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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2020 · IF 5.162

Comparative study of two poly(amino acid)-based photosensitizer-delivery systems for photodynamic therapy

Yanli Bao,Haiyang Yu,Yu Zhang,Li Chen

The photosensitizers (PS) play a vital role in photodynamic therapy (PDT), but the clinical therapeutic effect is limited by its low solubility, easy aggregation and lack of selective tumor uptake. Hence, some biocompatible materials such as poly(amino acid) have been chosen to deliver PS to solve these problems. In this study, we fabricated two kind of poly(amino acid)-based PS delivery systems by using poly ( L -glutamic acid) (PLG) as the backbone material to physically encapsulate (P(T)) and chemically conjugate PS (PT), respectively. Moreover, the anticancer effect of these two PS delivery systems had been comparatively investigated. In vitro experiments verified that the delivery system of PT exhibited more effective treatment effect than that of P(T) because PS was chemically conjugated with PLG in PT which could obviously avoid the π-π stacking effect of PS and induced the aggregation. The less aggregation avoiding the quenching effect could result in an enhanced generation ability of reactive oxygen species to improve PDT treatment effect. Contrarily, the treatment effect of P(T) was lower due to the rigid structure and hydrophobic π-π stacking effect, in which the physically encapsulated PS was easier to aggregate and quench. Hence, the way how to combine carrier with drug is significant for satisfied treatment effect.

研究领域: 生物医学工程 · 药学 · 肿瘤学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY · 2018 · IF 4.816

A tumor-targeted Ganetespib-zinc phthalocyanine conjugate for synergistic chemo-photodynamic therapy

Liangfeng Huang,Gaofei Wei,Xiaoqi Sun,Yali Jiang,Zeqian Huang,Yanjuan Huang,Yifeng Shen,Xiaoyu Xu,Yunhui Liao,Chunshun Zhao

Therapeutic effects of photodynamic therapy (PDT) are limited by the selectivity of photosensitizer (PS). Herein, a novel tumor-targeted drug-PS conjugate (Gan-ZnPc) which integrated with zinc phthalocyanine (ZnPc) and Ganetespib has been developed. ZnPc is a promising PS with remarkable photosensitization ability. Ganetespib is a heat shock protein 90 (Hsp90) inhibitor with preferential tumor selectivity and conjugated to ZnPc as a tumor-targeted ligand. The multifunctional small molecule conjugate, Gan-ZnPc, could be bound to extracellular Hsp90 and then selectively internalized into the tumor cells, followed by the generation of abundant intracellular reactive oxygen species (ROS) upon irradiation. Besides, Gan-ZnPc can arrest cell proliferation and induce apoptosis by the inhibition of Hsp90. Herein, with combination of the inhibition of Hsp90 and the generation of cytotoxic ROS, Gan-ZnPc implements tumor selectivity, concentrated PDT and chemotherapy in a synergistic manner, which results in highly effective anti-tumor activity in vitro and in vivo.

研究领域: 药理学 · 肿瘤学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Materials Chemistry A · 2015 ·Vol. 3 ·期 19 ·10386-10394 · IF 7.443

Incorporation of a [Ru(dcbpy)(bpy)2]2+ photosensitizer and a Pt(dcbpy)Cl2 catalyst into metal–organic frameworks for photocatalytic hydrogen evolution from aqueous solution

Chun-Chao Hou,Ting-Ting Li,Shuang Cao,Yong Chen,Wen-Fu Fu

A molecular photosensitizer [Ru(dcbpy)(bpy)2]2+ (dcbpy = 2,2′-bipyridyl-5,5′-dicarboxylic acid) and a proton reduction catalyst Pt(dcbpy)Cl2 were successfully incorporated into a highly robust metal–organic framework (MOF) of Zr(IV)6O4(OH)4(bpdc)6 (bpdc = 4,4′-biphenyldicarboxylic acid) by making use of a mix-and-match approach. The molecular integrity of the Ru and Pt complexes within the MOFs was demonstrated by a variety of techniques, including XRD, BET, TGA, SEM, TEM, HAADF-STEM, EDX, DRUS and XPS. This di-component Ru–Pt@UIO-67 MOF assembly allows a facile arrangement of the photosensitizer and the reduction catalyst with close spatial proximity, promotes the electron transfer between them, and thus leads to a significantly improved hydrogen evolution activity in aqueous solution at pH 5.0 upon visible light irradiation. This Ru–Pt@UIO-67 system represents the first example of MOFs functionalized with two different transition metal complexes, which can be used as a photosensitizer and catalyst, respectively, for hydrogen generation from water.

