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学者姓名：陈涓涓
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Abstract ：
Malignant tumors pose a serious threat to human life. Dual-functional agents with near-infrared fluorescence imaging and photodynamic therapy (PDT) activities have significant potential for synchronous cancer diagnosis and treatment due to their high sensitivity and noninvasiveness. In this study, based on the "organelle-targeted PDT" strategy, we developed a mitochondria-targeted and endoplasmic reticulum (ER)-located fluorescent probe, HCy-BA, which was constructed by the introduction of the phenylboronic acid group in the receptor component and the alpha-beta unsaturated ester in the donor component of hemicyanine. HCy-BA enables near-infrared fluorescence imaging of ONOO- and viscosity with high sensitivity and specificity, and can effectively distinguish cancer cells from normal cells. Meanwhile, HCy-BA exhibits excellent 1O2 generation capacity, showing significant phototoxicity toward tumor cells and effective tumor suppression in tumor-bearing mice. Furthermore, HCy-BA allows real-time monitoring of mitochondrial autophagy during PDT, facilitating visualization of the treatment process and enabling real-time assessment of PDT. These results highlight the potential of HCy-BA in cancer diagnosis and treatment, offering new insights into the design of integrated molecular for diagnosis and therapy in the future.
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| GB/T 7714 | Wang, Xuyan , Chen, Yingying , Liu, Chunjiang et al. An ONOO-/Viscosity-Sensitive and Mitochondria-Targeted Near-Infrared Fluorophore for Real-Time Tracking Mitophagy and Photodynamic Therapy of Cancer [J]. | ANALYTICAL CHEMISTRY , 2025 , 97 (19) : 10244-10251 . |
| MLA | Wang, Xuyan et al. "An ONOO-/Viscosity-Sensitive and Mitochondria-Targeted Near-Infrared Fluorophore for Real-Time Tracking Mitophagy and Photodynamic Therapy of Cancer" . | ANALYTICAL CHEMISTRY 97 . 19 (2025) : 10244-10251 . |
| APA | Wang, Xuyan , Chen, Yingying , Liu, Chunjiang , Sa, Rongjian , Hu, Xiaoyi , Chen, Juanjuan et al. An ONOO-/Viscosity-Sensitive and Mitochondria-Targeted Near-Infrared Fluorophore for Real-Time Tracking Mitophagy and Photodynamic Therapy of Cancer . | ANALYTICAL CHEMISTRY , 2025 , 97 (19) , 10244-10251 . |
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Metal-organic frameworks, which are the desired candidates for biosensing application due to their tunable properties, are significantly hindered by their rapid degradation in aqueous solutions, as well as the loss of their inherent fluorescence. Most studies aim to improve the hydrophobicity of materials by modifying their contact angle, thereby enhancing water stability. However, water droplets poorly adhere to the surface of hydrophobic materials, limiting their application for direct contact and detection in aqueous environments. Drawing inspiration from the sacrificial protection mechanism of butterfly wings used to evade predation and entanglement, a universal approach is successfully developed to protect water-sensitive MIL-MOFs from water molecule attack while preserving good hydrophilicity. Using the organic ligand 2,2 '-bipyridine-5,5 '-dicarboxylic acid (bpydc) as sacrificial protection scales, the MIL-125-NH2-bpydc demonstrated broad pH structural stability (pH 2-12) and fluorescence stability increased by 10.17 time in aqueous solutions, achieving the highest performance in MILMOFs. The MIL-125-NH2-bpydc is biocompatible enabling it to perform long-term fluorescence imaging in living cells and zebrafish, further detecting hydrogen sulfide (H2S) in the aqueous and biological systems via turn-on fluorescence emission. This study offers a novel and universal sacrifice-protection strategy for the design and development of the luminescent biocompatible MOFs tailored for biosensing applications.
