INORGANICA CHIMICA ACTA
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2020
·
IF 2.304
Yang Hu,LongChao Du,Jie Yang
A novel salen derivative, named as 6,6′-((1E,1′E)-(1,2-phenylenebis(azaneylylidene))bis(methaneylylidene))bis(4-(4-iodobutyl)-2-methylphenol) (PA), was obtained for the detection of Zn 2+ . PA exhibited highly sensitive and selective via a chelation mechanism, which was promoted by Zn 2+ , accompanied by enhanced fluorescence. After adding various metal ions in the PA solution, only Zn 2+ caused PA fluorescence enhancement. Other cations (such as Ag + , Al 3+ , Ba 2+ , Ca 2+ , Cd 2+ , Cr 3+ , Cu 2+ , Fe 3+ , Hg 2+ , K + , La 3+ , Li + , Mg 2+ , Na + , Ni 2+ and Pb 2+ ) cannot induce similar response. The binding stoichiometry and detection limit was 1:1 and 16.3 nM, respectively, which is superior to the reported Zn 2+ fluorescent probes based on salen derivatives. The binding process was reasonably speculated by fluorescence measurements, infrared spectroscopy, 1 H NMR titrations, FT-IR, mass spectroscopy (MS) and density functional theory (DFT) calculation. In addition, PA can be used for Zn 2+ fluorescence imaging in HeLa cells. This work indicated that this probe would be of great application prospect in medical diagnosis.
研究领域:
分析化学
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生物医学
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材料科学
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DOI
高影响因子
ANALYTICAL SCIENCES
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2023
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IF 1.6
Yang Yu Meng,Yan Yuan,Zhou Jia Ying,Huang Cheng Zhi,Zhen Shu Jun,Zhan Lei
Real-time monitoring of hypochlorous acid (HClO) in biological systems is of great significance for exploring and regulating its pathological functions because abnormal production of HClO is closely related with many diseases, such as atherosclerosis, rheumatoid arthritis, and cancer. Herein, we developed a reliable fluorescent Fe-doped carbon dots (Fe-CDs) for the sensitive and selective detection of biological HClO using ferrocenecarboxylic acid and m -phenylenediamine as precursors through a one-step solvothermal procedure. The Fe-CDs exhibited excellent a wide HClO detection range from 20 nmol/L to 1000 nmol/L with corresponding limits of detection at 7.8 nmol/L. The sensing mechanism is based on the chemical oxidation of the hydroxyl groups on the surface of Fe-CDs by HClO. In addition, Fe-CDs also displayed high photoluminescence yield, excitation-independence emission, as well as good biocompatibility, enabling the successful imaging of endogenous and exogenous HClO in HeLa cells. These results revealed that Fe-CDs holds great promise as a robust fluorescent probe for investigating HClO-mediated biological events. Graphical abstract
研究领域:
分析化学
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生物医学
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材料科学
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产品关联
DOI
PubMed
高影响因子
RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
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2025
·Vol. 51
·期 6
·2582-2592
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IF 1.7
Wang Yong,Liu Li-Na,Wei Shang-Hua,Wang Wei,Liu Cong-Jun,Gao Song,Yu Shu-Ping,Yao Ning,Wang Yu-Fei
Objective: Dehydroabietic acid (DHAA) is an important natural triterpene resin acid with a wide range of pharmacological activities, including antibacterial, antifungal, antiviral, and anti-inflammatory effects, particularly in antitumor activity. The aim of this study was to synthesize a series of novel dehydroabietic acid 1,2,3-triazole derivatives and evaluate their antitumor activity. Methods: Click chemistry was employed to conjugate dehydroabietic acid (DHAA) with 1,2,3-triazole, yielding 12 DHAA derivatives containing 1,2,3-triazole with yields ranging from 64.5 to 90%. The structures of the target compounds were confirmed by 1 H, 13 C NMR, and HR-MS (ESI). The initial antiproliferative activity of these compounds was assessed in vitro using two tumor cell lines (human cervical cancer cells, HeLa, and human breast carcinoma cells, MCF-7), with cisplatin used as a reference. Results and Discussion: The results indicated that three compounds, VII , VIII , and IX , exhibited significant antiproliferative activity against the tumor cell lines. Among them, compound VIII (4-(4-fluorophenyl)-1-(((1 R ,4a S )-7-isopropyl-1,4a-dimethyl-1,2,3,4,4a,9,10,10a-octahydrophenanthren-1-yl)methyl)-1 H -1,2,3-triazole) demonstrated particularly remarkable activity, with an IC 50 value of 22.1 μM against HeLa cells and 23.2 μM against MCF-7 cells. Conclusions: This study provides useful strategies for the design and synthesis of novel antitumor agents. The synthesized compounds exhibit some inhibitory effects on tumor cell growth and proliferation while causing minimal damage to normal cells, warranting further investigation.
