Article
Chemistry, Multidisciplinary
Jiaqi Guo, Weiyi Tan, Hongjian He, Bing Xu
Summary: This study demonstrates that diglycine-activated succinic esters can significantly enhance the cellular uptake of supramolecular assemblies or prodrugs by converting nanofibers into nanoparticles through autohydrolysis. The autohydrolysis of diglycine-activated succinic esters and drug conjugates also restores the efficacy of the drugs. The U-turn conformation of diglycine promotes intramolecular hydrolysis of diglycine-activated succinic esters, providing a nonenzymatic bond cleavage approach for effective intracellular targeting.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Multidisciplinary
Lingpu Zhang, Lin Zhu, Lin Tang, Jiayi Xie, Yajuan Gao, Changyuan Yu, Kun Shang, Hongbin Han, Chaoyong Liu, Yunfeng Lu
Summary: This study reports a prodrug that releases Camptothecin (CPT) in response to glutathione (GSH), aiming to improve its bioavailability and reduce systemic toxicity. By incorporating the prodrug into nanoparticles, it enhances tumor targeting ability and therapeutic efficacy of CPT, as well as promotes immune cell activation and tumor infiltration.
Article
Materials Science, Biomaterials
Peng Liu, Weifei Zhang, Jiapeng Deng, Yien Zheng, Jian Weng, Fei Yu, Deli Wang, Ming Zheng, Bin Kang, Hui Zeng
Summary: A chain-shattering polymeric SO2 prodrug micelle system was developed for effective SO2 based gas therapy. The system enables efficient delivery and on-demand stimuli triggered release at tumor sites, with low tissue toxicity.
JOURNAL OF MATERIALS CHEMISTRY B
(2022)
Article
Pharmacology & Pharmacy
Huiyun Zhang, Shunru Wei, Yu Zhang, Anran Pan, Michael Adu-Frimpong, Congyong Sun, Gang Qi
Summary: In this study, a small molecule prodrug was integrated into PEGylated liposome to enhance the efficiency of periplocymarin in vivo. The PEGylated liposome showed better stability, sustained drug release kinetics, and enhanced cellular uptake compared to the self-assembling nano-prodrug. This study highlights the potential of PEGylated liposome as a promising strategy for delivering periplocymarin in clinical applications.
Article
Nanoscience & Nanotechnology
Ankan Kumar Sarkar, Santanu Shaw, Himali Arora, Pankaj Seth, Nikhil R. R. Jana
Summary: Subcellular targeting of drugs can be enhanced by designing nanocarriers for direct cell membrane translocation, bypassing endosomal/lysosomal trafficking. This approach allows rapid and extensive delivery of drugs to the cell nucleus within a few minutes, without undergoing vesicular coating and lysosomal trafficking. This nonendocytic uptake method provides a potential strategy for nanocarrier-based subcellular targeting of drugs for more effective therapy.
ACS APPLIED MATERIALS & INTERFACES
(2023)
Article
Polymer Science
Yuxin Wan, Zhenze Xie, Mingjie Wang, Yuelian Liu, Mubin Zheng, Dong Xu, Chang Du
Summary: Osteosarcoma is a common bone malignancy in children and adolescent. High-dose chemotherapy often fails due to serious side effects and multi-drug resistance. Curcumin has shown selective cytotoxicity towards osteosarcoma cells while being less toxic to healthy osteoblasts, but its delivery poses challenges. This study developed a co-polymer-Cur prodrug with improved solubility and stability, and demonstrated its potential in inhibiting osteosarcoma cell proliferation and promoting apoptosis. The prodrug showed no systemic toxicity and suppressed osteosarcoma growth in vivo, providing a new perspective for formulation design of controlled release of insoluble and unstable anticancer agents.
