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CURRENT MOLECULAR MEDICINE · 2021 ·Vol. 21 ·期 9 ·795-805 · IF 2.222

Inducing Tumor Cell Apoptosis: Mediated Survivin miRNA by Ultrasound and Cationic Lipid Contrast Agent

Yang Feng,Chun Liu-Fu,Chen Zhi-Yi

Background: Non-viral delivery systems is a promising method for gene or drug delivery. Polyethyleneimine (PEI) is a double-edged sword. It internalizes itself into the cell through endocytosis and promotes gene transfer efficiency. However, the strong positive charge also makes PEI highly toxic to cells. Ultrasound-targeted microbubble destruction (UTMD) is a promising non-viral method for gene and drug delivery, but its efficiency still needs to be improved. Objective: The aim of this study was to explore a system that combines ultrasound with non-viral gene delivery for the treatment of cervical cancer HeLa cells. Methods: In this study, we synthesized a kind of cationic ultrasound contrast agent(CUCA) that the physical and chemical properties, gene carrying capacity and cytotoxicity were verified. On the basis of previous studies, we further optimized the following transfusion parameters including ultrasound parameters, microbubble concentration, plasmid concentration, cell density and other parameters. The experiment was designed to compare the following six groups: (1) Plasmid group (P group), plasmid 15 μg; (2) PEI + plasmid group (PEI + P group),1 μl of PEI containing 10 nmol nitrogen and 1 μg of DNA containing 3 nmol phosphate for a PEI/DNA ratio equal to a nitrogen/phosphate ratio of 7 for transfection; (3) Ultrasound + plasmid group (US + P), plasmid 15 μg; (4) Ultrasound + cationic liposomal ultrasound contrast agent + plasmid group (UTMD + P group), plasmid 15 μg and cationic liposomal ultrasound contrast agent 5%; (5) Ultrasound + cationic liposomal ultrasound contrast agent + PEI + plasmid group (UTMD + PEI + P group), PEI/DNA ratio equal to a nitrogen/phosphate ratio of 7 for transfection and cationic liposomal ultrasound contrast agent 5%; and (6) Blank group, no treatment), The influence on Hela cells was observed under microscope, the efficiency of apoptosis was measured by flow cytometry, and cell viability was tested in CCK 8. Results: The optimized transfection parameters can improve the transfection efficiency of ultrasound combined with C-UCA to a certain extent, but its transfection efficiency is still lower than that of branched polyethyleneimine (bPEI) 25 kDa. By investigating the effect of HeLa cells apoptosis induced by UTMD in combination with PEI mediated survivin miRNA, we found that both PEI alone and ultrasound in combination with CUCA were able to transfect cells with survivin miRNA to effectively induce HeLa cell apoptosis. However, the synergistic effect between the two methods was not significant. Conclusion: In contrast, the combined use of ultrasound, C-UCA and PEI may significantly reduce the transfection efficiency of UTMD and PEI, and the specific mechanism remains to be further studied.

研究领域: 肿瘤学 · 医学超声 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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RSC Advances · 2016 ·Vol. 6 ·期 89 ·86012-86018 · IF 3.289

Aggregation induced emission controlled by a temperature-sensitive organic–inorganic hybrid polymer with a particular LCST

Mengmeng Li,Xiaoyan Song,Tingbin Zhang,Lintao Zeng,Jinfeng Xing

In this study, an organic–inorganic temperature-sensitive polymer encapsulating tetraphenylethene (TPE) was designed. Its fluorescence intensity is sensitive to temperature changes and reaches a maximum at normal cell temperature. Firstly, the organic–inorganic hybrid polymer, polyhedral oligomeric silsesquioxane-based-poly(N-isopropylacrylamide) (POSS-b-PNIPAM) with a particular LCST of 37.5 °C, was synthesized by atom transfer radical polymerization. POSS-b-PNIPAM self-assembled in aqueous solutions to form stable micelles and then TPE was assembled into the micelles in water. The fluorescence intensity of TPE encapsulated in POSS-b-PNIPAM can be tuned by changing the temperature. The fluorescence intensity of TPE encapsulated in POSS-b-PNIPAM reached a maximum at 37 °C, which is much higher than the TPE fluorescence intensity at the same temperature. TPE encapsulated in POSS-b-PNIPAM still showed high fluorescence intensity after entering HeLa cells at 37 °C.

CAS / MDL: 20769-85-1
研究领域: 材料科学 · 高分子化学 · 生物医学工程
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JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH · 2021 · IF 1.571

Two new coumarins from branches of Zanthoxylum schinifolium

Tian Chai,Yin Qiang

Two new coumarins (1–2) have been isolated from a methanol extract of Zanthoxylum schinifolium branches. The structures of compounds 1 and 2 have been elucidated as 6-isopentenyl −7-benzoyl-coumarin and 3-isopentenyl-7-benzoyl-coumarin based on extensive spectroscopic analysis, including IR, NMR, and MS. The inhibitory activity of compounds 1 and 2 against HeLa and HepG2 cell lines has been described.

