Chemistry & Biodiversity最新文献

Propolis is a natural bee product rich in phenolic and flavonoid compounds and is well known for its remarkable biological properties. In this study, the phenolic compositions of propolis samples collected from various localities in the Caucasus region of Türkiye were characterized using LC-MS/MS, and their antioxidant, antidiabetic, and antibacterial activities were also evaluated. LC-MS/MS analyses identified caffeic acid, ferulic acid, and p-coumaric acid as the major phenolic acid compounds, while pinocembrin, chrysin, and galangin were determined as the major flavonoid constituents. Overall, these findings indicate that the antioxidant capacity of propolis samples obtained from different regions may be particularly associated with these key phenolic and flavonoid compounds. Consistent with this composition, total phenolic and flavonoid contents ranged from 34.72 to 120.54 mg GAE/g and 6.88 to 47.19 mg QE/g, respectively. The extracts exhibited a relatively high antioxidant capacity, with FRAP values between 60.47 and 311.87 mg TE/g and DPPH IC₅₀ values ranging from 215.80 to 37.96 µg/mL. Regarding antidiabetic activity, the IC₅₀ values for α-amylase and α-glucosidase inhibition were determined as 5.86-3.47 and 12.22-5.02 mg/mL, respectively, indicating a pronounced antidiabetic potential. Antimicrobial analyses revealed activity against E. faecalis, B. cereus, E. coli, K. pneumoniae, and C. albicans. Overall, this study provides a comprehensive LC-MS/MS-based phenolic profile of Caucasian propolis and demonstrates its antioxidant properties together with its antidiabetic potential.

Curcuma caesia Roxb. (black turmeric) has long been used in Ayurveda and traditional medicine to treat various ailments. Considering the contribution of oxidative stress and inflammation to the development of various diseases, such as cancer, diabetes, and metabolic syndrome, the current study investigated the antioxidant and anti-inflammatory properties of C. caesia Roxb. rhizome methanolic extract (CCM), along with phytochemical profiling. Antioxidant activity experiments showed IC₅₀ values of 66.5 ± 8.81 µg/mL, 42.69 ± 5.78 µg/mL, and 132.35 ± 8.08 µg/mL, for DPPH, ABTS, and metal chelating assay, respectively. In the in vivo study, antioxidant and inflammatory mediator expression was evaluated, where the levels of TNF-α, IL-6, ALT, AST, and iNOS, were reduced, and IL-10 and SOD were increased significantly at high dose. Phytochemical characterization by UPLC-ESI-HRMS tentatively annotated curcumenol, curzerenone, furanogerenone, and germacrone as major compounds and zederone as a minor trace constituent. Molecular docking analysis was performed by targeting NF-κB, ERK, p38, JNK, and Nrf2 pathways, where docking scores ranged from -5.5 to -8.6 kcal/mol. Overall, these findings provide the mechanistic insights into the interconnection between the antioxidant and anti-inflammatory effects of CCM, highlighting its potential as a therapeutic agent against oxidative stress and inflammation-associated diseases.

This study provides an analysis of the endemic plant Mattiastrum paphlagonicum Bornm.(Synonym Paracaryum paphlagonicum (Bornm.) R.R. Mill), focusing on enzyme activity, secondary metabolite content, antioxidant capacity (DPPH, ABTS, and FRAP), as well as phenolic and flavonoid levels, all within the context of a hydroethanolic extract prepared from M. paphlagonicum and its biodiversity, for the first time. Rosmarinic acid and rutin were identified at concentrations of 87.56 ± 0.09  and 0.96 ± 0.15 mg/g of the plant extract, respectively. The total polyphenol and flavonoid contents were measured as 0.85 ± 0.004 mg gallic acid equivalent/mL and 0.077 ± 0.014 mg rutin equivalent/mL. The extract exhibited exceptionally strong DPPH radical-scavenging activity, with a value of 231.746 ± 0.009 mg ascorbic acid equivalents (AAE)/mL extract, and high ferric reducing antioxidant power (FRAP), reaching 168.229 ± 0.004 mg AAE/mL extract. The percentage inhibition for tyrosinase and carbonic anhydrase by the extract was 97.6 ± 0.011% and 77.07 ± 0.996%, respectively. The extract is a rich source of bioactive compounds and has considerable inhibitory effects on tyrosinase and carbonic anhydrase enzymes. These findings highlight the plant's potential for neuroprotective and renoprotective pharmacological applications.