EUROPEAN POLYMER JOURNAL
(2023)
Article
Biophysics
Yanan Wang, Yanan Li, Lingyun He, Baiping Mao, Sian Chen, Vanessa Martinez, Xiaoling Guo, Xian Shen, Baohua Liu, Chao Li
Summary: The study found that the esterified alginate-curcumin conjugate exhibited effective anti-inflammatory effects in Raw 264.7 cells, and after oral administration in animals, the majority reached the colon rapidly and released curcumin, effectively reducing colonic inflammation and tissue damage. The curcumin release triggered by commensal flora shows great potential for ulcerative colitis treatment.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2021)
Article
Nanoscience & Nanotechnology
Bing Xu, Mengmeng Yan, Fei Zhou, Desheng Cai, Wenbo Guo, Xiaohui Jia, Runping Liu, Tao Ma, Tong Li, Feng Gao, Penglong Wang, Haimin Lei
Summary: The study developed self-assembled nanoparticles that respond to PSMA and esterase, leading to efficient delivery of CPT for cancer therapy. These nanoparticles exhibited programmable release of CPT at the tumor site, providing excellent cytotoxic selectivity and antitumor activity against PSMA-expressing cells, demonstrating a promising strategy for efficient drug delivery.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2021)
Article
Chemistry, Physical
Si Xu, Shanshan Liang, Bing Wang, Jiali Wang, Meng Wang, Lingna Zheng, Hao Fang, Tingfeng Zhang, Yi Bi, Weiyue Feng
Summary: Pre-coating nanomaterials (NMs) with a protein corona is an effective strategy to reduce non-specific absorption of serum proteins while maintaining targeting specificity. This study presents a new approach using lipoic acid-terminated polyethylene glycol and transferrin bi-functionalized MoS2 nanosheets (Tf@MoS2-PEG NSs) to enhance cellular uptake. The results demonstrate that Tf coating enhances the cellular uptake of MoS2 NSs, with a broader range of uptake amounts observed in HepG2 cells compared to BSA-coated MoS2 NSs.
Article
Chemistry, Analytical
Dheeraj K. Agrohia, Peidong Wu, Uyen Huynh, S. Thayumanavan, Richard W. Vachet
Summary: This article introduces a metal-coded mass tagging approach that enables the multiplexed quantification of the PNC uptake in cells using mass spectrometry. The conjugation of different metals to the PNCs allows the simultaneous multiplexed analysis of multiple distinct PNCs, which should improve the design and optimization of PNCs.
ANALYTICAL CHEMISTRY
(2022)
Article
Medicine, Research & Experimental
Tao Lu, Dieter Haemmerich, Hui Liu, Ann L. B. Seynhaeve, Gerard C. van Rhoon, Adriaan B. Houtsmuller, Timo L. M. ten Hagen
Summary: The study demonstrates that IDA is taken up over 10 times more rapidly by cancer cells than DXR in vitro, leading to 4-times higher whole tumor drug uptake. IDA-SDDS shows improved intratumoral drug distribution and superior tumor response compared to DXR-SDDS at the same dose, suggesting a shift in selection of chemotherapeutics based on properties of a chemotherapeutic in the context of nanoparticle and delivery mode is urgently needed to maximize therapeutic efficacy.
Article
Engineering, Biomedical
Xiaobei Huang, Ning Mu, Yuanfu Ding, Hou Wang Lam, Ludan Yue, Cheng Gao, Tunan Chen, Zhen Yuan, Ruibing Wang
Summary: In this study, an innovative nanomedicine for combined chemo-photodynamic therapy of melanoma was developed, which improved cellular uptake through targeted drug delivery and the charge-reversal phenomenon.
ACTA BIOMATERIALIA
(2022)
Article
Materials Science, Biomaterials
Aparna Loecher, Michael Bruyns-Haylett, Pedro J. Ballester, Salvador Borros, Nuria Oliva
Summary: The delivery efficiency of genetic material to cells is limited by the carrier system. Poly-beta-amino esters (pBAEs) are promising polymer-based vectors that can improve cell membrane uptake and gene delivery. However, the optimal formulation for high uptake in a new cell line requires trial and error. Therefore, machine learning models, such as gradient-boosted trees and neural networks, were trained to predict cellular internalisation of pBAE polyplexes.
