Bioactivity Tests Research Articles

Bio-Recycling Hazelnut Shells to Improve Antioxidant Properties of Lentinus tigrinus Sporophore

Lentinus tigrinus is a wood-decay fungus known for its nutritional, culinary, and medicinal benefits. It contains bioactive compounds like polyphenols, terpenes, and flavonoids that exhibit antioxidant, anti-microbial, and anti-inflammatory effects. These natural antioxidants are increasingly recognized for their potential to prevent oxidative damage linked to aging and chronic diseases. This study investigates the antioxidant activity of hydroalcoholic extracts obtained from L. tigrinus sporophores cultivated on hazelnut shells (Lt1_HS), a waste material rich in phenolic compounds, and sporophores cultivated on sawdust (Lt1_S). Bioactivity tests, including DPPH, TBARS, MTT, and DCFH-DA assays, were performed to assess the hydroalcoholic extracts’ efficiency. The results showed that all the extracts contained various bioactive compounds, primarily polyphenols. Notably, the caffeoylquinic acids present in HS and Lt1_HS are linked to anti-peroxidant effects. Biological analyses demonstrated that the Lt1_HS extract has higher anti-peroxidant activity (IC50 0.77 ± 0.01 mg/mL) compared to Lt1_S (IC50 1.36 ± 0.01 mg/mL) and reduces the accumulation of reactive oxygen species in HaCaT cells by 80%. However, the specific bioactive compounds responsible for these antioxidant effects are still unclear, and further analysis will be conducted. Additionally, this study promotes recycling hazelnut shells as a valuable substrate for fungal cultivation, supporting sustainable waste management.

Design, Synthesis, and Biological Activity Evaluation of 5-Aryl-cyclopenta[c]pyridine Derivatives.

Taking the natural product cerbinal as the lead compound, 30 novel 5-aryl-cyclopenta[c]pyridine derivatives were designed and synthesized based on the previous bioactivity studies of the cyclopenta[c]pyridines. The modification of the position-5 of compound 2 was achieved by amination, bromination, and cross coupling using cerbinal as the raw material. The results of the bioactivity tests demonstrated that partial compounds exhibited superior activity against plant viruses compared to compound 2. Compounds 4g and 4k showed higher anti-TMV activity levels than commercial varieties of ribavirin at concentrations of 500 and 100 μg/mL. In particular, compound 4k, which contained a m-methoxyphenyl substitution, displayed the most potent anti-TMV activity in vivo (inactivation effect 51.1 ± 1.9%, curative effect 50.7 ± 3.6%, protection effect 53.8 ± 2.8% at 500 μg/mL) The toxicological experiments also revealed that compound 4k exhibited low toxicity to zebrafish. Additionally, molecular docking results indicated that access to the benzene ring enhanced the binding affinity of these derivatives for TMV receptor proteins. Furthermore, studies on the insecticidal and fungicidal activities of these derivatives showed that most of the compounds exhibited good larvicidal efficacy against Plutella xylostella and broad-spectrum fungicidal activities. Notably, compound 4i (3,4,5-trifluorophenyl) displayed an outstanding inhibition ratio of 91.9% against Sclerotinia sclerotiorum, 75% against Botrytis cinerea, and 62.5% against Phytophthora infestans at a concentration of 50 μg/mL. These results suggest that 5-aryl-cyclopenta[c]pyridine derivatives could serve as promising candidate agents for antiviral, insecticidal, and fungicidal applications in agricultural production.

Exploring the bioactivity and antibacterial properties of silver and cerium co-doped borosilicate bioactive glass.

