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1.
Chem Biodivers ; : e202401355, 2024 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-39099184

RESUMO

Melipona beecheii pot-pollen is a natural product that has barely been studied, unlike other hive products such as honey and propolis. Its application has been reported since ancient times in traditional Mayan medicine, and it is also a functional food with high nutritional value. In the present study, samples of ethanolic pot-pollen extracts from five locations in the Yucatán Peninsula were analyzed to determine their antibacterial and antioxidant properties. All the extracts showed activity against five medically important bacteria; Pseudomonas aeruginosa and Listeria monocytogenes were the most susceptible bacteria in all samples. The evaluated antioxidant activity was higher than that reported by other studies. Palmitic, linoleic, and linolenic fatty acids and their respective ethyl ethers were detected by Gas Chromatography-Mass Spectrometry (GC-MS) in all samples in different concentrations. Based on these results, pot-pollen extract from Mama, Yucatán exhibited the best biological activities (Minimum Inhibitory Concentrations (MICs) between 6 and 40 mg/mL, EC50 DPPH 28 µg/mL, EC50 RP 30 µg/mL), which could be related to a higher content of unsaturated fatty acids and their ethyl esters. The present study demonstrates that M. beecheii pot-pollen has therapeutic potential in addition to its benefits as a nutritional supplement.

2.
J Pediatr ; : 114220, 2024 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-39097265

RESUMO

OBJECTIVE: To assess whether beta-lactam extended or continuous beta-lactam infusions (EI/CI) improve clinical outcomes in children with proven or suspected bacterial infections. STUDY DESIGN: We included observational and interventional studies that compared beta-lactam EI or CI with standard infusions in children less than 18 years old, and reported on mortality, hospital or intensive care unit LOS, microbiological cure and/or clinical cure. Data sources included PubMed, Medline, EBM Reviews, EMBASE, and CINAHL and were searched from January 1, 1980, to November 3, 2023. Thirteen studies (2,945 patients) were included: 5 randomized control trials (RCTs), and 8 observational studies. Indications for antimicrobial therapies and clinical severity varied, ranging from cystic fibrosis exacerbation to critically ill children with bacteriemia. RESULTS: EI and CI were not associated with a reduction in mortality in RCTs (n = 1,464; RR 0.93, 95% CI 0.71, 1.21), but were in observational studies (n = 833; RR 0.43, 95% CI 0.19, 0.96). We found no difference in hospital length of stay. Results for clinical and microbiological cures were heterogeneous and reported as narrative review. The included studies were highly heterogeneous, limiting the strength of our findings. The lack of shared definitions for clinical and microbiological cure outcomes precluded analysis. CONCLUSIONS: EI and CI were not consistently associated with reduced mortality or LOS in children. Results were conflicting regarding clinical and microbiological cures. More well-designed studies targeting high-risk populations are necessary to determine the efficacy of these alternative dosing strategies.

3.
Drug Dev Ind Pharm ; : 1-13, 2024 Aug 06.
Artigo em Inglês | MEDLINE | ID: mdl-39093556

RESUMO

OBJECTIVE: Preparation and characterization of nano-emulsion formulations for Asparagus densiflorus aerial and root parts extracts. SIGNIFICANCE: Genus Asparagus is known for its antimicrobial and anticancer activities, however, freeze dried powder of aqueous - alcoholic extract prepared in this study, exhibited a limited water solubility, limiting its therapeutic application. Thus, encapsulation of its phytochemicals into nano-emulsion is proposed as a solution to improve water solubility, and facilitate its clinical translation. METHODS: the composition of extracts for both aerial and root parts of Asparagus densiflorus was identified by HPLC and LC-MS analysis. Nano-emulsion was prepared via homogenization where a mixture of Castor oil: phosphate buffered saline (10 mM, pH 7.4): Tween 80: PEG 600 in a ratio of 10: 5: 2.5: 2.5, respectively. Nano-emulsion formulations were characterized for particle size, polydispersity index (PDI), zeta potential, TEM, viscosity and pH. Then, the antibacterial and anticancer activities of nano-emulsion formulations versus their pure plant counterparts was assessed. RESULTS: The analysis of extracts identified several flavonoids, phenolics, and saponins which were reported to have antimicrobial and anticancer activities. Nano-emulsion formulations were monodispersed with droplet sizes ranging from 80.27 ± 2.05 to 111.16 ± 1.97 nm, and polydispersity index ≤0.3. Nano-emulsion formulations enhanced significantly the antibacterial (multidrug resistant bacteria causing skin and dental soft tissues infections) and anticancer (HuH7, HEPG2, H460 and HCT116) activities compared to their pure plant extract counterparts. CONCLUSION: Employing a nano-delivery system as a carrier for phytochemicals might be an effective strategy to enhance their pharmacological activity, overcome their limitations, and ultimately increase their potential for clinical applications.

