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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2022 · IF 3.571

Forced degradation studies of elagolix sodium with the implementation of high resolution LC-UV-PDA-MSn (n = 1,2,3…) and NMR structural elucidation

Xueni Zhong,Qianqian Lv,Qiyun Yong,Wenping Hu,Dan Li,Shuhui Ji,Liuyue Zhan,Wenbin Chen,Min Li,Jinsheng Lin,Cuirong Sun

Elagolix sodium (ELS) is a marketed product using to release moderate to severe endometriosis-associated pain. It contains functional groups such as carboxyl group , secondary amino group , 2,4-dioxo pyrimidinyl and several benzyl or benzyl-like position hydrogen atom that are susceptive to occur stress degradation. Forced degradation studies of ELS reveal different degradation profiles of the drug substance which are conducted under photo, thermal, acidic, neutral, alkaline and hydrogen peroxide oxidative conditions in the direction of the ICH guidances. With structural elucidation of LC-PDA/UV-MS n and NMR, the degradants were identified, and seven new degradants are reported in this study. It is confirmed that most of the degradation behaviors of ELS are related to the carboxyl group and secondary amino group in the 3-carboxyl propylamine side chain. Under the oxidative condition using hydrogen peroxide as the oxidant , the secondary amine was oxidized to form an N -hydrogen amine degradant and two further degradants of amine and carbonyl analogs were generated. Under the alkaline degradation condition, the ELS is proven to be stable and no obvious degradants are produced. On the other hand, under the acidic and neutral degradation condition, the 2,4-dioxo pyrimidinyl core of elagolix sodium is stable but the carboxyl group and secondary amine will occur ring cyclization to form the δ -lactam analogs of elagolix sodium. The plausible mechanisms for the degradation of acidic, thermal, photo-degradative and hydrogen peroxide mediated oxidative of elagolix sodium are proposed. It is worth to note that DP-3–4 are the potential degradants which are only found in the solution degradation and are not the real impurities of elagolix sodium.

CAS / MDL: 631-61-8 70197-13-6
研究领域: 药物化学 · 分析化学 · 药学
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CHEMICAL ENGINEERING JOURNAL · 2025 · IF 13.2

In-situ growth of highly stable CsPbBr3@MSN@PbBr(OH) through water-assisted strategy for high sensitivity immunochromatographic assay

Jie Liu,Tongxu Gu,Rui sun,Jiaojiao Sun,Jian Yin,Pengli Bai,Huancai Yin

Classical gold nanoparticle-based colorimetric immunochromatographic assay (ICA) exhibits moderate performance, limiting their application in trace detection. In this study, perovskite-MSN nanocomposites with high quantum yield (74.7 %), a narrow full width at half maximum (29.5 nm) and excellent water stability were synthesized using in situ crystallization growth and a water-assisted strategy. Carboxyl-modified perovskite-MSN nanocomposites were employed to label anti-gliadin monoclonal antibody (mAb) and construct dual-mode fluorescent ICA (FICA) for determination of gliadin in milk and beef samples. Compared to the traditional AuNP-based colorimetric ICA strips, the CsM-H-based FICA demonstrated improved sensitivity, with a limit of detection (LOD) of 3.62 ng/mL in quantitative analysis. The CsM-H-based FICA strips exhibited average recoveries ranging from 90.2 % to 110.0 %, with coefficients of variation (CVs) between 3.3 % and 7.4 % for milk and beef samples. The ultra-stable perovskite-MSN nanocomposites provided the FICA strip with excellent stability, enabling storage for up to six months at room temperature. This study highlights the advantages of CsM-H-based FICA, including its rapidity, simplicity, and cost-effectiveness, as a promising POCT biosensor.

研究领域: 材料科学 · 分析化学 · 医学诊断
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MICROCHIMICA ACTA · 2020 ·Vol. 187 ·期 11 ·1-13 · IF 6.232

Magnetic hollow bimetallic zinc/cobalt zeolitic imidazolate framework as sorbent for efficiently enriching aflatoxins combined with UHPLC-IT-MSn determination