Bone defects resulting from trauma or diseases that lead to bone loss have created a growing need for innovative materials suitable for treating bone-related conditions. The purpose of this study is, therefore, to synthesize and analyse the synergistic effects of cerium (Ce) and cerium-silver (Ce-Ag) doping of borosilicate bioactive glass (BBG) on the bioactivity, antibacterial properties, and biocompatibility for potential applications in bone tissue engineering. This study utilized a sol-gel Stöber method to synthesize doped BBGs based on S49B4. Characterization techniques were utilized to evaluate the thermal stability, elemental composition, structural integrity, and morphological properties of the synthesized Ce and AgCe-BBGs. Cytotoxicity was evaluated using a GMSM-K gingival cell line, while antimicrobial tests were conducted using clinical isolates of Escherichia coli and Staphylococcus aureus. The characterization results confirmed the successful incorporation of Ce and Ag, resulting in elongated pineal to spherical nanosized BG particles (33-68 nm). Thermal analysis indicated that silver exhibited lower thermal stability compared to cerium. Bioactivity tests indicated that while silver has intrinsic bioactive qualities, elevated cerium levels above 0.5 wt% may inhibit or delay apatite formation by generating insoluble cerium phosphate ions. Lactate dehydrogenase assays demonstrated that among other BBGs, SBAgCe1 showed the highest LDH activity, suggesting mild cytotoxicity. The co-doped BBG exhibited strong antibacterial activity through a complex interaction between Ag and Ce ionic exchange. Nonetheless, a careful balance of Ce and Ag concentrations is critical, as high levels can compromise bioactivity and increase cytotoxicity. The results highlight the potential of SBAgCe0.5 as a candidate for bone tissue engineering applications due to its favourable bioactivity, and antibacterial and cytocompatible properties, emphasizing the importance of optimizing dopant concentrations for therapeutic applications in favour of good health and the well-being of humanity.

Podocarpane and cleistanthane diterpenoids from Strophioblachia glandulosa: Structural elucidation, anti-hypertrophy activity and network pharmacology

In the present investigation, fourteen unprecedented podocarpane diterpenoids strophiolosas A-J, L-N and P (1–10, 12–14, 16), two new cleistanthane derivatives strophiolosas Q-R (17–18), two new dibenzopyroan-ones and one new tetralone strophiolosas S-U (19–21), were isolated from the whole plant of Strophioblachia glandulosa. The structures were elucidated via various spectroscopic analysis, quantum chemistry calculations, and X-ray diffraction. Bioactivity test indicated that compounds 5 and 17 possessed promising anti-cardiac hypertrophy effect in vitro (IC50 values of 16.50 and 9.67 μM). Additionally, through network pharmacology prediction, PARP1 may be a potential target of compound 17, mediating its anti-hypertrophic effects through multiple pathways.

Green synthesis and characterization of NiO/Hydroxyapatite nanocomposites in the presence of peppermint extract and investigation of their antibacterial activities against Pseudomonas aeruginosa and Staphylococcus aureus

In many areas, antibiotic resistance is becoming a serious concern for public health. As a result of the interesting structural properties of nanomaterials, nanoscience-based methods have emerged as promising ways to increase the movement of existing antimicrobials. In this study, pristine nickel oxide (NiO) nanoparticles, hydroxyapatite (HAP) nanoparticles, and binary nickel oxide/hydroxyapatite (NiO/HAP) nanocomposites were fabricated through peppermint extract-assisted green route. The obtained results revealed that peppermint extract can be a superior green capping agent for the preparation of NiO, HAP, and NiO/HAP nanomaterials. The bioactivity tests revealed the bactericidal and anti-biofilm activities of synthesized NiO, HAP, and NiO/HAP nanostructures against Pseudomonas aeruginosa (PAO1) and Staphylococcus aureus (ATCC 43300) bacteria. The findings confirmed that the prepared NiO/HAP nanocomposites have more effective antibacterial activity than pure NiO and HAP. For Staphylococcus aureus, the minimal inhibitory concentration (MIC) values for NiO, HAP, and NiO/HAP nanocomposites were determined to be of about 9.60, 13.03, and 3.41 mg/mL, respectively. For Pseudomonas aeruginosa, the MIC values for NiO, HAP, and NiO/HAP nanocomposites were estimated as 9.6, 13.50, and 1.7 mg/mL, respectively. Although, all synthesized samples are remarkable in their ability to prevent the formation of biofilms at MIC and sub-MIC concentrations (p < 0.01), NiO/HAP illustrated biofilm inhibitory activity up to 95 % for Pseudomonas aeruginosa and to 81 % for Staphylococcus aureus. In the present study, it was demonstrated that NiO/HAP nanocomposites prepared in a green environment can be excellent antibacterial agents against Staphylococcus aureus and Pseudomonas aeruginosa.

