Green synthesis of silver nanoparticles from discarded shells of velvet tamarind (Dialium cochinchinense) and their antimicrobial synergistic potentials and biofilm inhibition properties.

In the field of nanomedicine, biogenic metal nanoparticles are commonly synthesized using edible plant products as bio-reducing or stabilizing agents. In this study, discarded shell of velvet tamarind fruit is explored as a potent reducing agent for biogenic synthesis of silver nanoparticles (VeV-AgNPs). Silver nanoparticles were formed in minutes under sunlight exposure, which was considerably fast compared to under ambient conditions. The optical, structural and morphological studies revealed that the nanoparticle colloidal solution consisted of particles with quasi-spherical and rodlike morphologies. To investigate antimicrobial properties, eight microorganisms were exposed to the VeV-AgNPs. The results indicated that VeV-AgNPs had enhanced antimicrobial activity, with a recorded minimum inhibitory concentration (MIC) of 3.9 µg/mL against E. coli. Further studies were conducted to examine the biofilm inhibition properties and synergistic effect of the VeV-AgNPs. The findings showed a biofilm inhibition potential of around 98% against E. coli, and the particles were also found to increase the efficacy of standard antimicrobial agents. The combinatory effect with standard antifungal and antibacterial agents ranged from synergistic to antagonistic effects against the tested microorganisms. These results suggest that silver nanoparticles produced from discarded shells of velvet tamarind are potent and could be used as a potential drug candidate to combat antimicrobial resistance.

Isolation and Identification of Flavanone Derivative Eriodictyol from the Methanol Extract of Afzelia africana Bark and Its Antimicrobial and Antioxidant Activities.

Background: Afzelia africana is a plant species with well-documented ethnobotanical and medicinal properties. The plant is reported to have various secondary metabolites and had been applied for the treatment of various diseased conditions. Objectives: The study objectives include fractionation, isolation, purification, and characterization of eriodictyol from the bark of A. africana, and the determination of its antimicrobial and antioxidant activities. Methodology. The series of methodologies that were employed include fractionations and purification (column chromatography), characterization (HPLC, LC-MS, IR, 1H, 13C, DEPT-135, HSQC, and HMBC), antimicrobial assays (microbroth dilution and checkerboard assay), and antioxidant activities assays (ABTS and DPPH scavenging capacity). Results: The study reports the identification and characterization of eriodictyol from the bark of A. africana which exhibited potent antioxidant activities against ABTS and DPPH radicals with scavenging capacities (SC50) of 2.14 ± 0.05 and 2.51 ± 0.06 µg/mL, respectively. The compound exhibited its antimicrobial activity by reporting good bacteriostatic activities (MBC/MIC > 4) against Staphylococcus aureus (SA), methicillin-resistant Staphylococcus aureus (MRSA), and fluconazole-resistant Candida albicans (CA2). Moreover, a broad spectrum of bactericidal effects (MBC/MIC ≤ 4) was reported against Streptococcus mutans (SM), Escherichia coli (EC), Bacillus subtilis (BS), Klebsiella pneumonia (KP), Pseudomonas aeruginosa (PA), Salmonella typhi (ST), and standard Candida albicans (CA1). The compound further exhibited synergistic effects against EC, KP, ST, and MRSA; ST; and CA2 when combined with ciprofloxacin, tetracycline, and nystatin, respectively. However, antagonistic effects were observed against PA and CA1 when combined with ciprofloxacin and ketoconazole, respectively. Conclusion: The study reports for the first time the identification of eriodictyol from the bark of A. africana which exhibited significant antioxidant and antimicrobial properties.

Green synthesis of silver nanoparticles from peel extract of Chrysophyllum albidum fruit and their antimicrobial synergistic potentials and biofilm inhibition properties.

