Fraction F1 Research Articles

Bee pollen peptides as potent tyrosinase inhibitors with anti-melanogenesis effects in murine b16f10 melanoma cells and zebrafish embryos

One important functional food ingredient today, valued for its health properties and ability to prevent disease, is bee pollen, which comprises a combination of nectar, pollen from plants, and the secretions of bees. In this research, the tyrosinase (TYR) inhibiting abilities of the peptides derived from bee pollen protein hydrolysates are investigated. Various proteases were utilized to generate these peptides, followed by testing at different concentrations. Tyrosinase inhibition activity was detected in all cases, while the hydrolysate drawn from 5.0% w/v neutrase exhibited the best IC50 value and was thus investigated further via ultrafiltration to separate the active fractions. The highest potential for tyrosinase inhibition was recorded for the fractions below 0.65 kDa. Subsequent purification steps via SEC and RP-HPLC led to the identification of the VDGYPAAGY (named VY-9) peptide via LC-Q-TOF-MS/MS in fraction F1–2, known for its non-toxic and hydrophobic characteristics albeit poor water solubility. The synthesized VY-9 peptide demonstrated competitive inhibition, with IC50 values of 0.55 ± 0.03 µM for mono-phenolase and 2.54 ± 0.06 µM for di-phenolase activities, as confirmed by molecular docking analysis revealing dominant hydrogen bond interactions with TYR. Effective concentrations of 0.2–1.6 µM of VY-9 showed negligible cytotoxicity in B16F10 cells. Melanin synthesis suppression was examined via qRT-PCR, and western blot in MITF, TYR, TRP-1, and TRP-2. Cell death in zebrafish embryos was evaluated in vivo using a toxicity assay which revealed no significant influence from VY-9, while anti-melanogenic effects were observed when the concentration was 4 µM, suggesting bee pollen-derived peptides’ potential in cosmetic and pharmaceutical depigmentation applications.

Ligilactobacillus-Derived Extracellular Vesicles Inhibit Growth and Virulence of Enteric Pathogens.

Bacterial intra-kingdom communication involves the secretion of outer membrane vesicles as signaling carriers to the target cells. However, limited research exists on extracellular vesicles (EVs) from Gram-positive gut bacteria, their interactions with enteric pathogens, and potential inhibitory effects. In this study, we characterized the structure, protein content, and inhibitory effects of EVs from three new potential probiotic gut symbionts, Ligilactobacillus salivarius UO.C109, Ligilactobacillus saerimneri UO.C121, and Ligilactobacillus salivarius UO.C249. EVs were isolated and characterized using three different methods (ultracentrifugation, density gradient purification, and size exclusion chromatography). The purity, dose-dependency, structure, and proteome profiles of the purified EVs were evaluated. Antibacterial and anti-virulence activities of EV subpopulations were assessed against Salmonella enterica serovar Typhimurium and Campylobacter jejuni. EVs from Lg. salivarius UO.C109 and Lg. saerimneri UO.C121 showed inhibitory activity against S. Typhimurium, whereas EVs from Lg. salivarius UO.C249 inhibited the growth of C. jejuni. Notably, purified F3 fraction exhibited the highest inhibitory activity and was enriched in lysin motif (LysM)-containing proteins, peptidoglycan hydrolases, peptidoglycan recognition proteins (PGRPs), and metallopeptidases, which have been shown to play a prominent role in antimicrobial activities against pathogens. F3 had the highest concentration (73.8%) in the 80-90nm size compared to the other fractions. Gene expression analysis revealed that EVs from Lg. salivarius UO.C109 and Lg. saerimneri UO.C121 downregulated adhesion and invasion factors in S. Typhimurium. Likewise, EVs from Lg. salivarius UO.C249 reduced pathogenicity gene expression in C. jejuni. This study highlighted the potential of gut bacterial EVs as therapeutic agents against enteric pathogens.

