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DALTON TRANSACTIONS · 2022 ·Vol. 51 ·期 27 ·10543-10551 · IF 4.569

GaIIItriarylcorroles with push–pull substitutions: synthesis, electronic structure and biomedical applications

Yingjie Niu,Lin Wang,Yingxin Guo,Weihua Zhu,Rodah C. Soy,Balaji Babu,John Mack,Tebello Nyokong,Haijun Xu,Xu Liang

Two A2B type H3corroles and two GaIIItriarylcorroles with carbazole substitutions at 10-positions were synthesized and characterized. An analysis of structure–property relationships of the corroles has been carried out by investigating the optical spectroscopy of the dyes to trends predicted in DFT and TD-DFT calculations. Interestingly, the photodynamic therapy (PDT) and photodynamic antimicrobial chemotherapy (PACT) activity properties of the GaIIItriarylcorroles were determined against the MCF-7 breast cancer line, and Staphyloccocus aureus (S. aureus) and Escherichia coli (E. coli), respectively. The cationic G-2Q species exhibited the most favorable properties with an IC50 value of 7.8 μM against MCF-7 cells, and Log reduction values of 7.78 and 3.26 against planktonic S. aureus and E. coli at 0.5 and 10 μM, respectively.

研究领域: 有机化学 · 生物医学 · 材料科学
✓ 已验证 DOI PubMed 高影响因子
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Nature Communications · 2022 ·Vol. 13 ·期 1 ·1-10 · IF 17.694

An unexpected strategy to alleviate hypoxia limitation of photodynamic therapy by biotinylation of photosensitizers

An Jing,Tang Shanliang,Hong Gaobo,Chen Wenlong,Chen Miaomiao,Song Jitao,Li Zhiliang,Peng Xiaojun,Song Fengling,Zheng Wen-Heng

The most common working mechanism of photodynamic therapy is based on high-toxicity singlet oxygen, which is called Type II photodynamic therapy. But it is highly dependent on oxygen consumption. Recently, Type I photodynamic therapy has been found to have better hypoxia tolerance to ease this restriction. However, few strategies are available on the design of Type I photosensitizers. We herein report an unexpected strategy to alleviate the limitation of traditional photodynamic therapy by biotinylation of three photosensitizers (two fluorescein-based photosensitizers and the commercially available Protoporphyrin). The three biotiylated photosensitizers named as compound 1 , 2 and 3 , exhibit impressive ability in generating both superoxide anion radicals and singlet oxygen. Moreover, compound 1 can be activated upon low-power white light irradiation with stronger ability of anion radicals generation than the other two. The excellent combinational Type I / Type II photodynamic therapy performance has been demonstrated with the photosensitizers 1 . This work presents a universal protocol to provide tumor-targeting ability and enhance or trigger the generation of anion radicals by biotinylation of Type II photosensitizers against tumor hypoxia.

CAS / MDL: 298-83-9 553-12-8
研究领域: 肿瘤学 · 药物化学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Non-coding RNA Research · 2025 · IF 4.7

Inhibition of MALAT1 facilitates ROS accumulation via the Keap1/HO-1 pathway to enhance photodynamic therapy in secondary hyperparathyroidism

Ying Wen,Yitong Li,Danhua Zhang,Ziru Liu,Hong Liu,Xiejia Li,Wei Wu,Liyun Zeng,Qiongyan Zou,Wenjun Yi

