CHEMICAL ENGINEERING JOURNAL
·
2021
·
IF 13.273
Sihan Li,Yanqi Gan,Syed Jalil Shah,Ruimeng Wang,Wenxue Gong,Rule Wei,Hongbing Ji,Zhongxing Zhao,Zhenxia Zhao
Competitive adsorption of complex nonsteroidal anti-inflammatory drugs (NSAIDs) from wastewater often reduces the adsorption capacity of object pollutants on most porous materials. To address this issue, NSAIDs molecules were proposed for engineering imprinted pores in UiO-66s to boost their adsorption capacity towards diclofenac sodium (DCF) and Cu(II) in a complex solution. Naproxen (NAP) with proper chemical structure was proved to introduce more imprinted pores (at ~19 Å) with enhanced mesoporous volume, abundant unsaturated metal sites, and terminal hydroxyl groups in UiO-66@NAP. These new intriguing properties awarded high adsorption affinity to UiO-66@NAP for DCF and Cu(II), and their adsorption capacities reached up to 385 and 52 mg/g for single DCF and Cu(II) components, respectively. When DCF and Cu(II) simultaneously appeared in an aqueous solution, DCF was proved to preferentially occupy adsorption sites on UiO-66@NAP with higher adsorption kinetics compared to Cu(II). Afterwards, these pre-adsorbed DCF acted as new adsorption sites to bridge more Cu(II) in the solution. Similarly, the adsorbed Cu(II) on UiO-66@NAP had the same reciprocal bridging effect towards DCF, which realized the synergistic adsorption of DCF and Cu(II) over UiO-66@NAP. Notably, DCF was found to greatly boost the synergistic effect of the Cu(II) adsorption. As a result, UiO-66@NAP exhibited 1.5 and 2.6 times higher uptakes for DCF (573 mg/g) and Cu(II) (135 mg/g) in the binary system compared to their single pollutant system, and its equilibrium adsorption capacity was much higher compared to several state-of-the-art adsorbents. The current work set out a new strategy to modify MOFs for enhanced adsorption of complex NSAID contaminants and revealed a deep understanding of the interactions between NSAIDs and heavy metals ions .
研究领域:
环境科学
·
材料科学
·
药物化学
✓ 已验证
产品关联
DOI
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2020
·
IF 10.652
Ying Liang,Lijuan Feng,Xin Liu,Yuxiang Zhao,Qi Chen,Zhuyin Sui,Ning Wang
A suitable porous adsorbent with prominent adsorption performance and better selectivity for the target containments such as non-steroidal anti-inflammatory drugs (NSAIDs) is highly desired in wastewater treatment . Owing to the intrinsic attributes known as predictable structure, tunable pore size, high chemical stability as well as the reliable post-synthetic modification, covalent organic frameworks (COFs) are considered as brilliant adsorbent candidates which have drawn great attentions. Herein, two COFs with different functional groups (COF-NO 2 and COF-NH 2 ) were designed and prepared in order to enhance selective adsorption ability toward the Ketoprofen (KTP) molecule via functional group tuning. For KTP, due to amino group which could interact with not only carboxylic acid but also carbonyl group, COF-NH 2 exhibited twice adsorption capacity as high as other two counterparts Ibuprofen (IBP) and Naproxen (NPX). However, there was no selectivity for those three NSAIDs when COFs containing nitro groups (COF-NO 2 ) were used as adsorbents. We also found that the adsorption process followed the pseudo-second-order kinetic model well, which confirmed the capture of KTP onto COF-NH 2 was dominated by chemical adsorption . The COF-NH 2 will be a particularly promising porous adsorbent to selectively eliminate the KTP from effluents, and COFs with specific binding sites for various pollutants can be acquired via functional group tuning.