Current methods for green synthesis of metal nanoparticles often require continuous harvesting of fresh bio-materials for every synthesis cycle. Practices and procedures that economize bio-materials need to be employed if green synthesis could become a sustainable and eco-friendly method for synthesizing metal nanoparticles. This study explores Chrysophyllum albidum peels (mostly regarded as waste) to prepare silver nanoparticles (Alb-AgNPs). The technique employed in the synthesis allows repeated use of the peels, thus, reducing the heavy dependence on bio-materials. The optical and structural properties of the Alb-AgNPs were studied with Scanning electron microscope, Fourier transform infrared spectrometer, UV-Vis spectrophotometer and powder X-ray diffractometer. The antimicrobial properties of the Alb-AgNPs were studied with selected microorganisms namely; S. aureus, E. coli, K. pneumoniae, B. subtilis, S. mutans, P. aeruginosa, S. typhi, and Candida albicans. High inhibitory activity against the microorganisms were exhibited with MICs ranging from 15.62 to 1000 µg/mL. Again, the Alb-AgNPs showed the ability to enhance the efficacy of standard antimicrobial agents. The results of the combined interaction with standard antibacterial and antifungal agents ranged from synergistic to antagonistic effects against the tested microorganisms. In addition, the Alb-AgNPs could serve as a biofilm inhibitor with the highest percent inhibition of about 92% against methicillin-resistant Staphylococcus aureus. The results from this study thus provide access to the simple, sustainable, economic and eco-friendly synthesis of silver nanoparticles with efficient antimicrobial properties as drug candidates as a means of overcoming the prevailing antibiotic resistance menaces.

Antifungal synergistic effects and anti-biofilm formation activities of some bioactive 2,3-dihydro-1,5-benzoxazepine derivatives.

Benzoxazepines constitute a significant class of organic compounds extensively described in the literature. Several derivatives with pharmacological properties have been produced due to the semi-rigid azepine scaffold, which allows for the addition of other heteroatoms. This study investigated the possible antifungal effect and antioxidant activity of 2,3-dihydro-1,5-benzoxazepines. The antifungal effect was investigated using the broth dilution assay, while the antioxidant property was determined using the ABTS and DPPH scavenging tests. The results indicated that the 2,3-dihydro-1,5-benzoxazepine derivatives had antifungal properties and could be working via its fungicidal and biofilm inhibitory properties. It was also realized that it had synergistic effects when administered concomitantly with standard antifungal drugs. The antioxidant effects were high with 2,2-dimethyl-4-[(E)-2-(4-methylphenyl)ethenyl]-2,3-dihydro-1,5-benzoxazepine (1) compared to the other derivatives. It could be concluded that 2,3-dihydro-1,5-benzoxazepines could possess fungicidal and possible antioxidant properties. And hence could serve as new drug leads in discovering novel drugs that could help manage fluconazole-resistant vulvovaginal candidiasis.

Metabolite profiling, antifungal, biofilm formation prevention and disruption of mature biofilm activities of Erythrina senegalensis stem bark extract against Candida albicans and Candida glabrata.

The antifungal activity of the 70% ethanol stem bark extract of Erythrina senegalensis (ESB) against different strains and drug resistant clinical isolates of Candida albicans and Candida glabrata were evaluated in the study. The effect of ESB on biofilms as well as its activity in combination with fluconazole, nystatin or caspofungin against the Candida strains were also evaluated. We then evaluated the antifungal activity of a microemulsion formulation of ESB against planktonic and biofilms of the Candida species. UPLC-QTOF-MS2 analysis was then undertaken to identify the phytoconstituents of the extract and UPLC fingerprints developed for the routine authentication as part of quality control measures. ESB exerted strong antifungal activities against C. albicans ATCC 10231 and SC5314 strains, and C. glabrata ATCC 2001 strain with minimum inhibitory concentration (MIC) values from 3.91 to 31.25 µg/mL and minimum fungicidal concentrations (MFCs) that ranged from 62.5 to 250 µg/mL. It also exhibited potent antifungal activities (MIC = 4-64 µg/mL) against a collection of C. albicans and C. glabrata clinical isolates that were resistant to either nystatin or azole antifungals. The formulated ESB demonstrated higher antifungal potency against the C. albicans and C. glabrata strains with MIC values of 3.91-31.25 µg/mL which was the same as the MFC values. The extract and its microemulsion formulation were active against biofilms of the strains of the Candida species inhibiting their biofilm formations (SMIC50 = 16-64 µg/mL) and their preformed biofilms (SMIC50 = 128 ->512 µg/mL). ESB also exhibited synergistic antifungal action with fluconazole and nystatin against C. albicans ATCC 10231 and C. glabrata ATCC 2001 strains in the checkerboard assay. Chemical characterization of the extract revealed the presence of phenolic compounds such as flavonoids and their prenylated derivatives, anthracene glycosides and alkaloids. UPLC Fingerprints of the extract was also developed and validated for routine identification and authentication of the stem bark of E. senegalensis. The study findings have demonstrated that the stem bark of E. senegalensis is as a potential source of bioactive compounds that could be developed as novel antifungal agents.

