Search Results (84)

Curcuminoids from Curcuma longa L. (curcumin, demethoxycurcumin, bisdemethoxycurcumin) are attractive bioactives yet constrained by low water solubility and chemical instability. Herein, we introduce a Supramolecular Deep Eutectic Solvent (SupraDES) as a “Janus” green platform, combining extraction and stabilization with a subsequent solvent-to-material strategy. Eight NaDES/SupraDES formulations based on choline chloride (ChCl) or betaine with glycerol (Gly) or citric acid (CitA), with/without β-cyclodextrin (βCD), were assessed. The extinction coefficients of the most promising solvents were extrapolated at 425 nm for the UV–vis quantification of curcuminoids, to determine extraction performance. The SupraDES ChCl:Gly:βCD gave the best performance during the first solvent screening, improving at the same time the bioactive stability (after 30-day, 47.5% loss vs. 62.8% of ChCl:Gly alone). Subsequent microwave-assisted extraction (MAE) optimization identified 80 °C as the optimal process temperature, with near-equilibrium reached within 15 min (3139.4 µgCurc/gEXT). Peleg modelling (R² = 0.997) indicated a fast extraction rate and limited benefit from longer residence times. Finally, the curcuminoid-loaded SupraDES was incorporated into polyvinyl alcohol (PVA) networks crosslinked with CitA and 2,5-bis(hydroxymethyl)furan (BHMF); thermal analysis confirmed the formation of a stable crosslinked structure. To the best of our knowledge, this is the first report of a βCD-based SupraDES acting as a Janus platform that couples supramolecular extraction of lipophilic bioactives with their direct incorporation into bio-based polymeric materials, exemplifying an integrated green chemistry approach aligned with circular bioeconomy principles. Full article

Turmeric has a long history of use as a colorant and flavoring agent. Turmeric extract (TE) is a feed additive containing at least 90% total curcuminoids, comprising mainly curcumin, desmethoxycurcumin and bisdemethoxycurcumin. The published antioxidant effects of TE in humans have sparked interest and feeding studies in companion animals. Studies describing the feeding of TE to cats are scarce and do not provide adequate toxicology data; regulatory approval is required to allow use of TE as a nutritional antioxidant in pet food. The current study describes a safety test of TE in cats. Control cats were fed a standard extruded dry diet whilst two groups of test cats were fed the same diet supplemented with two different levels of TE for four months. Physical examination, body weight, body condition score, food intake, fecal score, monitoring of adverse effects (vomiting, diarrhea, clinical signs), complete blood count, and blood biochemistry (particularly liver enzymes) were used to monitor toxicity signs. The lack of statistically significant effects of clinical or toxicological concern concludes that feeding TE to cats at a dietary level providing up to 1040 ppm total curcuminoids is safe. This allows future application of this ingredient in cat food as a nutritional antioxidant. Full article

A new spiral nematode species, Scutellonema curcumae sp. n., was identified from the rhizosphere of turmeric (Curcuma longa L.) in the Western Highlands of Vietnam. Integrative taxonomical analysis, combining detailed morphology and molecular characterization (ITS, 28S D2–D3 rDNA, and COI mtDNA), confirmed its distinctiveness. Scutellonema curcumae sp. n. is characterized by a unique combination of a spiral body, a hemispherical lip region with four annuli, a robust stylet, and a rounded tail with a prominent scutellum, forming a highly divergent lineage within the genus. Beyond its description, this study reveals a significant inverse correlation between nematode population density and the phytochemical quality of the host. High infestation levels were associated with a marked decline in total curcuminoid content. Notably, lower nematode density favored a specific shift in the curcuminoid profile, with bisdemethoxycurcumin levels increasing by up to 250%. These phytochemical alterations directly influenced the therapeutic potential of the rhizomes: lower infestation levels resulted in significantly enhanced antioxidant capacity (lower SC₅₀ values) and cytotoxic activity (lower IC₅₀ against HepG2 and A549 cell lines). This work represents the first report of a Scutellonema species associated with turmeric in Vietnam and underscores its detrimental impact on the medicinal and nutraceutical value of the crop. Our findings suggest that effective nematode management is crucial not only for yield protection but as a strategic intervention in precision agriculture to optimize the secondary metabolite profiles of medicinal plants. Full article

