Strong Antimicrobial Activity Research Articles

Scalable Fabrication of Polymeric Composite Microspheres to Inhibit Oral Pathogens and Promote Osteogenic Differentiation of Periodontal Membrane Stem Cells.

Periodontitis is a worldwide bacterial infectious disease, resulting in the resorption of tooth-supporting structures. Biodegradable polymeric microspheres are emerging as an appealing local therapy candidate for periodontal defect regeneration but suffer from tedious procedures and low yields. Herein, we developed a facile yet scalable approach to prepare polylactide composite microspheres with outstanding drug-loading capability. It was realized by blending equimolar polylactide enantiomers at the temperature between the melting point of homocrystallites and stereocomplex (sc) crystallites, enabling the precipitation of sc crystallites in the form of microspheres. Meanwhile, epigallocatechin gallate (EGCG) and nano-hydroxyapatite were encapsulated in the microspheres in the designated amount. Such an assembly allowed the fast and sustained release of EGCG and Ca2+ ions. The resultant hybrid composite microspheres not only exhibited strong antimicrobial activity against typical oral pathogens (Porphyromonas gingivalis and Enterococcus faecalis), but also directly promoted osteogenic differentiation of periodontal ligament stem cells with good cytocompatibility. These dual-functional composite microspheres offer a desired drug delivery platform to address the practical needs for periodontitis treatment.

Controlled Size Oils Based Green Fabrication of Silver Nanoparticles for Photocatalytic and Antimicrobial Application.

The particle size at the nanometric level allows the manifestation of remarkable properties, chiefly due to changes in surface-to-volume ratio. This study is attributed to the novel green synthesis of nano silver by using essential oils as a capping and reducing agent. Clove oil, cinnamon oil, and cardamom oil were selected for the eco-friendly and low-cost fabrication of silver nanoparticles. The prepared nanoparticles were characterized by photoluminescence spectroscopy, FT-IR spectroscopy, X-Ray diffraction, energy dispersive X-ray spectroscopy, dynamic laser light scattering, thermogravimetric analysis, and transmission electron microscopy. It was found that samples prepared by using cinnamon oil (20 nm) and cardamom oil (12 nm) had smaller particle sizes as compared to those synthesized by using clove oil (45 nm). All the prepared samples exhibited very strong antimicrobial activities with a clear zone of inhibition (6-24 mm) against Staphylococcus aureus, Klebsiella pneumoniae, and Candida albicans. Very resilient photocatalytic activities of the samples were observed against Allura red and fast green dyes. It was concluded that the cinnamon oil-based system is the best size reducer and size homogenizer (less chances of agglomeration) as compared to clove oil and cardamom oil (more chances of agglomeration) for the synthesis of silver nanoparticles.

Antimicrobial and antioxidant potential from Piper marginatum roots

This is the first report of the antimicrobial and antioxidant potential of extract from Piper marginatum roots. The extract showed highest antioxidant activity with an EC50 of 47.3 ± 0.80 µg/mL and a total phenolic content of 42.7 ± 1.10 mg GAE/g. The extract exhibited strong antimicrobial activity with minimum inhibitory concentrations of 250, 250 and 125 µg/mL for the bacteria Bacillus subtilis, Staphylococcus aureus and fungus Mycobacterium smegmatis. Antimicrobial activity was attributed to (E,E)-N-Isobutyl -2,4-octadienamide and (E,E)-N-Isobutyl-2,4-decadienamide amides isolated as major compounds of the roots. Structural elucidation of the two amides was determined based on the interpretation of their IR, UV, MS, 1H and 13C NMR spectra. The results contribute significantly to the development of a herbal remedies based on P. marginatum roots.

Characterization of the Antimicrobial Activities of Trichoplusia ni Cecropin A as a High-Potency Therapeutic against Colistin-Resistant Escherichia coli.

