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As a common medicinal and edible plant, dandelion plays a crucial and significant role in the fields of traditional Chinese medicines, functional foods, healthcare products, daily chemicals, and feed additives, which are closely related to its rich chemical constituents and remarkable biological activities. Modern studies have demonstrated that dandelion contains all kinds of bioactive constituents, including flavonoids, amino acids, fatty acids, organic acids, phenolic acids, coumarins, lignans, polysaccharides, phytosterols, terpenes, glycoproteins, oligosaccharides, alkaloids, etc. Meanwhile, dandelion has been proven to possess antioxidant, antibacterial, anti-inflammatory, antitumor, antivirus, hypoglycemic, and hypolipidemic properties, as well as the ability to regulate hormone levels and protect some visceral organs. Among them, flavonoids derived from dandelion and their antioxidant activities have received considerable attention. This study reviews dandelion flavonoids and their in vitro and in vivo antioxidant activities by consulting and organizing relevant domestic and international works of literature to provide a scientific and theoretical basis for further research, development, and utilization of dandelion. [ABSTRACT FROM AUTHOR]

Introduction: Scutellaria baicalensis Georgi, a traditional Chinese medicine, is widely applied to treat various diseases among people, especially in East Asia. However, the specific active compounds in S. baicalensis aqueous extracts (SBAEs) responsible for the hypoglycemic and hypolipidemic properties as well as their potential mechanisms of action remain unclear. Objectives: This work aimed to explore the potential hypoglycemic and hypolipidemic compounds from SBAE and their potential mechanisms of action. Methodology: The in vitro inhibitory tests against lipase and α‐glucosidase, and the effects of SBAE on glucose consumption and total triglyceride content in HepG2 cells were first performed to evaluate the hypoglycemic and hypolipidemic effects. Then, affinity ultrafiltration liquid chromatography–mass spectrometry (LC–MS) screening strategy with five drug targets, including α‐glucosidase, α‐amylase, protein tyrosine phosphatase 1B (PTP1B), lipase and 3‐hydroxy‐3‐methylglutaryl‐coenzyme A reductase (HMGCR) was developed to screen out the potential active constituents from SBAE, and some representative active compounds were further validated. Results: SBAE displayed noteworthy hypoglycemic and hypolipidemic properties, and 4, 10, 4, 8, and 8 potential bioactive components against α‐amylase, α‐glucosidase, PTP1B, HMGCR, and lipase were initially screened out, respectively. The interaction network was thus constructed between the potential bioactive compounds screened out and their corresponding drug targets. Among them, baicalein, wogonin, and wogonoside were revealed to possess remarkable hypoglycemic and hypolipidemic effects. Conclusion: The potential hypolipidemic and hypoglycemic bioactive compounds in SBAE and their mode of action were initially explored through ligand–target interactions by combining affinity ultrafiltration LC–MS strategy with five drug targets. The potential hypolipidemic and hypoglycemic bioactive compounds in aqueous extract of Scutellaria baicalensis Georgi root and their mode of action were firstly explored through ligand–target interactions by combining affinity ultrafiltration LC‐MS strategy with five drug targets, that is, α‐amylase, α‐glucosidase, PTP1B, HMGCR, and lipase. [ABSTRACT FROM AUTHOR]

Introduction: Numerous species of the Euphorbiaceae family, including Euphorbia maculata, Euphorbia humifusa, and Acalypha australis, have been used to manage bleeding disorders. However, few investigations have demonstrated their hemostatic potential, and their procoagulant compounds remain elusive. Objective: This study aimed to determine the most active procoagulant extracts from the three species' crude extract (CE) and fractions in order to screen out the active compounds and to analyze their possible mechanisms of action. Methods: An integrative approach, comprising prothrombin time and activated partial thromboplastin time evaluations and urokinase‐type plasminogen activator (uPA) inhibitory assessment, followed by bio‐affinity ultrafiltration paired with UPLC/QTOF‐MS targeting uPA and docking simulations, was used. Results: The extracts with highest procoagulant activity were the CE for both E. maculata (EMCE) and E. humifusa (EHCE) and the n‐butanol fraction (NB) for A. australis (AANB). The most promising ligands, namely, isoquercetin, orientin, rutin, and brevifolin carboxylic acid, were selected from these lead extracts. All of these compounds exhibited pronounced specific binding values to the uPA target and showed tight intercalation with the crucial side chains forming the uPA active pocket, which may explain their mode of action. The activity validation substantiated their hemostatic effectivity in inhibiting uPA as they had better inhibition constant (Ki) values than the reference drug tranexamic acid. Conclusion: Collectively, the integrative strategy applied to these three species allowed the elucidation of the mechanisms underlying their therapeutic effects on bleeding disorders, resulting in the fast detection of four potential hemostatic compounds and their mode of action. The four most promising ligands (isoquercetin, orientin, rutin, and brevifolin carboxylic acid) against uPA target were firstly selected in the active fractions extracted from E. maculata (EMCE), E. humifusa (EHCE), and A. australis (AANB), and their activity validation substantiates their hemostatic effectivity in mediating uPA as they expressed great constant inhibition (Ki) compared to the reference drug. [ABSTRACT FROM AUTHOR]

