Article
Biochemistry & Molecular Biology
Zihan Zhang, Panpan Wang, Mengsong Chen, Lu Xie, Xiujuan Zhang, Yefan Shi, Wang Lu, Qiang Zhang, Chunhuan Li
Summary: In this study, two novel cassane diterpenoids (pulchins A and B) were isolated from the medicinal plant Caesaplinia pulcherrima (L.) Sw. Pulchin A exhibited significant antibacterial activity against B. cereus and Staphylococcus aureus. Further investigation revealed that the antibacterial activity of pulchin A against B. cereus may be attributed to its interference with bacterial cell membrane proteins, leading to membrane permeability changes and cell damage or death.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Engineering, Biomedical
Jiu Ge, Mengting Li, Jiahui Fan, Christian Celia, Yijun Xie, Qing Chang, Xiaoyong Deng
Summary: Bacterial infections pose a significant threat to human health, and the emergence of multidrug-resistant bacteria has reduced the effectiveness of antibacterial treatments. In this study, chitosan/silver nanoparticle complexes were developed to inhibit bacterial proliferation and induce membrane damage. The results demonstrated that increasing the chitosan concentration enhanced the antibacterial impact, and the nanoparticles showed broad-spectrum antimicrobial activity. The study provides valuable insights into the development of nano-antibacterial agents as a potential substitute for traditional antibiotics in medical applications.
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
(2024)
Article
Microbiology
Fengyu Guo, Qianping Chen, Qiong Liang, Ming Zhang, Wenxue Chen, Haiming Chen, Yonghuan Yun, Qiuping Zhong, Weijun Chen
Summary: Linalool exhibited strong antibacterial activity against Pseudomonas fluorescens by damaging the cell membrane, disrupting bacterial metabolism and oxidative respiration, inhibiting cellular respiration, and interfering with cellular functions to the extent of causing cell death.
FRONTIERS IN MICROBIOLOGY
(2021)
Article
Food Science & Technology
Yingying Cai, Guangming Zou, Meihua Xi, Yujie Hou, Heyu Shen, Jingfang Ao, Mei Li, Jun Wang, Anwei Luo
Summary: Juglone, a natural antibacterial agent, has the potential to control foodborne L. monocytogenes infections. Our study elucidated the antibacterial mechanism of juglone, which mainly involves membrane damage, cellular dysfunction, and protein destruction or inhibition.
Article
Chemistry, Physical
Junli Liu, Kaitao Zhang, Zhaoyang Gao
Summary: In this study, Ag2S/MoS2/Pal nanocomposites with excellent antibacterial activity were successfully synthesized using a simple method. The nanocomposites showed effective inhibition against Escherichia coli and Staphylococci aureus under different illuminations, achieving rapid bacterial death through physical interaction and photothermal effects.
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
(2022)
Article
Food Science & Technology
Hechao Du, Huibin Chi, Hongliang Yao, Zhaoxin Lu, Xiaomei Bie, Chong Zhang, Haizhen Zhao, Fengxia Lu, Meirong Chen
Summary: The study demonstrated that plantaricin GZ1-27 has potent inhibitory effects on MRSA and revealed its bactericidal mechanism through a series of experiments. In addition, combining with chitosan significantly improves the preservation of meat products.
INTERNATIONAL JOURNAL OF FOOD MICROBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Dalia A. Elsherbiny, Abdelrahman M. Abdelgawad, Mehrez E. El-Naggar, Bahaa A. Hemdan, Samaneh Ghazanfari, Stefan Jockenhoevel, Orlando J. Rojas
Summary: Current research focuses on innovative medical textiles with nanofibrous structure and antibacterial properties to prevent diaper dermatitis. Electrospun nanofibers of cellulose acetate and lignin polymers were used, with a series of new copper complexes synthesized and loaded onto the fibers. The resulting tricomponent bioactive mats showed improved surface morphology and enhanced antibacterial activity against commonly found pathogens.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Article
Biochemistry & Molecular Biology
Guangyao Wang, Dingwen Xiao, Yueguang Fang, Guiling Ning, Junwei Ye
Summary: This study developed nanofibrous membranes with remarkable antibacterial properties using coaxial electrospinning technology. The membranes were applied to facial masks and demonstrated excellent ability to capture airborne particles.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2024)
Article
Nutrition & Dietetics
Ya-Nan Chen, Hai-Lan Li, Jia-Jun Huang, Mei-Jin Li, Tao Liao, Xiao-Yan Zu
Summary: This study evaluated the antimicrobial activities and mechanism of sturgeon spermary protein extracts (SSPE) against Escherichia coli. The results showed that SSPE exhibited bacteriostatic effects on E. coli by destroying the cell membrane and genomic DNA. This suggests that SSPE has the potential to be a natural antiseptic.
