The crude extract of B. dracunculifolia demonstrated significant cellular anti-inflammatory and antioxidant activities, likely associated with its phenolic composition and the presence of metabolites reported in this study for the first time in this species, particularly morin and coniferaldehyde.
Abstract
Background and Objectives: Baccharis dracunculifolia DC. (Asteraceae), the main botanical source of Brazilian green propolis, is recognized for its high content of bioactive secondary metabolites. Given this potential, this study aimed to characterize the chemical profile of the crude extract (CE) from the aerial parts of B. dracunculifolia and to investigate its anti-inflammatory, antiproliferative, antioxidant, and photoprotective properties. Predictive computational analyses were used to assist the interpretation of the experimental findings. Methods: The CE was obtained by dynamic maceration with ethanol and chemically characterized by UHPLC-MS/MS using external calibration curves. Anti-inflammatory activity was evaluated by inhibiting nitric oxide (NO) in RAW 264.7 macrophages, while cellular antioxidant activity (CAA) was determined in the same model. Antiproliferative activity was evaluated against the human tumor cell lines AGS, Caco-2, MCF-7, and NCI-H460, as well as non-tumor VERO cells. Additionally, antioxidant potential was investigated using classical colorimetric methods (DPPH, FRAP, and ABTS). The extract was also quantified for total phenolic and flavonoid content, as well as sun protection factor (SPF). Furthermore, complementary computational analyses included PASS prediction, SwissTargetPrediction, Gene Ontology enrichment using PANTHER, SwissADME profiling, and toxicity prediction with ProTox-III. Results: UHPLC-MS/MS analysis revealed a profile rich in flavonoids and phenolic acids and led to the identification of 14 compounds not previously reported in B. dracunculifolia according to the literature examined, notably the flavonoid morin and the phenylpropanoid coniferaldehyde detected at comparatively high concentrations (>600 µg/g). CE inhibited NO production (IC50 = 62.00 µg/mL) suggesting anti-inflammatory activity, and reduced intracellular oxidation by 81% (at 2000 µg/mL) in RAW 264.7 macrophages. The extract showed total phenolic content (83.62 to 540.40 µg gallic acid equivalents/mg of CE) and high levels of flavonoids (472.00–515.00 µg quercetin equivalents/mg of CE), antioxidant activity in the DPPH assay (IC50 = 0.86 mg/mL), and relevant photoprotective potential (SPF = 7.79–19.30). Antiproliferative activity was moderate to weak (GI50 = 165.00–257.00 µg/mL). In silico analyses identified predicted activities, molecular targets, and enriched biological processes related to redox homeostasis, inflammation, apoptosis, and cellular responses to UV radiation, suggesting biological functions potentially associated with the identified metabolites. Conclusions: The crude extract of B. dracunculifolia demonstrated significant cellular anti-inflammatory and antioxidant activities, likely associated with its phenolic composition and the presence of metabolites reported in this study for the first time in this species, particularly morin and coniferaldehyde. These findings expand the phytochemical knowledge of B. dracunculifolia and reinforce its potential as a source of bioactive compounds for pharmaceutical, nutraceutical, and photoprotective applications.
Objective: This study aimed to characterize the phytochemical composition of the methanolic leaf extract of Dendrocnide meyeniana (Alingatong) and to determine whether the biological activities reported for its identified constituents are reflected in the antioxidant and cytotoxic properties of the crude extract.
Methods: Gas chromatography-mass spectrometry (GC-MS) analysis was performed to identify the phytochemical constituents of the plant extract. The reported biological activities of the identified compounds were subsequently examined through published literature. Based on the presence of compounds previously associated with antioxidant and anticancer activities, antioxidant capacity was evaluated using the 2,2-diphenyl-1- picrylhydrazyl (DPPH) radical scavenging assay, while cytotoxic effects were assessed against MIA PaCa-2, AGS, 4T1, and WM-266-4 cancer cell lines, as well as HF16 normal fibroblast cells. Half-maximal inhibitory concentration (IC50) and selectivity index (SI) values were determined to evaluate cytotoxic potency and selectivity.
