Μg mL-1 Research Articles

Design, synthesis and biological activity evaluation of eco-friendly rosin-based fungicides for sustainable crop protection.

Utilizing fungicides to protect crops from diseases is an effective method, and novel eco-friendly plant-derived fungicides with high efficiency and low toxicity are urgent requirements for sustainable crop protection. Two series of rosin-based fungicides (totally 35) were designed and synthesized. In vitro fungicidal activity revealed that Compound 6a (Co. 6a) effectively inhibited the growth of Valsa mali [median effective concentration (EC50) = 0.627 μg mL-1], and in vivo fungicidal activity suggested a significant protective efficacy of Co. 6a in protecting both apple branches (35.12% to 75.20%) and apples (75.86% to 90.82%). Quantum chemical calculations (via density functional theory) results indicated that the primary active site of Co. 6a lies in its amide structure. Mycelial morphology and physiology were investigated to elucidate the mode-of-action of Co. 6a, and suggested that Co. 6a produced significant cell membrane damage, accelerated electrolyte leakage, decreased succinate dehydrogenase (SDH) protein activity, and impaired physiological and biochemical functions, culminating in mycelial mortality. Molecular docking analysis revealed a robust binding energy (ΔE = -7.29 kcal mol-1) between Co. 6a and SDH. Subsequently, biosafety evaluations confirmed the environmentally-friendly nature of Co. 6a via the zebrafish model, yet toxicological results indicated that Co. 6a at median lethal concentration [LC50(96)] damaged the gills, liver and intestines of zebrafish. The above research offers a theoretical foundation for exploiting eco-friendly rosin-based fungicidal candidates in sustainable crop protection. © 2024 Society of Chemical Industry.

Phytofabricated ZnO-NPs mediated by Hibiscus tiliaceus leaf extract and its potential as a diosgenin delivery vehicle.

Zinc oxide nanoparticles (ZnO-NPs) have provided promising potential in the biomedical field, including the ability to overcome various health problems. Diosgenin is used to treat multiple health disorders but has very low solubility in water. Using ZnO-NPs as a diosgenin delivery vehicle was expected to increase the solubility of diosgenin, which would affect its bioavailability. This study demonstrates phytofabrication and characterization of ZnO-NPs, loading of diosgenin onto the ZnO-NPs, characterization of the product (ZnO-NPs/diosgenin), and evaluations of diosgenin release. Phytofabrication of the ZnO-NPs was carried out with zinc precursors and Hibiscus tiliaceus leaf extract (HLE) obtained with various extraction solvents. To explore the potential of using the ZnO-NPs as a diosgenin delivery vehicle, diosgenin release from the ZnO-NPs/diosgenin was studied. Based on the X-ray fluorescence (XRF) and X-ray diffraction (XRD) results, ZnO-NPs with high purity have been successfully fabricated. Nano-sized particles were detected using scanning electron microscopy (SEM) and confirmed by transmission electron microscopy (TEM), revealing the smallest particle size of 45.924 ± 27.910 nm obtained from the methanol extract with the zinc acetate precursor. The ZnO-NPs had hexagonal wurtzite and rod-like structures. Diosgenin was successfully added to the ZnO-NPs with loadings of 79.972% for ZnO-HLMEA-D500 (ZnO-NPs/diosgenin produced by doping with a 500 μg mL-1 of diosgenin solution) and 39.775% for ZnO-HLMEA-D1000 (ZnO-NPs/diosgenin produced by doping with a 1000 μg mL-1 of diosgenin solution). The solubilities of diosgenin from ZnO-HLMEA-D500 and ZnO-HLMEA-D1000 were higher than that of free diosgenin, confirming that ZnO-NPs have potential as delivery vehicles for diosgenin and conceivably other water-insoluble drugs.

A green, fluorescent probe employing erythrosine-B for tracing the accidental administration of levamisole in milk and plasma samples.

A simple and sensitive fluorescent probe has been developed and optimized to detect the non-intentional administration of levamisole (LVM). LVM is used as an anthelmintic therapy in cows, and hence, its residues appear in the drained milk until 60 hours after administering the drug. Meanwhile, levamisole is known to be an adulterant to cocaine and could be detected in addicts' plasma samples. Owing to its severe side effects, including agranulocytosis, which is lethal in many cases, detection and quantification of LVM in milk and plasma samples are of utmost importance. Therefore, a sensitive and selective analytical method is required for this purpose. This work develops a highly fluorescent probe obtained through the reaction between LVM and erythrosine-B in an acidic medium, where the produced ion pair complex has been measured at 553 nm after excitation at 528 nm. The proposed method provides linearity over the concentration range of 0.5-2.0 μg mL-1 for LVM, with a corresponding detection and quantitation limit of 0.5 and 0.3 μg mL-1. Full validation was performed, permitting the application of the suggested method to perform simple extraction steps. All the applied procedures followed the guidelines offered by green analytical chemistry, where the Green Analytical Procedure Index (GAPI) assessed the greenness of the proposed tool, and the yielded pictograms proved the eco-friendliness of the offered tool.

