Synthesis of substituted N'-(3-oxo-1,3-diphenylpropyl)isonicotinohydrazide and evaluation of their antimicrobial activities

ABSTRACT: Medicinal Plants have been used throughout the world by human beings as a drug and remedies for various diseases since time immemorial. A study was planned to count into the antimicrobial activity and phytochemical screening of Euphorbia helioscopia. The plants were gathered and tested against some standard strains and some human pathogenic microorganisms i.e Escherichia coli, Bacillus Subtilis, Staphylococcus aureus, Klebsiella pneumoniae, Salmonella typhi, Pseudomonas aeruginosa and three fungal strain Trichoderma, R hizopus nigricans, Aspergillus niger. The concentrations of extracting samples (500 and 1,000 mg mL-1) were used against pathogens. Ciprofloxacin was used as positive control in case of bacterial strains and Colfrimazol was used against the fungal strain while dimethyl sulfoxide as negative control. The outcomes indicated that the positive wells potency of Water extract had a 36 mm diameter of zone of inhibition against Escherichia coli and ethanol extract at 1,000 mg mL-1 had maximum (34 mm) zone of inhibition against Bacillus subtilus (36 mm) zone of inhibition against Klebsiella pneumonia and 33 mm of zone of inhibition against Trichoderma harzianum. Likewise, water extract at a concentration of 1,000 mg mL-1 resulted highest value of zone of inhibition (36 mm) against Staphylococcus aureus, a zone of inhibition ( mm) against Salmonella typhi, 36 mm zone of inhibition against Pseudomonas aeruginosa, (32 mm) zone of inhibition against Rhizopus nigricans, a 34 mm zone of inhibition against Acremonium and (34 mm) zone of inhibition against Aspergillus niger. The most susceptible bacteria were K. pneumonia and Bacillus subtilis, while E. coli was the most resistant bacteria and showed zone of inhibition. The ethanolic extract had tannins, lipid, total proteins, carbohydrates, flavonoids, Alkaloid and polyphenolics.

Background: Musa sapientum is a useful medicinal plant from the Musaceae family. Copper nanoparticles with a high surface to volume ratio can also be used as antifungal and antibacterial agents. The aim of the study is to access the antimicrobial activity of musa sapientum mediated copper nanoparticle against oral pathogens
 Materials and Methods: Plant extract was prepared by 1g of musa, was weighed aseptically and then dissolved in 100 ml of distilled water. Then the solution is boiled for about 5 minutes at a temperature of about 60-80 degree Celsius and then allowed to cool down followed by filtration of extract. The copper solution was prepared by dissolving 20 millimolar of copper sulphate in 80 ml of distilled water followed by 20 ml of plant extract and then the mixture is placed in the shaker for the synthesis and then allowed to mix for about 1 hour then the first reading was taken using UV spectrum and noted down. Antimicrobial activity was done against the strain of S. aureus, S. mutans, E. faecalis. Muller Hinton agar was utilised for this activity to determine the zone of inhibition different concentrations were loaded in the plates and incubated for 24 hrs 37 degree celsius after the incubation time the zone of inhibition was measured. Antifungal activity of zinc oxide nanoparticles was done against the strain Candida Albicans.
 Results: For the study, descriptive statistics was used. For 100 μL concentration 11 mm zone of inhibition was seen when compared to the standard drug Amoxyrite which had a zone of inhibition of 36mm, which means that the antimicrobial activity was low in case of E. Faecalis. In C. Albicans, at 100μL concentration 14mm zone of inhibition was seen, but the standard fluconazole had only a zone of inhibition of 10mm, which means antimicrobial activity was good in case of C. albicans which showed more zone of inhibition. For S. aureus, at 100μL 13mm zone of inhibition was seen, the standard value showed 28mm zone of inhibition which means there is less zone of inhibition when compared to standard drug. For S. mutans, at 100μL concentration 18mm zone of inhibition was seen and when compared to the standard value which was 23mm which showed poor antimicrobial activity.
 Conclusion: The research concludes that musa sapientum mediated copper nanoparticles showed a moderate antimicrobial activity against the pathogens Streptococcus mutans, Staphylococcus aureus, Enterococcus faecalis and Candida albicans.