Results: GC-MS analysis identified 76 phytochemical constituents, predominantly alkanes, together with fatty acid methyl esters, terpenoids, and phenolic compounds. The extract demonstrated concentration-dependent DPPH radical scavenging activity (EC50=1096.17 μg/mL), although substantially weaker than ascorbic acid (EC50=7.83 μg/mL). Cytotoxicity assays revealed concentration-dependent reductions in cell viability across all tested cancer cell lines, with IC50 values ranging from 134.64±3.48 to 165.26±8.46 μg/mL. WM-266-4 melanoma cells exhibited the greatest sensitivity and highest selectivity toward the extract, with an IC50 value of 134.64±3.48 μg/mL and an SI of 1.23. Overall, selectivity indices ranged from 1.00 to 1.23, indicating limited selectivity relative to HF16 normal fibroblasts.
Conclusion: The antioxidant and cytotoxic activities observed in the methanolic leaf extract of D. meyeniana are consistent with the reported biological properties of several compounds identified through GC-MS analysis. Although the extract exhibited limited selectivity toward cancer cells, its pronounced activity against WM-266-4 melanoma cells highlights its potential as a source of bioactive compounds for further pharmacological investigation and mechanistic studies.
Noralyn Arcillo, Bonglee Kim, Olive Anies-Amparado· Asian Journal of Pharmaceuti...· 0 citations
Background/Objectives: Berberis species are recognized for their ethnomedicinal importance and phytochemical richness associated with antidiabetic activity. Although B. crataegina is widely distributed in the Turkish flora and has a history of traditional use, its phytochemical properties and biological activities remain less extensively investigated than those of other Berberis species. This study aimed to comparatively evaluate the phytochemical profiles, in vitro antidiabetic potential, and cytoprotective effects of extracts prepared from different parts of B. crataegina in a high-glucose-induced SH-SY5Y cell-based model of diabetic neuropathy. Methods: Crude hydroethanolic extracts (70% ethanol) were prepared from the leaves, flowers, shoots, roots, and fresh fruits of B. crataegina collected from Kızılcahamam, Ankara, Türkiye. The total phenolic and flavonoid contents, antioxidant capacities and α-glucosidase inhibitory activities of leaf, flower, shoot, root, and fruit extracts were determined. The cytoprotective effects of the crude extracts were evaluated in a high-glucose-induced SH-SY5Y cell model. The metabolomic profiles of the extracts were comparatively analyzed using liquid chromatography–quadrupole time-of-flight mass spectrometry (LC-QTOF-MS). The most active fruit extract was fractionated by reversed-phase vacuum liquid chromatography (RP-VLC), and the phytochemical contents and α-glucosidase inhibitory activities of the fractions were evaluated. The major phenolic compounds in the most active fruit extract were quantitatively determined using high-performance liquid chromatography–diode array detection (HPLC-DAD). The relationships between metabolites and biological activities were investigated through correlation analysis. Results: The fruit extract was distinguished by its α-glucosidase inhibitory activity, total phenolic content, antioxidant capacity, and cytoprotective effect in the high-glucose-induced SH-SY5Y cell model. It showed no marked cytotoxicity at concentrations ranging from 25 to 400 µg/mL and, at 25 µg/mL, attenuated the high-glucose-induced reduction in cell viability, restoring viability to a level close to that of the normal control. Untargeted metabolomic analysis identified 191 metabolites detected in at least two crude extracts, while the metabolites detected exclusively in the fruit extract were predominantly flavonoids and flavonoid glycosides. Fractionation showed that α-glucosidase inhibitory activity was mainly concentrated in the medium-polarity fractions; however, none of the fractions reached the activity level of the crude extract. Chlorogenic acid, rutin, caffeic acid, protocatechuic acid, quercetin, and quercetin-3-O-glucoside were detected and quantified in the fruit extract by HPLC-DAD. Correlation analysis indicated that the observed biological activities may be associated with phenolic acids, flavonoids, and other polyphenolic metabolites. Conclusions: The fruit extract of B. crataegina showed promising α-glucosidase inhibitory activity and cytoprotective effects in the high-glucose-induced SH-SY5Y cell model. The findings suggest that these effects may arise from the combined contribution of multiple constituents within a polyphenolic matrix rather than from a single compound; however, synergistic interactions were not experimentally demonstrated. These results support further evaluation of the fruit extract through mechanistic, in vivo, and standardization studies.
