14 research outputs found
Microbial activity of some heterocyclic Schiff bases and metal complexes: A review
Microbial resistance to current drugs associated with food spoilage and complications in diseases’ treatment have resulted in increased mortality rate globally. Schiff bases are an important versatile class of organic compounds with notable pharmacological properties for various industrial applications. They are usually synthesized from a condensation reaction between a primary amine and a carbonyl. They have a wide range of activities against microbes and demonstrate good antimicrobial activity against fungi, bacteria, parasites, and viruses. The antimicrobial activity of Schiff base ligands is usually better upon metal complexation as a result of their chelating behaviour. The synthesis of Schiff bases and their metal complexes are well-documented. Therefore, it is important to categorize and compile them according to their biological significance. In this review, the antibacterial, antifungal, antiparasitic and antiviral activity of some selected heterocyclic Schiff bases and their metal complexes are discussed.Keywords: Heterocyclic Schiff bases, Metal complexes, Antibacterial, Antifungal, Antiparasitic, Antivira
Synthesis, antibacterial, and cytotoxicity evaluation of oleanolic acid-4-aminoquinoline based hybrid compounds
AIM : The study aims to prepare a class of oleanolic-based compounds.
BACKGROUND : Conventional drugs used to treat infectious diseases suffer from limitations such as drug toxicity and drug resistance. The resistance of microbes to antimicrobial agents is a significant challenge in treating microbial infections. Combining two or more drugs with different modes of action to treat microbial infections results in a delay in developing drug resistance by the microbes. However, it is challenging to select the appropriate drugs for combination therapy due to the differences in stability and pharmacokinetic profile of the drugs. Therefore, developing hybrid compounds using the existing drugs is a promising approach to design effective antimicrobial agents.
OBJECTIVES : To prepare oleanolic-based hybrid compounds followed by characterization, in vitro antibacterial and cytotoxicity evaluation.
METHODS : Oleanolic acid-4-aminoquinoline-based hybrid compounds were synthesized via esterification and amidation. The compounds were characterized using FTIR, NMR, and UHPLC-HRMS. Oleanolic acid (OA) was isolated from the flower buds of Syzygium aromaticum (L.) Merr. & L.M.Perry, a species from Kingdom Plantae, order Mytales in the Myrtaceae family. Antibacterial activity was determined against selected strains of bacteria using the microdilution assay and cytotoxicity activity was assessed using the sulforhodamine B assay against selected cancer cell lines.
RESULTS : The synthesized hybrid compounds exhibited antibacterial activity against the Gram-positive bacteria Enterococcus faecalis (ATCC13047), Bacillus subtilis (ATCC19659), Staphylococcus aureus as well as Gram-negative bacteria, Klebsiella oxytoca (ATCC8724), Escherischia coli (ATCC25922), and Proteus vulgaris (ATCC6380) with minimum inhibitory concentrations of 1.25 mg/mL compared to oleanolic acid (2.5 mg/mL). Compounds 13 and 14 displayed cytotoxicity in vitro against the cancer cell lines (MCF-7 and DU 145) compared to the oleanolic acid (IC50 ˃ 200 μM).
CONCLUSION : Modification of C28 of OA enhanced its biological activity.https://www.eurekaselect.com/journal/207hj2022Pharmacolog
Synthesis of silver nanoparticles from a Desmodium adscendens extract and its antibacterial evaluation on wound dressing material
The one-pot synthesis of silver nanoparticles (AgNPs) using the medium-polar extract of Desmodium adscendens (Sw.) DC. is presented here as an alternative synthesis of metal NPs. Characterisation of the formed NPs showed polydispersed AgNPs ranging from 15 to 100 nm where the concentration of metal ions was found to play a role in the size and shape of the prepared NPs. It could be established that the flavonoids, saponins, and alkaloids present in the extract acted as both reducing and stabilising agents during the formation of the capped metal NPs. This means of NP synthesis was also employed during the in situ immobilisation of AgNPs on gauze and plaster. An evaluation of the antibacterial activity of the medium-polar D. adscendens extract, AgNPs suspended in solution, and the immobilised AgNPs against Staphylococcus aureus (ATCC 25923), Bacillus cereus (ATCC 11778), and Escherichia coli (ATCC 25922) showed high efficacy against the latter in particular. This suggests that gauze, dilute silver nitrate solutions, and D. adscendens extract could be used successfully in the simple in situ preparation of effective antibacterial wound dressings
Traditional uses, phytochemistry, pharmacology and other potential applications of Vitellaria paradoxa Gaertn. (Sapotaceae): A review
Vitellaria paradoxa Gaertn. is a multipurpose medicinal plant of the family Sapotaceae, and it has been widely used usually in the clinical traditional medicine as remedy for a wide range of diseases for several decades. In addition, the plant has also found applications in confectionery, cosmetics and soaps, and pharmaceuticals both locally and internationally. V. paradoxa, which has been identified with >150 phytoconstituents, is rich in oleanane-type triterpene acids and glycosides, such as paradoxosides A-E, tieghemelin A, parkiosides A-C, bassic acid, as well as flavonoids such as quercetin and catechin-type compounds. The extracts and the active constituents of V. paradoxa have been investigated for various pharmacological activities, including but not limited to anticancer, melanogenesis-inhibitory, antibacterial, anti-diabetic, antioxidant, anti-inflammatory, anti-diarrhoeal, and antifungal activities. Additionally, V. paradoxa has also been utilized in nanoparticles (NPs) synthesis. These NPs among other things have shown significant antinociceptive and antiedematogenic activities as well as environmental friendly adsorptive properties for the removal of pollutants from pharmaceutical effluents. Overall, this review comprehensively examines the traditional uses, phytochemistry, pharmacology, toxicology, clinical studies, and nanoparticles synthesized from V. paradoxa and their applications
