MOLECULAR PHARMACEUTICS
·
2019
·
IF 4.396
Mengting Lin,Wangwei Guo,Zhentao Zhang,Yi Zhou,Jiejian Chen,Tiantian Wang,Xincheng Zhong,Yiying Lu,Qiyao Yang,Qichun Wei,Min Han,Donghang Xu,Jianqing Gao
Nitrogen mustard (NM) is among the earliest drugs used to treat malignant tumors and it kills tumor cells by cross-linking DNA. Unfortunately, because of the short half-life and unfavorable selectivity, NM causes significant damage to normal tissues. As NM can increase the levels of reactive oxygen species (ROS) in tumor cells, a ROS-activated nitrogen mustard prodrug (NM-Pro) was synthesized and mixed with NM at a specific ratio to obtain an “NM-ROS-NM-Pro-NM” positive feedback system, which ultimately achieves a specific lethal effect on hematological neoplasms. The further encapsulation of NM/NM-Pro in liposomes allows the sustained release of the drug and prolongs the residence time in vivo. Here, we prepared stable liposomes with a uniform particle size of 170.6 ± 2.2 nm. The optimal ratio of NM to NM-Pro in this study was 2:1. The active drug NM in the NM/NM-Pro system continuously stimulated ROS production by the cells, which in turn further activated the NM-Pro to continuously generate NM. The positive feedback pathway between the NM and NM-Pro resulted in the specific death of tumor cells. Furthermore, the K562 hematological neoplasm model was utilized to evaluate the therapeutic effect of NM/NM-Pro liposomes in vivo. After encapsulation in liposomes, the targeting of tumor cells was increased approximately two times compared with that of normal cells, and NM/NM-Pro liposomes exhibited reduced toxicity, without an increase in drug activity compared to the NM/NM-Pro combination. The NM/NM-Pro delivery system exerts a positive feedback effect on ROS production in tumor cells and displays good potential for the specific killing of hematoma cells.
研究领域:
肿瘤学
·
药理学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2025
·
IF 4.6
Jiahui Wang,Zixian Shen,Xianfeng Ma,Wenjing Ding,Hua Wang,Mingqi Wang,Xiaofeng Yu
Mitochondria, the primary energy-producing organelles, critically regulate cellular activities. Their internal viscosity—a key microenvironmental parameter—directly affects material transport and energy conversion, with aberrant levels linked to disease pathogenesis. Most reported mitochondrial viscosity probes were susceptible to polar interference, resulting in insufficient specificity for viscosity detection. This study designed and developed a novel polar-insensitive fluorescent probe, Y-CN , based on a phenothiazine skeleton - a small molecular compound with excellent fluorescent properties. The experimental data revealed an excellent linear relationship (R 2 > 0.99) between Y-CN 's fluorescence intensity and viscosity over a wide range from 1.005 to 219 cP. When viscosity increased from 1.005 cP (aqueous buffer) to 219 cP, Y-CN demonstrated a dramatic 209-fold fluorescence amplification. Furthermore, the probe exhibited excellent selectivity, pH stability, and low toxicity. Moreover, Y-CN could detect viscosity changes induced by food thickeners. Y-CN successfully monitored dynamic changes in mitochondrial viscosity within live cells, providing a powerful tool for specific investigation of mitochondria-associated physiological and pathological processes, with significant potential for biological applications.
研究领域:
生物化学
·
细胞生物学
·
生物物理
·
荧光成像
·
分子探针
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Omega
·
2024
·
IF 3.7
Komal Hayat,Gemma Nixon,Qian Zhang,Magdalini Matziari
A highly efficient method to synthesize diverse symmetrical phosphinic acids with the potential to act as pivotal candidates in the design of HIV-1 protease inhibitors has been developed. Such compounds have been designed based on the enzyme–substrate specificity, and their elongated analogues are expected to demonstrate significant inhibition against the HIV-1 protease with IC50 values in the low nanomolar range. Moreover, a highly efficient esterification protocol with carbohydrates and flavonoids has been devised to address the inherent absorption challenges associated with phosphinic-based drugs. These esters not only exhibit low toxicity but also have the potential to generate flavonoid moieties in situ, which are associated with hepatoprotective effects, or naturally occurring carbohydrate metabolites. The methodology utilizes effective peptide coupling reagents, such as aminium-based TBTU and carbodiimide-based DIC, and affords the target products in excellent to quantitative yields. This research represents a promising avenue for the development of novel HIV-1 protease inhibitors with significant therapeutic benefits.