4.
Colloids Surf B Biointerfaces ; 243: 114126, 2024 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-39106631

RESUMO

Presently, the non-biodegradable polypropylene (PP) patches frequently used for hernia repair can cause fibrous tissue growth and adhesions. This study created a Janus Patch with anti-adhesion and antimicrobial properties to improve hernia repair while promoting tissue repair. The biologically active 4arm-PLGA-BLPD was initially synthesized through the modification of 4arm-PLGA with lysine, followed by the fabrication of a Janus patch using a layer-by-layer electrostatic spinning technique. This patch consisted of three layers: a repair layer composed of 4arm-PLGA-BLPD/PCL fiber membrane, a mechanical layer of 4arm-PLGA/PCL fiber membrane, and an antimicrobial layer of EMO-4arm-PLGA/PCL fiber membrane loaded with Emodin (EMO). The results showed that Janus patch exhibited notable tensile strength and elongation at break, enabling it to offer enhanced mechanical reinforcement for abdominal wall defects. In addition, it slowly releases lysine for repair and inhibits bacterial growth with EMO. In vivo experiments demonstrated that the patch effectively induced neovascularization, reduced collagen ac-cumulation, and stabilized the expression of relevant proteins through the up-regulation of MMP1 and MMP9. This facilitated successful repair of the abdominal wall defect model and prevented adhesions. In summary, the Janus patch offers both practical application and theoretical insight for hernia repair.

5.
Eur J Med Chem ; 277: 116712, 2024 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-39106657

RESUMO

Quaternization of ruthenium complexes may be a promising strategy for the development of new antibiotics. In response to the increasing bacterial resistance, we integrated the quaternary amine structure into the design of ruthenium complexes and evaluated their antibacterial activity. All the ruthenium complexes showed good antibacterial activity against the tested Staphylococcus aureus (S. aureus). Ru-8 was the most effective antibacterial agent that displayed excellent antibacterial activity against S. aureus (MIC = 0.78-1.56 µg/mL). In vitro experiments showed that all nine ruthenium complexes had low hemolytic toxicity to rabbit erythrocytes. Notably, Ru-8 was found to disrupt bacterial cell membranes, alter their permeability, and induce ROS production in bacteria, all the above leading to the death of bacteria without inducing drug resistance. To further explore the antibacterial activity of Ru-8in vivo, we established a mouse skin wound infection model and a G. mellonella larvae infection model. Ru-8 exhibited significant antibacterial efficacy against S. aureus in vivo and low toxicity to mouse tissues. The Ru-8 showed low toxicity to Raw264.7 cells (mouse monocyte macrophage leukemia cells). This study indicates that the ruthenium complex ruthenium quaternary was a promising strategy for the development of new antibacterial agents.

