Search Results (55)

The herb and flowers of yarrow (Achillea millefolium) are sources of multiple bioactive secondary metabolites used in medicine and cosmetology. This study aimed to establish the location of phenolic compounds in tissues of flowers and stems of A. millefolium via light and fluorescence microscopy and histochemical assays. The spectrophotometric and HPLC methods were deployed to quantify total phenolic compounds (PC), phenolic acids, and flavonoids in extracts from flowers and herb, whereas the LC-QTOF-MS method was used for their qualitative analysis. The results demonstrated that PC occurred in external and internal tissues of yarrow stems, petals, and other parts of the flower, as well as in involucral bracts. Qualitative phytochemical analyses demonstrated ca. 16% more PC and flavonoids in flowers than in the herb. This analysis allowed identifying 48 PC. A higher number of PC was identified in flowers than in herbs, with rosmarinic acid followed by chlorogenic acid being the major polyphenols found in both sample types. One of the flavonoids, namely luteolin, was detected in significantly higher quantities in the flowers than in the herb. This study results provide new data on the location of PC in flowers and stems of A. millefolium as well as extend knowledge on their contents in the raw material of yarrow. Full article

Among aquatic organisms, marine dinoflagellates are essential sources of bioactive metabolites. The benthic dinoflagellate Coolia malayensis produces metabolites that have exhibited substantial and specific cytotoxicity on cancer cells; however, isolation and identification of the purified compounds remain a challenge. This study reports C. malayensis biomass multi-step extraction plus chemical analyses for identifying compounds with antineoplastic activity. Through bio-directed fractionation, the cytotoxicity of extracts and fractions was tested on H1299 (lung), PC-3 (prostate), HeLa (cervical), and MCF-7 (breast) cancer cell lines. Dichloromethane (DCM) phase, hydroalcoholic (HYD) secondary extract, and methanolic (MET) extract showed cytotoxic effects on all cell lines. Active extracts and fractions were analyzed by HPLC-QTOF-MS, ¹H, and ¹³C NMR. Cell lines H1299 and PC-3 treated with fractions F4, F7, and DCM2-AQ-Ch sub-extract showed morphological changes resembling those observed in the apoptosis control, and no signs of necrosis were observed. The selectivity of fraction F7 was above 100 μg mL⁻¹ for healthy cells, while cytotoxic activity was observed in cancer cells. This fraction was identified as mostly fatty acids (FA) by NMR. Seventeen compounds with reported biological activities, such as antioxidant, analgesic, antiviral, and anticancer, were identified from C. malayensis extracts and fractions. Among them, the phycotoxins gambieric acid A and B, okadaic acid, and dinophysistoxin-1 were detected. Further studies are needed to reveal more significant anti-cancer potential from C. malayensis. Full article

Human exposure to mycotoxins is a global concern since several mycotoxins, such as enniatins and aflatoxins, have shown carcinogenic and neurotoxic effects, and the toxicologic mechanisms of most of them still need to be clarified. This study aims to investigate the metabolic pathways affected by mycotoxin exposure by evaluating metabolite alterations in urine. The participants were 540 women from the Spanish Childhood and Environment Project (INMA). For metabolite identification, a dilute and shoot extraction, followed by HPLC-Q-TOF-MS identification analysis, was performed. Data were processed using Agilent Mass Hunter Workstation with the METLIN database, Agilent Mass Profiler Professional 10.0, and Metaboanalyst 6.0. Over 2000 metabolites were obtained in each sample after feature extraction, and the most significant metabolites (p-value ≤ 0.05, fold change ≥ 2.0) were considered for pathway analysis. Enrichment analysis and topology showed that the most significantly affected pathway was the biosynthesis of unsaturated fatty acids (adjusted p-value = 0.007), with four metabolomic hits associated: linoleic acid, octadecanoic acid/stearic acid, an arachidonic acid metabolite, and (9Z)-octadecenoic acid/oleic acid. Other related pathways (unadjusted p-value ≤ 0.1) included fatty acid biosynthesis, glycerophospholipid metabolism, and ether lipid metabolism. The present study highlights the importance of metabolomics in increasing knowledge of the toxicity mechanisms and health effects of mycotoxins, especially emerging ones. Full article