The prevalence of secondary hyperparathyroidism (SHPT) in advanced chronic kidney disease (CKD) exceeds 80%. Our previous study indicated that photodynamic therapy (PDT) has potential for treating SHPT. Long noncoding RNA (lncRNA) is involved in various oxidative stress and apoptotic processes, but the molecular mechanism remains unreported. In this study, we found that PDT induced apoptosis in SHPT through reactive oxygen species (ROS) accumulation. The expression of metastasis-associated lung adenocarcinoma transcript 1 (MALAT1) and heme oxygenase 1 (HO-1) within SHPT was upregulated after PDT. Inhibition of MALAT1 increased PDT-induced ROS, which promoted the apoptosis. Pearson correlation analysis confirmed that there was a positive correlation between MALAT1 and HO-1, and MALAT1 inhibition down-regulated HO-1, whereas concomitant overexpression of HO-1 was able to eliminate the PDT-induced ROS and inhibit apoptosis. The direct binding of MALAT1 to Kelch-like ECH-associated protein 1 (Keap1) protein was confirmed by high-throughput sequencing, RNA pulldown, silver staining and western blotting assays. Si-Keap1 was able to rescue the down-regulation of HO-1 caused by MALAT1 inhibition, restoring the elimination of ROS by HO-1 and attenuating the effect of PDT. In addition, PDT effectively reduced parathyroid hormone (PTH) secretion in SHPT rats, and this effect was further enhanced in combination with MALAT1 inhibitors. Overall, MALAT1 activates downstream HO-1 expression by binding to Keap1, thereby reducing ROS and inhibiting apoptosis, which in turn mediates PDT resistance in SHPT. Inhibition of MALAT1 significantly enhanced the efficacy of PDT, suggesting a potential therapeutic target for improving PDT for SHPT outcomes.

CAS / MDL: 5451-09-2
研究领域: 医学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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RSC Advances · 2022 ·Vol. 12 ·期 16 ·10005-10013 · IF 4.036

pH-responsive curcumin-based nanoscale ZIF-8 combining chemophotodynamic therapy for excellent antibacterial activity

Xiaofeng Meng,Jingwei Guan,Shanshan Lai,Liming Fang,Jianyu Su

Antimicrobial photodynamic therapy (aPDT) is a highly attractive therapy due to its advantages of being a non-antibiotic procedure for reducing drug-resistant microbes. Curcumin (CCM) has been considered as a natural photosensitizer for PDT with prominent antibacterial, antifungal, and anti-proliferative activity. However, its excellent biological and pharmacological activities are limited because of its low solubility, rapid metabolization and instability. Herein, we reported a promising agent based on CCM-incorporated into zeolitic imidazolate framework-8 (ZIF@CCM). The as-prepared nanoparticle exhibited high drug loading capability (11.57%) and drug loading encapsulation (82.76%). Additionally, ZIF@CCM displayed a pH-responsive drug release behavior and chemophotodynamic therapy for excellent antibacterial activity. The underlying mechanism elucidated that Zn2+ released from ZIF-8 increased the permeability of the bacterial cell membrane with leakages of K+. The overproduction of extracellular ROS further resulted in the disrupted bacterial cell membrane and distorted bacterial morphology. Thus, ZIF@CCM-mediated photodynamic activation might be a promising treatment strategy for microbial inactivation.

CAS / MDL: 458-37-7 3599-32-4
研究领域: 药学 · 纳米技术 · 生物医学工程 · 微生物学
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DYES AND PIGMENTS · 2022 · IF 5.122

Biodegradable polyphosphazene-based nanodrug to regulate redox homeostasis for augmented chemo-photodynamic therapy

Xunan Jing,Lingjie Meng,Tingting Yang,Ning Zhang,Shu Fan,Yanni Chen,Hongbo Yang,Daquan Wang,Wenchen Ji,Junjun She

Photodynamic therapy (PDT) is more precise than traditional tumor therapy. Nevertheless, PDT efficiency often is hindered by the antioxidant defense system which deplete the required reactive oxide species (ROS). Here we developed a simple but universal method by assembling anticancer drug (resveratrol, RV), photosensitizer (methylene blue, MB) and glutathione (GSH)-sensitive molecules (bis-(4-hydroxyphenyl)-disulfide, HPS) to covalent linking with hexachlorocyclotriphosphazene (HCCP) onto the Fe 3 O 4 to construct a versatile drug delivery nanosystem (FHRHM). Notably, as a multifunctional nanodrug it shows good physiological stability, biocompatibility, and pH/GSH-responsive property to realize the RV and MB controlled release in tumor microenvironment (TME), maximum magnetic resonance (MR)/fluorescence (FL) imaging guided for synergistic chemo-photodynamic therapy (CT-PDT). Especially, the cross-linked FHRHM could be decomposed via reacting with high level of GSH to accelerate release MB for exogenous ROS generation, as well as disrupted disulfide bond (-S-S-) of HPS through depleting GSH to further reduce the endogenous ROS scavenging in TME, thus double amplifying the PDT and simultaneously enhancing CT to induce Hela cells death. This work highlights a novel strategy to construct TME-dissociable nanodrug for augmented CT-PDT via regulation of redox homeostasis, may provide a promising translational approach for tumor theranostics.