6.
Microb Cell Fact ; 23(1): 220, 2024 Aug 06.
Artigo em Inglês | MEDLINE | ID: mdl-39107838

RESUMO

BACKGROUND: Biotechnology provides a cost-effective way to produce nanomaterials such as silver oxide nanoparticles (Ag2ONPs), which have emerged as versatile entities with diverse applications. This study investigated the ability of endophytic bacteria to biosynthesize Ag2ONPs. RESULTS: A novel endophytic bacterial strain, Neobacillus niacini AUMC-B524, was isolated from Lycium shawii Roem. & Schult leaves and used to synthesize Ag2ONPS extracellularly. Plackett-Burman design and response surface approach was carried out to optimize the biosynthesis of Ag2ONPs (Bio-Ag2ONPs). Comprehensive characterization techniques, including UV-vis spectral analysis, Fourier transform infrared spectroscopy, transmission electron microscopy, X-ray diffraction, dynamic light scattering analysis, Raman microscopy, and energy dispersive X-ray analysis, confirmed the precise composition of the Ag2ONPS. Bio-Ag2ONPs were effective against multidrug-resistant wound pathogens, with minimum inhibitory concentrations (1-25 µg mL-1). Notably, Bio-Ag2ONPs demonstrated no cytotoxic effects on human skin fibroblasts (HSF) in vitro, while effectively suppressing the proliferation of human epidermoid skin carcinoma (A-431) cells, inducing apoptosis and modulating the key apoptotic genes including Bcl-2 associated X protein (Bax), B-cell lymphoma 2 (Bcl-2), Caspase-3 (Cas-3), and guardian of the genome (P53). CONCLUSIONS: These findings highlight the therapeutic potential of Bio-Ag2ONPs synthesized by endophytic N. niacini AUMC-B524, underscoring their antibacterial efficacy, anticancer activity, and biocompatibility, paving the way for novel therapeutic strategies.


Assuntos
Antibacterianos , Nanopartículas Metálicas , Compostos de Prata , Humanos , Nanopartículas Metálicas/química , Compostos de Prata/farmacologia , Compostos de Prata/química , Antibacterianos/farmacologia , Antibacterianos/biossíntese , Testes de Sensibilidade Microbiana , Bacillaceae/metabolismo , Óxidos/farmacologia , Óxidos/química , Fibroblastos/efeitos dos fármacos , Apoptose/efeitos dos fármacos
7.
Front Microbiol ; 15: 1419917, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39091304

RESUMO

The prevalent life-threatening microbial and cancer diseases and lack of effective pharmaceutical therapies created the need for new molecules with antimicrobial and anticancer potential. Bee venom (BV) was collected from honeybee workers, and melittin (NM) was extracted from BV and analyzed by urea-polyacrylamide gel electrophoresis (urea-PAGE). The isolated melittin was hydrolyzed with alcalase into new bioactive peptides and evaluated for their antimicrobial and anticancer activity. Gel filtration chromatography fractionated melittin hydrolysate (HM) into three significant fractions (F1, F2, and F3), that were characterized by electrospray ionization mass spectrometry (ESI-MS) and evaluated for their antimicrobial, anti-biofilm, antitumor, and anti-migration activities. All the tested peptides showed antimicrobial and anti-biofilm activities against Gram-positive and Gram-negative bacteria. Melittin and its fractions significantly inhibited the proliferation of two types of cancer cells (Huh-7 and HCT 116). Yet, melittin and its fractions did not affect the viability of normal human lung Wi-38 cells. The IC50 and selectivity index data evidenced the superiority of melittin peptide fractions over intact melittin. Melittin enzymatic hydrolysate is a promising novel product with high potential as an antibacterial and anticancer agent.

8.
Int J Nanomedicine ; 19: 7673-7689, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39099793

RESUMO

Purpose: In this study, wound dressings were designed using zinc-modified marine collagen porous scaffold as host for wild bilberry (WB) leaves extract immobilized in functionalized mesoporous silica nanoparticles (MSN). These new composites were developed as an alternative to conventional wound dressings. In addition to the antibacterial activity of classic antibiotics, a polyphenolic extract could act as an antioxidant and/or an anti-inflammatory agent as well. Methods: Wild bilberry leaves extract was prepared by ultrasound-assisted extraction in ethanol and its properties were evaluated by UV-Vis spectroscopy (radical scavenging activity, total amount of polyphenols, flavonoids, anthocyanins, and condensed tannins). The extract components were identified by HPLC, and the antidiabetic properties of the extract were evaluated via α-glucosidase inhibitory activity. Spherical MSN were modified with propionic acid or proline moieties by post-synthesis method and used as carriers for the WB leaves extract. The textural and structural features of functionalized MSN were assessed by nitrogen adsorption/desorption isotherms, small-angle XRD, SEM, TEM, and FTIR spectroscopy. The composite porous scaffolds were prepared by freeze drying of the zinc-modified collagen suspension containing WB extract loaded silica nanoparticles. Results: The properties of the new composites demonstrated enhanced properties in terms of thermal stability of the zinc-collagen scaffold, without altering the protein conformation, and stimulation of NCTC fibroblasts mobility. The results of the scratch assay showed contributions of both zinc ions from collagen and the polyphenolic extract incorporated in functionalized silica in the wound healing process. The extract encapsulated in functionalized MSN proved enhanced biological activities compared to the extract alone: better inhibition of P. aeruginosa and S. aureus strains, higher biocompatibility on HaCaT keratinocytes, and anti-inflammatory potential demonstrated by reduced IL-1ß and TNF-α levels. Conclusion: The experimental data shows that the novel composites can be used for the development of effective wound dressings.


