Excellent Antibacterial Activity Research Articles

A bi-functional nanofibrous composite membrane for wound healing applications.

Various wound dressings have been developed so far for wound healing, but most of them are ineffective in properly reestablishing the skin's structure, which increases infection risks and dehydration. Electrospun membranes are particularly interesting for wound dressing applications because they mimic the extracellular matrix of healthy skin. In this study, a potential wound healing platform capable of inducing synergistic antibacterial and antioxidation activities was developed by incorporating bio-active rosmarinic acid-hydroxyapatite hybrid (HAP-RA) with different contents (0.5, 1, and 1.5 wt.%) into the electrospun polyamide 6 (PA6) nanofibers. Then, polyethylene glycol (PEG) was introduced to the nanofibrous composite to improve the biocompatibility and biodegradability of the dressing. The results indicated that the hydrophilicity, water uptake, biodegradability, and mechanical properties of the obtained PA6/PEG/HAP-RA nanofibrous composite enhanced at 1 wt.% of HAP-RA. The nanofibrous composite had excellent antibacterial activity. The antioxidation potential of the samples was assessed in vitro. The MTT assay performed on the L929 cell line confirmed the positive effects of the nanofibrous scaffold on cell viability and proliferation. According to the results, the PA6/PEG/HAP-RA nanofibrous composite showed the desirable physiochemical and biological properties besides antibacterial and antioxidative capabilities, making it a promising candidate for further studies in wound healing applications.

Green Synthesis and Characterization of Silver Anchored ZnO Nanoparticle as the Antimicrobial Reinforcement for Polylactide (PLA) Films

AbstractThe aqueous extract of endophytic fungi (Periconia sp.) was effectively used as a reducing agent to anchor Ag nanoparticles on the ZnO surface. The XRD, UV‐Vis, SEM‐EDX and TEM analyses were performed to ensure the formation of AgNP@ZnO architecture. TEM analysis confirmed that the 4‐20 nm sized Ag nanoparticles were anchored evenly on the surface of ZnO with 16‐78 nm in size. The antimicrobial study showed the superior performance of AgNP@ZnO functional nanoparticles than the pristine ZnO against pathogenic bacteria Staphylococcus aureus (gram‐positive) and Escherichia coli (gram‐negative). Hence, AgNP@ZnO functional particles were effectively explored as antimicrobial reinforcement for fabricating composite films using polylactic acid (PLA) as a matrix. The obtained nanocomposite films showed excellent antibacterial activity, which increases with increasing AgNP@ZnO loading.This article is protected by copyright. All rights reserved.

New isoxazolidine derivatives: Synthesis, spectroscopic analysis, X-ray, DFT calculation, biological activity studies

The isoxazolidine skeleton is an important component of biologically active natural products, and many compounds containing isoxazolidine ring exhibit excellent antibacterial and anticancer activities. Based on the variously biological activity of isoxazolidines, a new series of isoxazolidine derivatives were designed and synthesized. All the structure of target compounds was characterized by NMR and HRMS. Especially, compound 8a ((Z)-2-methyl-4-(phenoxymethylene)-3-phenylisoxazolidine) was prepared for single crystal X-ray diffraction and FT-IR. Density functional theory (DFT) calculations were also performed on compound 8a at the B3LYP/6–311 level. In addition, after evaluation with MTT method of compounds 8a-8k against A549 cells, it was found that some compounds performed well antitumor activities.

Antimicrobial mechanism of linalool against Vibrio parahaemolyticus and its application in black tiger shrimp (Penaeus monodon)

Vibrio parahaemolyticus (V. parahaemolyticus) is a seafood-derived pathogen that poses a serious threat to seafood and human health. Biofilm production is a necessary process for V. parahaemolyticus to colonize the host and release virulence factors. Therefore, preventing biofilm formation or eliminating biofilm cells is an effective strategy to combat V. parahaemolyticus infection. Linalool is a food additive of natural origin with excellent antibacterial activity. In this study, we investigated the antimicrobial and anti-biofilm effects of linalool against V. parahaemolyticus and elucidated its mechanism through metabolomics analysis. The results showed that the minimum inhibitory concentration (MIC) of linalool against V. parahaemolyticus is 1.7 mg/mL. The treatment with linalool disrupted the integrity of the cell membrane, resulting in the leakage of nucleic acids and proteins, impaired motility, and reduced release of extracellular polysaccharide (EPS). The metabolomics results revealed that linalool perturbed the metabolic pathways of amino acids and nucleic acids in V. parahaemolyticus, thereby impeding biofilm production. Moreover, linalool significantly inactivated V. parahaemolyticus in black tiger shrimp. These findings have practical implications for the utilization of linalool in controlling bacterial contamination in seafood and enhancing food safety.