In vitro activity of 5-(2,4-dimethylbenzyl) pyrrolidin-2-one extracted from marine Streptomyces VITSVK5 spp. against fungal and bacterial human pathogens

his research investigates the antimicrobial and antioxidant properties of three essential oils (EO): Aegle marmelos, Aristolochia indica, and Piper nigrum roots. The antimicrobial effectiveness of the EOs was demonstrated against four bacteria and a fungus strains. Antimicrobial activity was evaluated by measuring the size of the inhibition zone, as well as determining the minimum inhibitory concentration and minimum bactericidal concentration. Upon analyzing the inhibition zone diameters, we noted an increased effectiveness of A. indica, which displayed the highest values across all microbial species tested. Antifungal activity of essential oil was tested against the selected C. albicans. A. marmelos, A. indica, and P. nigrum essential oils showed 11 mm, 12 mm and 12 mm zone of inhibition against C. albicans. A. indica essential oil showed maximum activity against E. coli (15 mm zone of inhibition) than P. nigrum essential oil (18 mm zone of inhibition), and A. marmelos essential oil (16 mm zone of inhibition). The minimum inhibitory concentration of essential oils were determined against various bacterial pathogens. Essential oil was highly active against Streptococcus sp. and E. coli than K. pneumoniae and S. aureus.

The Pd-precatalyst was found to exhibit high catalytic activity for C-C bond formation in Suzuki-Miyaura crosscoupling reactions of differentheteroaryl (5-bromo-2-bromoacetyl) thiophene,4-(5-bromothiophen-2-yl)-methyl-1,3thiazole,isoquinolinium bromide salt) with either aryl or heteroarylboronic acids.All reactions in this study were conducted in water under thermal heating as well as microwave irradiation conditions.The antimicrobial activities of synthesized compounds were evaluated against eight different strains of microorganisms (four fungal strains, two Gram-positive bacteria and two Gram-negative bacteria) using a cup plate diffusion method.The results showed that, most of the 20 tested compounds exhibited varying degrees of antimicrobial activities.However, 6 compounds recorded high antifungal activity (≤ 20 mm zone of inhibition), 3 were antibacterial (against Gram-positive) and 4 showed high broad-spectrum antibacterial efficacy (against Gram-positive and Gram-negative).These bioactive compounds are recommended for further pharmacological and toxicological investigations for possible formulation as wide spectrum antibacterial and antifungal agents.

Antibiotic resistance and the hazardous nature of synthetic drugs is threatening issue in the health sector. The alternative for this problem is to focus on plants that attribute to various compounds that exhibit therapeutic properties. Therefore, the study aims to evaluate the antimicrobial efficacy of Salacia oblonga leaf and root extracts against tested human pathogens. The S. oblonga extracts showed a significant zone of inhibition against bacteria and fungi. The leaf and root extracts of S. oblonga are prepared using low polar to high polar solvents in the Soxhlet apparatus and tested on the selected bacterial and fungal strains. Agar well diffusion and broth dilution methods evaluate antibacterial activity, antifungal activity, and Minimum Inhibitory Concentration (MIC) of extracts. Among the extracts tested, the ethyl acetate extract of root showed more antimicrobial activity against the tested bacterial and fungal strains. The most susceptible bacterial and fungal species against ethyl acetate extract are Micrococcus luteus, Mycobacterium tuberculosis, Microsporum canis, Trichophyton interdigitale, and Microsporum gypseum. The MIC for bacteria ranged from 13.0 to > 200µg/ml, whereas for fungi, the MIC ranged from 25.9 to > 200µg/ml. Ethyl acetate extract of root with 100µg/ml concentration showed 29.1mm and 28.7mm zone of inhibition against bacterial strains M. luteus and M. tuberculosis, respectively. The ethyl acetate extract of root with a 100µg/ml concentration showed 15.8, 15.2, and 15.6mm zone of inhibition against fungal isolates M. canis, T. interdigitale, and M. gypseum, respectively. The activity of root and leaf extracts increased in a concentration-dependent manner, and further, the compounds isolated from the crude extracts of leaf and root showed antimicrobial activity. Structural elucidation of isolated compounds Lambertic acid and Ferruginol was done using NMR spectroscopy. Reports indicate that Lambertic acid was isolated previously, but the isolation of hydroxy Ferruginol from S. oblonga leaf extract was reported unprecedented.

In this study, methanolic crude extracts and their different fractions i.e. hexane, carbon tetrachloride, dichloromethane and aqueous soluble fractions of the B. daigremontianum(Raym.), C. cordifolia, (Linn.), L. glutinosa(Laur.) and M. minutum(G. Forst.)were subjected for antimicrobial activity. All the fractions were tested against different gram positive and gram negative bacteria and fungi to find out their antimicrobial activity. This study showed that among different fractions of the four important medicinal plants, carbon tetrachloride fraction and crude methanol soluble fraction of leaves' extract of L. glutinosa showed significant activity against gram positive bacteria, gram negative bacteria and fungi at a dose of 400 μg/ disc. Leaves' extract of B. daigremontianum showed mild to moderate antimicrobial activity, especially dichloromethane solvent extract showed significant antimicrobial activity showing 10-13 mm zone of inhibition in diameter, against Shigelladysenteriaethe extract showed highest activity (13 mm). Carbon tetrachloride extracts of leaves' extract of L. glutinosa showed significant antimicrobial activity which ranged from 11-16 mm zone of inhibition. For extract of M. minutum, dichloromethane solvent extract showed marked antimicrobial activity ranging from 9-13 mm zone of inhibition in diameter. Kanamycin at a concentration of 30 μg/dise was used as positive control in this study.

