scholarly journals Analysis of a “3-(Naphthalen-1-ylimino)indolin-2-one” Compound and Its Antimicrobial Assessment Using Lipid-Based Self-Nanoemulsifying Formulations

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 15
Author(s):  
Saeed Ali Syed ◽  
Ahmed Bari ◽  
Mohammed S. Aldughaim ◽  
Md Abdur Rashid ◽  
Mohammad Hossain Shariare ◽  
...  

In recent years, indole derivatives have acquired conspicuous significance due to their wide spectrum of biological activities—antibacterial, antiviral, and anticonvulsant. This compound is derived from naturally grown plants. Therefore, synthesis of a novel “3-(Naphthalen-1-ylimino)indolin-2-one” compound (2) and its analysis using UPLC systems along with antimicrobial assessment was the aim of the current study. Isatin was used as a parent drug for synthesizing compound (2). Liquid Chromatographic analysis was performed using a C18 BEH column (1.7 μm 2.1 × 50 mm) by UPLC systems. Degradation studies were carried out to see whether acid, base, thermal, and oxidizing agents had any impact on the synthesized molecule in stress conditions (100 °C). A lipid-based self-nanoemulsifying formulation was developed and selectivity, specificity, recovery, accuracy, and precision were measured as part of the UPLC system’s validation process. Antimicrobial studies were conducted using gram-positive and gram-negative bacteria. The standard samples were run with a concentration range of 5.0–100.0 μg/mL using the isocratic mobile phase comprising of methanol/water (70/30 %v/v) at 234 nm; good linearity (R2 = 0.9998) was found. The lower limits of detection (LOD) and quantitation (LOQ) of the method were found to be 0.81 μg/mL and 2.5 μg/mL, respectively. The coefficients of variation were found to be less than 2%. The antimicrobial study suggests that compound (2) has a substantial growth effect against gram-negative bacteria. It was successfully synthesized and applied to measure the concentrations in lipid-based dosage form, along with potent antimicrobial activities.

2009 ◽  
Vol 23 (1) ◽  
pp. 45-50 ◽  
Author(s):  
Ghulam Rabbani ◽  
Anvarhusein A. Isab ◽  
Abdul Rahman Al-Arfaj ◽  
Saeed Ahmad ◽  
Muhammad Saleem ◽  
...  

Mercury(II) complexes of thiolates having the general formula [Hg(RS)Cl2]−and [Hg(RS)2] have been prepared and characterized by IR and NMR (1H and13C) spectroscopy (RSH = 2-aminoethanethiol hydrochloride (Aet), cysteine (Cys), thiosalicylic acid (Ts) and 2-mercaptonicotinic acid (Mnt)). The spectral data suggests that the coordination of thiolates to mercury(II) occurs through the sulfur as indicated by the absence of S–H vibrations in IR and significant downfield shifts in the C–S resonance in13C NMR. However, in Mnt complexes, coordination through both sulfur and nitrogen is indicated. Antimicrobial activities of the complexes were evaluated by minimum inhibitory concentration and the results showed that the complexes exhibited a wide range of activities against gram-negative bacteria (E. coli, P. aeruginosa), while moderate activity was observed against a mold,P. citrinum.


2010 ◽  
Vol 5 (6) ◽  
pp. 1934578X1000500 ◽  
Author(s):  
Raphaël Bikanga ◽  
Thomas Makani ◽  
Huguette Agnaniet ◽  
Louis Clément Obame ◽  
Fatouma Mohamed Abdoul-Latif ◽  
...  

Water-distilled essential oils from leaves and bark of Santiria trimera (Oliv.) Aubrév. (Burseraceae) collected in Gabon were analyzed using capillary GC-FID and GC-MS. The leaf essential oil, which is described for the first time, was dominated by sesquiterpenes (76.5%), among which α-humulene (34.6%) and β-caryophyllene (14.9%) were the major components. The bark essential oil was almost exclusively monoterpenic, with α-pinene (51.5%) and α-terpineol (16.8%) as main constituents. The antimicrobial activities of both essential oils were tested against eight Gram-positive and three Gram-negative bacteria by using agar disc diffusion and broth microdilution methods; anticandidal effect was also tested on different strains of Candida albica. The Gram-negative bacteria were the less sensitive to the leaf essential oil, which was effective against Bacillus cereus and Enterococcus faecalis. The bark essential oil was more active and, in particular, exhibited significant antimicrobial activity against Proteus mirabilis, which was resistant to the leaf oil. A weak anticandidal effect of both essential oils was observed.