Parasitic infections impose a significant burden on public health worldwide. European pharmacopoeia records and ethnopharmacological studies indicate that Hagenia abyssinica (Bruce) J.F. Gmel. has traditionally been used to treat a variety of parasitic infections, while the potential antiparasitic compounds remain ambiguous. Acetylcholinesterase (AChE), lactate dehydrogenases (LDH), and glutathione reductase (GR) are the key target enzymes in the survival of parasites. The aim of our work was to screen antiparasitic compounds targeting AChE, LDH, and GR from H. abyssinica. Ultrafiltration-liquid chromatography–mass spectrometry (UF-LC–MS) combined with molecular docking was used in this study. Therein, the alamarBlue® and Ellman's methods were employed to reveal the antitrypanosomal effect and AChE inhibitory activity. Meanwhile, the UF-LC–MS was carried out to screen the potential active compounds from H. abyssinica. Subsequently, molecular docking was performed to evaluate the binding mechanisms of these active compounds with AChE, LDH, and GR. Finally, the AChE inhibitory activity of potential inhibitors was detected in vitro. H. abyssinica exhibited significant antitrypanosomal and AChE inhibitory activity. Corilagin, brevifolin carboxylic acid, brevifolin, quercetin, and methyl ellagic acid were recognized as potential AChE inhibitors by UF-LC–MS, while methyl brevifolin carboxylate was identified as AChE, LDH, and GR multi-target inhibitor, with binding degree ranged from 20.96% to 49.81%. Molecular docking showed that these potential inhibitors had a strong affinity with AChE, LDH, and GR, with binding energies ranging from −6.98 to −9.67 kcal/mol. These findings were further supported by the observation that corilagin, quercetin, brevifolin carboxylic acid, and methyl brevifolin carboxylate displayed significant AChE inhibitory activity compared with the positive control (gossypol, 0.42 ± 0.04 mM), with IC 50 values of 0.15 ± 0.05, 0.56 ± 0.03, 0.99 ± 0.01, and 1.02 ± 0.03 mM, respectively. This study confirms the antiparasitic potential of H. abyssinica , supporting the traditional use of H. abyssinica in local ethnopharmacology to treat parasites. At the same time, corilagin, brevifolin carboxylic acid, brevifolin, quercetin, methyl ellagic acid, and methyl brevifolin carboxylate exert their anti-parasitic effects by inhibiting AChE, LDH, and GR, and they are expected to be natural lead compounds for the treatment of parasitic diseases. [Display omitted] • Hagenia abyssinica exhibited good antiparasitic activity against T. b. brucei. • Explore AChE, LDH and GR inhibitors from H. abyssinica with an integrated strategy. • Six compounds revealed as potential AChE inhibitors. • Methyl brevifolin carboxylate was AChE, LDH, and GR multi-target inhibitor. • Mechanisms of enzyme-inhibitor interactions explored by molecular docking. [ABSTRACT FROM AUTHOR]

Introduction: Quaternary alkaloids (QAs) are the major alkaloids in several traditional Chinese medicines, especially in Zanthoxylum simulans. However, few studies on enrichment of QAs from Z. simulans were conducted due to their high polarity and low content. Objective: To develop a weak cation exchange (WCX) solid‐phase extraction (SPE) coupled with liquid chromatography mass spectrometry (LC–MS) method to enrich and identify QAs from Z. simulans. Meanwhile, the qualitative and quantitative analyses of QAs were carried out based on the optimum conditions of the method. Methods: Fresh stem bark of Z. simulans was extracted with 70% aqueous methanol and enriched by WCX‐SPE. A high‐performance liquid chromatography coupled with tandem mass spectrometry (HPLC–MS/MS) with an electrospray ionisation (ESI) source was used for the qualitative and quantitative analyses of QAs. Results: Significant improvements were observed in resolution and abundance of the peaks with WCX‐SPE. The linearity, limit of detection (LOD) and limit of quantification (LOQ) were determined for this analytical method. The linear relationship (A = 338.85C – 187.72, R2 = 0.99) was explored in the range of 0.5 to 312.5 μg/mL for chelerythrine. The LOD and LOQ for chelerythrine standard solutions were 0.0539 μg/mL and 0.1798 μg/mL, respectively. In addition, 22 peaks were detected successfully with WCX‐SPE and nine of them are undetectable without the processing of WCX‐SPE. Conclusion: A highly selective and efficient method for simultaneous enrichment and identification of QAs from crude extract of Z. simulans was developed for the first time by combining WCX‐SPE with LC–MS. Quaternary alkaloids (QAs) are the major active alkaloids in Zanthoxylum simulans, but poorly studied due to lack of efficient enrichment method for QAs. WCX‐SPE method was developed for successful enrichment and quantitation of twenty‐two QAs, compared with only nine peaks detected without enrichment. The WCX‐SPE coupled with LC‐MS is a simple and fast method for the simultaneous enrichment and identification of QAs. [ABSTRACT FROM AUTHOR]

A phytochemical investigation onLagotis brevitubaled to the isolation and characterisation of 11 phenolic compounds:p-hydroxy-benzoic acid1, methyl 3,4-dihydroxybenzoate2, vanillic acid3, protocatechuic acid4, caffeic acid5, glucose ester of (E)-ferulic acid6,p-coumaric acid7, vanillin8, diosmetin-7-O-β-d-glucoside9, chrysoeriol10and luteolin11. Their structures were elucidated using spectroscopic methods and by comparison with data in the literature. Compounds1–6were first obtained from the genusLagotis, and compounds1–9were isolated fromL. brevitubafor the first time. Compound4and11displayed remarkable antioxidant activities against DPPH radical (IC50 = 5.60 ± 0.09, 27.5 ± 0.06 mg/L, respectively), which were superior to positive control rutin. And compound11was also superior to rutin in ABTS assay (IC50 = 2.04 ± 0.13 mg/L). [ABSTRACT FROM PUBLISHER]