Covalently grafting polycation to bacterial cellulose for antibacterial and anti-cell adhesive wound dressings

Hydrogel-based wound dressings are becoming increasingly important for wound healing. Bacterial cellulose (BC) has been commonly used as wound dressings due to its good in vitro and in vivo biocompatibility. However, pure BC does not possess antibacterial properties. In this regard, polycation gel was grafted onto the BC using a surface-initiated activator regenerated by electron transfer atom transfer radical polymerization (SI-ARGET ATRP) with subsequent quaternization for antibacterial wound dressing. Dimethylethyl methacrylate (DMAEMA) was successfully polymerized on the BC surface which was confirmed by Fourier transform infrared spectroscopy and elemental analysis. The morphology structure, specific surface area, pore size, and mechanical properties were also characterized. The quaternized PDMAEMA grafted on the BC endowed it with excellent antibacterial activity against E. coli (Gram-negative) and S. aureus (Gram-positive) with a killing rate of 89.2 % and 93.4 %, respectively. The number of cells was significantly reduced on QPD/BC hydrogel, demonstrating its good anti-adhesion ability. In vitro cellular evaluation revealed that the antibacterial wound dressing exhibited good biocompatibility. Overall, this study provides a feasible method to develop antibacterial and anti-cell adhesive hydrogel, which has a promising potential for wound healing.

Construction of versatile fibroin/nanozyme hybrid microneedles with controllable phototherapeutic sterilization property against periodontitis

Periodontitis is a highly prevalent disease that affects up to 90% of the worldwide population. The highly dynamic oral environment, tissue-teeth “pocket” structure, and antimicrobial resistance pose challenges to periodontitis local treatments, which urgently need to be upgraded with advanced biomaterials and novel therapeutics. Herein, a new treatment strategy for periodontitis is proposed by synergistic nanozyme catalyzed phototherapeutic/chemodynamic sterilization and microneedles (MNs) in situ delivery platform. A biodegradable versatile photothermal microneedles (MN-SF/CuS) patch was constructed by the in situ growth of monodispersed ultrasmall CuS nanozyme on silk-fibroin (SF) biomolecule and then hybridization in methacrylated hyaluronic acid (HAMA). The synthetic SF/CuS nanozyme endows microneedles with amplifies phototherapeutic/chemodynamic sterilization, excellent mechanical properties, and promotes periodontal tissue regeneration. The constructed MN-SF/CuS can be conveniently and minimally invasively inserted deeply into periodontal tissue without being affected by saliva, where it delivers thermal action, reactive oxygen species, and copper to the specified depth, achieving rapid sterilization and inhibition of bacterial growth. Meanwhile, MN-SF/CuS achieves on-demand phototherapy effect without damaging surrounding normal tissues. A preclinical large animal model confirmed that the MN-SF/CuS provided excellent irreversible antibacterial activity and promoted tissue regeneration, substantially improving the tolerance and compliance of periodontal treatment.