In this study, methanolic crude extracts and their different fractions i.e. hexane, carbon tetrachloride, dichloromethane and aqueous soluble fractions of the B. daigremontianum(Raym.), C. cordifolia, (Linn.), L. glutinosa(Laur.) and M. minutum(G. Forst.)were subjected for antimicrobial activity. All the fractions were tested against different gram positive and gram negative bacteria and fungi to find out their antimicrobial activity. This study showed that among different fractions of the four important medicinal plants, carbon tetrachloride fraction and crude methanol soluble fraction of leaves' extract of L. glutinosa showed significant activity against gram positive bacteria, gram negative bacteria and fungi at a dose of 400 μg/ disc. Leaves' extract of B. daigremontianum showed mild to moderate antimicrobial activity, especially dichloromethane solvent extract showed significant antimicrobial activity showing 10-13 mm zone of inhibition in diameter, against Shigelladysenteriaethe extract showed highest activity (13 mm). Carbon tetrachloride extracts of leaves' extract of L. glutinosa showed significant antimicrobial activity which ranged from 11-16 mm zone of inhibition. For extract of M. minutum, dichloromethane solvent extract showed marked antimicrobial activity ranging from 9-13 mm zone of inhibition in diameter. Kanamycin at a concentration of 30 μg/dise was used as positive control in this study.

The antifungal activity of aqueous and organic(acetone and methanol) leaf extracts of Anastatica hierochuntica was evaluated a gainst some common pathogenic fungi using the paper disc diffusion method .ALL the extracts were active against the test organisms with the methanol extracts showing the highest activity against candida albicans (28 mm zone of inhibition ), Cryptococcus neoformans(24 mm zone of inhibition ) ,fusarium oxysporum and penicillium digitatam ( 18 mm zone of inhibition ), followed by the acetone extracts against penicillium digitatam ( 16 mm zone of inhibition ), at 250 mg /ml . the aqueous extracts demonstrated the lowest activity (8 mm zone of inhibition ),against penicillium digitatam and (6 mm zone of in hibition) against Aspergillus niger at 250 mg /ml .preliminary phytochemical studies revealed that the leaves contained Hydrocarbonate, glocoberin ,Aminoacid ,glycoside ,Asteroids ,carbohydrate ,flavonoid (one structure: isovitexin and four structures flavonoloids, campferol ,Raminoglocozid ,Rutin ,Qurcetn ) ,Alkaloids, tannins.The activity of the extracts was stable at high temperatures and at acidic PH ,but decreased at alkaline PH .the minimum Inhibitory concentration ( MIC) and the minimum fungicidal concentration ( MFC) of the extracts ranged between 12.5- 150 mg /ml .the plant contain chemicals substances that can be used in the formulation of very potent antifungal agents that can be used for the treatment of Mycotic infections.

Antibiotic resistance has become a global concern and hence, the search for other source of antimicrobials initiated to find a way to control infections in future. The main objective of this paper is to screen Giloy (Tinospora cordifolia) for its antibacterial activity. The stem of Tinospora cordifolia is used to prepare extract for determining it’s in vitro antibacterial activity as per the agar well diffusion method. In the agar well diffusion method 100μl of 24 hr broth culture of bacteria was aseptically and evenly swabbed on Mueller Hinton agar plates. Wells of about 8 mm diameter were aseptically cut using sterile cork-borer. 100 μl of plant extracts of different concentrations were then placed into the separate wells. The plates were incubated at 37 oC for 24hr. Antimicrobial activity of the giloy was determined by measuring the diameter of zone of inhibition. The methanolic extract of Tinospora cordifolia showed 13, 11, 9 and 5 mm zone of inhibition in S. aureus cultures by using 100, 75, 50 and 25 mg/ml concentration, respectively while hot water extract of Tinospora cordifolia showed 14, 12, 10 and 8 mm zone of inhibition for S. aureus by using 100, 75, 50 and 25 mg/ml concentration, respectively and the cold extract of Tinospora cordifolia showed 10, 8, 5 and 0 mm zone of inhibition for S. aureus by using 100, 75, 50 and 25mg/ml concentration, respectively. The methanolic extract of Tinospora cordifolia indicated 12, 10, 6 and 4 mm zone of inhibition in cultures of E.coli by using 100, 75, 50 and 25 mg/ml concentration, respectively and the hot water extract of Tinospora cordifolia showed 16, 14, 12 and 10 mm zone of inhibition in cultures of E.coli by using 100, 75, 50 and 25mg/ml concentration, respectively. The cold water extract of Tinospora cordifolia showed 13, 10, 8, and 5 mm zone of inhibition in cultures of E.coli by using 100, 75, 50 and 25 mg/ml concentration, respectively. It has been observed that Tinospora cordifolia showed very promising results as indicated by the zone of inhibition of bacterial culture through agar well diffusion method that varies from few mm to few cm. This study indicates the in-vitro antibacterial effect of Giloy which needs further validation through in-vivo studies.