GC/MS Composition and Resistance Modulatory Inhibitory Activities of Three Extracts of Lemongrass: Citral Modulates the Activities of Five Antibiotics at Sub-Inhibitory Concentrations on Methicillin-Resistant Staphylococcus aureus.

We investigated whether three extractable fractions of lemongrass (Cymbopogon citratus): aqueous and ethanol extracts and lemongrass essential oil exhibited any antimicrobial resistance modulatory effects if used in combination with selected antibiotics ampicillin, tetracycline, streptomycin, cefloxacin and amoxicillin on methicillin-resistant Staphylococcus aureus (MRSA). MRSA growth inhibition (zones of inhibition) was greatest for the lemongrass oil at concentrations of 1, 2, 5, 10 and 20 % (wt/vol). The MIC for lemongrass oil was 0.5 mg/mL, while it was 4 mg/mL for both the aqueous and ethanol extracts. Evaluation of extracts for antibacterial resistance modifying activities when used in combination with either of the five antibiotics at sub-inhibitory concentrations, showed that lemongrass oil highly potentiated the activities of three antibiotics; amoxicillin, streptomycin and tetracycline. The ethanol extract enhanced the activity of tetracycline and ampicillin, while the aqueous extract only increased the activity of tetracycline against MRSA. The activity of cefloxacin with the extracts was either indifferent. Analysis of the lemongrass oil by GC/MS showed the prominence of three compounds: the two isomers neral and geranial of citral and, the acetate geranyl acetate, which together made up 94 % of the composition. The compounds were also observed in the ethanol and water extracts but to a lesser extent when analyzed by HPLC-UV (λ 233 nm). Our study confirms the antibacterial properties of the extracts especially, lemongrass oil. It also demonstrates that lemongrass oil potentiates the activities of three antibiotics against the biofilm-forming MRSA. This biocidal, anti-biofilm disruption and antibiotic potentiating abilities are mainly attributable to citral and geranyl acetate, further evidence of lemongrass oil as a very useful source of phytochemicals, especially citral for the fight against antibiotic resistance.

Antifungal Activities of Phytochemically Characterized Hydroethanolic Extracts of Sclerocarya birrea Leaves and Stem Bark against Fluconazole-Resistant Candida albicans Strains.

The study evaluated the antifungal activities of the 70% ethanol extracts of Sclerocarya birrea leaves (SBL) and stem bark (SBB) against C. albicans strains and fluconazole-resistant isolates, their antifungal effects in combination with conventional antifungals as well as their effects on the biofilms of the C. albicans strains and isolates. UPLC-QTOF-MS/MS analysis was then carried out to investigate the metabolite profile of the extracts and UPLC fingerprints developed for their routine identification as part of quality control measures. The extracts exhibited considerable antifungal activity with MIC ranging from 12.21 to 97.66 µg/mL and MFC from 12.21 to 390.63 µg/mL against the C. albicans strains and isolates. The antifungal activity of the stem bark extract was higher than the leaf extract. SBL and SBB also significantly inhibited biofilm formation (IC50 = 12.49 to 164.42 µg/mL) and the mature biofilms (IC50 = 91.50 to 685.20 µg/mL) of the strains and isolates of the C. albicans and demonstrated potential for their use in combination therapies with currently used antifungals especially the stem bark extract with nystatin. Metabolite profiling identified the presence of polyphenolic compounds in both leaves and stem bark mostly flavonoids, their derivatives, and proanthocyanidins, which contribute in part to the bioactivity of the plant. Whereas flavonoids like quercetin, myricetin, and their derivatives were abundant in the leaves, epicatechin monomers with their condensed tannins, including procyanidin B2 and procyanidin C, were abundant in the stem bark. Fingerprints of SBL and SBB were developed and validated and could be used as qualitative tools to authenticate the plant. The outcomes of the study show the promise of the leaf and stem bark extracts of S. birrea to be studied further and developed as antifungal agents.

