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Foods (Basel, Switzerland) May 2024Herbal teas have attracted attention as functional beverages containing luteolin and apigenin, which exhibit antioxidant and anti-inflammatory effects. The objective of...
Herbal teas have attracted attention as functional beverages containing luteolin and apigenin, which exhibit antioxidant and anti-inflammatory effects. The objective of this study was to develop a sensitive online automated method to determine these flavones' contents in herbal teas using in-tube solid-phase microextraction (IT-SPME) coupled with liquid chromatography-tandem mass spectrometry (LC-MS/MS). These compounds were extracted and concentrated by IT-SPME using a Supel Q PLOT capillary column and then separated and detected within 6 min using a CAPCELL PAK C18 MG III analytical column and a negative electrospray ionization-mode multiple-reaction monitoring system by LC-MS/MS. The detection limits ( = 3) for luteolin and apigenin were 0.4 and 0.8 pg mL, respectively, and the calibration curves were linear in the range of 2-2000 pg mL with correlation coefficients above 0.9995, and intra-day and inter-day precisions with relative standard deviations below 2.9 and 3.6% ( = 6), respectively. The luteolin and apigenin in herbal tea were quantified using IT-SPME/LC-MS/MS following the acid hydrolysis of their glycosides. Among the 10 herbal teas tested, luteolin was detected in peppermint and sage at concentrations of 375 and 99 µg mL, respectively, while apigenin was detected in German chamomile at 110 µg mL, which were higher than in the other herbal teas. The method is expected to be a useful method for evaluating the efficacy of luteolin and apigenin in herbal teas as functional beverages.
PubMed: 38890915
DOI: 10.3390/foods13111687 -
RSC Advances Jun 2024This study explored the flavonoid-rich extract of beetroot ( L.) for type 2 diabetes mellitus (T2D) and Alzheimer's disease (AD) dual therapy by using and molecular...
This study explored the flavonoid-rich extract of beetroot ( L.) for type 2 diabetes mellitus (T2D) and Alzheimer's disease (AD) dual therapy by using and molecular simulation studies. Flavonoid-rich extracts of fruit were evaluated for their antidiabetic and anti-alzheimic activities. Molecular docking and dynamic simulation were performed to identify potential bioactive flavonoids with dual therapeutic effects on T2D and AD. Flavonoid-rich extracts of fruit (IC = 73.062 ± 0.480 μg mL) had moderate activity against α-amylase compared to the standard acarbose (IC = 27.104 ± 0.270 μg mL). Compared with acarbose, flavonoid-rich extracts of fruit had appreciable activity against α-glucosidase (IC = 17.389 ± 0.436 μg mL) (IC = 37.564 ± 0.620 μg mL). For AChE inhibition, flavonoid-rich extracts of fruit exhibited ( < 0.0001) inhibitory activity (IC = 723.260 ± 5.466 μg mL), albeit weaker than that of the standard control, galantamine (IC = 27.950 ± 0.122 μg mL). Similarly, flavonoid-rich extracts of fruit showed considerable ( < 0.0001) inhibitory effects on BChE (IC = 649.112 ± 0.683 μg mL). In contrast, galantamine (IC = 23.126 ± 0.683 μg mL) is more potent than the extracts of fruit. Monoamine oxidase (MAO) activity increased in FeSO-induced brain damage. In contrast, flavonoid-rich extracts of fruit protected against Fe-mediated brain damage by suppressing MAO activity in a concentration-dependent manner. HPLC-DAD profiling of the extracts identified quercetrin, apigenin, rutin, myricetin, iso-quercetrin, -coumaric acid, ferulic acid, caffeic acid, and gallic acid. Molecular docking studies revealed quercetrin, apigenin, rutin, iso-queretrin, and myricetin were the top docked bioactive flavonoids against the five top target proteins (α-amylase, α-glucosidase AchE, BchE, and MAO). Molecular dynamic simulations revealed that the complexes formed remained stable over the course of the simulation. Collectively, the findings support the prospect of flavonoid-rich extracts of root functioning as a dual therapy for T2D and AD.
