrobial activity of compounds was determined by disc diffusion and tube dilution methods. Molecular docking of compounds was studied to determine the relationship between the structure of compounds with DNA gyrase interactions of microorganisms by using the version of Autodock vina 4.2.6. Mol inspiration and Swiss ADME prediction online software programs were also used to identify drug-like properties of compounds. Results: The results showed that some compounds exhibited quite pronounced antibacterial and antifungal activities compared to reference drugs. These results were also supported by molecular docking studies and in silico ADME calculations presented that all tested compounds obey Lipinski’s Rule of Five and are metabolized by CYP450 enzymes. Conclusion: It can be concluded that these results can be taken as a reference in the development of new indole-based antimicrobial agents.

Endophytic Fungus from Opuntia ficus-indica: A Source of Potential Bioactive Antimicrobial Compounds against Multidrug-Resistant Bacteria.

Endophytic Aspergillus species represent an inexhaustible source for many medicinally important secondary metabolites. The current study isolated the endophytic Aspergillus niger (OL519514) fungus from Opuntia ficus-indica fruit peels. The antibacterial activities were reported for both Aspergillus species and Opuntia ficus-indica fruit peel extract. Extraction of the endophytic fungal metabolites using ethyl acetate and fractionation was performed, yielding dihydroauroglaucin (C1), isotetrahydroauroglaucin (C2), and cristatumin B (C3). Resistant bacterial strains were used to investigate the efficiency of the total fungal ethyl acetate extract (FEA) and the isolated compounds. FEA showed promising wide spectrum activity. (C3) showed excellent activity against selected Gram-negative resistant bacteria; However, (C2) exhibited tremendous activity against the tested Gram-positive resistant strains; conversely, (C1) possessed the lowest antibacterial activity compared to the two other compounds. An in silico virtual molecular docking demonstrated that cristatumin B was the most active antimicrobial compound against the selected protein targets. In conclusion, the active metabolites newly isolated from the endophytic fungus Aspergillus niger (OL519514) and present in plants’ waste can be a promising antimicrobial agent against multidrug-resistant bacteria.

Antimicrobial Effects and Active Compounds of the Root of Aucklandia Lappa Decne (Radix Aucklandiae).

The development of new biological fungicides using plant metabolites has become an important direction for pesticide development, and previous studies found that Radix Aucklandiae had a certain inhibitory effect on plant pathogens. In this study, we systematically studied the antimicrobial activity of extracts of Radix Aucklandiae, and the active compounds were isolated, purified and structurally identified. Ethanol extracts of Radix Aucklandiae had different inhibitory effects on seven common plant-pathogenic fungi, with EC50 (concentration for 50% of maximal effect) values ranging from 114.18 mg/L to 414.08 mg/L. The extract at concentration of 1,000 mg/L had a significant control effect on strawberry grey mould and wheat powdery mildew of more than 90%. Three active compounds were isolated and purified from the extract, which were identified as alantolactone, dehydrocostus lactone and costunolide. All three compounds showed significant inhibitory effects on Botrytis cinerea, and the MIC (minimal inhibitory concentration) values were 15.63 mg/L, 3.91 mg/L and 15.63 mg/L. Dehydrocostus lactone also showed obvious inhibitory effect on Fusarium graminearum with an MIC value of 62.25 mg/L. The extract of Radix Aucklandiae has high antimicrobial activity against some common plant-pathogenic fungi, and the work lays a foundation for the development of extracts of Radix Aucklandiae as botanical fungicides.

An Annotated Inventory of Tanzanian Medicinal Plants Traditionally Used for the Treatment of Respiratory Bacterial Infections.

This review comprehensively covers and analyzes scientific information on plants used in Tanzanian traditional medicine against respiratory diseases. It covers ethnobotanical and ethnopharmacological information extracted from SciFinder, Google Scholar, and Reaxys as well as the literature collected at the Institute of Traditional Medicine in Dar-es-Salaam. Crude extracts and fractions of 133 plant species have literature reports on antimicrobial bioassays. Of these, 16 plant species had a minimum inhibitory activity of MIC ≤ 50 µg/mL. Structurally diverse compounds were reported for 49 plant species, of which 7 had constituents with MIC ≤ 5 µg/mL against various bacteria: Bryophyllum pinnatum (Lam.) Oken, Warburgia ugandensis Sprague, Diospyros mespiliformis Hochst. ex DC., Cassia abbreviata Oliv., Entada abyssinica A. Rich., Strychnos spinosa Lam., and Milicia excelsa (Welw.) C.C. Berg. The low number of antimicrobial active extracts and compounds suggests that antibacterial and antimycobacterial drug discovery needs to have a fresh look at ethnobotanical information, diverting from too reductionist an approach and better taking into account that the descriptions of symptoms and concepts of underlying diseases are different in traditional African and modern Western medicine. Nevertheless, some structurally diverse compounds found in anti-infective plants are highlighted in this review as worthy of detailed study and chemical modification.