The spread of colistin-resistant bacteria is a serious threat to public health. As an alternative to traditional antibiotics, antimicrobial peptides (AMPs) show promise against multidrug resistance. In this study, we investigated the activity of the insect AMP Tricoplusia ni cecropin A (T. ni cecropin) against colistin-resistant bacteria. T. ni cecropin exhibited significant antibacterial and antibiofilm activities against colistin-resistant Escherichia coli (ColREC) with low cytotoxicity against mammalian cells in vitro. Results of permeabilization of the ColREC outer membrane as monitored through 1-N-phenylnaphthylamine uptake, scanning electron microscopy, lipopolysaccharide (LPS) neutralization, and LPS-binding interaction revealed that T. ni cecropin manifested antibacterial activity by targeting the outer membrane of E. coli with strong interaction with LPS. T. ni cecropin specifically targeted toll-like receptor 4 (TLR4) and showed anti-inflammatory activities with a significant reduction of inflammatory cytokines in macrophages stimulated with either LPS or ColREC via blockade of TLR4-mediated inflammatory signaling. Moreover, T. ni cecropin exhibited anti-septic effects in an LPS-induced endotoxemia mouse model, confirming its LPS-neutralizing activity, immunosuppressive effect, and recovery of organ damage in vivo. These findings demonstrate that T. ni cecropin exerts strong antimicrobial activities against ColREC and could serve as a foundation for the development of AMP therapeutics.

Silver nanoclusters with Ag2+/3+ oxidative states are a new highly effective tool against phytopathogenic bacteria

The main measure worldwide adopted to manage plant bacterial diseases is based on the application of copper compounds, which are often partially efficacious for the frequent appearance of copper-resistant bacterial strains and have raised concerns for their toxicity to the environment and humans. Therefore, there is an increasing need to develop new environmentally friendly, efficient, and reliable strategies for controlling plant bacterial diseases, and among them, the use of nanoparticles seems promising. The present study aimed to evaluate the feasibility of protecting plants against attacks of gram-negative and gram-positive phytopathogenic bacteria by using electrochemically synthesized silver ultra nanoclusters (ARGIRIUM‑SUNCs®) with an average size of 1.79 nm and characterized by rare oxidative states (Ag2+/3+). ARGIRIUM‑SUNCs strongly inhibited the in vitro growth (effective concentration, EC50, less than 1 ppm) and biofilm formation of Pseudomonas syringae pv. tomato and of quarantine bacteria Xanthomonas vesicatoria, Xylella fastidiosa subsp. pauca, and Clavibacter michiganensis subsp. michiganensis. In addition, treatments with ARGIRIUM‑SUNCs also provoked the eradication of biofilm for P. syringae pv. tomato, X. vesicatoria, and C. michiganensis subsp. michiganensis. Treatment of tomato plants via root absorption with ARGIRIUM‑SUNCs (10 ppm) is not phytotoxic and protected (80%) the plants against P. syringae pv. tomato attacks. ARGIRIUM‑SUNCs at low doses induced hormetic effects on P. syringae pv. tomato, X. vesicatoria, and C. michiganensis subsp. michiganensis as well as on tomato root growth. The use of ARGIRIUM‑SUNCs in protecting plants against phytopathogenic bacteria is a possible alternative control measure.Key points• ARGIRIUM‑SUNC has strong antimicrobial activities against phytopathogenic bacteria;• ARGIRIUM‑SUNC inhibits biofilm formation at low doses;• ARGIRIUM‑SUNC protects tomato plants against bacterial speck disease.

Biochemical and Antioxidant Properties as well as Antimicrobial and Antibiofilm Activities of Allium scorodoprasum subsp. jajlae (Vved.) Stearn.

In this study, the chemical composition and biological activity of Allium scorodoprasum subsp. jajlae (Vved.) Stearn were investigated for the first time, focusing on its antimicrobial, antioxidant, and antibiofilm properties. A GC-MS analysis was employed to evaluate the composition of its secondary metabolites, identifying linoleic acid, palmitic acid, and octadecanoic acid 2,3-dihydroxypropyl ester as the major compounds in ethanol extract. The antimicrobial activity of A. scorodoprasum subsp. jajlae was assessed against 26 strains, including standard, food isolate, clinical isolate, and multidrug-resistant ones, as well as three Candida species using the disc diffusion method and the determination of the minimum inhibitory concentration (MIC). The extract showed strong antimicrobial activity against Staphylococcus aureus strains, including methicillin-resistant and multidrug-resistant strains, as well as Candida tropicalis and Candida glabrata. Its antioxidant capacity was evaluated using the DPPH method, revealing a high level of antioxidant activity in the plant. Additionally, the antibiofilm activity of A. scorodoprasum subsp. jajlae was determined, demonstrating a reduction in biofilm formation for the Escherichia coli ATCC 25922 strain and an increase in biofilm formation for the other tested strains. The findings suggest potential applications of A. scorodoprasum subsp. jajlae in the development of novel antimicrobial, antioxidant, and antibiofilm agents.