Synthesis, Antifungal Activity and Action Mechanism of Anethole‐Derived Amide‐Urea Compounds

In order to develop new antifungal molecules and explore further applications of natural products, 25 novel amide‐urea compounds were synthesized from anethole in this work by a few simple reactions, and structural confirmation was conducted using 1H‐NMR, 13C‐NMR, HRMS, and FT‐IR. Preliminary bioactivity tests were performed against eight plant pathogens. The results demonstrated that all compounds exhibited antifungal activity against the tested fungi, and 5p exhibited the most potent antifungal activity. To explore the action mechanism of the antifungal compounds, the inhibitory activity of 5p against SDH was evaluated and found to be comparable to that of boscalid. Furthermore, the binding mode of the compound to SDH was simulated by molecular docking, and similarities between 5p and boscalid's binding with SDH were identified. The results indicate that further investigation of compound 5p may prove beneficial in determining its potential as a fungicide.

Bioactive Properties of Phosphate-Modified Silicon Oxycarbide Protective Coatings: Morphology and Functional Evaluation.

This article presents a study on the functional properties and morphology of coatings based on amorphous silicon oxycarbide modified with phosphate ions and comodified with aluminum and boron. The objective of this modification was to enhance the biocompatibility and bioactivity without affecting its protective properties. The comodification was aimed toward stabilization of phosphate in the structure. The coatings were prepared according to the typical procedure for polymer-derived ceramics: synthesized via the sol-gel method, deposited using the dip-coating technique, and subsequently pyrolyzed. Comprehensive analyses of the morphology, surface properties, corrosion resistance, and bioactivity were conducted to assess their functional performance. The coatings exhibited uniform and smooth surfaces, with phase separation observed in the boron-modified SiBPOC series. Surface wettability and free energy measurements demonstrated that SiPOC and SiBPOC coatings possessed moderate hydrophilicity and favorable surface free energy for cell adhesion and bone tissue mineralization. Corrosion resistance tests in Ringer's solution revealed that SiBPOC coatings provided the highest protection against ion leaching, while SiAlPOC showed decreased resistance due to surface cracks. Bioactivity tests indicated calcium phosphate precipitation on the surface of all samples with higher hydroxyapatite formation on SiPOC and SiAlPOC coatings. In vitro tests using MG-63 osteoblast-like cells confirmed the biocompatibility of the coatings, with SiPOC and SiBPOC exhibiting the best combination of bioactivity, cell adhesion, and proliferation. These findings suggest that the phosphate- and boron-modified SiOC-based coatings are promising candidates for enhancing bone integration in orthopedic implants.

Multifunctional alumina scaffolds with enhanced bioactivity and antimicrobial properties for bone tissue engineering

Inert ceramic implants suffer from significant complications such as lack of osseointegration, biofilm formation, and infections, necessitating the development of novel materials with both osteogenic and antibacterial properties to prevent implant failure. In this study, we aimed to multifunctionalize a tridimensional macroporous alumina scaffold with a biomimetic calcium phosphate (CaP) coating combined with a silver-based extra-thin film to enhance bioactivity and provide an additional antibacterial effect. The porous alumina scaffolds were fabricated through a powder metallurgy technique, followed by biomimetic deposition and DC magnetron sputtering. The coatings were characterized using SEM/EDS and AFM measurements to examine their morphology and topography. To evaluate the osteoconductive response of the materials, in vitro tests were conducted by immersing the samples in Simulated Body Fluid (SBF). The bioactivity tests revealed that the CaP-AgO coating, in line with the roughness surface and free surface energy values, exhibited a higher Ca/P ratio formation. This indicated an increased affinity for apatite adhesion, ultimately leading to a higher osseointegration ability compared to the CaP-Ag coating. Furthermore, the CaP-AgO coating demonstrated superior activity against S. aureus. These findings demonstrate the potential of the multifunctional coatings to address the challenges associated with inert ceramic implants by promoting bioactivity and combating bacterial infections.