研究领域: 肿瘤学 · 药剂学 · 生物材料学
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Bioactive Materials · 2021 · IF 14.593

Persistent luminescence phosphor as in-vivo light source for tumoral cyanobacterial photosynthetic oxygenation and photodynamic therapy

Meiqi Chang,Wei Feng,Li Ding,Hongguang Zhang,Caihong Dong,Yu Chen,Jianlin Shi

Tumor oxygenation level has been regarded as an attractive target to elevate the efficiency of photodynamic therapy (PDT). Cyanobacterial photosynthesis-mediated reversal of tumor hypoxia could enable an oxygen-boosted PDT, but is limited by scant penetration depth and efficiency of external light. Herein, aiming at the dual purposes of reducing biological toxicity induced by long-term light irradiation and alleviating hypoxia, we here introduce a novel-designed CaAl 2 O 4 :Eu,Nd blue persistent luminescence material (PLM) as the in vivo light source after pre-excited in vitro . The ingenious construction of blue-emitting PLM with “optical battery” characteristics activates cyanobacterial cells and verteporfin simultaneously, which performs the successive oxygen supply and singlet oxygen generation without the long-term external excitation, resulting in the modulated tumor hypoxic microenvironment and enhanced photodynamic tumor proliferation inhibition efficiency. Both in vitro cellular assessment and in vivo tumor evaluation results affirm the advantages of self-produced oxygen PDT system and evidence the notable antineoplastic outcome. This work develops an irradiation-free photosynthetic bacteria-based PDT platform for the optimization of both oxygen production capacity and light utilization efficiency in cancer treatment, which is expected to promote the clinical progress of microbial-based photonic therapy.

研究领域: 癌症治疗 · 生物光子学 · 材料科学 · 生物工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY · 2025 · IF 3.7

Combined nanodiamond-mediated drug delivery and upconversion phototherapy for enhanced liver cancer treatment

Yun Teng,Zhige Li,Zheng Cui,Linfeng Wan,Zhuo Li,Xin Zhang,Lesheng Teng,Junsong Liu,Hongdong Li

To mitigate the significant side effects and limited efficacy of traditional treatment methods, we propose a novel strategy that involves the use of nanodiamond (ND) drug loading combined with up-converted blue light irradiation to achieve highly efficient chemotherapy-photodynamic treatment of liver tumor cells, specifically those of the HepG2 cell line. ND-loaded drugs delivered a high concentration of doxorubicin to HepG2 cells, enhancing the chemotherapy effect. Upon exposure to near-infrared irradiation, blue light is excited by up-conversion nanoparticles (UCNPs), thereby activating the production of reactive oxygen qdemonstrated that the dual-mode therapy of chemotherapy and photodynamic therapy showed significantly improved anticancer effects. The inhibition rates were 77.4 % in vitro and 88.1 % in vivo for HepG2 cells, which are significantly higher than those treated with single photodynamic therapy (18.9 %, 28.6 %) or drug-loaded therapy (62.6 %, 71.4 %). It is noted that under the treatment conditions, no obvious tissue injury or inflammation was observed in the heart, liver, spleen, lung, and kidney samples collected from mice, indicating that the UCNPs and NDs exhibit good biocompatibility and are less toxic to normal cells and tissues, which would be favorable for clinical applications.