研究领域:
药物化学
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肿瘤学
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有机合成
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药理学
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天然产物研究
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产品关联
DOI
高影响因子
TALANTA
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2014
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IF 3.511
Qingqing Zhang,Ming Zhou
A ratiometric pH probe composed of a fluorescein moiety and an ionic near-infrared-emitting phosphorescent cyclometalated iridium(III) complex bis(6-(benzo[b]thien-2-yl)phenanthridinato)(4-(3-carboxypropyl)-4′-methyl-2,2′-bipyridine)iridium(III) was synthesized. With good cell permeability, the probe demonstrated a linear ratiometric response to the pH variation in the physiological range in HeLa cell assay.
研究领域:
生物化学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2021
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IF 4.098
Kanagaraj Rajalakshmi,Selvaraj Muthusamy,Yun-Sik Nam,Yujun Li,Kang-Bong Lee,Yuanguo Xu
Developing new reaction based recognizing units can enhance the specificity of target analyte molecules in practical applications of real samples and biosystems. Therefore, introducing a recognizing moiety diphenylborinate was encountered for the detection of pyruvate biomolecule through Lewis acid-base reaction based sensing strategy. The construction of the Schiff-base back bone between quinoline and N-(diethylamino)salicylaldehyde-diphenylborinate ( QSB) were expressed the red shift from blue emission of quinoline in to green as that of dative bond developed between Schiff base nitrogen and boron atoms. The new sensing approach was involved such a way that fluorophore QSB is a Lewis acid while pyruvate acts as Lewis base, where the elimination of Lewis pair produced a weak green fluorescence including the formation of quinoline, N-(diethylamino)salicylaldehyde ( QS ). The switching products were witnessed through 1 H NMR titration, HR-MS and FT-IR studies. The good selectivity and interference ability were achieved in presence of 1000-fold excess of possible interferences with LOD of 16 nM. Moreover, the tracking ability of the probe was employed towards pyruvate in live HeLa cell imaging for evaluating an exogenous and endogenous signals producing ability and its mitochondria targeting property was investigated successfully. Further, the practical utility of the probe was tested with milk samples and obtained good recovery results.
研究领域:
分析化学
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生物医学
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产品关联
DOI
PubMed
高影响因子
MOLECULAR DIVERSITY
·
2024
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IF 3.9
Zhou Meng,Duan Xiujie,Jin Tao,Feng Xibing,Liu Ying,Wang Shuo,Feng Jiankang,Zhang Mengtong,Chai Tiantian,Mao Boneng,Shao Shihe,Jin Guofan
Fluorescent drugs and pyrimidine-indole scaffolds have been shown to have advantages in cancer treatment. Fluorescent antitumor drugs BF 3 - o, m, p- phenylenediamine pyrimidine-indole derivatives (PYB1, PYB2, and PYB3) were synthesized by linking pyrimidine and indole groups with aniline through a simple step and introducing BF 3 . The drugs exhibit promising antitumor activity and their fluorescent properties make them useful for imaging purposes. The optical properties of the three compounds have been investigated. All of them have fluorescent properties and compound PYB2 has good fluorescent properties. Additionally, the in vitro cytotoxicity of these compounds was evaluated against the human cancer cell line HeLa and the human normal cell line L02. The inhibition rates of HeLa cells treated with PYB1, PYB2, and PYB3 at a concentration of 19.2 μg/mL were 80.91%, 77.72%, and 65.94%, respectively. These results indicate a strong inhibitory effect on cancer cells. Further through the cell imaging experiment, we can see that PYB2 can enter the cell through the cell membrane through the fluorescence scattering diagram, which has good biocompatibility. In addition, the possible interactions between the compounds and Ras protein active sites were analyzed by molecular docking. The three compounds can bind well to Ras protein through hydrogen bonding. This study provides a basis for the development and modification of pyrimidine-indole fluorescent anticancer drugs. Compound PYB2 shows potential as a fluorescent anticancer drug. Graphical abstract
研究领域:
药物化学
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肿瘤学
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生物医学
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产品关联
DOI
PubMed
高影响因子
TALANTA
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2019
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IF 4.916
Haihong Chen,Lingyi Zhang,Weibing Zhang,Shuai Wang
Exosomal proteins play an important role in screening disease biomarker and clinic diagnosis. However, low concentration, complex composition and difficulty in extraction hindered the study of their structure and properties. In this study, a new protein pre-fractionation system, discontinuous monolithic immobilized pH gradient capillary isoelectric focusing (DM-IPG-CIEF), was constructed by reassembling pieces of monolithic IPG-CIEF column to create small cavity with well-defined pH range. The monolithic IPG-CIEF column exhibited good linearity (R 2 = 0.9997) and preparation and operation reproducibility. Then removal of high-abundant proteins and enrichment of low-abundant proteins were performed by the DM-IPG-CIEF system successfully. The system was applied to pre-fractionation and enrichment of exosomal proteins extracted from HeLa cells. The exosomal proteins with pI in the range of 6.0–9.0 were focused in enrichment cavity and collected. According to nano-HPLC-MS/MS analysis, 130 proteins in this range were identified, indicating great potential of the DM-IPG-CIEF system in pretreatment of exosomal proteins.
