Search Results (578)

Fritillaria species are rich in steroidal alkaloids and are traditionally used for various medicinal purposes. This study investigated the biological activities of methanol, tertiary alkaloid, and quaternary alkaloid extracts obtained from the bulbs of Fritillaria imperialis and Fritillaria pinardii. Methanol, tertiary alkaloid, and quaternary alkaloid extracts prepared from the bulbs of both species were analyzed for secondary metabolites using LC-HRMS. Antimicrobial, cytotoxic, antioxidant, anti-inflammatory, and anticholinesterase activities were evaluated using standard in vitro assays. LC-HRMS analysis identified fumaric acid as the major metabolite in both species, together with (-)-epigallocatechin, cynarin, herniarin and several pyrrolizidine alkaloid N-oxides. Antibacterial activity was restricted to Staphylococcus aureus, whereas alkaloid-rich fractions displayed strong antifungal activity, particularly against Aspergillus fumigatus and Candida spp., with inhibition zones reaching 40 mm. At 80 μg/mL, the most pronounced reductions in cell viability were observed for F. imperialis methanol extract in A549 cells (55.19 ± 2.74%) and for F. pinardii tertiary alkaloid extract and F. imperialis quaternary alkaloid extract in MCF-7 cells (49.68 ± 1.83% and 49.76 ± 1.09%, respectively), whereas all extracts maintained J774 macrophage viability above 94%. Antioxidant activity was most pronounced in the quaternary alkaloid extract of F. pinardii (DPPH IC₅₀ = 90.42 μg/mL; ABTS IC₅₀ = 57.22 μg/mL), although all extracts were less active than the reference antioxidants. The tertiary alkaloid extract of F. pinardii exhibited potent anti-inflammatory activity, showing 5-LOX inhibition comparable to indomethacin (IC₅₀ = 20.05 ± 0.23 μg/mL) and suppressing LPS-induced nitric oxide production by up to 62.22%. Among the tested samples, the tertiary alkaloid extract of F. pinardii exhibited the strongest cholinesterase inhibitory activity against AChE (IC₅₀ = 13.39 ± 0.02 μg/mL). The results indicate that both F. imperialis and F. pinardii extracts exhibit measurable biological activities under in vitro conditions, with the alkaloid-rich extracts of F. pinardii showing comparatively stronger antifungal, anti-inflammatory, and anticholinesterase effects. Full article

Cauliflower by-products represent a valuable source of bioactive compounds that can be valorized as functional ingredients within circular food systems; however, their stability is strongly influenced by processing conditions. This study evaluated the combined effects of plant section (leaves and stems) and drying method (freeze-drying, hot-air drying at 40 °C and solar drying at approximately 30–45 °C) on the nutritional composition, pigment content, antioxidant activity and colour of cauliflower by-product flours. Proximate composition, chlorophylls, carotenoids, total polyphenols, total flavonoids, glucosinolates, sulforaphane and antioxidant activity (ABTS and DPPH assays) were determined, and colour was assessed using CIELAB parameters (L*, a*, b*, chroma, hue angle and browning index). Freeze-drying showed the highest preservation of pigments, phenolic compounds, sulforaphane and antioxidant activity, followed by hot-air drying, while solar drying resulted in the lowest retention. Leaf-derived flours consistently presented higher pigment and phenolic contents and more favorable colour attributes than stem-derived flours. Antioxidant activity was strongly associated with matrices richer in pigments and phenolics. Although leaves exhibited higher glucosinolate contents, sulforaphane levels showed only minor differences between plant sections, suggesting that stem-derived fractions may also represent a valuable raw material considering their greater biomass availability and industrial scalability. Overall, these findings demonstrate that both plant section and drying method significantly influence the techno-functional quality of cauliflower by-product flours and should be jointly considered to optimize the development of stable, functional and sustainable food ingredients. Full article

The growing demand for clean-label products has intensified the search for natural and sustainable alternatives to synthetic colorants. Anthocyanins stand out as promising pigments due to their coloring capacity and bioactive properties. This study evaluated the efficiency of natural deep eutectic solvents (NADES) in extracting anthocyanins from agro-industrial by-products—molasses grass, black corn cobs, and grape skins—and their application in food and cosmetic matrices. A simplex-centroid mixture design with Response Surface Methodology was used to optimize solvent composition based on sorbitol, citric acid, and glycine. NADES showed high extraction efficiency, especially for black corn cobs, reaching 54.20 mg/100 g under optimized conditions. Although conventional extraction performed better for grape skins, NADES demonstrated competitive efficiency and superior environmental performance (AGREE index 0.73 vs. 0.58). The extracts were successfully incorporated into yogurt and moisturizing gel formulations. Yogurts maintained stable physicochemical properties and color, while gels showed good homogeneity and chromatic stability. These findings support the use of NADES as green solvents for recovering natural colorants from agro-industrial residues, with potential applications in sustainable food and cosmetic products. Full article