Abscess formation is commonly precipitated by bacterial infection. This study delineates the phytochemical composition and evaluates the antioxidant, antibacterial, and anti-biofilm activities of a Thai traditional anti-abscess herbal formulation comprising Curcuma zedoaria, Vitex trifolia, and Azadirachta indica. Validated high-performance liquid chromatography–photodiode array detection (HPLC–PDA) analysis of the ethanolic extract identified curcumin, demethoxycurcumin, bisdemethoxycurcumin, and vitexicarpin as principal constituents. Total phenolic and flavonoid contents were 32.08 ± 2.54 mg GAE/g and 17.52 ± 1.28 mg QE/g dry weight, respectively. Antioxidant assessment by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay yielded an half maximal inhibitory concentration (IC₅₀) of 53.46 ± 3.24 µg/mL, while reducing power corresponded to 383.97 ± 13.24 µg FeSO4/g dry weight. Molecular orbital analysis revealed a highest occupied molecular orbital and lowest unoccupied molecular orbital (HOMO–LUMO) gap for vitexicarpin (ΔE = 9.7710 eV), indicative of greater radical-scavenging potential relative to curcuminoids. Antibacterial assays demonstrated selective activity against Staphylococcus epidermidis (inhibition zone 1.48 ± 0.16 cm), with no observed inhibition of Staphylococcus aureus or Streptococcus pyogenes. Curcumin exhibited the highest activity against S. epidermidis (minimum inhibitory concentration (MIC) 62.5 µg/mL; minimal bactericidal concentration minimal bactericidal concentration (MBC) 125 µg/mL). Molecular docking showed curcumin binding to the teicoplanin-associated transcriptional regulator (TcaR) with a binding energy of −8.00 kcal/mol, comparable to methicillin (−8.16 kcal/mol), suggesting a potential mechanism for modulation of biofilm-associated regulatory pathways. Collectively, these findings indicate that the formulation has measurable antioxidant activity and targeted antibacterial efficacy against S. epidermidis, which may contribute to attenuation of abscess progression via interference with biofilm regulation. Full article

Fungal secondary metabolites are valuable sources of natural antioxidants and antimicrobials. This study evaluated the submerged fermentation of Penicillium crustosum OR889307 supplemented with lemon peel as a co-substrate to enhance the production of bioactive compounds. Lemon peel was selected for its phenolic precursors and sustainable availability as an agro-industrial byproduct. Crude extracts, aqueous and organic fractions, and molecular-weight partitions were assessed for antioxidant activity using the DPPH assay and for antimicrobial activity against Escherichia coli, Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), Pseudomonas aeruginosa, and Candida albicans. Semi-purified extracts from co-substrate fermentations exhibited enhanced bioactivity, showing MIC values of 185 µg/mL against P. aeruginosa and 225 µg/mL against MRSA, along with strong ABTS radical-scavenging capacity (238.95 ± 2.17 µmol TE). RP-HPLC-ESI-MS profiling revealed phenolic acids, flavanones, flavonols, and lignans, including ferulic acid 4-O-glucoside, bisdemethoxycurcumin, secoisolariciresinol, and quercetin 3-O-xylosyl-glucuronide. These findings demonstrate that lemon peel supplementation promotes the biosynthesis of antimicrobial and antioxidant metabolites by P. crustosum. This approach supports sustainable agro-waste valorization and offers a promising strategy for obtaining natural bioactive compounds with potential applications in food preservation and health-related formulations. Full article