Croton grewioides essential oil and anethole reduce oxidative stress and improve growth of bovine primordial follicles during culture of ovarian tissue.

This study aims to evaluate the effects of Croton grewioides essential oil (CGEO) and anethole on follicle survival, growth, and oxidative stress in cultured bovine ovarian tissues. Ovarian tissues were cultured for 6 days in a medium supplemented with different concentrations (1, 10, 100, or 1000 µg mL-1) of CGEO or anethole and then, follicular survival and growth, collagen content, and stromal cell density in ovarian tissues cultured in vitro were evaluated by histology. The mRNA levels of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase 1 (GPX1), peroxirredoxin 6 (PRDX6), and nuclear factor erythroid 2-related factor 2 (NRF2) were evaluated by real-time PCR. The activity of SOD, CAT, glutathione peroxidase (GPx), and thiol concentrations were investigated. Ovarian tissues cultured with 1 µg mL-1 CGEO or anethole had a higher percentage of healthy follicles than those cultured in a control medium (P < .05). The 1 µg mL-1 CGEO also increased the number of stromal cells, collagen fibers, and thiol levels. Anethole (1 µg mL-1) increased CAT activity and reduced that of GPx. The activity of SOD was reduced by CGEO. In contrast, 1 µg mL-1 anethole reduced mRNA for CAT, PRDX1, and NRF2 (P < .05). In addition, 1 µg mL-1 CGEO reduced mRNA for CAT, PRDX6, and GPx1 (P < .05). The presence of 1 µg mL-1 anethole or CGEO in a culture medium promotes follicle survival and regulates oxidative stress and the expression of mRNA and activity of antioxidant enzymes in cultured bovine ovarian tissues.

A study on anticancer and antioxidant ability of selected brown algae biomass yielded polysaccharide and their chemical and structural properties analysis by FT-IR and NMR analyses

The study was conducted to determine the chemical and structural properties of polysaccharides extracted from the marine macroalgae Nemalion cari-cariense. Furthermore, evaluate the anticancer and free radical scavenging activity of purified N. cari-cariense polysaccharide. Approximately 41.6% (w/w) of crude polysaccharide was extracted from N. cari-cariense macroalgae biomass. After deproteinization, the purified polysaccharide's major chemical composition was found to be 92.6%, with all protein content removed. The purified polysaccharide had ash and moisture % of 23.01% and 4.03%, respectively. The C, H, and N of the test polysaccharide were analyzed using GC-MS, with results of 39.21%, 5.87%, and 4.29%, respectively. Furthermore, this analysis also revealed the monosaccharide composition such as glucose, galactose, mannose, xylose, and rhamnose glucose, galactose, mannose, xylose, and rhamnose 54.62%, 29.64%, 2.8%, 5.9%, and 6.8% respectively. The molecular weight of purified polysaccharide was found as 49 kDa through PAGE analysis. The FT-IR analysis revealed that the presence of functional groups exactly attributed to polysaccharide and 1H and 13C-NMR analyses confirmed the structural properties of N. cari-cariense polysaccharide. The free radicals scavenging ability of purified N. cari-cariense polysaccharide was investigated by various assays such as total antioxidant assay (22.3%–72.5% at 50–250 μg mL−1), DPPH assay (23.6%–76.9% at 10–160 μg mL−1), OH radical scavenging assay (13.6%–70.2% at 50–250 μg mL−1 dosage, and SO radical scavenging assay (27.6–68.41% at 50–250 μg mL−1 concentration). The polysaccharide demonstrated 82.63% anticancer activity towards the A549 lung cancer cell line at 1000 μg mL−1 dosage. The findings suggest that this polysaccharide has biological applications.

Electrochemical detection of atrial natriuretic peptide-coated nanocarriers based on a molecularly imprinted polymer receptor thin film

Molecularly imprinted polymers (MIPs) are biomimetic materials of great interest in the scientific and industrial fields for the development of innovative sensing strategies. Herein, we proposed a new sensing application by developing an electrochemical sensor using molecular imprinting (MI) technology for recognition of atrial natriuretic peptide (ANP) both as a free molecule in solution and attached to nanoparticle-based drug delivery systems (DDSs), aiming to provide fast and reliable information on the cell uptake of nanoparticles (NPs). As proof of concept, poly(lactic-co-glycolic acid) (PLGA) NPs were synthesized and used as nanocarriers for ischemic heart disease therapy were synthesized and then functionalized with ANP (named here as PLGA-NPs@ANP). The MIP receptor film was prepared by electrochemical polymerization of dopamine over the working area of a gold screen-printed electrode (AuSPE), using cyclic voltammetry (CV) technique. The construction of the ANP sensor was carefully optimized to enhance its performance, including the film thickness and the procedures for effective template extraction from the MIP matrix. The MIP biosensor presented a linear response against polymeric NPs (PLGA-NPs@ANP) concentration logarithm ranging from 4.0 μg mL-1 to 100 μg mL-1, with a sensitivity of – 0.0129 mA mL μg-1 decade-1 and an LOD < 4.0 μg mL-1. Furthermore, the developed MIP receptor film was able to discriminate ANP-functionalized nanocarriers from non-functionalized NPs.