Comparing the Ability of Secretory Signal Peptides for Heterologous Expression of Anti-Lipopolysaccharide Factor 3 in Chlamydomonas reinhardtii

Anti-lipopolysaccharide factor 3 (ALFPm3) possesses a wide antimicrobial spectrum and high antibacterial and viral activities for broad application prospects in the aquaculture industry. However, the application of ALFPm3 is limited by its low production in nature, as well as its low activity when expressed in Escherichia coli and yeast. Although it has been proven that its secretory expression can be used to produce antimicrobial peptides with strong antimicrobial activity, there is no study on the high-efficiency secretory expression of ALFPm3 in Chlamydomonas reinhardtii. In this study, signal peptides ARS1 and CAH1 were fused with ALFPm3 and inserted into the pESVH vector to construct pH-aALF and pH-cALF plasmids, respectively, that were transformed to C. reinhardtii JUV using the glass bead method. Subsequently, through antibiotic screening, DNA-PCR, and RT-PCR, transformants expressing ALFPm3 were confirmed and named T-JaA and T-JcA, respectively. The peptide ALFPm3 could be detected in algal cells and culture medium by immunoblot, meaning that ALFPm3 was successfully expressed in C. reinhardtii and secreted into the extracellular environment. Moreover, ALFPm3 extracts from the culture media of T-JaA and T-JcA showed significant inhibitory effects on the growth of V. harveyi, V. alginolyticus, V. anguillarum, and V. parahaemolyticus within 24 h. Interestingly, the inhibitory rate of c-ALFPm3 from T-JcA against four Vibrio was 2.77 to 6.23 times greater than that of a-ALFPm3 from T-JaA, indicating that the CAH1 signal peptide was more helpful in enhancing the secreted expression of the ALFPm3 peptide. Our results provided a new strategy for the secretory production of ALFPm3 with high antibacterial activity in C. reinhardtii, which could improve the application potentiality of ALFPm3 in the aquaculture industry.

Impact of Mt. Olympus Honeys on Virulence Factors Implicated in Pathogenesis Exerted by Pseudomonas aeruginosa

The aim of this study was to examine the impact of twenty honey samples, harvested in Mt. Olympus (Greece), on the virulence factors implicated in P. aeruginosa pathogenesis. Six key virulence factors (protease and elastase activity, pyocyanin and pyoverdine concentration, biofilm formation, and swimming motility) were selected in order to assess the effect of the tested honeys compared with Manuka honey. All tested honeys demonstrated a significant inhibition of protease and elastase activity compared with the control. Six and thirteen honeys exerted superior protease (no inhibition zone) and elastase (values lower than 55%) activity, respectively, compared with Manuka honey. Seventeen tested honeys exhibited reduced pyoverdine production compared with the control; all tested honeys, except for one, showed an inhibitory effect on pyocyanin production compared with the control. Regarding swimming motility, nine tested honeys demonstrated significantly higher inhibition compared with Manuka honey. Honey concentrations (6% v/v and 8% v/v) had the most profound impact, as they reduced biofilm formation to less than 20% compared with the control. Overall, our data demonstrate a significant inhibition of the virulence factors in the tested Mt. Olympus honeys, highlighting the strong antimicrobial activity against P. aeruginosa, an antibiotic-resistant pathogen of growing concern, which is implicated in severe nosocomial infections globally.