Impacts of Different Vegetation Types on Soil Aggregate Stability in the Key Ecological Rehabilitation Area of the Tarim River Basin, Northwest China

Disentangling the responses of total soil organic carbon (SOC), organic carbon fractions and soil aggregate stability to various vegetation types is essential for better understanding the carbon cycling process in terrestrial ecosystems, maintaining soil quality and mitigating global warming. To study the effects of vegetation types on soil aggregates in a specific area, the desert riverbanks of arid regions were studied. We set up experiments using three typical vegetation types in the arid zone of the Tarim River Basin (TRB), including Forestland, Shrubland, and Grassland. The total SOC content in the bulk soil and different soil aggregates was determined by oxidation with K2Cr2O7 and H2SO4, and three carbon fractions (F1, very labile; F2, inert; F3, oxidizable resistant) were classified according to the degree of oxidation using the modified Walkley-Black method. The total SOC and three carbon fractions in the soil were significantly greater in the Forestland than in the other vegetation types, and the effect was more pronounced in macro-aggregate (MA) than in the other aggregates. In the bulk soil and soil aggregates, the percentages of F1, F2 and F3 in the total SOC with mean values of 0.36%, 0.28% and 0.36%, respectively, at soil depths of 0–20 cm, indicated that stabilizing carbon is the major carbon fraction of the SOC. The stability of the SOC in the aggregates across each vegetation type was greater in the lower layer (10–20 cm) than in the topsoil layer (0–10 cm). The SOC stability and MA content were positively related to the SOC in the soil aggregates and its F2 and F3 fractions (p < 0.05). In summary, the Forestland significantly increased the SOC content and enhanced SOC stability. Conservation measures for poplar forests in vulnerable arid zones can sustainably accumulate SOC sequestration.

Screening of a Fraction with Higher Amyloid β Aggregation Inhibitory Activity from a Library Containing 210 Mushroom Extracts Using a Microliter-Scale High-Throughput Screening System with Quantum Dot Imaging.

Alzheimer's disease (AD) is a highly prevalent neurodegenerative disease hallmarked by amyloid plaques and neurofibrillary tangles. Amyloid plaques are formed by the amyloid β (Aβ) aggregation, so substances that inhibit this aggregation are useful for preventing and treating AD. Mushrooms are widely used medicinal fungi with high edible and nutritional value. Mushrooms have a variety of biologically active ingredients, and studies have shown that they have certain effects in anti-bacterial, anti-oxidation, anti-inflammatory, anti-tumor, and immune regulation. Previously, we developed a microliter-scale high-throughput screening (MSHTS) system using quantum dot (QD) nanoprobes to screen Aβ aggregation inhibitors. In this study, we appraised the Aβ aggregation inhibitory activity of 210 natural mushrooms from Hokkaido (Japan) and found 11 samples with high activity. We then selected Elfvingia applanata and Fuscoporia obliqua for extraction and purification as these samples were able to suppress Aβ-induced neurocytotoxicity and were readily available in large quantities. We found that the ethyl acetate (EtOAc) extract of E. applanata has high Aβ aggregation inhibitory activity, so we performed silica gel column chromatography fractionation and found that fraction 5 (f5) of the EtOAc extract displayed the highest Aβ aggregation inhibitory activity among all mushroom samples. The half-maximal effective concentration (EC50) value was 2.30 µg/mL, higher than the EC50 of 10.7 µg/mL for rosmarinic acid, a well-known Aβ aggregation inhibitor. This inhibitory activity decreased with further purification, suggesting that some compounds act synergistically. The f5 fraction also inhibited the deposition of Aβ aggregates on the cell surface of human neuroblastoma SH-SY5Y cells. Our expectation is that f5, with additional tests, may eventually prove to be an inhibitor for the prevention of AD.

Phytol and bilimbi phytocompounds induce thermogenic adipocyte differentiation: An in vitro study on potential anti-obesity effects

BackgroundObesity is a major health concern associated to diabetes, cardiovascular disease, and cancer. Brown adipocytes, which specialise in thermogenesis, offer a potential therapeutic target for obesity prevention and related conditions. This study builds on previous findings of the browning activity of Averrhoa bilimbi hexane fractions and aims to elucidate the underlying mechanisms in vitro. Squalene and phytol, key phytocompounds from bilimbi leaf extract and fractions, were assessed for their ability to induce thermogenic adipocyte using 3T3-L1 preadipocytes and C2C12 myoblasts in vitro models. The result shows that bilimbi fractions F7, F8, and F9, along with squalene and phytol, effectively induced thermogenic adipocyte differentiation. This was evidenced by the upregulation of key markers, including Ucp1, Prdm16, and Pgc1α, and increased expression of the brown adipocyte-specific protein CIDEA in treated 3T3-L1 preadipocytes. Notably, all treatments promoted thermogenic adipocytes differentiation in C2C12 myoblasts via the upregulation of Pgc1α, Ucp1 genes, and UCP1 protein. These findings suggest that bilimbi fractions and its phytocompounds may hold potential as nutraceutical interventions for obesity management.

