INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2020
·
IF 4.845
Longbing Ling,Muhammad Ismail,Zhihao Shang,Yihui Hu,Benhong Li
Irinotecan (Ir) is a potent antitumor chemotherapeutics in clinic and used for the treatment of a various cancers, but the degree of its application is critically limited by toxic side-effects and marked heterogeneities. Nano-formulation of prodrugs, based on “all-in-one” carrier-free self-assemblies offers an effective approach to alter pharmacokinetics and safety profiles of cytotoxic agents. In this study, a novel vitamin E succinate-based formulation of Ir (VES-Ir) combined with nanoscaled characteristics and synergistic combination was constructed through esterification. The conjugation makes amphiphilic VES-Ir prodrug self-assemble into nanoparticles with a fine diameter (VES-Ir NPs, 75.4 nm) of spherical morphology. Furthermore, VES-Ir NPs with a 1:1 drug-to-drug ratio was demonstrated to possess respectable physiological stability within 72 h test, while can react to pH/esterase-sensitive drug release in lysosomes internalized into tumor cells, potentially highlighting their alleviating side effects. Compared with single and mixture drugs administration, the nanoformulated VES-Ir NPs codelivered both VES and Ir with different anticancer mechanisms to induce the highest suppress proliferation of MCF-7 (IC 50 0.18 μM) and A549 (IC 50 0.29 μM) cells in a synergistic way (CI < 1). More importantly, the formulating nanoparticulate Ir is to significantly enhance its bioavailability in vivo with long retention time in bloodstream and thereby, resulting the superior tumor inhibitory rate (TIR) of 85.2% versus controls. This simple nanoformulation of Ir drug deprived from VES conjugation, together with self-delivery and synergistic property, may provide an effective strategy for multiple chemotherapeutics delivery to treat cancers or other diseases.
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Analytical Methods
·
2019
·Vol. 12
·期 2
·193-199
·
IF 2.378
Yan-Jun Huang,Qi-Xin Deng,Hong-Qiao Lan,Zheng-Zhong Fang,Hui Chen,Yan Lin,Han-Chun Xu,Tony D. James,Wei Xie
Nicotine exists in e-liquids primarily as the monoprotonated form and free-base form, the former is absorbed by the smoker relatively slowly and the latter is considered the bioavailable form of nicotine. Nowadays e-liquid manufacturers tend to increase nicotine in smoke aerosols, up to a content comparable to conventional cigarettes. Organic acids are added to suppress nicotine in free-base from, because the quick absorption of free-base nicotine (FBN) by the upper respiratory tract produces more bitterness and harshness to smokers. Although several methods have been developed to access FBN in conventional cigarettes or electronic cigarettes, spectrometric methods have rarely been reported. A water-solubility indicator Alizarin Red S (ARS) was introduced for the measurement of free-base nicotine. Since ARS exhibits lower acidity than organic acids, it does not compete for the tertiary amine with organic acids, but can only interact with FBN. The ARS turns from pale yellow to pink once it has been deprotonated by nicotine, and the binding constant between ARS and nicotine was determined to be 1.08 × 106 M−1. A linear calibration curve A = 0.0056c + 0.3309 with r2 = 0.9984 as a function of FBN was constructed, and applied for the evaluation of FBN in prepared e-liquid samples, with RMSE 1.12 mg g−1 for the 20 mg g−1 liquids, and 1.37 mg g−1 for the 50 mg g−1 liquids. The evaluation of FBN in commercial e-liquids agreed well with published e-liquid values. It is believed that the convenient method herein developed will be useful for manufacturers to balance the strength and harshness levels of nicotine in e-liquids.
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THERMOCHIMICA ACTA
·
2023
·
IF 3.5
Ningrui Zhao,Jumei Xu,Zuoxiang Zeng,Weilan Xue
The density of (E)-isobutyl cinnamate at 297.95–535.20 K was measured using a capillary pycnometer and linearly related to temperature. The vapor pressure of (E)-isobutyl cinnamate at 420.15–570.05 K was measured by the ebulliometric method, and correlated by Antoine equation with an average relative deviation of 1.11 %. The vaporization enthalpy Δ vap H (T b ) of (E)-isobutyl cinnamate at normal boiling point was obtained based on the Clausius-Clapeyron equation. The standard vaporization enthalpy Δ vap H (298.15 K) was calculated to be 73.67±0.5 kJ·mol −1 by Othmer's method and verified by the Corresponding State Group Contribution (CSGC) method. The heat capacities at saturation vapor pressure ( C SL ) of (E)-isobutyl cinnamate were measured at 298.15–533.15 K by an automatic calorimeter and correlated by a quadratic polynomial.