Assuntos
Bandagens , Colágeno , Nanopartículas , Extratos Vegetais , Folhas de Planta , Dióxido de Silício , Cicatrização , Zinco , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Dióxido de Silício/química , Dióxido de Silício/farmacologia , Colágeno/química , Colágeno/farmacologia , Zinco/química , Zinco/farmacologia , Nanopartículas/química , Cicatrização/efeitos dos fármacos , Antibacterianos/farmacologia , Antibacterianos/química , Humanos , Alicerces Teciduais/química , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Linhagem Celular , Porosidade , Fibroblastos/efeitos dos fármacos , Antioxidantes/farmacologia , Antioxidantes/química
9.
Bioact Mater ; 41: 30-45, 2024 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-39101029

RESUMO

Cataract patients look forwards to fewer postoperative complications and higher vision quality after surgery. However, the current intraocular lens (IOL) implanted after cataract surgery neither can adjust focal length in response to ciliary muscle contraction as natural lens nor have the ability to prevent postoperative complications. Herein, a thermosensitve Poloxamer based hybrid hydrogel with antibacterial anti-inflammatory and photothermal functional elements doping was designed and used as injectable, in situ curable, and adjustable IOL (FHTAB IOL). The FHTAB IOL was composed of thermosensitve triblock-polymer F127DA and a small amount of HAMA, combined with BP NS, TA, and Ag NPs. FHTAB IOL can be injected into the empty lens capsule after cataract surgery via an injectable thermos-gel under NIR illumination and then be rapidly cured to form a full-size IOL under short-time blue light irradiation. The designed injectable FHTAB IOL possesses high transparency and transmittance, with a refractive index similar to the natural lens and adjustable properties. It was stabilized as a refractive medium without any leakage in the eye. In addition, the TA and Ag NPs loaded in the FHTAB IOL displayed significant antibacterial and anti-inflammatory effects in vitro and vivo. This study presents a potentially effective new strategy for the development of multifunctional adjustable IOLs.

10.
Int J Biol Macromol ; : 134357, 2024 Aug 03.
Artigo em Inglês | MEDLINE | ID: mdl-39102916

RESUMO

Developing durable protective cotton fabrics (CF) against potential environmental dangers such as fire hazards and bacterial growth remains an imperative but tough challenge. In this study, flame retardant, antibacterial and hydrophobic CF were successfully prepared via two-step coating. The inner coating entailed polyelectrolyte complexes consisting of polyethyleneimine and ammonium polyphosphate with the goal of enhancing the flame retardancy of CF. Halloysite nanotubes (HNTs), a kind of tubular silicate mineral, were creatively modified and introduced to multifunctional coatings to improve flame retardant and antibacterial properties of CF. N-halamine modified HNTs (HNTs-EA-Cl) and polydimethylsiloxane were applied as the outer coating to endow CF with antibacterial and hydrophobic properties and further improve the flame retardancy of CF. After halloysite-based inorganic-organic hybrid coatings, the limiting oxygen index of the treated samples (PAHP-CF) was over 28 %, and the release of heat and smoke was significantly inhibited. PAHP-CF could inactivate 100 % E. coli and S. aureus within 2 h. More importantly, PAHP-CF showed excellent hydrophobicity with a water contact angle of 148° and exhibited great prevention of bacterial adhesion. PAHP-CF exhibited excellent washing durability undergoing 5 washing cycles. This study promotes the development of multifunctional coatings and offers a new way to manufacture multifunctional cotton fabrics.