A new antibacterial neo-clerodane diterpenoid and other constituents from Chasmantheradependens Hochst. (Menispermaceae) and their chemotaxonomic significance

The leaves, stems and fruits methanol extracts of Chasmanthera dependens were chemically investigated to afford one new neo-clerodane diterpenoid (1) along with seventeen known compounds including three diterpenoids (2–4), six triterpenoids (5–10), four steroids (11–14), one sesquiterpenoid (15), one lignan (16) and two phenolic acids (17 and 18). Structures were established by analysis of their spectroscopic and spectrometric data and in comparison with those reported from the literature. Except columbin (2), compounds are reported for the first time from the genus Chasmanthera. The extracts, fractions, and isolated compounds were subjected to in vitro antibacterial assays against three Gram-positive and three Gram-negative bacteria, using the broth microdilution method. The MeOH extract of the leaves and its fractions F1–F4 had significant (MIC = 93.8 μg/mL for F4) or moderate (187.5 ≤ MIC ≤ 375 μg/mL) activities against Pseudomonas aeruginosa. Chasmantherenolide (1) was moderately active (MIC = 75 μg/mL, 202.6 μM) against Gram-positive bacterial strains. Significant antibacterial activity (MIC = 9.4 μg/mL, 20.6 μM) was recorded for oleanolic acid (7) against Mycobacterium smegmatis. The chemotaxonomic significance of the isolated compounds was discussed.

GC-MS Characterization and Bioactivity Study of Eucalyptus globulus Labill. (Myrtaceae) Essential Oils and Their Fractions: Antibacterial and Antioxidant Properties and Molecular Docking Modeling.

Eucalyptus globulus is a medicinal plant extensively used by the Moroccan population for treating a range of illnesses, especially respiratory conditions. This study aimed to assess the antioxidant and antibacterial properties of E. globulus essential oil and its individual fractions (F1, F2, and F3). Antioxidant activity was evaluated through iron-reducing power, 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays. Antibacterial activity was tested using disk diffusion and dilution methods, supported by molecular docking studies. Furthermore, GC-MS analysis was conducted on the essential oil and its individual fractions. GC-MS analysis identified the major compounds in the essential oil and its fractions as eucalyptol (62.32-42.60%), globulol (5.9-26.24%), o-cymene (6.89-24.35%), cryptone (7.10-15.95%), terpinen-4-ol (2.43-15.24%), and α-pinene (2.46-7.89%). Fraction F3 displayed the highest antioxidant activity in DPPH (IC50 = 3.329 ± 0.054 mg/mL) and ABTS assays (IC50 = 3.721 ± 0.027 mg/mL), while fraction F2 was most effective in the FRAP assay (IC50 = 1.054 ± 0.008 mg/mL). The essential oil and its fractions also showed antibacterial activity against Staphylococcus aureus, Staphylococcus epidermidis, Klebsiella pneumoniae, Enterobacter cloacae, Escherichia coli, and Acinetobacter baumannii. Molecular docking further corroborated these findings, supporting both antioxidant and antibacterial activities. The present findings demonstrate the antioxidant and antimicrobial properties of Eucalyptus globulus essential oil and its fractions, underscoring the need for further research to confirm their medicinal potential and explore pharmaceutical applications.

Predicting the Thermodynamic Solubility and Stability of Co-crystals and Eutectics of Febuxostat by using a Thermodynamic Model involving Flory Huggins Interaction Parameter.