研究领域:
药物化学
·
生物化学
·
抗病毒研究
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF NANOBIOTECHNOLOGY
·
2020
·Vol. 18
·期 1
·1-15
·
IF 6.518
Fu Ji-jun,Li Chu-wen,Liu Yang,Chen Ming-yue,Zhang Qiang,Yu Xi-yong,Wu Bo,Li Jie-xia,Du Ling-ran,Dang Yuan-ye,Wu Dan,Wei Min-yan,Lin Zhi-qiang,Lei Xue-ping
Backgrounds Surgical resection and adjunct chemotherapy or radio-therapy has been applied for the therapy of superficial malignant tumor in clinics. Whereas, there are still some problems limit its clinical use, such as severe pains and side effect. Thus, it is urgent need to develop effective, minimally invasive and low toxicity therapy stagey for superficial malignant tumor. Topical drug administration such as microneedle patches shows the advantages of reduced systemic toxicity and nimble application and, as a result, a great potential to treat superficial tumors. Methods In this study, microneedle (MN) patches were fabricated to deliver photosensitizer IR820 and chemotherapy agent cisplatin (CDDP) for synergistic chemo-photodynamic therapy against breast cancer. Results The MN could be completely inserted into the skin and the compounds carrying tips could be embedded within the target issue for locoregional cancer treatment. The photodynamic therapeutic effects can be precisely controlled and switched on and off on demand simply by adjusting laser. The used base material vinylpyrrolidone—vinyl acetate copolymer (PVPVA) is soluble in both ethanol and water, facilitating the load of both water-soluble and water-insoluble drugs. Conclusions Thus, the developed MN patch offers an effective, user-friendly, controllable and low-toxicity option for patients requiring long-term and repeated cancer treatments.
研究领域:
肿瘤学
·
药学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Materials Horizons
·
2023
·Vol. 10
·期 11
·5004-5015
·
IF 13.3
Dong-Yang Li,Yan-Bing Shang,Qi Liu,Hua-Wu Zhang,Xin-Yue Zhang,Cheng-Yang Yue,Xiao-Wu Lei
Halide perovskite nanocrystal (PNC) of 3D CsPbX3 as a scintillator has aroused intensive attention with advanced applications in radiation detection and X-ray imaging. However, the low light yield and serious toxicity of Pb2+ severely hinder advanced optoelectronic applications. To reduce these fatal shortcomings, a family of new environmentally friendly 0D hybrid lead-free indium halides of [DADPA]InX6·H2O (DADPA = 3,3′-diaminodipropylamine; X = Cl and Br) was prepared. Upon UV excitation, these halides display strong broadband yellow-orange light emissions, and the photoluminescence quantum yield (PLQY) can be optimized up to near unity through the Sb3+-doping strategy. Significantly, high PLQY, negligible self-absorption and low attenuation ability toward X-ray render extraordinary scintillation performance with a high light yield of 51 875 photons MeV−1 and ultralow detection limit of 98.3 nGyair s−1, which is far superior to typical 3D PNC scintillators. Additionally, the ultra-high spatial resolution of 25.15 lp mm−1, negligible afterglow time (2.75 ms) and robust radiant stability demonstrates excellent X-ray imaging performance. To the best of our knowledge, this is the first report on X-ray scintillation based on 0D indium halide materials.
研究领域:
材料科学
·
光学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
POLYMER BULLETIN
·
2021
·Vol. 79
·期 4
·2173-2188
·
IF 2.87
Hou Jiazi,Zhou Guibin,Hu Jinlun,Wang Yihuan,Gao Shuang
Microparticles had attracted a lot of attention for biomedical applications because of their injectable and biomimetic properties. We reported a method for preparing Polylactic acid (PLA)/Polyvinylpyrrolidone (PVP) core–shell microparticles by single capillary electrospraying and explored their potential applications for drug-loading. The shape of microparticles can be controlled by varying ratios of PLA and PVP during the electrospraying process. Different morphologies were achieved including spindle-like, erythrocyte-like and disk-like microparticles. Furthermore, the method of preparing core–shell microparticles was simple and repeatable. Compared with spherical microparticles, erythrocyte-like microparticles can flow through capillaries by morphing into a parachute-like shape. When the particle morphology converted to disk-like, the increase of water contact angle attributed to the PVP rapid dissolution and the residual PLA interconnection to form a continuous hydrophobic membrane. Besides, the microparticle membrane was extremely low-toxic to cells by MTT assay. Taken together, we prepared injected core–shell microparticles by single capillary electrospraying, which had potential application in drug-loading.