In the present study, the prevalence of pathogenic bacteria from poultry environment was investigated. Potentially pathogenic organisms were isolated and identified notably; Salmonella enteritidis, Shigella sp., Clostridium perfringens, Pseudomonas sp., E. coli, Staphylococcus aureus, Vibrio cholerae and Vibrio parahemolyticus. The susceptibility of the isolates to different antibiotics was tested and it was observed that Pseudomonas sp. was very sensitive to the antibiotics, Ceporex (10µg) and Tarivd (10µg) with 16mm zone of inhibition. Clostridium sp. was more susceptible to Levofloxacin (20µg) with 20 mm zone of inhibition, Staph. aureus was more susceptible to Streptomycin (30µg) and Levoflaxacin (20µg) with 18mm zone of inhibition, E. coli was more susceptible to Gentamycin (10µg) with 20mm zone of inhibition, Salmonella enteritidis was more sensitive to Augmentin (30µg) with 20mm zone of inhibition and Shigella sp. was more sensitive to Ciproflox (10µg) with 20mm zone of inhibition. The pathogenicity of these isolates was studied by infecting each on mice. There was death of two mice infected with Clostridium perfringens. Mice infected with Shigella sp., suffered swollen of the scrotum and scrotal sac which was observed after dissection. Mice infected with Pseudomonas sp., Staphylococcus aureus, and Salmonella enteritidis and E. coli, 25x108, 8x108, 20x108, 10x108 cfu/ml of the infected organisms were recovered from their intestine respectively. It seems that the organisms colonized their intestine at high level and they shed them in their faeces, though the infections were asymptomatic at the stage.

In this study, bacterial cellulose was produced through the fermentation of a mixture of black tea, ginger, and sugar, and used to create bio-textile films on sugarcane-based media. Characterization included ribosomal RNA gene sequencing, FTIR spectroscopy, XRD, and SEM was used to examine surface morphology. The bio-textile films showed increasing UV resistance beyond 10 days of cultivation (T.UVA%; 0.13 ± 0.02, T.UVB%; 0.22 ± 0.01, UPF; 629 ± 2.12) and antimicrobial resistance was assessed by quantifying Colony-Forming Units (CFU), resulting in a 100% reduction in growth for both Escherichia coli and Staphylococcus aureus. Subsequently, after 15 days of cultivation, antimicrobial activity was evaluated using the disc agar diffusion method, yielding noteworthy outcomes. E. coli displayed a 25 mm zone of inhibition, S. aureus exhibited a 31 mm zone of inhibition, Candida albicans showed a 35 mm zone of inhibition, and Aspergillus niger presented a 22 mm zone of inhibition.

Clausena anisata is one of the medicinal plants used traditionally for treatment of parasitic infections, irritation (boils, ringworm, and eczema), flatworm infestations, influenza, abdominal cramps, and constipation. Phytochemical screening test of dichloromethane/methanol (1 : 1) roots extract revealed the presence of flavonoids, phytosterols, coumarins, phenols, alkaloids, tannins, terpenoids, and free reducing sugars and the absence of saponins. Silica gel column chromatographic separation of the dichloromethane/methanol (1 : 1) extract afforded a carbazole alkaloid derivative of heptazoline (1) and three coumarins (2–4), including the known coumarins imperatorin (3) and chalepin (4). Structures of the compounds were elucidated by spectroscopic techniques (IR, 1H NMR, 13C NMR, and DEPT-135). Antibacterial activity of the crude extracts and isolated compounds was screened using agar diffusion method against strains of Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Bacillus substilis. The results of antibacterial test revealed derivative of heptaphylline (1) and imperatorin (3) exhibited comparable antibacterial activity against S. aureus and B. substilis (14 and 13 mm zone of inhibition, respectively) to that of ciprofloxacin (15 mm zone of inhibition) at a concentration of 20 µg/mL. Chalepin (4) revealed more antibacterial activity against B. substilis (16 mm zone of inhibition) compared to ciprofloxacin (15 mm).