A method is presented for determining the thermodynamic (equilibrium) solubility of a drug in coformer for the non-covalent derivative (NCD) systems i.e. eutectics/co-crystals. The method is based on a thermodynamic model to calculate the Gibbs energy change ∆GCC associated with forming a drug-coformer NCD system. This model includes contributions from heat capacity differences between the mixed and unmixed components, breaking up of the solid drug and coformer lattice structure, and drug ─ coformer mixing. Calculation of ∆GCC from thermal analysis data is demonstrated, and the equilibrium drug solubility in coformer is represented by minima of plots of ∆GCC versus the dissolved drug fraction(f1). Eight (8) coformer molecules, namely, 1-hydroxy 2-naphthoic acid (1H-2NPH), 4-hydroxy benzoic acid (4-HBA), salicylic acid (SLC), 4-amino salicylic acid (4-ASA), 5-nitro isophthalic acid (5N-IPH), pyrazinamide (PZD), isonicotinamide (ISNCT), and picolinamide (PICO) were used for the formation of NCDs of a highly water insoluble drug febuxostat (FXT). The importance of heat capacity and interaction parameter in determining the solubility behavior of drug-coformer in the formed NCDs was discussed. Further, ∆GCC for FXT in selected NCDs were plotted as a function of composition and temperature to determine the thermodynamic stability over the range of room temperature to formulation melting. It was concluded that the thermodynamic model can reasonably predict the maximum stable drug loading in a multi-crystalline system at a particular temperature, and serve as a complementary screening tool in determining the best stoichiometric ratio of the drug and coformer in terms of solubility and thermodynamic stability.

Schinus molle Resin Essential Oil as Potent Bioinsecticide Against Tribolium castaneum: Chemical Profile, In Vitro Acetylcholinesterase Inhibition, DFT Calculation and Molecular Docking Analysis.

Plants offer a bountiful source of natural pest control solutions through their essential oils. This research introduces and analyzes an eco-friendly natural essential oil for red flour beetle control. Therefore, the current study was included to show the chemical profile and the insecticidal efficacy of resin essential oil (REO) and its fractions (F1-3), resulting from chromatographic separation, from the plant Schinus molle against Tribolium castaneum adults. The trunk bark resin essential oil and its fractions' composition were analyzed by GC-MS. Overall, 33 constituents with 98.3% of the total EO composition were identified. REO and F1-3 displayed impressive repellent properties at a concentration of 0.12 µL/cm2. After 120 min of exposure, repellency ranged from 73.3% to a remarkable 96.7%. They also exhibited noteworthy fumigant properties, with median lethal doses of LD50 = 120.6-160.8 μL/L. The fractions F1 and F3 showed the most notable topical toxicity at a concentration of 10%, with LD50 values of 8.6% and 5.6%, respectively. Fractions F3 and F2 demonstrated the most effective inhibition of acetylcholinesterase (AChE) activity, providing insight into their insecticidal mechanisms. The in silico molecular docking and DFT studies corroborate the results of in vitro tests performed to identify new insecticide products derived from natural sources.

Evaluation of herbicidal potential of Siderophores produced by Amycolatopsis lurida strain 407

The urgent need for sustainable agriculture has intensified the search for environmentally friendly alternatives to chemical herbicides. This study investigates the herbicidal potential of siderophores produced by Amycolatopsis lurida strain 407, focusing on its effects on the growth of ryegrass and redroot weeds. Strain 407 exhibited two distinct colony morphologies—red and white—when cultured under varying environmental conditions. The cell-free culture filtrate (CFCF) from both colony types significantly inhibited the growth of ryegrass and redroot. The concentration of siderophore produced in the iron-deficient medium was measured to be 613.4 ppm for 407 red and 388.5 ppm for 407 white, which indicates significant iron chelating activity. This study also showed a direct relationship between the presence of siderophore in plant culture medium and reduced growth. Also, analysis of fractions of the aqueous phase resulting from column chromatography revealed that all fractions from the 407 red reduced ryegrass shoot length by up to 45% and root length by 83–86%, while redroot seedling length decreased by up to 36%. Fractions from 407 white completely inhibited germination or reduced ryegrass root length by up to 94% and redroot seedling length by 52%. Fractions F4 W to F7 W and F2 R to F8 R, which showed iron chelating activity were most effective in reducing plant growth, suggesting that there are metabolites, alone or in company with siderophores, synergistically do herbicidal activity. The innovative application of siderophores as bioherbicide presents a promising environmentally friendly alternative to chemical herbicides.

Antihyperglycemic and Hypolipidemic Activities of Flavonoids Isolated from Smilax Dominguensis Mediated by Peroxisome Proliferator-Activated Receptors.