The identification of antinociceptive compounds often relies on animal models such as zebrafish, in which TRPA1 activation induces hyperlocomotion. This study presents the first evaluation of the anti-inflammatory and antinociceptive properties of the europium complex [Eu(dbm)₃.LAP], derived from Lapachol, and investigates its possible interaction with the TRPA1 channel in adult zebrafish. The complex was administered intramuscularly, and its effects were compared with camphor and morphine controls. In vivo findings were integrated with in silico docking, molecular dynamics simulations, and predictive pharmacokinetic analysis. Eu(dbm)₃.LAP (40 mg/kg, oral) was effective specifically in the inflammatory phase, and its effect was blocked by camphor, indicating TRPA1 modulation. The compound also reduced carrageenan-induced inflammation and attenuated oxidative stress in nerve and liver tissues. In silico predictions indicated high intestinal absorption (∼100%), good blood-brain permeability (LogBB = 0.62), and low cardiotoxicity (pKi_hERG = 7.73). Docking revealed a binding energy of -8.1 kcal·mol^{- 1} with stable interactions involving LYS1046, TYR1049, and LYS1052. Molecular dynamics confirmed stability over 100 ns and preservation of key hydrogen bonds, supporting the modulatory potential observed in vivo.

Aegle marmelos (Rutaceae) and Syzygium aromaticum (Myrtaceae), have a rich use in Indian traditional medicine with broad-spectrum cures for a range of illnesses. Although crude extract of these plants was found to exhibit antimalarial potential, we employed bioassay-guided fractionation to isolate and purify the compounds responsible for the effect. For this purpose, in vitro assays using SYBR Green-I-based fluorescence tests and in silico molecular docking studies were employed. The methanolic extracts of A. marmelos leaves and S. aromaticum flower buds, alongside their fractions (hexane, chloroform, ethyl acetate, and methanol), were appraised against Plasmodium falciparum 3D7 strain. Further, cytotoxicity was assessed in HeLa cell lines by MTT assay. Comprehensive spectroscopic analyses, including NMR and IR, were carried out for bioactive compound structural characterization. On fractionation, purification, and characterization, four compounds were isolated from A. marmelos leaves and S. aromaticum flower buds, and they exhibited significant antimalarial activity. Lupeol, isolated from A. marmelos, exhibited the most significant effect with 94.0% inhibition and an IC₅₀ of 8.73 µg/mL. β-Sitosterol and 1,3-dimethylpyrimidine-2,4(1H,3H)-dione, also isolated from A. marmelos, showed moderate activity. Eugenol, isolated from S. aromaticum, displayed moderate antimalarial activity with an IC₅₀ of 19.30 µg/mL. The cytotoxicity investigation indicated a TC₅₀ value over 100 µg/mL for lupeol, whereas other drugs exhibited mild toxicity. Docking studies revealed binding affinities of -9.5 and -9.4 kcal/mol for lupeol and β-sitosterol, respectively, toward ribosome inhibitor protein, current candidate drug target of P. falciparum 3D7. Lead compounds were also advantageous with drug-likeness and safety profiles. These results scientifically substantiate the conventional utilization of A. marmelos and S. aromaticum as potential sources of antimalarial compounds.

The global health landscape continues to be challenged by cancer, prompting ongoing investigations aimed at developing treatments that are both less invasive and more effective. Photodynamic (PDT) and photothermal (PTT) treatments have gained prominence due to their efficacy in inhibiting tumors while minimizing impact on surrounding healthy tissues. The integration of these methodologies with fluorescent molecular imaging (FMI), recognized for its significant potential in early cancer detection, presents a compelling noninvasive treatment strategy. Near-infrared (NIR) fluorescent dyes, including cyanine dyes and boron-dipyrromethene (BODIPY) derivatives, along with aza-BODIPY derivatives, represent some of the most efficient organic small molecules employed in cancer FMI and phototherapy. Their robust tissue penetration, minimal light scattering, and reduced autofluorescence make these compounds highly suitable for biological applications. Aza-BODIPY, a derivative from the organoboron family of BODIPY, is notable for its exceptional spectral properties, featuring red-shifted absorption and elevated molar extinction coefficients that enhance both imaging and therapeutic outcomes. This study examines potential modifications to aza-BODIPY aimed at enhancing its effectiveness in phototherapy and cancer detection, thereby expanding its application as a versatile tool for effective cancer treatment strategies.

Lead hepatotoxicity was experimentally induced in rats, followed by treatment with antioxidant-rich rosemary (Rosmarinus officinalis) ethanol extract (REE). Lipid profile parameters, liver function markers, antioxidant enzymes (SOD, GSH, and MDA), free fatty acids, and HMG-CoA reductase levels were evaluated using standard biochemical assay kits and ELISA methods. REE exhibited high phenolic (56.69 ± 0.05 GAE/g) and flavonoid contents (8.41 ± 0.02 mg QE/g), and HPLC analysis identified quercetin, p-coumaric acid, caffeic acid, and rosmarinic acid as major phenolic constituents. Hepatic lead accumulation (2.70 ± 0.32; p < 0.05) not only caused significant body weight loss but also resulted in dyslipidemia and hyperglycemia, evidenced by elevated serum cholesterol (118 ± 5.69 mg/dL) and triglycerides (130 ± 4.34 mg/dL). Exposure to PbAc induced hepatotoxicity and oxidative stress, as shown by elevated ALT levels (65 ± 3.75 U/L), increased lipid peroxidation, and depletion of antioxidant defenses, especially GSH (17 ± 1.77 U/L) (p < 0.05). Treatment with REE or trans-resveratrol (RSV), either alone or in combination with PbAc, significantly attenuated lead-induced toxicity by restoring lipid homeostasis, antioxidant status, liver enzymes, and normal hepatic architecture (p > 0.05 vs. control). These findings demonstrate the hepatoprotective potential of REE, likely mediated by its antioxidant-rich phytoconstituents.