Mesoporous silica nanoparticles based on a dual environmental response corresponding to temperature and α-amylase for the control of Spodoptera litura

The design and development of stimuli-responsive nanocarriers hold the promise of the smart delivery of pesticides to target organisms. Herein, we successfully prepared mesoporous silica nanoparticles using the self-templating method, which were grafted with both N-isopropylacrylamide (NIPAM) and cyclodextrin (CD) and loaded with indoxacarb (IN) to afford a pesticide release system with a dual-stimulated response of temperature and α-amylase, referred to as IN@MSNs@NIPAM@CD. Physicochemical characterisation revealed the successful preparation of IN@MSNs@NIPAM@CD with 46.30 % indoxacarb loading. The results showed that IN@MSNs@NIPAM@CD was able to release IN rapidly in the environment of high temperature and α-Amylase, with excellent dual-responsive property. The UV resistance evaluation showed that IN@MSNs@NIPAM@CD could effectively improve the photodegradation resistance of indoxacarb. Fluorescent inverted microscope showed that FITC@MSNs@NIPAM@CD has excellent uptake and translocation properties in corn plants. Bioactivity tests showed that at 14 d, IN@MSNs@NIPAM@CD (LC50 = 9.83 mg L−1) exhibited higher insecticidal activity and longer effective duration than IN@EC (LC50 = 14.64 mg L−1). Acute toxicity test revealed that the IN@MSNs@NIPAM@CD nanoparticles were less acutely toxic to earthworms, zebrafish, BEAS-2B cells and MSNs@NIPAM@CD nanocarriers were safe for the growth of corn. Thus, the dual-responsive nano-controlled-release formulation of IN@MSNs@NIPAM@CD can provide an effective way of achieving the precise delivery and reduced use of pesticides.

Potential pesticide substrates of an insect ABCC transporter.

The use of synthetic pesticides carries a significant risk of pests developing resistance, leading to decreased pesticide effectiveness. ATP-binding cassette (ABC) transporters, especially the ABCC subfamily members, have been suggested to act as efflux pumps for various pesticides, thereby contributing to pesticide resistance. So far, the identification of potential pesticide substrates of insect ABC transporters is most often based on the quantification of transcript in arthropods. Here, we screened and identified the potential pesticide substrates of ABCC-9C from Tribolium castaneum based on an in vitro ATPase activity assay. Together with affinity evaluation-, cytotoxicity analysis-, and RNA interference-based bioactivity tests, we revealed that the insecticides, carbofuran, and buprofezin, are potential substrates of TcABCC-9C. Additionally, we identified an amphipathic translocation channel in the transmembrane domain of TcABCC-9C formed by 8 transmembrane helices. Molecular docking suggested that both carbofuran and buprofezin bind at the same site within the translocation channel via hydrophobic interactions. These findings indicate that TcABCC-9C might play a critical role in multi-pesticide resistance, providing a potential target for managing pesticide resistance and laying the groundwork for future pest control strategies. Given the conservations among ABCC subfamily members, the experimental model we developed in this study can be also applied to identify the potential substrates of other ABCC transporters, as well as to predict insecticide resistance mediated by ABCC transporters.

Antioxidant potential, antimicrobial activity, polyphenol profile analysis, and cytotoxicity against breast cancer cell lines of hydro-ethanolic extracts of leaves of (Ficus carica L.) from Eastern Morocco.

Many beneficial compounds found in fig leaves can be used in tea and medicine. These compounds aid with digestion, reduce inflammation, and treat diabetes and bronchitis. Chetoui, Malha, Ghoudane, and Onk Hmam fig leaf hydro-ethanol extracts from Eastern Morocco were analyzed for metabolites and biological activities. HPLC-UV examination revealed that the leaf extract included mainly caffeine, rutin, and ferrulic acid. Spectrophometric results show that Malha leaf is rich in polyphenols (62.6 ± 1.3mg GAE/g) and flavonoids (26.2 ± 0.1mgQE/g). Chetoui leaf contains the highest vitamin C content (8.2 ± 0.1mg Asc A/100gDW), while Onk Hmam leaf has the highest condensed tannin (4.9 ± 0.1mgCatE/g). The investigations found that all leaf extracts were antioxidant-rich, with strong Pearson bivariate correlation between bioactive polyphenol levels and antioxidant tests for DPPH, β-carotene, ABTS, and TAC (values of -0.93, -0.94, -0.85, and 0.98, respectively). The coefficients for flavonoid content were -0.89, -0.89, -0.97, and 0.80, respectively. Disk diffusion and MIC results show that the hydro-ethanol fig leaf extracts eliminate fungi and bacteria. In addition, these fig leaf extracts showed promise cytotoxicity against the breast cancer cell lines MCF-7, MDA-MB-231, and MDA-MB-436 and an interesting selectivity index. In silico leaf bioactive component analysis revealed that myricitin inhibited NADPH oxidase the greatest (gscore -6.59Kcal/mol). Trans-ferulic acid inhibits Escherichia coli beta-ketoacyl-[acyl carrier protein] synthase (-6.55kcal/mol), whereas quercetin inhibits Staphylococcus aureus nucleoside diphosphate kinase (-8.99). CYP51 from Candida albicans is best treated with kaempferol and myricitin. Both had a glide gscore of -7.84kcal/mol. Rutin has the most potent Sespace 3 anticancer activity, with a glide gscore of -7.09kcal/mol. This research indicates that fig leaf extracts from the region can be used in medicine, food, natural cosmetics, and breast cancer prevention. To maximize the value of these leaves, their use must be carefully studied. Naturally, this fortunate tree's diversity must be preserved and enhanced.