This study developed a two-step statistically integrated optimization framework to identify the effects of key fermentation medium components controlling hyaluronic acid (HA) biosynthesis by Streptococcus zooepidemicus. As an initial phase, the Plackett–Burman design was employed to identify the most influential components among yeast extract, casein, peptone, beef extract, MgSO₄·7H₂O, K₂HPO₄, KH₂PO₄, and (NH₄)₂SO₄ by conducting 12 fermentation runs, and 30 g/L of glucose was used as the carbon source. Among the eight ingredients, yeast extract, MgSO₄·7H₂O, and KH₂PO₄ were identified as the most significant factors in enhancing HA production. The following steps were based on the selection of the best carbon and yeast extract sources. Sucrose was selected as the optimal carbon source among glucose and lactose, and Tastone 900-Baker’s yeast extract was selected as the optimal nitrogen source among various yeast extract sources. The final phase of the optimization procedure employed the Box–Behnken design to determine the optimal concentrations of three ingredients: yeast extract (10–30 g/L), MgSO₄·7H₂O (0.2–2.0 g/L), and KH₂PO₄ (1–4 g/L). The results depicted that the optimized media formulation, composed of 30.0 g/L of yeast extract, 1.16 g/L of MgSO₄·7H₂O, and 4.0 g/L of KH₂PO₄, enhanced HA production and biomass OD600 to 545.9 mg/L with 1250–1500 kDa and 2.53 OD600 in a 250 mL shake flask scale, which was around a 10-fold increase in HA production compared with run #10 of Plackett–Burman (57.42 mg/L). This study provided preliminary results for future process conditions optimization, scale-up studies, and techno-economic evaluation. Full article

Background: Functional dyspepsia (FD) is a disorder of gut–brain interaction characterized by heterogeneous pathophysiological mechanisms, including altered gastric motility, visceral hypersensitivity, low-grade inflammation, impaired mucosal defence, and oxidative stress. Multi-target botanical strategies may represent a rational approach for addressing this complexity. Methods: This study evaluated the mechanistic rationale supporting a botanical formulation containing Zingiber officinale, Cynara scolymus, and Citrus limon extracts, here referred to as DyspepCyn^®. A focused narrative review was conducted to summarize the available mechanistic and clinical evidence for the three botanicals. In addition, the formulation was characterized through solubility testing in aqueous and biorelevant simulated gastrointestinal media, together with antioxidant assessment using ORAC and DPPH assays. Results: DyspepCyn^® showed favourable dispersion and solubility behaviour across simulated gastrointestinal conditions, with complete solubilization up to approximately 700 mg/100 mL in water and up to approximately 800 mg/100 mL in simulated intestinal fluids. No precipitation was observed in the tested media. The formulation also showed measurable antioxidant activity, with an ORAC value of 365 µmol Trolox equivalents/g and a DPPH radical scavenging EC₅₀ of 32 µg/mL. Conclusions: DyspepCyn^® combines botanicals with complementary actions on gastric motility, postprandial digestive processes, mucosal protection, and oxidative stress. The observed physicochemical stability and antioxidant capacity support the mechanistic rationale for this multi-target botanical strategy in FD. Clinical studies are required to confirm its efficacy in patients with FD. Full article

S. Tomé and Principe (STP) islands have been studied in recent years for their wide range of medicinal plants which exhibit several biological activities of great medicinal interest for some diseases. Experimental design for optimization of several parameters was carried out by a full-factorial test of two levels of three factors for secondary metabolite extraction from Rauvolfia caffra leaves. The best conditions for highest extraction of phenolic compounds (i.e., 89.90 μmoles gallic acid equivalent/g leaves) were obtained at 25 °C in H₂O and at 5 days of incubation. Several phytochemical assays were performed for characterization of these plant extracts, and the highest levels of TFC, DPPH and reducing power were obtained with aqueous plant extraction at 25 °C and for 5 days of incubation, whereas leaf extraction with water at 40 °C for 5 days of incubation revealed the highest levels of ABTS scavenging activity. The levels of SOD and superoxide radical scavenging activities were highest in plant extraction, with hexane at 25 and 40 °C for 5 days of incubation, respectively. The present report consists of a novel and intrinsic synchronous fluorescence and phosphorescence characterization of secondary metabolites from this plant extract. Intrinsic and non-destructive synchronous fluorescence was carried out in the range of 250 to 750 nm with a Δλ range of 5–30 nm, which exhibited several fluorescence peaks in hexane and aqueous plant extracts. On the other hand, intrinsic and non-destructive synchronous phosphorescence was also performed which also exhibited several peaks in aqueous and hexane extracts. 3D spectra of secondary metabolites confirmed the fluorescence peaks observed in SFS in plant extracts. FTIR spectroscopy was selected to investigate the structural properties of secondary metabolites in these plant extracts. Therefore, the present work describes a novel characterization of secondary metabolites by a non-destructive and intrinsic synchronous fluorescence technique for plant extracts. Full article