Wang Zelan,Meng Zhe,Zhao Mengxin,Men Xiuqin,Yang Jinhui,Li Jiguang

A novel magnetic hollow bimetallic zinc/cobalt-based zeolitic imidazolate framework (MHB-Zn/Co-ZIF-8) was prepared via a microwave-assisted chemical etching in methanol. The structure, morphology, and specific surface area were characterized by X-ray diffraction and FTIR spectroscopy, scanning and transmission electron microscopy, and N 2 adsorption. The hollow nanostructures with high internal specific surface area, abundant active sites, and reduced aggregation of nanoparticles endow the hollow zeolitic imidazolate framework (ZIF) nanoparticle with high chemical stability, desirable durability, and excellent adsorption abilities. The MHB-Zn/Co-ZIF-8 nanoparticle was used as an effective sorbent for magnetic solid-phase extraction (MSPE) of trace aflatoxins B 1 , B 2 , G 1 , and G 2 from fruit juice and fruit samples. The main parameters affecting the efficiency of MSPE procedures were investigated and optimized. The results show that, under optimized conditions, enrichment factors ranging from 67- to 355-fold are obtained for the target analytes. The method is linear in the range 1.0 to 100.0 ng mL −1 with correlation coefficients ( R 2 ) from 0.9960 to 0.9992. The limits of detection of four aflatoxins are in the range 0.18 to 1.50 ng mL −1 and the average recoveries range from 75.1 to 102.4%, with relative standard deviations (RSDs) less than 13.6%. This work presents the excellent extraction performance of aflatoxins B 1 , B 2 , G 1 , and G 2 on MHB-Zn/Co-ZIF-8. In addition, the applicability of the MSPE coupling with ultrahigh-performance liquid chromatography-ion trap tandem mass spectrometry (UHPLC-IT-MS n ) for trace analysis in complex matrices is shown. Schematic presentation of magnetic hollow bimetallic zinc/cobalt zeolitic imidazolate framework as sorbent for efficiently enriching aflatoxins B 1 , B 2 , G 1 , and G 2 from fruit juice samples prior to ultrahigh-performance liquid chromatography-ion trap tandem mass spectrometry (UHPLC-IT-MS n ) determination.

研究领域: 分析化学 · 食品安全 · 材料科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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World Journal of Traditional Chinese Medicine · 2018 ·Vol. 4 ·期 1 ·21 · IF 0

An Integrated Study for the Utilization of Anthraquinone Compounds Extract “Heshouwu” In vivo and their Comparative Metabolism in Liver Microsomes Using UPLC-ESI-Q-TOF/MSn

Chen Sha,Ma Hong-Yu,Deng Zhe,Zhang Jun,Cheng Jin-Tang,Chen Chang,Liu An

Objective: Anthraquinone (AQ), a major bioactive component of the traditional Chinese medicine HeShouWu, has widespread applications in industry and medicine. The objective of the current study is to explore the differences in the bioavailability of anthraquinones in vivo and the metabolism in liver microsomes. Materials and Methods: In vivo , we used a reliable UPLC-ESI-QqQ-MS/MS method to measure seven AQ compounds in the jugular vein plasma of rats following oral administration of HeShouWu. Furthermore, in order to quantify the bioavailability of AQs in vivo and to further understand the metabolism of these compounds, we compared the in vitro metabolism of AQ in different species with respect to metabolic profiles, the enzymes involved, and catalytic efficiency using liver microsomes from human (HLM), mouse (MLM), rat (RLM), and beagle dog (DLM). Results: We identified two metabolic pathways, including the hydroxylation and glucuronidation of AQ, in the liver microsomes of humans and other species using UPLC-ESI-Q-TOF. We found that substitutions on the AQ ring were crucial to the activity and regioselectivity of its hydroxylation. In general, hydroxylation activity decreased greatly with β-COOH (rhein) and enhanced dramatically with β-OH (emodin). We also found that glucuronidation of the compound emodin-8-O-β-D-glucoside acts as the main isoform in AQ hydroxylation in HLM and DLM. Total microsomal intrinsic clearance values for AQ were greatest in mouse microsomes, followed by those in dog, human, and rat microsomes. Conclusion: The absorption of different anthrquinone compounds varied based on the compound structure, the metabolism types and products of anthraquinones in liver microsomes were different in different species. These findings provide vital information for a deeper unuunderstanding of the metabolism of AQs.