BIOMATERIALS SCIENCE
(2023)
Article
Materials Science, Multidisciplinary
Yingnan Zhang, Changhao Fang, Wildemar S. P. Carvalho, Yongfeng Gao, Michael J. Serpe
Summary: The light- and temperature-responsive poly(N-isopropylacrylamide-co-nitrobenzyl methacrylate) microgels demonstrated efficient release of fluorescein through UV irradiation-induced cleavage and heating-induced deswelling, showing potential applications in triggered cargo release systems.
ACS APPLIED POLYMER MATERIALS
(2021)
Article
Chemistry, Applied
Jie Chen, Ming-Shun Mei, Yongbin Xu, Si Xiong, Yonglin Zhao, Ruimin Liu, Songshan Shi, Huijun Wang, Shunchun Wang
Summary: A homogalacturonan from Ficus pumila L. have anti-diabetic activity, which is influenced by the degree of methyl-esterification. The hypoglycemic effect increases and then decreases with the degree of methyl-esterification, with the most pronounced effect at DM54. The degree of methyl-esterification may regulate activity through altering cellular uptake. Additionally, different cellular uptake mechanisms are involved in the hypoglycemic activity.
CARBOHYDRATE POLYMERS
(2022)
Article
Pharmacology & Pharmacy
Yushu Huang, Wanli Zhang, Yanyun Xu, Shulei Zhu, Yanqian Wu, Tiandong Chen, Yi Xiao, Wei Lu, Xiongwen Zhang, Jiahui Yu
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2020)
Article
Chemistry, Medicinal
Shulei Zhu, Qianqian Shen, Yinglei Gao, Lei Wang, Yanfen Fang, Yi Chen, Wei Lu
JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Biochemistry & Molecular Biology
Ying Huang, Chen Jin, Jiahui Yu, Lei Wang, Wei Lu
BIOORGANIC CHEMISTRY
(2020)
Article
Chemistry, Organic
Pingxuan Shao, Wei Lu, Lei Wang
CURRENT ORGANIC SYNTHESIS
(2020)
Article
Biophysics
Yang He, Yanyun Xu, Yushu Huang, Hao Quang, Xiaoyan Xia, Hongbo Zhao, Yi Xiao, Wei Lu, Jiahui Yu
Summary: In this study, a pH and redox dual-responsive polymer prodrug was developed for the efficient delivery of drugs to metastatic breast cancer cells, leading to inhibition of cancer metastasis to the lung. The nanocapsules showed enhanced drug release under low pH and high redox conditions, as well as active targeting and selectivity to breast cancer cells. Furthermore, the nanocapsules significantly inhibited cell migration and invasion, and suppressed lung metastasis with minimal toxicity.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2022)
Article
Chemistry, Applied
Shulei Zhu, Yingxin Lu, Jiyu Jin, Jiahui Yu, Wei Lu
Summary: A fluorescent probe based on an HSP90 inhibitor was synthesized in this study, showing potential for selective tumor targeting and early diagnosis.
Article
Chemistry, Medicinal
Zhiyang Cheng, Ying Huang, Qianqian Shen, Yangrong Zhao, Lei Wang, Jiahui Yu, Wei Lu
Summary: The study presented an albumin-based drug delivery system, synthesized an antitumor prodrug Mal-glu-CPTS0001, and demonstrated its in vivo antitumor effects. The prodrug covalently binds to plasma albumin, releases the drug in tumors, and achieves reduced toxicity and enhanced selectivity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Ying Huang, Lei Wang, Zhiyang Cheng, Biyu Yang, Jiahui Yu, Yi Chen, Wei Lu
Summary: The novel Mal-glu-SN38 prodrug showed selective delivery of SN38 to tumour sites and enhanced efficacy. With slower plasma clearance, increased drug exposure over time, and enhanced accumulation at the tumour site, Mal-glu-SN38 significantly delayed tumour growth after multiple doses, leading to an impressive reduction or even disappearance of tumours without observable side effects in 67% of mice.