2000 ◽  
Vol 44 (4) ◽  
pp. 848-852 ◽  
Author(s):  
C. M. Kunin ◽  
W. Y. Ellis

ABSTRACT Mefloquine was found to have bactericidal activity against methicillin- and fluoroquinolone-susceptible and -resistant strains ofStaphylococcus aureus and Staphylococcus epidermidis and gentamicin- and vancomycin-resistant strains ofEnterococcus faecalis and Enterococcus faecium. The MICs were 16 μg/ml, and the minimal bactericidal concentrations (MBCs) were 16 to 32 μg/ml. These concentrations cannot be achieved in serum. Mefloquine was active at a more achievable concentration against penicillin-susceptible and -resistant Streptococcus pneumoniae, with MICs of 0.2 to 1.5 μg/ml. Mefloquine was not active against gram-negative bacteria and yeasts. In an attempt to find more active derivatives, 400 mefloquine-related compounds were selected from the chemical inventory of The Walter Reed Army Institute of Research. We identified a series of compounds containing a piperidine methanol group attached to pyridine, quinoline, and benzylquinoline ring systems. These had activities similar to that of mefloquine against S. pneumoniae but were far more active against other gram-positive bacteria (MICs for staphylococci, 0.8 to 6.3 μg/ml). They had activities similar to that of amphotericin B againstCandida spp. and Cryptococcus neoformans. Combinations of the compounds with gentamicin and vancomycin were additive against staphylococci and pneumococci. The MIC and MBC of gentamicin were decreased by four- to eightfold when this drug was combined with limiting dilutions of the compounds. There was no antagonism with other antimicrobial drugs. The compounds were rapidly bactericidal. They appear to act by disrupting cell membranes. Combinations of the compounds with aminoglycoside antibiotics may have potential for therapeutic use.


2021 ◽  
Vol 2 (2) ◽  
Author(s):  
Eti Nurwening Sholikhah ◽  
Maulina Diah ◽  
Mustofa ◽  
Masriani ◽  
Susi Iravati ◽  
...  

Pycnarrhena cauliflora (Miers.) Diels., local name sengkubak, is one of indigenous plants from West Kalimantan that has been used as natural flavor. Pycnorrhena cauliflora is one of species of Menispermaceae family which is rich in bisbenzylisoquinoline alkaloids. This alkaloids are known to have various biological activities including antiprotozoal, antiplasmodial, antifungal and antibacterial activities. This study aimed to investigate antimicrobial activity of  the P. cauliflora (Miers.) Diels. methanolic extracts against gram-positive and gram-negative bacteria. The methanolic extract of P. cauliflora (Miers.) Diels., root, leaf and stem were prepared by maceration. The disk-diffusion method was then used to determine the antimicrobial activity of the extracts against Streptococcus pyogenes, S. mutants, Staphylococcus aureus, S. epidermidis, Salmonella typhi, Shigella flexneri, Pseudomonas aeruginosa and Escherichia coli after 18-24 h incubation at 37 oC. Amoxicillin was used as positive control for gram-positive bacteria and ciprofloxacin was used as gram-negative bacteria. The inhibition zones were then measured in mm. Analysis were conducted in duplicates. The results showed in general the methanolic extracts of P. cauliflora (Miers.) Diels. root (inhibition zone diameter= 10-23 mm) were more active than that leaf (0-15 mm) and stem (0-17 mm) extracts against gram-positive bacteria. The zone inhibition diameter of amoxicillin as positive control was 8-42 mm. In addition, the methanolic extracts of P. cauliflora (Miers.) Diels. root (12-17 mm) were also more active than that leaf (0-12 mm) and stem (0-12 mm) extracts against gram-negative bacteria. The zone inhibition diameter of ciprofloxacin as positive control was 33-36 mm. In conclusion, the methanolic extract of P. caulifloria (Miers.) Diels. root is the most extract active against both gram-positive and gram-negative bacteria. Further study will be focused to isolate active compounds in the methanolic extract of the root.