The division of labor among honeybee workers contributes to efficient pollination activities. Lipids play a crucial role in behavioral regulation, with pollen serving as a primary source of these lipids. However, the regulatory effect of pollen lipids on the division of labor of honeybee workers remains to be studied. In this study, an in-depth lipidomic analysis based on HPLC-QTOF-MS and UPLC-IM-QTOF-MS was applied. We conducted the first comprehensive lipidomic profiling of the abdomen, brain, and intestine of emerging, nursing, and foraging bees, as well as pollen, thereby establishing a lipid library comprising 646 lipid species. The lipid composition of pollen was found to exhibit characteristics similar to those of honeybee workers, with alpha linolenic acid (ALA) validated as a key labor characteristic lipid. Moderate dietary ALA supplementation reshaped lipid levels and facilitated metabolism related to the labor of division. These findings advance the field of lipidomic analysis in honeybee workers, revealing a novel behavioral regulator and extending the understanding of the nutritional regulation of ALA in the division of labor among honeybee workers. Full article

Avocado (Persea americana Mill.) is a widely cultivated fruit known for its nutritional benefits, with the seed representing a significant portion of the fruit that is often discarded as waste. In the Dominican Republic, the cultivar Semil 34 represents 58% of the national production. This study aimed to explore the potential of Semil 34 avocado seed (AS) as a source of bioactive compounds with applications in the food industry. We conducted the chemical characterization of the seed extract, focusing on its total phenolic content, total flavonoids, and antioxidant capacity. High-performance liquid chromatography–quadrupole time-of-flight mass spectrometry (HPLC-QTOF-MS) was employed to identify key phytochemicals, including phenolic acids and flavonoids, that were responsible for the antioxidant properties of the extract. The hydroalcoholic extract of the Semil 34 seeds exhibited an antioxidant capacity of 1743.3 ± 52.3 µM Trolox/g extract, total phenolic content of 25.86 ± 2.17 mg gallic acid equivalents/g extract, and total flavonoid content of 2.09 ± 0.10 mg quercetin equivalents/g extract. However, the extract’s antioxidant capacity was found to be sensitive to pH changes, suggesting the need for stabilization when used in acidic or basic food matrices. The present work identified 53 compounds in the Semil 34 seed extracts; among these, 23 are being reported for the first time in avocado seeds. This study demonstrates the potential of the avocado seed as a source of bioactive compounds and hence a functional ingredient, supporting its value in sustainable production and its possible contribution to environmental goals by reducing waste in the avocado industry. Full article

Phenolic allelochemicals from root exudates dominate rhizosphere formation, lead to autotoxicity in plants subjected to continuous monoculture (CM) stress and induce the emergence of replant disease. However, the regulatory mechanisms governing the transport of phenolics from plant roots to the rhizosphere remain poorly understood. A potential phenolic efflux transporter from Rehmannia glutinosa, designated RgMATE35, has been preliminarily characterized. The objective of this study was to elucidate the molecular function of RgMATE35 in the secretion of phenolics and to investigate its role in the development of plant replant disease using quantitative real-time PCR (qRT-PCR), genetic transformation, HPLC-Q-TOF-MS and other analytical techniques. A tissue expression pattern analysis of RgMATE35 revealed that it is highly expressed in plant roots. Transient expression analysis confirmed the localization of the protein in plasma membranes. An assessment of the transport activity of RgMATE35 in Xenopus oocytes indicated that it plays a role in facilitating the efflux of labeled ferulic acid ([²H₃]-FA) and trans-p-coumaric acid [²H₆]-pCA. The results of functional studies in R. glutinosa demonstrated that RgMATE35 positively mediates the secretion of FA and pCA from plant roots into the rhizosphere. A molecular and physiological analysis of RgMATE35 transgenic plants subjected to CM stress revealed that the overexpression or repression of RgMATE35 resulted in notable changes in the degree of autotoxic injury in plants. These findings demonstrate that RgMATE35 plays a positive role in the development of replant disease through the secretion of phenolic acids from plant roots. They also provide a fundamental framework for elucidating the molecular regulatory mechanism through which MATEs regulate replant disease through the root secretion of allelochemicals. Full article