Chitosan-based multifunctional films reinforced with cerium oxide nanoparticles for food packaging applications

The current study discusses the use of nanoceria as a multifunctional filler in food packaging biopolymer films for the first time. Nanoceria was synthesized using co-precipitation method. Chitosan-based food packaging films incorporated with 1 wt% and 2 wt% nanoceria were prepared and characterized. The FTIR absorption spectra confirms the presence of hydrogen bonding between nanoceria and chitosan structure. The nanocomposite films displayed strong UV-A and UV-B blocking properties besides being mechanically strong, thermally stable and possessing high moisture barrier properties. Further, due to the switching of oxidation states by cerium between Ce3+ and Ce4+, nanoceria shows high photocatalytic activity. This results in strong antimicrobial activity against E. coli and L. monocytogenes, especially under visible light. Further, the nanocomposite films displayed ∼1.25 times and ∼2.3 times higher ABTS and DPPH free radical scavenging potential, respectively, compared to pristine chitosan films, which indicate their high antioxidant potential. Moreover, the films depicted good biocompatibility towards L929 cells indicating their safety for food contact applications. With all these properties, the nanoceria-added chitosan films display strong potential for use in active food packaging, especially for high fat food products such as nuts and meats.

Comparative genomics reveals key molecular targets for mutant Pediococcus pentosaceus C23221 producing pediocin

Listeria monocytogenes is a common microorganism that causes food spoilage. Pediocins are some biologically active peptides or proteins encoded by ribosomes, which have a strong antimicrobial activity against L. monocytogenes. In this study, the antimicrobial activity of previously isolated P. pentosaceus C-2-1 was enhanced by ultraviolet (UV) mutagenesis. A positive mutant strain P. pentosaceus C23221 was obtained after 8 rounds of UV irradiation with increased antimicrobial activity of 1448 IU/mL, which was 8.47 folds higher than that of wild-type C-2-1. The genome of strain C23221 and wild-type C-2-1 was compared with identify the key genes for higher activity. The genome of the mutant strain C23221 consists of a chromosome of 1,742,268 bp, with 2052 protein-coding genes, 4 rRNA operons, and 47 tRNA genes, which is 79,769 bp less than the original strain. Compared with strain C-2-1, a total of 19 deduced proteins involved in 47 genes are unique to C23221 analyzed by GO database; the specific ped gene related to bacteriocin biosynthesis were detected using antiSMASH in mutant C23221, indicating mutant C23221 produced a new bacteriocin under mutagenesis conditions. This study provides genetic basis for further constituting a rational strategy to genetically engineer wild-type C-2-1 into an overproducer.

PH-responsive chitosan/acrylamide/gold/nanocomposite supported with silver nanoparticles for controlled release of anticancer drug

In this study, we prepared a pH-responsive nanocomposite hydrogel based on chitosan grafted with acrylamide monomer and gold nanoparticles using gamma irradiation method (Cs-g-PAAm/AuNPs). The nanocomposite was enhanced with a layer coating of silver nanoparticles to improve the controlled release of the anticancer drug fluorouracil while increasing antimicrobial activity and decreasing the cytotoxicity of silver nanoparticles in nanocomposite hydrogel by combining with gold nanoparticles to enhance the ability to kill a high number of liver cancer cells. The structure of the nanocomposite materials was studied using FTIR spectroscopy and XRD patterns, which demonstrated the entrapment of gold and silver nanoparticles within the prepared polymer matrix. Dynamic light scattering data revealed the presence of gold and silver in the nanoscale with the polydispersity indexes in the mid-range values, indicating that distribution systems work best. Swelling experiments at various pH levels revealed that the prepared Cs-g-PAAm/Au–Ag-NPs nanocomposite hydrogels were highly responsive to pH changes. Bimetallic pH-responsive Cs-g-PAAm/Au–Ag-NPs nanocomposites exhibit strong antimicrobial activity. The presence of AuNPs reduced the cytotoxicity of AgNPs while increasing their ability to kill a high number of liver cancer cells.Cs-g-PAAm/Au–Ag-NPs has a high amount of fluorouracil drug loaded at pH 7.4 reaching 95 mg/g with a maximum drug release of 97% within 300 min. Cs-g-PAAm/Au–Ag-NPs have been recommended to use as oral delivery of anticancer drugs because they secure the encapsulated drug in the acidic medium of the stomach and release it in the intestinal pH.