PubMed: 38887650
DOI: 10.1039/d4ra03638g -
ACS Omega Jun 2024Apigenin, a flavonoid, is reported to have multiple health benefits including cancer prevention; this study evaluates the drug likeliness and Swiss ADME properties of...
Apigenin, a flavonoid, is reported to have multiple health benefits including cancer prevention; this study evaluates the drug likeliness and Swiss ADME properties of apigenin. Apoptosis, which is a key hallmark of cancer, is associated with the deregulation of the balance between proapoptotic proteins and antiapoptotic proteins such as BCL-2,BCL-xl, BFL-1, BCL-w, BRAG-16, and MCL-1. The docking studies of apigenin with the mentioned proteins was performed to identify the interactions between the ligand and proteins, which suggested that apigenin was able to bind to most of the proteins similar to the inhibitory molecules of its native structure. A remarkable reduction in the total energy after energy minimization of apigenin-antiapoptotic protein complexes suggested increased stability of the docked complexes. The same complexes were found to be stable over a 10 ns period of molecular simulation at 300 K. These findings advocated the study to evaluate apigenin's potential to inhibit the HeLa cells at 5, 10, and 15 μM concentrations in the clonogenic assay. Apigenin inhibited the colony-forming ability of HeLa cells in a dose-dependent manner over a fortnight. Light microscopy of the treated cells displayed the morphological evidence characteristic of apoptosis in HeLa cells such as blebbing, spike formation, cytoplasmic oozing, and nuclear fragmentation. Thus, these results clearly indicate that apigenin may be used as a potential chemopreventive agent in cervical cancer management.
PubMed: 38882173
DOI: 10.1021/acsomega.4c01300 -
Translational Cancer Research May 2024Apigenin is a natural flavonoid compound with proven antitumor activity. However, its precise underlying pharmacological mechanism remains unclear. Oxaliplatin (OXA) is...
BACKGROUND
Apigenin is a natural flavonoid compound with proven antitumor activity. However, its precise underlying pharmacological mechanism remains unclear. Oxaliplatin (OXA) is commonly utilized for cancer treatment as a platinum-based chemotherapy drug. However, the utilization of low-dose OXA carries the risk of inducing epithelial-mesenchymal transition (EMT) in cancer cells and promoting tumor metastasis, thereby giving rise to potential side effects. The purpose of this study is to investigate the synergistic inhibitory effect of apigenin and OXA and its potential mechanism.
METHODS
HSC-3 cells of oral squamous carcinoma cells (OSCCs) were divided into control, apigenin-treated and co-treated groups. A wound healing assay was conducted to assess alterations in cellular motility and migration, an invasion assay was performed to assess invasiveness, and a three-dimensional culture assay was employed to evaluate angiogenic capacity. Cultured cells were utilized for total DNA extraction, followed by reverse transcription. Relative RNA levels were obtained, and quantitative polymerase chain reaction (qPCR) analysis was conducted to assess the efficiency of LINC00857 expression.
RESULTS
The administration of a low dose of OXA promoted the migratory, invasive, and angiogenic capabilities of HSC-3 cells, while also regulating EMT-associated molecular markers to facilitate the process of EMT. The inhibitory impact on OSCC proliferation was enhanced by the synergistic effect of apigenin and OXA. Furthermore, the tumor-promoting effects induced by low-dose OXA were notably suppressed through LINC00857.
CONCLUSIONS
Evidence from this study indicates that apigenin can effectively suppress the metastasis of OSCC cancer cells induced by low-dose OXA through inhibiting the level of LINC00857, suggesting a promising therapeutic strategy.
PubMed: 38881938
DOI: 10.21037/tcr-23-2335 -
BMC Complementary Medicine and Therapies Jun 2024Alzheimer's disease is a neurodegenerative age-related disease that primarily affects the elderly population leading to progressive memory impairments and neural...