The effects of thermal and non-thermal pretreatments combined with different drying methods on the drying kinetics, physicochemical properties, and bioactive compounds of the Chilean wild mushroom Morchella conica were investigated. Fresh samples were subjected to hot-air drying (HAD, 60 °C), freeze-drying (FD), and a hybrid process (FD–HAD), applied directly or after pretreatments including thermal pre-drying (55 and 75 °C), ultrasound (US, 10 and 20 min), and high hydrostatic pressure (HHP, 600 MPa). Drying curves were successfully fitted using the Weibull model (R² > 0.987), showing that HAD combined with thermal and ultrasound pretreatments increased drying rates, while FD–HAD reduced total drying time. Freeze-drying better preserved color (ΔE < 2) and minimized shrinkage (<8%), whereas HAD produced darker samples and greater structural deformation. Water activity decreased below 0.30 in most treatments, ensuring microbiological stability. Thermal pretreatments enhanced total phenolic content, while FD preserved antioxidant capacity. Principal component analysis explained 62.2% of the total variance, revealing distinct quality profiles among drying methods. Overall, FD and hybrid FD–HAD combined with moderate pretreatments showed the best balance between drying efficiency and quality preservation, while HHP improved antioxidant properties under specific conditions. These findings highlight the potential of integrating innovative pretreatments with drying technologies to optimize processing of Morchella conica. Full article

Reliable analytical methods are essential for the assessment, effective quality control, and guarantee of consistent and reproducible performance of chemical profiles of non-psychoactive low-THC Cannabis sativa L. samples and their products. An integrated analytical approach was applied for the first time to evaluate low-THC C. sativa products on the Serbian legal market using chemometrics combined with five complementary techniques: ultraviolet–visible spectroscopy (UV–Vis), high-performance thin-layer chromatography (HPTLC), portable Raman spectroscopy, Fourier transform infrared spectroscopy (FTIR) and gas chromatography–mass spectrometry (GC–MS). HPTLC rapidly differentiated key cannabinoids with R_F at 0.39 and 0.61, while GC–MS enabled comprehensive identification of major cannabinoids (CBG and CBD). Spectroscopic fingerprints provided characteristic UV–Vis absorption maximum (215, 235, and 275 nm), Raman (1700, 1550, 1517, 1224, 1096 cm⁻¹) and FTIR marker bands (615, 1059, 1288, 1620, 2932 cm⁻¹), supporting robust monitoring. Principal component analysis (PCA) across all five techniques revealed two major distinct sample clusters and identified the most influential analytical signals. The combined separation, spectroscopic, and multivariate approach is proven to be effective for systematic cannabinoid content assessment, authentication, and chemical profiling within a process-oriented context, thus enabling effective quality control in the cultivation process by targeting compounds of interest. Full article

Microalgae and cyanobacteria have emerged as platforms for producing recombinant biologics, vaccine antigens, and bioactive compounds of pharmaceutical interest. However, their translation beyond proof-of-concept remains limited by light-field heterogeneity, gas–liquid mass-transfer constraints, product instability, and matrix complexity, all of which affect recovery, selectivity, and batch comparability. This review synthesizes and organizes published evidence using a process-engineering framework organized around product class, product localization, upstream–downstream coupling, and photobioreactor scale-up. It further considers the role of Quality by Design (QbD), model-informed development, techno-economic assessment (TEA), and life cycle assessment (LCA) in route selection and quality-oriented process development. Across the reported routes, the dominant burden shifts from disruption and clarification in intracellular products to extracellular stability and time-to-capture in secreted products, whereas biomass-based formulations are governed by potency and stabilization consistency, and analog-rich metabolites by profile control and selective fractionation. Current limitations include the scarcity of models that incorporate quality attributes as explicit outputs, the incomplete representation of regulated manufacturing burdens in TEA and LCA, and the lack of minimal, reproducible analytical panels adapted to product class and matrix. By framing these organisms as pharmaceutical process platforms rather than as hosts assessed only by titer, this review provides an engineering basis for scale-up, route prioritization, and controllable manufacturing. Full article