Papaya leaves have been used as food and traditional herbs for the treatment of cancer, diabetes, asthma, and virus infections, but the active principle has not been understood. We hypothesized that the anti-inflammatory activity could be the predominant underlying principle. To test this, we extracted papaya leaf juice with different organic solvents and found that the ethyl acetate (EA) fraction showed the most outstanding anti-inflammatory activity by suppressing the production of nitric oxide (NO, IC₅₀ = 24.94 ± 2.4 μg/mL) and the expression of pro-inflammatory enzymes, such as inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX-2), and cytokines including interleukins (IL-1β and IL-6), and a tumor necrosis factor (TNF-α) in lipopolysaccharide (LPS)-induced RAW 264.7 cells. Transcriptomic analysis and Western blot results revealed its anti-inflammatory mechanisms were through the MAPK signaling pathway by inhibiting the phosphorylation of ERK1/2, JNKs, and p38 and the prevention of the cell surface expression of TLR4. Furthermore, we discovered that the EA fraction could inhibit the replication of alpha-coronavirus (HCoV-229E) and beta-coronavirus (HCoV-OC43 and SARS-CoV-2) and might be able to prevent cytokine storms caused by the coronavirus infection. From HPLC-QTOF-MS data, we found that the predominant phytochemicals that existed in the EA fraction were quercetin and kaempferol glycosides and carpaine. Counter-intuitively, further fractionation resulted in a loss of activity, suggesting that the synergistic effect of different components in the EA fraction contribute to the overall potent activity. Taken together, our results provide preliminary evidence for papaya leaf as a potential anti-inflammatory and anti-coronavirus agent, warranting further study for its use for human health promotion. Full article

Ulva prolifera, a type of green algae that can be consumed, was utilized in the production of an angiotensin-I converting enzyme (ACE) inhibitory peptide. The protein from the algae was isolated and subsequently hydrolyzed using a neutral protease. The resulting hydrolysate underwent several processes including Sephadex-G100 filtration chromatography, ultrafiltration, HPLC-Q-TOF-MS analysis, ADMET screening, UV spectrum detection test, molecular docking, and molecular dynamic simulation. Then, the ACE inhibitory peptide named KAF (IC₅₀, 0.63 ± 0.26 µM) was identified. The effectiveness of this peptide in inhibiting ACE can be primarily attributed to two conventional hydrogen bonds. Additionally, it could activate endothelial nitric oxide synthase (eNOS) activity to promote the generation of nitric oxide (NO). Additionally, KAF primarily increased the intracellular calcium (Ca²⁺) level by acting on L-type Ca²⁺ channel (LTCC) and the ryanodine receptor (RyR) in the endoplasmic reticulum, and completed the activation of eNOS under the mediation of protein kinase B (Akt) signaling pathway. Our study has confirmed that KAF has the potential to be processed into pharmaceutical candidate functions on vasoconstriction. Full article

Achyranthes bidentata is always salt-processed before being prescribed for treating osteoarthritis. Yet the salt-processing parameters have not been optimized, and the specific bioactive constituents responsible for the osteoarthritis effect of salt-processed A. bidentata have not been fully elucidated. In this study, a Box–Behnken experimental design was chosen for the optimization of the salt-processing parameters of A. bidentata, including stir-frying time, concentration of brine, and soak time. Meanwhile, HPLC–Q-TOF-MS was utilized to analyze the chemical profiles of various batches of raw and salt-processed A. bidentata. The anti-inflammatory potential of nine batches of both raw and salt-processed A. bidentata was assessed via a cyclooxygenase-2 (COX-2) inhibitory assay. A gray correlation analysis was conducted to correlate the peak areas of the compounds in raw and salt-processed A. bidentata with their COX-2 inhibitory effects. Finally, the optimal salt-processing conditions are as follows: soak time: 29 min; concentration of brine: 1.8%; stir-frying time: 4.4 min. Twenty-nine compounds were identified. Eight compounds were found to have a strong positive correlation with anti-inflammatory activity, as confirmed by the COX-2 inhibitory assay. Notably, this is the first report of the COX-2 inhibitory effects of sanleng acid, stachysterone D, dihydroactinidiolide, N-cis-feruloyl-3-methoxytyramine, 9,12,13-trihydroxy-10-octadecenoic acid, azelaic acid, and dehydroecdysone. Full article