研究领域: 材料科学 · 化学
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JOURNAL OF CONTROLLED RELEASE · 2017 · IF 7.786

Plasma membrane activatable polymeric nanotheranostics with self-enhanced light-triggered photosensitizer cellular influx for photodynamic cancer therapy

Hao-Ran Jia,Yao-Wen Jiang,Ya-Xuan Zhu,Yan-Hong Li,Hong-Yin Wang,Xiaofeng Han,Zhi-Wu Yu,Ning Gu,Peidang Liu,Zhan Chen,Fu-Gen Wu

To address the issue of low cellular uptake of photosensitizers by cancer cells in photodynamic therapy (PDT), we designed a smart plasma membrane-activatable polymeric nanodrug by conjugating the photosensitizer protoporphyrin IX (PpIX) and polyethylene glycol (PEG) with glycol chitosan (GC). The as-prepared GC-PEG-PpIX can self-assemble into core-shell nanoparticles (NPs) in aqueous solution and the fluorescence of PpIX moieties in the inner core is highly quenched due to strong π – π stacking. Interestingly, when encountering plasma membranes, the GC-PEG-PpIX NPs can disassemble and stably attach to plasma membranes due to the membrane affinity of PpIX moieties, which effectively suppresses the self-quenching of PpIX, leading to significantly enhanced fluorescence and singlet oxygen ( 1 O 2 ) production upon laser irradiation. The massively produced 1 O 2 can compromise the integrity of the plasma membrane , enabling the influx of extracellular nanoagents into cells to promote cell death upon further laser irradiation. Through local injection, the membrane anchored GC-PEG-PpIX enables strong physical association with tumor cells and exhibits highly enhanced in vivo fluorescence at the tumor site. Besides, excellent tumor accumulation and prolonged tumor retention of GC-PEG-PpIX were realized after intravenous injection, which ensured its effective imaging-guided PDT.

CAS / MDL: 67-68-5 6066-82-6
研究领域: 生物医学工程 · 肿瘤学 · 纳米医学
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BIOMACROMOLECULES · 2017 · IF 5.246

Enhanced Fluorescence Emission and Singlet Oxygen Generation of Photosensitizers Embedded in Injectable Hydrogels for Imaging-Guided Photodynamic Cancer Therapy

Liu-Yuan Xia,Xiaodong Zhang,Meng Cao,Zhan Chen,Fu-Gen Wu

Benefiting from their inherent localized and controlled release properties, hydrogels are ideal delivery systems for therapeutic drugs or nanoparticles. In particular, applications of hydrogels for the delivery and release of photoresponsive drugs or nanoparticles are receiving increasing attention. However, the effect of the hydrogel matrix on the fluorescence emission and singlet oxygen generation efficiency of the embedded photosensitizers (PSs) has not been clarified. Herein, meso-tetrakis(1-methylpyridinium-4-yl)porphyrin (TMPyP) as a water-soluble PS was encapsulated into an injectable hydrogel formed by glycol chitosan and dibenzaldehyde-terminated telechelic poly(ethylene glycol). Compared to free TMPyP solution, the TMPyP encapsulated in the hydrogel exhibits three distinct advantages: (1) more singlet oxygen was generated under the same laser irradiation condition; (2) much longer tumor retention was observed due to the low fluidity of the hydrogel; and (3) the fluorescence intensity of TMPyP was significantly enhanced in the hydrogel due to its decreased self-quenching effect. These excellent characteristics lead to remarkable anticancer efficacy and superior fluorescence emission property of the TMPyP–hydrogel system, promoting the development of imaging-guided photodynamic therapy.