Effects of Grape Pomace Polyphenols and In Vitro Gastrointestinal Digestion on Antimicrobial Activity: Recovery of Bioactive Compounds.

Grape pomace (GP), a major byproduct obtained from the winemaking process, is characterized by a high amount of phenolic compounds and secondary plant metabolites, with potential beneficial effects on human health. Therefore, GP is a source of bioactive compounds with antioxidant, antimicrobial, and anti-inflammatory activity. As people are paying more attention to sustainability, in this work, we evaluate two different extractions (aqueous and hydroalcoholic) of GP bioactive compounds. In vitro simulated gastrointestinal digestion of the GP extracts was performed to improve the bioavailability and bioaccessibility of polyphenols. The antioxidant activity (ABTS and DPPH assays) and the phenolic characterization of the extracts by UHPLC-DAD were evaluated. The antimicrobial effects of GP antioxidants in combination with a probiotic (Lactiplantibacillus plantarum) on the growth of pathogenic microorganisms (Escherichia coli, Bacillus megaterium, and Listeria monocytogenes) were evaluated. As a result, an increase of antioxidant activity of aqueous GP extracts during the gastrointestinal digestion, and a contextual decrease of hydroalcoholic extracts, were detected. The main compounds assessed by UHPLC-DAD were anthocyanins, phenolic acids, flavonoids, and stilbenes. Despite lower antioxidant activity, due to the presence of antimicrobial active compounds, the aqueous extracts inhibited the growth of pathogens.

Sesquiterpene and Sorbicillinoid Glycosides from the Endophytic Fungus Trichoderma longibrachiatum EN-586 Derived from the Marine Red Alga Laurencia obtusa.

An unusual sesquiterpene glycoside trichoacorside A (1) and two novel sorbicillinoid glycosides sorbicillisides A (2) and B (3), together with a known compound sorbicillin (4), were isolated and identified from the culture extract of an endophytic fungus Trichoderma longibrachiatum EN-586, obtained from the marine red alga Laurencia obtusa. Trichoacorside A (1) is the first representative of a glucosamine-coupled acorane-type sesquiterpenoid. Their structures were elucidated based on detailed interpretation of NMR and mass spectroscopic data. The absolute configurations were determined by X-ray crystallographic analysis, chemical derivatization, and DP4+ probability analysis. The antimicrobial activities of compounds 1–4 against several human, aquatic, and plant pathogens were evaluated.

Effect of Different Extraction Methods and Geographical Origins on the Total Phenolic Yield, Composition, and Antimicrobial Activity of Sugarcane Bagasse Extracts.

Several parameters, including particle size, solvent, temperature, and extraction method, affect phenolic compounds' extraction yield from a plant matrix. Considering the wide availability of sugarcane bagasse (SCB), this study analyzed the effect of different extraction methods and geographical origins on the yield, quality, and antimicrobial activity of phenolic compounds from SCB extracts. Samples from three geographical locations (Veracruz, Mexico; Santa Rosa, Texas, USA; and St. Mary, Louisiana, USA) were analyzed. Extraction was performed using an orbital shaker or ultrasonic bath at various times at a fixed temperature of 50°C, with 90% ethanol or methanol. The highest yield (5.91 mg GAE) was obtained using an orbital shaker for 24 h with 90% methanol as the solvent. HPLC-MS identified desferrioxamine b, baicalein, madecassic acid, and podototarin at different concentrations in all three SCB samples. The antimicrobial activity of these compounds was tested against Escherichia coli K12, Bacillus cereus, Enterobacter aerogenes, Streptococcus aureus, and Enterobacter cloacae. The antimicrobial activity was also tested against modifications of the Saccharomyces cerevisiae: the MutL Homolog 1 (MLH1), Slow Growth Suppressor (SGS1), O-6-MethylGuanine-DNA methyltransferase (MGT1), and RADiation sensitive (RAD14), carrying mutations related to different cancer types. In addition, the results were compared with the effect of ampicillin and kanamycin. The SCB extracts showed up to 90% growth inhibition against B. cereus at 200–800 μg/mL and 50% growth inhibition against S. aureus at 800 μg/mL. The inhibitory effect against modified yeast SGS1, RAD14, and MLH1 was 50–80% at 800 μg/mL. The percentage of inhibition and the phenolic compound contents differed depending on the origin of the SCB sample. These findings are promising for using this industrial byproduct to obtain compounds for nutraceutical, food additive, or medical uses.