Preliminary phytochemical and biological activity screening of Sargassum lapazeanum

Algae are exposed to substantial stress. In response, these organisms have developed efficient defense systems, such as protective secondary metabolite synthesis, making algae a primary source of bioactive compounds with a wide spectrum of biological activities. Thus, algae show potential for use in treatments of thrombotic, infectious, and chronic degenerative diseases. Therefore, the objective of this study was to evaluate the phytochemical compounds and pharmacological activity of an extract obtained from Sargassum lapazeanum. Algae were collected in the intertidal zone of Tarabillas beach (Bahía de La Paz, BCS). The biological activities of an ethanolic extract and its fractions were evaluated using chromatographic techniques. In addition, a bioautographic assay of hemolytic activity was conducted, and phytochemical profiles and acute toxicity in Artemia franciscana were evaluated. The relationships among the main extract components were also determined. The ethanolic extract exhibited significant antioxidant and hemolytic activity, which was mainly attributed to its content of anthrones, anthraquinones, and unsaturated triterpenes. Its toxicological activity reached an LC50 value of 225.1 μg mL-1, which was mainly attributed to alkaloids, flavonoids, anthrones, and saponins. The results suggest that Sargassum lapazeanum, which is endemic to the Gulf of California, has great pharmacological potential with biomedical applications.

Increased water intake dilutes protective uromodulin levels in urine and results in increased rates of pyelonephritis in a murine model.

Urinary tract infections (UTIs) rank among the most prevalent infections in humans, carrying substantial implications for public health. Women experiencing recurrent UTIs are often advised to boost their fluid intake to help eliminate bacteria. In this study, we explored the impact of elevated fluid consumption during UTIs using a mouse model of pyelonephritis. UTI was induced in 8-10 w female BALB/cJ-mice by surgically injecting Escherichia coli (O6:K13:H1) into the bladder whereafter mice were randomized to gel food (GF) or regular chow. Immune response and infection severity were determined 24-h post-infection. Invitro bacterial growth (OD600) was determined in urine from mice or from human volunteers. Gel feeding increased urine output (1.40 ± 0.77 μL min-1, p < 0.01) and diluted the urine (668.7 ± 177 mOsmol kg-1, p < 0.0001) compared to controls on regular chow (urine output: 0.34 ± 0.27 μL min-1, osmolality: 1439 ± 473.5 mOsmol kg-1). Mice on GF had a higher risk of pyelonephritis (87.5%) and more severe infections (26.22 ± 9.88 CFU mg-1 tissue) compared to controls (43.75%; 3.87 ± 3.56 CFU mg-1, p < 0.01). Correspondingly, the growth of E.coli was markedly reduced at osmolalities above 1200 mOsmol kg-1 compared to 600 mOsmol kg-1 and GF mice had lower urine levels of uromodulin (13.70 ± 1.89 μg mL-1, p < 0.01) compared to controls (24.65 ± 2.70 μg mL-1). Increased water intake and urine flow in mice will markedly increase the risk of pyelonephritis. The increased risk may reflect reduced urine uromodulin combined with optimized growth conditions for E. coli. The study does not immediately support the notion that established UTIs can be eliminated by increased water intake.

Occurrence of Neopestalotiopsis clavispora Causing Leaf Blight on Acer oblongum in China.