Background/objetives: Mexican people use Smilax dominguensis as a traditional medicine for diabetes control. Some reports have shown an anti-hyperglycemic effect in animal models. In the current research, a chemical bio-guided fractionation in vitro and in silico was performed to identify compounds with anti-hyperglycemic and hypolipidemic effects through PPARγ/α dual agonist activity because they regulate genes involved in energy storage and burning, such as GLUT4 and FATP. Methods: The S. dominguensis extract was evaluated in mice through oral glucose tolerance tests. The bioactive extract was fractionated by open-column chromatography, and seven final fractions (F1-F7) were obtained and evaluated. C2C12 myoblasts were treated with the fractions, and the mRNA expression levels of PPARs, GLUT-4, and FATP were quantified. The most active fractions were evaluated on GLUT-4 translocation and lipid storage in C2C12 cells and 3T3-L1 adipocytes, respectively. Results: The F3 fraction increased the expressions of PPARγ, GLUT-4, PPARα, and FATP, and it induced GLUT-4 translocation and decreased lipid storage. F3 was then analyzed by NMR, identifying three flavonoids: luteolin, apigenin, and kaempferol. These compounds were analyzed by molecular docking and on PPAR expressions. Luteolin, apigenin, and kaempferol produced a discrete increase in the mRNA expression of PPARs. Luteolin and kaempferol also decreased lipid storage. Conclusions: Our findings indicate that the compounds identified in S. dominguensis exhibit dual agonist activity on PPARγ/PPARα and have the potential for the development of new therapeutic agents helpful in diabetes, obesity, or metabolic syndrome.

Exploring the traits and possible ecological risks of heavy metals in biochars derived from rice husk and sugar beet pulp.

This research investigated the properties and potential environmental hazards associated with biochars derived from rice husk (RH) and sugar beet pulp (SBP), both of which are rich in heavy metals (HMs). The results indicated that the concentration of various HM fractions is significantly affected by the type of feedstock and the pyrolysis temperature. Specifically, the total concentrations of HMs in biochars produced at 600°C were found to be 10-140% higher than those in the original biomasses, a phenomenon attributed to the precipitation of HMs. Cd was a notable exception, exhibiting a reduction of 3-7% in the resultant biochars when compared to biomass, likely attributable to its volatilization. The results also revealed that the F1 + F2 fraction of HMs were largely transformed into F3 + F4 fraction during combustion, indicating that pyrolysis may reduce the ecotoxicity of HMs present in contaminated biomass. However, the process did not effectively diminish the F1 and F2 fractions of Cr and Cd. Elevated pyrolysis temperature significantly enhanced the reduction of HMs phytoavailability. Specifically, the phytoavailability of HMs in biochars produced at 600°C exhibited a decrease ranging from 10 to 92% when compared to the original biomass. Conversely, an unexpected rise in the phytoavailable fractions of Cr and Cd was noted in both RH and SBP biochars as the pyrolytic temperature increased, which correspondingly raised the potential ecological risk index (PERI). All materials analyzed exhibited a very high risk level, with PERI values exceeding 800, primarily due to the significant toxicity of Cd. Excluding Cd from consideration, the biomasses and their resultant biochars displayed PERI values ranging from 7 to 13. It is important to acknowledge that pyrolysis may not effectively diminish the environmental toxicity associated with HMs present in contaminated biomass, thereby limiting its safe application.

Geochemical Characteristics and Environmental Risks of Cu in the Soil of A Sloping Vineyard (Phu Tho Province, Vietnam)

In the vineyards, the intensive use of cupric fungicides and fertilizers has resulted in Cu enrichment in the soils. Specifically, in sloping vineyards, the mobility of Cu can contribute to intensify the environmental risks. The research on geochemical characteristics of Cu is a key solution to explore the distribution of Cu in different geochemical fractions and understand the mobility and toxicity of this element in the environment. In this study, we aim to investigate the geochemical properties of Cu in the vineyard topsoil (0-20 cm) and subsoil (20-40-60 cm), using the improved three-step sequential extraction procedure developed by the Commission of the European Communities Bureau of Reference (BCR). In addition, the environmental risk is calculated by the environmental risk code (RAC) based on the percentage of Cu in the acid-soluble fraction. The results reveal that the mobility of Cu in the acid-soluble fraction (F1) and reducible fraction (Cu associated with the iron and manganese oxyhydroxides) (F2) tends to decrease with increasing soil depth. The major portion of Cu mostly exists in the strong bond with silicate clays (F4), accounting for 84% of total Cu content on average. Contrarily, the minor propotion of Cu associates with soil organic matter (F3) (3% on average). On the other hand, the content and proportion of Cu in the soil fractions are largerly influenced by basic soil properties (organic matter contents and fine soil particles). In addition, under the impact of soil erosion, higher percentages of F1 and F2 fractions of Cu are observed in the surface soil layers at the top of the hill compared to those at the backslope of the hill. The mean calculated RAC of 10.66%, 5.76%, and 5.38% for the 0-20 cm, 20-40 cm, and 40-60 cm soil layers, respectively, demonstrate a low risk to medium environmental risk level in the studied vineyard. Although an overall low risk level is observed for Cu in the studied vineyard soil, the deposition of Cu originating from repeated Cu-based pesticides and erosion is of particular concern in the vineyard soils.

