Frontiers in Pharmacology
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2022
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IF 5.988
Huang Dan,Sun Chaoqun,Chen Min,Bai Shuyou,Zhao Xuanna,Wang Weiming,Geng Kang,Huang Wenbo,Zhao Tingting,Wu Bin,Zhang Guilin,Wu Dong,Xu Youhua
Airway inflammation and remodeling are critical pathological changes in asthma, and macrophage activation plays a vital role in this process. Sirtuin 1 (SIRT1) reduces airway inflammation by affecting macrophages in asthma. This study aimed to investigate the potential benefit and underlying mechanism of the SIRT1 agonist bergenin as a treatment for asthma. We performed in vivo and in vitro experiments by establishing a Sirt1fl/fl-LysMcre mouse asthma model and using the alveolar macrophage-like cell line MH-S, respectively. Our results show that Sirt1fl/fl-LysMcre asthmatic mice exhibited more severe airway inflammation and airway remodeling than wild-type mice. As an activator of SIRT1, bergenin attenuated asthmatic airway pathology and reduced production of interleukins 1β, IL-5, IL-6, and matrix metalloproteinase 9 (MMP-9) in wild-type asthmatic mice. However, the therapeutic effects of bergenin were significantly attenuated in Sirt1fl/fl-LysMcre asthmatic mice or following coadministration with the SIRT1 inhibitor EX-527. Further experiments showed that activation of SIRT1 by bergenin deacetylates nuclear factor κB and hinders its nuclear translocation, thereby affecting IL-1β, IL-5, IL-6, and MMP-9 production by regulating transcriptional activity. Our study suggests that bergenin can improve asthma-induced airway inflammation and remodeling by activating SIRT1 in macrophages.
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PULMONARY PHARMACOLOGY & THERAPEUTICS
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2020
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IF 2.681
Min Chen,Cuifen Chen,Yun Gao,Dongming Li,Dan Huang,Ziyu Chen,Xuanna Zhao,Qiu Huang,Dong Wu,Tianwen Lai,Guomei Su,Bin Wu,Beixian Zhou
Background Bergenin , a type of polyphenol compound, exhibits antiulcerogenic, anti-inflammatory, antitussive , and burn wound-healing properties. However, its therapeutic effect on tumor necrosis factor α (TNF-α)-induced proinflammatory responses in the airway and potential mechanisms of actions are still unclear. This study aimed to investigate the anti-inflammatory effects and mechanism of bergenin in TNF-α-stimulated human bronchial epithelial (16-HBE) cells. Methods Cell Counting Kit-8 was used to evaluate cytotoxicity. Cytokine expression was analyzed by reverse transcription-quantitative PCR (RT-qPCR) and enzyme-linked immunosorbent assay. Immunofluorescence, western blot , and sirtuin-1 (SIRT1) activity assays were employed to investigate potential molecular mechanisms. Results Bergenin obviously decreased both mRNA and protein expression levels of interleukins 6 and 8 (IL-6 and IL-8) in TNF-α-stimulated 16-HBE cells. Bergenin blocked TNF-α-mediated activation of nuclear factor κB (NF-κB) signaling and NF-κB nuclear translocation. Interestingly, RT-qPCR and western blotting results revealed that bergenin did not affect SIRT1 expression, but significantly increased its activity. Bergenin-mediated SIRT1 activation was further confirmed by results indicating decreased acetylation levels of NF-κB-p65 and p53. Moreover, the inhibitory effects of bergenin on mRNA and protein expression levels of IL-6 and IL-8 were reversed by a SIRT1 inhibitor. In addition, combining bergenin and dexamethasone (DEX) yielded additive effects on the reduction of IL-6 and IL-8 expression. Conclusions These findings demonstrate that bergenin could suppress TNF-α-induced proinflammatory responses by augmenting SIRT1 activity to block the NF-κB signaling pathway , which may provide beneficial effects for the treatment of airway inflammation associated with asthma.
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高影响因子
LUMINESCENCE
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2015
·Vol. 30
·期 8
·1269-1273
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IF 1.518
Yinggui Zhu,Lili Zou,Qin Dong,Derong Jiang
Quenching effects of bergenin, based on the electrochemiluminescence (ECL) of the tris(2,2′-bipyridyl)-ruthenium(II) (Ru(bpy) 3 2+ )/tri-n-propylamine (TPrA) system in aqueous solution, is been described. The quenching behavior can be observed with a 100-fold excess of bergenin over Ru(bpy) 3 2+ . In the presence of 0.1 m TPrA, the Stern–Volmer constant ( K SV ) of the ECL quenching is as high as 1.16 × 10 4 M −1 for bergenin. The logarithmic plot of the inhibited ECL versus logarithmic plot of the concentration of bergenin was linear over the range 3.0 × 10 −6 –1.0 × 10 −4 mol/L. The corresponding limit of detection was 6.0 × 10 −7 mol/L for bergenin (S/N = 3). In the mechanism of quenching it is believed that the competition of the active free radicals between Ru(bpy) 3 2+ /TPrA and bergenin was the key factor for the ECL inhibition of the system. Photoluminescence, cyclic voltammetry, coupled with bulk electrolysis, supports the supposition mechanism of the Ru(bpy) 3 2+ /TPrA–bergenin system. Copyright © 2015 John Wiley & Sons, Ltd.