In this study, Asparagus stipularis was characterized concerning its phytochemical composition, antioxidant potential, cytotoxicity, and pancreatic lipase inhibitory activities. Twenty-seven compounds were identified and quantified by HPLC-DAD-MS in the leaf, stem, pericarp, and rhizome of ethanolic extracts. Seven steroidal saponins were detected, and the highest content was quantified in rhizome and pericap. A. stipularis also contained significant amounts of flavonoids in the aerial part. Isorhamnetin tetra-glycoside, quercetin-3-glucosyl-rutinoside, and rutin were the main flavonoid derivatives in leaf, stem, and pericarp extracts, respectively. In addition, eleven phenolic acids were also detected; among them, caffeic acid, protocatechuic acid, p-hydroxybenzoic acid, and ferulic acid were the predominant phenolics, with these having the highest amounts quantified in the rhizome extracts. All the tested extracts possessed antioxidant capacities, with pericarp and rhizome extracts exhibiting the highest activity in DPPH, ABTS, and FRAP assays. The extracts from pericarp and rhizome were revealed to also be the strongest inhibitors of pancreatic lipase. The rhizome extracts exhibited potent cytotoxic activity against HCT-116 and HepG2 with IC50 values of 30 and 54 µg/mL after 48 h of treatment. The present study demonstrated that A. stipularis can be used as a new source of natural antioxidants and potential anticancer and antiobesity compounds. Full article

The aim of this study was to determine the relationship between antioxidant and anticancer properties of extracts from blackcurrant (Ribes nigrum L.) leaves and their fractions and chemical contents. Dried ethanolic extract was divided into three fractions using solid phase extraction: aqueous (F1), 40% MeOH (F2), and 70% MeOH (F3). Both the extract and the fractions were analyzed in terms of antiradical activity (DPPH^• and ABTS^+•), total phenolic compounds, and total flavonoids. The antitumor potential of the fractions was evaluated in vitro on human colorectal (HCT 116) and prostate (PC-3) cancer cells. Phenolics were identified using HPLC-QTOF-MS, and twelve compounds were quantified by HPLC-DAD. Finally, principal component analysis was carried out to assess the relationship between the tested factors. The results confirmed that blackcurrant leaves are a rich source of phenolics with high antioxidant activity and anticancer properties. It was demonstrated that the F2 fraction had the highest content of phenolics and the highest antiradical activity. Additionally, only this fraction showed cytotoxic activity against HCT 116 cells. It was confirmed that both the blackcurrant leaf extract and its fractions are a promising source of condensed active compounds and can be used as natural functional food additives. Full article

Cadmium (Cd) pollution is an important environmental problem, as it is easily absorbed by plants and gradually accumulates in the human body through the food chain. This study aimed to elucidate the changes in the metabolic response of the rice cultivar “TanLiangYou215” under Cd stress. Rice was grown in soil culture at 0 (Control), 2 (Low group), and 10 (High group) mg/kg CdCl₂ for 90 days. The ultrastructural, Cd content, antioxidant activity, and metabolic changes to the rice in different tissues were analyzed. Phenotypic characterization and ultrastructure showed that the rice roots and leaves were significantly damaged and plant growth was inhibited in the High group, while plant growth was promoted in the Low group. Overall, Cd showed a regularity of “low promotion and high inhibition”. Physiological indices revealed that rice was significantly affected by Cd stress. Compared to the Control, Cd stress resulted in higher antioxidant enzyme activities, and the Low group suffered less oxidative damage than the High group. Metabolomic studies revealed that Cd stress significantly altered the metabolic profiles of rice plants. Rice responded to Cd stress by upregulating amino acids and regulating related pathways, including alanine, aspartate and glutamate metabolism, and arginine and proline metabolism. The significant expression of flavonoids with antioxidant properties helped rice resist the oxidative damage caused by Cd accumulation in the root tissue; Cd stress significantly downregulated glycerophospholipid metabolism in the stem and leaf tissues, which affected the cellular activities in rice stem and leaf tissues. We investigated the effects of Cd stress on ultrastructure, antioxidant activity, and metabolic changes in different tissues of the rice variety TLY215. Moreover, the different tissues of TLY215 can regulate these metabolic pathways to resist Cd stress, which provides valuable insights into the response of TLY215 to different concentrations of Cd. Full article