研究领域: 生物医学工程 · 肿瘤学 · 药剂学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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POLYMER · 2024 · IF 4.1

A strategy for improving self-healing efficiency: Application of sensitizer in thymine photoresponsive materials

Bin Pu,Gaolang Xiao,Juying Xiao,Hua-Bing Yin,Jin Wang

Self-healing materials based on photodimerization have advantages such as being fast, efficient, environmentally friendly and controllable. However, most of photoresponsive self-healing materials suffer from a problem that there is a compromise between the strength and the self-healing efficiency. Therefore, most of the research focuses on using flexible materials to reach high self-healing efficiency. The absorption wavelengths of some photosensitive groups are narrow, which limits the application fields of self-healing properties of self-repairing materials. Here, we use photodimerizable thymine as the photoresponsive group and exploit the sensitivity of a methoxyacetophenone photosensitizer to increase the self-healing efficiency of a rigid membrane material from beyond repairing to 85% recovery under the same conditions. The tensile strength of the self-healing material is 33.88 MPa, and the elastic modulus reaches 3 GPa after 80 min of photo-irradiation at 308 nm. The maximum thermogravimetric decomposition rate temperature exceeds 400 °C, exhibiting their excellent thermal stability. This strategy provides a novel and effective approach to endow rigid materials with high self-healing efficiency at benign conditions, and opens a new avenue to functionalise a wide range of rigid engineering materials.

研究领域: 材料科学 · 化学工程
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JOURNAL OF MEDICINAL CHEMISTRY · 2024 · IF 6.8

An Activatable Heavy-Atom-Free Upconversion Photosensitizer for Targeted Imaging and Treatment of Tumors

Chao Zhao,Wanlu Sun,Yanyan Zhu,Xiaoyan Huang,Ye Sun,Hai-Yan Wang,Yi Pan,Yi Liu

Photodynamic therapy (PDT) is an innovative and promising method for treating tumors that has attracted significant interest but still faces several challenges, such as a lack of selectivity, deep penetration of light, and efficient ROS generation. To address these challenges, we optimized and synthesized a series of photosensitizers and successfully developed a heavy-atom-free near-infrared FUCL photosensitizer NFh-NMe-2. This photosensitizer can generate singlet oxygen (1O2) and induce cellular apoptosis under 808 nm light. For the safe ablation of microtumors in vivo, an activatable FUCL photosensitizer NFh-NTR was developed based on the overexpression of nitroreductase (NTR). NFh-NTR could be activated by NTR, leading to the release of the photosensitizer NFh-NMe-2, restoring the fluorescence signal, and effectively killing tumor cells under 808 nm light irradiation. This work opens new possibilities in the chemical design of an FUCL photosensitizer for cancer treatment.

研究领域: 生物医学工程 · 肿瘤学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Asian Journal of Pharmaceutical Sciences · 2024 · IF 10.7

Deep near infrared light-excited stable synergistic photodynamic and photothermal therapies based on P-IR890 nano-photosensitizer constructed via a non-cyanine dye

Dawei Jiang,Chao Chen,Peng Dai,Caiyan Li,Zhiyi Feng,Na Dong,Fenzan Wu,Junpeng Xu,Ping Wu,Liuxi Chu,Shengcun Li,Xiaokun Li,Youjun Yang,Weian Zhang,Zhouguang Wang