Bio-based phytic acid/amino acid complex coating for antimicrobial and flame-retardant cotton fabrics

Here, a novel multifunctional coating containing bio-based phytic acid (PA), L-glutamic acid (L-Glu), and trimesoyl chloride (TMC) is constructed by a simple soaking strategy, giving cotton fabrics excellent flame retardancy, washability, and antibacterial properties. The coating layer on the cotton surface was prepared via the electrostatic and hydrogen bonding between PA and L-Glu, accompanied by the interface polymerization between PA, L-Glu, and TMC. Among them, the limiting oxygen index value of the treated cotton fabrics (C2 and C2-TMC) was as high as 40 %. During the vertical flammability test, both C2 and C2-TMC cotton showed self-extinguished behavior with a short damaged length (≤50 mm). Remarkably, the LOI of C2-TMC sustained a high value (30 %) even after 300 laundering cycles, maintaining its self-extinguishing behavior in the vertical combustion test. Additionally, in the cone calorimetry test, peak heat release rate and total heat release of treated cotton were lower than control cotton. Surprisingly, after 30 or 60 laundering cycles, the C2-TMC cotton exhibited excellent antibacterial activity against Escherichia coli, Staphylococcus aureus, and Candida albicans due to the continuous exposure of PA and L-Glu. Moreover, the coating layer on the cotton surface had little impact on the mechanical properties and feel of the fabric.

Bioactive compounds, Antioxidant and Antimicrobial Attributes of Cordia Sinensis Lam

The aim of this study is to discover the efficacy of various parts of Cordia sinensis plant against some particular pathogens that are recognized to cause diseases and to check antioxidant and bioactive compounds from different parts of plant C. sinensis. Plant extracts were examined by quantification of phytochemical compounds and antimicrobial activity. Phytochemicals and several secondary metabolites were quantified and also qualitatively analyzed in C. sinensis extracts such as phenolic compounds, flavonoids, alkaloids, tannins, steroids, glycosides, and saponins. Similarly, biochemical primary metabolites like protein, total sugar, and reducing sugar were also estimated in different parts of C. sinensis and these results correlated with antimicrobial activity. This study reveals that acetone extracts of stems, leaves, and roots of the C. sinensis showed excellent antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Klebsiella pneumonia and also against fungal species Aspergillus niger, Candida albicans, and Penicillium notatum.

Quaternary branched polyethylenimine‐based nanocomposite for removal of NO3− ions from aqueous solutions

AbstractThis study synthesized a nanocomposite based on quaternary branched polyethyleneimine containing sodium alginate and graphene oxide and characterized by FE‐SEM, EDX‐MAP, XRD, FT‐IR, and TGA and used as an efficient sorbent for the removal of nitrate ions. The maximum ion exchange in optimized conditions was discovered to be 75%. The experimental studies showed that nitrate removal follows the pseudo‐first‐order model due to more consonance. Also, Weber–Morris and Boyd models suggested that the nitrate ions adsorption on the surface of nanocomposite is not controlled only by the intraparticle diffusion step. Moreover, Langmuir, Redlich–Peterson, and Hill models exhibited high regression coefficients of 0.991, 0.993, and 0.992, respectively. Thermodynamic studies confirmed the adsorption system was spontaneous and exothermic. Recovery assay showed that more than 98% of the nitrate ion exchanged by the nanocomposite was regenerated and nanocomposite could be reused seven cycles without efficacy reducing significantly. The nanocomposite showed excellent antibacterial activity against Staphylococcus aureus and Escherichia coli cells, with minimum inhibitory concentrations of 62.5 and 125 μg mL−1, and zone of growth inhibition of 17.5 ± 0.5 and 10.5 ± 0.5 mm, respectively. The results represented that the introduced nanocomposite is a useful material for the removal of nitrate ions from aqueous solution and has antibacterial properties.

Layer-by-layer self-assembly of PLL/CPP-ACP multilayer on SLA titanium surface: Enhancing osseointegration and antibacterial activity in vitro and in vivo