Bioassay-Guided Fractionation, ESI-MS Scan, Phytochemical Screening, and Antiplasmodial Activity of Afzelia africana.

Background: Afzelia africana is a plant species with reported numerous medicinal potentials and secondary metabolites. Various parts of the plant have been applied for the treatment of hernia, rheumatism, pain, lumbago, malaria, etc. The study seeks to evaluate the phytochemical constituents, antiplasmodial, and ESI-MS scan of bioassay-guided fractions from the methanol extract of the bark of the plant. Aims: The main aim of the study was to carry out bioassay-guided fractionation of the crude methanol extract of Afzelia africana in order to isolate fractions and to evaluate their antiplasmodial activities and ESI-MS fingerprints. Methods: The methods employed include column chromatographic fractionation, phytochemical screening, antiplasmodial activity (malaria SYBER green assay (MSF)), and ESI-MS profile (full ESI-MS scan). Results: The column chromatographic fractionation and phytochemical screening of the plant led to the separation of the following four fractions: 1 (flavonoids, phenolics, glycosides, terpenoids, and steroids), 2 (alkaloids, anthraquinones, flavonoids, phenolics, glycosides, terpenoids, and steroids), 3 (anthraquinones, flavonoids, phenolics, glycosides, terpenoids, and steroids), and 4 (alkaloids, flavonoids, phenolics, glycosides, terpenoids, and steroids). The antiplasmodial activities of the fractions were tested against the 3D7 strain of Plasmodium falciparum with reported stronger activities for 1 (IC50: 0.097 ± 0.034 µg/mL) and 3 (IC50: 1.43 ± 0.072 µg/mL), and weaker activities for 2 (IC50: >100 µg/mL) and 4 (IC50: 37.09 ± 6.14 µg/mL). The full ESI-MS fingerprint of fractions 1, 2, 3, and 4 revealed the presence of 14, 24, 34, and 37 major molecular ions or compounds in each fraction, respectively.

Antibiofilm Activity of Azadirachta indica and Catharanthus roseus and Their Synergistic Effects in Combination with Antimicrobial Agents against Fluconazole-Resistant Candida albicans Strains and MRSA.

The rapid emergence and spread of antimicrobial resistance has become a global public health concern that threatens the effective treatment of infectious diseases. One major approach adopted to overcome antimicrobial resistance is the use of plant extracts individually and/or with combination of antibiotics with plant extracts, which may lead to new ways of treating infectious diseases and essentially representing a potential area for further future investigations. In this study, the antifungal activities of Azadirachta indica leaf and Catharanthus roseus flower extracts against fluconazole-resistant Candida albicans strains (isolated from pregnant women with vulvovaginal candidiasis) and anti-methicillin-resistant Staphylococcus aureus (MRSA) were evaluated by agar well diffusion, microdilution, and biofilm inhibition assays. Subsequently, the determination of the combined antimicrobial activity of the individual plant extracts with (fluconazole and voriconazole) and (ampicillin, tetracycline, and streptomycin) against C. albicans strains and MRSA, respectively, was evaluated by checkerboard microdilution assay. Results from the study showed that the antimicrobial activity of the two plant extracts determined by time-kill kinetics was fungistatic with their MICs ranging from 0.1 to 4 mg/mL. Interestingly, all extracts were proved as good biofilm inhibitors of resistant C. albicans and MRSA from 10.1 to 98.82%. Their combination interaction with fluconazole, voriconazole, ampicillin, tetracycline, and streptomycin ranged from synergy to antagonism as per the parameters used. Overall, these results showed that A. indica leaf and C. roseus flower extracts have significant antifungal property. Furthermore, A. indica leaf and C. roseus flower extracts alone or in combination with fluconazole and voriconazole could provide a promising approach to the management of candidiasis caused by drug-resistant strains as well as their interaction with the antibacterial agents to combat the common infections caused by MRSA.

