Search Results (105)

Natural coumarins are a structurally privileged group of bioactive benzopyranone lactones widely spread across the Apiaceae, Rutaceae, and Leguminosae families, and hold significant potential as inhibitors of pathological protein aggregation in Alzheimer’s disease, Parkinson’s disease, and type 2 diabetes mellitus. The fully planar, rigid bicyclic structure of the coumarin nucleus (~3.4–3.5 Å thickness) is geometrically compatible with intercalative π–π stacking with aggregation-nucleating aromatic residues, including Phe19 of Aβ(1–42), providing a mechanistically coherent pharmacophoric basis for anti-aggregation activity according to computational and indirect biophysical evidence. This review critically evaluates the peer-reviewed literature on naturally occurring coumarins and their synthetic derivatives as candidate β-sheet intercalators, with analysis of SAR at C-3 to C-8 positions; multi-target-directed ligand designs with dual activities of inhibiting AChE, BACE-1, GSK-3β, and MAO-B, and as blood–brain barrier-penetrating neuroprotective agents validated in cellular and rodent models. The critical analysis identifies the translational gap between in vitro IC₅₀ values and attainable brain drug concentrations as the primary pharmacological obstacle. It identifies the absence of systematic investigation of coumarin against IAPP, a directly relevant amyloid target in metabolic neurodegeneration, as the most significant unmet research priority in the field. Full article

Cortex Dictamni, the dried root bark of the plant Dictamnus dasycarpus Turcz. from the Rutaceae family, contains alkaloids as its primary bioactive components, which exhibit a wide range of pharmacological effects. This study aims to optimize the extraction process and to characterize the chemical composition of Cortex Dictamni extract (CDE), as well as to evaluate its in vitro antioxidant and antibacterial activities. The response surface methodology (RSM) was employed to optimize the extraction process of CDE, while Q-Orbitrap high-resolution liquid chromatography–mass spectrometry (LC-MS) was utilized to identify the chemical components in the CDE. Antioxidant and antibacterial activities were evaluated using ABTS and DPPH radical scavenging assays and by determining the minimum inhibitory concentration (MIC), respectively. The results indicated that the optimized extraction yield of CDE was 44.73%. The optimal extraction conditions were: ethanol concentration of 70%, material-to-liquid ratio of 1:40 g/mL, and extraction time of 35 min. A total of 10 components were identified in the extract, including alkaloids, lactones, terpenes, and flavonoids. The extract demonstrated notable oxygen-free radical scavenging capabilities, as evidenced by its DPPH (IC50 = 0.316 mg/mL) and ABTS (IC50 = 0.166 mg/mL) values. Additionally, it exhibited antibacterial effects, particularly against Escherichia coli and Pseudomonas aeruginosa, with a minimum inhibitory concentration (MIC) of ≥128 mg/mL. CDE may serve as a potential natural compound for applications in the food and pharmaceutical industries. Full article

Phellodendri amurensis Cortex is the dried bark of the cork tree (Phellodendron amurense Rupr.) from the Rutaceae family, and possesses traditional efficacy in clearing heat, drying dampness, purging fire, relieving steaming sensations, detoxifying, and healing sores. Clinically, it is commonly used for treating symptoms such as damp-heat diarrhea and dysentery, jaundice with reddish urine, leukorrhea with vaginal itching, painful and difficult urination due to heat strangury, flaccidity and weakness of the lower limbs, bone-steaming and consumptive fever, night sweats and seminal emission, sores, ulcers, swellings, and toxins, eczema, damp sores, and urinary tract infections. Modern pharmacological studies have further revealed its diverse bioactivities, including antioxidant, antibacterial, anti-inflammatory, immunosuppressive, and anticancer effects. To provide an updated and comprehensive review of the research into Phellodendri amurensis Cortex, this study conducted a thorough literature search and analysis based on databases such as SciFinder, Web of Science, and China National Knowledge Infrastructure. The review integrates information on the plant’s botanical characteristics, geographical distribution, traditional applications, chemical components, quality control methods, and pharmacological effects to present a current and holistic overview of its research status. To date, approximately 170 compounds have been isolated and identified from Phellodendri amurensis Cortex, primarily including alkaloids, phenolics, terpenoids, sterols, lignans, flavonoids, and others. Among these, alkaloids exhibit significant antioxidant and anti-inflammatory activities and demonstrate potential pharmacological value in antibacterial, anticancer, hypoglycemic, and multi-organ protective effects. Although substantial foundational research exists, the mechanisms of action and quality control of Phellodendri amurensis Cortex require further in-depth exploration. Future efforts should focus on clarifying its pharmacodynamic material basis, uncovering new targets and pathways, and improving analytical methods for component analysis and quality control to advance the scientific development and rational utilization of this medicinal material. Full article