研究领域:
生物化学
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蛋白质组学
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医学诊断
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产品关联
DOI
PubMed
高影响因子
Nanomaterials
·
2017
·Vol. 7
·期 10
·338
·
IF 3.553
Xiaobo Pan,Xinyue Liang,Longfang Yao,Xinyi Wang,Yueyue Jing,Jiong Ma,Yiyan Fei,Li Chen,Lan Mi
TiO2nanoparticles modified with phthalocyanines (Pc) have been proven to be a potential photosensitizer in the application of photodynamic therapy (PDT). However, the generation of reactive oxygen species (ROS) by TiO2nanoparticles modified with Pc has not been demonstrated clearly. In this study, nitrogen-doped TiO2conjugated with Pc (N-TiO2-Pc) were studied by means of monitoring the generation of ROS. The absorbance and photokilling effect on HeLa cells upon visible light of different regions were also studied and compared with non-doped TiO2-Pc and Pc. Both N-TiO2-Pc and TiO2-Pc can be activated by visible light and exhibited much higher photokilling effect on HeLa cells than Pc. In addition, nitrogen-doping can greatly enhance the formation of1O2and •O2−, while it suppresses the generation of OH•. This resulted in significant photodynamic activity. Therefore, N-TiO2-Pc can be an excellent candidate for a photosensitizer in PDT with wide-spectrum visible irradiation.Keywords:titanium dioxide;phthalocyanine;reactive oxygen species;photodynamic therapy
研究领域:
材料科学
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生物医学工程
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化学
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癌症治疗
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产品关联
DOI
PubMed
高影响因子
ORGANIC & BIOMOLECULAR CHEMISTRY
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2022
·Vol. 20
·期 28
·5558-5565
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IF 3.89
Hai-Yan Peng,Gang Zhang,Yu-Jie Xu,Ru Sun,Jian-Feng Ge
In this paper, two cationic probes 1a and 1b and a neutral dye 1c were successfully designed and synthesized according to the Knoevenagel condensation reaction, which combines the good optical properties of hemocyanine and the biocompatibility of nitrogen-containing heterocyclic rings based on a quinoxaline skeleton. Probes 1a and 1b showed an OFF–ON fluorescence response to nucleic acids with excellent selectivity. Specifically, the fluorescence intensity of probe 1a was enhanced by 18 and 133 times, respectively, along with the increase of DNA or RNA concentrations (0–600 μg mL−1). Furthermore, a good linear correlation between the fluorescence intensity of probes 1a and 1b and the concentrations of DNA or RNA (0–350 μg mL−1) was obtained. In particular, the maximum emission wavelengths of probes 1a and 1b reached the near-infrared region (660–664 nm) when DNA or RNA was detected, which might reduce the light damage to cells and facilitate cell experiments. Fluorescence imaging revealed that all three dyes could be localized in the mitochondria of HeLa cells. The difference was that probes 1a and 1b could stain the nucleic acid in the mitochondria, while dye 1c was only a neutral mitochondrial biomarker. The results indicated that probes 1a and 1b are promising in the development of low toxicity mitochondrial nucleic acid probes and are expected to be used in monitoring the normal state of mitochondrial nucleic acids for living cells, which will help improve the situation in that currently reported studies of fluorescent probes are mainly focused on the nucleic acids in the nucleus, but less so on DNA in the mitochondria.
研究领域:
生物化学
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分子生物学
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医学影像学
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产品关联
DOI
PubMed
高影响因子
SENSORS AND ACTUATORS B-CHEMICAL
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2025
·
IF 7.7
Meiqing Zhu,Manjie Chen,Xinfu Zhu,Xingyu Zhu,Rimao Hua,Xiaofan Yang,Saraschandra Naraginti,Yi Wang
Hg 2+ -induced oxidative stress is an important pathway mediating biotoxicity, and the dynamics of reactive oxygen/nitrogen species (ROS/RNS) is a key indicator for quantitatively assessing the level of oxidative stress. Herein, a novel “targeted dual recognition” NIR fluorescent chemosensor (DDPT) was constructed for the specific recognition of Hg 2+ and ONOO - . The DDPT activated by Hg 2+ for the detection of ONOO - exhibited rapid response (<50 s), high sensitivity (16.8 nM) and excellent selectivity. The P = S bond in DDPT is oxidized to P = O by Hg 2+ , followed by ONOO - the specific attack on the P-O bond to break it, releasing the DDPT-OH to generate a significant fluorescence enhancement (with a Stokes shift up to 188 nm). The response mechanism of DDPT was systematically verified by 1 HNMR, HRMS and DFT theoretical calculations. Furthermore, DDPT was successfully evaluated for imaging Hg 2+ -induced ONOO - dynamics in cellular, zebrafish and mouse models due to its advantages of low cytotoxicity, high tissue permeability and biocompatibility. The results reveal that Hg 2+ induces oxidative stress and increases ONOO - concentration to destroy the antioxidant defense system of organisms, thus triggering the toxic pathway of oxidative stress. The development of DDPT provides a basis for analyzing pollutant-oxidative stress interactions, assessing health risks, and developing targeted intervention strategies.