Our previous study demonstrated that thiophene-substituted synthetic curcumin analogs possessed better antibacterial activity and stability than natural curcumin, demethoxycurcumin, or bisdemethoxycurcumin in antibacterial photodynamic therapy (aPDT). In addition, the activity of the furan-substituted analogs was weaker than that of the thiophene-substituted compounds. As oxygen, sulfur, and selenium belong to the same group in the periodic table, the antibacterial and anticancer activities of these three different elemental analogs were compared and investigated. The thiophene-substituted analog (compound 3) exhibited the most potent antibacterial activity in aPDT experiments. However, the furan-substituted analog (compound 1) exhibited the most potent anticancer activity. These results indicate that the differences in atomic radii or energy levels in these compounds produce different cell-attack results on generated free radicals. Ruthenium(II) complexes have a good reputation for use in PDT for cancer treatment. Our results show that complexation of ruthenium(II) with thiophene-substituted curcumin analogs does not enhance their antibacterial or anticancer activity. Full article

Background/Objectives: Recent studies have revealed that plants produce lipid-derived microvesicles with potent anti-inflammatory properties. In turmeric (Curcuma longa L.), such microvesicles have been identified in rhizome juice and shown to exert beneficial effects in murine models of colitis. In this study, we investigated whether turmeric extracts commonly used in phytotherapy (30% ethanolic or aqueous extracts, and freeze-dried or spray-dried preparations) contain Curcuma-derived microvesicles (CuMVs), and we evaluated the influence of extraction processes on their aggregation and morphology. Methods: All extracts were processed using a standardized protocol involving differential centrifugation, filtration, and ultracentrifugation. CuMVs with sizes from 50 to 200 nm were detected in all pellets, but CuMVs from dehydrated extracts were markedly aggregated compared to those from liquid preparations. Results: The 30% ethanolic extract yielded the most polydisperse CuMVs and was therefore selected for functional immunomodulatory analyses on macrophages. Protein quantification indicated that 600 mL of 30% ethanolic extract contained approximately 60 µg of CuMVs which contained curcumin and its derivatives demethoxycurcumin (DMC), and bisdemethoxycurcumin (BDMC) identified by high-performance thin-layer chromatography (HPTLC). Green fluorescence in the form of small dots close to the nuclei was detected in recipient THP-1 macrophages, indicating the incorporation of CuMVs and therefore the transfer of the naturally fluorescent curcumin. CuMV treatment reduced ROS production, downregulated CD86, and upregulated CD163 expression. Furthermore, CuMVs increased the expression of IL-10 and TGF-β, as well as antibacterial cytokines (IL-1β, IL-6, and TNF-α), and enhanced RAW macrophage migration. Depletion of CuMVs from turmeric extracts markedly reduced their immunomodulatory effects. Conclusions: Collectively, these findings emphasize the importance of preserving CuMVs during the industrial processing of turmeric, as they play a crucial role in curcuminoid delivery and in mediating the immunomodulatory properties of turmeric extracts. Full article

Curcumin (CUR) is the primary metabolite isolated from the Curcuma longa L. rhizome. Most synthetic and biological studies have focused mainly on the curcumin molecule due to its essential biological activity as an antioxidant, anti-cancer, and anti-Alzheimer’s disease agent. However, the natural extract of turmeric also contains two essential curcuminoids (demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC)), which altogether comprise the so-called C-3 complex. They are present in commercial compositions for treating biliary or digestive ailments. The vegetal rhizome’s extraction typically leads to a mixture of the three main curcuminoids, CUR, DMC, and BDMC, in variable proportions, and each of these metabolites has reported specific synthetic routes. Herein, we have performed the synthesis and isolation of the three major curcuminoids using the method called scrambling of aldehydes followed by aldol di-condensation reactions. A density functional theory (DFT) approach supported the experimental results by inspecting the predicted energies for the aldol condensation. Thus, the di-condensation reaction is substantially favoured (ΔG° = −2685.9 kJ/mol) over the mono-condensation reaction (ΔG° = −1393.753 kJ/mol). Our approach allows us to mimic closely the proportions of these curcuminoids found in extracts from natural sources that follow the order CUR > DMC > BDMC, respectively. The proportion of aldehydes can be modified in the scrambling reaction with an adequate mixture of aldehydes to render the order DMC > CUR > BDMC. This is an advantageous way to increase the amount of the unsymmetric DMC metabolite. Full article