FRONTIERS IN NUTRITION
(2022)
Article
Chemistry, Physical
Junli Liu, Zhaoyang Gao, Hui Liu, Lingyan Pang, Xuanmeng He, Aiping Hui, Aiqin Wang
Summary: In this study, Co-doped ZnO nanoparticles were prepared and decorated on palygorskite to enhance its antibacterial properties. The nanocomposites showed excellent antibacterial performance due to the production of superoxide anions and hydroxyl radicals by Co-ZnO, as well as the physical piercing effect of palygorskite on cell surfaces. This result paves the way for future functional clay materials.
APPLIED CLAY SCIENCE
(2021)
Article
Food Science & Technology
Ping Zeng, Qipeng Cheng, Jiangtao Xu, Qi Xu, Yating Xu, Wei Gao, Kwok-Yin Wong, Kin-Fai Chan, Sheng Chen, Lanhua Yi
Summary: In this study, three novel antibacterial peptides were designed and synthesized, among which (3)K(5)K(7)G showed good antibacterial activity against drug-resistant Vibrio strains and could effectively kill Vibrio alginolyticus cells in instant jellyfish. Moreover, (3)K(5)K(7)G exhibited low cytotoxicity to mammalian cells.
Article
Chemistry, Multidisciplinary
Jia Liu, Shuxia Wang, Lei Jiang, Wei Shao
Summary: Novel antimicrobial BC membranes were prepared by covalently grafting kanamycin onto regenerated bacterial cellulose (RBC) membranes. The kanamycin grafted RBC membrane displayed excellent antibacterial activity towards various microorganisms without any kanamycin leaching, and also showed good biocompatibility in MTT assay.
JOURNAL OF INDUSTRIAL AND ENGINEERING CHEMISTRY
(2021)
Review
Biotechnology & Applied Microbiology
Xiaoyu Chen, Yajun Lu, Mengyuan Shan, Hongyuan Zhao, Zhaoxin Lu, Yingjian Lu
Summary: Surfactin, a powerful biosurfactant produced by Bacillus subtilis, has broad-spectrum antimicrobial activities and other biological activities such as antiviral and antiprotozoal activities. It may serve as a promising alternative to antibiotics. This mini-review discusses its chemical structure, antibacterial mechanism, and application in the food industry.
WORLD JOURNAL OF MICROBIOLOGY & BIOTECHNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Deepti Singh, Ananda Guha Majumdar, Sunita Gamre, Mahesh Subramanian
Summary: The study demonstrates that HC induces oxidative stress, membrane damage, and DNA damage in bacterial cells, leading to cell filamentation or breakage, and the damaging effect on the cell membrane can be influenced by external ions. HC pretreatment may sensitize E. coli to antibiotics, suggesting a potential strategy to combat antibiotic resistance.
Review
Biotechnology & Applied Microbiology
Taja Zeleznik Ramuta, Tina Sket, Marjanca Starcic Erjavec, Mateja Erdani Kreft
Summary: The fetal membranes provide a supportive environment for the embryo and fetus and have gained attention for their antimicrobial properties in recent years. Antimicrobial peptides secreted by perinatal derivatives contribute to a healthy pregnancy and the prevention of complications. Research on the antimicrobial properties of fetal membranes and their derivatives has provided valuable insights for potential clinical applications, emphasizing the importance of standardization in preparation, testing methods, in vivo studies, and donor selection criteria.