研究领域:
生物化学
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毒理学
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医学影像
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产品关联
DOI
高影响因子
PHYTOMEDICINE
·
2019
·
IF 4.18
Wensong Yao,Zhen Lin,Gang Wang,Shaoguang Li,Bing Chen,Yuxia Sui,Jianyong Huang,Qicai Liu,Peiying Shi,Xinhua Lin,Qicai Liu,Hong Yao
Background Cervical cancer (CCa) represents the fourth most common cause of cancer-related death in women worldwide. CCa therapy is still a major clinical challenge worldwide. Finding and developing new anti-CCa chemotherapeutic drugs is a very significant issue. Delicaflavone is a rare biflavonoid from Selaginella doederleinii Hieron , which has shown strong anti-cancer activities in our preliminary screening. Purpose The present study aimed to investigate the apoptotic effect and mechanism of delicaflavone against CCa. Methods In this study, the effect and potential mechanism of delicaflavone against CCa were investigated in vitro and in vivo by MTT assay , TEM , flow cytometry, western blot assay, qPCR assay, immunofluorescence assay and the mouse xenograft tumor model. Results It was confirmed that delicaflavone inhibited the proliferation of human CCa HeLa cells, and induced morphological changes, G2/M phase arrest and apoptosis in a dose- and time-dependent manner. HeLa cells treated with delicaflavone showed the loss of mitochondrial membrane potential , release of Cytochrome c , activation of caspases , alteration of Bax/Bcl-2 balance, and the inhibition of MAPK signaling cascades. Furthermore, delicaflavone significantly decreased tumor growth in a dose-dependent manner without apparent side effects in a xenograft tumor model of HeLa cells. Immunohistochemistry analysis confirmed the up-regulation of Caspase-9, Caspase-3, Bax protein and down-regulation of Bcl-2 protein in the xenografts tumors , which was consistent with the results in vitro . Conclusion The results of the current study show that apoptosis is induced by the mitochondrial pathway accompanying with G2/M cycle arrest and inhibition of MAPK signaling cascades in human CCa HeLa cells, which can be used as a promising therapeutic drug for CCa.
研究领域:
肿瘤学
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药理学
·
细胞生物学
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分子生物学
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DOI
PubMed
高影响因子
MEDICAL SCIENCE MONITOR
·
2018
·
IF 1.894
Xi Chen,Kai Li,Guoqing Zhao
Background Propofol has antitumor effects against various cancers. However, the mechanism of action of propofol in HeLa human cervical cancer cells has not been elucidated. Material/Methods We treated HeLa human cervical cancer cells with different concentrations of propofol. Cell viability was evaluated with Cell Counting Kit-8 and apoptosis was analyzed by annexin V-fluorescein isothiocyanate and propidium iodide staining and flow cytometry. Autophagosome formation was evaluated based on microtubule-associated protein light chain (LC)3 conversion and light chain 3 puncta formation. Autophagosome clearance was assessed according to p62 protein level and autolysosome generation. Results We found that propofol decreased cell viability and increased autophagosome generation in HeLa cells. Autophagosome formation was evaluated based on LC3 conversion and LC3 puncta formation. Autophagosome clearance was assessed according to p62 protein level. The AMPK/mTOR signaling pathway was found to be activated in propofol-induced autophagosome accumulation. Fluorescence analysis using LysoTracker dye revealed that propofol blocked autophagosome–lysosome fusion. Administration of rapamycin increased autophagosome clearance in propofol-treated HeLa cells. Additionally, propofol induced endoplasmic reticulum (ER) stress and disrupted intracellular Ca 2+ balance, thereby enhancing autophagosome accumulation. Suppressing ER stress by treatment with tauroursodeoxycholic acid (TUDCA) enhanced these effects, suggesting that the cytotoxicity of propofol is related to induction of ER stress. Conclusions This study is the first to provide evidence that propofol-mediated autophagy regulation is an underlying part of the mechanism by which propofol regulates HeLa cells progression.
研究领域:
肿瘤学
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细胞生物学
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药理学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）