研究领域:
生物医学工程
·
材料科学
·
药剂学
✓ 已验证
DOI
高影响因子
JOURNAL OF HAZARDOUS MATERIALS
·
2024
·
IF 12.2
Ziyan Niu,Shenghua Xiao,Guoning Zhou,Kai Sun,Hui Lin,Guodong Fang,Youbin Si
While laccase humification has an efficient capacity to convert estrogenic pollutants, the roles of wheat ( Triticum aestivum L.) root exudates (W-REs) in the enzymatic humification remain poorly understood. Herein, we presented the research into the effects of W-REs on 17 β -estradiol (E2) and bisphenol A (BPA) conversion in vitro laccase humification. W-REs inhibited E2 removal but promoted BPA conversion in the enzymatic humification, and the first-order kinetic constants for E2 and BPA were 0.27–0.69 and 0.28–0.55 h −1 , respectively. Specialized small phenols and amino acids in W-REs were susceptible to laccase humification, resulting in increased copolymerization of estrogen and W-REs. In greenhouse hydroponics, the accumulated amounts of E2 (BPA) in the roots and shoots were estimated to be 0.87 (2.15) and 0.43 (0.51) nmol·plant −1 at day 3, respectively. By forming low- and eventually non-toxic copolymeric precipitates between estrogen and W-REs, laccase humification lowered the phytotoxicity and bioavailability of estrogen in the rhizosphere solution, consequently relieving its uptake, accumulation, and distribution in the wheat cells. This work sheds light on the roles of W-REs in regulating laccase-catalyzed estrogen humification, and gives an insight into the path of addressing organic contamination in the rhizosphere and ensuring food safety.
研究领域:
环境科学
·
植物生理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CERAMICS INTERNATIONAL
·
2018
·
IF 3.057
Shuang Yin,Senchuan Jiang,Limei Pan,Chao Liu,Yongbao Feng,Tai Qiu,Jian Yang
In this work, Si 3 N 4 ceramics were fabricated through an aqueous gelcasting method using a low–toxic monomer called N, N–dimethylacrylamide (DMAA) followed by gas pressure sintering at 1850 °C for 2 h under 6 MPa N 2 atmosphere. The effect of solid loading on performance of slurries, green and sintered bodies was investigated systematically. The results show that the slurries with a solid loading as high as 50 vol% (viscosity 0.17 Pa.s at 100 s –1 ) were achieved. With the increase of solid loading (30–50 vol%), the green bodies exhibited a monotonically decreased, however high enough in general, flexural strength of 16.50–11.52 MPa, which was comparable to that of widely–used neurovirulent acrylamide (AM) gelling system. In regard to the sintered bodies, increasing solid loading significantly promoted sintering and improved mechanical properties and thermal conductivity as a result of the increased density, bimodal distribution structure, as well as suitable interfacial bonding strength . The best performance parameters of Si 3 N 4 ceramics, bulk density of 3.25 g/cm 3 , apparent porosity of 0.67%, flexural strength of 898.92 MPa, fracture toughness of 6.42 MPa m 1/2 , Vickers hardness of 2.81 GPa, and thermal conductivity of 34.69 W m –1 K –1 , were obtained at 50 vol% solid loading. This work renders low–toxic DMAA gelling system promising prospect in preparation of high–performance Si 3 N 4 ceramics by gelcasting.
研究领域:
材料科学
·
陶瓷工程
✓ 已验证
产品关联
DOI
高影响因子
SENSORS AND ACTUATORS B-CHEMICAL
·
2018
·
IF 5.667
Shan Huang,Erli Yang,Yi Liu,Jiandong Yao,Wei Su,Qi Xiao
Heteroatom doping of carbon dots (CDs) can efficiently tune the structure of electronic energy levels and modulate the photochemical properties of CDs. However, the reported synthesis routes of heteroatom-doped CDs are complicated and rigorous. Herein, a simple and rapid low-temperature heating strategy was applied to synthesize fluorescent nitrogen and phosphorus dual-doped CDs (N,P-CDs) using sucrose as carbon source, and 1,2-ethylenediamine (EDA) and phosphoric acid as dopants, respectively. These N,P-CDs exhibit excellent fluorescent stability over wide pH range solutions (4–11), ultrahigh ion strength (3 M KCl), and longtime UV light irradiation (3 h continuously), which makes these N,P-QDs promising good candidates for fluorescent probes. These N,P-CDs showed excellent biocompatibility, multicolor cellular imaging, and non-cytotoxicity to human hepatocellular carcinoma HepG2 cells even at 500 μg/mL levels for 48 h incubation. These N,P-CDs exhibited a strong blue emission and a sensitive response to hemoglobin. The N,P-CDs based fluorescent probe was then applied to sensitively determine hemoglobin with a detection limit of 0.29 nM. Notably, it was also applied for label-free detection of hemoglobin in human urine samples and human blood samples, which indicated its potential applications in clinical diagnosis and other biologically related study.