研究领域:
环境科学
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
CHEMOSPHERE
·
2017
·
IF 4.208
Liyun Ma,Xiaojing Mao,Xiao Sun,Li Xu
Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most frequently used pharmaceuticals in animals. In the current study, the biotransformation of five NSAIDs by pig liver microsomes (PLMs) was studied. The pseudo-first-order kinetics mode was obtained for the metabolization of the studied NSAIDs by PLMs in vitro . The metabolites were identified by high performance liquid chromatography with a high-resolution LTQ-Orbitrap mass spectrometry. The hydroxylation of benzene was confirmed to be the dominating metabolic pathway. Finally, the toxicity of the metabolites was predicted by the Estimation Programs Interface Suite software based on quantitative structure-activity relationships. Decreased toxicity was expected for the most metabolites of the studied NSAIDs except flurbiprofen, whose main metabolite exhibited slightly more toxicity. The present study provided a preliminary foundation to understand the metabolites of some NSAIDs and their toxicity, which was of great significance in animal food safety.
研究领域:
药理学
·
毒理学
·
动物医学
✓ 已验证
DOI
高影响因子
Letters in Drug Design & Discovery
·
2019
·Vol. 16
·期 12
·1378-1386
·
IF 0.953
Cai Xingchen,Huang Weiwei,Huang Yi,Xia Lihua,Liu Miao,Wang Mengke,Wang Wenchao,Li Qingyong
Background: The single-agent therapy was unable to provide an effective control of the malignant process, a well-established strategy to improve the efficacy of antitumor therapy is the rational design of drug combinations aimed at achieving synergistic effects. Objective: The
objective of this study is generating the new potential anticancer agents with synergistic activity. Owing to the unique mechanism of action of Camptothecin (CPT), it has shown abroad spectrum of anti-cancer activity against human malignancies, and growing evidence revealed that Nonsteroidal
Anti-Inflammatory Drugs (NSAIDs) reduce the risk of different kinds of cancers. So four CPT-NSAIDs conjugates were synthesized and evaluated. Methods: In this study, a series of novel CPT - NSAIDs derivatives were synthesized by esterification. These new compounds were evaluated for in
vitro antitumor activity against tumor cell lines A549, Hela, HepG2, HCT116 by MTT assay. To probe the required stabilities as prodrugs, stability tests were studied in human plasma. To further evaluate the stability of Ketoprofen-CPT in vivo, the female SD rats were used to determine the
pharmacokinetics following a single oral dose. Results: In vitro results showed that Ketoprofen-CPT and Naproxen-CPT conjugates possessed nice efficacy. In a molecular docking model, the two conjugates interacted with Topo I-DNA through hydrogen bonds, - stacking and
so on.In human plasma results showed that the prodrug was converted to ketoprofen and another compound. The female SD rats were used to determine the pharmacokinetics following a single oral dose, the half-life (t1/2) of Ketoprofen-CPT was approximately 12 h which was much longer than that
of CPT. Conclusion: Good activity was noted for some compounds will be helpful for the design of dualaction agents with most promising anti-cancer activity.
研究领域:
肿瘤学
·
药物化学
·
药理学
✓ 已验证
DOI
高影响因子
JOURNAL OF GASTROENTEROLOGY
·
2013
·Vol. 49
·期 3
·388-399
·
IF 3.788
Yuhara Hiroki,Ogawa Masami,Kawaguchi Yoshiaki,Igarashi Muneki,Shimosegawa Tooru,Mine Tetsuya
Post-endoscopic retrograde cholangiopancreatography (ERCP) pancreatitis is the most frequent complication of ERCP. Several meta-analyses have examined the effects of protease inhibitors (gabexate mesilate, ulinastatin, and nafamostat mesilate) and non-steroidal anti-inflammatory drugs (NSAIDs) on post-ERCP pancreatitis, but the results have been confusing. Since the previous meta-analysis, several new studies have been published on this topic. To provide an updated quantitative assessment of the effectiveness of protease inhibitors and NSAIDs in preventing post-ERCP pancreatitis, we conducted a meta-analysis of randomized trials for patients at risk of post-ERCP pancreatitis. Twenty-six articles were included in this meta-analysis. Nafamostat mesilate (summary RR = 0.41; 95 %CI 0.28–0.59; n = 4 studies) and NSAIDs (summary RR = 0.58; 95 %CI = 0.44–0.76; n = 7 studies) were associated with decreased risk of post-ERCP pancreatitis in the high-quality studies. However, gabexate mesilate (summary RR = 0.64; 95 %CI = 0.36–1.13; n = 6 studies) and ulinastatin (summary RR = 0.65; 95 %CI = 0.33–1.30; n = 2 studies) were not associated with decreased risk of post-ERCP pancreatitis in the high-quality studies. This is the first meta-analysis to compare the effects of three protease inhibitors. Solid evidence supports the use of nafamostat mesilate and NSAIDs for preventing post-ERCP pancreatitis.