Study of Phenolic Compounds of Prunus Domestica Presscake and Antimicrobial Activity of Its Extract

Prunus domestica - is one of the main fruit crops in Ukraine with a production of about 200 tons per year. In the world over then 2000 varieties of this plant are grown. In Ukraine, the following varieties of plums are zoned: Anna Shpet, Renklod Altana, Ugorka Stanley, Ugorka Italian, Ugorka Azhanska, and others. This plant is the valuable source of polysaccharides and phenolic compounds. That is why plum fruits are a part of many dietary supplements with laxative and anti-inflammatory activity in treating chronic constipation. In our previous research, we studied the chemical composition of alcohol extracts and polysaccharide complex of plum fruits. Following types of pharmacological activities: diuretic, membrane stabilizing, anticoagulant laxative, hepatoprotective, were confirmed in the analysed substances. In the article, we present the results of a study of the chemical composition of the plum presscake that remained after the plum juice was obtained. The composition of phenolic compounds was analyzed by using TLC, SF and HPLC methods. Antimicrobial activity of the alcohol extract of plum presscake was investigated by agar diffusion method. The results obtained indicate the possibility of complex processing of raw materials and obtaining new antimicrobial drugs from the presscake of plum juice production.

TABLET ANTIMIKROBA UNTUK APLIKASI KEMASAN AKTIF

Antimicrobial active packaging is designed to extend the shelf life of packaged products by adding antimicrobial agents to the packaging system. Trend of green consumerism has led to an increasing demand for the use of natural antimicrobial agents for food packaging applications. The natural antimicrobial agents that are the focus of current research are essential oils, however, the application of essential oils directly to packaging materials can affect mechanical characteristics such as a decrease in the tensile strength of the packaging materials. One of the innovations to solve this weakness is the application of an antimicrobial agent with a carrier material in the form of sachets, pads and tablets. The principle of the antimicrobial active packaging is the adsorption of active compounds on the carrier material and allows the slow release of active antimicrobial compounds in the packaging system. Furthermore, challenges in the food sector related to packaging waste have prompted research on biodegradable materials, such as the use of starch and cellulose as carrier materials. This paper examines the development of antimicrobial packaging with essential oil active agents using several types of carrier materials, how to produce these packages with several types of materials, and the advantages and disadvantages of selecting the materials used.

Synthesis and characterization of Cu(II) complexes of proton transfer salts derived from piperazine derivatives and 5-sulfosalicylic acid

In this study, proton transfer salts (H2Etpip)(Hssa), (H2HOEtpip)(Hssa) and (HAcpip)(H2ssa), have been obtained by reactions between 1-ethylpiperazine (Etpip), 1-(2-hydroxyethyl)piperazine (HOEtpip) and 1‑acetylpiperazine (Acpip) and 5-sulfosalicylic acid (H3ssa). Also, Cu(II) complexes of proton transfer salts (H2Etpip)[Cu(Hssa)2]·5H2O, (H2HOEtpip)[Cu(Hssa)2]·5H2O and (H2Acpip)[Cu(Hssa)2]·5H2O) have been synthesized. The structures of proton transfer salts have been proposed by using FT-IR, 1H and 13C NMR spectroscopy, and elemental analysis. The structures of the amorphous metal complexes have been proposed by atomic absorption spectrometry, FT-IR, magnetic susceptibility, molar conductivity techniques, and elemental analysis. Antimicrobial activities of compounds have been tested against Staphylococcus aureus (ATCC 29213) (Gram-positive), Escherichia coli (ATCC 25922) (Gram-negative), Candida krusei (ATCC 6258) (yeast), and Candida parapsilosis (ATCC 22019) (yeast) microorganisms. For S. aureus, the minimum inhibitory concentration (MIC) values of the synthesized salts were between 31.25 and 62.50 µg/ml, and 15.60 µg/ml for complexes. The MIC values of salts and complexes for E. coli were in the range 125.00–500.00 µg/ml and 31.25–62.50 µg/ml, respectively. The MIC values of the salts for C. krusei were 62.50 µg/ml, and for the complexes in the range 15.60–31.25 µg/ml. For C. parapsilosis, these values were 31.25 µg/ml for all salts and in the range 15.60–62.50 µg/ml for complexes.