Hypoglycaemic activity of Oleanonic acid, a 3-oxotriterpenoid isolated from Aidia Genipiflora (DC.) Dandy, involves inhibition of carbohydrate metabolic enzymes and promotion of glucose uptake.

The present study evaluated the antidiabetic activities of the 70% ethanol stem bark extract of Aidia genipiflora (AGB) and one of its constituents, oleanonic acid in streptozotocin (40 mg/kg)-induced diabetic rats. In vitro assays of glucose uptake and inhibition of carbohydrate metabolizing enzymes were then used to investigate their mechanism(s) of hypoglycaemic action. In silico evaluation of the pharmacokinetic and toxicity properties of the compound was also carried out. Administration of AGB (100-400 mg/kg) and oleanonic acid (15 - 60 mg/kg) resulted in significant reductions (p < 0.001) in the blood glucose and considerable decrease (p < 0.05) in the elevated lipid parameters of the diabetic animals. AGB activity at 200 and 400 mg/kg; and oleanonic acid at 60 mg/kg were comparable to glibenclamide (5 mg/kg). The extract and its isolate strongly inhibited α-glucosidase and α-amylase activity with IC50 values of (10.48 ± 1.39 µg/mL and 14.51 ± 1.26 µg/mL) and (36.52 ± 1.95 µM and 105.84 ± 1.08 µM) respectively. The glucose uptake assays showed that AGB and oleanonic acid exerted both insulin-dependent and independent promotional effect of glucose transport into the periphery by upregulating the expression of PI3K and PPARγ transcripts with a concomitant increase in GLUT-4 transcripts. Although oleanonic acid was predicted to be teratogenic, it was found to be generally non-lethal with favourable pharmacokinetics properties making it suitable for further studies. The study has shown that the stem bark of A. genipiflora is a source of new hypoglycaemic agents and that oleanonic acid possesses hypoglycaemic and anti-hyperlipidaemic activities.

Antioxidant, antibacterial, antifungal activities and gas chromatographic fingerprint of fractions from the root bark of Afzelia africana.

BACKGROUND: Afzelia africana is a tropical plant with numerous ethno-medicinal benefits. The plant has been used for the treatment of pain, hernia, fever, malaria, inflammation and microbial infections. OBJECTIVES: To perform bioassay-guided fractionation, antioxidant and antimicrobial activities of the bark of Afzelia africana. METHODS: Column chromatography fractionation, antioxidant activity (% (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and 1,1-diphenyl picrylhydrazyl (DPPH) scavenging activity))), antimicrobial activity (microbroth dilution: Minimum Inhibitory Concentration (MIC), Minimum Bactericidal Concentration (MBC), MBC/MIC ratio), and synergistic activities (Checkerboard assay: Fraction Inhibitory Concentration Index (FICI)). RESULTS: Bioassay-guided fractionation of A. africana produced four fractions that displayed promising free radical scavenging activities in the ABTS (54-93)% and the DPPH (35-76)% assays in the ranking order of F1(93-54)>F4(81-58)>F2(74-58)>F3(72-55) and F3(77-42)>F1(64-46)>F4(55-44)>F2(47-35) respectively at a concentration range of 1.0-0.01 mg/mL. The fraction F1 (MBC: 2.5-5.0 mg/mL) and F4 (MBC: 1.25-10.0 mg/mL) exhibited broad spectrum of superior bactericidal effects than F2 (MBC≥100.0 mg/mL) and F3 (MBC: 12.5-100.0 mg/mL) against Staphylococcus mutans, Staphylococcus aureus, Escherichia coli, fluconazole-resistant Candida albicans, methicillin-resistant S. aureus, Bacillus subtilis, Klebsiella pneumonia, Pseudomonas aeruginosa, Salmonella typhi, and Candida albicans (standard strain). The two most active fractions (F1 and F4) reported synergistic effects (FICI≤0.5) against S. typhi whilst the F4 reported additional synergism against E. coli, K. pneumonia, and S. typhi when combined with ciprofloxacin. Furthermore, the two fractions reported synergistic effects against Escherichia coli, Klebsiella pneumonia, Salmonella typhi, and Pseudomonas aeruginosa when combined with tetracycline whilst F1 reported antifungal synergism against fluconazole resistant Candida albicans when combined with fluconazole and ketoconazole. CONCLUSION: The study has confirmed the antioxidant, antimicrobial and synergistic uses of A. africana for the treatment of both infectious and non-infectious disease.