CAS / MDL: 33069-62-4
研究领域: 药用植物学 · 药物化学 · 癌症研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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SENSORS AND ACTUATORS B-CHEMICAL · 2024 · IF 8

Dual color carbon dots for simultaneous dynamic fluorescence tracking of mitochondria and lysosomes

Xinlu Li,Tongtong Zhu,Xiangli Quan,Haiyang Yan,Yuwei Du,Ruhong Yan,Wen-Fei Dong,Li Li

The development of fluorescent probes to monitor mitochondria and lysosomes will be helpful not only to realize the status monitoring of the organelles, but also to gain insights into their functions in both healthy and diseased states. Carbon Dots (CDs), as a nanomaterial with excellent properties, have provided new tools and methods for research in organelle imaging in recent years. In this study, we synthesized green fluorescence-emitting carbon dots (G-CDs) with mitochondria-targeting ability and red fluorescence-emitting carbon dots (R-CDs) with lysosome-targeting ability by using the same precursors. G-CDs are brightly with a quantum yield of up to 51.8 % and R-CDs have a long-wavelength emission of 611 nm. Based on the unique properties of G-CDs and R-CDs, we observed the changes of mitochondria during apoptosis and mitochondrial autophagy in HeLa cells by using G-CDs. And the dynamics of lysosomes in the inhibition of cellular autophagy and cellular necrosis were observed by utilizing the R-CDs. Furthermore, we observed human intestinal organoids samples stained by G-CDs and R-CDs, extending the relevant applications of carbon dots imaging to the organoids field, which brings forth new possibilities for research and drug development of related diseases.

研究领域: 纳米技术 · 细胞生物学 · 生物医学工程 · 药物开发
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DYES AND PIGMENTS · 2020 · IF 4.613

Near-infrared fluorescent probes for detection of exogenous and endogenous hypochlorite in living cells

Yu Chen,Yu Qiang Zhao,Ping Xie,Lina Huang,Yumin Wang,Jun Feng Zhang,Xiang Hua Wu,Ying Zhou

Hypochlorous acid (HClO)/hypochlorite (ClO − ) play crucial roles in many physiological and pathological processes. Herein, two near-infrared fluorescent probe FDOCl-1 and FDOCl-2 were designed and synthesized for selective and sensitive detecting ClO − . The probe showed fast response ( FDOCl-1 : less than 50 s, FDOCl-2 : less than 30 s), remarkable colorimetric change, excellent selectivity and sensitivity, low limit of detection ( FDOCl-1 : 53.5 nM, FDOCl-2 : 31.7 nM) and good pH stability. Moreover, the probe FDOCl-2 could penetrate cell membranes , and was used to detect exogenous and endogenous ClO − in living HeLa cells and Caenorhabditis elegans . Thus, we suggest that our newly generated probe FDOCl-2 might have potential application in the rapid and sensitive detection of ClO − in vivo .

研究领域: 生物化学 · 医学 · 分析化学
✓ 已验证 DOI 高影响因子
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ACS Applied Polymer Materials · 2024 · IF 4.4

Synthesis of Fluorescent Functionalized Polyacrylamide and Detection of Cu2+ and CN– in a Pure Water System

Xingtian Zhang,Liwei Hou,Yong Zhang,Xiaoyu Du,Boyuan Yang,Tao Zhou,Hongtao Chu,Wenhui Ma

In this paper, a fluorescent functionalized polyacrylamide material (P) was prepared by free radical precipitation polymerization based on a coumarin derivative (COMN) and acrylamide (AM). The chemical structure and composition of P were analyzed by 1H NMR, UV–vis, and FT-IR spectra. The results of fluorescence spectra of common cations illustrate that P can realize the sensitive detection of copper (Cu2+) within 30 s in the pure water system, and the fluorescence quenching rate is as high as 95.47%, the limit of detection is 7.2 nM. It is worth noting that the above system rapidly changed from green to orange within 0.5 s. In addition, the fluorescence spectra of common anions reveal that P/Cu2+ had a strong interaction with cyanide (CN–) (0–180 μM), and the limit of detection was 39.12 nM. The results of the cell imaging test show that P still manifests a good fluorescence response to Cu2+ and CN– in HeLa cells, which provides a new method for the detection of these ions in vivo.