Bioactive substances from Red ginger rhizome (Zingiber officinale Roscoe var. sunti Val) as Anti-atherosclerotic agent: Inhibition of Lipoxygenase in arachidonic acid metabolism

Atherosclerosis is a systemic disease, a combination of inflammatory conditions, endothelial dysfunction, and theaccumulation of lipids to form plaques in blood vessels. The inflammatory environment within the atherosclerotic lesion stimulates the lipoxygenase pathway of arachidonic acid metabolism, resulting in biosynthesis of the potent lipid inflammatory mediator. Our previous study showed fractions collected from n-hexane extract of red ginger rhizome has potential as NF-κB pathway inhibitor. This study aimed to examine its anti-inflammatory activity in macrophage cells and its effect on the lipoxygenase pathway also determined its metabolite profiles by gas chromatography–mass spectrometry (GC-MS) method. Results showed fraction F6 from red ginger n-hexane extract is a potent inhibitor of the lipoxygenase enzyme (IC50 36.40 ± 0.76 µg/ml), reduces the release of TNF-α and IL-6 cytokines, and inhibits lipid peroxidation(IC50 45.97 ± 5.14µg/ml).Not only high in 6-gingerol (194,99 ± 1,43mg/g extract), this fraction also contains zingerone, 6-paradol, and 6-shogaol which have been shown to have anti-inflammatory effects.

Aqueous Extracts of Rhus trilobata Inhibit the Lipopolysaccharide-Induced Inflammatory Response In Vitro and In Vivo.

Chronic noncommunicable diseases (NCDs) are responsible for approximately 74% of deaths globally. Medicinal plants have traditionally been used to treat NCDs, including diabetes, cancer, and rheumatic diseases, and are a source of anti-inflammatory compounds. This study aimed to evaluate the anti-inflammatory effects of Rhus trilobata (Rt) extracts and fractions in lipopolysaccharide (LPS)-induced inflammation models in vitro and in vivo. The aqueous extract (RtAE) and five fractions (F2 to F6) were obtained via C18 solid-phase separation and tested in murine LPS-induced J774.1 macrophages. Key inflammatory markers, such as IL-1β, IL-6, TNF-α, and COX-2 gene expression were measured using RT-qPCR, and PGE2 production was assessed via HPLC-DAD. The in vivo effects were tested in an LPS-induced paw edema model in Wistar rats. Results showed that RtAE at 15 μg/mL significantly decreased IL-1β and IL-6 gene expression in vitro. Fraction F6 further reduced IL-1β, TNF-α, and IL-6 gene expression, COX-2 expression, and PGE2 production. In vivo, F6 significantly reduced LPS-induced paw edema, inflammatory infiltration, and IL-1β and COX-2 protein expression. Chemical characterization of F6 by UPLC/MS-QTOF revealed at least eight compounds with anti-inflammatory activity. These findings support the anti-inflammatory potential of RtAE and F6, reinforcing the medicinal use of Rt.