Evaluation of the Modulatory Effect of Annona muricata Extracts on the Activity of Some Selected Antibiotics against Biofilm-Forming MRSA.

The study investigated the influence of Annona muricata extracts on the action of selected antibiotics against biofilm-forming MRSA. The various parts of the plant were processed into powder and extracted with ethanol or hot water and then screened for the presence of phytochemicals. The modulatory effect of the Annona muricata extract was also tested on some antibiotics against Methicillin-resistant Staphylococcus aureus (MRSA). The findings from this study revealed that the various parts of the Annona muricata extract (ethanolic and aqueous) contained different proportions of secondary metabolites. Varied antimicrobial activities were observed when the extract of the A. muricata was exposed to MRSA strain at a concentration of 100 mg/mL. The stem recorded the highest (17.00 and 18.00 mm) inhibitory activity against MRSA for both the aqueous and the ethanolic extract, respectively, and this was not different from the control, tetracycline. Again, the results on the modulatory action indicated that out of the 10 extracts of A. muricata, 4 of them antagonized the activity of ampicillin against the tested MRSA by a factor of 0.5 folds and the rest potentiated the drug within 1-4 folds, respectively. On the other hand, the various test extracts significantly potentiated the efficacy of streptomycin and tetracycline against the MRSA by a range of 1-32 folds with the aqueous root extract recording the highest synergistic effect and ethanol seed extract with the least effect. The findings of this study support the antibacterial activities of the A. muricata plant parts.

Bioactive triterpenoids from Solanum torvum fruits with antifungal, resistance modulatory and anti-biofilm formation activities against fluconazole-resistant candida albicans strains.

Vulvovaginal candidiasis (VVC) is the second most common vaginal infection that affects women of reproductive age. Its increased occurrence and associated treatment cost coupled to the rise in resistance of the causative pathogen to current antifungal therapies has necessitated the need for the discovery and development of novel effective antifungal agents for the treatment of the disease. We report in this study the anti-Candida albicans activity of Solanum torvum 70% ethanol fruit extract (STF), fractions and some isolated compounds against four (4) fluconazole-resistant strains of C. albicans. We further report on the effect of the isolated compounds on the antifungal activity of fluconazole and voriconazole in the resistant isolates as well as their inhibitory effect on C. albicans biofilm formation. STF was fractionated using n-hexane, chloroform (CHCl3) and ethyl acetate (EtOAc) to obtain four respective major fractions, which were then evaluated for anti-C. albicans activity using the microbroth dilution method. The whole extract and fractions recorded MICs that ranged from 0.25 to 16.00 mg/mL. From the most active fraction, STF- CHCl3 (MIC = 0.25-1.00 mg/mL), four (4) known compounds were isolated as Betulinic acid, 3-oxo-friedelan-20α-oic acid, Sitosterol-3-ß-D-glucopyranoside and Oleanolic acid. The compounds demonstrated considerably higher antifungal activity (0.016 to 0.512 mg/mL) than the extract and fractions and caused a concentration-dependent anti-biofilm formation activity. They also increased the sensitivity of the C. albicans isolates to fluconazole. This is the first report of 3-oxo-friedelan-20α-oic acid in the plant as well as the first report of betulinic acid, sitosterol-3-ß-D-glucopyranoside and oleanolic acid from the fruits of S. torvum. The present study has demonstrated the anti-C. albicans activity of the constituents of S. torvum ethanol fruit extract and also shown that the constituents possess anti-biofilm formation and resistance modulatory activities against fluconazole-resistant clinical C. albicans isolates.