Chinese Chemical LettersPub Date : 2026-04-01Epub Date: 2025-10-22DOI: 10.1016/j.cclet.2025.112002
Siwei Wang , Fanxu Zeng , Yuan Yan , Jinghai Liu , Wei-Lei Zhou , Yong Chen
{"title":"Monochromophore-tunable supramolecular fluorescence-phosphorescence dual light-harvesting NIR emission for multi-dimensional information encryption","authors":"Siwei Wang , Fanxu Zeng , Yuan Yan , Jinghai Liu , Wei-Lei Zhou , Yong Chen","doi":"10.1016/j.cclet.2025.112002","DOIUrl":"10.1016/j.cclet.2025.112002","url":null,"abstract":"<div><div>Organic fluorescence-phosphorescence dual-emitting materials based on tunable single chromophores have attracted much attention for their broad application prospects in information technology, display media and other fields due to their high luminescence stability, simple preparation process and excellent reproducibility. Herein, we constructed a novel LP-activated fluorescence-phosphorescence dual-light-harvesting (FPRET) supramolecular assembly based on LP with orthogonal charges, the phosphorescent molecule G and the NIR dye NIB through a supramolecular non-covalent strategy. The energy transfer efficiency of fluorescence is 54.68 % when the molar ratio of <strong>G</strong>/LP to NIB is 10:1, while the energy transfer efficiency and antenna effect of phosphorescence are 48.75 % and 241.43 respectively when the molar ratio of G/LP to NIB is 50:1. In addition, by co-assembling with carbon dots (CDs) and adjusting the ratio of donor to acceptor components, the full-color spectral regulation including white light (CIE chromaticity coordinates x, <em>y</em> = 0.31, 0.33) was realized. Utilizing this LP to promote the supramolecular full-color FPRET assembly of single fluorophore <strong>G</strong> and showing the multi-level anti-counterfeiting of intelligent logic gates through pattern, time, and color editing, it provides a new insight and direction for the development of a new generation of high-performance optical functional materials.</div></div>","PeriodicalId":10088,"journal":{"name":"Chinese Chemical Letters","volume":"37 4","pages":"Article 112002"},"PeriodicalIF":8.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145975308","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chinese Chemical LettersPub Date : 2026-04-01Epub Date: 2025-06-26DOI: 10.1016/j.cclet.2025.111516
Meng-Xin Liu , Xiao-Long Su , Pu Chen , Yan-Yan Liu , Jian-Peng Li , Li Zou , Ben Zhong Tang , Hai-Tao Feng
{"title":"Sequential FRET system based on macrocyclic AIEgens for versatile photocatalysis","authors":"Meng-Xin Liu , Xiao-Long Su , Pu Chen , Yan-Yan Liu , Jian-Peng Li , Li Zou , Ben Zhong Tang , Hai-Tao Feng","doi":"10.1016/j.cclet.2025.111516","DOIUrl":"10.1016/j.cclet.2025.111516","url":null,"abstract":"<div><div>Supramolecular architectures exhibiting cascade energy transfer characteristics represent pivotal model systems for advancing biomimetic light-harvesting systems (LHS) that emulate the natural photosynthesis. To now, the engineering of aqueous-phase artificial LHS with optimized energy transfer cascades is still a challenge. In this study, we designed and synthesized two tetraphenylethylene (TPE)-based macrocyclic compounds (namely TPE-1 and TPE-2) with different cavity sizes as supramolecular scaffolds to study their energy transfer behaviors. As a control model, a linear molecule TPE-3 was also prepared. The bigger-cavity macrocycle TPE-1 can emit green fluorescence and self-assemble into nanospherical structures in aqueous media, acting as an energy donor. Through self-assembly with eosin Y (EY) and a red-emitting fluorophore (TPE-Se), a sequential Förster resonance energy transfer (FRET) cascade: TPE-1→EY→TPE-Se was achieved thanks to their excellent spectral overlap and proximity between the donor and acceptors. The optimized ternary system (TPE-1/EY/TPE-Se) with a ratio of 1000:90:60 afforded a high energy transfer efficiency (<span><math><mstyle><mi>Φ</mi></mstyle></math></span><sub>ET</sub>) of 95 %. Then, the artificial LHS platform catalyzed the oxidative coupling of benzylamines with 93 % yield in aqueous media. Moreover, the system demonstrated broad catalytic utility oxidation reactions, the good conversion of methylthiobenzyl ester to methylbenzene sulfoxide and the aerobic cross-dehydrogenation coupling reaction of N-phenyltetrahydroisoquinoline with indole. These results robustly demonstrate the promising potential of this artificial LHS in the field of aqueous photocatalysis.</div></div>","PeriodicalId":10088,"journal":{"name":"Chinese Chemical Letters","volume":"37 4","pages":"Article 111516"},"PeriodicalIF":8.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145975319","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chinese Chemical LettersPub Date : 2026-04-01Epub Date: 2025-10-10DOI: 10.1016/j.cclet.2025.111938
