Search Results (90)

Background/Objectives: The increasing resistance of Candida species to conventional antifungals, particularly azoles, poses a critical public health challenge due to high mortality rates associated with candidemia. This study aimed to describe the chemical composition of the essential oil from Haplopappus foliosus (EO-BAI) and evaluate its antifungal properties, along with its nanoemulsion (NE-BAI) and major constituents, against a panel of clinical Candida isolates. Methods: EO-BAI was extracted via steam distillation and analyzed using GC-MS. A nanoemulsion was synthesized through ultrasonic emulsification and characterized by DLS and microscopy (SEM/STEM). Antifungal activity (MIC/MFC) was determined following CLSI M27-A3 guidelines. Time–kill kinetic studies were conducted on C. albicans, and an in silico approach was used to describe interactions with Als9-2 and CYP51 targets. Results: The EO-BAI profile was dominated by terpinen-4-ol (27.27%) and α-bisabolol (10.40%). The NE-BAI exhibited a droplet size of approximately 22 nm with an encapsulation efficiency of 88.72%. Among the tested samples, α-bisabolol emerged as the core bioactive driver (MIC = 16 µg/mL against C. albicans). While NE-BAI showed reduced initial activity at 24 h, it demonstrated enhanced efficacy by 48 h, matching fluconazole’s potency and maintaining a definitive fungicidal effect. Docking analysis confirmed that α-bisabolol establishes stabilizing interactions with key virulence and membrane homeostasis targets. Conclusions: The NE-BAI provides a sustained delivery of its bioactive terpenes, preserving their fungicidal nature and positioning them as robust therapeutic alternatives to conventional treatments. Full article

Plant-derived products, particularly essential oils, represent a promising source of antiviral scaffolds. Although Populus balsamifera L. has been traditionally used to manage respiratory ailments and infections, the antiviral potential of its bud essential oil remains unexplored. In this study, we evaluated the in vitro antiviral cytoprotective activity of P. balsamifera bud essential oil and its major constituents against HCoV-OC43, a human betacoronavirus associated with seasonal respiratory infections, using a cell-based cytoprotection assay. The assay reliably detected the activity of reference antivirals, including chloroquine (EC₅₀ = 0.11 ± 0.01 µg/mL), molnupiravir, and fluvoxamine, supporting its suitability for antiviral screening. Under these conditions, P. balsamifera bud essential oil exhibited strong cytoprotective activity, with an EC₅₀ of 3.3 ± 0.5 µg/mL. Chemical analysis revealed a sesquiterpene-rich composition. Two major constituents, α-bisabolol and nerolidol, also showed marked cytoprotection, with EC₅₀ values of 2.7 ± 0.3 µg/mL and 2.6 ± 0.4 µg/mL, respectively, supporting their contribution to the overall activity of the oil. To our knowledge, this study provides the first experimental evidence of antiviral cytoprotective activity of P. balsamifera bud essential oil against a human coronavirus and identifies α-bisabolol and nerolidol as active compounds in this model. Full article

The increasing demand for sustainable pest management has positioned essential oils (EOs) as viable bio-based alternatives to synthetic pesticides. This study investigates the insecticidal potential of Haplopappus foliosus EO, a Chilean endemic medicinal plant, against Drosophila melanogaster as a key toxicological model for fruit fly control. Chemical characterization identified 56 compounds, with 4-terpineol (27.27%) and α-bisabolol (10.40%) as the primary constituents, marking the first report of α-bisabolol in this species. To enhance bioavailability and overcome EO volatility, a nanoemulsion was developed, achieving an exceptionally small and stable particle size of 2.10 nm that remained consistent for over 90 days. Nanoencapsulation significantly optimized the EO’s efficacy, reducing the median lethal concentration (LC₅₀) from 120.26 µg/mL to a potent 54.57 µg/mL. While in vitro assays showed the free oil as a more potent acetylcholinesterase (AChE) inhibitor, molecular docking confirmed the high affinity of 4-terpineol and α-bisabolol for the enzyme’s active site, elucidating the neurotoxic mechanism at a molecular level. In silico analysis predicted a favorable human safety profile within GHS classes 4 and 5. Overall, this stable nanoformulation represents a sustainable biotechnological strategy for agricultural pest management, leveraging the synergistic effects and enhanced delivery of natural products. Full article