Keyword ：
fluorescence fluorescence H2S H2S metal-organic frameworks metal-organic frameworks sacrifice-protection strategy sacrifice-protection strategy water stable water stable
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| GB/T 7714 | Weng, Zhanglin , Xie, Zhijie , Wu, Xiaoping et al. Water-Stable MIL-MOFs Developed Through a Novel Sacrifice-Protection Strategy Inspired by Butterfly Wings' Scales for Long-Term Turn-On Fluorescence Sensing of H2S [J]. | SMALL METHODS , 2025 . |
| MLA | Weng, Zhanglin et al. "Water-Stable MIL-MOFs Developed Through a Novel Sacrifice-Protection Strategy Inspired by Butterfly Wings' Scales for Long-Term Turn-On Fluorescence Sensing of H2S" . | SMALL METHODS (2025) . |
| APA | Weng, Zhanglin , Xie, Zhijie , Wu, Xiaoping , Qiu, Bin , Chen, Juanjuan , Sun, Weiming et al. Water-Stable MIL-MOFs Developed Through a Novel Sacrifice-Protection Strategy Inspired by Butterfly Wings' Scales for Long-Term Turn-On Fluorescence Sensing of H2S . | SMALL METHODS , 2025 . |
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Advanced prostate cancer is regarded as a fatal disease, characterized by limited treatment options, poor prognosis and considerable tumor metastasis closely related to angiogenesis. Photodynamic therapy emerges as a promising and safe therapeutic modality for advanced prostate cancer with high metastasis and high fatality rate due to its focal damage to tumor cells, as well as its anti-angiogenesis and antitumor immunity capabilities. Herein, a tumor-targeting vascular disrupting agent ASA-404 was introduced to conjugate with a photosensitizer ZnPc for targeted prostate cancer treatment and enhanced vascular-disrupting efficiency. Notably, this novel organic small-molecule photosensitizer Pc-ASA possess a well-defined chemical structure and purity, as well as good photophysical and photochemical properties, which are of benefit for clinical approval and application. PcASA prefers to accumulate in both prostate cancer cells and vascular endothelial cells. Moreover, the conjugation of ASA-404 boosts the photodynamic anticancer effect of Pc-ASA towards both prostate cancer cells and vascular endothelial cells. Ultimately, PC-ASA can successfully inhibit the migration and metastasis of prostate cancer cells, offering significant advantages in advanced prostate cancer management. Our study might open a window in the development of the tumor and vascular dual-targeted small-molecule photosensitizers, with the potential to achieve safe and efficient treatment of metastatic advanced prostate cancer through dual mode of antitumor and anti-vascular action.
Keyword ：
Advanced prostate cancer Advanced prostate cancer Anti-metastasis Anti-metastasis Dual action mode Dual action mode Dual-targeting Dual-targeting Photodynamic therapy Photodynamic therapy Vascular disruption Vascular disruption
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| GB/T 7714 | Chen, Juanjuan , Xu, Jiaqi , Wang, Qilu et al. A dual-targeted small-molecule photosensitizer with enhanced dual antitumor and anti-vascular effect for metastatic advanced prostate cancer photodynamic therapy [J]. | DYES AND PIGMENTS , 2025 , 232 . |
| MLA | Chen, Juanjuan et al. "A dual-targeted small-molecule photosensitizer with enhanced dual antitumor and anti-vascular effect for metastatic advanced prostate cancer photodynamic therapy" . | DYES AND PIGMENTS 232 (2025) . |
| APA | Chen, Juanjuan , Xu, Jiaqi , Wang, Qilu , Lin, Feifei , Zhang, Xueqing , Tang, Lirui et al. A dual-targeted small-molecule photosensitizer with enhanced dual antitumor and anti-vascular effect for metastatic advanced prostate cancer photodynamic therapy . | DYES AND PIGMENTS , 2025 , 232 . |