Turmeric oleoresin (TO), a natural pigment derived from Curcuma longa rhizomes, is valued for its health benefits, which are primarily attributed to its rich curcuminoid content (curcumin, demethoxycurcumin, and bisdemethoxycurcumin). Despite these benefits, curcuminoids are known to be light-sensitive and possess photosensitizing properties. This study investigated the impact of common light sources, fluorescent light and white LED (both at 10 W/m²), on the chemical stability, antioxidant activity, cytotoxicity, and photosensitizing properties of TO. Exposure to both light sources significantly reduced TO’s color and fluorescence intensity, with white LED causing greater instability. HPLC analysis confirmed a decrease in individual curcuminoid levels, with curcumin degrading most rapidly under both conditions. The DPPH radical scavenging activity of irradiated TO decreased compared to fresh or dark-stored turmeric, whereas its ABTS radical scavenging activity increased upon light exposure. Photosensitizing potency, measured by formazan decolorization and lipid peroxide formation, declined as TO decomposed under light. Conversely, the cytotoxicity of TO against B16F10 melanoma cells was significantly enhanced under light exposure, though this effect was diminished significantly after 24 h of pre-irradiation. These findings underscore the instability of turmeric pigment under common lighting conditions, which should be a crucial consideration when processing, storing, and distributing turmeric-containing products. Full article

Background/Objectives: The anti-Leishmania potential of Curcuma longa and its derivatives, such as curcuminoids, is well-established, yet their mechanisms of action remain underexplored. This study investigates the inhibitory effects of C. longa extracts and curcumin on Leishmania infantum arginase, a key enzyme in polyamine and trypanothione biosynthesis, and evaluates their antiparasitic activity. Methods: Extracts were prepared via rhizome successive maceration with hexane (HEXCURC), dichloromethane (DCCURC), and ethanol (ETOHCURC) and chemically characterized by a combination of chromatographic and spectrometric methods. The inhibition of recombinant L. infantum arginase (LiARG) was assessed by urea quantification, while molecular docking explored interactions between the main compounds annotated in the extracts and the enzyme’s active site. Biological activity was tested against L. infantum promastigotes, intracellular amastigotes, and mammalian cells. Results: LC-MS and GC-MS revealed curcuminoids and turmerones as main compounds annotated in the extracts. DCCURC, HEXCURC, and curcumin showed the strongest LiARG inhibition (IC₅₀ = 10.04, 14.4, and 17.55 μg/mL, respectively). Docking analysis revealed that curcumin, demethoxycurcumin, and bisdemethoxycurcumin bind near the active site, with binding energies of –3.43, –4.14, and –3.99 kcal/mol, respectively. Curcumin demonstrated superior anti-promastigote activity (IC₅₀ = 15.01 μg/mL) and selectivity (SI = 12.7) compared to the extracts. It also significantly reduced amastigote burden in infected macrophages (IC₅₀ = 13.6 μg/mL). Conclusions: This is the first report demonstrating that C. longa extracts and curcumin inhibit LiARG. These findings support curcumin’s potential as a lead compound for developing multi-target therapies against leishmaniasis, combining enzyme inhibition with direct antiparasitic effects. Full article