Implants are expected to possess both excellent osteointegration and antibacterial activity because poor osseointegration and infection are two major causes of titanium implant failure. In this study, we constructed layer-by-layer self-assembly films consisting of anionic casein phosphopeptides-amorphous calcium phosphate (CPP-ACP) and cationic poly (L-lysine) (PLL) on sandblasted and acid etched (SLA) titanium surfaces and evaluated their osseointegration and antibacterial performance in vitro and in vivo. The surface properties were examined, including microstructure, elemental composition, wettability, and Ca2+ ion release. The impact the surfaces had on the adhesion, proliferation and differentiation abilities of MC3T3-E1 cells were investigated, as well as the material’s antibacterial performance after exposure to the oral microorganisms such as Porphyromonas gingivalis (P. g) and Actinobacillus actinomycetemcomitans (A. a). For the in vivo studies, SLA and Ti (PLL/CA-3.0)10 implants were inserted into the extraction socket immediately after extracting the rabbit mandibular anterior teeth with or without exposure to mixed bacteria solution (P. g & A. a). Three rabbits in each group were sacrificed to collect samples at 2, 4, and 6 weeks of post-implantation, respectively. Radiographic and histomorphometry examinations were performed to evaluate the implant osseointegration. The modified titanium surfaces were successfully prepared and appeared as a compact nano-structure with high hydrophilicity. In particular, the Ti (PLL/CA-3.0)10 surface was able to continuously release Ca2+ ions. From the in vitro and in vivo studies, the modified titanium surfaces expressed enhanced osteogenic and antibacterial properties. Hence, the PLL/CPP-ACP multilayer coating on titanium surfaces was constructed via a layer-by-layer self-assembly technology, possibly improving the biofunctionalization of Ti-based dental implants.

High-compatibility properties of Aronia melanocarpa extracts cross-linked chitosan/polyvinyl alcohol composite film for intelligent food packaging

Although the active and intelligent properties of rich in anthocyanin extracts added to films have been extensively studied, there remains a sparsity of research pertaining to the miscibility of blended films. This work focused on the miscibility of the chitosan/polyvinyl alcohol (CP) film caused by the addition of Aronia melanocarpa extracts (AME), which are rich anthocyanins and phenolic acids, and its effect on physicochemical and functional properties. AME facilitated the amidation reaction and ionic interaction of chitosan in CP films, leading to loss of the crystallinity degree of chitosan. Furthermore, the crystal disruption promoted the formation of hydrogen bonds with polyvinyl alcohol (PVA) with the promoted miscibility. CP film incorporated with 8 % AME possessed the highest tensile strength (26.79 MPa), and elongation at break (66.38 %) as well as excellent ultraviolet–visible (UV–vis) light barrier property, water vapor barrier properties, due to its high miscibility degree. Moreover, this film also showed excellent antioxidant, antibacterial activity, and pH response function, which could be used to monitor the storage of highly perishable shrimp. Hence, the AME provided extra functionality and improved miscibility between chitosan and PVA, which showed great potential for the preparation of high-performance bioactive-fortified and intelligent food packaging films.

The antibacterial and hemostatic curdlan hydrogel–loading epigallocatechin gallate for facilitating the infected wound healing

The infected wounds pose one of the major threats to human health today. To address this issue, it is necessary to develop innovative wound dressings with superior antibacterial activity and other properties. Due to its potent antibacterial, antioxidant, and immune-boosting properties, epigallocatechin gallate (EGCG) has been widely utilized. In this study, a multifunctional curdlan hydrogel loading EGCG (Cur-EGCGH3) was designed. Cur-EGCGH3 exhibited excellent physicochemical properties, good biocompatibility, hemostatic, antibacterial, and antioxidant activities. Also, ELISA data showed that Cur-EGCGH3 stimulated macrophages to secrete pro-inflammatory and pro-regenerative cytokines. Cell scratch results indicated that Cur-EGCGH3 promoted the migration of NIH3T3 and HUVECs. In vivo experiments confirmed that Cur-EGCGH3 could inhibit bacterial infection of the infected wounds, accelerate hemostasis, and promote epithelial regeneration and collagen deposition. These results demonstrated that Cur-EGCGH3 holds promise for promoting healing of the infected wounds.

Breath moisture-induced electroactive nanofibrous membrane for efficient antibacterial and antiviral air filtration

