Pharmaceutics
·
2026
·Vol. 18
·期 1
·102
·
IF 5.5
Yujing Huangfu,Wei Chen,Dandan Guo,Peiyao Wang,Aifang Li,Yi Yang,Shuxuan Li,Qianfang Wang,Baiyan Wang,Shuying Feng
Background: As a widely used chemotherapeutic agent, cisplatin frequently induces acute kidney injury (AKI), which severely compromises patient survival and limits its clinical use. While the natural flavonoid diosmetin (Dio) shows promise in mitigating cisplatin-induced nephrotoxicity, its clinical translation is challenged by poor solubility, low bioavailability, and incompletely elucidated mechanisms. This study aimed to overcome these limitations by developing a novel drug delivery system using the microalgae Dunaliella salina ( D. salina , Ds ) to load Dio ( Ds -Dio), thereby enhancing its efficacy and exploring its therapeutic potential. Methods: We first characterized the physicochemical properties of Ds and Dio, and then Ds -Dio complex was synthesized via co-incubation. Its nephroprotective efficacy and safety were systematically evaluated in a cisplatin-induced mouse AKI model by assessing renal function (serum creatinine, blood urea nitrogen), injury biomarkers, histopathology, body weight, and organ index. The underlying mechanism was predicted by network pharmacology and subsequently validated experimentally. Results: The novel Ds -Dio delivery system has been successfully established. In the AKI model, Ds -Dio significantly improved renal function and exhibited a superior protective effect over Dio alone; this benefit is attributed to the enhanced bioavailability provided by Ds carrier. In addition, Ds -Dio also demonstrated safety performance, with no evidence of toxicity to major organs. Network pharmacology analysis predicted the involvement of PI3K/AKT pathway, which was experimentally verified. Specifically, we confirmed that Ds -Dio alleviates AKI by modulating the PI3K/AKT pathway, resulting in concurrent suppression of NF-κB-mediated inflammation and activation of NRF2-dependent antioxidant responses. Conclusions: This study successfully developed a microalgae-based drug delivery system, Ds -Dio, which significantly enhances the nephroprotective efficacy of Dio against cisplatin-induced AKI. The nephroprotective mechanism is associated with modulation of the PI3K/AKT pathway, resulting in the simultaneous attenuation of oxidative stress and inflammation.
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高影响因子
SEPARATION AND PURIFICATION TECHNOLOGY
·
2026
·
IF 9.1
Dong Fu,Linhui Xing,Xin Sui,Yang Xie,Guoxian Hu,Chengzhi Zhao,Yanhong Guo
Novel selective magnetic molecularly imprinted covalent organic framework polymers (MMCIPs) for the selective recognition and enrichment of diosmetin were fabricated via the Schiff base reaction of amino-functionalized magnetic nanoparticles (Fe 3 O 4 -NH 2 ), diamine with different stereostructures, and triformylphloroglucinol (TFP). Various analytical techniques were utilized to systematically characterize the MMCIPs. A notable discrepancy was observed between the practical adsorption performance of MMCIPs and the functional monomer screened by computational simulation. Detailed optimization of preparation parameters was performed. The types and recognition sites of intermolecular forces, adsorption mechanism, and adsorption performances of MMCIPs were comprehensively investigated through computational simulation and various adsorption tests. The optimized MMCIPs possessed a large specific surface area (132.3 m 2 /g), satisfactory magnetic responsiveness (28.4 emu/g), and excellent recyclability over seven cycles of adsorption-desorption. Moreover, synergistic intermolecular interactions endowed the MMCIPs with outstanding adsorption performance for diosmetin (69.9 μg/mg) and specific recognition capability (imprinting factor (IF) up to 2.16). Leveraging these advantages, MMCIPs successfully enabled the selective enrichment, rapid magnetic separation, and efficient purification of diosmetin from lemon peel extract. This work offers a new fabrication strategy for the imprinted polymers with high adsorption capacity and excellent specific recognition capability
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JOURNAL OF ETHNOPHARMACOLOGY
·
2024
·
IF 4.8
Yun-Lu Xu,Xue-Jian Li,Wei Cai,Wen-Ying Yu,Jing Chen,Qin Lee,Yong-Jun Choi,Fang Wu,Ying-Jun Lou,Hua-Zhong Ying,Chen-Huan Yu,Qiao-Feng Wu