FRONTIERS IN BIOENGINEERING AND BIOTECHNOLOGY
(2021)
Article
Oncology
Yajing Xing, Weikai Guo, Min Wu, Jiuqing Xie, Dongxia Huang, Pan Hu, Miaoran Zhou, Lin Zhang, Qiansen Zhang, Peili Wang, Xin Wang, Guixue Wang, Huangan Wu, Cili Zhou, Yihua Chen, Mingyao Liu, Zhengfang Yi, Zhenliang Sun
Summary: Researchers have identified a small molecule compound named WK500B that can block the inhibition of BCL6, reactivate target genes, kill DLBCL cells, and display strong anti-tumor effects in animal models. Therefore, WK500B holds promise as an effective orally available therapeutic agent for DLBCL.
Article
Chemistry, Medicinal
Wangrui Jin, Tao Zhang, Wenbo Zhou, Peng He, Yue Sun, Shijia Hu, Huang Chen, Xinglong Ma, Yangrui Peng, Zhengfang Yi, Mingyao Liu, Yihua Chen
Summary: Osteosarcoma, a common malignant bone tumor, has seen little progress in treatment and clinical outcomes due to its heterogeneity and high mutation rate. Targeting STAT3 has shown potential as a feasible therapeutic strategy for osteosarcoma.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Shijia Hu, Yunqi Li, Weiqiong Kan, Tingting Ding, Haijun Gu, Ting Zhang, Zhengfang Yi, Yihua Chen
Summary: A series of diphenyl-N-heteroaromatic compounds were synthesized and evaluated for their anticancer activities. Compound 4b and 4c, optimized from favorable compound 4a, showed more potent antimigratory and antiproliferative activities. The results suggest that compounds 4b and 4c with 1,2,3-triazole scaffold may have potential as potent anticancer agents.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Editorial Material
Oncology
Dazhao Mi, Yuzhan Li, Yihua Chen
Summary: This article provides an overview of the role of SHP2 protein tyrosine phosphatase in cancer-related signaling pathways, as well as the therapeutic strategies targeting SHP2, including PTP inhibitors, allosteric inhibitors, and SHP2-targeting PROTACs. The benefits and limitations of these strategies are discussed. The opportunities and challenges of targeting SHP2 are also presented.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2023)
Article
Oncology
Luzhen Wang, Dazhao Mi, Jinhui Hu, Wenjing Liu, Yi Zhang, Chunyan Wang, Yihua Chen, Ceshi Chen
Summary: TNBC is a highly malignant tumor with poor prognosis. This study identified DZ-514 as a potent compound with high toxicity against TNBC cells, independent of BCL6 inhibition. DZ-514 reduced cell viability, inhibited cell cycle progression, and induced caspase-independent cell death in TNBC cells. Importantly, DZ-514-induced vacuoles were derived from macropinosomes rather than autophagosomes.
Article
Oncology
Huang Chen, Wenbo Zhou, Aiwu Bian, Qiansen Zhang, Ying Miao, Xuan Yin, Jiangnan Ye, Shifen Xu, Chaowen Ti, Zhenliang Sun, Jianghua Zheng, Yihua Chen, Mingyao Liu, Zhengfang Yi
Summary: This study identifies a novel drug called WB436B as a selective STAT3 inhibitor for the treatment of pancreatic cancer. WB436B effectively inhibits tumor growth and metastasis, providing hope for the treatment of pancreatic cancer.
CLINICAL CANCER RESEARCH
(2023)
Article
Oncology
Yuzhu Zhang, Jing Chen, Dazhao Mi, Jun Ling, Huachao Li, Peng He, Ning Liu, Qianjun Chen, Yihua Chen, Luqi Huang
Summary: In this study, the natural product harmine was identified as a potential compound for treating triple-negative breast cancer (TNBC). The compound was further modified and optimized to obtain a lead compound, YH677, which showed strong anti-proliferative and anti-migratory effects in vitro and suppressed breast cancer growth and metastasis in vivo. Mechanistic studies revealed that YH677 inhibits the expansion of cancer stem cells by regulating the TGF beta/Smad signaling pathway.