The high humidity environment created by human breath can easily lead to charge loss in the mask's filter and weaken the mask's filtration effect on aerosols containing bacteria and viruses. Therefore, in this study, a breath moisture-induced electroactive nanofibrous membrane was prepared by incorporating Cu/Zn nanoparticles into cellulose acetate/poly (vinyl butyral) fibers. Adjacent Cu/Zn nanoparticles can form galvanic couples that can be activated by human breath to undergo redox discharge reactions, thus imparting moisture-induced electroactivity to nanofibrous membrane. Based on the moisture-induced electroactivity, nanofibrous membrane demonstrated antibacterial rates of 98.32 % against Escherichia coli (E. coli) and 99.06 % against Staphylococcus aureus (S. aureus). Moreover, moisture-induced electroactive nanofibrous membrane significantly reduced the titer of Enterovirus 71 (EV71) transmitted through the respiratory tract within 5 min. The excellent antibacterial and antiviral performance of electroactive nanofibrous membrane can be attributed to the synergistic effect of Cu/Zn’s electrical stimulation (ES) interference on the electrodynamics of bacteria and viruses, the generated reactive oxygen species (ROS), and the released metal ions. Benefiting from the increased surface potential from Cu/Zn galvanic couples, moisture-induced electroactive nanofibrous membrane exhibited a filtration efficiency of 99.61 % for PM0.3 particles while maintaining a low-pressure drop (78 Pa). Meanwhile, electroactive nanofibrous membrane showed excellent wear comfort and non-cytotoxicity. In summary, this moisture-induced electroactive nanofibrous membrane maintains high filtration performance and exhibits excellent antibacterial and antiviral activities, shedding some light on developing novel efficient air filters.

Tamarindus indica seed polysaccharide-copper nanocomposite: An innovative solution for green environment and antimicrobial studies

The purpose of this study was to synthesize ecofriendly nano-composite in which agricultural waste (seeds of Tamarindus indica) was used to synthesize tamarind seed polysaccharides (TSP) and its composite with copper nanoparticles (Cu-NPs) for the purpose of green and clean environment as well as reduction of green-house gases. Confirmation of extracted TSP, synthesized nanocomposite was carried out using FTIR, SEM, PXRD and EDX techniques. In FTIR analysis TSP gives a strong broad peak at 3331 cm−1 due to –OH group and in case of composite its intensity is reduced which might be due to the interactions between –OH and Cu+2 ions. SEM analysis gives that TSP have irregular and rough surface while Cu-NPs exhibited spherical morphology and composite showed clustering of spherical shape to rough surface. EDX analysis quantitatively represented copper having atomic ratio 0.57 % which confirms the synthesis of composite. Furthermore, synthesized composite demonstrated excellent antibacterial activity against gram-positive (S.aureus) and gram-negative bacteria (E.coli) even greater than standard medicine (ciprofloxacin). From this study it was revealed that agriculture waste can be utilized to make environment green as well as synthesized composite from agricultural waste seed also displayed excellent antimicrobial activities which directs that they can be utilized in medical field. This study aims to assess the antimicrobial properties of the nanocomposite, aiming to contribute to the development of effective antimicrobial agents. Through these objectives, the research seeks to bridge the gap between green technology and antimicrobial efficacy, offering a promising avenue for both environmental conservation and healthcare advancements.

Versatile Aggregation Induced Emissive Molecular Probes Incorporating different Donor/Acceptor groups for Tunable Multiple Color Fluorescence

Excited state intramolecular proton transfer (ESIPT) and aggregation induced emission active multicolour fluorescent probes for bioimaging applications has grown popularly in recent years. Herein, we report a series of different donor/acceptor units (Cl, NO2 and O-CH3) bearing anthracene-salicylaldehyde based fluorescent probes and their antibacterial activity and fluorescence imaging of E. Coli bacteria and zebrafish embryos. All the compounds (ASA1, ASA2, ASA3 and ASA4) synthesized via facile one pot condensation reaction of anthracene hydrazide with Salicylaldehyde, 5-Chlorosalicylaldehyde, 5-Nitrosalicylaldehyde, 5-methoxysalicylaldehyde and characterized using all the possible spectroscopic techniques. The noteworthy tuneable emission wavelength shifts from 471 nm to 625 nm and ESIPT characteristics of the compounds were demonstrated through photophysical experiments and single crystal X-ray diffraction analysis. All the experimental results were completely analysed theoretically on the ground as well as the excited state using density functional theory (DFT) and time dependant density functional theory (TD-DFT) calculations. Compounds ASA1-ASA4 showed fascinating different colour fluorescent (Green, Yellow and Orange) aggregation induced emission features in the THF-H2O mixture. AIE characteristics of ASA1, ASA2, ASA3 and ASA4 were recognized using absorption, emission, fluorescence quantum yield (φ), DLS and SEM analysis. ASA1, ASA2, ASA3 and ASA4 showed excellent antibacterial activity and ROS generation against E. Coli bacteria. Further, owing to the multicolour fluorescent property of the compounds successfully applied for fluorescent imaging in E. Coli bacteria and live zebrafish embryos.