Essential oils (EOs), complex volatile compounds synthesized by plants, represent a vital class of natural products that are increasingly significant in scientific research due to their diverse biological properties and broad-spectrum medicinal applications. This study provides a comprehensive overview of EOs, commencing with a historical perspective and detailing their applications. It systematically catalogs their primary botanical sources, with specific examples of the most common and important plant families, including Lamiaceae (e.g., sage, oregano, thyme), Verbenaceae (vervain), Magnoliaceae (magnolia), Rutaceae (lemon), Myrtaceae (eucalyptus) and Lauraceae (cinnamon). A key focus is their antifungal activity, including the bioactive constituents involved and their mechanisms of action, with particular emphasis on their defense against pathogenic postharvest fungi. This includes an analysis of the key bioactive constituents responsible for these bioeffects and an exploration of their possible mechanisms of action against phytopathogenic fungi, with particular emphasis on postharvest pathogens infecting several crops. The discussion further highlights the role of EOs as sustainable alternatives to synthetic fungicides for controlling plant diseases that avoid the negative ecological and public health impacts associated with conventional agrochemicals. The study addresses these objectives by describing methods for testing antimicrobial efficacy, including kill-time studies, LD₅₀ determination, growth-curve analysis, the poisoned food technique, Spore-germination assays, and metabolic CO₂ measurement. The current review also highlights some recent studies reviewing the in vitro and in vivo antifungal performance of specific EOs against postharvest diseases. Full article

Several members of the Rutaceae (citrus) family are widely cultivated and processed. Tocopherol (T) synthesis and composition are well-documented, while tocotrienols (T3) in most plant families remain underreported. To amend this, mass screening of Rutaceae species’ seed tocochromanols were analysed. Of the 53 analysed species, seed tocochromanols were tocotrienol-dominated in 22 species, including a majority of species Zanthoxyloideae (Choisya, Dictamnus, Melicope, Ptelea, Skimmia, Tetradium, Zanthoxylum) and the Cneoroideae (Cneorum) subfamily. Total tocochromanol content ranged from 0.20–25.98 mg 100 g⁻¹ dry weight (dw) seeds. The highest tocochromanol content was observed in Murraya paniculata, Ruta graveolens seeds, the highest tocotrienol (T3) content was observed in Skimmia anquetilia and Dictamnus albus—19.80 and 19.70 mg 100 g⁻¹ dw, respectively. The major tocochromanols in the seeds were γ-T and γ-T3, while others were present in low concentration or absent. Linear discriminant analysis (LDA), principal component analysis (PCA) and non-hierarchal cluster analysis (N-HCA) identified similar tocochromanol content trends in the Rutoideae subfamily species and the Bergera and Murraya genus, while the Zanthoxyloideae subfamily species’ seed tocochromanol composition was highly variable. The efficient extractability of tocochromanols using sustainable solvent–ethanol is demonstrating suitability of this approach for daily samples screening and bioactive extraction. Full article

Ptelea trifoliata L. is a perennial plant of the Rutaceae family and contains secondary metabolites with potential biological relevance. Due to limited information on its activity, the objective of this study was to evaluate the biological properties of its flower extracts and to determine their phytochemical composition. Flowers were dried and subjected to ultrasound-assisted extraction using methanol, 60% methanol and water. LC–MS/MS was used for qualitative profiling, HPLC for quantitative determination, and spectrophotometry for measuring total phenolic and flavonoid content. The antioxidative capacity of the extracts was determined using DPPH, CUPRAC, FRAP, and iron chelation assays. Enzymatic inhibition analyses were performed for hyaluronidase, indicative of anti-inflammatory properties, and tyrosinase, associated with pigmentation mechanisms. The wound-healing capacity was evaluated in vitro using a scratch assay. Our research revealed the highest levels of polyphenols in the 60% methanol extract and of flavonoids in the methanol extract. The occurrence of chlorogenic acid, rutin, hyperoside, and astragalin was also demonstrated. Both methanol and 60% methanol extracts demonstrated antioxidant effects. The methanol extract showed the greatest hyaluronidase inhibition, while the 60% methanol extract was the most effective in suppressing tyrosinase activity and promoting wound closure. Principal component analysis showed that the contents of polyphenols or flavonoids were associated with enzyme-inhibitory or antioxidant activities. Moreover, the 60% methanol and water extracts exhibited notable wound healing properties. These results highlight the antioxidant, enzyme-modulating and regenerative potential of P. trifoliata flower extracts, suggesting their possible use in biomedical and dermatological applications. Full article