Jatobá is a fruit-bearing plant whose pod husk accounts for approximately 70% of the fruit weight, becoming a residue after consumption or processing. Recent studies indicate that this byproduct is a promising source of phenolic compounds. However, extraction process variables, particularly solvent composition, can significantly impact recovery yields, although their effect remains poorly understood. In this context, a simplex-centroid mixture design was applied to optimize the solvent system to maximize the extraction of phenolic compounds and antioxidants from jatobá fruit husk. Different combinations of water, methanol, and acetone were evaluated using TPC, ABTS, and FRAP as response variables. Statistical analyses confirmed the significance of the models, with no lack of fit and high coefficients of determination. Multi-response optimization using the desirability function identified a nearly equivalent mixture of water and acetone (51.52%:48.48%, water/acetone) as the optimal condition, yielding predicted values of 41.51 mg GAE/g dw (TPC), 340.36 µmol TE/g dw (ABTS), and 485.74 µmol TE/g dw (FRAP), which did not differ statistically from the experimental values obtained in the validation assay (40.64 mg GAE/g dw for TPC, 334.31 µmol TE/g dw for ABTS, and 482.69 µmol TE/g dw for FRAP). HPLC-DAD analysis revealed that the fruit husk is predominantly composed of monomeric and dimeric procyanidins, especially epicatechin and procyanidin B2. Overall, these findings demonstrate the effectiveness of mixture design in optimizing extraction conditions and highlight jatobá fruit husk as a promising byproduct for the sustainable obtention of phenolic compounds and antioxidants with potential applications in products intended for human consumption after security validation. Full article

This study aimed to develop a 100 mg immediate-release (IR) tablet containing dasatinib monohydrate, a tyrosine kinase inhibitor, using a Quality by Design (QbD) framework at laboratory scale. The development strategy focused on systematic identification and control of critical process parameters (CPPs) affecting tablet quality during wet granulation. Preformulation studies were conducted to evaluate key physicochemical properties of the active pharmaceutical ingredient (API), including solubility, particle size distribution, and crystallinity, which may influence dissolution behavior. A risk assessment approach based on preliminary hazard analysis (PHA) and failure mode and effects analysis (FMEA) was applied to identify high-risk process variables. Based on the risk assessment results, chopper speed during wet granulation and compression force during tableting were identified as critical process parameters. These factors were further investigated using a Design of Experiments (DoE) approach based on Define Custom Design (DCD) and response surface methodology (RSM) to evaluate their effects on critical quality attributes (CQAs), including dissolution performance, disintegration time, and tablet friability. Response surface analysis established a design space in which chopper speed ranged from approximately 2300–2500 rpm and compression force ranged from 11 to 13 kN, ensuring consistent tablet quality within the investigated operating range. The optimized process conditions produced tablets that satisfied predefined quality targets. Comparative dissolution studies demonstrated dissolution profiles comparable to the reference product across pH 1.2, 4.0, and 6.8 media, with similarity factor (f₂) values ranging from 51.18 to 85.23. The experimentally established design space demonstrated reproducible in vitro performance and physicochemical stability under accelerated storage conditions. Overall, this study demonstrates the practical application of a QbD-based development strategy integrating risk assessment and response surface optimization to improve process understanding and manufacturing robustness in wet granulation-based tablet production. Full article

Edible mushrooms have long been valued as functional foods and traditional remedies, yet a significant developmental gap hinders their transition from nutraceuticals to standardized pharmaceutical ingredients. This narrative review provides a comprehensive and integrative analysis of edible mushroom-derived bioactive compounds as emerging candidates for pharmaceutical development. It examines major chemical classes, including polysaccharides (e.g., β-glucans), proteins (e.g., lectins, FIPs), triterpenoids (e.g., ganoderic acids), nucleosides (e.g., adenosine and cordycepin), and phenolic compounds, which underpin immunomodulatory, anticancer, antioxidant, anti-inflammatory, and metabolic activities. Beyond bioactivity, the review critically examines the downstream processing pipeline required for translation into pharmaceutical ingredients, encompassing controlled biomass production, pre-extraction processing, extraction technologies, isolation and purification strategies, and structural elucidation techniques. Key bottlenecks are identified, including bioavailability limitations of β-glucans (2–5%), lack of standardization, limited human clinical evidence, and regulatory constraints, explaining why robust preclinical evidence has not consistently translated into clinical success. Emerging solutions are also highlighted, including application of multi-omics tools, nano-encapsulation strategies, and synthetic biology approaches to improve scalability and reproducibility. By synthesizing research on natural product chemistry, biotechnology, and pharmacology, this study maps the journey of edible mushrooms from traditional dietary components to pharmaceutical-grade ingredients, providing a focused resource for researchers and industry stakeholders aiming to navigate mushroom-based drug development. Full article