Correction
Oncology
Yuzhu Zhang, Jing Chen, Dazhao Mi, Jun Ling, Huachao Li, Peng He, Ning Liu, Qianjun Chen, Yihua Chen, Luqi Huang
Article
Chemistry, Medicinal
Peng He, Juanjuan Feng, Xinting Xia, Yue Sun, Jia He, Tian Guan, Yangrui Peng, Xueli Zhang, Mingyao Liu, Xiufeng Pang, Yihua Chen
Summary: HP661 is a highly effective OXPHOS inhibitor that can inhibit mitochondrial oxygen consumption in high OXPHOS lung cancer cells. It also shows significant sensitivity in MEK inhibitor-resistant lung cancer cells and has therapeutic efficacy against high OXPHOS lung cancer.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Jia He, Luzhen Wang, DaZhao Mi, Tian Guan, Wenjing Liu, Peng He, Haijun Gu, Yuzhan Li, Yangrui Peng, Ai-Qun Jia, Ceshi Chen, Yihua Chen
Summary: JH530 is a drug that can induce cell death in triple-negative breast cancer cells and has shown significant suppression of tumor growth in vitro and in vivo.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Medicine, Research & Experimental
Yali Wang, Wenbo Zhou, Jianfeng Chen, Jinghong Chen, Peng Deng, Huang Chen, Yichen Sun, Zhaoliang Yu, Diwen Pang, Lizhen Liu, Peili Wang, Jing Han Hong, Bin Tean Teh, Huiqiang Huang, Wenyu Li, Zhengfang Yi, Soon Thye Lim, Yihua Chen, Choon Kiat Ong, Mingyao Liu, Jing Tan
Summary: A new and potent STAT3 inhibitor, WB737, has been developed as a potential therapeutic option for NKTL. It selectively inhibits NKTL with STAT3-activating mutations and suppresses both canonical and noncanonical STAT3 signaling. WB737 shows significant antitumor effects with minimal toxicity, providing a promising strategy for treating NKTL patients.
Article
Medicine, Research & Experimental
Lin Zhang, Min Wu, Weikai Guo, Shuangshuang Zhu, Shen Li, Shiyi Lv, Yan Li, Layang Liu, Yajing Xing, Huang Chen, Mingyao Liu, Shihong Peng, Yihua Chen, Zhengfang Yi
Summary: BCL6 is a transcriptional repressor that plays a role in immune cell differentiation, DNA damage repair, cell cycle, and apoptosis. A small molecule compound called WK499 has been identified as a inhibitor of BCL6, which inhibits the proliferation of AML cells and enhances the sensitivity of AML to chemotherapy. WK499 achieves this by disrupting the interactions between BCL6 and its corepressor proteins, leading to changes in downstream genes and induction of cell cycle arrest and apoptosis.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Review
Chemistry, Medicinal
Dazhao Mi, Yuzhan Li, Haijun Gu, Yan Li, Yihua Chen
Summary: Proteolysis-targeting chimeras (PROTACs) have gained significant attention as an emerging modality in drug discovery. After over 20 years of development, accumulated studies have shown that PROTACs offer unique advantages over traditional therapy in terms of target scope, efficacy, and overcoming drug resistance. However, the limited availability of E3 ligases, essential components of PROTACs, poses a challenge for their design. This review provides a systematic summary of the current status of E3 ligases and corresponding ligands for PROTACs design, including their discovery history, design principles, application benefits, and potential limitations. The prospects and future directions in this field are also briefly discussed.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Chemistry, Medicinal
Weikai Guo, Manjie Wang, Zhengfan Yang, Danyang Liu, Borui Ma, Yanqun Zhao, Yihua Chen, Yanzhong Hu
Summary: This article comprehensively reviews the structure, physiological functions, and recent progress of GRP78, and discusses the merits and demerits of GRP78 inhibitors as well as novel strategies for drug discovery targeting GRP78. The feasibility of PROTACs and covalent inhibition as new opportunities for targeted antitumor therapy are also explored.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Peng He, Ying Miao, Yue Sun, Aiwu Bian, Wangrui Jin, Jiangnan Ye, Huang Chen, Jia He, Yangrui Peng, Haijun Gu, Mingyao Liu, Zhengfang Yi, Yihua Chen
Summary: This study describes the design, synthesis, and structure-activity relationship studies of triaromatic heterocyclic derivatives as potent dual phosphorylation STAT3 inhibitors. The best compound 3h (HP590) was discovered with high inhibitory activity against p-Tyr(705) and p-Ser(727), resulting in the growth inhibition of gastric cancer both in vitro and in vivo.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)