2021 ◽  
Vol 13 (1) ◽  
pp. 106-112
Author(s):  
Sri Kasmiyati ◽  
Elizabeth Betty Elok Kristiani ◽  
Maria Marina Herawati ◽  
Andreas Binar Aji Sukmana

The medicinal plant-derived bioactive compounds have a potential for many biological activities, including antimicrobial activity. Artemisia cina is a medicinal plant from the Compositae family with the potential of having antitumor, antifungal, and antibacterial activity. This study aimed to determine the antibacterial activity and the flavonoid content of A. Cina’s ethyl acetate extract. Plants samples were extracted by ethyl acetate maceration method. Antibacterial activity was tested against Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) by a disk diffusion method using 25, 50, and 100 mg/l extract concentrations. The flavonoid contents (quercetin and kaempferol) were measured using High-Performance Liquid Chromatography. The extracts of diploid and polyploid A. cina displayed some antibacterial activity, with the Gram-negative bacteria being more resistant than the Gram-positive counterpart. However, no significant difference was observed between the diploid and polyploid extracts. As for the flavonoid content, the highest quercetin content (0.5501 mg/ml) was found in the polyploid A. cina (J), while the highest kaempferol content (0.5818 mg/ml) was observed in the diploid A. cina (KJT). Although A. cina is widely grown in Indonesia, compared to other Artemisia species, A. cina has not been widely studied, especially its antibacterial  potential and in related to its flavonoid content and the use of ethyl acetate as the extraction solvent.  This study reveals the potential of A. cina as a natural antibacterial agent. 


1962 ◽  
Vol 8 (5) ◽  
pp. 621-628 ◽  
Author(s):  
W. A. Taber ◽  
B. B. Wiley

The antimicrobial activities of a branched, monoalkyl benzene sulphonate complex (ABS), the active component of a commercial liquid household detergent, and of the detergent have been investigated. Cultures of dermatophytes, Candida albicans, saprophytic phycomycetes, ascomycetes, fungi imperfecti, Gram-positive and Gram-negative bacteria were tested. Only the Fusarium species and the Gram-negative bacteria were not inhibited by a concentration of 0.1 ml of the detergent/50 ml medium. Microgram quantities of ABS inhibited the Gram-positive bacteria and the fungi except Fusarium spp. ABS was lethal in microgram quantities, the effect being detectable within 30 minutes. Inhibition of exogenous respiration of glucose by C. albicans began upon contact and was complete within 50 minutes. A linear and biodegradable ABS was more active than the branched form against C. albicans.


2020 ◽  
Vol 9 (6) ◽  
pp. 238-244
Author(s):  
Meharrar Nadjet ◽  
Bekada Ahmed Mohamed Ali ◽  
Dris Ibrahim ◽  
Jacques Dommes ◽  
Arabi Abed ◽  
...  

The genera Cistus present groups of about twenty species of shrubs belon- ging to the Cistaceae family are very common throughout the Mediterranean region. Cistus salviifolius, known as Melliya is a species of this genus that occurs in the forest region of Mount Ouarsenis (northwest Algeria), exactly in Thniet El Had Na onal Park in the Wilaya of Tissemsilt. This study was un- dertaken to evaluate the an bacterial effects of C. salviifolius and its chemical composition in addition the effect of shade drying me on essen al oil yield in order to op mize this parameter which is most o en not controlled for producers. The op mal yield recorded is about 0.07± 0.02%. Its characte- riza on by gas chromatography coupled with mass spectrometry shows a dominance of hydrocarbon compounds. The minimum inhibitory concentration (MIC) is established using 6 strains of Gram-positive and negative bacteria. The antibiotic susceptibility test is performed using the giliose- environment diffusion method, a bacterial suspension is prepared and subsequently well homogenized. Opacity must be adjusted to 0.5 McF (McFarland), from a young exponen al culture (18 to 24 hours). The an mi- crobial ac vity of C. salviifolius EO was tested against three Gram-posi ve and three Gram-nega ve bacteria. In fact, a strong inhibitory and bactericidal effect has been demonstrated against all Gram-positive and Gram- negative bacteria tested. It appears from this study that the EO of C. salviifo- lius has a very high antimicrobial activity, it shows a wide spectrum covering Gram positive and Gram negative bacteria. Taking into account the results of this study, new an bacterial agents could be developed and the use of C.salviifolius should be encouraged in the pharmaceutical and perfumery industries.