11.
Int J Nanomedicine ; 19: 6427-6447, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38952675

RESUMO

Background: Implants are widely used in the field of orthopedics and dental sciences. Titanium (TI) and its alloys have become the most widely used implant materials, but implant-associated infection remains a common and serious complication after implant surgery. In addition, titanium exhibits biological inertness, which prevents implants and bone tissue from binding strongly and may cause implants to loosen and fall out. Therefore, preventing implant infection and improving their bone induction ability are important goals. Purpose: To study the antibacterial activity and bone induction ability of titanium-copper alloy implants coated with nanosilver/poly (lactic-co-glycolic acid) (NSPTICU) and provide a new approach for inhibiting implant-associated infection and promoting bone integration. Methods: We first examined the in vitro osteogenic ability of NSPTICU implants by studying the proliferation and differentiation of MC3T3-E1 cells. Furthermore, the ability of NSPTICU implants to induce osteogenic activity in SD rats was studied by micro-computed tomography (micro-CT), hematoxylin-eosin (HE) staining, masson staining, immunohistochemistry and van gieson (VG) staining. The antibacterial activity of NSPTICU in vitro was studied with gram-positive Staphylococcus aureus (Sa) and gram-negative Escherichia coli (E. coli) bacteria. Sa was used as the test bacterium, and the antibacterial ability of NSPTICU implanted in rats was studied by gross view specimen collection, bacterial colony counting, HE staining and Giemsa staining. Results: Alizarin red staining, alkaline phosphatase (ALP) staining, quantitative real-time polymerase chain reaction (qRT-PCR) and western blot analysis showed that NSPTICU promoted the osteogenic differentiation of MC3T3-E1 cells. The in vitro antimicrobial results showed that the NSPTICU implants exhibited better antibacterial properties. Animal experiments showed that NSPTICU can inhibit inflammation and promote the repair of bone defects. Conclusion: NSPTICU has excellent antibacterial and bone induction ability, and has broad application prospects in the treatment of bone defects related to orthopedics and dental sciences.


Assuntos
Antibacterianos , Materiais Revestidos Biocompatíveis , Escherichia coli , Osteogênese , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Ratos Sprague-Dawley , Staphylococcus aureus , Animais , Antibacterianos/farmacologia , Antibacterianos/química , Osteogênese/efeitos dos fármacos , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Camundongos , Staphylococcus aureus/efeitos dos fármacos , Materiais Revestidos Biocompatíveis/química , Materiais Revestidos Biocompatíveis/farmacologia , Escherichia coli/efeitos dos fármacos , Diferenciação Celular/efeitos dos fármacos , Próteses e Implantes , Ligas/farmacologia , Ligas/química , Ratos , Titânio/química , Titânio/farmacologia , Prata/química , Prata/farmacologia , Proliferação de Células/efeitos dos fármacos , Cobre/química , Cobre/farmacologia , Masculino , Microtomografia por Raio-X , Linhagem Celular , Nanopartículas Metálicas/química
12.
Artigo em Inglês | MEDLINE | ID: mdl-38954328

RESUMO

The purpose of this investigation was to evaluate the efficacy of ultrasonic subgingival curettage in conjunction with antibacterial polypeptide periodontal gel in the management of chronic periodontitis of moderate to severe severity. Methods included dividing 500 hospitalised patients with moderate to severe chronic periodontitis evenly between an observation group and a control group. Subgingival ultrasonic curettage was performed on the placebo group. The non-treatment group received ultrasonic subgingival curettage and a periodontal gel rinse containing polypeptides. Results were compared before and after treatment in terms of the periodontal index, inflammation in the gingival crevicular fluid, and occlusal and masticatory efficiency. Both groups saw significant reductions in occlusal duration and occlusal force balance after treatment compared to pre-treatment levels, though the observation group saw a more dramatic decrease in these indices than the control group with P ≤ 0.05. The treatment and observation groups both saw significant reductions in the masticatory efficiency standard deviation afterward, but the index in the observation group was significantly lower than that of the control group with P ≤ 0.05.The authors claim that moderate to severe chronic periodontitis can be effectively treated with a combination of polypeptide periodontal gel and ultrasonic subgingival curettage. Substantial decreases from pre-treatment levels for both groups, with the Observation Group's index being significantly lower than the Control Group's index (P ≤ 0.05). It is possible that this treatment will help reduce inflammation and improve your periodontal health. Biting strength and occlusion stability can both be improved at the same time to help patients improve their chewing efficiency. Therefore, this method can be used securely in real-world patient care settings.