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本发明公开了一种靶向Mcl‑1酶的锌酞菁3‑氯‑6甲基苯并[b]噻吩‑2‑羧酸轭合物及其制备方法，属于药物化学技术领域。以3‑硝基邻苯二甲腈为原始原料，通过亲核反应得到3‑(4‑羧基甲酯苯氧基)邻苯二腈，再通过成环反应和亲核反应生成1‑(4‑羧基苯氧基)酞菁，最后通过亲核取代反应生成目标产物锌酞菁3‑氯‑6甲基苯并[b]噻吩‑2‑羧酸轭合物。该轭合物能增强对于三阴性乳腺癌细胞的杀伤作用，为提高光动力治疗提供新思路。
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| GB/T 7714 | 陈涓涓 , 薛金萍 , 黄坤山 . 靶向Mcl-1酶的锌酞菁3-氯-6甲基苯并[b]噻吩-2-羧酸轭合物及其制备方法 : CN202210103571.2[P]. | 2022-01-28 00:00:00 . |
| MLA | 陈涓涓 et al. "靶向Mcl-1酶的锌酞菁3-氯-6甲基苯并[b]噻吩-2-羧酸轭合物及其制备方法" : CN202210103571.2. | 2022-01-28 00:00:00 . |
| APA | 陈涓涓 , 薛金萍 , 黄坤山 . 靶向Mcl-1酶的锌酞菁3-氯-6甲基苯并[b]噻吩-2-羧酸轭合物及其制备方法 : CN202210103571.2. | 2022-01-28 00:00:00 . |
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The major challenges in photodynamic therapy (PDT) are the neutralization of cytotoxic reactive oxygen species (ROS) by the excessive antioxidant glutathione (GSH) in tumor cells, high self-aggregation of most photosensitizers (PSs), and long time to protect from light after treatment. Thus, to develop the molecular PSs for the improved and safe PDT in clinic, a novel and versatile PS (Mal-Pc) has been designed by di-substituting maleimides to the axial positions of silicon (IV) phthalocyanine. Owning to the conjugation of maleimides, Mal-Pc can not only entry tumor cells more easily and faster, but also can react with the intracellular overexpressed GSH after entry. In addition, upon electrophilic reaction with GSH, the inhibition of self-aggregation of Mal-Pc has been demonstrated by the restoration of the fluorescence emission in aqueous media. As a result, the intracellular ROS levels and photocytotoxicity of Mal-Pc are dramatically enhanced. Finally, the high hydrophilicity of the product GS-conjugates facilitates Mal-Pc eliminate from the normal cells more rapidly. Overall, this work revealed the high potential of the versatile molecular Mal-Pc for highly efficient and safe PDT in clinical translation.
Keyword ：
Glutathione Glutathione Maleimides Maleimides Photodynamic therapy Photodynamic therapy Phthalocyanine Phthalocyanine
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| GB/T 7714 | Chen, Juanjuan , Yan, Meiqi , Huang, Kunshan et al. Novel molecular photosensitizer with simultaneously GSH depletion, aggregation inhibition and accelerated elimination for improved and safe photodynamic therapy [J]. | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY , 2023 , 245 . |
| MLA | Chen, Juanjuan et al. "Novel molecular photosensitizer with simultaneously GSH depletion, aggregation inhibition and accelerated elimination for improved and safe photodynamic therapy" . | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 245 (2023) . |
| APA | Chen, Juanjuan , Yan, Meiqi , Huang, Kunshan , Xue, Jinping . Novel molecular photosensitizer with simultaneously GSH depletion, aggregation inhibition and accelerated elimination for improved and safe photodynamic therapy . | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY , 2023 , 245 . |
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As one of the most malignant breast cancer types, triple-negative breast cancer (TNBC) treatment is a particularly great challenge in the current era of precision medicine. Due to the limited effectiveness and targeting of current treatment methods, it is urgently need to develop an effective precision strategy to combat TNBC. Herein, a novel TNBC targeted molecular drug based on zinc(II) phthalocyanine (BF-Pc) was rationally designed by conjugating a Pim-1 kinase inhibitor with high TNBC selectivity. In our in vitro investigation, BF-Pc not only exhibits extremely high targeting to TNBC cells overexpressed Pim-1 kinases, but also shows ultra-efficient photocytotoxicity toward TNBC cells far beyond the normal cells. Significantly, BF-Pc-induced PDT can obviously suppress TNBC cell migration and invasion. The proposed manner in our work offers a promising approach to combat TNBC effectively and precisely.