Antibacterial oxygen-sulfur terminal polymers from a facile initiator-strategy

Bacterial infection has become a long-term concern that seriously threatens human health. However, the application of conventional antibacterial materials in antibacterial treatment and infection prevention has been severely hindered due to their limitations such as complex synthesis, high cost, and high cytotoxicity. Therefore, developing a facile and cost-effective route to prepare high-performance antibacterial materials is of urgent need and significant importance. In this work, we for the first time reported that oxygen-sulfur terminal bonds possess excellent antibacterial properties, and the oxygen-sulfur terminal polymer (OSTP) can effectively kill bacteria when contacting and interacting with the bacteria. A universal and simple initiator strategy has been developed to fabricate OSTPs through a facile solution polymerization process. Via this approach, the PEGDA-APS OSTPs exhibited superfast and superior antibacterial properties against both Gram-positive and Gram-negative bacteria while maintaining good hemocompatibility and cytocompatibility, outperforming many common antibacterial agents that usually require several hours of bacterial extinction. Moreover, it is demonstrated that OSTPs exhibited excellent antibacterial activity in a wide range of application situations, including textile, medicine, washing, food, and coating, as well as antibacterial hydrogels.

A Self-Transformed N-chlorinated ε-Polylysine coating endows titanium implants with programmed integration of robust antibacterial and Pro-Osteogenic abilities

Implant-associated infection and poor osseointegration are the main causes of orthopedic implantation failure. For a long-term successful implantation, simultaneously introducing prevention of infection and promotion of osteogenesis into implants is highly desired but remains a grand challenge. Inspired by the human immune mechanism of tissue repair under bacterial infection, we propose a self-transformed strategy for the modification of titanium with porous N-chlorinated ε-polylysine coating (Ti-PL-NCl) through pore-making, surface grafting and chlorination. The as-prepared Ti-PL-NCl exhibits an excellent antibacterial activity against S. aureus and E. coli in the presence of N-chloramine in the early stage, with an antibacterial rate as high as 95.8% and 99.4%, respectively. With the consumption of oxidative chlorine, the N─Cl groups of Ti-PL-NCl are transformed into N─H groups with moderate antibacterial yet strong pro-osteogenic abilities. The self-transformed N-chlorinated ε-polylysine coating enables Ti-PL-NCl to achieve long-lasting antibacterial activity as well as enhanced pro-osteogenesis, thus providing adaptive bioactivities for bone-implant integration. Rat implant-associated osteomyelitis model confirms that Ti-PL-NCl has excellent efficacy of infection prevention and osseointegration promotion. This work may provide a new paradigm of designing multifunctional implants to achieve long-term successful implantation.

Conjugating HA bundles with ZIF-8 for catalytic degradation of tetracycline and antibacterial capacity

The overused of antibiotics had led to major environmental issues and drug-resistant bacteria, which inevitably harmed the environment and public health. In this work, in order to obtain environmentally friendly bi-functional materials to combat with residual antibiotics and bacterial contamination, ZIF-8, a typical Zn based zeolitic imidazolate framework (ZnZIF) with excellent chemical stability, was conjugated to hydroxyapatite nanowire bundles (HAnBs) by a simple in-situ synthesis. The obtained ZnZIFs@HAnBs was characterized by SEM, EDS, XPS, FT-IR, XRD and BET. The effects of catalysts, catalyst dosage, TC initial concentration, PMS concentration and pH on TC degradation were investigated. Notably, ZnZIFs@HAnBs (94.0%) exhibited excellent degradation effect of tetracycline (TC) within 15min, which was 1.7 and 5.2 times than that of ZIF-8 (55.9%) and HAnBs (18.1%) under optimal conditions, respectively. Moreover, after recycling 10 times, the degradation rate still more than 86.8%. The degradation mechanism was confirmed by free radical quenching experiment coupling with electron paramagnetic resonance (EPR), and the 1O2 and O2•- were the major reactive oxygen species in TC degradation. Furthermore, it presented excellent antibacterial activity (95.0%) against E. coli and S. aureus, which was attributed to the synergistic effect of sustained release of Zn2+ and phosphate in ZnZIF@HAnBs. In summary, an eco-friendly bi-functional materials of HA nanowire bundles could be synthesized by simple strategy, and it could be applied in the fields of environmental remediation, as well as in treatment of antibiotic and bacterial pollution.