研究领域: 药物代谢 · 中药药理学 · 分子药理学 · 生物分析化学 · 转化医学
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ANALYTICA CHIMICA ACTA · 2022 · IF 6.911

MSN/NA-doped nanoflower enhancing isothermal fluorescent sensor with a portable PCR tube fluorescence reader for the on-site detection of Vibrio parahaemolyticus

Yuan Su,Xuetong Li,Longjiao Zhu,Huashuo Chu,Yangzi Zhang,Jingjing Tian,Shuxia Lyu,Wentao Xu

To develop an on-site, thermostatic and rapid sensor for the detection of Vibrio parahaemolyticus (V. parahaemolyticus) , A single cross-priming fluorescence (SCPF) sensor was designed using a 3D nano-nucleic acid hybrid material that termed mesoporous silica nanoparticle/nucleic acid-doped nanoflower (MSN/NA-doped nanoflower). In addition, a portable polymerase chain reaction (PCR) tube fluorescence reader was built. Further analysis of the MSN/NA-doped nanoflower morphology and the enhancement mechanism indicated that the MSNs aggregated into larger nanoclusters by adsorbing single cross-priming amplification (sCPA) components, forming MSNs/NAs-doped nanoflowers, and increasing the local concentrations to enhance sCPA efficiency. Cyclic amplification relied mainly on the self-folding hairpin-like structure of the amplified product that continuously formed, opened, re-formed, and opened again. The target DNA was detected with a detection limit of 2.4 copies/μL.

CAS / MDL: 102-71-6
研究领域: 生物技术 · 分子生物学 · 分析化学 · 微生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Materials Chemistry B · 2022 ·Vol. 11 ·期 4 ·826-836 · IF 7.571

A dual aperture (mesoporous and macroporous) system loaded with cell-free fat extract to optimize bone regeneration microenvironment

Enhui Qiu,Yan Gong,Jieran Yao,Jinqing Lai,Zhihua Liu,Da-Peng Yang,Li Shen,Xiangrong Chen

Injured bone regeneration requires a systemically and carefully orchestrated series of events involving inflammation, angiogenesis, and osteogenesis. Thus, we designed a multifunctional cell-supporting and drug-retarding dual-pore system: cell-free fat extract (Ceffe)-mesoporous silica nanoparticle (MSN)@poly(lactic-co-glycolic acid) (PLGA) (Ceffe-MSN@PLGA) to mimic the developmental spatial structure, the microenvironment of bone regeneration and integration during injured bone regeneration. In this system, a macroporous scaffold (pore size 200–250 μm) of PLGA is combined with mesoporous MSN (pore size 2–50 nm), aiming at realizing the slow release of Ceffe. Besides, PLGA and MSN are used to recruit the temporary support of cells that are able to degrade simultaneously with bone regeneration and provide space for bone tissue regeneration. And the Ceffe isolated from fresh human adipose tissue has a therapeutic effect in regulating the important functions of early inflammatory cell transformation, neovascularization and eventual osteogenic differentiation. Our results suggest that the mesoporous and macroporous Ceffe-MSN@PLGA system represents a promising strategy to better fit the regeneration of injured bone tissue.

研究领域: 组织工程 · 生物材料 · 再生医学 · 骨生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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DALTON TRANSACTIONS · 2017 ·Vol. 46 ·期 35 ·11875-11883 · IF 4.029

An enhanced chemotherapeutic effect facilitated by sonication of MSN

Yi Ding,Ziyi Song,Qian Liu,Shaohua Wei,Lin Zhou,Jiahong Zhou,Jian Shen

Sonodynamic therapy (SDT) is a non-invasive therapeutic modality for cancer treatment. Finding new effective sonosensitizers has attracted great attention in the field of SDT. Mesoporous silica nanoparticles (MSN) have been extensively explored as a drug delivery system because of their good biocompatibility and satisfactory drug loading ability. However, there are relatively few studies devoted to using MSN as an efficient sonosensitizer. In this paper, we found that MSN could be used as an efficient sonosensitizer to induce cell apoptosis after ultrasound (US) treatment. To make the full use of MSN and increase its activity for cancer treatment, a chemotherapeutic drug was encapsulated inside MSN to achieve a chemotherapy-SDT synergistic function. Furthermore, photoinitiated polymerization cross-linked methacrylated hyaluronic acid (m-HA) gel was covered on the surface of DOX@MSN to improve its tumour targeting ability. In vitro and in vivo research studies indicated that the degradation of the m-HA shell by hyaluronidase (HAase) that is concentrated in the tumour environment results in the release of DOX@MSN. Importantly, subsequent US treatment could not only trigger SDT of MSN but also promote DOX release from MSN to show chemotherapeutic activity.