Hui Chen , Xieraili Tuerxun , Amina Abula , Yenan Sun , Hanqi Zhang , Guangmin Yao , Haji Akber Aisa
{"title":"Discovery of pyrethalkalines A and B as potent analgesics with unprecedented chemical skeletons dual targeting TRPM8 and Kv1.2 ion channels","authors":"Hui Chen , Xieraili Tuerxun , Amina Abula , Yenan Sun , Hanqi Zhang , Guangmin Yao , Haji Akber Aisa","doi":"10.1016/j.cclet.2025.111938","DOIUrl":"10.1016/j.cclet.2025.111938","url":null,"abstract":"<div><div>Two pairs of potent analgesic alkaloid enantiomers with unprecedented chemical architectures, named pyrethalkalines A (<strong>1</strong>) and B (<strong>2</strong>), were isolated from the roots of <em>Anacyclus pyrethrum</em>. Pyrethalkaline A (<strong>1</strong>) is an unprecedented 6/6/6/6/5-fused pentacyclic triamino alkaloid featuring a unique 8,15-diaza-pentacyclo[12.3.1.1<sup>1,9</sup>.0<sup>5,19</sup>.0<sup>10,14</sup>]nonadecane core, and pyrethalkaline B (<strong>2</strong>) is a novel 6/6/6/6/5/6-fused hexacyclic triamino alkaloid possessing an unprecedented 8,13,19-triazahexacyclo[16.3.1.1<sup>1,9</sup>.0<sup>5,23</sup>.0<sup>10,18</sup>.0<sup>11,16</sup>]tricosane motif. Their structures were elucidated by comprehensive spectroscopic data analysis, quantum <sup>13</sup>C nuclear magnetic resonance (NMR) DP4+ and electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction analysis, and their plausible biosynthetic pathways were proposed. Alkaloids (±)-<strong>1</strong> and (−)-<strong>1</strong> at three lower doses of 1, 0.2, and 0.04 mg/kg, and (+)-<strong>2</strong> at two lower doses of 1 and 0.2 mg/kg showed more potent analgesic activity than the positive control morphine. Further investigation revealed that (+)-<strong>1</strong> and (−)-<strong>1</strong> are dual transient receptor potential melastatin 8 (TRPM8) (half-maximal inhibitory concentration (IC<sub>50</sub>) = 1.90 ± 0.09 and 1.40 ± 0.17 µmol/L, respectively) and Kv1.2 inhibitors. Molecular dockings of <strong>1</strong> provide a novel structural model to develop potent analgesics dual targeting TRPM8 and Kv1.2 ion channels, and (±)-<strong>1</strong> have the potential for the development of a non-opioid potent analgesic to treat neurogenic pains.</div></div>","PeriodicalId":10088,"journal":{"name":"Chinese Chemical Letters","volume":"37 4","pages":"Article 111938"},"PeriodicalIF":8.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145975249","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chinese Chemical LettersPub Date : 2026-04-01Epub Date: 2025-09-05DOI: 10.1016/j.cclet.2025.111788
Mengyuan Zhao , Xianming Liu , Haiyue Ye , Dachuan Ma , Yue Hou , Hongyu Dong , Yangyang Long , Ningning Liu , Xiaoxu Wang , Xiaodan Yu , Yahong Chen , Xinmiao Liang , Yao Lu
{"title":"Digital microfluidics actuated multiplexed heterogeneous immunoassay with enhanced automation and efficiency","authors":"Mengyuan Zhao , Xianming Liu , Haiyue Ye , Dachuan Ma , Yue Hou , Hongyu Dong , Yangyang Long , Ningning Liu , Xiaoxu Wang , Xiaodan Yu , Yahong Chen , Xinmiao Liang , Yao Lu","doi":"10.1016/j.cclet.2025.111788","DOIUrl":"10.1016/j.cclet.2025.111788","url":null,"abstract":"<div><div>Digital microfluidics (DMF) shows great promise in addressing the need for miniaturization and automation in immunoassay detection. Despite recent advances, an automatically operated, multiplexed heterogeneous immunoassay platform powered by DMF remains underdeveloped. Here we present a DMF platform for automated and multiplexed heterogeneous immunoassay detection by coupling spatial barcoding with automatic and uniform droplet dispensing. FluoroPel was selected as a robust hydrophobic reagent for coating the DMF top plate, and it also served as the substrate for the immuno-reaction. Its mechanical robustness was further enhanced with a Cytop CTL-809A adhesive layer under the top hydrophobic