The cyanine dyes represented by IR780 can achieve synergistic photodynamic therapy (PDT) and photothermal therapy (PTT) under the stimulation of near-infrared (NIR) light (commonly 808 nm). Unfortunately, the stability of NIR-excited cyanine dyes is not satisfactory. These cyanine dyes can be attacked by self-generated reactive oxygen species (ROS) during PDT processes, resulting in structural damage and rapid degradation, which is fatal for phototherapy. To address this issue, a novel non-cyanine dye (IR890) was elaborately designed and synthesized by our team. The maximum absorption wavelength of IR890 was located in the deep NIR region ( ca. 890 nm), which was beneficial for further improving tissue penetration depth. Importantly, IR890 exhibited good stability when continuously illuminated by deep NIR light. To improve the hydrophilicity and biocompatibility, the hydrophobic IR890 dye was grafted onto the side chain of hydrophilic polymer (POEGMA-b-PGMA-g-C CH) via click chemistry. Then, the synthesized POEGMA- b -PGMA- g -IR890 amphiphilic polymer was utilized to prepare P-IR890 nano-photosensitizer via self-assembly method. Under irradiation with deep NIR light (850 nm, 0.5 W/cm 2 , 10 min), the dye degradation rate of P-IR890 was less than 5%. However, IR780 was almost completely degraded with the same light output power density and irradiation duration. In addition, P-IR890 could stably generate a large number of ROS and heat at the same time. It was rarely reported that the stable synergistic combination therapy of PDT and PTT could be efficiently performed by a single photosensitizer via irradiation with deep NIR light. P-IR890 exhibited favorable anti-tumor outcomes through apoptosis pathway. Therefore, the P-IR890 could provide a new insight into the design of photosensitizers and new opportunities for synergistic combination therapy of PDT and PTT.

研究领域: 生物医学工程 · 肿瘤学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Nanoscale · 2025 · IF 5.1

Decreasing the aggregation of photosensitizers to facilitate energy transfer for improved photodynamic therapy

Zhenhua Wang,Jianyang Ao,Xiaoran Lai,Gang Liu,Yun Meng,Yurong Zhang,Jieyun Shi,Yelin Wu,Chaochao Wang

The mode of energy transfer between photosensitizers and oxygen determines the yield of singlet oxygen (1O2), crucial for photodynamic therapy (PDT). However, the aggregation of photosensitizers promotes electron transfer while inhibiting pure energy transfer, resulting in the generation of the hypotoxic superoxide anion (O2−) and consumption of substantial oxygen. Herein, we achieve the reduction of the aggregation of photosensitizers to inhibit electron transfer through classical chemical crosslinking, thereby boosting the production of 1O2. Specifically, we constructed a cross-linked hydrogel-like nanophotosensitizer (HA-TPP NHs) via amidation reactions between hyaluronic acid (HA) and tetrakis(4-aminophenyl)porphyrin (TATPP). In HA-TPP NHs, porphyrin is anchored at the crosslinking sites, preventing their close proximity. Simultaneously, HA-TPP NHs swell in a physiological environment due to water absorption, further increasing the distance between porphyrin molecules to avoid their aggregation. Compared to porphyrin–hyaluronic acid assembling nanoparticles (HA-TPP NPs), we find that the 1O2 generation efficiency of HA-TPP NHs is elevated by over 80%. Furthermore, leveraging the targeting capabilities of hyaluronic acid, HA-TPP NHs demonstrate a remarkable anticancer effect in in vitro and in vivo experiments. This study offers a novel insight and method for improving the therapeutic efficacy of PDT.

CAS / MDL: 9004-61-9
研究领域: 生物医学工程 · 肿瘤学 · 药剂学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ANALYTICAL CHEMISTRY · 2022 · IF 8.008

Novel “Turn-On” Luminescent Chemosensor for Arginine by Using a Lanthanide Metal–Organic Framework Photosensitizer

Xiaoliang Zeng,Siqi Wei,Jing Hu,Lichen Gou,Li Wu,Xiandeng Hou

Arginine is considered as a biomarker of cystinuria and other diseases, and thus, it is of urgency to develop a simple and rapid method with high sensitivity and selectivity for arginine detection to meet the demand of on-site analysis and bedside diagnosis. In this work, a lanthanide metal–organic framework, La(TATB), was prepared using a triazine-based planar ligand, 4,4′,4″-s-triazine-2,4,6-triyltribenzoate (H3TATB), and lanthanide ion (La3+). La(TATB) can be used as a highly photosensitive agent to activate molecular oxygen to 1O2 to achieve efficient photosensitive oxidation of arginine accompanied by strong blue fluorescence emission under 302 nm UV irradiation. Due to the porous structure and high specific surface area of La(TATB), short-life 1O2 can effectively approach and react with amino acid substrate molecules, thus leading to higher sensitivity than other systems. Therefore, the “turn-on” fluorescence sensing of trace arginine can be realized, with a measured linear response range of 10–20,000 nM and a limit of detection as low as 7 nM. This method can be used for the detection of trace arginine in urine, which is conducive to the bedside diagnosis and rapid screening of cystinuria and other diseases. The proposed method not only expands the application scope of Ln-MOFs but also provides a new construction strategy for “turn-on” luminescence sensors.