Investigating amyloid–β (Aβ) peptides in solution is essential during the initial stages of developing lead compounds that can influence Aβ fibrillation while the peptide is still in a soluble state. The tendency of the Aβ(1–42) peptide to misfold in solution, correlated to the aetiology of Alzheimer’s disease (AD), is one of the main hindrances to characterising its aggregation kinetics in a cell-mimetic environment. Moreover, the Aβ(1–42) aggregation triggers the unfolded protein response (UPR) in the endoplasmic reticulum (ER), leading to cellular dysfunction and multiple cell death modalities, exacerbated by reactive oxygen species (ROS), which damage cellular components and trigger inflammation. Antioxidants like curcumin, a derivative of Curcuma longa, help mitigate ER stress by scavenging ROS and enhancing antioxidant enzymes. Furthermore, evidence in the literature highlights the effect of curcumin on the secondary structure of Aβ(1–42). This explorative study investigates the Aβ(1–42) peptide conformational behaviour in the presence of curcumin and six derivatives using circular dichroism (CD) to explore their interactions with lipid bilayers, potentially preventing aggregate formation. The results suggest that the synthetic tetrahydrocurcumin (THC) derivative interacts with the amyloid peptide in all the systems presented, while cyclocurcumin (CYC) and bisdemethoxycurcumin (BMDC) only interact when the peptide is in a less stable conformation. Molecular dynamics simulations helped visualise the curcuminoids’ effect in an aqueous system and hypothesise the importance of the peptide surface exposition to the solvent, differently modulated by the curcumin derivatives. Full article

Denervation-induced calcium/calmodulin-dependent protein kinase II (CaMKII) activation and inflammation can result in muscle atrophy. Curcumin and bisdemethoxycurcumin are well known to exhibit an anti-inflammatory effect. In addition, curcumin has been shown to attenuate CaMKII activation in neuronal cells. This study aimed to examine the effect of curcumin or bisdemethoxycurcumin on CaMKII activation, inflammation, and muscle cross-sectional area (CSA) in spinal nerve ligated rats. Sixteen female rats were assigned to sham (CON), spinal nerve ligation (SNL), SNL+ curcumin 100 mg/kg BW (100CUR), and SNL+ bisdemethoxycurcumin 50 mg/kg BW (50CMO) for 4 weeks. Ipsilateral (surgical) soleus and tibialis anterior (TA) muscles was stained for dystrophin to measure CSA. Ipsilateral and contralateral (non-surgical) plantaris muscles were analyzed for protein content for acetylcholine receptor (AChR), CaMKII, CaMKII^Thr286, nuclear factor-κB (NF-κB), NF-κB^Ser536, and interleukin-1β (IL-1β) and normalized to α-tubulin and then CON. A significant (p < 0.050) group effect was observed for TA CSA where CON (11,082.25 ± 1617.68 μm²; p < 0.001) and 100CUR (9931.04 ± 2060.87 μm²; p = 0.018) were larger than SNL (4062.25 ± 151.86 μm²). In the ipsilateral plantaris, the SNL (4.49 ± 0.69) group had greater CaMKII activation compared to CON (1.00 ± 0.25; p = 0.010), 100CUR (1.12 ± 0.45; p = 0.017), and 50CMO (0.78 ± 0.19; p = 0.009). The ipsilateral plantaris (2.11 ± 0.66) had greater IL-1β protein content than the contralateral leg (0.65 ± 0.14; p = 0.041) in the SNL group. In plantaris, the SNL (1.65 ± 0.51) group had greater NF-κB activation compared to CON (1.00 ± 0.29; p = 0.021), 100CUR (0.61 ± 0.10; p = 0.003), 50CMO (0.77 ± 0.25; p = 0.009) groups. The observed reduction in Ca²⁺ signaling and inflammation in type II plantaris muscle fibers might reflect the changes within the type II TA muscle fibers which may contribute to the mitigation of TA mass loss with curcumin supplementation. Full article