2016 ◽  
Vol 78 (3-2) ◽  
Author(s):  
Nor Syafawani Sarah Md Saad ◽  
Nik Ahmad Nizam Nik Malek ◽  
Chun Shiong Chong

The aim of this research was to determine the antimicrobial activity of kaolinite modified with antimicrobial compounds against Gram positive and Gram negative bacteria. Copper kaolinite (Cu-kaolinite) was prepared by loading raw kaolinite with copper nitrate trihydrate (CuNO3) while surfactant modified Cu-kaolinite (SM-Cu-kaolinite) was prepared by adding cationic surfactants hexadecyltrimethyl ammonium (HDTMA) on Cu-Kaolinite. Samples was characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) analyzer. The antimicrobial activity of the samples was tested against Gram negative bacteria (Escherichia coli ATCC 11229 and Pseudomonas aeruginosa ATCC 15442), and Gram positive bacteria (Staphylococcus aureus ATCC 6538 and Enterococcus faecalis ATCC 29212) through disc diffusion technique (DDT) and minimum inhibition concentration (MIC). The results showed that the antimicrobial activity of Cu-kaolinite increased after modified with HDTMA due to the synergistic effects of Cu ions and HDTMA molecules on the kaolinite. The antimicrobial activity for surfactant modified Cu-kaolinite was greater for Gram positive bacteria compared to Gram negative bacteria. In conclusion, the attachment of HDTMA on Cu-kaolinite contributed to the enhanced antimicrobial activity against wide spectrum of bacteria (Gram positive and Gram negative bacteria).


Polymers ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 670 ◽  
Author(s):  
Alzagameem ◽  
Klein ◽  
Bergs ◽  
Do ◽  
Korte ◽  
...  

The antiradical and antimicrobial activity of lignin and lignin-based films are both of great interest for applications such as food packaging additives. The polyphenolic structure of lignin in addition to the presence of O-containing functional groups is potentially responsible for these activities. This study used DPPH assays to discuss the antiradical activity of HPMC/lignin and HPMC/lignin/chitosan films. The scavenging activity (SA) of both binary (HPMC/lignin) and ternary (HPMC/lignin/chitosan) systems was affected by the percentage of the added lignin: the 5% addition showed the highest activity and the 30% addition had the lowest. Both scavenging activity and antimicrobial activity are dependent on the biomass source showing the following trend: organosolv of softwood > kraft of softwood > organosolv of grass. Testing the antimicrobial activities of lignins and lignin-containing films showed high antimicrobial activities against Gram-positive and Gram-negative bacteria at 35 °C and at low temperatures (0–7 °C). Purification of kraft lignin has a negative effect on the antimicrobial activity while storage has positive effect. The lignin release in the produced films affected the activity positively and the chitosan addition enhances the activity even more for both Gram-positive and Gram-negative bacteria. Testing the films against spoilage bacteria that grow at low temperatures revealed the activity of the 30% addition on HPMC/L1 film against both B. thermosphacta and P. fluorescens while L5 was active only against B. thermosphacta. In HPMC/lignin/chitosan films, the 5% addition exhibited activity against both B. thermosphacta and P. fluorescens.


1999 ◽  
Vol 43 (5) ◽  
pp. 1072-1076 ◽  
Author(s):  
Junko K. Akada ◽  
Mutsunori Shirai ◽  
Kenji Fujii ◽  
Kiwamu Okita ◽  
Teruko Nakazawa

ABSTRACT The new rifamycin derivatives KRM-1657 and KRM-1648 were evaluated for their in vitro antimicrobial activities against 44 strains ofHelicobacter pylori. Although the drugs were not very active against other gram-negative bacteria, the MICs at which 90% of isolates are inhibited for these drugs were lower (0.002 and 0.008 μg/ml, respectively) than those of amoxicillin and rifampin forH. pylori. Time-kill studies revealed that the bactericidal activities of these agents were due to cell lysis. The results presented here indicate that these new rifamycin derivatives may be useful for the eradication of H. pylori infections.


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