The structure elucidation and alleviating effect on liver fibrosis in vivo of a pectin-like polysaccharide isolated from Buddleja officinalis

Buddleja officinalis has been used as a traditional Chinese medicine for years. Although evidence has demonstrated it can enhance liver function, the active material basis remains unknown. We hypothesize polysaccharides from Buddleja officinalis may be the active material against liver disease. Herein, we elucidated the structure of a novel pectin-like polysaccharide designed BOM0.05S2 with a molecular weight of 13.6 kDa. Combined with endo-1, 4-β-Mannanase degradation, we found its backbone consists of alternate 1, 2, 4-linked α-Rhap and 1, 4-linked α-GalpA (RG-I type pectin) and mannoglucan, with branches of 1, 4-, 1, 6- and 1, 3, 6-linked β-Galp, T-, 1, 5- and 1, 3, 5-linked α-Araf, T-linked β-Manp and T-linked α-Glcp substituted at C-4 of 1, 2, 4-linked α-Rhap and C-6 of 1, 4, 6-linked α-Glcp. As speculated, BOM0.05S2 showed a significant improvement on carbon tetrachloride (CCl4)-induced liver damage in mice. Bioactivity test showed that BOM0.05S2 reduced AST, ALT and four indexes of liver fibrosis including LN, HA, IV-C, PC-III. Further, we demonstrated that BOM0.05S2 attenuated the collagenous fiber and α-SMA in liver. These findings highlight the potential of BOM0.05S2 as a lead compound for the treatment of liver fibrosis.

The Latest Progress in the Chemistry of Daphniphyllum Alkaloids.

Daphniphyllum alkaloids (DAs) are interesting molecules with rich molecular skeletons and diverse biological activities. Since their discovery, phytochemists have isolated, purified, and identified more than 350 DAs. Synthetic chemists, attracted by the structure and activity of DAs, have accomplished many elegant synthetic jobs. Herein, we summarize work on the isolation, structural identification, bioactivity testing, and synthesis of DAs from 2018 to 2023, with the aim of providing a reference for future studies.

Exploring the potential of Fargesin from Chrysanthemum indicum for chronic migraine: in-silico and pharmacokinetic study.

Chronic migraine is recognized by the WHO as one of the most debilitating chronic conditions. It is primarily caused by central sensitization of the trigeminal nucleus caudalis. Key biomarkers associated with migraine include NFkB, IL-1β, CGRP, and iNOS. While CGRP antagonists have proven effective in treating migraines, Chrysanthemum indicum L., a traditional herbal remedy, has not been established as a treatment. To address this, we investigated whether Fargesin, a lignan found in CI, could potentially reduce migraines by targeting these biomarkers. We conducted pharmacokinetic, toxicological, and in-silico studies. Molecular docking studies revealed a strong interaction between Fargesin and CGRP/iNOS. The pharmacokinetic analysis indicated robust intestinal absorption and effective penetration of the blood-brain barrier. In-silico toxicity assessments showed favorable results. Promising interactions with drug targets were observed in bioactivity tests. Fargesin from Chrysanthemum indicum may hold potential as a therapeutic agent for migraines.

Rapid Exploration of Chemical Space by High-Throughput Desorption Electrospray Ionization Mass Spectrometry.

