Xiao-Cui Zhuang

Taraxacum mongolicum Hand.-Mazz (TMHM), a primary source of dandelion, is a globally recognized edible and medicinal plant with significant potential in food, medicine, daily chemical products, and animal husbandry. Although hypoglycemic effects have been reported in other Taraxacum species, the specific hypoglycemic constituents and mechanisms of TMHM are not well understood. The absence of comprehensive multi-target screening methodologies has hindered the elucidation of TMHM’s dual inhibitory effects on α-amylase and α-glucosidase, as well as its associated molecular mechanisms. In this study, a multi-target screening strategy was developed to concurrently evaluate α-amylase and α-glucosidase inhibition, integrating multi-target affinity ultrafiltration coupled with ultra-performance liquid chromatography-tandem mass spectrometry (MTAUF-UPLC-MS/MS), molecular docking, and molecular dynamics (MD) simulations. Using this approach, 13 dual-target inhibitors were identified from TMHM. Moreover, at least 5 of these compounds exhibited anti-diabetic activities comparable to the positive control drug acarbose, suggesting that they are principal bioactive constituents responsible for its hypoglycemic effects. Subsequent investigation of the antioxidant capacities of 7 out of the 13 bioactive compounds revealed that most exhibited more potent antioxidant activities than vitamin C (Vc). Based on these findings, molecular docking and MD simulations further validated that quercetin (8) and kaempferol (15), which demonstrated significant hypoglycemic and antioxidant activities, exhibited particularly strong affinities and stable interactions with α-amylase and α-glucosidase, respectively. In conclusion, these findings underscored the considerable potential of TMHM as a natural source of multifunctional bioactive compounds for nutraceutical, functional, and pharmaceutical applications. This study provided a critical foundation for elucidating the mechanisms underlying TMHM’s anti-diabetic effects and its therapeutic potential in mitigating diabetes-related complications, thereby facilitating future development and utilization.

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.

Warburgia ugandensis Sprague (WU) is a traditional medicinal plant used for the treatment of various diseases, including cancer, in Africa. This study aimed to evaluate the anti-non-small cell lung cancer (NSCLC) activities of WU against A549 cells and to reveal potential molecular mechanisms. The cytotoxicity of various WU extracts was evaluated with HeLa (cervical cancer), HepG2 (liver cancer), HT-29 (colorectal cancer), and A549 (non-small cell lung cancer) cells by means of Sulforhodamine B (SRB) assay. Therein, the dimethyl carbonate extract of WU (WUD) was tested with the most potent anti-proliferative activity against the four cancer cell lines, and its effects on cell viability, cell cycle progression, DNA damage, intracellular reactive oxygen species (ROS), and expression levels of G₀/G₁-related proteins in A549 cells were further examined. First, it was found that WUD inhibited the proliferation of A549 cells in a time- and dose-dependent manner. In addition, WUD induced G₀/G₁ phase arrest and modulated the expression of G₀/G₁ phase-associated proteins Cyclin D1, Cyclin E1, and P27 in A549 cells. Furthermore, WUD increased the protein abundance of P27 by inhibiting FOXO3A/SKP2 axis-mediated protein degradation and also significantly induced the γH2AX expression and intracellular ROS generation of A549 cells. It was also found that the inhibitory effect of WUD on the proliferation and G₀/G₁ cell cycle progression of A549 cells could be attenuated by NAC, a ROS scavenger. On the other hand, phytochemical analysis of WUD with UPLC-QTOF-MS/MS indicated 10 sesquiterpenoid compounds. In conclusion, WUD exhibited remarkable anti-proliferative effects on A549 cells by improving the intracellular ROS level and by subsequently modulating the cell proliferation and G₀/G₁ cell cycle progression of A549 cells. These findings proved the good therapeutic potential of WU for the treatment of NSCLC.

Previous reports have illustrated that the incidence and mortality of cancer are increasing year by year worldwide. In addition, the occurrence, development, recurrence and metastasis of cancer are closely related to inflammation, which is a kind of defensive response of human body to various stimuli. As an important medicinal plant in Africa, Warburgia ugandensis has been reported to have certain anti-inflammatory and anti-proliferative activities, but its specific components and mechanisms of action remain elusive. To tackle this challenge, affinity ultrafiltration with drug targets of interest coupled to high-performance liquid chromatography-mass spectrometry (AUF-HPLC-MS/MS) could be utilized to quickly screen out bioactive constituents as ligands against target enzymes from complex extracts of this plant. AUF-HPLC-MS/MS with four drug targets, i.e., cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), topoisomerase I (Top I) and topoisomerase II (Top II) were used to rapidly screen and characterize the anti-inflammatory and anti-proliferative natural ligands from W. ugandensis, and the resulting potential active compounds as ligands with specific binding affinity to COX-2, 5-LOX, Top I and Top II, were isolated with modern separation and purification techniques and identified with spectroscopic method like NMR, and then their antiinflammatory and anti-proliferative activities were tested to verify the screening results from AUF-HPLC-MS/MS. Compounds 1 and 2, which screened out and identified from W. ugandensis showed remarkable binding affinity to COX-2, 5-LOX, Top I and Top II with AUF-HPLC-MS/MS. In addition, 1 new compound (compound 3), together with 5 known compounds were also isolated and identified from W. ugandensis. The structure of compound 3 was elucidated by extensive 1D, 2D NMR data and UPLC-QTOF-MS/MS. Furthermore, compounds 1 and 2 were further proved to possess both anti-inflammatory and anti-proliferative activities which are in good agreement with the screening results using AUF-HPLC-MS/MS. This work showcased an efficient method for quickly screening out bioactive components with anti-inflammatory and anti-proliferative activity from complex medicinal plant extracts using AUF-HPLC-MS/MS with target enzymes of interest, and also demonstrated that neolignanamides (compounds 1 and 2) from W. ugandensis would be the active components responsible for its anti-inflammatory and anti-proliferative activity with the potential to treat cancer and inflammation.

Warburgia ugandensis, also known as “green heart,” is widely used for the treatment of various diseases as a traditional ethnomedicinal plant in local communities in Africa. In this work, 9 and 12 potential superoxide dismutase (SOD) and xanthine oxidase (XOD) ligands from W. ugandensis were quickly screened out by combining SOD and XOD affinity ultrafiltration with LC-MS, respectively. In this way, four new lignanamides (compounds 11–14) and one new macrocyclic glycoside (compound 5), along with three known compounds (compounds 1, 3, and 7), were isolated and identified firstly in this species. The structures of the new compounds were elucidated by spectroscopic analysis, including NMR and UPLC-QTOF-MS/MS. Among these compounds, compound 14 showed the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azinobis-(3-ethylbenzthiazoline)-6-sulfonic acid (ABTS) radical scavenging activities, and total ferric-reducing antioxidant power (FRAP) with IC₅₀ values of 6.405 ± 0.362 µM, 5.381 ± 0.092 µM, and 17.488 ± 1.625 mmol TE/g, respectively. Moreover, compound 14 displayed the highest inhibitory activity on cyclooxygenase-2 (COX-2) with IC₅₀ value of 0.123 ± 0.004 µM, and the ranking order of other compounds’ IC₅₀ values was 13 > 11 > 7 > 1 > 12. The present study suggested that lignanamides might represent interesting new characteristic functional components of W. ugandensis to exert remarkable antioxidant and anti-inflammatory activities. Moreover, compound 14, a new arylnaphthalene lignanamide, would be a highly potential natural antioxidant and anti-inflammatory agent from W. ugandensis.