Acer oblongum is native to Southwest China and is also distributed in Nepal and Northern India. It is an excellent garden ornamental tree species, suitable for solitary planting in courtyards and parks. From June to August 2022, severe leaf blight occurred on A. oblongum in Baihe Wetland Park (32°5'42" N, 112°28'13" E) in Nanyang City, China. The foliar disease rate reached 59% (n=100). Early signs were yellow spots on the leaves, mainly on the middle and edge parts. Then, the lesions gradually expanded, became amorphous, and turned yellowish brown, eventually led to necrosis on leaves and branches. Twenty diseased leaves were collected and the junction areas between infected and healthy tissues were cut into 5 x 5 mm2 pieces. The collected plant materials were sterilized in 75% ethanol and 1% NaClO for 30 s and 1 minute, respectively, followed by rinsing in sterile water, and placing on a potato dextrose agar (PDA) plate supplemented with 50 µg ml-1 streptomycin at 25 °C for 3 days. Colony edges were cut and transferred to new PDA plates for purification culture. A total of 18 purified fungal strains were obtained, which showed similar phenotypes in morphological characteristics. All colonies had spread radially with wavy surfaces, and dense cream to white aerial hyphae. After 14 days in culture, black fruiting bodies appeared. Conidia were fusiform to slightly clavate, with five cells and two or three setae, 4.2 to 7.9 μm × 17.5 to 25.4 μm in diameter (n = 100). The apical and basal cells and setae were colorless, three median cells were brown, and the middle cell was dark brown. Morphological characteristics of all 18 strains were consistent with the genus description of Neopestalotiopsis spp. (Maharachchikumbura et al. 2014). Further molecular identification showed that the ITS region sequences of all strains have extremely high homology with Neopestalotiopsis spp. The β-tubulin gene (TUB), and the translation elongation factor 1-alpha gene (TEF1) were amplified for molecular identification (Shu et al. 2020). The sequences of three representative strains (FE-05, 09, 16) from different regions were deposited in GenBank with accession Nos. OQ867279, OQ867288, OQ867289 (ITS), OQ870207, OQ870208, OQ870209 (TUB), and OQ870204, OQ870205, OQ870206 (TEF1). BLASTn analysis of these sequences showed 99 to 100% identity to Neopestalotiopsis clavispora strains (OK655673, MZ648263 for ITS, ON000362, MZ286974 fr TUB, MH423941, MK512481 for TEF1). These morphological features and molecular identification indicated that the pathogen has the same characteristics as N. clavispora. Pathogenicity was tested on ten healthy 3-month-old seedlings using the three representative strains through in vivo experiments. For each strain, the conidial suspension (106 conidia ml-1) in absorbent cotton balls (50 µl of inoculum) were inoculated onto the healthy leaves of two seedlings, while a total of two other plants were served with sterile water as a blank control. The plants were potted in a climate incubator at 28°C and a relative humidity of approximately 90%. Symptoms consistent with natural lesions were observed on the inoculated leaves after 5 days while the control plants remained healthy. The strains of N. clavispora were reisolated from the symptomatic inoculated leaves, fulfilling Koch's postulates. N. clavispora is known to cause disease in a variety of plants in China, such as Dendrobium officinale (Cao et al., 2022), Fragaria ananassa (Shi et al., 2022), and Garcinia mangostana (Qiu et al., 2019). To the best of our knowledge, this is the first report of N. clavispora causing leaf blight on A. oblongum in China. The yellowing and falling off of leaves would seriously affects the garden landscape. It is necessary to further clarify the host range of the pathogen to select appropriate landscape matching plants in future planning.

First Report of Anthracnose on Wurfbainia villosa var. villosa Caused by Colletotrichum gloeosporioides in China.

Wurfbainia villosa var. villosa is a traditional Chinese herbal medicine under the family Zingiberaceae, and its ripe fruits (called Fructus Amomi) are widely used clinically for the treatment of gastrointestinal disorders (Yang et al. 2023; Chen et al. 2023). In September 2023, plants of W. villosa var. villosa exhibited anthracnose-like symptoms on leaf with a disease incidence of 35% (n = 100 investigated plants) in an approximately 90 m2 field in Guangning, China (N23°42'51.70″, E112°26'35.75″). Light yellowish-green spots (~2 mm diameter) initially appeared on the infected leaves, gradually formed sub-circular or irregular spots, then fused and expanded, resulting in wilting of the leaves. To identify the causal agent, 10 symptomatic leaves were collected and transferred to the laboratory. The symptomatic leaf samples were surface sterilized in 0.5% NaClO for 2 min, and in 70% ethanol for 30 s, then washed three times with sterile water and air-dried on sterile filter paper. The leaf tissues were placed on potato dextrose agar (PDA) medium containing 100 μg mL-1 of ampicillin (Sigma-Aldrich, St. Louis, MO) and incubated for 7 days at 28°C in darkness. Nine isolates with similar colony morphology were isolated from the 10 plated leaves. Three representative isolates (GNAF03, GNAF06, GNAF09 with approximately 3.5 cm in diameter after 3 days of incubation) appeared gray to dark brown with dense aerial hyphae at the front and gray to black colonies on the reverse of the plates. Conidia were cylindrical and measured 21.2 to 29.3 μm long × 7.1 to 9.6 μm wide (n = 50). Appressoria were formed by the tips of germ tubes or hyphae and were brown, ellipsoid, thick-walled, and smooth-margined, measuring 10.2 to 12.3 μm long × 6.4 to 8.2 μm wide (n = 50). Morphologically, the fungal isolates resembled Colletotrichum sp. (Weir et al. 2012). For molecular analysis, genomic DNA was extracted from fresh mycelia of the three isolates, and the primers ACT-512F/ACT-783R, CL1/CL2A, GDF/GDR, and ITS1/ITS4 were used to amplify partial regions of rDNA-ITS, actin (ACT), calmodulin (CAL), and glyceraldehyde-3-phosphate dehydrogenase (GAPDH) regions, respectively (Weir et al. 2012). The resulting sequences with more than 99% nucleotide identity to C. gloeosporioides were submitted to GenBank (accession numbers PP552725, PP552726, and OR827444 for ACT; PP552727, PP552728, and OR827443 for CAL; PP552729, PP552730, and OR827445 for GAPDH; PP549996, PP549999, and OR841394 for ITS). A phylogenetic tree was generated by the maximum likelihood method using the concatenated sequences of ACT, CAL, GADPH, and ITS by Polysuite software (Damm et al. 2020). Based on morphological and molecular analysis, the three isolates were characterized as C. gloeosporioides. The pathogenicity of the GNAF09 isolate was assessed on W. villosa var. villosa seedling leaves inoculated by spraying with 40 μL of conidial suspension at 106 conidia mL-1 or wounded with a sterile toothpick then inoculated with mycelial agar plugs (5 mm diameter). Control leaves were inoculated with 40 μL of sterile distilled water or agar plugs without mycelia. The inoculated plants were placed in a humid chamber at 28°C with 80% humidity and a 12 h light-dark photoperiod. Symptoms similar to those seen on naturally infected leaves were observed on all inoculated leaves after 7 days inoculation. Re-isolation was performed from 80% of the inoculated leaves and isolates were confirmed as C. gloeosporioides morphologically, confirming Koch's postulates, and by sequencing the ACT, CAL, GADPH, and ITS regions. The control groups remained asymptomatic. In previous studies, C. gloeosporioides has also caused anthracnose on Chinese medicinal plants, including Baishao (Radix paeoniae alba) (Zhang et al. 2017) and Rubia cordifolia L. (Tang et al. 2020). To our knowledge, this is the first report of C. gloeosporioides causing anthracnose on W. villosa var. villosa in China. The results of our report serve as valuable references for further research on this disease.