Keyword ：
Invasion Invasion Migration Migration Photodynamic therapy Photodynamic therapy Pim-1 kinase Pim-1 kinase Targeting Targeting Triple -negative breast cancer Triple -negative breast cancer
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| GB/T 7714 | Huang, Kunshan , Yang, Si , Zhang, Yalan et al. A novel Pim-1 kinase-targeted photosensitizer to combat triple-negative breast cancer with enhanced photodynamic efficacy and reduced metastasis [J]. | DYES AND PIGMENTS , 2022 , 207 . |
| MLA | Huang, Kunshan et al. "A novel Pim-1 kinase-targeted photosensitizer to combat triple-negative breast cancer with enhanced photodynamic efficacy and reduced metastasis" . | DYES AND PIGMENTS 207 (2022) . |
| APA | Huang, Kunshan , Yang, Si , Zhang, Yalan , Xue, Jinping , Chen, Juanjuan . A novel Pim-1 kinase-targeted photosensitizer to combat triple-negative breast cancer with enhanced photodynamic efficacy and reduced metastasis . | DYES AND PIGMENTS , 2022 , 207 . |
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Photodynamic therapy (PDT), as an alternative non-invasive clinical treatment modality, has been extensively employed for various anticancer applications in preclinical and clinical trials. However, there is hardly any PDT research based on invasive or metastatic tumors. But it can't be ignored that cancer metastases are responsible for 90% of all cancer-related death. Among these metastatic cancers, prostate cancer (PCa) is regarded as one of the leading causes of cancer related deaths amongst male patients due to its high metastasis and high fatality rate. At present, it remains a great challenge to apply traditional PDT technology for inhibiting prostate cancer metastasis. In this work, we successfully designed and synthesized a novel MAO-A targeted photosensitizer Pc-MLB for targeted photodynamic treatment of prostate cancer and inhibiting its metastasis in vitro. In vitro ex-periments demonstrate that Pc-MLB shows high target affinity and specificity towards prostate cancer cells and remarkable photodynamic anticancer activity compared with the control. More significantly, the migration and invasion assays show that Pc-MLB exhibits the ability to inhibit the migration and metastasis of prostate cancer cells to some extent.
Keyword ：
Anticancer Anticancer Anti-metastasis Anti-metastasis Monoamine oxidase-A Monoamine oxidase-A Photodynamic therapy Photodynamic therapy Phthalocyanine Phthalocyanine
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| GB/T 7714 | Zhao, Xuan , Wang, Qilu , Jia, Xiao et al. A monoamine oxidase-A inhibitor phthalocyanine conjugate for targeted photodynamic therapy and inhibition of prostate cancer metastasis in vitro [J]. | DYES AND PIGMENTS , 2022 , 207 . |
| MLA | Zhao, Xuan et al. "A monoamine oxidase-A inhibitor phthalocyanine conjugate for targeted photodynamic therapy and inhibition of prostate cancer metastasis in vitro" . | DYES AND PIGMENTS 207 (2022) . |
| APA | Zhao, Xuan , Wang, Qilu , Jia, Xiao , Xue, Jinping , Chen, Juanjuan . A monoamine oxidase-A inhibitor phthalocyanine conjugate for targeted photodynamic therapy and inhibition of prostate cancer metastasis in vitro . | DYES AND PIGMENTS , 2022 , 207 . |
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Photodynamic therapy (PDT) has been appeared as a promising clinical diagnosis and treatment for malignant tumor. However, its non-specific distribution and phototoxicity to normal tissues and skinspartially hinders the clinical applications of PDT in cancer diagnosis and therapy. Herein, 2,4-dinitrobenzenesulfonyl chloride, a commonly used quenching agent, is introduced to conjugate with 5,10,15,20-tetra(4-hydroxyphenyl)porphyrin for maximizing therapeutic effects and minimizing side effects of the photosensitizer. Owing to the conjugated 2,4-dinitrobenzenesulfonyl chloride, our designed photosensitizer TDBP can be activated by glutathione (GSH) and hydrogen sulfide (H2S) in solution and cancer cells, and then obtain recuperative fluorescence and photosensitive activity. Moreover, TDBP can achieve enhanced phototoxicity to GSH and H2S overexpressed cancer cells and reduced phototoxicity to normal cells and skins. Overall, the dual responsive photosensitizer developed here is a promising candidate for precisely therapy on GSH and H2S overexpressed cancer cells.