Fleas have major veterinary and public health relevance by causing dermatopathies and transmitting zoonotic agents. The limitations and environmental impact of synthetic insecticides have driven the search for safer and more sustainable tick control alternatives, such as essential oils (EOs) and their bioactive compounds. We conducted searches in the PubMed, Scopus and Google Scholar databases (May–August 2025), using predefined inclusion and exclusion criteria, resulting in 25 studies. The species investigated most was Ctenocephalides felis, followed by Xenopsylla cheopis. The most common botanical families were Lamiaceae, Cupressaceae, Rutaceae, and Lauraceae, comprising 48 plant species. For C. felis, the EOs of Cinnamomum spp., Ocimum gratissimum, Syzygium aromaticum and Piper aduncum showed the most pronounced insecticidal effects, as did their bioactive compounds cinnamaldehyde, eugenol, and dillapiole, respectively. For X. cheopis, the EOs of Cinnamomum verum, Calocedrus decurrens, and Salvia rosmarinus were the most effective. Essential oils from different plant species also exhibited repellent activity against C. felis, Pulex irritans and Diamanus montanus. In summary, essential oils and their bioactive compounds have promising potential for the control of fleas of medical and veterinary importance, representing sustainable alternatives with reduced environmental impacts. Full article

Zanthoxylum caribaeum Lam. is a member of the Rutaceae Family that can be naturally found in South and central America (Brazil, Paraguay, Bolivia, Caribbean, etc.). Its traditional medicinal uses are well documented among native communities, such as that of the Guarani, in Paraguay. More than 60 metabolites, including alkaloids, terpenoids, coumarins, and alkylamides, have been identified in its leaves, bark, and fruits. The biological activities and mechanisms of action of several of these compounds, as well as those of crude extracts, have also been investigated by previous studies. As a medicinal and edible plant, Z. caribaeum shows promising applications in the pharmacological industry. For the last 25 years, a significant amount of research has been conducted with Z. caribaeum to better understand its toxicity and complex mechanisms of action, bringing science-based clinical safety to its traditional uses. This review integrates available knowledge chemical and biological data on this species. It emphasizes the diversity of bioactive metabolites, their associated bioactivities, and provides an updated overview of the plant’s advances in ethnopharmacology, phytochemistry, pharmacology, agricultural exploitation, and potential utilization. Full article

Melicope pteleifolia (Rutaceae) is a shrub or tree with high medicinal value. Although the physical features of M. pteleifolia are evident, the mitochondrial (mt) genome has yet to be investigated, and its evolutionary relationship within Rutaceae is unclear. The organelle genomes of M. pteleifolia were constructed using Nanopore and Illumina sequencing data. The circular mt genome is 780,107 base pairs (bp) long, with a GC content of 44.85%. It has 66 genes, consisting of 33 protein-coding genes (PCGs), 30 tRNA genes, and 3 rRNA genes. The length of the chloroplast (cp) genome was 158,987 bp, containing 88 PCGs, 37 tRNAs, and 8 rRNAs. The mtDNA and cpDNA contained 507 and 353 repetitive sequences, respectively. RNA editing sites were abundant in M. pteleifolia organelle genomes, including 323 sites in mtDNA and 260 sites in cpDNA. Phylogenetic research using the cp and mt genomes of M. pteleifolia and nine additional species of the Rutaceae family precisely delineates its evolutionary and taxonomic position. Ka/Ks and nucleotide diversity indicated that the majority of the PCGs in the mitochondrial genome had experienced negative selection. These findings provided comprehensive information on the M. pteleifolia mitogenome for studying phylogenetic relationships in Rutaceae, with chloroplast-derived sequences providing critical evidence for inter-organellar genome evolution. Full article