BACKGROUND
Alzheimer's disease is a neurodegenerative age-related disease that primarily affects the elderly population leading to progressive memory impairments and neural deficits. It is counted as a major cause of geriatric dependency and disability. The pathogenesis of Alzheimer's disease incidence is complex and involves various hypotheses, including the cholinergic hypothesis, deposition of β-amyloid plaques, neuroinflammation, oxidative stress, and apoptosis. Conventional treatments such as donepezil aim to delay the symptoms but do not affect the progression of the disease and may cause serious side effects like hepatoxicity. The use of natural candidates for Alzheimer's disease treatment has drawn the attention of many researchers as it offers a multitargeted approach.
METHODS
This current study investigates the metabolic profiles of total defatted methanolic extract of Vitex pubescens bark and its polar fractions, viz. ethyl acetate and n-butanol, using ultra-performance liquid chromatography-electrospray ionization-quadrupole time-of-flight tandem mass spectrometry(UPLC-ESI-QTOF/MS/MS) technique as well as evaluate the antioxidant using free radical scavenging assays, viz. DPPH and ABTS assays and in-vitro acetylcholinesterase inhibitory activities using Ellman's microplate assay.
RESULTS
Metabolic profiling revealed a total of 71, 43, and 55 metabolites tentatively identified in the defatted methanolic extract, ethyl acetate, and n-butanol fractions, respectively. Phenolic acids were the most abundant class, viz. benzoic acids, and acyl quinic acid derivatives followed by flavonoids exemplified mainly by luteolin-C-glycosides and apigenin-C-glycosides. Quantification of the total phenolic and flavonoid contents in the total defatted methanolic extract confirmed its enrichment with phenolics and flavonoids equivalent to 138.61 ± 9.39 µg gallic acid/mg extract and 119.63 ± 4.62 µg rutin/mg extract, respectively. Moreover, the total defatted methanolic extract exhibited promising antioxidant activity confirmed through DPPH and ABTS assays with a 50% inhibitory concentration (IC) value equivalent to 52.79 ± 2.16 µg/mL and 10.02 ± µg/mL, respectively. The inhibitory activity of acetylcholine esterase (AchE) was assessed using in-vitro Ellman's colorimetric assay, the total defatted methanolic extract, ethyl acetate, and n-butanol fractions exhibited IC values of 52.9, 15.1 and 108.8 µg/mL that they proved the significant inhibition of AchE activity.
CONCLUSION
The results obtained herein unraveled the potential use of the total methanolic extract of Vitex pubescens bark and its polar fractions as natural candidates for controlling Alzheimer's disease progression.
Topics: Plant Extracts; Antioxidants; Cholinesterase Inhibitors; Plant Bark; Tandem Mass Spectrometry; Vitex; Chromatography, High Pressure Liquid; Spectrometry, Mass, Electrospray Ionization; Humans
PubMed: 38877470
DOI: 10.1186/s12906-024-04520-3 -
Chemistry & Biodiversity Jun 2024This research focused on the molecular diversity of A. carambola collected from three Brazilian biomes (Cerrado, Amazônia, and Mata Atlântica), whose results revealed...
This research focused on the molecular diversity of A. carambola collected from three Brazilian biomes (Cerrado, Amazônia, and Mata Atlântica), whose results revealed significant differences in metabolite profiles among these biomes through PSI-MS analysis. Chemometric analysis provided valuable insights into the clustering patterns and metabolic distinctions. Cerrado and Mata Atlântica biomes exhibited a 70 % similarity, indicating a notable degree of resemblance. In Cerrado, carambolaside A was notably abundant, while carambolaside M was low in Amazônia and moderate in Cerrado samples. Carambolaside B was abundant in Amazônia but relatively low in the Cerrado and Mata Atlântica. In contrast, the Amazônia biome samples appeared to be more dissimilar. In Cerrado, epicatechin, kaempferol, and procyanidin B showed lower abundance, while apigenin, quercetin, myricetin, and rutin displayed moderate levels. Mata Atlântica showed relatively higher levels of kaempferol, quercetin, and rutin. This study indicated the environmental influence on secondary metabolites production in A. carambola fruits.
PubMed: 38874121
DOI: 10.1002/cbdv.202400458 -
Biomedicine & Pharmacotherapy =... Jul 2024
PubMed: 38871545
DOI: 10.1016/j.biopha.2024.116916 -
Food Chemistry Jun 2024Sesame leaves contain rich phenolic acids and flavonoids. However, their potential in nanozyme synthesis has not been investigated yet. Herein, we report the preparation...