Isolation of the active fraction of mace (Myristica fragrans Houtt) essential oil and their evaluation of antioxidant, antibacterial, and antiaging activities

This paper aims to isolate and identify the active fraction present in mace essential oil, as well as to evaluate its antioxidant, antibacterial, and antiaging properties. The chemical composition of the oil extracts and fraction were evaluated using gas chromatography-mass spectroscopy (GC-MS). Antioxidant and antibacterial activity were assessed using DPPH, ABTS, and Kirby–Bauer-Disc diffusion method. The antiaging activity of the active fractions was determined using Schizosaccharomyces pombe yeast as organism model. The GC-MS analysis revealed that the F3 fraction mainly contains a myristicin compound (34.37%). Results from the DPPH and ABTS assays demonstrated that the F3 fraction exhibited the highest antioxidant activity with half maximal inhibitory concentration values of 8.49 ppm and 8.10 ppm, respectively. Antimicrobial activity measurement confirmed that the F3 fraction displayed the strongest antibacterial activity against Staphylococcus aureus, with the diameter inhibition of 11.34 ± 0.32 ppm. Regarding antiaging activity, it was observed that the F3 fractions extended the lifespan of S. pombe at the concentrations tested. The F3 active fraction demonstrated the highest levels of antioxidant, antimicrobial, and antiaging activities.

Assessment of Piper longum L. (Piperaceae) leaves toxicity on the adults of Tribolium castaneum (Herbst, 1797) (Coleoptera: Tenebrionidae)

BackgroundNumerous insect pests attack stored grains causing both qualitative and quantitative losses. The most damaging pest that infests dry stored produce is the red flour beetle, Tribolium castaneum, a secondary pest of stored goods. This pest, especially in its adult stage, exhibits resistance to chemical insecticides, thereby rendering the traditional pesticides ineffective in controlling it. Phyto-derivatives, which are strong insecticides and also ecologically benign, have gained interest as non-chemical solutions for controlling this pest. Hence, the objective of this study was to investigate the potential of Piper longum leaf extract insecticidal action as an environmentally benign insecticide for the first time against the adults of T. castaneum. In this study, P. longum leaf ethanol extract was tested against the adults of T. castaneum by petri dish bioassay method. Ad hoc studies to verify significant mortality for the initial confirmation of adulticidal activity were conducted for 24 h at different dosages of 62.5, 125, 250, 500 and 1000 mg/L of P. longum leaf ethanol extract. Thereafter, dosages set at 10, 20, 30 and 40 mg/L for the fractions of P. longum leaf ethanol extract were conducted. Prior to this, the leaf extract of this plant was subjected to column chromatography for fractionation. The fractions tested for adulticidal activity were subjected to gas chromatography–mass spectroscopy.ResultsSignificant adulticidal action with 100% adult mortality was observed in ethanol extract of P. longum leaves. Among the fourteen fractions (F0–F13) obtained tested, only fractions, F5, F10 and F13, demonstrated adulticidal activity, and the remaining fractions displayed poor activity. One hundred per cent morality was noted in T. castaneum adults after 96 h at 40 mg/L in F5 and F10, and in F13 at 20 mg/L, and their respective LD50 values were 17.6, 26.6 and 10.0 mg/L. The fractions F5, F10 and F13 contained fatty acids, viz., hexadecanoic acid, dotriacontane and heptacosane in F5; tetradecanoic acid and nonadecanoic acid in F10; and octadecanoic acid, aspartame and tridecanoic acid in F13, revealed through gas chromatography–mass spectroscopy.ConclusionsThe results of the study showed that P. longum ethanol leaf extract revealed significant adulticidal activity and is a promising toxic agent to the adults of T. castaneum. The fatty acids in the ethanolic leaf extract fractions of P. longum could have caused toxicity to the adults of T. castaneum. According to the current literature survey, this is the first research report on the adulticidal activity of P. longum leaf extracts against the adults of T. castaneum.

Evaluation of antimalarial compounds in Prosopis africana stem bark fractions against Plasmodium berghei