Specific Expression of Antimicrobial Peptides from the Black Soldier Fly in the Midgut of Silkworms (Bombyx mori) Regulates Silkworm Immunity.

Antimicrobial peptides are molecules with strong antimicrobial activity and are of substantial interest for the immunization of insects. As a type of dipteran insect that can turn organic waste into animal feed, the black soldier fly (BSF) can "turn waste into treasure". In this study, we investigated the antimicrobial activity of the antimicrobial peptide genes, HiCG13551 and Hidiptericin-1, of BSF in silkworms, by overexpressing the genes specifically in the midgut. Changes in the mRNA levels of the transgenic silkworms after infection with Staphylococcus aureus were evaluated using transcriptome sequencing. The results showed that Hidiptericin-1 had stronger antimicrobial activity than HiCG13551. KEGG enrichment analysis showed that the differentially expressed genes in the transgenic overexpressed Hidiptericin-1 silkworm lines from the D9L strain were mainly enriched in the starch and sucrose metabolism, pantothenate and CoA biosynthesis, drug metabolism (other enzymes), biotin metabolism, platinum drug resistance, galactose metabolism, and pancreatic secretion pathways. In addition, immune-related genes were up-regulated in this transgenic silkworm strain. Our study may provide new insights for future immune studies on insects.

"Prevention of the Dramatic Increase of Multi Resistant Microorganisms. In Situ Generated Biocides Provided by Catalysts Show Fast and Strong Antimicrobial Activity on Surfaces"

"Prevention of the Dramatic Increase of Multi Resistant Microorganisms. In Situ Generated Biocides Provided by Catalysts Show Fast and Strong Antimicrobial Activity on Surfaces"

Antioxidant, Antimicrobial and Phenolic Component Analysis of Some Edge Medicinal Plants

Objective: The plants, which grow wild in the Eastern Anatolia Region and are known as kari (Arum elongatum;Ae) and mende (Chaerophyllum macrospermum;Cm), are used for treatment purposes such as pain reliever and wound healing properties. It is aimed to determine some biological properties of these plants, which are also used medicinally.
 Material-Method: Firstly, hexane(H), ethanol(E) and acetone(A) extracts of dried plants were prepared and antimicrobial activities of extracts against 13 indicator microorganisms were determined by agar well diffusion method. Antioxidant activities were determined by DPPH and ABTS analyses and the total phenolic component contents were determined by the Folin-Ciocalteu method. 
 Results: The maximum extract yield was obtained in the ethanol extracts of the plants (AeE;10.4011% CmE;2.4898%), the minimum extract yield was obtained in the acetone extracts (AeA;0.8422% CmA;0.3510%). The hexane extract of A. elongatum has no inhibition activity against E. faecalis and L. monocytogenes, but it has inhibition activity against other indicator microorganisms. The other extracts of A. elongatum and all extracts of C. macrospermum were found to have inhibitory activity against all indicator microorganisms. Furthermore, the highest phenolic content was calculated as 54.60±0.486 µg mL-1 (AeE) and the lowest content as 3.47±0.001 µg mL-1 (CmA). As a result of the DPPH method the highest IC50 was calculated as 32.4140 µg mL-1 (CmH) and the lowest IC50 as 12.7876 µg mL-1 (AeA) and ABTS method the highest IC50 was calculated as 10.3203 µg mL-1 (CmE), and the lowest IC50 as 0.2744 µg mL-1 (CmA). 
 Conclusion: These results show that the plant extracts have strong antimicrobial activity and antioxidant activity.

An Assassin's Secret: Multifunctional Cytotoxic Compounds in the Predation Venom of the Assassin Bug Psytalla horrida (Reduviidae, Hemiptera).