研究领域:
消化病学
·
介入内镜学
·
胰腺疾病
·
临床药理学
·
循证医学
·
围手术期管理
✓ 已验证
DOI
高影响因子
CRYSTAL GROWTH & DESIGN
·
2026
·
IF 3.6
Zhiling Chen,Yue Feng,Can Wang,Xiaomin Han,Yangyang Song,Xingyu Yao,Guisen Zhang,Rongbin Wei,Tao Zhuang
Ribociclib (RBC), an antitumor drug, is categorized as a BCS Class IV drug with low solubility and permeability. Despite achieving clinically relevant bioavailability in its marketed malate salt form, the limited aqueous solubility of RBC still poses significant challenges for formulation development. In this work, three novel RBC salts with nonsteroidal anti-inflammatory drugs (diclofenac, DIC; ibuprofen, IBU; loxoprofen, LOX) were successfully synthesized and comprehensively characterized. Among them, compared with pure RBC, the multicomponent RBC-LOX salt showed 2.97-fold higher solubility and 1.90-fold faster dissolution rate in pH 7.4 buffer, and 1.73-fold stronger in vitro cytotoxicity against MDA-MB-231 breast cancer cells. Moreover, in vivo pharmacokinetic evaluations revealed that the RBC-LOX salt significantly improved the oral bioavailability of RBC (1.49-fold), demonstrating enhanced bioavailability. Overall, these findings highlight the potential of RBC-NSAID salts as a strategy to enhance the solubility, anticancer activity, and bioavailability of ribociclib, offering a promising approach for optimizing its therapeutic efficacy.
✓ 已验证
DOI
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2026
·
IF 5.2
Ben Xu,Yue Wu,Xiao-Min Han,Zi-Yuan Liu,Yang-Yang Song,Ji-Yang Zhang,Tao Zhuang,Gui-Sen Zhang
Chronic pain affects more than 30% of people worldwide and represents a highly prevalent clinical problem. However, current analgesics are often limited by inadequate efficacy, serious adverse effects, and the need for frequent administration. Therefore, developing novel long-acting analgesics is crucial for the effective treatment of chronic pain. In this study, we synthesized four new co-prodrugs of non-steroidal anti-inflammatory drugs (NSAIDs) with the endogenous lipid palmitoylethanolamide (PEA), which were further prepared as nanocrystal (NC) formulations to achieve long-acting and enhanced antinociceptive effects. The chemical structures of co-prodrugs NSAIDs-PEA were characterized through HR-MS, and NMR spectroscopy. In mouse liver microsomal stability assays, these co-prodrugs were metabolized into two individual drugs. The NCs of co-prodrugs NSAIDs-PEA were prepared using the wet milling method and tween 80 as the only excipient. All prepared NCs were spherical and had a size between 100 and 200 nm, polydispersity index (PDI) ≤ 0.3 and Zeta potential values from −20 to −30 mV. In a rat model of chronic pain elicited by complete Freund's adjuvant (CFA), intramuscular administration of naproxen-palmitoylethanolamide (NAP-PEA) NCs produced a rapid onset of analgesia and sustained pain relief lasting up to 72 h. Moreover, NAP-PEA NCs had good biocompatibility and induced only a minor local inflammatory reaction, which gradually returned to normal within 5 days. These results indicated that NAP-PEA NCs provided a promising strategy for chronic pain treatment.
