Chemistry & Biodiversity最新文献

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.

Panax ginseng is a well-known medicinal and edible plant rich in polysaccharides. However, research on the impact of microwave power (MP) on ginseng polysaccharides (GPs) remains limited. This study investigated the effects of varying MP (300-700 W) on the structure and bioactivity of microwave-extracted polysaccharide (MEP) using spectroscopy, and chromatography, and by evaluating antioxidant, antitumor, and immunomodulatory activities. The results were determined under the extraction conditions of 300 and 700 W that showed the polysaccharide yield (40.15% vs. 47.97%), content (85.77% vs. 88.60%), and the IC₅₀ values for ·OH scavenging ability (7.67 ± 0.25 mg/mL vs. 8.53 ± 0.18 mg/mL). The inhibition rates against HeLa cells at a polysaccharide concentration of 10 mg/mL were 26.78% and 1.08%, respectively. The release of nitric oxide (NO) at a polysaccharide concentration of 250 µg/mL was 2.23 and 1.82 µmol/L, respectively. Notably, the polysaccharides obtained at 700 W exhibited weak bioactivity, primarily due to severely damaged structure characterized by extensive O-glycosidic bond cleavage, a significant reduction in molecular weight, and the worst thermal stability. Overall, these findings emphasize how MP affects polysaccharide structure and function, offering critical insights for processing other plant-derived polysaccharides.

Parkinson's disease (PD) is characterized by advanced neuronal degeneration, mitochondrial impairment, and aberrant lipid metabolism. Emerging evidence suggests that dysregulated sphingolipid biosynthesis, particularly through the upregulation of serine palmitoyltransferase (SPTLC1), contributes to the pathogenesis of PD. This study investigates the neuroprotective potential of Zanthoxylum armatum essential oil (ZAEO) in an MPP⁺-induced SH-SY5Y cell model of PD, focusing on modulation of SPTLC1 expression and associated neurotoxicity. GC-MS (Gas Chromatography-Mass Spectroscopy) analysis identified 28 phytoconstituents in ZAEO, accounting for 99.9% of its composition, with linalool (66.74%) and limonene (17.78%) as the principal components. ZAEO treatment significantly attenuated MPP⁺-induced cytotoxicity, restored neuronal nuclear marker NeuN (Neuronal nuclei), and notably suppressed the overexpression of SPTLC1, a key enzyme driving ceramide accumulation and mitochondrial stress in PD pathology. Immunofluorescence and cell viability assays corroborated these protective effects. Furthermore, molecular docking of ZAEO constituents with SPTLC1 (PDB ID: 7K0K) revealed high-affinity binding of minor compounds, including phellandral, humulene, and (-)-carvone, suggesting direct interactions with the enzyme and potential inhibition. These findings underscore the ability of ZAEO to mitigate neurodegeneration by modulating the sphingolipid axis and support its development as a multi-targeted phytotherapeutic strategy for Parkinson's disease.

The extraction methods significantly affect the yield and structure of polysaccharides. Based on single-factor experiments, response surface methodology optimized ultrasound-assisted extraction conditions for corn silk polysaccharides (CSP): liquid-to-solid 43 mL/g, extraction time 3 h, and ultrasonic power 640 W, yielding 5.83% CSP. Sulfated, phosphorylated, and selenylated derivatives (CSP-S, CSP-P, and CSP-Se) were prepared with substitution degrees of 0.6 and 0.4, and selenium content of 5.3%, respectively. After confirming structures by UV, FT-IR, SEM, monosaccharide, and Congo-red analyses, the bioactivities of the modified CSP were compared. All derivatives improved antioxidant capacity in vitro: phosphorylation boosted DPPH scavenging, while sulfation enhanced hydroxyl and superoxide anion radical elimination. Selenylation markedly inhibited the activities of α-amylase and lipase, and promoted glucose consumption in HepG2 cells, demonstrating hypoglycemic potential. Moreover, all polysaccharides enhanced RAW264.7 cell viability, phagocytosis, and nitric oxide (NO) release, with CSP-S being most effective. Chemical modifications markedly improved CSP bioactivities, highlighting their application prospects.

Gastric ulcers are common gastrointestinal lesions resulting from oxidative stress and inflammation. Artemisia herba-alba, a medicinal plant with antioxidant and anti-inflammatory properties, was evaluated for its curative effects against acetic acid-induced gastric ulcers in Wistar rats. The aqueous leaf extract was characterized by LC-MS and qualitative screening, and the major compound, quinic acid, was analyzed through in silico ADMET and molecular docking studies. In vitro assays assessed antioxidant activity, while in vivo experiments involved ulcer induction with 3% acetic acid and restraint stress for 8 days. After ulcer induction, rats received either no treatment or the extract (100 or 200 mg/kg) for 3 days. Gastric tissues were analyzed macroscopically, microscopically, and biochemically for oxidative stress markers. The extract showed moderate radical scavenging capacity, and docking results indicated strong binding of quinic acid to key antioxidant enzymes. ADMET predictions revealed favorable pharmacokinetic and safety profiles. Treatment significantly reduced the ulcer area, improved gastric pH, and restored antioxidant enzyme activities in a dose-dependent manner. Histological evaluation confirmed marked mucosal healing, particularly at 200 mg/kg. These findings indicate that Artemisia herba-alba extract accelerates gastric healing through antioxidant and anti-inflammatory mechanisms, supporting its traditional use and therapeutic potential in ulcer management.