Distillation time (DT) is a key parameter influencing yield and chemical composition, and its optimisation is crucial for production. This study is the first laboratory-scale investigation of the effect of distillation time (DT) on the leaf essential oils of Abies koreana, aiming to maximise oil yield and target bioactive components for cosmetic applications. Essential oils were obtained by hydrodistillation at 14 DTs (1, 3, 5, 10, 20, 40, 80, 120, 160, 200, 240, 280, 360, and 480 min), and the yields, chemical profiles, and fragrance characteristics were comparatively analysed. The control (exhaustive hydrodistillation: 20 h) yielded 2.82% and was dominated by D-limonene, bornyl acetate, and camphene. The contents of bioactive compounds associated with whitening and anti-wrinkle activities (α-pinene, D-limonene, borneol, and bornyl acetate) varied markedly with DT. The highest oil yield was obtained at 80 min (0.30 ± 0.01%), while the targeted components were achieved at 80–160 min. Heatmap-based multivariate analysis revealed distinct compositional differences between oils distilled at 80 min and 160 min, with DT shifting fragrance profiles from fresh, monoterpene-rich notes (linalyl acetate, camphor, and fenchol) to longer-lasting, sesquiterpene-dominated aromas (α-bisabolol and β-eudesmol). Therefore, distillation time significantly influenced A. koreana oil, with shorter distillation (80 min) maximising yield and longer distillation (80–160 min) enriching bioactive components for cosmetic applications. Full article

α-Bisabolol is naturally occurring in many plants and has great potential in health products and pharmaceuticals. However, the current extraction method from natural plants is unsustainable and cannot fulfil the increasing requirement. This study aimed to develop a sustainable strategy to enhance the biosynthesis of α-bisabolol by metabolic engineering. Integration of ERG20 (encoding farnesyl diphosphate synthase) and tHMG1 (encoding truncated 3-hydroxy-3-methylglutaryl-CoA reductase) genes with a constitutive strong promoter into the yeast genome elevated α-bisabolol production from 20.21 mg/L to 98.30 mg/L, representing a 4.86-fold increase. Further optimization of the mevalonate pathway and amplification of ERG20, tHMG1, and OsTPS1 copy numbers enhanced α-bisabolol synthesis to 423.01 mg/L, achieving a 20.93-fold improvement relative to the baseline. This work establishes a reference strategy for high-yield α-bisabolol biosynthesis in engineered yeast. Full article

Exogenous application of methyl jasmonate (MeJ) at different concentrations (0, 1, 10, and 100 µM) during flowering was studied for its impact on phytochemical profile, antioxidant activity, and biomass accumulation in hemp inflorescences of the monoecious cv. Codimono. MeJ treatments had no significant effect on CBD levels, while a 23–54% decrease in total terpene levels was observed in plants treated with 1 and 10 μM MeJ. In particular, MeJ treatments reduced β-caryophyllene and α-humulene levels by 24–43%, α-bisabolol levels by 30–40%, and α-pinene, β-pinene, and β-myrcene levels by 32–61%. By contrast, MeJ treatments had a positive effect on all other classes of phytochemicals analyzed. Plants treated with 100 μM MeJ experienced the highest increases in total flavonoid and phenolic acid levels (+42% and +50%, respectively). In particular, this treatment increased orientin, vitexin, and isovitexin levels by 36–52%, while ferulic acid level increased by 103%. Treatments with 10 and 100 µM MeJ resulted in the highest increases in total carotenoid and tocopherol levels (+41% and +33%, respectively). In particular, lutein, β-carotene, and α-tocopherol levels increased by 44%, 35%, and 36%, respectively. In line with these findings, total antioxidant activity increased by 26% following treatment with 100 μM MeJ and by 13% following the other two treatments. Interestingly, MeJ treatments did not affect plant growth and biomass accumulation in the inflorescences. This implies higher yields for those phytochemicals whose concentrations were increased by MeJ. In summary, our results indicate that hemp plants treated with 100 μM MeJ represent an interesting source of phytochemicals, fiber, and biomass. These characteristics make them suitable for multiple industrial applications and enhance both the economic and health-related value of this crop. Full article