CAS / MDL: 79-06-1
研究领域: 材料化学 · 分析化学 · 生物医学
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BIOLOGICAL & PHARMACEUTICAL BULLETIN · 2020 ·Vol. 43 ·期 1 ·102-109 · IF 1.863

Design, Preparation and Studies Regarding Cytotoxic Properties of Glycyrrhetinic Acid Derivatives

Qing-Xuan Zheng,Rui Wang,Yan Xu,Chang-Xin He,Cai-Yun Zhao,Zhi-Fang Wang,Rui Zhang,Wim Dehaen,Hui-Jing Li,Qi-Yong Huai

Glycyrrhetinic acid (GA) is a natural product with certain antitumor activity. In order to enhance the cytotoxicity, a total of eighteen derivatives of GA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells) and HeLa cells (human cervical cancer cells), were evaluated by the MTT method (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide). The results indicated that these target compounds have a wide molar activity range and some of them show better activity than the commercial drugs gefitinib and doxorubicin. Compound 6g induces apoptosis of 7, 10 and 44% of MDA-MB-231 cells at 5, 10, and 20 µM, respectively.

研究领域: 药理学 · 肿瘤学 · 药物化学
✓ 已验证 DOI PubMed 高影响因子
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BIOMATERIALS · 2013 · IF 7.604

Ultra-small BaGdF5-based upconversion nanoparticles as drug carriers and multimodal imaging probes

Dongmei Yang,Yunlu Dai,Jianhua Liu,Ying Zhou,Yinyin Chen,Chunxia Li,Ping'an Ma,Jun Lin

A new type of drug-delivery system (DDS) was constructed, in which the anti-cancer drug doxorubicin (DOX) was conjugated to the ultra-small sized (sub-10 nm) BaGdF 5 :Yb 3+ /Tm 3+ based upconversion nanoparticles (UCNPs). This multifunctional DDS simultaneously possesses drug delivery and optical/magnetic/X-ray computed tomography imaging capabilities. The DOX can be selectively released by cleavage of hydrazone bonds in acidic environment, which shows a pH-triggered drug release behavior. The MTT assay shows these DOX-conjugated UCNPs exhibit obvious cytotoxic effect on HeLa cells . Moreover, to improve the upconversion luminescence intensity, core–shell structured UCNPs were constructed. The in vitro upconversion luminescence images of these UCNPs uptaken by HeLa cells show bright emission with high contrast. In addition, these UCNPs were further explored for T 1 -weighted magnetic resonance (MR) and X-ray computed tomography (CT) imaging in vitro . Long-term in vivo toxicity studies indicated that mice intravenously injected with 10 mg/kg of UCNPs survived for 40 days without any apparent adverse effects to their health. The results indicate that this multifunctional drug-delivery system with optimized size, excellent optical/MR/CT trimodal imaging capabilities, and pH-triggered drug release property is expected to be a promising platform for simultaneous cancer therapy and bioimaging .

研究领域: 纳米医学 · 生物医学工程 · 肿瘤学
✓ 已验证 DOI PubMed 高影响因子
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NEW JOURNAL OF CHEMISTRY · 2021 ·Vol. 45 ·期 27 ·11983-11991 · IF 3.591

A coumarin-based reversible fluorescent probe for Cu2+ and S2− and its applicability in vivo and for organism imaging

Wen Lu,Jiuzhou Shi,Jichao Chen,Lu Sun,Lingcen Shao,Hongyu Ren,Mengmeng Huang,Yanqin Wang,Shilong Yang,Xu Li

This study describes the synthesis of a coumarin-based reversible fluorescent probe BuCAC for the detection of Cu2+ and S2− in CH3CN : PBS (v/v = 8 : 2, pH = 7.4) solution. The resulting BuCAC exhibited high sensitivity (detection limit = 3.03 × 10−7 M) and selectivity towards Cu2+ through a 2 : 1 binding mode. In the presence of S2−, the BuCAC–Cu2+ recovered to BuCAC and CuS, which in turn perform the function of a sensitive probe with a lower detection limit of about 1.7 × 10−7 M. This “on–off–on” process can easily occur in 1 min with a repetition of at least 5 times. The sensing mechanism was confirmed by Job's plot analysis, MS, and density theory calculation. Besides, fluorescence imaging in zebrafish, HeLa cells, and soybean root tissue revealed that the probe BuCAC could serve as a valuable tool for monitoring and tracking intracellular Cu2+ and S2− while benefiting from its excellent fluorescence performance and lower cytotoxicity.