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JOURNAL OF THE AMERICAN CERAMIC SOCIETY
·
2023
·Vol. 107
·期 2
·956-967
·
IF 3.9
Sai-Dong Xue,Yu-Jing Yang,De-Long Zhang
Growth of Er 3+ -doped 100-nm thick LiNbO 3 (LN) films on Z-cut LiTaO 3 (LT) single-crystal by e -beam evaporation and in-situ anneal at 600–800°C was studied. Crystalline phase, crystallographic orientation, Er 3+ spectroscopic properties, constituent element valence states, defects, Er 3+ concentration and stoichiometry of the films were characterized. The results show that the films are in LN single-crystal state and orient along with c crystallographic axis. Constituent elements Li, O and Er are present in their respective single valence states Li + , O 2− , Er 3+ , while the Nb is in two valence states Nb 5+ and Nb 4+ . The films have Li 2 O-contents around congruent point. Antisite(Nb Li 4+ ) is the major defect. Its concentration decreases, while Li 2 O-content, crystallinity degree, and fluorescence intensity increase with increased growth temperature. The presence of Er 3+ in the grown films is in the form of LN crystalline phase. Its concentration is considerably lower than that in initial target material because of lower e -beam evaporation efficiency of heavy Er 3+ .
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International Journal of Nanomedicine
·
2016
·
IF 4.32
Yuling Liu,Yingqi Xu,Minghui Wu,Lijiao Fan,Chengwei He,Jian-Bo Wan,Peng Li,Meiwan Chen,Hui Li
Mitoxantrone (MIT) is a chemotherapeutic agent with promising anticancer efficacy. In this study, Pluronic F68-vitamine E succinate (F68-VES) amphiphilic polymer micelles were developed for delivering MIT and enhancing its anticancer activity. MIT-loaded F68–VES (F68–VES/MIT) micelles were prepared via the solvent evaporation method with self-assembly under aqueous conditions. F68–VES/MIT micelles were found to be of optimal particle size with the narrow size distribution. Transmission electron microscopy images of F68–VES/MIT micelles showed homogeneous spherical shapes and smooth surfaces. F68–VES micelles had a low critical micelle concentration value of 3.311 mg/L, as well as high encapsulation efficiency and drug loading. Moreover, F68–VES/MIT micelles were stable in the presence of fetal bovine serum for 24 hours and maintained sustained drug release in vitro. Remarkably, the half maximal inhibitory concentration (IC50) value of F68–VES/MIT micelles was lower than that of free MIT in both MDA-MB-231 and MCF-7 cells (two human breast cancer cell lines). In addition, compared with free MIT, there was an increased trend of apoptosis and cellular uptake of F68–VES/MIT micelles in MDA-MB-231 cells. Taken together, these results indicated that F68–VES polymer micelles were able to effectively deliver MIT and largely improve its potency in cancer therapy.
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DALTON TRANSACTIONS
·
2023
·Vol. 52
·期 42
·15484-15488
·
IF 4
Xiangyu Zhang,Yunlei Chen,Yongfang Sun,Fei Wang,Xiao-Dong Wen,Tian-Nan Ye
Wide application of novel materials often requires low-cost preparation methods. In this study, we present a simplified and facile preparation method for the [Ca24Al28O64]4+(e−)4 electride material (C12A7:e−). Successful preparation of the C12A7:e− electride was confirmed by XRD patterns and magnetic behavior analysis. The concentration of electrons in the prepared C12A7:e− powder was calculated to be approximately 2.23 × 1021 cm−3, as evaluated by iodometry and TPD. DFT calculations provided insight into the unique electronic structure of C12A7:e−. Additionally, the substitution of the Ca reductant with CaH2 led to a reduction in the solid-state reaction temperature from 1100 to 950 °C, which can be attributed to thermodynamic effects such as a reduction in ΔG°.