Profiling of volatile flavor compounds in nkui (a Cameroonian food) by solid phase extraction and 2D gas chromatography time of flight mass spectrometry (SPME-GC×GC-TOF-MS)
Abstract: The objective of this study was to investigate the volatile flavor compounds of nkui, a Cameroonian food, using solid phase microextraction (SPME) and a two-dimensional gas chromatography time of flight mass spectrometry GC×GC-TOF- MS system. Using SPME, volatile compounds were extracted from nkui and analyzed by GC×GC-TOF- MS. The data retrieved revealed the presence of flavor volatiles including acids (20%), alcohols (4%), aldehydes (10%), aromatic compounds (4%), esters (7%), furans (4%), ketones (11%), terpenes and terpernoids (27%). Although the terpene compounds were the most predominant, an ester (linalyl acetate) had the highest percentage of 19%, conferring a sweet, green and citrus flavor. Results obtained from this study suggest that the characteristic flavor of nkui was due to the combination of different volatile flavor compounds, which contributed to its aroma. Considering the medicinal importance of these compounds, their presence positions nkui as a vital food source with health benefits and medicinal properties
Synthesis, FTIR, NMR, UV–vis and electrochemistry analysis of ferrocenyl Schiff bases
DATA AVAILABILITY : Data will be made available on request.Please read abstract in the article.The Department of Chemical Sciences, the University of Johannesburg.http://www.elsevier.com/locate/ica2023-12-02hj2023ChemistryNon
Carboxymethyl cellulose/poloxamer gels enriched with essential oil and Ag nanoparticles: promising wound dressings. Supplementary materials.
Supplementary figures 1-3
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Ecdysteroids from the Stem Bark of Vitex doniana Sweet (Lamiaceae; ex. Verbenaceae): A Geographically Variable African Medicinal Species.
Vitex doniana Sweet is an African medicinal species that is prescribed as an aqueous bark extract to be applied topically or orally to achieve anti-infective outcomes. In select regions it is also taken orally as an antimalarial agent. The aim of the current study was to explore the biological properties of V. doniana and isolated compounds in the context of pathogenic bacteria and the protozoan parasite Plasmodium falciparum. Three compounds were isolated and assigned by nuclear magnetic resonance spectroscopy as ecdysteroids: (1) 20-hydroxyecdysone, (2) turkesterone, and (3) ajugasterone C. Interestingly, two of these compounds had not previously been identified in V. doniana, providing evidence of chemical variability between regions. The bark extract and three ecdysteroids were screened for activity against a panel of pathogenic bacteria associated with skin, stomach and urinary tract infections, and the protozoan parasite P. falciparum. The crude extract of the bark inhibited all bacterial strains with MIC values of 125–250 μg.mL−1. The three isolated compounds demonstrated less activity with MIC values of 500–1000 μg.mL−1. Furthermore, no activity was observed against P. falciparum at the screening concentration of 4.8 μg.mL−1. Nevertheless, we present a hypothesis for the possible mechanism for symptomatic relief of malarial fever, which may involve reduction of prostaglandin E(1) & E(2) activity in the hypothalamus via modulation of the monoaminergic system. While further studies are required to identify all antimicrobial agents within this plant species and to determine the cytotoxicity of each of these compounds, these data suggest that the traditional application of this species as an antiseptic is valid
Pentacyclic Triterpenoids, Phytosteroids and Fatty Acid Isolated from the Stem-bark of Cola lateritia K. Schum. (Sterculiaceae) of Cameroon origin; Evaluation of Their Antibacterial Activity
The phytochemical investigation on the chemical constituents of dichloromethane-methanol (1:1) stem-bark extract ofCola lateritiaK. Schum. (Sterculiaceae) led to the isolationand characterization of five pentacyclic triterpenoids, one fatty acid and two phytosteroids. Thecompounds were identified as heptadecanoic acid (1), maslinic acid (2), betulinic acid (3), lupenone(4), lupeol (5), friedelin (6),b-stigmasterol (7) andß-sitosterol-3-O-ß-D-glucoside (8). Their struc-tures were determined by NMR analysis (1H,13C, DEPT-135, COSY, HMBC and HSQC), high-resolution mass spectrometry (HR-ESI-MS) and comparisons with published data in the literature.This work, to the best of our knowledge, is the first isolation and identification of these compoundsin pure forms fromCola lateritia. Also, compounds1–3are reported for the first time fromColagenus.In vitroantibacterial activity of the isolated compounds (1–8) and the crude extract wereevaluated againstBacillus subtilis,Staphylococcus epidermidis,Enterococcus faecalis,Mycobacterium smegmatis,Staphylococcus aureus,Enterobacter cloacae,Klebsiella oxytoca,Proteusvulgaris,Klebsiella pneumonia,Escherichia coli, Proteus mirabilisandKlebsiella aerogeneswithstreptomycin, nalidixic acid and ampicillin as standard antibacterial drugs. Compound2was activeagainstE. faecalis(MIC = 18.5mg/mL), and it was 6.9 and 28 times lower and active than that ofstreptomycin (MIC 128mg/mL) and nalidixic acid (MIC>512mg/mL) respectively. All the isolatedcompounds and crude extract showed significant activities against the tested bacterial strains.National Research Foundatio