Ultrasensitive self-powered biosensor with facile chemical signal amplification strategy using hydrogen peroxide-triggered silver oxidation reaction

The amplification strategies used for self-powered biosensor based on biofuel cell (BFC-SPB) need to be further developed. Because the currently developed strategies utilized the complicated hybridization of DNA or poorly readable current signal of capacitors for amplification, which limits the practical application in public health emergencies. Here, we present a facile chemical amplification strategy for BFC-SPB. The 5-min amplification was triggered by simply adding H2O2 solution dropwise to the sensing cathode after the formation of the immune sandwich. The Ag NP of immunoprobe were oxidized to Ag(I), which can be served as the electron acceptor of the cathode. The amount of immunoprobe was positively correlated with that of the antigen, resulting in corresponding and high concentration of Ag(I) after the amplification, which enhanced the ability of the cathode as the electron acceptor. Meanwhile the glucose oxidation reaction (GOR) was performed on the bioanode modified with glucose oxidase (GOx). After assembling the bioanode and sensing cathode, the open circuit voltage of the BFC-SPB, measured by digital multimeter, distinctly rised with the elevated concentration of the antigen. To demonstrate the proof of concept, immunoglobulin G (IgG), selecting as a model analyte, was sensitively detected using this method. Result indicated that the limit of detection was 4.4 fg mL−1 (0.03 amol mL−1) in the linear range of 1 pg mL−1-10 μg mL−1. This work initiates a brand-new way of chemical amplification strategy for BFC-SPB, and offers a promising platform for practical applications.

Design, synthesis, and anti-mycobacterial evaluation of 1,8-naphthyridine-3-carbonitrile analogues.

Twenty-eight compounds, viz., 1,8-naphthyridine-3-carbonitrile (ANC and ANA) derivatives, were designed and synthesized through a molecular hybridization approach. The structures of these compounds were analyzed and confirmed using 1H NMR, 13C NMR, LCMS, and elemental analyses. The synthesized compounds were evaluated by in vitro testing for their effectiveness against tuberculosis using the MABA assay, targeting the Mycobacterium tuberculosis H37Rv strain. Their minimum inhibitory concentration (MIC) was determined, showing that the tested compounds' MIC values ranged from 6.25 to ≤50 μg mL-1. Among the derivatives studied, ANA-12 demonstrated prominent anti-tuberculosis activity with a MIC of 6.25 μg mL-1. Compounds ANC-2, ANA-1, ANA 6-8, and ANA-10 displayed moderate to good anti-tuberculosis activity with MIC values of 12.5 μg mL-1. Compounds with MIC ≤ 12.5 μg mL-1 were screened against human embryonic kidney cells to assess their potential cytotoxicity. Interestingly, these compounds showed less toxicity towards normal cells, with a selectivity index value ≥ 11. To further evaluate the binding pattern in the active site of enoyl-ACP reductase (InhA) from Mtb (PDB-4TZK), a molecular docking analysis of compound ANA-12 was performed using the glide module of Schrodinger software. The stability, confirmation, and intermolecular interactions of the cocrystal ligand and the highly active compound ANA-12 on the chosen target protein were investigated through molecular dynamics simulations lasting 100 ns. In silico predictions were utilized to assess the ADMET properties of the final compounds. A suitable single crystal was developed and analyzed for compound ANA-5 to gain a deeper understanding of the compounds' structures.