13.
Foodborne Pathog Dis ; 2024 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-38957974

RESUMO

This study aimed to evaluate the effects of Euryale ferox Seed Shell Polyphenol Extract (EFSSPE) on a foodborne pathogenic bacterium. EFSSPE showed antimicrobial activity toward Salmonella Typhimurium CICC 22956; the minimum inhibitory concentration of EFSSPE was 1.25 mg/mL, the inhibition curve also reflected the inhibitory effect of EFSSPE on the growth of S. Typhimurium. Detection of alkaline phosphatase outside the cell revealed that EFSSPE treatment damaged the cell wall integrity of S. Typhimurium. EFSSPE also altered the membrane integrity, thereby causing leaching of 260-nm-absorbing material (bacterial proteins and DNA). Moreover, the activities of succinate dehydrogenase and malate dehydrogenase were inhibited by EFSSPE. The hydrophobicity and clustering ability of cells were affected by EFSSPE. Scanning electron microscopy showed that EFSSPE treatment damaged the morphology of the tested bacteria. These results indicate that EFSSPE can destroy the cell wall integrity and alter the permeability of the cell membrane of S. Typhimurium.

14.
Front Nutr ; 11: 1405708, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38946786

RESUMO

The study highlighted the potential of sesame seed coat (SSC), typically discarded during sesame paste processing, as a valuable resource for valorization through extracting bioactive compounds. It examined the phenolic composition and antioxidant activity of SSC, and evaluated its antibacterial properties against foodborne pathogens such as Listeria monocytogenes, Escherichia coli O157:H7, and Salmonella Typhimurium. Additionally, SSC underwent nanoemulsion coating, analyzed using dynamic light scattering and scanning electron microscopy, to enhance its application as a natural preservative. The research specifically focused on incorporating SSC nanoemulsion into milk to determine its effectiveness as a preservative. SSC demonstrated considerable antioxidant activity and phenolic content, with catechin identified as the predominant polyphenol. GC-MS analysis revealed seven major compounds, led by oleic acid. Notably, SSC effectively inhibited L. monocytogenes in broth at 100 mg/ml. The application of SSC and its nanoemulsion resulted in changes to bacterial morphology and a significant reduction in bacterial counts in milk, highlighting its potential as an effective natural antibacterial agent. The findings of this study highlight the potential use of SSC as a valuable by-product in the food industry, with significant implications for food preservation.

15.
Food Chem X ; 23: 101510, 2024 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-38947341

RESUMO

We prepared tea tree essential oil microcapsules, and the microcapsules and pullulan were coated on kraft paper to prepare an antibacterial paper. The antibacterial activity, structural characterization, and thermal stability of the prepared microcapsules and packaging paper were then tested. We found that the retention rate of microcapsules reached 87.1% after a 70 min of high-temperature treatment. The minimum inhibitory concentrations of microcapsules to S. aureus and E. coli were 112 mg/mL and 224 mg/mL, and the bacteriostatic zones of the packaging paper to E. coli and S. aureus were 17.49 mm and 22.75 mm, respectively. The prepared microcapsules were irregular. The paper coating was formed via hydrogen bonding, which filled the pores of paper fibers. When compared with the base paper, the roughness of the paper was reduced to 7.16 nm (Rq) and 5.61 nm (Ra), and no thermal decomposition occurred at <288 °C, which together implies a good application prospect.

16.
Heliyon ; 10(11): e32257, 2024 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-38947436

RESUMO

New 3-furan-1-thiophene-based chalcones were synthesized, characterized and pharmacologically evaluated as antibacterial and anticancer agents against two bacterial species; Gram-positive (Streptococcus pyogenes) and Gram-negative (Pseudomonas aeruginosa). All tested final compounds were active against the two bacterial species; S. pyogenes and P . aeruginosa. Especially compound AM4 showed large inhibition zone (27.13 and 23.30 mm), respectively. Using the DPPH assay, the new chalcones were evaluated for their free radical scavenging activity and found to reach up to 90 %, accomplished at a test concentration of 200 µg/mL. Furthermore, the chalcone derivatives were investigated against two breast cell lines; MCF-7 (cancerous) and MCF-10A (non-cancerous). Compound AM4 showed potent anticancer activity (IC50 = 19.354 µg/mL) in comparison to the other tested chalcone derivatives. In silico study was achieved using the PyRx AutoDock Vina software (0.8) to study the interaction types between the new hits and the binding sites of targeted proteins; glucosamine-6-phosphate synthase and tubulin, the target for antibacterial and anticancer drugs, respectively. Based on the molecular docking results the tested chalcones bind to the active pocket of the respective proteins, which support the in vitro results. In conclusion, 3-furan-1-thiophene-based chalcones could serve as new hits in the discovery of novel anticancer and/or antibacterial drugs.