研究领域:
生物医学工程
·
分析化学
·
纳米材料科学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2022
·
IF 9.965
Hao Zhang,Duxia Cao,Xiao Cheng,Ruifang Guan,Chuanjian Zhou
A novel and simple approach of using amide salt pyrolysis to produce photoluminescent (multi-excitation and single color emission) graphene nanosheets ( GNs ) with a thickness of <1 nm and a diameter of about 100–200 nm is described herein. It has characteristics of high water solubility, low toxicity, easy manufacturing, etc., and has potential application prospects in analytical chemistry and biomedicine.
研究领域:
分析化学
·
生物医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF HAZARDOUS MATERIALS
·
2025
·
IF 11.3
Jiaojie He,Qingwang Cai,Ziyi Kang,Jingxin Zhang,Jiaqi Shen,Yuxin Gu,Zhiquan Liu,Tinglin Huang
This study compared the coagulation performance, floc characteristics, and algal cell integrity between cerium-based coagulants and polyaluminum chloride (PAC). Under optimal dosage (6 mg Ce/L), both CAN (Ce(IV)-based) and CCl (Ce(III)-based) exhibited comparable algal removal efficiency to PAC (>90 %), while generating larger flocs (>1200 µm) that settled rapidly (90 % within 5 min). However, CAN caused significant algal cell lysis during floc aging, whereas CCl exhibited minimal cell damage. Analysis of CCl flocs revealed a distinct increase in the Ce(IV) concentration post-coagulation, accompanied by pronounced phosphate and carboxyl peaks on the floc surface. Further investigation into the extracellular polymeric substances (EPS) during algal coagulation proved that the coagulation mechanism of CCl proceeded in two steps: 1) Anchoring of the coagulant onto the algal surface via strong adsorption of phosphate and carboxyl groups; 2) Synergistic interactions between algae and EPS, which induced partial oxidation of Ce(III) to Ce(IV), triggering in-situ hydrolysis of Ce(IV). This process generated large floc structures and the subsequent coagulation targeted to algae. This study highlights CCl as an eco-friendly and effective alternative with high algal removal and low toxicity (attributed to reduced Ce(IV) dosage), offering practical advantages for water treatment applications.
研究领域:
环境科学
·
水处理技术
·
胶体与界面化学
·
生态毒理学
·
给排水工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOORGANIC CHEMISTRY
·
2024
·
IF 4.5
Haitao Zhu,Houcong Li,Yuxin Ji,Min Hou,Qingling Yang,Lili Liang,Wenge Li
A non-platinum-metal decanuclear complex [Ni 10 L 4 (CH 3 COO) 8 (C 2 H 5 OH) 8 ]·8(C 2 H 5 OH) ( Ni 10 complex) has been developed with a tri-dentate 2,3-dihydroxybenzaldehyde-2-aminophenol Schiff base ligand (H 3 L). Single crystal X-ray analysis reveals that the Ni 10 complex displays a sandwich loaf-shaped decanuclear structure and its anticancer activity was evaluated. The cell cytotoxicity results indicating that the Ni 10 complex is most effective to human breast cancer cells MDA-MB-231 and its mechanism were further investigated. Flow cytometry analysis showed that the Ni 10 complex triggered cell cycle arrest and induced apoptosis of MDA-MB-231 cells. Western blot analysis of the changes of intracellular protein expression showed that Ni 10 triggers MDA-MB-231 apoptosis through mitochondrial mediated apoptosis signaling pathways. In vivo experiments showed that the Ni 10 complex significantly suppressed breast tumor growth with low toxicity against major organs in a nude mice model. The good treatment effect, low toxicity and pharmacological mechanisms of the decanuclear Ni II complex may provide a clue for the research and development of non-platinum multinuclear based chemotherapeutic drugs.
研究领域:
肿瘤学
·
药理学
·
分子生物学
✓ 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）