Predatory assassin bugs produce venomous saliva that enables them to overwhelm, kill, and pre-digest large prey animals. Venom from the posterior main gland (PMG) of the African assassin bug Psytalla horrida has strong cytotoxic effects, but the responsible compounds are yet unknown. Using cation-exchange chromatography, we fractionated PMG extracts from P. horrida and screened the fractions for toxicity. Two venom fractions strongly affected insect cell viability, bacterial growth, erythrocyte integrity, and intracellular calcium levels in Drosophila melanogaster olfactory sensory neurons. LC-MS/MS analysis revealed that both fractions contained gelsolin, redulysins, S1 family peptidases, and proteins from the uncharacterized venom protein family 2. Synthetic peptides representing the putative lytic domain of redulysins had strong antimicrobial activity against Escherichia coli and/or Bacillus subtilis but only weak toxicity towards insect or mammalian cells, indicating a primary role in preventing the intake of microbial pathogens. In contrast, a recombinant venom protein family 2 protein significantly reduced insect cell viability but exhibited no antibacterial or hemolytic activity, suggesting that it plays a role in prey overwhelming and killing. The results of our study show that P. horrida secretes multiple cytotoxic compounds targeting different organisms to facilitate predation and antimicrobial defense.

Molecular Modification of Kex2 P1' Site Enhances Expression and Druggability of Fungal Defensin.

Pichia pastoris is the widely used expression system for producing recombinant secretory proteins. It is known that Kex2 protease plays a vital role in the process of protein secretion, in which the P1' site affects its cleavage efficiency. To enhance the expression level of fungal defensin-derived peptide NZ2114, this work attempts to optimize the P1' site of Kex2 by replacing it with 20 amino acids in turn. The results showed that when the amino acid of the P1' site was changed to Phe (F), the yield of target peptide significantly increased from 2.39 g/L to 4.81 g/L. Additionally, the novel peptide F-NZ2114 (short for FNZ) showed strong antimicrobial activity against Gram-positive (G+) bacteria, especially for Staphylococcus aureus and Streptococcus agalactiae (MIC: 4-8 μg/mL). The FNZ was very stable and retained high activity in various conditions; in addition, a low cytotoxicity and no hemolysis were observed even at a high concentration of 128 μg/mL, and a longer postantibiotic effect was reached. The above results indicate that this engineering strategy provided a feasible optimization scheme for enhancing the expression level and druggability of this antimicrobial peptide from fungal defensin and other similar targets by this updated recombinant yeast.

In vitro antimicrobial studies of some major bioactive compounds isolated from Strychnos innocua (Delile) root bark

Plant based therapies are very essential in modern medicine, and have long been used to cure and prevent chronic diseases in many parts of the world. Medicinal herbs have been shown to have biological properties due to the presence of active compounds. Strychnos innocua, a medicinal plant from Loganiaceae, is commonly consumed for medicinal purposes in various African countries. The need to assess the usefulness of the plant’s root bark in the treatment of disease spurred this study, which involved the isolation of six bioactive compounds and screening for antimicrobial properties against some pathogens using the agar well diffusion method. Chromatography separation led to first time isolation of Umbelliferone (1), Linalool (2), Nerolidol (3), Campesterol (4), β-sitosterol (5), and 2,13-Octadecadien-1-ol (6). GC–MS and NMR spectra, as well as comparisons with published data, were used to determine their structures. The compounds exhibited strong antimicrobial activity comparable to ciprofloxacin and fluconazole against MRSA, B. subtilis, S. pyogenes, S. aureus, K. pneumoniae, E. coli, P. aeruginosa, S. typhii, A. fumigatus, C. albicans, C. krusei, and A. nigre. The MIC as well as the MBC/MFC were determined. In conclusion, the compounds (1 – 6) isolated from S. innocua root bark have remarkable antibacterial action against pathogenic microbes.

Zinc and phosphorus fertilization in Galanthus elwesii Hook: Changes in the total alkaloid, flavonoid, and phenolic content, and evaluation of anti-cancer, anti-microbial, and antioxidant activities

