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| 1 | Radical induced quartet photosensitizers with high ^(1)O_(2) production for in vivo cancer photodynamic therapy显示文摘Singlet oxygen(^(1)O_(2)) is a strong oxidant which plays important roles in photodynamic therapy(PDT). The exploitation of photosensitizers with high ^(1)O_(2) production is crucial to improve PDT efficiency. In this study, a radical labeled quartet photosensitizer Cy-DENT is reported with high singlet oxygen quantum yield(Φ_(Δ)=32.3%) due to a radical enhanced inter-system crossing(ISC) process. After the introduction of 2,2,6,6-tetramethylpiperidinyloxy(TEMPO) radical, quartet state ^(4)[R,T] of CyDENT could be formed to give an over 20-fold enhancement of singlet oxygen quantum yield compared to Cy-DEN(without TEMPO radical) under irradiation of near infrared(NIR) light. In addition, the ^(1)O_(2 )production is well controlled by varying the electron-donating ability of the terminal substituent group. Cy-DENT possesses good cell permeability and is localized in mitochondria. Under the irradiation of 700 nm light, Cy-DENT can produce high levels of ROS to destroy the mitochondria membrane potential and induce cell apoptosis. Through the encapsulation of PEG-SS-PCL micelle, Cy-DENT can be effectively delivered to tumors and suppresses the tumor growth after PDT treatment. | Feng Xu Haoying Ge Ning Xu Cheng Yang Qichao Yao Saran Long Wen Sun Jiangli Fan Xinsheng Xu Xiaojun Peng | 2021 | Science China Chemistry2021，64，3： | 2 |
| 2 | A Cyanine-based Liposomal Nanophotosensitizer for Enhanced Cancer Chemo-Photodynamic Therapy显示文摘Currently,chemotherapy is one of the most important treatment modalities for malignant tumors in the clinic,however,it exhibits some shortcomings,such as poor selectivity,limited efficacy and serious adverse effects.Therefore,synergistic therapy and accurate drug delivery at tumor sites become a promising strategy for achieving tumor eradication.Herein,a smart NIR fluorescence imaging-guided nanoliposome was fabricated by encapsulating a chemotherapeutic drug(doxorubicin,DOX),liposomes(L)and a near-infrared(NIR)photosensitizer(CY)to form L@CY@DOX,which could realize enhanced therapeutic efficacy of chemo-PDT in cancer therapy(PDT=photodynamic therapy).L@CY@DOX can induce mitochondrial apoptosis and produce severe toxicity at the cellular level,and L@CY@DOX can enrich in the tumor site,which significantly induces tumor death.In vitro and in vivo studies demonstrated that L@CY@DOX exhibited great antitumor efficacy compared with each one of these monotherapies,indicating that the combination of chemotherapy and PDT possessed potential development prospects and is anticipated in clinical application. | LI Mengqi MA He SHI Chao ZHANG Han LONG Saran SUN Wen DU Jianjun FAN Jiangli PENG Xiaojun | 2021 | Chemical Research in Chinese Universities2021，37，4： | 0 |
| 3 | A sulfur-substituted hemicyanine for cancer photothermal therapy without influence of intracellular viscosity显示文摘Although photothermal therapy(PTT) has emerged as an appealing strategy for cancer treatment, the development of photothermal agents capable of precisely controlling temperature remains a challenge. In this paper, we present a novel synthetic photosensitizer based on a sulfur-substituted hemicyanine. It was discovered that replacing an oxygen atom in a hemicyanine derivative with a sulfur atom significantly enhances photothermal efficiency and enables lysosome targeting in cancer cells.More importantly, because of the rigid planer structure of the sulfur-substituted hemicyanine, which differs from traditional photothermal agents(PTAs) based on twisted intramolecular charge transfer(TICT) or group rotation mechanisms, the efficiency of photothermal conversion is not affected by intracellular viscosity, allowing precise temperature control during PTT.Further modifying the agent with a glutathione-responsive moiety allows the PTAs to be activated only in cancer cells. The newly proposed PTA achieves efficient PTT in a tumor-bearing mouse model while having negligible toxic side effects on healthy tissues. | Xiang Xia Ran Wang Yingqi Hu Qichao Yao Saran Long Wen Sun Jiangli Fan Xiaojun Peng | 2022 | Science China Chemistry2022，65，4： | 0 |