✓ 已验证
DOI
高影响因子
CHEMOSPHERE
·
2021
·
IF 7.086
Jingna Yan,Wenting Lin,Zhihan Gao,Yuan Ren
The mass load of pharmaceuticals in the municipal wastewater based on wastewater-based epidemiology (WBE) is a good indication of population consumption in the catchment. After successful application of illicit drugs’ estimation, this method holds the potential to measure the geographical and temporal consumption of prescription medicines. In this study, we investigated the occurrence of four non-steroidal anti-inflammatory drugs (NSAIDs), acetaminophen (ACM), diclofenac (DCF), ibuprofen (IBU) and naproxen (NPX), in two wastewater treatment plants in Guangzhou City, China and compared the spatial and temporal consumption variation of them. Over a period of 28 days’ sampling, the detection frequency of ACM, DCF, IBU, and NPX in the influent of two wastewater treatment plants (WWTPs) in Guangzhou City were 91%, 66%, 100%, and 95%, and their concentrations were up to 128, 131, 372, and 324 ng/L, respectively. No significant inter-catchment difference was observed regarding the per capita mass load in the two WWTPs investigated. A literature review which covered 160 WWTPs in 18 countries was conducted to compare the population normalized mass load of four commonly used NSAIDs. ACM had the highest population normalized mass loads (29–17,430 mg/d/1000 inhabitants) and DCF had the lowest population normalized mass load (6.5–628 mg/d/1000 inhabitants) in the catchments located in 18 countries. The mass loads of selected NSAIDs in China were lower than those in European and North American. ACM and IBU consumptions were at least 2 times higher in winter than that in summer, in contrast, DCF and NPX consumptions had no significant seasonal variation.
研究领域:
环境科学
·
公共卫生
·
药物分析
✓ 已验证
产品关联
DOI
PubMed
高影响因子
LANGMUIR
·
2026
·
IF 4.4
Yunyun Li,Xiaohui Zeng,Ge Wang,Dingyi Zhang
The widespread misuse of nonsteroidal anti-inflammatory drugs (NSAIDs) has become a growing concern due to their severe threats to aquatic ecosystems and human health. Current adsorption technologies face limitations including low capacity, poor efficiency for trace-level contaminants, and unclear removal mechanisms. These limitations stem from poorly optimized pore architectures and surface chemistries in existing materials, necessitating the development of multifunctional adsorbents with tailored active sites. Herein, a series of MnO2/UiO-66-x composites were rationally designed via a solvothermal approach and comprehensively characterized using powder X-ray diffraction (PXRD), Fourier transform infrared (FTIR) spectroscopy, N2 physisorption, scanning electron microscopy (SEM), and zeta potential analysis. Systematic optimization demonstrated that MnO2/UiO-66-1 (5 mg) achieved exceptional adsorption capacity (qmax = 659.49 mg·g–1) for diclofenac sodium (DCF, 20 mg·L–1, 30 mL), with >90% removal within 10 min (k2 = 0.0081 g·mg–1·min–1). Mechanistic studies revealed that this performance was attributed to hierarchical porosity (micro-/mesopores), which enables size-selective uptake, synergistic binding, and pH-dependent electrostatic enhancement. Structure–activity relationships indicated that NSAIDs adsorption efficiency (naproxen ≈ ibuprofen ≈ ketoprofen > indomethacin > paracetamol) was governed by molecular structure, size, and pKa values. Thermodynamic and kinetic studies confirmed a spontaneous (ΔG0 < 0), endothermic (ΔH0 > 0), and entropy-driven (ΔS0 > 0) process dominated by chemisorption through synergistic interactions (including coordination bonding, hydrogen bonding, Lewis acid–base effects, electrostatic attraction, and π–π stacking). This study establishes a new paradigm for metal–organic-framework-based adsorbent design through precise control of metal–organic interfaces and defect engineering. With 87% capacity retention after 5 regeneration cycles, MnO2/UiO-66-x shows strong potential for practical water remediation applications.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
·
2026
·
IF 5.6
Yangyang Song,Jie Song,Shuxian Liu,Jiyang Zhang,Ziyuan Liu,Haoyun Chen,Shiwen Wang,Tao Zhuang,Guisen Zhang