Yiğit Erkmen, Zekiye Ceren Arıtuluk Aydın, E. Koçak et al.· Pharmaceuticals· 0 citations
Erythroxylum nummularium is a native Brazilian species with limited phytochemical and pharmacological characterization. This study aimed to investigate the chemical composition and biological properties of methanolic extracts and fractions obtained from the leaves, branches, stem bark, and stem of the plant. Total phenolic content (TPC), total flavonoid content (TFC), total alkaloid content (TAT), and GC–MS profiling were combined with antioxidant (DPPH, β-carotene bleaching, TAC), antimicrobial, toxicological, and antinociceptive assays. The extracts exhibited substantial variation in TPC, TFC, and metabolite profiles, which strongly influenced their biological activities. The ethyl acetate fraction from the leaves (ELEN) showed the highest TPC and TFC, correlating with superior antioxidant performance, antimicrobial activity against Staphylococcus aureus, low toxicity in Artemia salina, and significant antinociceptive effects in mice, with an LD50 above 2000 mg/kg. In the antioxidant assays, the ethyl acetate fraction from the stem bark (ESBEN) exhibited the highest overall activity, likely due to its elevated levels of highly polar phenolics and flavonoids. Among the fractions characterized by GC–MS, DSBEN, DLEN, and DBEN were the most active, with phenolic acids, their methylated derivatives, and low-molecular-weight organic acids contributing synergistically to antioxidant activity. These findings identify E. nummularium as a promising source of structurally diverse metabolites with antioxidant, antimicrobial, and antinociceptive potential and support further investigation toward the development of natural bioactive agents.
Nilmara Santos da Silva, Ícaro Tuyá Caires Amorim, Flávio Mendes de Souza et al.· Antioxidants· 0 citations
This study investigated the extracts and bioactive constituents of the aerial parts of Polygonum aviculare L., a well-known traditional medicine for inflammation and diuresis, through bioactivity-guided investigation and molecular docking analysis. Solvent extracts demonstrated significant antioxidant, anti-α-glucosidase, and anti-inflammatory activities, supporting their value for further pharmacological investigation. Among the isolated compounds, gallic acid (1), quercetin (3), myricetin (4), avicularin (6), and isorhamnetin (7) exhibited excellent antioxidant activity in the DPPH assay (SC50 ≤ 6.50 μM) and were stronger than the positive control BHT (SC50 = 36.99 μM). Kaempferol (9) (IC50 of 4.50 µM) demonstrated the highest α-glucosidase inhibition, surpassing that of the clinically used acarbose (IC50 = 519.7 µM). Additionally, gallic acid and quercetin demonstrated significantly stronger NO inhibition than apigenin, while kaempferol showed comparable activity (IC50 = 15.06 ± 1.50 μM vs. 16.08 ± 1.86 μM for apigenin). Molecular docking analyses supported favorable interactions between the active compounds and α-glucosidase and inducible nitric oxide synthase (iNOS). Kaempferol reduced the expression of iNOS and COX-2 in LPS-stimulated RAW 264.7 macrophages and was associated with increased KLF4 and Arg-1 expression and decreased phosphorylation of p38 MAPK and IκBα, suggesting a potential role in promoting an anti-inflammatory M2-like macrophage phenotype. Structure–activity relationship analysis indicated that flavonoid aglycones and specific hydroxylation patterns contribute to the observed biological activities. Collectively, these findings identify quercetin and kaempferol as highly active constituents of P. aviculare and support their potential for further pharmacological investigation.