JOURNAL OF CONTROLLED RELEASE
(2021)
Article
Biochemistry & Molecular Biology
Shuting Wang, Shulei Zhu, Yawen Tanzeng, Yuexing Zhang, Chuchu Li, Mingliang Ma, Wei Lu
Summary: A series of novel near-infrared fluorescent molecules were designed with a compact donor-acceptor-donor architecture, exhibiting significant variations in fluorescence intensity and viscosity sensitivity in different solvent polarities. Among them, one molecule M-3 showed a 3-fold increase in emission intensity in a high viscosity solvent system and a 4-fold increase in fluorescence intensity in the presence of proteins, demonstrating superior environmental sensitivity and potential for optical imaging probe development.
Article
Biochemistry & Molecular Biology
Yingxin Lu, Danwen Sun, Donghuai Xiao, Yingying Shao, Mingbo Su, Yubo Zhou, Jia Li, Shulei Zhu, Wei Lu
Summary: Novel CRBN-recruiting HDAC PROTACs were designed and synthesized, with 21a showing excellent activity and demonstrating the potential of the benzyl alcohol linker. These PROTACs exhibited outstanding inhibitory activity on different HDAC classes and showed better anti-proliferative activity on the MM.1S cell line.
Article
Biochemistry & Molecular Biology
Tingting He, Shulei Zhu, Wei Lu
Summary: Heat shock protein 90 (HSP90) is a promising target for anticancer drugs. In this study, a series of novel HSP90 inhibitors was synthesized and compound 6u exhibited the most potent anti-proliferative activity, particularly in Capan-1 cell line. Molecular modeling studies also confirmed the interaction mechanism between 6u and HSP90, suggesting it as a potential candidate for further research.
MOLECULAR DIVERSITY
(2023)
Article
Biochemistry & Molecular Biology
Longjun Ma, Yan Zhou, Dehua Yang, Ming-Wei Wang, Wei Lu, Jiyu Jin
Summary: Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, all containing a pyridine group, were synthesized to investigate their androgen receptor antagonistic activities. Among them, compounds 6a/6c/7g/19a/19b showed remarkable antagonistic activity against the androgen receptor, comparable to or even surpassing enzalutamide. Additionally, compounds 19a and 19b exhibited superior antiproliferative activity compared to enzalutamide in prostate cancer cells. These findings suggest that compound 19a holds promising potential as a novel AR antagonist.
Article
Biochemistry & Molecular Biology
Mengyuan Ding, Yingying Shao, Danwen Sun, Suorina Meng, Yi Zang, Yubo Zhou, Jia Li, Wei Lu, Shulei Zhu
Summary: This study designed and synthesized a series of small molecule BRD4 PROTACs, among which 8b could effectively degrade BRD4 and has the potential for treating related diseases such as leukemia, multiple myeloma, and pulmonary fibrosis.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Shulei Zhu, Jieyu Liu, Donghuai Xiao, Peipei Wang, Jingkun Ma, Xiaobei Hu, Jingfeng Fu, Yubo Zhou, Jia Li, Wei Lu
Summary: This study reports a novel Wee1 degrader based on PROTAC technology, which effectively degrades cellular Wee1 protein and has potential applications in cancer therapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Zhiyang Cheng, Ying Huang, Pingxuan Shao, Lei Wang, Shulei Zhu, Jiahui Yu, Wei Lu
Summary: Stimulus-responsive albumin-based prodrugs offer a promising drug delivery strategy for targeted and controlled release in tumor microenvironments, with hypoxia-activated Mal-azoExatecan showing potential for specific tumor targeting and release control.