CAS / MDL: 9067-32-7 760-93-0
研究领域: 纳米医学 · 肿瘤学 · 药物递送系统 · 治疗方式
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACS Biomaterials Science & Engineering · 2022 · IF 5.395

Hypothermia-Triggered Mesoporous Silica Particles for Controlled Release of Hydrogen Sulfide to Reduce the I/R Injury of the Myocardium

Wenyi Xia,Tao Yan,Lianlei Wen,Shijie Zhu,Wang Yin,Miao Zhu,Meidong Lang,Chunsheng Wang,Changfa Guo

Despite the fact that heart transplantation (HTx) is a relatively mature procedure, heart ischemic and reperfusion (I/R) injury during HTx remains a challenge. Even after a successful operation, the heart will be at risk of primary graft failure and mortality during the first year. In this study, temperature-sensitive polymer poly(N-n-propylacrylamide-co-N-tert-butyl acrylamide) (PNNTBA) was coated on diallyl trisulfide (DATS)-loaded mesoporous silica nanoparticles (DATS-MSN) to synthesize hypothermia-triggered hydrogen sulfide (H2S) releasing particles (HT-MSN). Because the PNNTBA shell dissolves in phosphate-buffered saline at 4 °C, the loaded DATS could continuously release H2S within 6 h when activated by glutathione (GSH). Furthermore, after co-culturing biocompatible HT-MSN with cardiomyocytes, H2S released from HT-MSN at 4 °C was found to protect cardiomyocytes from ischemic and reperfusion (I/R) injury. In detail, the rate of cell apoptosis and lactate dehydrogenase activity was decreased, as manifested by increased BCL-2 expression and decreased BAX expression. More importantly, in an isolated heart preservation experiment, HT-MSN demonstrated potent protection against cardiac I/R injury and reduced expression of inflammatory factors TNF-α and IL-1β. This study provided a new method for the controlled release of H2S by the donor and myocardial protection from I/R injury.

研究领域: 药理学 · 纳米技术 · 心脏病学 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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International Journal of Nanomedicine · 2023 · IF 8

Hybrid Hydrogel Loaded with Chlorhexidine⊂β-CD-MSN Composites as Wound Dressing

Jian Lin,Tianpeng Shi,Yi Wang,Zhiqi He,Zhixiang Mu,Xiaojun Cai,Hui Deng,Jianliang Shen,Fen Liu

Background Much attention has been paid to sustained drug release and anti-infection in wound management. Hydrogels, which are biocompatible materials, are promising tools for controlled drug release and infective protection during wound healing. However, hydrogels also demonstrate limitations in the highly efficient treatment of wounds because of the diffusion rate. In this work, we explored pH-sensitive hydrogels that enable ultra-long-acting drug release and sustained antibacterial properties.Methods We constructed a hybrid gelatin methacrylate (GelMA) system with sustainable antibacterial properties combining hyaluronic acid (HA)-coated mesoporous silica nanoparticles (MSN), which loaded host-guest complexes of chlorhexidine (CHX) with β-cyclodextrins (β-CD) (CHX⊂CD-MSN@HA@GelMA). The release mechanism of CHX was explored using UV-vis spectra after intermittent diffusion of CHX. The hybrid hydrogels were characterized, and the drug content in terms of the release profile, bacterial inhibition, and in vivo experiments were investigated.Results Except for dual protection from both hydrogels, MSN in the HA improved the drug loading efficiency to promote the local drug concentration. It showed that complicated CHX-loaded MSN releases CHX more gradually and over a longer duration than CHX-loaded MSNs. This demonstrated a 12-day CHX release time and antibacterial activity, primarily attributable to the capacity of β-CD to form an inclusion complex with CHX. Meanwhile, in vivo experiments revealed that the hydrogels safely promote skin wound healing and enhance therapeutic efficacy.Conclusion We constructed pH-sensitive CHX⊂CD-MSN@HA@GelMA hydrogels that enable ultra-long-acting drug release and sustained antibacterial properties. The combination of β-CD and MSN would be better suited to release a reduced rate of active molecules over time (slow delivery), making them great candidates for wound dressing anti-infection materials.