Type 2 Diabetes mellitus is a complex metabolic disorder often accompanied by oxidative stress, obesity, and dyslipidemia. The limitations of current treatments have increased interest in plant-derived compounds with multitarget potential. This study investigates the in vitro antidiabetic, anti-obesity, antihyperlipidemic, and antioxidant activities of ethanol extracts prepared from selected parts of eight plant species collected from various regions of Türkiye. Ethanol extracts of selected plant parts were evaluated for their inhibitory effects on α-glucosidase, α-amylase, pancreatic lipase, and cholesterol esterase. Antioxidant activities were assessed via DPPH radical scavenging, metal chelating, and ferric reducing power assays. Phytochemical contents were determined using spectrophotometric methods and LC-MS/MS profiling. Among the tested species, Euphorbia macroclada showed the most pronounced in vitro activity, including potent α-glucosidase inhibition (IC₅₀: 37.01 ± 3.37 µg/mL), strong DPPH radical-scavenging activity (89.34% ± 0.15%), and notable cholesterol esterase inhibition (IC₅₀: 79.99 ± 3.48 µg/mL). LC-MS/MS analysis of E. macroclada revealed a phenolic compound profile, with quinic acid and isoquercitrin as major constituents. Olea europaea (branch) and Cichorium intybus also exhibited notable α-glucosidase inhibitor and antioxidant activities. To the best of our knowledge, Silene vulgaris var. macrocarpa is reported here for the first time as a mild pancreatic lipase inhibitor, and the α-glucosidase inhibitory activity of the ethanol extract of E. macroclada is investigated for the first time in this study. Overall, these findings provide preliminary in vitro screening evidence and highlight promising candidates for further investigation; bioactivity-guided fractionation, enzyme kinetic studies, and validation in cellular and/or in vivo models are required before therapeutic conclusions can be drawn. In this study, Euphorbia macroclada was evaluated for its antidiabetic potential, and the results suggest it may be a promising candidate for further investigation.

Propolis is a polyphenol-rich natural resin with well-documented antioxidant activity; however, its practical application is restricted by poor aqueous solubility and limited stability. Herein, propolis-based organic-inorganic hybrid nanoflowers (Prp-Nfs) were synthesized by integrating a propolis extract into a Cu₃(PO₄)₂·3H₂O matrix under mild aqueous conditions (0.8 mM Cu^{2 +}, pH 7.4, 25°C, 72 h). SEM and laser diffraction analyses confirmed the formation of uniform spherical Prp-Nfs with a relatively narrow size distribution. EDX, FTIR, and XRD analyses verified the formation of well-integrated organic-inorganic hybrid architecture arising from interactions between copper ions and propolis-derived functional groups. Functionally, Prp-Nfs exhibited markedly enhanced peroxidase-like activity, reaching 2.76 EU mg^{- 1} at pH 7.4 and 40°C, while retaining 58.1% of their initial activity after five reuse cycles. Despite a lower total phenolic content, Prp-Nfs demonstrated superior DPPH radical scavenging activity (94.4%) together with a substantial ABTS antioxidant capacity (475.6 µmol Trolox g^{- 1}). Overall, these findings identify Prp-Nfs as a propolis-based hybrid nanozyme platform that combines peroxidase-like catalytic activity with enhanced antioxidant functionality.

The rise of multidrug-resistant (MDR) pathogens and the overharvesting of medicinal plants such as Prunus africana highlight the need for sustainable discovery platforms. In this study, the antimicrobial potential of 23 endophytic bacterial strains isolated from P. africana was evaluated. Stronger activity against Gram-negative than Gram-positive pathogens was observed (p < 0.001). Multivariate analysis identified six endophytic bacterial isolates that exhibited antimicrobial activity against all six tested pathogens. These were Ralstonia pickettii, Bacillus altitudinis, Stenotrophomonas maltophilia, Bacillus paramycoides, Sphingopyxis chilensis, and Virgibacillus halophilus. Gas chromatography-mass spectrometry (GC-MS) profiling of their ethyl acetate extracts revealed 74 metabolites, including terpenoids (e.g., 5-cedranone), phenolic acids (e.g., 4-hydroxybenzoic acid), diketopiperazines, and fatty acids (hexadecanoic, octadecanoic acids). The metabolomes showed biosynthetic congruence with the host plant producing analogous antimicrobial compounds alongside unique metabolites. These findings demonstrate that P. africana endophytes represent a sustainable, cultivable source of antibacterial agents active against Gram-negative pathogens, addressing both drug discovery and conservation needs.