研究领域: 纳米技术 · 肿瘤学 · 药学 · 生物医学工程 · 光化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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APPLIED SURFACE SCIENCE · 2021 · IF 6.707

Engineering Eu3+-incorporated MoS2 nanoflowers toward efficient photothermal/photodynamic combination therapy of breast cancer

Shengyu Zhou,Xiaodan Jiao,Ying Jiang,Yanan Zhao,Peng Xue,Yingshuai Liu,Jing Liu

Two-dimensional MoS 2 (2D-MoS 2 ) and its nanocomposites have been extensively studied in cancer therapy research since their prominent surface area and NIR absorption ability. In this work, Eu 3+ -incorporated MoS 2 (MoS 2 :Eu 3+ ) nanoflowers with enhanced photothermal conversion efficiency (PCE) were successfully developed by a one-step bottom-up hydrothermal method. Under 808 nm near-infrared (NIR) laser irradiation, the photothermal agents MoS 2 :5%Eu 3+ nanoflowers have a PCE at ~ 49.05%, which is 1.75 times higher than the pristine MoS 2 . MoS 2 :5%Eu 3+ as efficient photosensitizers also promote generation of cytotoxic reactive oxygen species (ROS) under 808 nm laser irradiation, thus achieving photodynamic therapy (PDT) for cancers at the same time. Enhanced in vitro breast cancer therapy through the combination of photothermal therapy (PTT) and PDT is clearly proved by using the MoS 2 :Eu 3+ nanosheet as a multifunctional nanoprobe. The unique MoS 2 :Eu 3+ works as a promising nanoprobe for PDT/PTT cancer therapies, and also provides a novel strategy for PCE improvement of the 2D-MoS 2 .

研究领域: 纳米医学 · 肿瘤学 · 材料科学
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Biomaterials Science · 2025 · IF 5.7

MOF-based nanoagent for self-illuminating photodynamic therapy

Jing-Lan Kan,Fan-Hong Lv,Wen-Xiu Ren,Qun Guan,Anqi Xue,Jie Feng,Yu-Bin Dong

Photodynamic therapy (PDT) is a minimally invasive and local light-activated treatment for annihilating tumor tissues. However, it is often limited by the tissue penetration depth of common external light sources. To address this issue, we herein report a self-illuminating ZIF-90 MOF-based composite photosensitive system prepared using a combined one-pot self-assembly and post-synthetic modification (PSM) methodology. The obtained PME@Zn/Fe-ZIF-90-Lum consists of the Fe(II)-doped and luminol-decorated MOF host as well as the protoporphyrin IX dimethyl ester (PME) guest. Under the given conditions, the light, which is generated from the Fe(II)-catalysed luminol oxidation by endogenous H2O2, can in situ activate the encapsulated photosensitizer PME to produce reactive oxygen species (ROS) via a chemiluminescence resonance energy transfer (CRET) process. In the absence of an external light source, antitumor PDT is successfully realized and high phototoxicity is fully evidenced by in vitro and in vivo experiments.

CAS / MDL: 5522-66-7
研究领域: 纳米医学 · 肿瘤学 · 生物无机化学 · 光动力治疗 · 材料科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2024 · IF 4.5

Fabrication and characterization of dissolving microneedles for transdermal delivery of hypocrellin A

Qi Zong,Guozhen Wang,Zijie Zhao,Wenzhuo Li,Xiaonan Hou,Mengfei Yao,Duo Tang,Chao Sheng,Zijia Liu,Yuchen Zheng,Zhixiang Zhou,Xiaofei Zhang,Xiao Li

Hypocrellin A (HA) is an efficient photosensitizer for photodynamic therapy in recent years. In order to improve the delivery of this photosensitizer, dissolving HA microneedles were established. Firstly, dissolving microneedles were prepared from HA by a two-step solvent casting method. Then, the dissolving HA microneedle were characterized by stereomicroscope, laser confocal microscope, scanning electron microscope, differential scanning calorimeter (DSC), X-ray diffractometer (XRD) and fourier infrared spectrometer (FTIR). Finally, the transdermal cumulative penetration experiments were conducted. The results showed that the dissolving HA microneedle has a conical shape with an average height of 650 μm. The mechanical strength endure a force of 44.78 N, resulting in 0.20 N per needle. The in vitro transdermal experiment showed that the dissolving HA microneedle almost completely dissolved in 5 minutes after insertion into the mouse skin. The depth of drug penetration through the skin can reach 601.36 μm. Moreover, the dissolving HA microneedle significantly improved the cumulative transdermal penetration efficiency of the photosensitizer through the skin. Therefore, the present study successfully established a dissolving microneedle of HA, which can quickly dissolve and significantly improve the transdermal delivery efficiency of HA.