Ultrasonic high-yield extraction of non-toxic fucose-containing Abroma augusta polysaccharide bearing emulsifying properties.

The stem of Abroma augusta contains mucilaginous polysaccharides having numerous ethnomedicinal properties. The present work aimed to develop a scalable ultrasonic-assisted aqueous Abroma augusta mucilage (AAM) extraction (UAE) method and further explores its emulsifying property and toxicity concern. The combination of ultrasonic power (750 W), solid-to-liquid ratio (1:15) and temperature (348 K) gave the highest extraction yield of 2.28% with a diffusivity value of 3.85 × 10-9 m2 s-1, which was higher than aqueous extraction method using a kinetic model based on Fick's second law of diffusion. The extracted polysaccharide showed no toxicity as measured through 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assay on RAW cell line. Additionally, the polysaccharide over its critical micelle concentration (400, 500, 600 and 700 μg mL-1) offered emulsifying properties with 0.5%, 1% and 5% oil (v/v). The emulsion with a polysaccharide concentration of 600 μg mL-1 with 5% oil (v/v) provides stability against coalescence for 3 days. The overall findings indicated that UAE of AAM polysaccharide can be used for an efficient extraction method, and the obtained polysaccharide is nontoxic in nature and bears emulsifying properties. © 2024 Society of Chemical Industry.

Virus-Shaped Mesoporous Silica Nanostars to Improve the Transport of Drugs across the Blood-Brain Barrier.

Conditions affecting the brain are the second leading cause of death globally. One of the main challenges for drugs targeting brain diseases is passing the blood-brain barrier (BBB). Here, the effectiveness of mesoporous silica nanostars (MSiNSs) with two different spike lengths to cross an in vitro BBB multicellular model was evaluated and compared to spherical nanoparticles (MSiNP). A modified sol-gel single-micelle epitaxial growth was used to produce MSiNS, which showed no cytotoxicity or immunogenicity at concentrations of up to 1 μg mL-1 in peripheral blood mononuclear and neuronal cells. The nanostar MSiNS effectively penetrated the BBB model after 24 h, and MSiNS-1 with a shorter spike length (9 ± 2 nm) crossed the in vitro BBB model more rapidly than the MSiNS-2 with longer spikes (18 ± 4 nm) or spherical MSiNP at 96 h, which accumulated in the apical and basolateral sides, respectively. Molecular dynamic simulations illustrated an increase in configurational flexibility of the lipid bilayer during contact with the MSiNS, resulting in wrapping, whereas the MSiNP suppressed membrane fluctuations. This work advances an effective brain drug delivery system based on virus-like shaped MSiNS for the treatment of different brain diseases and a mechanism for their interaction with lipid bilayers.

Synthesis and characterization of new 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol (MMTP) Schiff base for spectrophotometric detection of iron(III) and copper(II) ions in laboratory and different water samples: A biological and molecular docking exploration

New spectrophotometric techniques were introduced for the determination of Fe(III) and Cu(II) in many different analyzed samples. The concentrations of Fe(III) and Cu(II) ions were measured in the existence of a novel Schiff base (Z)-6-(3-mercapto-5-methyl-4H-1,2,4-triazol-4-ylimino)-2-thioxotetrahydropyrimidin-4(1H)-one (MMTP). The new chelates were formed rapidly at the room temperature at 510 and 550 nm in presence of triton X-100 and CPB surfactants for Fe(III) and Cu(II), respectively. Linear calibrated graphs were obtained at concentration ranges of 1.0–130 µg mL-1 for Fe(III) and 0.5–90 µg mL-1 for Cu(II). LOD were calculated to be 1.05, 1.98 µg mL-1 and LOQ were 3.18 and 6.02 µg mL-1 for Fe(III) and Cu(II), respectively. A large number of foreign ions were not interfering in the present method. The stoichiometric composition of the chelates was studied by molar ratio and job´s methods to be found 1:2 (metal ion: ligand) ratio. The Fe(III) and Cu(II) solid chelates were prepared and characterized using IR, UV–Vis., 1HNMR , 13CNMR TG-DTG, and XRD spectroscopy. The IR spectral revealed that MMTP chelated as a bidentate ligand via NO atoms. Thermal analysis revealed the decomposition mechanism of MMTP and its chelates. A suggested octahedral geometry encompasses all of the chelates. The UV–visible spectra and magnetic moment analyses confirm the octahedral geometrical geometries. The band gap (Eg) values are 1.53 and 1.56 for Fe(III) and Cu(II) respectively. The smallest band gaps imply that these chelates are semiconductors belonging to solar materials. The in-vitro antioxidant activity of the individual chelates was evaluated using the DPPH radical scavenging assay. All compounds showed antioxidant activity with IC50 values of 0.316, 0.186 and 0.124 mg/mL for MMTP, Fe(III) and Cu(II), respectively. MMTP and its chelates were tested for their antimicrobial activity against various types of bacteria and fungi using the disc diffusion method. The Cu(II) complex showed the greatest biological activity.