研究领域: 生物化学 · 医学诊断 · 材料科学
✓ 已验证 DOI PubMed 高影响因子
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CHEMICAL ENGINEERING JOURNAL · 2025 · IF 13.2

Multifunctional MnO2 nanosheet based DNA tetrahedron- photosensitizer nanoplatform for gene-photodynamic modulation

Yanlin Zheng,Fei Li,Xiaohui Zhu,Min Wang,Yuantao Wen,Tao Zeng,Wukun Zhong,Chao Xing,Chunhua Lu

Photodynamic therapy (PDT) holds great promise for treating various types of cancer. However, its clinical advancement is hindered by the intrinsic hypoxic tumor microenvironment, which reduces PDT efficacy, and safety concerns related to the biological specificity of photosensitizers. Here we constructed a MnO 2 nanosheet based DNA tetrahedron-photosensitizer (TMPyP4) nanoplatform (TPM), which integration with tumor targeting (aptamer), gene drugs (DNAzyme) and photosensitizer agents for enhanced PDT. Once the TPM entered cancer cells through aptamer targeting, the MnO 2 nanosheet reacts with endogenous acidic and H 2 O 2 to generate Mn 2+ and oxygen (O 2 ), thereby alleviating the tumor hypoxic. Subsequently, TMPyP4 further converts the generated O 2 into singlet oxygen ( 1 O 2 ) under near-infrared light, enhancing PDT efficacy both in vitro and in vivo. Specifically, the generated Mn 2+ activates the DNAzyme and accelerate tumor target mRNA cleavage, resulting in effective PDT-gene synergistic therapy for tumors. This work offers novel perspectives on advancing precise and highly effective gene-PDT systems.

CAS / MDL: 69-78-3
研究领域: 生物医学工程 · 肿瘤学 · 纳米医学
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CHEMICAL ENGINEERING JOURNAL · 2025 · IF 13.2

Versatile albumin as a booster to optimize the excited state energy redistribution in photosensitizers enabling fluorescence imaging-guided photodynamic therapy

Ting Wang,Lixin Ma,Yingcui Bu,Xinjie Xu,Xuan Zhao,Yingyong Ni,Qitao Zhao,Zhou Lu,Fei Ge,Hongping Zhou

Selectively transforming the non-radiative pathway of excited-state photosensitizers (PSs) into radiative and intersystem crossing (ISC) processes is crucial for fluorescence imaging-guided photodynamic therapy (PDT). Herein, human serum albumin (HSA), with abundant amino acid residues, was co-assembled with anion-π + PSs ( An-O , AnS-O , and AnSS-O ) to create PSs-albumin complexes ( An-O@HSA , AnS-O@HSA , and AnSS-O@HSA ), resulting in promoted biocompatibility and colloidal stability. Both in vitro and in vivo assessments demonstrated that AnSS-O@HSA exhibited the highest-performance fluorescence emission and superoxide anion (O 2 ‑• ) generation capacity, which can effectively induce enhanced apoptosis in HepG2 cells. In-depth mechanistic investigations revealed that HSA, functioning as a boosting agent, could effectively suppress nonradiative decay channels and prolong the triplet state lifetime of PSs. Additionally, HSA can also serve as an electronic reservoir, augmenting its photocurrent response, which further promoted the fluorescence imaging-guided PDT. This study presented a facile strategy for controlling the energy dissipation pathways in the excited state of PSs.

研究领域: 生物医学工程 · 药理学 · 分子生物学
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