The human skin, the body’s largest organ, undergoes continuous renewal but is significantly impacted by aging, which impairs its function and leads to visible changes. This study aimed to identify botanical compounds that mimic the anti-aging effects of baricitinib, a known JAK1/2 inhibitor. Through in silico screening of a botanical compound library, 14 potential candidates were identified, and 7 were further analyzed for their effects on cellular aging. The compounds were tested on both normal aged fibroblasts and premature aging fibroblasts derived from patients with Hutchinson–Gilford Progeria Syndrome (HGPS). Results showed that these botanical compounds effectively inhibited the JAK/STAT pathway, reduced the levels of phosphorylated STAT1 and STAT3, and ameliorated phenotypic changes associated with cellular aging. Treatments improved cell proliferation, reduced senescence markers, and enhanced autophagy without inducing cytotoxicity. Compounds, such as Resveratrol, Bisdemethoxycurcumin, Pinosylvin, Methyl P-Hydroxycinnamate, cis-Pterostilbene, and (+)-Gallocatechin, demonstrated significant improvements in both control and HGPS fibroblasts. These findings suggest that these botanical compounds have the potential to mitigate age-related cellular alterations, offering promising strategies for anti-aging therapies, particularly for skin health. Further in vivo studies are warranted to validate these results and explore their therapeutic applications. Full article

Researchers are increasingly interested in discovering new pancreatic lipase inhibitors as anti-obesity ingredients. Medicine-and-food homology plants contain a diverse set of natural bioactive compounds with promising development potential. This study screened and identified potent pancreatic lipase inhibitors from 20 commonly consumed medicine-and-food homology plants using affinity ultrafiltration combined with spectroscopy and docking simulations. The results showed that turmeric exhibited the highest pancreatic lipase-inhibitory activity, and curcumin, demethoxycurcumin, and bisdemethoxycurcumin were discovered to be potent pancreatic lipase inhibitors within the turmeric extract, with IC₅₀ values of 0.52 ± 0.04, 1.12 ± 0.05, and 3.30 ± 0.08 mg/mL, respectively. In addition, the enzymatic kinetics analyses demonstrated that the inhibition type of the three curcuminoids was the reversible competitive model, and curcumin exhibited a higher binding affinity and greater impact on the secondary structure of pancreatic lipase than found with demethoxycurcumin or bisdemethoxycurcumin, as observed through fluorescence spectroscopy and circular dichroism. Furthermore, docking simulations supported the above experimental findings, and revealed that the three curcuminoids might interact with amino acid residues in the binding pocket of pancreatic lipase through non-covalent actions, such as hydrogen bonding and π-π stacking, thereby inhibiting the pancreatic lipase. Collectively, these findings suggest that the bioactive compounds of turmeric, in particular curcumin, can be promising dietary pancreatic lipase inhibitors for the prevention and management of obesity. Full article

Natural curcumin is composed of three curcuminoids, namely curcumin (CUR), deme-thoxycurcumin (DMC) and bis-demethoxycurcumin (BDMC). These compounds are utilized in various biophotonics applications, including photodynamic therapy (PDT). This work aimed to evaluate the photodynamic action (alternative to antibiotics) of synthetic curcuminoids against Staphylococcus aureus. Herein, we evaluated an optimal proportion of the three curcuminoids mixed in solution to improve photoinactivation effects. Therefore, a set of computational calculations was carried out to understand the photodynamic action (stability and mechanism) of curcuminoids. Regarding computational analysis, the curcuminoid molecules were optimized using DFT with the hybrid exchange–correlation functional M06-2X, which includes long-range correction, and the 6-311++G(d,p) basis set. DMC and BDMC were more effective as photosensitizers than curcumin at a very low concentration of 0.75 µM, inactivating more than five orders of magnitude of S. aureus. Theoretical UV-vis absorption spectra showed that at maximum absorption wavelengths, electronic transitions of the π→π* type originated from H→L excitations. The BDMC was more stable than the other two curcuminoids after photobleaching, and the fluorescence emission was also higher, which could lead to its usage as a fluorescence dye to track bacteria. In fact, the results of electronic structure calculations proved that the stability order of curcuminoids is CUR < DMC < BDMC. The mixture of synthetic curcuminoids was more effective in the inactivation of S. aureus compared to curcumin by itself; for all proposed mixtures, an equal or superior reduction was achieved. Full article