Synthesis and Biochemical Evaluation of Baicalein Prodrugs

Son, Sang-Hyun; Kang, Jinhong; Ahn, Myunghwan; Nam, So‐Yeon; Jung, Yong Woo; Lee, Ki Yong; Jeon, Young Ho; Byun, Youngjoo; Lee, Kiho

doi:10.3390/pharmaceutics13091516

Cited by 9 publications

(5 citation statements)

References 17 publications

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“…Based on this investigation, the ability of free radical active molecules to trap and scavenge free radicals was tested by preparing six different free radical active molecules’ electrospinning membranes and using them as in situ trapping membranes for atmospheric ROS radicals, which are capable of trapping atmospheric ROS radicals. The free radical active molecules selected in this paper are flavonoids found in natural plants, respectively chrysin [ 38 , 39 ], baicalein, [ 40 , 41 ], scutellarin, genistein, [ 42 ], quercetin [ 43 , 44 ], and baicalin. All have a wide range of pharmacological effects, have antioxidant, free radical scavenging, anti-inflammatory, and anti-tumor effects, have a specific protective effect on the immune, cardiovascular, digestive, and neurological systems, and also have an excellent scavenging effect on reactive oxygen radicals.…”

Section: Resultsmentioning

confidence: 99%

Preparation of Electrospun Active Molecules Membrane Application to Atmospheric Free Radicals

Yang

Wang

et al. 2022

Membranes

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Atmospheric reactive oxygen species (ROS) play a key role in the process of air pollution and oxidative damage to organisms. The analysis of ROS was carried out by the capture-derivative method. Therefore, it is necessary to prepare an effective molecular membrane to trap and detect ROS. Electrospinning membranes were prepared by combining the electrospinning technique with chrysin, baicalein, scutellarin, genistein, quercetin, and baicalin. By comparing the structures of the membranes before and after the reaction, the fluorescence enhancement characteristics of the reactive molecular membranes and the atmospheric radicals were studied. The ability of the active molecular membranes to trap atmospheric radicals was also studied. It was found that the genistein active molecular membrane had good trapping ability in four environments. The fluorescence enhancement rates in ROS, OH radical and O3 simulated environments were 39.32%, 7.99% and 11.92%, respectively. The fluorescence enhancement rate in atmospheric environment was 16.16%. Indeed, the sites where the atmospheric radicals react with the active molecular membranes are discussed. It is found that it is mainly related to the 5,7 phenolic hydroxyl of ring A, catechol structure and the coexistence structure of 4′ phenolic hydroxyl of ring B and 7 phenolic hydroxyl of ring A. Therefore, the genistein molecular membrane has shown great potential in its trapping ability and it is also environmentally friendly.

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Section: Resultsmentioning

confidence: 99%

Preparation of Electrospun Active Molecules Membrane Application to Atmospheric Free Radicals

Yang

Wang

et al. 2022

Membranes

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“…Several biologics are widely used in clinical practice and are highly effective in patients who do not respond adequately to conventional inhalation therapy or oral steroid maintenance therapy [ 1 , 3 , 13 , 50 ]. However, the efficacy of available biologics depends on type 2 inflammation and, thus, their efficacy in non-type 2 asthma is limited [ 3 , 4 , 5 , 50 , 51 ]. Therefore, detailed treatment strategies for refractory non-type 2 asthma are not yet fully developed.…”

Section: Discussionmentioning

confidence: 99%

Comparative Efficacy and Safety of Tezepelumab and Other Biologics in Patients with Inadequately Controlled Asthma According to Thresholds of Type 2 Inflammatory Biomarkers: A Systematic Review and Network Meta-Analysis