Huanglongbing (HLB), also known as citrus greening, is a devastating disease affecting the citrus industry worldwide. This study aimed to investigate the transcriptional responses of two Rutaceae species, Ponkan Mandarin (susceptible) and Punctate Wampee (resistant), to HLB infection. Comparative transcriptome analysis was conducted to identify differentially expressed genes (DEGs) and pathways involved in defense mechanisms. The transcriptome data showed that in the susceptible Ponkan Mandarin, there were 1519 upregulated genes and 700 downregulated genes, while in the resistant Punctate Wampee variety, there were 1611 upregulated genes and 1727 downregulated genes. Upon infection, 297 genes were upregulated in both varieties, while 211 genes were downregulated in both. These genes included transcription factors from different families such as WRKY, ERF, and MYB. Ponkan Mandarin primarily relies on pathways like lignin synthesis and cell wall modification to defend against HLB, whereas Punctate Wampee mainly resists HLB by regulating cellular homeostasis and metabolism. Weighted Gene Co-expression Network Analysis (WGCNA) identified ten potential key resistance genes in the resistant Punctate Wampee variety, including genes involved in lignin biosynthesis and genes related to cellular signaling pathways. These findings not only enhance our understanding of the distinct defense mechanisms employed by citrus species against HLB infection but also offer novel perspectives for developing effective prevention and management strategies against this disease. Full article

Citrus lumia Risso is an ancient, cultivated Mediterranean lime belonging to the Rutaceae family. It is a species extremely difficult to retrieve, but it is still found in some private gardens in certain regions of Southern Italy. Citrus fruits are a rich source of bioactive compounds, particularly polyphenols, which have been linked to a reduction in the risk of several metabolic diseases. Here, hesperidium peel extracts were obtained by maceration with ethanol:water mixtures in different proportions (50:50, 80:20, 0:100) and the resulting crude extracts were then passed through a glass column containing adsorbent resins to concentrate the polyphenolic compounds. After phytochemical characterization, the extracts were evaluated for antioxidant activity using electron paramagnetic resonance (EPR) spectroscopy. Finally, the water polyphenolic-rich extract (ClumWp), which was the extract with the highest flavonoid content (18.355 ± 1.607 mg/mL) and the strongest antioxidant activity against hydroxyl radical, was tested to evaluate its potential protective effects on lipid accumulation in both 2D hepatocyte cultures and 3D spheroids. Treatment with 25 and 50 μg/mL resulted in a reduction in intracellular lipid content in the HepG2 liver cell line, while treatment with 100 µg/mL ClumWp resulted in a reduction in the intracellular lipid content in HepG2 + LX2 spheroids. In addition, treatment with ClumWp significantly increased ATP levels in the spheroids compared to those untreated, suggesting its ability to restore and promote ATP production. Our results highlight that the study of neglected species, such as Citrus lumia Risso, remains a valuable opportunity to valorize Mediterranean biodiversity, especially in the context of its potential applications to improve human health. In particular, the polyphenolic fraction of Citrus lumia peel showed promising effects on lipid metabolism and cellular energy balance and may prove valuable in the treatment of metabolic disorders such as MASLD, where lipid accumulation disrupts normal cellular functions. Full article

Clausena lenis Drake, a valuable medicinal plant in the Rutaceae family, faces threats from wildlife predation, overharvesting, and climate change. In the wild, C. lenis primarily propagates through seeds; however, their rapid loss of viability poses challenges for long-term storage and germplasm conservation. Plant tissue culture offers a practical solution for both its conservation and large-scale production. This study examines seed sterilization, callus induction, shoot multiplication, and root induction protocols for C. lenis. Seeds attained a 100% sterilization rate using 0.2% (w/v) HgCl₂ for 20 min without compromising germination. When cultured on MS medium containing 0.5 mg/L 2,4-D, seed, stem-node, and 1-week-old seedling explants produced abundant callus. A 2.0 mg/L BA treatment achieved 100% shoot induction, with stem-node explants yielding the highest shoot proliferation (3.90 ± 0.31 shoots/explant), followed by 1-week-old seedlings (2.30 ± 0.21 shoots/explant) and seed explants (1.60 ± 0.16 shoots/explant). Rooting was most effective on half-strength MS medium supplemented with 20.0 mg/L IBA, producing an average of 4.30 ± 0.83 roots per shoot in shoot-tip-deprived explants. The rooted plantlets successfully acclimatized, attaining a 100% survival rate in a 1:1:1 mixture of sterile soil, cocopeat, and vermiculite. These findings provide a robust platform for the sustainable propagation and conservation of C. lenis in response to its growing vulnerabilities. Full article