Sesame leaves contain rich phenolic acids and flavonoids. However, their potential in nanozyme synthesis has not been investigated yet. Herein, we report the preparation of flavonoid-rich sesame leaf extract (SLE), composition identification, and its use in the construction of iron (Fe)-based nanozymes (Fe-SLE CPNs). SLE was obtained with an extraction yield of ∼14.5% with a total flavonoid content (TFC) of ∼850.85 mg RE/g. There were 83 flavonoid compounds in SLE, primarily including scutellarin, apigenin-7-glucuronid, narcissin, and hyperoside. Fe-SLE CPNs exhibited nanodot morphology with a hydrodynamic size of 79.34 nm and good stability in various physiological solutions, pH levels, and temperatures. The Fe-SLE CPNs were more efficient in the scavenging ability of reactive oxygen species (ROS) than SLE alone. Furthermore, a stronger anti-inflammatory effect of the Fe-SLE CPNs was shown by modulating the MyD88-NF-κB-MAPK signaling pathways. These findings imply that SLE-based nanozymes hold great potential for diverse applications.
PubMed: 38870817
DOI: 10.1016/j.foodchem.2024.140021 -
Chemistry & Biodiversity Jun 2024A new monoterpene, (-)-10-hydroxydihydroactinidiolide (1), along with two known monoterpenes, loliolide (2) and (+)-isololiolide (3), three known megastigmanes,...
A new monoterpene, (-)-10-hydroxydihydroactinidiolide (1), along with two known monoterpenes, loliolide (2) and (+)-isololiolide (3), three known megastigmanes, 3a-hydroxy-5β,6β-epoxy-β-ionone (4), 3a-hydroxy-5a,6a-epoxy-β-ionone (5), and (+)-dehydrovomifoliol (6), an eudesmane-type sesquiterpene, 4a-hydroxy-4β-methyldihydrocostol (7), a monoterpene, 8-hydroxycarvotanacetone (8), two flavonoids, chrysoeriol (9) and apigenin (10), and a phenylpropanoid, 3-(4-hydroxyphenyl)-1-propanol (11), were isolated from the whole plant of Achillea millefolium. The structure of compound 1 was identified according to spectroscopic data of HRMS and NMR, and its absolute configuration was assigned by 13C NMR calculations with DP4+ probability analyses and ECD calculations. The absolute configuration of compound 6 was determined by ECD calculations. Compounds 3, 6, 9 and 10 could dose-dependently inhibited the NO release in LPS-induced RAW267.4 cells.
PubMed: 38869958
DOI: 10.1002/cbdv.202400946 -
Nature Communications Jun 2024Urate, the physiological form of uric acid and a potent antioxidant in serum, plays a pivotal role in scavenging reactive oxygen species. Yet excessive accumulation of...
Urate, the physiological form of uric acid and a potent antioxidant in serum, plays a pivotal role in scavenging reactive oxygen species. Yet excessive accumulation of urate, known as hyperuricemia, is the primary risk factor for the development of gout. The high-capacity urate transporter GLUT9 represents a promising target for gout treatment. Here, we present cryo-electron microscopy structures of human GLUT9 in complex with urate or its inhibitor apigenin at overall resolutions of 3.5 Å and 3.3 Å, respectively. In both structures, GLUT9 exhibits an inward open conformation, wherein the substrate binding pocket faces the intracellular side. These structures unveil the molecular basis for GLUT9's substrate preference of urate over glucose, and show that apigenin acts as a competitive inhibitor by occupying the substrate binding site. Our findings provide critical information for the development of specific inhibitors targeting GLUT9 as potential therapeutics for gout and hyperuricemia.
Topics: Humans; Glucose Transport Proteins, Facilitative; Uric Acid; Apigenin; Cryoelectron Microscopy; Binding Sites; Protein Binding; Hyperuricemia; Models, Molecular; Gout; HEK293 Cells
PubMed: 38866775
DOI: 10.1038/s41467-024-49420-9