Andō

Fukuda

Tanaka

et al. 2022

Cells

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The anti-thymic stromal lymphopoietin antibody (tezepelumab) has therapeutical potential for inadequately controlled asthma. However, evidence comparing tezepelumab with other biologics is scarce. To address this issue, we performed a network meta-analysis to compare and rank the efficacy of five treatments (tezepelumab, dupilumab, benralizumab, mepolizumab, and placebo) in overall participants and in subgroups stratified by the thresholds of type 2 inflammatory biomarkers, including peripheral blood eosinophil count (PBEC) and fractional exhaled nitric oxide (FeNO). The primary endpoints were annualized exacerbation rate (AER) and any adverse events (AAEs). In the ranking assessment using surface under the cumulative ranking curve (SUCRA) of AER, tezepelumab ranked the highest overall and across subgroups (based on PBEC and FeNO level thresholds). A significant difference was observed between tezepelumab and dupilumab in the patient subgroup with PBEC < 150, and between tezepelumab and benralizumab in overall participants and the patient subgroup with PBEC ≥ 300 and ≥150, respectively. There was no significant difference in the incidence of AAEs in the overall participants between each pair of five treatment arms. These results provide a basis for the development of treatment strategies for asthma and may guide basic, clinical, or translational research.

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“…Furthermore, we also identified and analyzed bioactive compounds in QF, including baicalin, wogonoside, amygdalin, cryptotanshinone, polydatin, emodin, resveratrol, and baicalein, among others, using UHPLC-MS/MS. Previous studies have shown that these compounds have anti-inflammatory ( He et al, 2020 ), anti-oxidation ( Nagappan et al, 2019 ), anti-allergic, spasmolytic, immune response inhibition ( Bui et al, 2017 ; Son et al, 2021 ) and other effects.…”

Section: Discussionmentioning

confidence: 99%

Anti-inflammatory activities of Qingfei oral liquid and its influence on respiratory microbiota in mice with ovalbumin-induced asthma

Zheng

Zhang

et al. 2022

Front. Pharmacol.

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Dysbiosis of respiratory microbiota is closely related to the pathophysiological processes of asthma, including airway inflammation. Previous studies have shown that Qingfei oral liquid (QF) can alleviate airway inflammation and airway hyper-responsiveness in respiratory syncytial virus-infected asthmatic mice, but its effect on the respiratory microbiota is unknown. We therefore aimed to observe the effects of QF on airway inflammation and respiratory microbiota in ovalbumin (OVA)-induced asthmatic mice. We also explored the potential mechanism of QF in reducing airway inflammation by regulating respiratory microbiota. Hematoxylin and eosin as well as periodic acid-Schiff staining were performed to observe the effects of QF on lung pathology in asthmatic mice. Cytokine levels in bronchoalveolar lavage fluid (BALF) specimens were also measured. Changes in respiratory microbiota were analyzed using 16S rRNA gene sequencing, followed by taxonomical analysis. In order to verify the metagenomic function prediction results, the expression of key proteins related to the MAPK and NOD-like receptor signaling pathways in the lung tissues were detected by immunohistochemistry. The current study found that QF had a significant anti-inflammatory effect in the airways of asthmatic mice. This is mainly attributed to a reduction in lung pathology changes and regulating cytokine levels in BALF. Analysis of the respiratory microbiota in asthmatic mice showed that the abundance of Proteobacteria at the phylum level and Pseudomonas at the genus level increased significantly and QF could significantly regulate the dysbiosis of respiratory microbiota in asthmatic mice. Metagenomic functional prediction showed that QF can downregulate the MAPK and Nod-like receptor signaling pathways. Immunohistochemical results showed that QF could downregulate the expression of p-JNK, p-P38, NLRP3, Caspase-1, and IL-1β, which are all key proteins in the signaling pathway of lung tissue. Our study therefore concluded that QF may reduce airway inflammation in asthmatic mice by regulating respiratory microbiota, and to the possibly downregulate MAPK and Nod-like receptor signaling pathways as its underlying mechanism.

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Synthesis and Biochemical Evaluation of Baicalein Prodrugs

Cited by 9 publications

References 17 publications

Preparation of Electrospun Active Molecules Membrane Application to Atmospheric Free Radicals

Preparation of Electrospun Active Molecules Membrane Application to Atmospheric Free Radicals

Comparative Efficacy and Safety of Tezepelumab and Other Biologics in Patients with Inadequately Controlled Asthma According to Thresholds of Type 2 Inflammatory Biomarkers: A Systematic Review and Network Meta-Analysis

Anti-inflammatory activities of Qingfei oral liquid and its influence on respiratory microbiota in mice with ovalbumin-induced asthma

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