CAS / MDL: 9002-89-5
研究领域: 药剂学 · 生物医学工程
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Theranostics · 2016 · IF 8.854

ROS-Responsive Mitochondria-Targeting Blended Nanoparticles: Chemo- and Photodynamic Synergistic Therapy for Lung Cancer with On-Demand Drug Release upon Irradiation with a Single Light Source

Caixia Yue,Yuming Yang,Chunlei Zhang,Gabriel Alfranca,Shangli Cheng,Lijun Ma,Yanlei Liu,Xiao Zhi,Jian Ni,Weihua Jiang,Jie Song,Jesús M. de la Fuente,Daxiang Cui

Mitochondria in cancer cells maintain a more negative membrane potential than normal cells. Mitochondria are the primary source of cellular reactive oxygen species (ROS), which are necessary for photodynamic therapy. Thus, the strategy of targeting mitochondria can maximize the photodynamic therapeutic efficiency for cancer. Here we report, for the first time, synthesis of a new mitochondria-targeting drug delivery system, ZnPc/CPT-TPPNPs. To synthesize this novel compound, polyethylene glycol was functionalized with thioketal linker-modified camptothecin (TL-CPT) and triphenylphosphonium to form the block copolymer, TL-CPT-PEG 1K -TPP. The ZnPc/CPT-TPPNPs was constructed for delivery of the photosensitizer Zinc phthalocyanine (ZnPc) by blending the block copolymer TL-CPT-PEG 1K -TPP with 1, 2-distearoyl- sn -glycero-3-phosphoethanolamine-N-[methoxy (polyethylene glycol)] (DSPE-PEG).Triphenylphosphine can accumulate selectively several hundred-fold within mitochondria. The thioketal linker is ROS-responsive and CPT can be released upon ROS cleavage. We also show that the ZnPc loaded in ZnPc/CPT-TPPNPs absorbed the 633 nm laser to produce ROS, which could be utilized both in photodynamic therapy and to cleave the thioketal linker thereby releasing camptothecin for chemotherapy. Thus, the mitochondria-targeting nanoparticles could elevate photodynamic therapeutic efficacy. Our results showed that surface modification of the nanoparticles with triphenylphosphine cations facilitated efficient subcellular delivery of the photosensitizer to mitochondria. The nanoparticles had a good ROS-responsive effect to release CPT, which could transfer to the nucleus and interfere with DNA replication as a topoisomeraseⅠinhibitor. Thus, the blended nanoparticles provide a new promising approach as a mitochondria-targeting ROS-activated chemo- and photodynamic therapy with a single light source for lung cancer.

研究领域: 肿瘤学 · 药剂学 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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Frontiers in Chemistry · 2021 · IF 5.221

NIR Photosensitizer for Two-Photon Fluorescent Imaging and Photodynamic Therapy of Tumor

Chen Lujia,Chen Meijuan,Zhou Yuping,Ye Changsheng,Liu Ruiyuan

Preparation of near-infrared (NIR) emissive fluorophore for imaging-guided PDT (photodynamic therapy) has attracted enormous attention. Hence, NIR photosensitizers of two-photon (TP) fluorescent imaging and photodynamic therapy are highly desirable. In this contribution, a novel D-π-A structured NIR photosensitizer (TTRE) is synthesized. TTRE demonstrates near-infrared (NIR) emission, good biocompatibility, and superior photostability, which can act as TP fluorescent agent for clear visualization of cells and vascular in tissue with deep-tissue penetration. The PDT efficacy of TTRE as photosensitizer is exploited in vitro and in vivo. All these results confirm that TTRE would serve as potential platform for TP fluorescence imaging and imaging-guided photodynamic therapy.

CAS / MDL: 307554-62-7 2044-85-1
研究领域: 生物医学工程 · 分子影像 · 诊疗学 · 癌症研究
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