layer. Hourglass-shaped electrode patterns ensured consistent and uniform distribution of immunoassay reagents, with volume variation down to 1.0 %. The analysis duration was significantly reduced from 75 min to 20 min after a heating module was integrated to elevate the immuno-reaction temperature to 37 °C. Utilizing a compact instrument featuring a multi-droplet manipulation protocol, we successfully implemented fully operated, multi-sample, multiplexed immunoassays using recombinant proteins on cell culture supernatants on the DMF platform. This innovative platform significantly enhances the efficiency, reliability, and degree of automation of DMF-actuated multiplexed heterogeneous immunoassays, potentially providing a viable solution for field deployment and multi-sample parallel diagnosis.</div></div>","PeriodicalId":10088,"journal":{"name":"Chinese Chemical Letters","volume":"37 4","pages":"Article 111788"},"PeriodicalIF":8.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146035432","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chinese Chemical LettersPub Date : 2026-04-01Epub Date: 2025-09-02DOI: 10.1016/j.cclet.2025.111781
Xia Jiang , Yan-Xin Chen , Rui Chen , Hao-Yan Shi , Ke-Xian Li , Wen-Ya Zhong , Jian-Feng Li , Can-Zhong Lu
{"title":"Thermo-photocatalytic CO2 conversion with H2O to C2 products in a continuous process by ZIF-67/biochar composites","authors":"Xia Jiang , Yan-Xin Chen , Rui Chen , Hao-Yan Shi , Ke-Xian Li , Wen-Ya Zhong , Jian-Feng Li , Can-Zhong Lu","doi":"10.1016/j.cclet.2025.111781","DOIUrl":"10.1016/j.cclet.2025.111781","url":null,"abstract":"<div><div>Thermo-photocatalytic CO<sub>2</sub> conversion to C<sub>2</sub> products exhibits high research value and industrial potential. Enhancing the catalyst’s adsorption activation for CO<sub>2</sub> and H<sub>2</sub>O, along with multistep proton-coupled electron transfer (PCET) and C-C coupling, is crucial for achieving thermo-photocatalytic CO<sub>2</sub> reduction conversion to C<sub>2</sub> products with H<sub>2</sub>O as a proton source in a continuous process. In this paper, we explore a novel approach utilizing biochar to obtain catalysts with more defects and combine reducing biochar with MOF Materials (ZIF-67) to get a composite (ZIF-67/PC) with substantial CO<sub>2</sub> and H<sub>2</sub>O adsorption activation capabilities and electron density gradients. Compared to PC and ZIF-67, the ZIF-67/PC exhibited excellent catalytic performance, particularly in obtaining a certain amount of C<sub>2</sub> products (yield 5.59 µmol g<sup>-1</sup> h<sup>-1</sup>, selectivity 55.96%). We also investigated the structure-function relationship of the catalyst and the contributions of thermal and light effects to the catalytic reaction, aiming to guide the establishment of efficient, high-throughput catalytic CO<sub>2</sub> conversion technologies.</div></div>","PeriodicalId":10088,"journal":{"name":"Chinese Chemical Letters","volume":"37 4","pages":"Article 111781"},"PeriodicalIF":8.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146035431","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chinese Chemical LettersPub Date : 2026-04-01Epub Date: 2024-12-14DOI: 10.1016/j.cclet.2024.110755
Zhi-Long Li , Hao-Fei Ni , Bo Zhuang , Kun Ding , Da-Wei Fu , Qiang Guo , Meng-Meng Lun
{"title":"Halogen substitution strategy for regulating the photoluminescence and dielectric response of ferroelastics","authors":"Zhi-Long Li , Hao-Fei Ni , Bo Zhuang , Kun Ding , Da-Wei Fu , Qiang Guo , Meng-Meng Lun","doi":"10.1016/j.cclet.2024.110755","DOIUrl":"10.1016/j.cclet.2024.110755","url":null,"abstract":"<div><div>Ferroelastics have attracted considerable interest because of their promising uses in areas such as energy conversion, sensing technologies, and beyond. However, exploring ferroelastics with high-temperature dielectric switching and photoluminescence remains a challenge. Here, we have synthesized two ferroelastics (DMTP)PbBr<sub>3</sub> (DMTP = <em>N,N</em>-dimethyl-1,2,3,6-tetrahydropyridine) and (DMTP)PbI<sub>3</sub> under the guidance of halogen substitution strategy. (DMTP)PbI<sub>3</sub> experiences the dielectric switching at 371 K, and upon halogen substitution, the strengthened intermolecular interactions lead to (DMTP)PbBr<sub>3</sub> undergoing a similar switching at around 390 K. Additionally, two compounds both emit orange light under ultraviolet illumination. (DMTP)PbI<sub>3</sub> has the photoluminescence quantum yield of 2.68 %, while (DMTP)PbBr<sub>3</sub>, due to the increased distortion of the inorganic part after halogen substitution, achieves the higher quantum yield of 12 %. This work offers meaningful perspectives on exploring the search for ferroelectrics with photoluminescence and high-temperature dielectric switching, and also demonstrates the rationality of the halogen substitution strategy.