Background: Functional dermatological bases can contribute more than just delivery—they may actively modulate cutaneous homeostasis. Cleoderm™ is a dermofunctional base containing a patented Cleome gynandra extract, palmitoyl tripeptide-8, bisabolol, hyaluronic acid, and functional oils, rationally designed to provide anti-inflammatory, antioxidant, and barrier-supportive properties. Objective: To determine whether Cleoderm™ exhibits intrinsic immunomodulatory and matrix-protective effects in a physiologically relevant skin co-culture and to clarify the biomarkers most impacted, with translational relevance to acne and rosacea. Methods: Human keratinocytes and fibroblasts were maintained in a transwell co-culture. Non-cytotoxic concentrations of Cleoderm™ (1.0% and 10.0%, v/v) were tested with or without LPS stimulation (1 μg/mL). Viability was assessed by MTT and Trypan Blue. Cytokines (IL-6, TNF-α, IL-10, TGF-β) and MMPs (MMP-1, -3, -13) were quantified by ELISA and RT-qPCR. LL-37, IGFBP-3, and TGF-β protein levels were evaluated by Western blot. Results: Cleoderm™ showed no cytotoxicity up to 10% (v/v). It significantly reduced pro-inflammatory mediators (IL-6, TNF-α) and matrix-degrading enzymes (MMP-1, MMP-3, MMP-13) while increasing anti-inflammatory/reparative cytokines (IL-10, TGF-β). A dual, biomarker-level modulation was observed: (i) LL-37 was reduced, with a particularly pronounced decrease in secreted levels; and (ii) IGFBP-3 was markedly upregulated, indicating potential attenuation of the IGF-1 axis relevant to sebaceous lipogenesis. Collectively, these effects indicate immunoregulatory and matrix-protective activity consistent with improved cutaneous homeostasis. Conclusion: In a dermo-epidermally relevant in vitro model, Cleoderm™ functions as an active dermofunctional base, not merely a vehicle simultaneously tempering inflammatory signaling, preserving extracellular matrix integrity, and modulating mechanistic nodes (LL-37 and IGFBP-3) linked to rosacea and acne. These findings is consistent with the use of Cleoderm™ as a biologically supportive base for personalized compounding and justify controlled clinical evaluation. Full article

Chamomile (Matricaria chamomilla L.) is a popular herb of great economic and medicinal value. Despite its significant potential, there are currently no commercially available varieties specifically adapted to Mediterranean low-input farming systems. The present study aimed to develop a genetically improved breeding population derived from indigenous Greek chamomile germplasm, following a multi-year strategy, based on pedigree selection under low-input conditions. This selection process constituted the first phase of the breeding program, during which selection focused on improving inflorescence dry weight and essential oil quality, particularly with respect to α-bisabolol and chamazulene content. After three cycles of selection, considerable genetic gains were achieved. The realized heritability values exceeded 0.5 for all assessed traits, confirming strong genetic control. In the fourth year, representing the second phase of the breeding program, the breeding population—developed through selection during the first phase—was evaluated alongside the initial population and commercial diploid and tetraploid varieties. The breeding population exhibited significant observed gains compared to the initial population: inflorescence dry weight increased by 12.17%, α-bisabolol content by 71.45%, and chamazulene content by 6.57%. Additionally, the breeding population not only surpassed all evaluated diploid genotypes in essential oil composition, but also displayed a chemotypic shift, indicating successful alignment with tetraploid varieties characterized by high-value chemical profiles. Furthermore, this selection process targeting specific commercial chamomile traits indirectly contributed to improvement in plant height and inflorescence morphology. Overall, these results demonstrate that conventional breeding, when applied effectively to native resources, can enhance both agronomic performance and essential oil profile. The newly developed breeding population provides a strong foundation for future cultivar development tailored to Mediterranean low-input sustainable farming systems. Full article