Galanthus elwesii Hook belongs to the Amaryllidaceae family and is an ornamental plant that naturally spreads in the region between Turkey and Europe. It also contains bioactive compounds in the nutraceutical and pharmaceutical field. The objective of this study was to evaluate the effects of zinc (Zn) and phosphorus (P) in the synthesis of alkaloid compounds and bioactive properties in G. elwesii. The plants were subjected to three different concentrations of zinc (2.5, 5, and 10 mg kg−1), and phosphorus (3, 6, and 12 mg kg−1), and compared with the control. Two harvests were evaluated, between 2020 and 2021. The total phenolic content (TPC), total flavonoid content (TFC), and total alkaloid content (TAC) were identified by Folin-Ciocalteu, aluminum chloride, and bromocresol green-complex assays, respectively. TPC (85.09 ± 0.4 mg QE/g), TFC (267.7 ± 1.6 mg GAE/g), and TAC (320.58 ± 2.4 mg CoE/g) were the highest in the treatments of Zn 10, Zn 10 and Zn 2.5 + P 3 mg kg−1, respectively. RP-HPLC analysis revealed that, compared with the control group, galanthamine, and lycorine synthesis were increased by 755% (Zn 5 + P 3 mg kg−1) and 815% (Zn 2.5 mg kg−1) respectively. The highest antioxidant activities of were found to be 80.21% (10 mg kg−1 Zn) and 78.05% (2.5 mg kg−1Zn + 3mg kg−1 P), respectively. The extracts exhibit strong anti-microbial activity, particularly against Bacillus subtilis, Candida albicans, Pseudomonas aeruginosa, Saccharomyces cerevisiae, and Staphylococcus aureus. The MCF-7 cell line was used to investigate its anti-cancer activity properties. The MTT assay result was obtained from extracts treated with Zn 10 mg kg−1 for the best cytotoxic activity against the MCF-7 cell line (IC50 value: 31.57 ± 0.70 μg/mL).

Synthesis of Novel Benzenesulfonamide-Bearing Functionalized Imidazole Derivatives as Novel Candidates Targeting Multidrug-Resistant Mycobacterium abscessus Complex.

Infections caused by drug-resistant (DR) Mycobacterium abscessus (M. abscessus) complex (MAC) are an important public health concern, particularly when affecting individuals with various immunodeficiencies or chronic pulmonary diseases. Rapidly growing antimicrobial resistance among MAC urges us to develop novel antimicrobial candidates for future optimization. Therefore, we have designed and synthesized benzenesulfonamide-bearing functionalized imidazole or S-alkylated derivatives and evaluated their antimicrobial activity using multidrug-resistant M. abscessus strains and compared their antimycobacterial activity using M. bovis BCG and M. tuberculosis H37Ra. Benzenesulfonamide-bearing imidazole-2-thiol compound 13, containing 4-CF3 substituent in benzene ring, showed strong antimicrobial activity against the tested mycobacterial strains and was more active than some antibiotics used as a reference. Furthermore, an imidazole-bearing 4-F substituent and S-methyl group demonstrated good antimicrobial activity against M. abscessus complex strains, as well as M. bovis BCG and M. tuberculosis H37Ra. In summary, these results demonstrated that novel benzenesulfonamide derivatives, bearing substituted imidazoles, could be further explored as potential candidates for the further hit-to-lead optimization of novel antimycobacterial compounds.

Chemical characterization and toxicity evaluation of fungal pigments for potential application in food, phamarceutical and agricultural industries

Concerns associated with the use of synthetic colourants backs the demand for natural colourants. Thus, the current study aimed at characterizing crude fungal pigments produced by Penicillium multicolour, P. canescens, Talaromyces verruculosus, Fusarium solani and P. herquie. This included their antioxidant and antimicrobial properties together with acute toxicity evaluation on zebrafish embryos. The identification of pigment compounds was achieved through MS and IR data. The study demonstrated a substantial radical scavenging activity of extracts ranging from 65.49 to 74.46%, close to that of ascorbic acid (89.21%). Penicillium canescens and F. solani exhibited a strong antimicrobial activity against Escherichia coli and Enterococcus aerogenes and Salmonella typhi, Staphylococcus aureus and Bacillus cereus at MIC values ranging from 1.5 to 2.5 mg/mL. However, some levels of toxicity were observed for all extracts at a concentration range of 3–5 mg/mL. Pigment by P. multicolour, T. verruculosus and F. solani were tentatively identified through IR and MS data as sclerotiorin (yellow), rubropunctamine (red) and bostrycoidin (red). In conclusion, the study demonstrates a market potential of filamentous fungi pigments due to their antioxidant, antimicrobial activities, and prominent colours. Although there are some toxicity concerns, further tests must be done using molecular docking, albino mice and cell linings.