</div></div>","PeriodicalId":10088,"journal":{"name":"Chinese Chemical Letters","volume":"37 4","pages":"Article 110755"},"PeriodicalIF":8.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146035379","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chinese Chemical LettersPub Date : 2026-04-01Epub Date: 2025-08-05DOI: 10.1016/j.cclet.2025.111669
Mengjiao Xie , Nadeeshani Nanayakkara , Yanbiao Liu
{"title":"Pulsed electrochemistry for water decontamination: Fundamental principles and environmental application","authors":"Mengjiao Xie , Nadeeshani Nanayakkara , Yanbiao Liu","doi":"10.1016/j.cclet.2025.111669","DOIUrl":"10.1016/j.cclet.2025.111669","url":null,"abstract":"<div><div>Sustainable and efficient solutions are essential to address increasingly critical environmental issues, particularly in the field of pollutant removal and resource recovery. The latest research has shown that pulsed electrochemistry significantly contributes to these goals by precisely altering the local reaction environment, accelerating the reaction kinetics and decreasing the overall energy requirements. However, knowledge gaps exist in dynamic evolution mechanism of electric double layer (EDL) in this technology, and challenges remain toward fully implementation of this promising technology. In this review, the fundamentals of pulsed electrochemistry and its connection to the theoretical models of EDL are comprehensively presented. The critical parameters (<em>e.g.</em>, duty ratio, frequency and waveform) for boosting the performance of the system are systematically discussed and the typical electrochemical reactions that occur with pulsed electrochemistry are outlined. The proposed pulsed electrochemistry methodologies tailored for environmental applications are also reviewed in detail. Finally, future opportunities and challenges of this promising but fledgling field are discussed, with the expectation that this technology offers a route to transform conventional chemical industries into cleaner and more sustainable production.</div></div>","PeriodicalId":10088,"journal":{"name":"Chinese Chemical Letters","volume":"37 4","pages":"Article 111669"},"PeriodicalIF":8.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146035381","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Augmenting heptamethine cyanine photosensitivity while retaining strong fluorescence emission: Forming dye-albumin nanocomplex enables tumor-targeted photodynamic therapy","authors":"Mengxing Liu, Jing Liu, Hongxing Zhang, Lijuan Wang, Jianan Tao, Wei Guo","doi":"10.1016/j.cclet.2025.111141","DOIUrl":"10.1016/j.cclet.2025.111141","url":null,"abstract":"<div><div>In this work, the spin-orbit charge transfer intersystem crossing (SOCT-ISC) mechanism is introduced into the near-infrared and highly photon-capturing heptamethine cyanine (Cy7) class to construct photosensitizer (PS) for photodynamic therapy (PDT) of tumor. The target PS AN<img>Cy7 shows an obviously improved singlet oxygen (<sup>1</sup>O<sub>2</sub>) quantum yield than the Food and Drug Administration (FDA)-approved indocyanine green (ICG) under 750 nm low-power photoirradiation (30 mW/cm<sup>2</sup>) while retaining strong fluorescence at ∼805 nm. Importantly, the PS forms a 2:1 dye-human serum albumin (HSA) nanocomplex, ensuring its strong accumulation and retention at tumor site (up to five days) post intravenous injection. After a single PDT treatment, the nanocomplex almost completely ablates primary tumor while triggering an antitumor immune response to suppress the growth of distant tumors. Overall, the nanocomplex overcomes many shortcomings of clinically used PSs, thus being promising for future clinical translation.</div></div>","PeriodicalId":10088,"journal":{"name":"Chinese Chemical Letters","volume":"37 4","pages":"Article 111141"},"PeriodicalIF":8.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145975311","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chinese Chemical LettersPub Date : 2026-04-01Epub Date: 2025-03-25DOI: 10.1016/j.cclet.2025.111140