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Nanomedicine-Nanotechnology Biology and Medicine
·
2023
·
IF 5.4
Chunjing Guo,Min Cao,Ningning Diao,Wenxin Wang,Hongxu Geng,Yanguo Su,Tianying Sun,Xinyue Lu,Ming Kong,Daquan Chen
Diabetic nephropathy (DN) is an important complication of diabetes and is the main cause of end-stage renal disease. The pathogenesis of DN is complex, including glucose and lipid metabolism disorder , inflammation, and so on. Novel hybrid micelles loaded Puerarin (Pue) based on Angelica sinensis polysaccharides (ASP) and Astragalus polysaccharide (APS) were fabricated with pH-responsive ASP-hydrazone-ibuprofen (BF) materials (ASP-HZ-BF, SHB) and sialic acid (SA) modified APS-hydrazone-ibuprofen materials (SA/APS-HZ-BF, SPHB) by thin-film dispersion method. The SA in hybrid micelles can specifically bind to the E -selectin receptor which is highly expressed in inflammatory vascular endothelial cells . The loaded Pue could be accurately delivered to the inflammatory site of the kidney in response to the low pH microenvironment . Overall, this study provides a promising strategy for developing hybrid micelles based on natural polysaccharides for the treatment of diabetic nephropathy by inhibiting renal inflammatory reactions, and antioxidant stress.
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ANNALS OF BIOMEDICAL ENGINEERING
·
2018
·Vol. 46
·期 9
·1254-1266
·
IF 3.405
Huang Ruiying,Gao Xiangkai,Wang Jian,Chen Haoxiang,Tong Chunyi,Tan Yongjun,Tan Zhikai
Small-diameter tissue-engineered vascular grafts are urgently needed for clinic arterial substitute. To simulate the structures and functions of natural blood vessels, we designed a novel triple-layer poly(ε-caprolactone) (PCL) fibrous vascular graft by combining E-jet 3D printing and electrospinning techniques. The resultant vascular graft consisted of an interior layer comprising 3D-printed highly aligned strong fibers, a middle layer made by electrospun densely fibers, and an exterior structure composed of mixed fibers fabricated by co-electrospraying. The biocompatible triple-layer graft was used for in vivo implantation, and results demonstrated that the longitudinally-aligned fibers within the lumen of the graft could enhance the proliferation and migration of endothelial cells, while maintained good mechanical properties. The exterior layer provided a pathway that encouraged cells to migrate into the scaffold after implantation. This experimental graft overcame the limitations of conventionally electrospun vascular grafts of inadequate porosity and lowly cell penetration. The unique structure of the triple-layer vascular graft promoted cell growth and infiltration in vivo , thus provided an encouraging substitute for in situ tissue engineering.
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ANALYST
·
2025
·
IF 3.3
Chenyan Li,Yilan Liang,Qincong Feng
Electrochemical biosensors are frequently employed to identify harmful microbes and disease indicators. However, their practical applicability is constrained by poor signal amplification efficiency and immobilization processes on the probe surface. To get over these restrictions, we here integrated roll-cycling amplification (RCA) and CRISPR/Cas12a gene editing tools with electrochemical biosensors. We constructed an electrochemical biosensor based on RCA to activate the cleavage activity of Cas12a. First, by double-stranded nucleic acid aptamer (ds Apt) specifically binding to E. coli-2571, Apt-b was competitively isolated to bind to T4 ligase and produce circular DNA. This in turn activates RCA, which in turn activates the accessory cleavage activity of CRISPR/Cas12a, which in turn cleaves DNA sequences loaded onto the electrode, changing electrochemical signals. With a linear range of 1 × 102–1 × 107 CFU mL−1, a detection limit of 5.28 CFU mL−1, and experimental recoveries of 93.01–101.53%, the measured electrochemical signals were positively connected with the concentration of E. coli-2571 under the optimal experimental conditions. Therefore, by combining two approaches—RCA and CRISPR/Cas12a—our electrochemical biosensor was able to detect E. coli-2571 specifically and sensitively, providing new research opportunities for the detection of other harmful bacteria.