This study leverages accelerated reactions at the solution/air interface of microdroplets generated by desorption electrospray ionization (DESI) to explore the chemical space. DESI is utilized to synthesize drug analogs at an overall rate of 1 reaction mixture per second, working on the low-nanogram scale. Transformations of multiple drug molecules at specific functionalities (phenol, hydroxyl, amino, carbonyl, phenyl, thiophenyl, and alkenyl) are achieved using electrophilic/nucleophilic, redox, C-H functionalization, and coupling reactions. These transformations occur under ambient conditions on the millisecond time scale with direct detection of products being successful in all but three of the reaction types studied. The large scope (22 bioactive compounds, >20 chemical transformations, and >300 functionalization reagents) and high speed (>3000 reactions/hour) provide access to a wide array of drug analogs that can be used for bioactivity testing. A total of ∼6800 unique reactions were examined through a data-driven workflow, and more than 3000 unique derivatives (∼44%) were identified tentatively by the m/z value and signal-to-control ratio in single-stage mass spectrometry (MS) analysis, with over 1000 being further characterized by tandem MS. The speed of the DESI-MS reaction screen provides potential advantages for emerging machine learning-based predictions of organic synthesis, and it sets the stage for future online DESI-MS bioassays and scaled-up microdroplet synthesis before formal characterization of hit compounds is sought using traditional methods of drug discovery.

Electrophoretic deposition of bioactive glass 58S- xSi3N4 (0 < x < 20 wt.%) nanocomposite coating on AISI 316L stainless steel substrate for biomedical applications

This paper aims to investigate the biocompatibility, bioactivity and properties of bioactive glass 58S-xSi3N4 (0 < x < 20 wt.%) nanocomposite coating on AISI 316 L stainless steel substrate, applied by electrophoretic deposition method. The implications of adding Si3N4 nanoparticles up to 20 wt.% to the bioactive glass coating for the structural and biomedical properties of deposited coatings were investigated. The deposited coating samples were characterized by X-ray diffraction (XRD) analysis, field emission scanning electron microscope (FE-SEM), Fourier-transform infrared spectroscopy (FTIR), and energy dispersive X-ray spectroscopy (EDS). For the evaluation of cellular toxicity, the MTT cytotoxicity test with MG63 bone cell was performed. Bioactivity test was also conducted in simulated body fluid (SBF) up to 28 days. Results showed that increase in the Si3N4 content of composite samples is associated with a significant decrease in the average size of composite powder, inferring that Si3N4 additive has become nucleation sites during synthesis. Stereomicroscope images showed that with an increase in deposition time up to 70 min, a uniform coating can be attained. An increase in the Si3N4 content is associated with a significant reduction in surface roughness and non-uniformities of the deposited layer. The addition of Si3N4 in the composite layer slightly increases the wetting angle. The highest cellular toxicity was observed for the AISI 316 L sample at the concentration of 10 micromolar, while the lowest cellular toxicity is attributed to the BG-20 %Si3N4 sample at the concentration of 75 micromolar, exhibiting viability values similar to the control sample. Bioactivity assessment of deposited coatings indicated a remarkable improvement in the bone-forming ability of Si3N4-containing bioactive glass composite.

Control of membrane biofouling in MBR for wastewater treatment by biohybrid membrane with superhydrophilic self-QQ function

Quorum quenching (QQ) is an effective method for controlling MBR (membrane bioreactor) membrane biofouling by regulating the release of autoinducer during the quorum sensing (QS) process. However, the addition of QQ bacteria solution or QQ carriers inevitably leads to unpredictable effects on MBR microbial systems and operational efficiency (for example, reduced stability of nitrification and denitrification processes, reduced biodegradation efficiency and unbalanced biofilm formation etc.). Here, we present a biohybrid membrane called ES-BM (electrospinning-biohybrid membrane), which features a unique pore size structure consisting of electrospun superhydrophilic nanofiber sheaths, a self-QQ layer (active QQ bacteria are immobilized within the interlayer structure of this biohybrid membrane to inhibit the QS process of biofilm-forming associated bacteria at the source surface where membrane biofouling occurs), and a basement filter layer, which maintain the activity of QQ bacteria for an extended period. The ES-BM extends operational cycles up to 21 days at a constant flux of 24 L/m²/h, which is three times longer than conventional MBR systems. The membrane exhibits exceptional hydrophilicity (water contact angle of approximately 0° within 2 seconds) and high tensile strength (Young’s modulus of 135 MPa). Long-term bioactivity tests confirm the stability and recyclability of the ES-BM. Additionally, microbial community analysis suggests that the biohybrid membrane suppresses the growth of biofilm-related bacteria without significantly affecting the indigenous microbial population, further enhancing system performance. This work demonstrates the potential of ES-BM for improving MBR biofouling resistance and presents insights into scalable electrospinning fabrication techniques.