Prosopis africana, a traditional medicinal plant for malaria treatment, requires further scientific evidence. This study aimed to assess the antimalarial potential of Prosopis africana stem bark fractions in Plasmodium berghei-infected mice and identify the responsible compounds. The aqueous extract underwent partitioning with n-hexane, ethyl acetate, and methanol, followed by antimalarial evaluation. F5 was the most potent fraction based on its antimalarial potential. The study pooled 36 chromatographic separation sub-fractions into five using TLC analysis Rf values. In Plasmodium berghei-infected mice, fraction F5 at 6.25, 12.5, 25, and 50 mg/kg body weight (bw) was tested for antimalarial activity. Compound analysis of F5 utilized ultra-performance liquid chromatography-quadrupolar mass spectrometry. Statistical analysis employed Analysis of Variance and Duncan's multiple range tests (p < 0.05). The methanol, n-hexane, and ethylacetate extracts displayed suppression of P. berghei by 90%, 72.2%, and 73.6%, respectively. Methanol, n-hexane, and ethylacetate extracts suppressed P. berghei by 90%, 72.2%, and 73.6% respectively. F5 showed significantly higher chemo-suppression (67.21%) than F1 (63.94%), F2 (6.99%), F3 (2.81%), and F4 (37.3%). At 12.5 mg/kg bw, F5 suppressed P. berghei by 91.09%, surpassing chloroquine (87.79%), and restored altered hematological indices and CD4+ counts. Compounds identified in F5 included caffeate, linalool, terpinene-4-ol, quinovic acid, quercetin, prosopinine, catechin, and apigeninin. In conclusion, the fraction F5 of P. africana stem bark exhibited higher antimalarial activity than chloroquine and the identified compound might likely contribute to its activity.

High-Throughput Screening System Evaluation of Andrographis paniculata (Burm.f.) Extracts and Their Fractions against Mosquito Vectors.

Infectious diseases that cause illness and/or death in humans can be contracted from mosquito bites. A viable and alternate method of personal protection that can lower the danger of human exposure to mosquito-borne diseases is the use of plant-based repellents. Using a high-throughput screening system, the current work examined the toxicity, contact irritancy, and spatial repellency of Andrographis paniculata crude extract and its fractions against Aedes aegypti, Anopheles minimus, and An. dirus. Five fractions (i.e., F1, F2, F3, F4, and F5) were separated from the crude extract by column and thin layer chromatography and analyzed using high-performance liquid chromatography and mass spectrometry. The major active compounds identified from F3 and F5 were 4-deoxy-11,12-didehydroandrographolide and andrographolide. Three concentrations (1.0, 2.5, and 5.0%) for each of the crude extracts and the five fractions were individually impregnated on nylon netting strips and evaluated against the three mosquito species. Results showed that the highest contact irritancy was elicited by the crude extract at 5% concentration against Ae. aegypti (43.70% escaped). Results of the spatial activity index (SAI) showed that fractions F3 and F5 at 2.5% demonstrated the strongest repellency against Ae. aegypti (SAI = 0.84) and An. minimus (SAI = 0.83), respectively. Both the crude extract and its components did not cause any knockdown or mortality. These findings suggest that fractionation of A. paniculata extracts is valuable in assessing their spatial repellent efficacy against mosquitoes. Fractions F3 and F5 hold promise as natural mosquito repellents and could contribute to developing effective mosquito control strategies.

Development of sustainable Lignin-Based coatings for layered double Hydroxides: Enhancing synergistic Anti-Aging properties in bitumen

Layered Double Hydroxides (LDHs) have poor dispersibility in bitumen and limited effectiveness in enhancing its thermal oxidative aging resistance. To address these issues, this study aims to purify lignin to improve its radical scavenging efficiency and use the purified lignin to coat LDHs (Φ@LDHs), thereby increasing their lipophilicity and radical scavenging efficiency for use in bitumen. sodium lignosulfonate (SL) was fractionated into five parts using a stepwise water/ethanol fractionation method, and these fractions were then applied to coat the LDHs to produce Φ@LDHs. The morphology, antioxidant activity, and chemical structure of Φ@LDHs were analyzed. Subsequently, the effect of Φ@LDHs on the aging properties of bitumen was evaluated. The test results indicated that SL and its fractions effectively coated the surfaces of LDHs, thereby enhancing their interlayer spacing and hydrophobicity. Among all fractions, lower molecular weight fractions, F4 and F5, retained most of the phenolic hydroxyl groups in SL, demonstrating significant antioxidant activities. The incorporation of F4@LDHs and F5@LDHs effectively mitigated changes in rheological properties of bitumen and oxidation product formation during thermal oxidation and UV aging, with F5@LDHs showing the best performance. Furthermore, a synergistic anti-aging mechanism was elucidated for the F4@LDHs and F5@LDHs composites. The purified F4 and F5 fractions not only improved the compatibility of LDHs with bitumen but also delayed the oxidative reactions initiated by free radicals to achieve a synergistic anti-aging effect.