Depression and anxiety disorders are highly comorbid, yet their complex pathogenesis often limits the efficacy of monotherapy. Growing evidence implicates neuroinflammation in their pathogenesis. Co-drugs that linked two active molecules into a single compound and released the drugs after administration, which offering improved efficacy and tolerability than individual drug mixtures or monotherapy. In this work, five new co-drugs ODV-NSAIDs were synthesized from O -desmethylvenlafaxine (ODV) with non-steroidal anti-inflammatory drugs (NSAIDs) to achieve synergistic antidepression and anxiolytic effects. In vitro stability studies exhibited that these co-drugs can be metabolized into two single drugs within 60 min in simulated intestinal fluid. In both acute and chronic LPS-induced models, co-drug ODV-NAP significantly ameliorated depressive-like behaviors, evidenced by increased sucrose preference, reduced immobility in the tail suspension test (TST) and forced swim test (FST), and enhanced locomotion in the open field test (OFT). Furthermore, ODV-NAP decreased brain levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) and malondialdehyde (MDA), while elevating serotonin (5-HT), norepinephrine (NE), and superoxide dismutase (SOD) activity. Nissl staining confirmed ODV-NAP significantly attenuated hippocampal neuronal damage. Moreover, western blotting revealed ODV-NAP inhibited the TLR4/NF-κB signaling pathway and upregulated BDNF and p-TrkB protein expression. ODV-NAP also inhibited LPS-induced p65 nuclear translocation in BV-2 microglia in vitro , and caused no toxicity in histology. Thus, co-drug ODV-NAP represented a promising novel candidate for treating depression and anxiety.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2022
·
IF 6.819
Wenhao Xu,Jinli Yang,Xiangyang Gu,Wenjing Su,Faxiang Pu,Zhangfu Xie,Kongliang Jin,Weike Su,Lichan Mao
Ibuprofen (IBU) was a widely used NSAID (a type of nonsteroidal anti-inflammatory drug) worldwide, and many drug deliveries had been reported to enhance bioavailability. However, higher bioavailability would increase the danger of renal injury caused by oxidative stress. This study prepared IBU-Polygonatum sibiricum polysaccharide (IBU-PSP) drug delivery system via mechanochemical method. Due to drug delivery and renal protection effect of Polygonatum sibiricum polysaccharide (PSP), the solubility of IBU-PSP was increased 8.22 times, and the bioavailability was increased 2.52 times compared with IBU, carrageenin-induced rat paw edema test also increased. Meanwhile, short-term and long-term renal injuries induced by IBU were notable decreases. In conclusion, IBU-PSP was a multifunctional drug delivery system with superior anti-inflammatory and renal protection effects. It will benefit from developing high-efficiency NADIs preparations with safer clinical applications while providing an efficient and energy-saving technology for polysaccharide drug delivery.
研究领域:
药理学
·
药物递送
·
药物化学
·
肾病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ANALYTICAL AND BIOANALYTICAL CHEMISTRY
·
2026
·
IF 4.1
Xiao Le,Zheng Yuanyuan,Jiang Xingyi,Wang Manyi,Luo Yanbo,Pang Yongqiang,Wang Hongjuan,Chen Di
This study presents a liquid-filled stick microextraction method with a built-in acidifier (LFSME-BA) that enables ready-to-use, pH-adjustment-free extraction of non-steroidal anti-inflammatory drugs (NSAIDs) from complex herbal matrices. Similar to an alcohol swab, the device contains an H 3 PO 4 -saturated hydrophobic deep eutectic solvent (DES) loaded inside a hollow plastic stick and a polypropylene fabric tip. Upon use, the acidified DES is released and absorbed by the fabric tip. When immersed in the sample solution, H 3 PO 4 gradually diffuses outward and, in the aqueous model solution used in this study, reduces the sample pH to approximately 1.97. This in situ acidification converts the NSAIDs from their ionized forms to their neutral molecular species, markedly increasing hydrophobicity, thereby facilitating their diffusion into the DES phase. Following desorption with 0.4 mL acetonitrile and LC–UV analysis, the LFSME-BA method provided excellent linearity ( R 2 ≥ 0.994, 20–2000 ng/mL), low detection limits (3.04–5.80 ng/mL), and satisfactory accuracy (93.7–102.5%) and precision (RSD ≤ 8.3%). Application to herbal oral liquids and granules yielded relative recoveries of 85.1%–108.8%, further confirming the method’s reliability. This ready-to-use, disposable platform combines extraction and pH self-regulation in one step, offering a simple and efficient approach for screening adulterated pharmaceuticals in herbal products. Graphical
The alternative text for this image may have been generated using AI.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）