Keyword ：
GSH GSH H2S H2S Photodynamic therapy Photodynamic therapy Porphyrin Porphyrin Responsive photosensitizer Responsive photosensitizer
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| GB/T 7714 | Huang, Kunshan , Xie, Song , Jiang, Lizhi et al. A glutathione and hydrogen sulfide responsive photosensitizer for enhanced photodynamic therapy [J]. | DYES AND PIGMENTS , 2022 , 205 . |
| MLA | Huang, Kunshan et al. "A glutathione and hydrogen sulfide responsive photosensitizer for enhanced photodynamic therapy" . | DYES AND PIGMENTS 205 (2022) . |
| APA | Huang, Kunshan , Xie, Song , Jiang, Lizhi , Li, Jinyu , Chen, Juanjuan . A glutathione and hydrogen sulfide responsive photosensitizer for enhanced photodynamic therapy . | DYES AND PIGMENTS , 2022 , 205 . |
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Multi-modal synergistic therapy, especially the integration of near-infrared laser phototherapies and chemo-therapy, is often sought after owing to its minimal invasiveness, low side effects, and improved anticancer therapeutic efficacy. Herein, CuS nanoparticles were first coated with zinc phthalocya-nine derivant (Pc)-functionalized mesoporous silica (mSiO2-Pc) to achieve a drug delivery system (CuS@mSiO2-Pc) with photo-thermal/photodynamic therapy. Chemical drug DOX was subsequently loaded for chemotherapy, and hyaluronic acid (HA) was employed as a covering material with cancer targeting. The as-obtained CuS@mSiO2-Pc(DOX)@HA nanoparticles were nano-sized with good biocompatibility, effective DOX loading, and controllable DOX releasing. Expectedly, this multifunctional nanoplatform exhibits effective generation of reactive oxygen species and hyperthermia upon the near-infrared laser irradiation. Most importantly, the nanoparticles were targeted into 4T1 cells and showed significantly remarkable cytotoxicity under near -infrared laser irradiation, proving their synergistic therapeutic efficacy. Therefore, this targeted drug system based on CuS with synergistic photothermal therapy/photodynamic therapy/chemotherapy has great application prospects in clinical anticancer treatment for triple negative breast cancer.
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| GB/T 7714 | Lv, Huihui , Zhu, Yuchao , Xue, Jinping et al. Targeted Drug Delivery System Based on Copper Sulfide for Synergistic Near-Infrared Photothermal Therapy/Photodynamic Therapy/Chemotherapy of Triple Negative Breast Cancer [J]. | LANGMUIR , 2022 . |
| MLA | Lv, Huihui et al. "Targeted Drug Delivery System Based on Copper Sulfide for Synergistic Near-Infrared Photothermal Therapy/Photodynamic Therapy/Chemotherapy of Triple Negative Breast Cancer" . | LANGMUIR (2022) . |
| APA | Lv, Huihui , Zhu, Yuchao , Xue, Jinping , Jia, Xiao , Chen, Juanjuan . Targeted Drug Delivery System Based on Copper Sulfide for Synergistic Near-Infrared Photothermal Therapy/Photodynamic Therapy/Chemotherapy of Triple Negative Breast Cancer . | LANGMUIR , 2022 . |
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As a topoisomerase I inhibitor, the prodrug irinotecan has been widely used in the chemotherapy of metastatic cancers. However, the transformation from irinotecan to its active metabolite SN-38 is slow and non-selective in cancer cells, which is not desired for clinical oncotherapy. Additionally, the fluorescence turn-on response of irinotecan is poor, prohibiting real-time observations on SN-38 release. Here, we developed a new prodrug (BDD-SN38) that is well suited for real-time monitoring SN-38 release and reducing its activation in normal cells. The fluorescence and activity of BDD-SN38 was significantly quenched by dinitrobenzene group. The in vitro and in cell results showed that BDD-SN38 could be selectively and rapidly activated by hydrogen sulfide (H2S) to obtain significantly enhanced fluorescence and activity. Moreover, BDD-SN38 achieved remarkable toxicity towards H2S-overexpressed cancer cells. Overall, the H2S-responsive prodrug developed here was proved to be a prom-ising candidate for real-time monitoring SN-38 release and improving its therapeutic effect.
Keyword ：
Chemotherapy Chemotherapy H2S H2S Irinotecan Irinotecan Prodrug Prodrug SN-38 SN-38
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| GB/T 7714 | Huang, Kunshan , Xie, Song , Wang, Weijun et al. A hydrogen sulfide-responsive prodrug for monitoring real-time release and improving therapeutic effects of anticancer drug SN-38 [J]. | SENSORS AND ACTUATORS B-CHEMICAL , 2022 , 373 . |
| MLA | Huang, Kunshan et al. "A hydrogen sulfide-responsive prodrug for monitoring real-time release and improving therapeutic effects of anticancer drug SN-38" . | SENSORS AND ACTUATORS B-CHEMICAL 373 (2022) . |
| APA | Huang, Kunshan , Xie, Song , Wang, Weijun , Wu, Zai-Sheng , Wu, Juhong , Jiang, Lizhi et al. A hydrogen sulfide-responsive prodrug for monitoring real-time release and improving therapeutic effects of anticancer drug SN-38 . | SENSORS AND ACTUATORS B-CHEMICAL , 2022 , 373 . |
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