Background: Plectranthus vettiveroides is an aromatic medicinal herb traditionally used in Ayurvedic and Siddha medicine. Although previous studies have reported its antioxidant, antidiabetic, and anticancer properties, its phytochemical profile and broad biological activities remain incompletely characterised. In parts of South Asia, the roots (Vilamichai root) are traditionally soaked in drinking water for health benefits, but scientific evidence supporting this practice is limited. Objectives: This study aimed to characterise the phytochemical constituents of Plectranthus vettiveroides roots and evaluate their biological activities using multiple in vitro assays. Methods: Ethanolic root extracts were subjected to qualitative and quantitative phytochemical analyses. Their antidiabetic, anti-inflammatory, antilipidemic, antioxidant, antiurolithiatic, immunomodulatory, cytotoxic, and antibacterial activities were assessed using established in vitro methods. Results: Qualitative analysis demonstrated tannins, saponins, flavonoids, steroids, alkaloids, and anthraquinones. The extract contained high total phenolic (223.57 mg GAE/g) and flavonoid (173.19 mg QE/g) contents. It inhibited α-amylase (87.66%) and α-glucosidase (85.75%) activities, suppressed protein denaturation (88.22%), and exhibited strong antioxidant activity across multiple assays. The extract also inhibited calcium oxalate crystallisation, enhanced phagocytic activity, showed cytotoxicity against HeLa cells (IC₅₀ 267.44 µg/mL), and demonstrated antibacterial activity against Vibrio parahaemolyticus and Vibrio harveyi. Conclusion: Plectranthus vettiveroides root extract possesses diverse bioactive phytochemicals with promising antidiabetic, antioxidant, anti-inflammatory, antiurolithiatic, immunomodulatory, cytotoxic, and antibacterial properties. These findings support its traditional use as a health-promoting herbal preparation and warrant further in vivo and clinical studies to validate its therapeutic potential.
Srinivasan Parthasarathy, Parthasarathy Krubaa, Melapalayam Rengarajan Suchitra et al.· International Journal of Adv...· 0 citations
The dewberry, or Rubus caesius L. (Rosaceae), has long been used in traditional medicine, although scientific research has primarily focused on its roots and aerial portions. Notable biological activity associated with a rich phytochemical profile has been reported in these investigations. In contrast, limited information is available regarding the biological potential and chemical composition of R. caesius roots collected from Turkmenistan, Central Asia. The present study aimed to investigate, for the first time, the biological potential of R. caesius root extracts prepared as an aqueous infusion (a traditional, food-relevant preparation) and an ethanol extract (a polyphenol-enriching extraction), and to relate differences in bioactivity to UHPLC-QqQ-MS/MS-based phytochemical composition. The extracts were screened using complementary antioxidant assays (radical-scavenging and reducing power), a multi-target panel of enzyme inhibitory activities relevant to metabolic and cosmetic/neurobiological pathways (including α-amylase, α-glucosidase, acetyl-/butyrylcholinesterase, and tyrosinase), and antimicrobial/antifungal tests against representative bacterial and fungal strains. UHPLC-QqQ-MS/MS profiling revealed a root metabolome dominated by phenolic acids, flavonoids, and anthocyanin-related constituents, with clear qualitative and quantitative differences between infusion and ethanol extracts. In agreement with the chemical findings, both extracts expressed pronounced antioxidant capacity, while enzyme inhibition was extract-dependent, indicating that solvent polarity influenced the recovery of constituents responsible for carbohydrate-hydrolyzing enzyme and cholinesterase/tyrosinase inhibition. The antimicrobial and antifungal screenings demonstrated selective growth inhibition that varied by microorganism and extraction type. The integrated chemical–biological approach highlights R. caesius roots from Turkmenistan as a promising source of multifunctional natural products and provides baseline data to support their future use in nutraceutical, functional food, or phytopharmaceutical development.
Serdar Korpayev, Emre Can Buluz, Savas Kaya et al.· RSC Advances· 0 citations
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