Xiaodan Liang , Tong Tong , Caihong Xian , Jiyuan Du , Biying Tan , Liying Wang , Jingyi Hou , Jun Wu
{"title":"Metal-based biomaterials for treating bone diseases","authors":"Xiaodan Liang , Tong Tong , Caihong Xian , Jiyuan Du , Biying Tan , Liying Wang , Jingyi Hou , Jun Wu","doi":"10.1016/j.cclet.2025.111140","DOIUrl":"10.1016/j.cclet.2025.111140","url":null,"abstract":"<div><div>Bone-related diseases resulting from accidents, illnesses, and injuries have become increasingly common in recent years. Treating these conditions poses significant challenges, including prolonged recovery times, high costs, and unpredictable outcomes, which can lead to complications such as infections and reduced muscle strength. Although autologous bone transplantation is regarded as the \"gold standard\" for addressing bone diseases, its application is often limited by complications at the donor site and the risk of infection. This underscores the urgent need to explore alternatives to autogenous bone transplantation. In response, a range of biomaterials for bone repair have been developed, with metal-based biomaterials emerging as effective adjuncts that enhance and optimize the repair and regeneration of bone tissue. These materials can actively influence the bone repair process through mechanisms such as inductive osteogenesis, immunomodulation, and pro-angiogenesis. This review begins by highlighting the biological effects of metal-based biomaterials, followed by a comprehensive overview of their macro- and micro-scale classifications and applications for treating various bone diseases. Finally, the review addresses future directions and challenges associated with the use of metal-based biomaterials in bone repair, aiming to propose promising strategies for the treatment of bone-related diseases.</div></div>","PeriodicalId":10088,"journal":{"name":"Chinese Chemical Letters","volume":"37 4","pages":"Article 111140"},"PeriodicalIF":8.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145975312","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chinese Chemical LettersPub Date : 2026-04-01Epub Date: 2025-03-07DOI: 10.1016/j.cclet.2025.111047
Haolin Zhang , Kai Feng , Guisen Li, Weijiao Chen, Yuan Shao, Jiayu Ding, Mingming Zheng, Kai Yuan, Xiaolian Sun, Peng Yang
{"title":"Carbonic anhydrase IX-targeted SMDCs for cancer precision treatment","authors":"Haolin Zhang , Kai Feng , Guisen Li, Weijiao Chen, Yuan Shao, Jiayu Ding, Mingming Zheng, Kai Yuan, Xiaolian Sun, Peng Yang","doi":"10.1016/j.cclet.2025.111047","DOIUrl":"10.1016/j.cclet.2025.111047","url":null,"abstract":"<div><div>In the process of tumor treatment, chemotherapy drugs have been widely used in clinical practice due to their broad-spectrum and significant therapeutic effects. However, the serious side effects caused by off-target effects also limit the actual efficacy of such drugs in clinical. Here, we developed a series of small molecule-drug conjugates (SMDCs) with carbonic anhydrase IX (CAIX)-targeted unit, which can deliver chemotherapy drugs to CAIX-positive cancer cells and release them in the tumor microenvironment. These SMDCs can quickly captured by the highly expressed CAIX on the tumor membrane, forming a high local concentration difference that allows SMDCs to enter the tumor cells faster. The optimized SMDC (CAIXi-R-HCPT) with ROS-sensitive linker showed higher cytotoxicity than Irinotecan. In MDA-MB-231 solid tumor-bearing mice, CAIXi-R-HCPT showed higher tumor/normal tissue (T/N) ratio than the corresponding SMDC and Irinotecan control and it also exhibited <em>in vivo</em> anti-tumor activity comparable to HCPT at the same dosage, and there was no significant weight loss. These findings emphasize the potential of CAIXi-R-HCPT as a promising anti-cancer SMDC that exhibits targeted delivery, tumor-specific release, and strong anti-tumor effects.</div></div>","PeriodicalId":10088,"journal":{"name":"Chinese Chemical Letters","volume":"37 4","pages":"Article 111047"},"PeriodicalIF":8.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145975314","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}