Ethnopharmacological relevance Viral pneumonia is the leading cause of death after SARS-CoV-2 infection. Despite effective at early stage, long-term treatment with glucocorticoids can lead to a variety of adverse effects and limited benefits. The Chinese traditional herb Pogostemonis Herba is the aerial part of Pogostemon Cablin (Blanco) Benth., which has potent antiviral, antibacterial, anti-inflammatory, and anticancer effects. It was used widely for treating various throat and respiratory diseases, including COVID-19, viral infection, cough, allergic asthma, acute lung injury and lung cancer. Aim of the study To investigate the antiviral and anti-inflammatory effects of chemical compounds from Pogostemonis Herba in SARS-CoV-2-infected hACE2-overexpressing mouse macrophage RAW264.7 cells and hACE2 transgenic mice. Materials and methods The hACE2-overexpressing RAW264.7 cells were exposed with SARS-CoV-2. The cell viability was detected by CCK8 assay and cell apoptotic rate was by flow cytometric assay. The expressions of macrophage M1 phenotype markers (TNF-α and IL-6) and M2 markers (IL-10 and Arg-1) as well as the viral loads were detected by qPCR. The mice were inoculated intranasally with SARS-CoV-2 omicron variant to induce viral pneumonia. The levels of macrophages, neutrophils, and T cells in the lung tissues of infected mice were analyzed by full spectrum flow cytometry. The expressions of key proteins were detected by western blot assay. Results Diosmetin-7-O-β-D-glucopyranoside (DG) presented the strongest anti-SARS-CoV-2 activity. Intervention with DG at the concentrations of 1.25-50 μM not only reduced the viral replication, cell apoptosis, and the productions of inflammatory cytokines (IL-6 and TNF-α) in SARS-CoV-2-infected RAW264.7 cells, but also reversed macrophage polarity from M1 to M2 phenotype. Furthermore, treatment with DG (25-100 mg/kg) alleviated acute lung injury, and reduced macrophage infiltration in SARS-COV-2-infected mice. Mechanistically, DG inhibited SARS-COV-2 gene expression and HK3 translation via targeting YTHDF1, resulting in the inactivation of glycolysis-mediated NF-κB pathway. Conclusions DG exerted the potent antiviral and anti-inflammatory activities. It reduced pneumonia in SARS-COV-2-infected mice via inhibiting the viral replication and accelerating M2 macrophage polarization via targeting YTHDF1, indicating its potential for COVID-19 treatment.
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PubMed
高影响因子
Chemical Biology & Drug Design
·
2024
·Vol. 104
·期 4
·e70003
·
IF 3.2
Xiang Yu,Di Zhang,Chengming Hu,Zejun Yu,Yang Li,Cheng Fang,Yinsheng Qiu,Zhinan Mei,Lingyun Xu
Hepatocellular carcinoma (HCC) is the sixth most prevalent malignant tumor. Hepatocellular carcinogenesis is closely linked to apoptosis, autophagy, and inflammation. Diosmetin and chrysin, are two flavonoid compounds, exhibit anti-inflammatory and anticancer properties. In this study, the TCGA database was utilized to identify differentially expressed genes between normal subjects and HCC patients. Molecular docking and molecular dynamics analyses were employed to assess the binding affinity of chrysin and diosmetin to key proteins in the PI3K/AKT/mTOR/NF-κB signaling pathway. Western blotting and RT-qPCR were used to measure the protein and gene expression within this pathway. The results indicated that HCC patients had elevated levels of PI3K, AKT, mTOR, and P65 proteins compared to normal subjects, which adversely affected patient survival. Molecular docking and dynamics studies demonstrated that diosmetin and chrysin are effectively bound to these four proteins. In vitro experiments revealed that the combination of diosmetin and chrysin could induce apoptosis, enhance autophagy, reduce inflammatory mediator production, and improve the tumor cell microenvironment by inhibiting the PI3K/AKT/mTOR/NF-κB signaling pathway. Notably, the synergy score for the combination of diosmetin (25 μM) and chrysin (10 μM) was 16. Thus, the diosmetin–chrysin combination shows promise as an effective therapeutic approach for hepatocellular carcinoma due to its strong synergistic effect.
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高影响因子
INSTRUMENTATION SCIENCE & TECHNOLOGY
·
2022
·
IF 1.509
Shan Wang,Yamei Han,Jiangwei Chen,Ligai Bai,Hongyuan Yan,Haiyan Liu
A metal organic framework (MOF)-based monolithic column was prepared by in situ polymerization using modified MIL-101-NH2 and glycidyl methacrylate (GMA) as monomers. The monolithic column was used as a solid phase extraction (SPE) adsorbent for on-line enrichment and preliminary purification of diosmetin in traditional Chinese medicine. After being characterized by scanning electron microscopy (SEM) and nitrogen adsorption-desorption, the advantages of the monolithic column with MIL-101-NH2 added were reflected in the pore structure and specific surface area. The monolithic column for SPE had a linear relationship from 0.13 µg/mL to 5.0 × 102 µg/mL. The limit of detection (LOD) and the limit of quantification (LOQ) were 0.04 µg/mL and 0.13 µg/mL, respectively. The recovery was from 96% to 104%, and the intra-day and inter-day relative standard deviations (RSDs) were below 1.1%. This method was suitable for the determination of diosmetin in complex samples.
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高影响因子
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