17.
PeerJ ; 12: e17588, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38948224

RESUMO

In the present study, zinc oxide nanoparticles (ZnO-NPs) were synthesized using neem leaf aqueous extracts and characterized using transmission electron microscopy (TEM), ultraviolet visible spectroscopy (UV-Vis), and dynamic light scattering (DLS). Then compare its efficacy as anticancer and antibacterial agents with chemically synthesized ZnO-NPs and the neem leaf extract used for the green synthesis of ZnO-NPs. The TEM, UV-vis, and particle size confirmed that the developed ZnO-NPs are nanoscale. The chemically and greenly synthesized ZnO-NPs showed their optical absorbance at 328 nm and 380 nm, respectively, and were observed as spherical particles with a size of about 85 nm and 62.5 nm, respectively. HPLC and GC-MS were utilized to identify the bioactive components in the neem leaf aqueous extract employed for the eco-friendly production of ZnO-NPs. The HPLC analysis revealed that the aqueous extract of neem leaf contains 19 phenolic component fractions. The GC-MS analysis revealed the existence of 21 bioactive compounds. The antiproliferative effect of green ZnO-NPs was observed at different concentrations (31.25 µg/mL-1000 µg/mL) on Hct 116 and A 549 cancer cells, with an IC50 value of 111 µg/mL for A 549 and 118 µg/mL for Hct 116. On the other hand, the antibacterial activity against gram-positive and gram-negative bacteria was estimated. The antibacterial result showed that the MIC of green synthesized ZnO-NPs against gram-positive and gram-negative bacteria were 5, and 1 µg/mL. Hence, they could be utilized as effective antibacterial and antiproliferative agents.


Assuntos
Antibacterianos , Antineoplásicos , Extratos Vegetais , Folhas de Planta , Óxido de Zinco , Óxido de Zinco/farmacologia , Óxido de Zinco/química , Antibacterianos/farmacologia , Antibacterianos/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Humanos , Folhas de Planta/química , Antineoplásicos/farmacologia , Antineoplásicos/química , Azadirachta/química , Nanopartículas Metálicas/química , Testes de Sensibilidade Microbiana , Química Verde/métodos , Tamanho da Partícula , Linhagem Celular Tumoral
18.
Front Vet Sci ; 11: 1408376, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38948675

RESUMO

Streptococcus agalactiae (S.agalactiae), also known as group B Streptococcus (GBS), is a highly infectious pathogen. Prolonged antibiotic usage leads to significant issues of antibiotic residue and resistance. Chelerythrine (CHE) is a naturally occurring benzophenidine alkaloid and chelerythrine chloride (CHEC) is its hydrochloride form with diverse biological and pharmacological activities. However, the antibacterial mechanism of CHEC against GBS remains unclear. Thus, this study aims to investigate the in vitro antibacterial activity of CHEC on GBS and elucidate its underlying mechanism. The antibacterial effect of CHEC on GBS was assessed using inhibitory zone, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) assays, as well as by constructing a time-kill curve. The antibacterial mechanism of CHEC was investigated through techniques such as scanning electron microscopy (SEM) and transmission electron microscopy (TEM), measurement of alkaline phosphatase (AKP) activity, determination of Na+ K+, Ca2+ Mg2+-adenosine triphosphate (ATP) activity, observation of membrane permeability, and analysis of intracellular reactive oxygen species (ROS) and mRNA expression levels of key virulence genes. The results demonstrated that the inhibition zone diameters of CHEC against GBS were 14.32 mm, 12.67 mm, and 10.76 mm at concentrations of 2 mg/mL, 1 mg/mL, and 0.5 mg/mL, respectively. The MIC and MBC values were determined as 256 µg/mL and 512 µg/mL correspondingly. In the time-kill curve, 8 × MIC, 4 × MIC and 2 × MIC CHEC could completely kill GBS within 24 h. SEM and TEM analyses revealed significant morphological alterations in GBS cells treated with CHEC including shrinkage, collapse, and leakage of cellular fluids. Furthermore, the antibacterial mechanism underlying CHEC's efficacy against GBS was attributed to its disruption of cell wall integrity as well as membrane permeability resulting in extracellular release of intracellular ATP, AKP, Na+ K+, Ca2+ Mg2+. Additionally CHEC could increase the ROS production leading to oxidative damage and downregulating mRNA expression levels of key virulence genes in GBS cells. In conclusion, CHEC holds potential as an antimicrobial agent against GBS and further investigations are necessary to elucidate additional molecular mechanisms.