Potential of the plant growth-promoting rhizobacterium Rhodococcus qingshengii LMR356 in mitigating lead stress impact on Sulla spinosissima L.

Mining-related lead (Pb) pollution of the soil poses serious hazards to ecosystems and living organisms, including humans. Improved heavy metal phytoremediation efficacy, achieved by using phytostabilizing plants assisted by plant-growth-promoting (PGP) microorganisms, has been presented as an effective strategy for remediating polluted soils. The objective of this research was to examine the response and potential of the plant-growth-promoting bacterium LMR356, a Rhodococcus qingshengii strain isolated from an abandoned mining soil, under lead stress conditions. Compared to non-contaminated culture media, the presence of lead induced a significant decrease in auxin production (from 21.17 to 2.65 μg mL-1) and phosphate solubilization (from 33.60 to 8.22 mg L-1), whereas other PGP traits increased drastically, such as 1-aminocyclopropane-1-carboxylic acid (ACC) deaminase activity (from 38.17 to 71.37 nmol mg-1 h-1 α-ketobutyrate), siderophore production (from 69 to 83%), exopolysaccharide production (from 1952.28 to 3637.72 mg mL-1), biofilm formation, and motility. We, therefore, investigated the behavior of Sulla spinosissima L. in the presence or absence of this strain under a variety of experimental conditions. Under hydroponic conditions, Sulla plants showed endurance to varying lead concentrations (500-1000 μM). Inoculation of plants with Rhodococcus qingshengii strain LMR356 enhanced plant tolerance, as demonstrated by the increase in plant biomass (ranging from 14.41 to 79.12%) compared to non-inoculated Pb-stressed and non-stressed control plants. Antioxidant enzyme activities (increasing by -42.71 to 126.8%) and chlorophyll (383.33%) and carotenoid (613.04%) content were also augmented. In addition to its impact on plant lead tolerance, strain LMR356 showed a growth-promoting effect on Sulla plants when cultivated in sterilized non-contaminated sand. Parameters such as plant biomass (16.57%), chlorophyll (24.14%), and carotenoid (30%) contents, as well as ascorbate peroxidase (APX), peroxidase (POD), and catalase (CAT) activities, were all elevated compared to non-inoculated plants. Furthermore, when the same plant species was cultivated in highly polluted soil, inoculation increased plant biomass and improved its physiological properties. These findings demonstrate that LMR356 is a phytobeneficial bacterial strain capable of enhancing Sulla growth under normal conditions and improving its heavy metal tolerance in multi-polluted soils. Thus, it can be considered a promising biofertilizer candidate for growing Sulla spinosissima L. or other selected plants intended for application in restoration and stabilization initiatives aimed at reviving and safeguarding environmentally compromised and polluted soils after mining activities.

Antifungal activity of propafenone on Candida spp. strains: interaction with antifungals and possible mechanism of action.

Introduction. The development of new antifungal drugs has become a global priority, given the increasing cases of fungal diseases together with the rising resistance to available antifungal drugs. In this scenario, drug repositioning has emerged as an alternative for such development, with advantages such as reduced research time and costs.Gap statement. Propafenone is an antiarrhythmic drug whose antifungal activity is poorly described, being a good candidate for further study.Aim. This study aims to evaluate propafenone activity against different species of Candida spp. to evaluate its combination with standard antifungals, as well as its possible action mechanism.Methodology. To this end, we carried out tests against strains of Candida albicans, Candida auris, Candida parapsilosis, Candida tropicalis, Candida glabrata and Candida krusei based on the evaluation of the MIC, minimum fungicidal concentration and tolerance level, along with checkerboard and flow cytometry tests with clinical strains and cell structure analysis by scanning electron microscopy (SEM).Results. The results showed that propafenone has a 50% MIC ranging from 32 to 256 µg ml-1, with fungicidal activity and positive interactions with itraconazole in 83.3% of the strains evaluated. The effects of the treatments observed by SEM were extensive damage to the cell structure, while flow cytometry revealed the apoptotic potential of propafenone against Candida spp.Conclusion. Taken together, these results indicate that propafenone has the potential for repositioning as an antifungal drug.

Bioactivity evaluation and active compounds identification of Symphoricarpos orbiculatus as potential botanical herbicide.