Cichorium glandulosum Boiss. et Huet (CG) and Cichorium intybus L. (CI) are widely used as the main raw material of functional food with hepatoprotective and hypoglycemic effects. Due to the lack of comparison on the chemical ingredients and efficacy, they were often used imprecisely and interchangeably. It is necessary to distinguish between them. With the plant metabolomics based on high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (HPLC-QTOF-MS) and multivariate chemometric techniques, the chemical ingredients were characterized and 59 compounds between CG and CI were classified. As for antioxidative and hypoglycemic activities in vitro, CI extraction exhibited better antioxidant activity than CG, while CG extraction showed stronger hypoglycemic activity. Furthermore, a bivariate correlation between the chemical composition and efficacy of the extract was also analyzed, and three differentially strong correlation components between CI and CG were prepared, and the antioxidative and hypoglycemic efficacies were compared in vivo and different active phenotypes were obtained. Finally, we revealed chemical and biological differences between CG and CI, providing a basis for achieving better quality control and developing more effective functional foods. Full article

Parishin compounds are rare polyphenolic glucosides mainly found in the rhizome of the traditional Chinese medicinal plant, Gastrodia elata. These constituents are reported to have several biological and pharmacological activities. In the present study, two novel parishin derivatives not previously reported as plant-based phytochemicals were identified from a twig of Maclura tricuspidata (MT) and two new compounds were elucidated as 1-(4-(β-d-glucopyranosyloxy)benzyl)-3-hydroxy-3-methylpentane-1,5-dioate (named macluraparishin E) and 1,3-bis(4-(β-d-glucopyranosyloxy)benzyl)-3-hydroxy-3-methylpentane- 1,5-dioate (macluraparishin C), based on the experimental data obtained by UV–Visible (UV–Vis) spectroscopy, high performance liquid chromatography–quadrupole time-of-flight mass spectrometry (HPLC-QTOF-MS) and nuclear magnetic resonance (NMR) spectroscopy. Additionally, gastrodin, parishin A and parishin B were positively identified by spectroscopic evidence and the comparison of HPLC retention time with the corresponding authentic standards. Gastrodin, parishin A and parishin B, macluraparishin E and macluraparishin C were found to be the most abundant constituents in the MT twig. The compositions and contents of these constituents were found to vary depending on the different parts of the MT plant. In particular, the contents of parishin A, parishin B, macluraparishin C and macluraparishin E were higher in the twig, bark and root than in the leaves, xylem and fruit. Full article

To clarify the differences in the clinical application scope of Chrysanthemum morifolium flower (CMF) and Chrysanthemum indicum flower (CIF), two herbs of similar origin, an integrated strategy of network pharmacology, molecular pharmacology, and metabolomics was employed, with a view to investigating the commonalities and dissimilarities in chemical components, efficacy and mechanisms of action. Initial HPLC-Q-TOF-MS analysis revealed that CMF and CIF had different flavonoid constituents. The biological processes underlying the therapeutic effects of CMF and CIF on liver-fire hyperactivity syndrome of hypertension (LFHSH) were predicted to be related to inflammatory response, fatty acid production, and other pathways based on network pharmacology analysis. ELISA, molecular docking, Western blot, and metabolomics techniques showed similar effects of CMF and CIF in lowering blood pressure, resistance to tissue, organ and functional damage, and dyslipidemia. However, distinct effects were found in the regulation of inflammatory response, PI3K-Akt and NF-κB signaling pathways, lipid anabolism, renin-angiotensin system, and metabolic abnormalities. The comparable efficacies of CMF and CIF, despite having distinct mechanisms of action, may be attributed to the integration and counteraction of their different regulating capabilities on the above anti-LFHSH mechanisms. This study offers a vital platform for assessment of differential and precise applications of herbs of close origin with similar but slightly different medicinal properties, and provides a research strategy for bridging Chinese medicine and modern precision medicine. Full article