| 4 | Hydrogen peroxide-activatable iodoBodipy-phthalhydrazid conjugate nanoparticles for cancer therapy显示文摘The dependence on outer light source strongly hinders clinical applications of photodynamic therapy(PDT)to the deep-seated tumor.However,the majority of documented PDT systems that function without the external light source rely on either the chemiluminescence resonance energy transfer(CRET)or fluorescence resonance energy transfer(FRET)mechanism,which decreases the energy transfer efficiency and reproducibility of PDT.Herein,we developed a novel single-molecule triplet photosensitizer(iodoBodipy(IBDP)-L)that can be chemiexcited to triplet excited state to generate reactive oxygen species instead of outer light irradiation.The direct bonding of phthalhydrazid moiety to iodoBodipy fluorophore evoked valid intramolecular energy transfer(IET),and once phthalhydrazid part is activated by hydrogen peroxide,the released reaction energy could excite the iodoBodipy-phthalhydrazid conjugate as a whole.Reaction product IBDP-L-COOH showed high triplet state quantum yield(ΦT=65%)and large spin-orbit coupling.A large amount of reactive oxygen species(ROS)was produced in MCF-7 cells,thus inhibiting the cell growth both in vitro and in vivo after IBDP-L was formulated into nanoparticles(NPs)via nanoprecipitation.We believe that the synthesized IodoBodipy-phthalhydrazid conjugate based on the IET mechanism will open a new door in the molecular design of efficient triplet photosensitizers for treating deeply seated tumors in the future. | Haijun Ning Yuxin Yang Chengyuan Lv Danhong Zhou Saran Long Wen Sun Jianjun Du Jiangli Fan Xiaojun Peng | 2023 | Nano Research2023，16，10： | 0 |
| 5 | Se-sensitized NIR hot band absorption photosensitizer for anti-Stokes excitation deep photodynamic therapy显示文摘Conventional anti-Stokes materials-involved deep photodynamic therapy(dPDT)requires much high-intensity irradiance due to low photosensitization efficiency.Herein,we proposed a'booster effector'approach to construct highly efficient hot band absorption phototherapeutics for low/biosafety power anti-Stokes light-triggered d PDT.Se,as'booster effector',was introduced into hot band absorption luminophores(HBAs),which not only significantly facilitated intersystem crossing,but also simultaneously enhanced hot band excitation efficiency atν808,as a result successfully enabling excellent photogenerated singlet oxygen capability of HBAs under ultra-low power anti-Stokes excitation(10 mW cm^(-2)in vitro).As far as we know,such low laser power-initiated photosensitization activity has never been reported in the existing anti-Stokes material systems.Importantly,FUC-Se ME can self-assemble into uniform nanospheres in water,greatly boosting cellular uptake(>25-fold larger than FUC-Se),and achieve superior cancer-killing effect(808 nm,10 mW cm^(-2),5 min,the half-maximal inhibitory concentration IC50=1.36μM).After further PEGylation with folate-attached polymer,the resultant FUC-Se ME@FA can effectively enrich at the tumor(signal-to-background ratio,10).Under safety irradiation(330 mW cm^(-2)),FUC-Se ME@FA effectively inhibits deep-seated tumor progression(the tumor growth inhibition rate,84%).This work provides a successful paradigm,possibly being more clinically beneficial than conventional anti-Stokes materials. | Dandan Ma Hui Bian Saran Long Panwang Zhou Ruisong Tian Yingnan Wu Haoying Ge Mingle Li Jianjun Du Jiangli Fan Yukui Zhang Xiaojun Peng | 2022 | Science China Chemistry2022，65，3： | 0 |
| 6 | Enhancing Intersystem Crossing by Intermolecular Dimer-Stacking of Cyanine as Photosensitizer for Cancer Therapy显示文摘Development of new photosensitizers(PSs)with high singlet oxygen quantumyield and minimal side effects is of great interest in photodynamic therapy(PDT).Herein,a facile strategy to significantly improve photosensitization has been demonstrated for the first time with two pentamethine dyes connected by a varying alkyl chain resulting in a series of cyanine dimers.The photophysical properties of the dimerswere studied with steady-state optical spectroscopies,a timecorrelated single photon counting technique,and laser flash photolysis spectrometry.X-ray crystallography confirmed that the molecular packing modes of Cy-Bu-D and Cy-He-D were dominated by H-aggregation.The H-aggregation by dimerization suppresses the radiative singlet decay,which helps to stabilize the highly efficient triplet excitation state.Moreover,the dimers show more intensewavelength absorption in the nearinfrared(ɛ1.5-2.0 times more than monomer Cy-H at 650 nm),better singlet oxygen quantum yield,and a longer triplet-state lifetime than monomer Cy-H,providing excellent performance as a triplet PS.In vivo experiments demonstrated that Cy-He-D successfully suppresses tumor growth after PDT treatment.This work is beneficial to the design of novel heavy atom free PSs for PDT-based theranostic systems. | Haiqiao Huang Dandan Ma Qiang Liu Daipeng Huang Xueze Zhao Qichao Yao Tao Xiong Saran Long Jianjun Du Jiangli Fan Xiaojun Peng | 2022 | CCS Chemistry2022，4，11： | 0 |
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