研究领域: 分析化学 · 生物化学 · 生物医学工程 · 细胞生物学
✓ 已验证 DOI 高影响因子
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RSC Advances · 2019 ·Vol. 9 ·期 2 ·924-930 · IF 3.049

Photo-patterned oxygen sensing films based on Pt porphyrin for controlling cell growth and studying metabolism

Fei Zeng,Zengju Fan,Shanshan Wu,Xing Cheng,Yanqing Tian

A new type of biocompatible and photo-polymerizable hydrogel with oxygen sensors for microengineering was developed. Herein, a red emitter as an oxygen probe which was chemically immobilized in a poly(2-hydroxyethyl methacrylate)-co-polyacrylamide-based matrix was expected to monitor cell metabolism. A few micropatterned films with gratings (5, 7, 10, 20, and 50 μm in width, respectively and with 1.2 μm in height) were designed and fabricated by photo-lithography using these hydrogels. SEM and AFM were used to validate these films to attain their lateral width and vertical depth. The oxygen responses of these films were characterized. Results showed that patterned films exhibited higher sensitivity than the non-patterned films. The films' construction can also have some influence on cell alignment and elongation. This phenomenon was evaluated by culturing human cervical cancer cells (HeLa cells) and mouse embryo fibroblasts (3T3-L1), on the film surfaces with different construction. Linear correlation between cell elongation and the logarithm of grating width was observed. Real-time monitoring of oxygen consumption of HeLa cells in cell culture medium was achieved. This study is expected to have potential to be applied in micro-structured design and to help understanding metabolism.

CAS / MDL: 9001-37-0
研究领域: 生物工程 · 细胞生物学 · 材料科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2015 · IF 2.912

Decreased Expression of Multidrug Resistance-Associated Protein 4 (MRP4/ABCC4) Leads to Reduced Glucuronidation of Flavonoids in UGT1A1-Overexpressing HeLa Cells: The Role of Futile Recycling

Hua Sun,Xiaotong Zhou,Xingwang Zhang,Baojian Wu

In this study, the role of futile recycling (or deglucuronidation) in the disposition of two flavonoids (i.e., genistein and apigenin) was explored using UGT1A1-overexpressing HeLa cells (or HeLa1A1 cells). Glucuronidation of the flavonoids by HeLa1A1 cell lysate followed the substrate inhibition kinetics (Vmax = 0.10 nmol/min/mg, Km = 0.54 μM, and Ksi = 2.0 μM for genistein; Vmax = 0.19 nmol/min/mg, Km = 0.56 μM, and Ksi = 3.7 μM for apigenin). Glucuronide was efficiently generated and excreted after incubation of the cells with the aglycone (at doses of 1.25–20 nmol). The excretion rates were 0.40–0.69 and 0.84–1.1 nmol/min/mg protein for genistein glucuronide (GG) and apigenin glucuronide (AG), respectively. Furthermore, glucuronide excretion and total glucuronidation were significantly reduced in MRP4 knocked-down as compared to control cells. The alterations were well characterized by a two-compartment pharmacokinetic model incorporating the process of futile recycling (defined by a first-order rate constant, Kde). The derived Kde values were 15 and 25 h–1 for GG and AG, respectively. This was well consistent with the in vitro observation that AG was subjected to more efficient futile recycling compared to GG. In conclusion, futile recycling was involved in cellular glucuronidation, accounting for transporter-dependent glucuronidation of flavonoids.

CAS / MDL: 520-36-5 446-72-0
研究领域: 药理学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ChemistrySelect · 2025 ·Vol. 10 ·期 37 ·e02241 · IF 2

Design, Synthesis, Biological Evaluation, and Molecular Docking of Heterocyclic Aromatic Thioether Derivatives Containing Amides

Yuan Yang,Li Jun Niu,Bian Xiang Zhang

Aromatic heterocyclic sulfides are an essential class of organic compounds and synthetic intermediates, with broad applications in fields such as medicine, agriculture, dyes, and materials science. Importantly, the combination of heterocycles through amide and thioether bonds can effectively enhance their biological activity by leveraging synergistic effects. In this study, we synthesized a series of heterocyclic aromatic sulfide derivatives containing amide groups by incorporating bromoacetic acid and benzylamine into thiol-containing heterocycles or thiophene derivatives. This synthesis was carried out under conditions that ensure high atom economy and environmental friendliness. Subsequently, their antiproliferative effects were evaluated using the MTT assay, which demonstrated selective inhibition of human cervical cancer (HeLa) cells with no significant toxicity to LO2 cells. Notably, compound 3f reduced HeLa cell viability to 63.67% and exhibited good solubility. Molecular docking studies further revealed that compound 3f showed strong interactions with the EGFR receptor, highlighting its potential as a promising anticancer agent. Graphical In this study, aromatic heterocyclic sulfides with amide groups were synthesized via eco-friendly methods using bromoacetate and benzylamine. Compound 3f showed strong HeLa cell inhibition (63.67% viability reduction) and EGFR binding (−8.57 kcal/mol), supported by hydrogen bonds and π–sulfur interactions, highlighting its potential as an anticancer lead.

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