Evaluation of herbicidal activity and identification of active compounds are important bases for the development of new botanical herbicides. This study confirmed that Symphoricarpos orbiculatus has high herbicidal activities against mono-dicotyledonous weeds, including Echinochloa crusgalli, Digitaria sanguinalis, Amaranthus retroflexus and Portulaca oleracea. By bioassay-guided isolation, 12 compounds were isolated and identified from S. orbiculatus for the first time, including iridoids: naucledal (K1), loganin (K2), loganigenin (K3), loganin acid (K4), glucologanin (K5) and vogeloside (K6), as well as flavonoids: quercetine (K7), luteolin (K8), nobiletin (K9), astragalin (K10), isorhamnetin 3-d-glucoside (K11) and rutin (K12). Biological assays showed that iridoids are the main active ingredients of S. orbiculatus. The compounds of K5 and K6 could inhibit both the root (IC50 = 37.54 and 38.91 μg mL-1, respectively) and shoot (IC50 = 42.78 and 45.72 μg mL-1, respectively) of Portulaca oleracea, which have a weeding toxicity similar to that of the commercialized plant-based herbicide pelargonic acid. In addition, the results of pot culture assay showed that S. orbiculatus ethanol extracts had high fresh weight control effect against Digitaria sanguinalis and P. oleracea at the concentration of 40 g L-1. After 7 days, both the soil treatment and the stem and leaf spray method resulted in severe leaf necrosis and significant leaf etiolation. Symphoricarpos orbiculatus and its herbicidal active compounds have the potential to develop into botanical herbicides, and are first reported in the present study. © 2024 Society of Chemical Industry.

Apramycin has high in vitro activity against Mycobacterium tuberculosis.

Introduction. Aminoglycoside antibiotics such as amikacin and kanamycin are important components in the treatment of Mycobacterium tuberculosis (Mtb) infection. However, more and more clinical strains are found to be aminoglycoside antibiotic-resistant. Apramycin is another kind of aminoglycoside antibiotic that is commonly used to treat infections in animals.Hypothesis. Apramycin may have in vitro activity against Mtb.Aim. This study aims to evaluate the efficacy of apramycin against Mtb in vitro and determine its epidemiological cut-off (ECOFF) value.Methodology. One hundred Mtb isolates, including 17 pansusceptible and 83 drug-resistant tuberculosis (DR-TB) strains, were analysed for apramycin resistance using the MIC assay.Results. Apramycin exhibited significant inhibitory activity against Mtb clinical isolates, with an MIC50 of 0.5 μg ml-1 and an MIC90 of 1 μg ml-1. We determined the tentative ECOFF value as 1 µg ml-1 for apramycin. The resistant rates of multidrug-resistant tuberculosis (MDR-TB), pre-extensively drug-resistant (pre-XDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) strains were 12.12 % (4/33), 20.69 % (6/29) and 66.67 % (14/21), respectively. The rrs gene A1401G is associated with apramycin resistance, as well as the cross-resistance between apramycin and other aminoglycosides.Conclusion. Apramycin shows high in vitro activity against the Mtb clinical isolates, especially the MDR-TB clinical isolates. This encouraging discovery calls for more research on the functions of apramycin in vivo and as a possible antibiotic for the treatment of drug-resistant TB.

Effect of Combining Wuyiencin and Pyrimethanil on Controlling Grape Gray Mold and Delaying Resistance Development in Botrytis cinerea.

By screening the compounding combination of Wuyiencin and chemical agents, this study aims to delay the emergence of chemical agent resistance, and provide a technical reference for scientific and rational fungicides technology. This study investigated the impacts of the antibiotic wuyiencin derived from Streptomyces albulus var. wuyiensis and its combination with pyrimethanil on the inhibition of Botrytis cinerea. Treatment with wuyiencin (≥80 µg mL-1) strongly inhibited the pathogenicity of B. cinerea and activated the plant defense response against B. cinerea. Application of 80-100 µg mL-1 wuyiencin effectively controlled grape gray mold (by 57.6-88.1% on leaves and 46.7-96.6% on fruits). Consequently, the application of 80-100 µg mL-1 wuyiencin effectively mitigated grape gray mold incidence, leading to a substantial reduction in disease symptoms to nearly imperceptible levels. When wuyiencin (at the median effective concentration [EC50]) was combined with pyrimethanil (EC50) at a ratio of 7:3, it exhibited the highest efficacy in inhibiting B. cinerea growth. This combination was significantly more potent (p < 0.05) than using wuyiencin or pyrimethanil alone in controlling gray mold on grape leaves and fruits. Furthermore, the combination effectively delayed resistance development in gray mold. The experimental results show that wuyiencin can delay resistance development by affecting the expression of methionine biosynthesis genes and reducing the activity of the cell wall-degrading enzyme activity.