Background: Management of ever growing multidrug resistant (MDR) bacteria becomes one of the biggest threats to public health worldwide. The situation is worsening due to lack of new generation antimicrobials in the arsenal of the clinicians. Development of new alternatives to the conventional antimicrobial agents is the need of the hour to control the menace of AMR. Plants based products are attractive alternatives with proven efficacy but needs scientific investigation to explore their potential antimicrobial, antibiofilm and antiquorum sensing activities against major bacterial pathogens of human and animals. The present study was conducted to explore the antimicrobial, antibiofilm and antiquorum sensing activity of aqueous and methanol extracts of leaf, flower, fruit and stem of the Himalayan yellow raspberry (Rubus ellipticus) against clinical isolates of Staphylococcus aureus and Escherichia coli. Methods: E. coli and S. aureus were isolated and identified from diarrhoeic pigs and poultry and mastitic milk of cattle of Mizoram, respectively. Leaf, flower, fruit and stem/bark of R. ellipticus were collected from Mizoram and extracted by methanol and aqueous solvents. The antimicrobial activity and MIC was determined by well diffusion method and 96 wells microtiter plate method, respectively. Antibiofilm activity of plant extracts was determined in 96 well tissue culture plate. Antiquorum sensing activity was determined by disc diffusion method. Result: Methanol leaf extract exhibited antimicrobial activity against S. aureus with 19 mm and 7 mm zone of inhibition at 200 mg/mL and 12.5 mg/mL, respectively. Methanol fruit extract also showed antimicrobial activity against S. aureus only. Highest and lowest activities were observed at 200 mg/mL and 25 mg/mL concentrations with 15 mm and 7 mm zone of inhibition, respectively. No antimicrobial activities by either of the extracts were observed against E. coli isolates. The MIC of R. ellipticus methanol leaf and fruit extracts against S. aureus was 0.203125 mg/mL and 0.8125 mg/mL, respectively. The methanol leaf (86.60%) and stem (85.60%) extracts of R. ellipticus showed significant antibiofilm activity against S. aureus isolates, whereas methanol fruit (89.20%) extracts exhibited antibiofilm activity against E. coli isolates at the concentration of 0.05 mg/mL. Significant antiquorum sensing (QS) activities was exhibited by the methanol leaf extract of R. ellipticus at 200 mg/mL concentration against E. coli. This is the first ever report on antibiofilm and anti QS activities of the R. ellipticus plant extracts against E. coli and S. aureus bacteria.

Objective: The aim of this study was to explicate antibacterial, antifungal, and antioxidant activities of Leucas aspera flowers.Methods: Antibacterial activity was done by agar diffusion method. The ethyl acetate extract of L. aspera flower was evaluated against both Gram-positive and Gram-negative bacteria. Antifungal activity was also done by agar diffusion method. The agar used for antifungal activity was Czapek Dox Agar. Nitric oxide scavenging assay and free radical scavenging assay were used for the antioxidant activity. Griess reagent was used in nitric oxide scavenging assay. 1,1-diphenyl-2-picryl hydrazyl was used in free radical scavenging assay.Results: L. aspera flower extract showed good antibacterial activity with the highest zone of inhibition against Vibrio cholera with 23 mm followed by Bacillus polymyxa showing 20 mm zone of inhibition. The ethyl acetate extract of L. aspera flower showed quite a good results with the highest inhibitory activity against Aspergillus niger with 13 mm zone of inhibition and lowest for Trichoderma viridae with 5 mm zone of inhibition. Antioxidant activity of L. aspera flower extract was done by free radical scavenging assay and nitric oxide scavenging assay. Nitric oxide scavenging assay showed prominent results almost performed equal to standard compound Butylated hydroxyl anisole (BHA) The values for 10 μl of L. aspera extract was 50.27, for the standard (BHA) showed 50.81. L. aspera extract values for 50 μl was 69.73 and for BHA, the values was 77.30. For 100 μl, the extract gave 82.70, and for standard BHA, the reading was 89.73.Conclusion: The results showed that L. aspera flower has broad-spectrum antibacterial activity ranging from 23 to 13 mm zone of inhibition. L. aspera flower has strong antioxidative power on nitric oxide radicals. The medicinal properties of plant species have made an outstanding contribution to the origin and evolution of many traditional herbal therapies.