Formation of bone tissue apatite on starch-based nanofiber-capped nanohydroxyapatite and reduced graphene oxide: a preliminary study.

In the present study, blends of polyvinyl alcohol (PVA), starch (SH), nanohydroxyapatite (Nano-HA), and reduced graphene oxide (r-GO) were used to fabricate an electrospun nano scaffold (ENS), via electrospinning for their potential application in oral and maxillofacial bone soft and hard tissue regeneration. The scaffold was characterized for its physicochemical and mechanical properties. An invitro study was carried out using human osteoblast MG-63 bone cells. Surface characterization, particularly the analysis of calcium content, was performed before and after immersion in the simulated body fluid (SBF). Additionally, the impact of surface treatment on antimicrobial activity was investigated. The results demonstrated that the tensile strength (18.12 ± 0.14MPa), elongation at break (19.23 ± 0.11%), and flexing index (20.15 ± 0.13%) of the ENS were outstanding, indicating promising performance. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assays demonstrated the biocompatible nature of the ENS. The bioactivity test result of ENS showed excellent deposition of bone apatite crystals. The ENS exhibited antimicrobial properties against E. coli (3.41 ± 0.03mm) and S. aureus (3.12 ± 0.08mm). The ENS, possessing the desired properties, has the potential to be tested in large animals for oral and maxillofacial bone and soft tissue regeneration after obtaining the necessary approvals. The developed ENS offers a promising solution for bone tissue regeneration in the oral and maxillofacial region.

Design and Synthesis of Dual Galectin-3 and EGFR Inhibitors Against Liver Fibrosis.

Liver fibrosis, mainly arising from chronic viral or metabolic liver diseases, is a significant global health concern. There is currently only one FDA-approved drug (Resmetirom) in the market to combat liver fibrosis. Both galectin-3 and epidermal growth factor receptor (EGFR) play important roles in liver fibrosis, while galectin-3 may interact with EGFR. Galectin-3 inhibitors, typically lactose or galactose derivatives may inhibit liver fibrosis. We hypothesized that targeting both galectin-3 and EGFR may have better effect against liver fibrosis. Here, EGFR inhibitor erlotinib was used in a series of designed galectin-3 inhibitors after hybridization with the pharmacophore structure in reported galectin-3 inhibitors to impede hepatic stellate cells (HSCs) activation by a typical method of click chemistry. Bioactivity test results showed that compound 29 suppressed TGF-β-induced upregulation of fibrotic markers (α-SMA, fibronectin-1, and collagen I). The preferred compound 29 displayed better binding to galectin-3 (KD=52.29 μM) and EGFR protein (KD=3.31 μM) by SPR assay. Further docking studies were performed to clarify the possible binding mode of compound 29 with galectin-3 and EGFR. Taken together, these results suggested that compound 29 could be a potential dual galectin-3 and EGFR inhibitor as leading compound for anti-liver fibrosis new drug development.

Design and research of new virulence factor inhibitors for plant bacterial disease control

In this work, various chalcone derivatives incorporating piperazine-isopropanolamine were elaborately designed and synthesized. The antibacterial efficacy revealed that compound Z6 showed notable biological activity, with a median effective concentration (EC50) of 0.29 mg/L against Xanthomonas oryzae pv. oryzae (Xoo) in vitro, which is around 200 times higher than thiodiazole copper (TC, 91.00 mg/L). Similarly, Z21 exhibited a strong biological response (EC50 = 0.83 mg/L) against Xanthomonas axonopodis pv. citri (Xac), outperforming TC (EC50 = 114.60 mg/L). Results of bioactivity test in vivo demonstrate that Z6 displayed significantly better curative and protective activities (51.5 %, 47.9 %) than TC (47.9 %, 30.5 %) against rice bacterial leaf blight (BLB). Further biochemical studies indicates that Z6 targeted multiple virulence factors and repressed the release of essential nutrients required for bacterial proliferation, thereby disrupting the reduction of cell membrane content of the pathogenic bacteria. According to the research, chalcone derivatives containing piperazine-isopropanolamine have potential to be antibacterial candidates.