Photophysicochemical and Biological Properties of New Phthalocyanines Bearing 4-(trifluoromethoxy)phenoxy and 2-(4-methylthiazol-5-yl)ethoxy Groups on Peripheral Positions.

As thiazoles and fluorinated groups are well known as active species of hybrid pharmaceutical agents, this study aimed to evaluate the synergic effect of these groups on the biological features of phthalocyanines for the first time in the hope of discovering efficient pharmaceutical agents. Therefore, a new phthalonitrile derivative namely 4-(2-(4-methylthiazol-5-yl)ethoxy)-5-(4-(trifluoromethoxy)phenoxy)phthalonitrile (1) and its metal-free (2)/metal phthalocyanines (3-5) were prepared and characterized using various spectroscopic techniques. Solubility of new phthalocyanines (2-5) was examined in a series of polar and nonpolar solvents. Additionally, sono/photochemical methods were applied to examine the photophysical and sono/photochemical properties of new zinc phthalocyanine to measure its potential as a probable material for sono/photodynamic therapies. The antioxidant activities of compounds (1-5) were evaluated using the DPPH scavenging activity method and the highest radical scavenging activity was obtained 92.13% (200 mg L-1 ) for manganese phthalocyanine. All the phthalocyanines demonstrated high DNA nuclease activity, as well. The antimicrobial activities of compounds (1-5) were investigated using disk diffusion and microdilution methods. The phthalocyanines exhibited effective microbial cell inhibition activity against Escherichia coli (E.coli). Antimicrobial photodynamic therapy activity was investigated against E.coli by LED irradiation. Compounds (2-5) acted as photosynthesizers. Also, they displayed significant biofilm inhibition activity against Staphylococcus aureus (S. aureus) and Pseudomonas aeruginosa (P. aeruginosa).

The Antidiabetic and Anti-microbial Activity Analyses in The Extract of Methanol, Ethyl Acetate, and Hexane from Flesh of Matoa (Pometia pinnata J. R. Forst. &amp; G. Forst)

The current research was designed to examine the antidiabetic and anti-microbial activities in the extracts of methanol, ethyl acetate and hexane from Flesh of Matoa (Pometia pinnata J. R. Forst. &amp; G. Forst) to find out the best solvent to produce antidiabetic and anti-microbial active compounds. In the phytochemical screening, hexane extracted alkaloids and terpenoids, while ethyl acetate extracted saponin and methanol extracted tannin, phenol and terpenoids. In the antidiabetic activity by a-glucosidase inhibition methods, ethyl acetate showed the highest percentage of inhibition and the smallest value of IC50, followed by hexane and methanol compared to the Quercetin as the control group. The maximum percentage inhibition was 36.74 ± 0.07 for 100 µg/mL of concentration. The minimum value of IC50 was observed at 159.74 ± 0.65 µg/ml compared to the control group 6.04 ± 0.14 µg/ml. The smaller the IC50 value, the stronger the antidiabetic activity. Anti-microbial inhibition activities assessed using anti-microbial diffusion test method. The hexane and ethyl acetate extracts provide an inhibition of fungi and bacteria compared to Ketoconazole and Amoxicillin as the standard. The maximum fungi inhibition zone was observed at 4 mm for A. flavus and 9 mm for A. niger by Hexane extracts compared to the standard 14 and 24 mm. The maximum bacteria inhibition zone was observed at 7 mm for B. cereus by both of hexane and ethyl acetate extracts compared to the standard 5 mm. Compared to the anti-microbe inhibitory power categories, hexane and ethyl acetate was on the range of weak and moderate. The methanol extract could not inhibit all types of microbe. This study concluded that various extract of flesh of Matoa showed antidiabetic and anti-microbial activities at different value with varying potencies. The ethyl acetate extract was found to be more potent among all, followed by hexane and methanol.&#x0D; HIGHLIGHTS&#x0D; &#x0D; Phytochemical screening of Flesh of Matoa (Pometia pinnata R. Forst. &amp; G. Forst) produced alkaloids, terpenoids, saponin, tannin, phenol and terpenoids&#x0D; In the antidiabetic activity by a-glucosidase inhibition methods, ethyl acetate showed the highest percentage of inhibition and the smallest value of IC50, followed by hexane and methanol&#x0D; The hexane and ethyl acetate extracts provide an inhibition of fungi and bacteria compared to Ketoconazole and Amoxicillin as the standard&#x0D; &#x0D; GRAPHICAL ABSTRACT