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MICROCHEMICAL JOURNAL
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2024
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IF 4.9
Yu-Zhen Zhang,Yi-Le Li,Zhi Jin,Mao-Fang He,Yi-Mei Tang,Jian Zhang,Bo Zhang
Flemingia philippinensis Merr.et Rolfe ( F. philippinensis ) is an important food ingredient as well as a traditional Chinese medicine with numerous pharmacological actions. Unfortunately, there was no defined method for monitoring the quality of F. philippinensis in the Chinese Pharmacopoeia. In this study, a magnetic covalent organic framework molecularly imprinted polymers (MCOFs-MIPs) was prepared using MCOFs as a support material, genistein (Gen), which was abundant in F. philippinensis , as a template molecule, and acrylamide as a functional monomer. The preparation process of MCOFs-MIPs was optimized and their structures and adsorption characteristics were characterized. In the selectivity test, the imprinting factor of Gen was 1.93, demonstrating that the imprinting effect of MCOFs-MIPs could selectively enrich Gen in complex samples. Following that, a new and effective quality control method (Gen-MCOFs-MIPs-HPLC) was established to determine Gen content in F. philippinensis roots. The method showed good linearity (R 2 = 0.9936) in the range of 0.12–80 µg mL −1 . The recoveries of Gen in F. philippinensis high, medium and low samples were 90.5–91.0 %, 92.1–100.1 and 92.8–100.8, respectively. Stability and reproducibility tests revealed that this method was stable (RSD of 1.20 %) and reproducible (RSD of 0.70 %). Moreover, the calculation showed that the amount of Gen in the F. philippinensis powder was 0.4489 mg g −1 . As a result, the approach was shown to be simple, repeatable, and stable, and it provided a sensitive and reliable method for the extraction and detection of Gen in natural products.
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REPRODUCTIVE TOXICOLOGY
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2024
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IF 3.3
Yanrong Zhu,Lichen Yao,Yilei Guo,Jing Zhang,Yufeng Xia,Zhifeng Wei,Yue Dai
Tripterygium wilfordii (TW) preparations have been utilized in China for treating rheumatoid arthritis and autoimmune diseases. However, their clinical use is limited due to reproductive toxicity, notably premature ovarian failure (POF). Our study aimed to investigate the effect and mechanism of bergenin in attenuating POF induced by triptolide in mice. POF was induced in female ICR mice via oral triptolide administration (50 μg/kg) for 60 days. Mice received bergenin (25, 50, 100 mg/kg, i.g.) or estradiol valerate (EV) (0.1 mg/kg, i.g.) daily, 1 h before triptolide treatment. In vitro , ovarian granulosa cells (OGCs) were exposed to triptolide (100 nM) and bergenin (1, 3, 10 μM). Antioxidant enzyme activity, protein expression, apoptosis rate, and reactive oxygen species (ROS) levels were assessed. The results showed that triptolide-treated mice exhibited evident atrophy, along with an increase in atretic follicles. Bergenin (50, 100 mg/kg) and EV (0.1 mg/kg), orally administered, exerted significant anti-POF effect. Bergenin and EV also decreased apoptosis in mouse ovaries. In vitro , bergenin (1, 3, 10 μM) attenuated triptolide-induced OGCs apoptosis by reducing levels of apoptosis-related proteins. Additionally, bergenin reduced oxidative stress through downregulation of antioxidant enzymes activity and overall ROS levels. Moreover, the combined use with Sh-Nrf2 resulted in a reduced protection of bergenin against triptolide-induced apoptosis of OGCs. Together, bergenin counteracts triptolide-caused POF in mice by inhibiting Nrf2-mediated oxidative stress and preventing OGC apoptosis. Combining bergenin with TW preparations may effectively reduce the risk of POF.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2025
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IF 5.2
Yao Sun,Shihao Cai,Hongting Liu,Conglu Zhao,Xiang Xu,Xiaoting Wang,Jia Zhang,Chaoyue Zheng,Keran Li,Shouchun Peng,Honggang Zhou,Aiguo Xu,Xiaoting Gu,Xiaoyu Ai,Cheng Yang
Idiopathic pulmonary fibrosis (IPF) is characterized by symptoms such as shortness of breath, persistent dry cough, and hypoxemia. The disease can progress rapidly, often leading to respiratory failure. Given its complex and multifactorial nature, pulmonary fibrosis involves multiple pathological progress, such as inflammation, oxidative stress, and fibroblast activation. A single drug cannot effectively address pulmonary fibrosis through multiple mechanisms, but combining drugs maybe create a synergistic effect, target different aspects of the pathological process and improve treatment efficacy. In our previous study, bergenin can improve pulmonary fibrosis. Vitexin is reported to have anti-inflammatory, antioxidant, and anticancer properties, which maybe influence pathways associated with pulmonary fibrosis. Therefore, bergenin and vitexin were chosen for the combined treatment of pulmonary fibrosis. To improve the targeting ability and the affinity of lung fibroblasts, mouse lung fibroblasts-derived exosomes are used as the carriers for drugs. In this study, exosomes loaded with bergenin and vitexin (Exo-Ber + Vit) were successfully prepared using ultracentrifugation and ultrasonication, with an average particle size of approximately 180 nm. Wound-healing assay showed that Exo-Ber + Vit significantly inhibited the excessive proliferation of TGF-β1 induced Mlg and NIH-3 T3 cells compared with bergenin and vitexin alone. Cell uptake experiments showed that exosomes enhanced the uptake of coumarin 6 in Mlg and 3 T3 cells. In vivo studies, compared to bergenin-loaded exosomes, vitexin-loaded exosomes, and the combination of bergenin and vitexin, Exo-Ber + Vit demonstrated superior effects in reducing pulmonary fibrosis area, collagen deposition, and improving lung function. In conclusion, the co-delivery strategy of bergenin and vitexin via Mlg-derived exosomes offers a promising new approach to the treatment of IPF.
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