CAS / MDL: 55-56-1 78-10-4
研究领域: 生物医学工程 · 材料科学 · 药剂学 · 伤口护理
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ACS Applied Materials & Interfaces · 2021 · IF 9.229

Smart MSN-Drug-Delivery System for Tumor Cell Targeting and Tumor Microenvironment Release

Jin-Hu Dong,Yao Ma,Rong Li,Wen-Tao Zhang,Meng-Qian Zhang,Fan-Ning Meng,Kai Ding,Hai-Tao Jiang,Yong-Kuan Gong

Tumor-targeted delivery and controlled release of antitumor drugs are promising strategies for increasing chemotherapeutic efficacy and reducing adverse effects. Although mesoporous silica nanoparticles (MSNs) have been known as a potential delivery system for doxorubicin (DOX), they have restricted applications due to their uncontrolled leakage and burst release from their large open pores. Herein, we engineered a smart drug-delivery system (smart MSN-drug) based on MSN-drug loading, cell membrane mimetic coating, on-demand pore blocking/opening, and tumor cell targeting strategies. The pore size of DOX-loaded MSNs was narrowed by polydopamine coating, and the pores/channels were blocked with tumor-targeting ligands anchored by tumor environment-rupturable −SS– chains. Furthermore, a cell membrane mimetic surface was constructed to enhance biocompatibility of the smart MSN-drug. Confocal microscopy results demonstrate highly selective uptake (12-fold in comparison with L929 cell) of the smart MSN-drug by HeLa cells and delivery into the HeLa cellular nuclei. Further in vitro IC50 studies showed that the toxicity of the smart MSN-drug to HeLa cells was 4000-fold higher than to the normal fibroblast cells. These exciting results demonstrate the utility of the smart MSN-drug capable of selectively killing tumor cells and saving the normal cells.

CAS / MDL: 25952-53-8 6066-82-6
研究领域: 生物医学工程 · 药剂学 · 肿瘤学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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NANO · 2021 · IF 1.556

Fabrication of a pH-Responsive 5-FU@MSN-SA Nanoplatform for Anti-Tumor Activity

Wenlong Li,Weiwei Zhang,Weihao Jin,Longbao Zhu,Wanzhen Li,Ping Song,Yugui Tao,Fei Ge

Design of high-performance drug delivery system is necessary to improve the anticancer ability of 5-fluorouracil (5-FU). In this work, we developed a pH-responsive 5-FU loaded and sodium alginate (SA) modified mesoporous silica nanoparticles (MSNs) drug delivery system (5-FU@MSN-SA). After 5-FU was loaded into the pores, MSNs were successfully functionalized with amino groups and then capped by sodium alginate. Compared to acidic conditions, the drug release rate in the neutral environment was quite low. Moreover, detailed investigations confirmed that 5-FU@MSN-SA can easily be up-taken by cancer cells and proved the high cytotoxicity to 4T1 cells. The calculated IC 5 0 values for 5-FU and 5-FU@MSN-SA were 34.67 μ g/mL and 54.95 μ g/mL, respectively. These results indicated that 5-FU@MSNs-SA can be a promising nanoplatform in cancer therapy.

研究领域: 药剂学 · 肿瘤学 · 纳米医学
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NEW JOURNAL OF CHEMISTRY · 2025 · IF 2.5

Acid-responsive MSN@RBA enhanced coating wound healing through alerting and releasing repairing agents

Zhiting Yang,Jiahua Tang,Yan Zhang,Xianzhi Hu,Futing Zi,Yue Lin,Jin Wu

Acid mine drainage (AMD) is a persistent and challenging environmental pollution problem. The consequences of AMD include soil pollution, biodiversity loss, and ecosystem collapse. Our study found that rhodamine B acylhydrazone (RBA) exhibits high sensitivity to Fe3+ and can be used as a corrosion inhibitor. This finding led us to hypothesize that the application of RBA is an effective strategy for constructing self-warning and self-healing integrated pH-responsive mercaptopropyl trimethoxysilane (PeopS-SH) coatings. We herein successfully prepared RBA-loaded mesoporous silica nanoparticles (MSN@RBA) designed to exhibit localized, acid-responsive behavior to avoid oxidation site diffusion and enhance wound healing. These MSN@RBA were sensitive to acidic environments, triggering the rapid release of RBA. The experiments showed that MSN@RBA effectively inhibited the oxidation rate of pyrite and enhanced the long-term passivation effect of the coating. Our findings further demonstrated that MSN@RBA reduced the corrosion current density (0.17 μA cm−2), increased the corrosion potential (335 mV), and improved the thickness and density of the coating. The results of release experiments, electrochemical tests and chemical leaching indicate that MSN@RBA releases RBA in acidic environments, and its spironolactam structure opens and forms a complex with Fe3+. The damaged site is fluorescently labeled and repaired. In conclusion, this acid-responsive nanoparticle system presents a new strategy for the treatment of tailings in harsh environments for a long time.

CAS / MDL: 74317-53-6
研究领域: 材料科学 · 环境科学 · 化学工程
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