Rational design, synthesis, and antimicrobial evaluation of novel 1,2,4-trizaole-substituted 1,3,4-oxadiazole derivatives with a dual thioether moiety.

In this paper, a series of novel 1,2,4-trizaole-substituted 1,3,4-oxadiazole derivatives with a dual thioether moiety were constructed. The synthetic compounds were characterized by 1H NMR, 13C NMR, HRMS, and single crystal diffraction. The antimicrobial activities of title compounds against fungi (Pyricutaria oryzae Cav., Phomopsis sp., Botryosphaeria dothidea, cucumber Botrytis cinerea, tobacco Botrytis cinerea, blueberry Botrytis cinerea) and bacteria (Xanthomonas oryzae pv. oryzicola, Xoc; Xanthomonas axonopodis pv. citri, Xac) revealed these compounds possessed excellent antibacterial activity through mycelial growth rate method and turbidity method, respectively. Among them, compounds 7a, 7d, 7g, 7k, 7l, and 7n had the antibacterial inhibition rate of 90.68, 97.86, 93.61, 97.70, 97.26, and 92.34%, respectively. The EC50 values of 7a, 7d, 7g, 7k, 7l, and 7n were 58.31, 48.76, 58.50, 40.11, 38.15, and 46.99μg/mL, separately, superior to that of positive control pesticide thiodiazole copper (104.26μg/mL). The molecular docking simulation of compound 7l and glutathione s-transferase also confirmed its good activity. The in vivo bioassay toward Xac infected citrus leaves was also performed to evaluate the potential of compounds as efficient antibacterial reagent. Further study of antibacterial mechanism was also carried out, including extracellular polysaccharide production, permeability of bacterial membrane, and scanning electron microscope observations. The excellent antibacterial activities of these compounds provided a strong support for its application for preventing and control plant diseases.

Evaluating the Metabolomic Profile and Anti-Pathogenic Properties of Cannabis Species

The Cannabis species is one of the potent ancient medicinal plants acclaimed for its medicinal properties and recreational purposes. The plant parts are used and exploited all over the world for several agricultural and industrial applications. For many years Cannabis spp. has proven to present a highly diverse metabolomic profile with a pool of bioactive metabolites used for numerous pharmacological purposes ranging from anti-inflammatory to antimicrobial. Cannabis sativa has since been an extensive subject of investigation, monopolizing the research. Hence, there are fewer studies with a comprehensive understanding of the composition of bioactive metabolites grown in different environmental conditions, especially C. indica and a few other Cannabis strains. These pharmacological properties are mostly attributed to a few phytocannabinoids and some phytochemicals such as terpenoids or essential oils which have been tested for antimicrobial properties. Many other discovered compounds are yet to be tested for antimicrobial properties. These phytochemicals have a series of useful properties including anti-insecticidal, anti-acaricidal, anti-nematicidal, anti-bacterial, anti-fungal, and anti-viral properties. Research studies have reported excellent antibacterial activity against Gram-positive and Gram-negative multidrug-resistant bacteria as well as methicillin-resistant Staphylococcus aureus (MRSA). Although there has been an extensive investigation on the antimicrobial properties of Cannabis, the antimicrobial properties of Cannabis on phytopathogens and aquatic animal pathogens, mostly those affecting fish, remain under-researched. Therefore, the current review intends to investigate the existing body of research on metabolomic profile and anti-microbial properties whilst trying to expand the scope of the properties of the Cannabis plant to benefit the health of other animal species and plant crops, particularly in agriculture.