Inflammatory bowel diseases (IBDs), such as ulcerative colitis, and Crohn’s disease are chronic idiopathic inflammatory diseases of the gastrointestinal system involving interaction between genetic and environmental factors mediating the occurrence of oxidative stress and inflammation. There is no permanent cure for IBD except long-term treatment or surgery (resection of the intestine), and the available agents in the long term appear unsatisfactory and elicit numerous adverse effects. To keep the disease in remission, prevent relapses and minimize adverse effects of currently used medicines, novel dietary compounds of natural origin convincingly appear to be one of the important therapeutic strategies for the pharmacological targeting of oxidative stress and inflammation. Therefore, it is imperative to investigate plant-derived dietary agents to overcome the debilitating conditions of IBD. In the present study, the effect of α-Bisabolol (BSB), a dietary bioactive monoterpene commonly found in many edible plants as well as important components of traditional medicines, was investigated in acetic acid (AA)-induced colitis model in rats. BSB was orally administered to Wistar male rats at a dose of 50 mg/kg/day either for 3 days before or 30 min after induction of IBD for 7 days through intrarectal administration of AA. The changes in body weight, macroscopic and microscopic analysis of the colon and calprotectin levels in the colon of rats from different experimental groups were observed on day 0, 2, 4, and 7. The levels of myeloperoxidase (MPO), a marker of neutrophil activation, reduced glutathione (GSH) and malondialdehyde (MDA), a marker of lipid peroxidation, and the levels of pro-inflammatory cytokines were measured. AA caused a significant reduction in body weight and induced macroscopic and microscopic ulcers, along with a significant decline of endogenous antioxidants (superoxide dismutase (SOD), catalase, and GSH), with a concomitant increase in MDA level and MPO activity. BSB significantly improved the AA-induced reduction in body weight, colonic mucosal histology, inhibited MDA formation, and restored antioxidant levels along with a reduction in MPO activity. AA also induced the release of pro-inflammatory cytokines such as interleukin-1 (IL-1), interleukin-23 (IL-23) and tumor necrosis factor-α (TNF-α). Furthermore, AA also increased levels of calprotectin, a protein released by neutrophils under inflammatory conditions of the gastrointestinal tract. BSB treatment significantly reduced the release of calprotectin and pro-inflammatory cytokines. The findings of the present study demonstrate that BSB has the potential to improve disease activity and rescue colonic tissues from damage by inhibiting oxidative stress, lipid peroxidation and inflammation. The findings are suggestive of the benefits of BSB in IBD treatment and substantiate its usefulness in colitis management, along with its gastroprotective effects in gastric ulcer. Full article

Background/Objectives: A prior placebo-controlled, double-blind clinical study demonstrated the superiority of a topical combination of heparin and levomenol over the control and single active constituents. The effect on pruritus and the total SCORAD index were used to evaluate efficacy, but not the effect on the individual SCORAD items. This analysis investigates the overall efficacy of the treatment and the relative contributions of heparin and levomenol to symptom relief in atopic dermatitis, including the effects on the affected body area and its implications for sleeplessness. Methods: The ITT group (combination group A: n = 79; levomenol group B: n = 80; heparin group C: n = 78; placebo group D: n = 41) of the previously published study was re-analysed. Results: The combination significantly improved symptoms such as erythema, edema/papulation, excoriations, and skin dryness compared to the control after eight weeks of treatment. No significant differences were observed for oozing/crust and lichenification among the active groups. Levomenol and heparin exhibited significant advantages over the control for erythema and excoriations, while heparin improved edema/papulation significantly. The inflamed body area significantly decreased using the combination or single active constituents, and sleeplessness significantly improved with the combination or with heparin alone compared to the control. Conclusions: These findings highlight the efficacy of the combination and individual active constituents in addressing specific symptoms of atopic dermatitis, providing insights into their therapeutic effects. The combination’s advantage over the control is most evident in improving excoriations, skin dryness, inflamed skin area, and sleeplessness, justifying its documented use as an intervention in the early stages of atopic dermatitis episodes. Full article