Eivissa/Ibiza, as per its names in its two official languages, Catalan and Spanish, is the third of the Balearic Islands in terms of extension and the second concerning population. It is also a well-known holiday destination in Europe. Numerous ethnobotanical prospections have been performed in the Balearic Islands, but to date, Ibiza lacks a monographic study on traditional knowledge related to plant biodiversity. In this paper, we present the results of the ethnobotanical investigation carried out in Ibiza from 2016 to 2023. A total amount of 95 interviews were conducted with 101 informants born between 1916 and 1983, with semi-structured interviews, participant observation and plant collection, identification and deposit in a public herbarium as basic methods. The total ethnoflora of the island is 254 taxa belonging to 71 botanical families. The most cited families are Solanaceae (1030 URs, 13.50%), followed by Fabaceae (770 URs, 10.09%), Lamiaceae (646 URs, 8.47%) and Rutaceae (578 URs, 7.57%). The most cited species are Vitis vinifera, Capsicum annuum, Solanum lycopersicum, Solanum tuberosum and Citrus sinensis. This study reveals that the local population still retains significant ethnobotanical knowledge. Further research in similar territories could help determine whether this pattern is consistent elsewhere. Full article

Citrus x limonia is an aromatic species, known locally in Ecuador as limón mandarina or limón chino. In the present study, the chemical composition and biological activity of the essential oil isolated from this species were determined. The essential oil was extracted through hydrodistillation. The chemical composition and enantiomeric distribution of the essential oil were determined by gas chromatography. Antimicrobial activity was determined using the broth microdilution method against tree Gram-positive cocci, a Gram-positive bacillus, four Gram-negative bacilli, a fungus, and a yeast. The antioxidant activity was determined through ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) and DPPH (2,2-diphenyl-1-picrylhydrazyl) methods. The spectrophotometric method was used to determine anticholinesterase activity. In the essential oil, thirty-nine compounds were identified, which represented 99.35% of the total composition. Monoterpene hydrocarbons were the most representative group in terms of number of compounds (thirteen) and in terms of relative abundance (91.39%). The main constituents were found to be limonene (57.38 ± 1.09%), γ-terpinene (13.01 ± 0.37%), and β-pinene (12.04 ± 0.63%). Five pairs of enantiomers were identified in the essential oil from fruits of Citrus x limonia. The essential oil presented a minimum inhibitory concentration of 4000 μg/mL against Aspergillus niger. The antioxidant activity of essential oil was weak per the ABTS method, with a SC₅₀ of 1.26 mg/mL. Additionally, the essential oil exhibited moderate anticholinesterase activity, with an IC₅₀ of 203.9 ± 1.03 µg/mL. This study provides the first comprehensive analysis of the chemical composition and biological activities of the essential oil from fruits of Citrus x limonia. Full article

Citrus x limonia is an aromatic species belonging to the Rutaceae family. In the present study, the chemical composition, enantiomeric distribution, and biological activity of the essential oil isolated from leaves of Citrus x limonia were determined. The essential oil was extracted through hydrodistillation. The chemical composition of the essential oil was determined by gas chromatography (GC) coupled to a flame ionization detector (GC-FID), and a mass spectrometer detector (GC-MS) using a nonpolar column. The enantiomeric distribution was performed using two enantioselective chromatographic columns. Antimicrobial activity was determined using the broth microdilution method. The antimicrobial activity was tested against eight bacteria and two fungi. The antioxidant activity was determined through ABTS and DPPH methods. The spectrophotometric method was used to determine anticholinesterase activity. In the essential oil, forty-three compounds were identified. These compounds represent 99.13% of the total composition. Monoterpene hydrocarbons were the most representative group in number of compounds (fourteen) and in terms of relative abundance (65.67%). The main constituent is found to be limonene (25.37 ± 0.80%), β-pinene (23.29 ± 0.15%) and sabinene (8.35 ± 0.10%). Six pairs of enantiomers were identified in the essential oil from fruits of Citrus x limonia. The essential oil showed moderate antibacterial activity against Gram-positive cocci Enterococcus faecalis, and Gram-positive bacillus Lysteria monocytogenes with a MIC of 1000 μg/mL. The oil exhibited strong antifungal activity against fungi Aspergillus niger, and yeasts Candida albicans with a MIC of 250 and 500 μg/mL, respectively. The antioxidant activity of essential oil was weak in ABTS method with a SC₅₀ of 9.12 mg/mL. Additionally, the essential oil presented moderate anticholinesterase activity with an IC₅₀ of 71.02 ± 1.02 µg/mL. Full article