Brazil is home to one of the greatest biodiversities on the planet, with numerous plant species with unexplored pharmacological potential. In this study, the antifungal activity and cytotoxicity of crude extracts obtained from the seeds of Sterculia foetida L., Bulbostylis capillaris (L.) Kunth ex CB Clarke, and Pouteria caimito (Ruiz & Pav.) Radlk were investigated. The previously dehydrated seeds were subjected to extraction with physiological saline (saline extract), hexane (hexane extract) and sequential extraction with hexane followed by saline (hexane-saline extract). To determine antifungal activity via disk diffusion assays, broth microdilution based on the CLSI and evaluation of cellular specificity (EC₅₀) by redox metabolism with resazurin were performed on C. albicans ATCC 14053, C. albicans ATCC 24433 and non-albicans species Candida krusei ATCC 6258 and C. glabrata ATCC 22019. Cytotoxicity was evaluated in mouse bone marrow cells by determining the cytotoxic concentration (CC₅₀/24 h). The selectivity index (SI) was calculated as the ratio between CC₅₀ and EC₅₀. Statistical analysis of the data was performed via ANOVA, with the significance level set at p < 0.05. Saline, hexane, and hexane—saline extracts of S. foetida, as well as the saline extract of B. capillaris, showed selectivity indices higher than those of ketoconazole against C. albicans and C. krusei. With respect to C. glabrata, only the saline extract of B. capillaris demonstrated greater selectivity than the reference drug. All P. caimito extracts presented lower EC₅₀/24 h values than did ketoconazole but presented a low selectivity index, suggesting high cellular toxicity. The results obtained demonstrate that the crude extracts of S. foetida and B. capillaris seeds have significant antifungal activity and represent promising sources of bioactive compounds. Future studies should focus on the purification, isolation, and characterization of the active principles responsible for the observed activity. Full article

Socheongryong-tang (SCRT), traditionally used in East Asia for managing chills and fever, has recently gained attention for its immunomodulatory potential. This study aimed to elucidate the biological activity and signaling features associated with SCRT-mediated modulation of innate immune readouts in murine macrophages and to evaluate its effects on selected markers in a 5-fluorouracil (5-FU)-associated immune suppression model. Our findings reveal that SCRT significantly enhances phagocytic activity, production of nitric oxide and prostaglandin E₂, and the mRNA expression of cytokines, including tumor necrosis factor-alpha, interleukin-1 beta, and interleukin-6. These immunomodulatory effects are associated with activation of the reactive oxygen species/mitogen-activated protein kinases/nuclear factor-κB signaling axis. In vivo, SCRT administration in a 5-FU–treated mouse model attenuated immune suppression-associated changes, showing partial restoration of selected serum cytokine markers and immune response indices. Taken together, these results suggest that SCRT aqueous extract may attenuate chemotherapy-associated immune dysfunction; however, further studies incorporating immune cell profiling, functional immune assessments, and pathway- and contamination-control approaches are warranted to establish causality and translational relevance. Full article

The identification of bioactive substances among new chemical compounds is based on analyzing the relationships between structure, physicochemical properties, and potential biological activity. The aim of this study was to characterize the physicochemical properties of a group of 3,28-disubstituted betulin derivatives, which have demonstrated promising antiproliferative activity in an in vitro study. The experimental lipophilicity parameters of betulin derivatives were obtained by RP-TLC and compared with theoretical values determined using various computational programs. Physicochemical and pharmacokinetic parameters were calculated using the SwissADME and pkCSM programs. The relationships between lipophilicity parameters (R_M0 and logP_TLC) and the anticancer activity, and physicochemical and pharmacokinetic parameters of the studied triterpenoids were analyzed. Chemometric analysis (cluster analysis, principal component analysis, and the sum of ranking differences analysis) was performed. Significant correlations were demonstrated between R_M0 and logP_TLC, as well as theoretically determined lipophilicity values, in the tested group of compounds. Propynoyl derivatives 4a, 5a and 6a with high antiproliferative activity against MV4-11, PC-3 and Hs249T cells are characterized by higher lipophilicity than their hydroxyl analogs (compounds 4, 5 and 6). Full article