The current research is focused on the discovery and optimization of an effective cosmetic carrier of alpha-bisabolol as a first step in the development of a cosmetic product with cleansing and antimicrobial action for facial skin hygiene. A micellar solution of Poloxamer 407 was selected as a cosmetic base because of the good washing ability, easy application, and high tolerability of this polymeric surfactant. The solubilization capacity of a 5% micellar solution with respect to α-bisabolol was investigated by applying varying solubilization techniques and increasing concentrations of the oily active substance. The test samples were subjected to an accelerated physical stability test, viscosimetry, dynamic light scattering (DLS), electrophoretic light scattering (ELS), foamability test, and antimicrobial screening. Over the course of this research, the advantage of the film-hydration method over direct solubilization was demonstrated by the narrower size distribution and smaller hydrodynamic size of the micellar nano-carriers (ranging from 29.02 to 116.5 nm) and the respective higher physical stability of the dispersions. The optimized composition was found to be suitable for application on large skin areas in terms of viscosity in the temperature range from 20 °C to 40 °C (3.4–2.3 mPa.s). Preservation of the washing capacity of the micellar solution in the presence of solubilized α-bisabolol was established. The active composition demonstrated inhibitory activity against Staphylococcus aureus and Escherichia coli and fungicidal activity against Candida albicans. This study concludes that the optimal concentration of α-bisabolol to be solubilized in a 5% Poloxamer 407 micellar solution by the film-hydration technique is 1%, considering the desirable physical endurance and antimicrobial activity. Full article

The application of shade during plants’ growth significantly alters the biochemical compounds of the essential oil (EO). We aimed to analyze the effect of shade on the volatile compounds and biochemical activities of EO extracted from Curcuma xanthorrhiza Roxb. (C. xanthorrhiza) plants. Four shading conditions were applied: no shading (S0), 25% (S25), 50% (S50), and 75% shade (S75). The volatile compounds of EO extracted from each shaded plant were analyzed by gas chromatography–mass spectrometry. The antioxidant, antibacterial, and antiproliferative activities of EO were also investigated. We found that shade application significantly reduced the C. xanthorrhiza EO yield but increased its aroma and bioactive compound concentration. α-curcumene, xanthorrhizol, α-cedrene, epicurzerenone, and germacrone were found in EO extracted from all conditions. However, β-bisabolol, curzerene, curcuphenol, and γ-himachalene were only detected in the EO of S75 plants. The EO of the shaded plants also showed higher antioxidant activity as compared to unshaded ones. In addition, the EO extracted from S75 exerted higher antiproliferative activity on HeLa cells as compared to S0. The EO extracted from S0 and S25 showed higher antibacterial activity against Gram-positive bacteria than kanamycin. Our results suggest that shade applications alter the composition of the extractable volatile compounds in C. xanthorrhiza, which may result in beneficial changes in the biochemical activity of the EO. Full article

Needle-free buccal anesthesia improves dental treatment outcomes for both patients and dentists. In this study, we report on an assessment of the enhancement effects of α-bisabolol on the in vitro transmucosal permeation of prilocaine hydrochloride (PCl) and lidocaine hydrochloride (LCl) from needleless buccal films. We also evaluated the mechanical properties of the film, which consisted of Methocel™ K100 LV as the film-forming polymer (3% m·m⁻¹), PEG 400 as a cosolvent (15% m·m⁻¹ based on drug loading), α-bisabolol (15 and 30% m·m⁻¹ based on drug loading), and the drugs combined at a 1:1 ratio (15 mg·unit⁻¹). The porcine esophageal epithelium was used as a membrane barrier, and artificial saliva was the release medium. After a 1 h experiment at 25 ± 2 °C, α-bisabolol significantly decreased, rather than enhanced, the permeation fluxes (five-fold), permeability coefficients (seven-fold), and retentions (two-fold) of both PCl and LCl through the epithelium, regardless of the concentration. Moreover, the resistance and flexibility of the films markedly decreased compared to those without α-bisabolol. Therefore, under the experimental conditions, using α-bisabolol as a buccal permeation enhancer for the hydrophilic local anesthetics PCl and LCl from buccal films is not feasible. Full article