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Molbank
·
2024
·Vol. 2024
·期 2
·M1818
·
IF 0.6
Zhongwei Wang,Luxiao Zhou,Peng He,Yukun Qin
This study presents a novel approach in the realm of catalytic organic synthesis by integrating biomass catalytic conversion with organic synthesis techniques. UtilizingN-acetylglucosamine as the primary feedstock, the first phase of the research involves its catalytic transformation into 5-hydroxymethylfurfural (HMF). The subsequent phase employs a condensation reaction between HMF and 3,3-Dimethyl-2-butanone to synthesize a new compound, (E)-1-(5-(hydroxymethyl) furan-2-yl)-4,4-dimethylpent-1-en-3-one. This two-step process not only demonstrates the feasibility of converting biomass into valuable chemical precursors but also exemplifies the synthesis of novel compounds through green chemistry principles. The successful execution of this methodology offers fresh insights and opens new avenues for advancements in catalytic organic synthesis, emphasizing sustainability and efficiency.
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Methods and Applications in Fluorescence
·
2024
·Vol. 12
·期 2
·025003
·
IF 2.4
Conghuan Lin,Huizhi Du
Forsythoside E is one secondary metabolite of Forsythia suspensa (Thunb.) Vahl. In the study, the interactions between forsythoside E and two types of cholinesterases, acetylcholinesterase and butyrylcholinesterase were investigated in the different conditions. Forsythoside E increased the fluorescence intensity of acetylcholinesterase but quenched the fluorescence of butyrylcholinesterase. Aβ25-35 used in the study may not form complexes with cholinesterases, and did not affect the interaction between forsythoside E and cholinesterases. The charged quaternary group of AsCh interacted with the 'anionic' subsite in acetylcholinesterase, which did not affect the interaction between forsythoside E and acetylcholinesterase. The enhancement rate of forsythoside E to acetylcholinesterase fluorescence from high to low was acid solution (pH 6.4), neutral solution (pH 7.4) and alkaline solution (pH 8.0), while the reduction rate of forsythoside E to butyrylcholinesterase fluorescence was in reverse order. Metal ions may interact with cholinesterases, and increased the effects of forsythoside E to cholinesterases fluorescence, in order that Fe3+ was the highest, followed by Cu2+, and Mg2+. A forsythoside E-butyrylcholinesterase complex at stoichiometric ratio of 1:1 was spontaneously formed, and the static quenching was the main quenching mode in the process of forsythoside E binding with butyrylcholinesterase. The K values of two complexes were pretty much the same, suggesting that the interaction between cholinesterases and forsythoside E was almost unaffected by acid–base environment and metal ions. The n numbers of two cholinesterases approximately equaled to one, indicating that there was only one site on each cholinesterase applicable for forsythoside E to bind to.
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BIOCHEMICAL PHARMACOLOGY
·
2024
·
IF 5.3
Yuge Long,Xiaoyuan Jia,Liang Chu
Gasdermin E ( GSDME ), which is also known as DFNA5 , was first identified as a deafness-related gene that is expressed in cochlear hair cells, and mutation of this gene causes autosomal dominant neurogenic hearing loss. Later studies revealed that GSDME is mostly expressed in the kidney, placenta, muscle and brain cells, but it is expressed at low levels in tumor cells. The GSDME gene encodes the GSDME protein, which is a member of the gasdermin (GSDM) family and has been shown to participate in the induction of apoptosis and pyroptosis. The current literature suggests that Caspase-3 and Granzyme B (Gzm B) can cleave GSDME to generate the active N-terminal fragment (GSDME-NT), which integrates with the cell membrane and forms pores in this membrane to induce pyroptosis. Furthermore, GSDME also forms pores in mitochondrial membranes to release apoptosis factors, such as cytochrome c (Cyt c ) and high-temperature requirement protein A2 (HtrA2/Omi), and subsequently activates the intrinsic apoptosis pathway. In recent years, GSDME has been shown to exert tumor-suppressive effects, suggesting that it has potential therapeutic effects on tumors. In this review, we introduce the structure and function of GSDME and the mechanism by which it induces cell death, and we discuss its tumor suppressive effect.
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