19.
Heliyon ; 10(11): e32419, 2024 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-38961897

RESUMO

Silver nanoparticles (Ag NPs) play a pivotal role in the current research landscape due to their extensive applications in engineering, biotechnology, and industry. The aim is to use fig (Ficus hispida Linn. f.) extract (FE) for eco-friendly Ag NPs synthesis, followed by detailed characterization, antibacterial testing, and investigation of bioelectricity generation. This study focuses on the crystallographic features and nanostructures of Ag NPs synthesized from FE. Locally sourced fig was boiled in deionized water, cooled, and doubly filtered. A color change in 45 mL 0.005 M AgNO3 and 5 mL FE after 40 min confirmed the bio-reduction of silver ions to Ag NPs. Acting as a reducing and capping agent, the fig extract ensures a green and sustainable process. Various analyses, including UV-vis absorption spectrophotometry (UV), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), Field emission scanning electron microscopy (FESEM), Energy dispersive X-ray spectroscopy (EDX) and Transmission electron microscopy (TEM) were employed to characterize the synthesized nanoparticles, and Gas chromatography-mass spectrometry (GC-MS) analysis of the fig extract revealed the presence of eleven chemicals. Notably, the Ag NPs exhibited a surface plasmon resonance (SPR) band at 418 nm, confirmed by UV analysis, while FTIR and XRD results highlighted the presence of active functional groups in FE and the crystalline nature of Ag NPs respectively. With an average particle size of 44.57 nm determined by FESEM and a crystalline size of 35.87 nm determined by XRD, the nanoparticles showed strong antibacterial activities against Staphylococcus epidermidis and Escherichia coli. Most importantly, fig fruit extract has been used as the bio-electrolyte solution to generate electricity for the first time in this report. The findings of this report can be the headway of nano-biotechnology in medicinal and device applications.

20.
Heliyon ; 10(11): e32599, 2024 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-38961917

RESUMO

Present scientific evidences about the biological activity and potential medical application of extracts derived from Marrubium friwaldskyanum Boiss. are limited. Therefore, our study was undertaken to define several main characteristics in this regard - in vitro cytotoxicity and antitumor properties, antibacterial activity and immunomodulatory potential. Extracts were obtained from different aerial parts of Marrubium friwaldskyanum - stems, leaves and flowers. The in vitro cytotoxicity and antitumor activity of the samples were evaluated by tetrazolium salt reduction tests and Neutral red uptake assays using four human cell lines (a normal fibroblastic and three adenocarcinoma cell lines/A549, HeLa, HT-29/) and by experiments with HT-29 tumor spheroids. Antibacterial activity toward Gram-negative (Escherichia coli) and Gram-positive (Bacillus cereus) species was assessed based on estimation of minimal inhibitory and minimal bactericidal concentrations as well as longitudinal studies on bacterial viability. Ex vivo assays with normal leukocytes were performed to define potential immunomodulatory activity of the extracts. Our results demonstrated selective antitumor activity of the extracts directed against colon adenocarcinoma HT-29 cells and cervical adenocarcinoma HeLa cell line. Metabolic activity of A549 lung adenocarcinoma cells was affected only by the sample derived from flowers. M. friwaldskyanum leaf and flower extracts showed the highest activity, which included reduction of HT-29 tumor spheroid growth and viability. The studied samples exhibited antibacterial activity against both bacterial species tested. Treatment with M. friwaldskyanum extracts affected specific leukocyte populations (HLA+, CD19+, CD11b+, CD25+ cells). These results demonstrate for the first time complex biological effects of extracts derived from M. friwaldskyanum and their potential to serve as a source of valuable compounds for the pharmaceutical industry.

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