Klebsiella pneumoniae is an opportunistic Gram-negative bacterium in the Enterobacteriaceae family associated with a wide range of diseases, such as pneumonia, bloodstream infections, meningitis and urinary tract infections. Infections caused by drug-resistant strains of Klebsiella pneumoniae pose a significant threat to the effectiveness of conventional antibiotics. Hence, this has led to the need to explore alternative antimicrobial therapies, especially natural products derived from plant sources. This study assessed the phytochemical composition and antibacterial properties and performed a molecular docking analysis of Henna leaves (Lawsonia inermis L.) extracts on strains of Klebsiella pneumoniae. Crude ethanol and methanol extracts of L. inermis L. were prepared at different concentrations (25, 50, 75 and 100 mg/mL) and tested on extended spectrum beta-lactamases (ESBLs)-producing strains of Klebsiella pneumoniae. Phytocompounds were identified using gas chromatography–mass spectrometry (GC-MS) and further subjected to virtual ligands screening with DataWarrior (v05.02.01) and a molecular docking analysis using AutoDock4.2 (v4.2.6). The active compounds of L. inermis L. were determined by the docking analysis, including phytochemical, physicochemical, pharmacokinetics and docking score. The GC-MS analysis identified 27 phytoconstituents, including ethyl acetate, sclareol, 2-[1,2-dihydroxyethyl]-9-[β-d-ribofuranosyl] hypoxanthine, α-bisabolol and 2-Isopropyl-5-methylcyclohexyl 3-(1-(4-chlorophenyl)-3-oxobutyl)-coumarin-4-yl carbonate. The 27 compounds were then screened for their physicochemical and pharmacokinetic properties. The results revealed that the methanol extracts at 100 mg/mL showed significantly higher (p < 0.05) zones of inhibition (13.7 ± 1.2 mm), while the ethanol extracts at 50 mg/mL were significantly lower (6.3 ± 0.6 mm) compared to all the other treatments. The docking analysis revealed that out of the 27 compounds identified, only twelve (12) compounds have a drug-likeness activity. The 12 compounds were further subjected to docking analysis to determine the binding energies with the CTX-M protein of Klebsiella pneumoniae. Only one compound [CID_440869; (2-[1,2-dihydroxyethyl]-9-[β-d-ribofuranosyl] hypoxanthine)] had the best binding energy of −9.76 kcal/mol; hence, it can be considered a potentially suitable treatment for infections caused by ESBLs-producing strains of Klebsiella pneumoniae. This study has demonstrated that L. inermis L. extracts have antibacterial effects. Further research could explore the potential antimicrobial applications of L. inermis L. extracts to many bacterial strains. Full article

Lower urinary tract inflammation is a very common problem which occurs particularly in women. That is why the idea of a biotextronics system for preventive and supportive treatment came to be. The system is a kind of a therapeutic clothing in the form of underwear integrated with a four-layer pantiliner with biological active compounds (from chamomile essential oil) immobilized on the insert with a cellulose agar or microcrystalline cellulose agar film. In this research, the outer part of the insert was investigated for its ability to release compounds with antibacterial and anti-inflammatory activity under the temperature of the treatment (40 °C). The research was conducted on the day of the insert preparation (day 0) and also after 7, 14, 28, and 56 days to test the ability of the insert to be stored without changing its properties. The results showed that even after 56 days of storage, there are compounds released that are known to have antibacterial activity, such as α-bisabolol. The system requires further tests involving bacteria; however, chamomile essential oil seems to be good substrate for biotextronics systems for preventive and supportive treatment of lower urinary tract inflammations. Full article