Article
Biochemistry & Molecular Biology
Laura Ortiz-Miravalles, Manuel Sanchez-Angulo, Jesus M. Sanz, Beatriz Maestro
Summary: A collection of 1200 compounds from a repurposing drugs library was screened for their antimicrobial effects against Streptococcus pneumoniae. After four rounds of screening, seven compounds were selected and found to inhibit pneumococcal growth and reduce bacterial viability by 90.0% to 99.9% at a concentration of 25 mu M. All compounds, except one, also increased bacterial membrane permeability and shared a common chemical structure. These findings offer new possibilities for combating pneumococcal diseases through drug repositioning and provide insights for the design of membrane-targeted antimicrobials.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Correction
Chemistry, Inorganic & Nuclear
M. Zalas, B. Gierczyk, M. Klein, K. Siuzdak, T. Pedzinski, T. Luczak
Summary: The authors of the corrected paper identified inappropriate experimental conditions in the original study, leading to inaccurate results. They repeated the experiments under more suitable conditions, obtaining more detailed data on the properties of the B1 dye. The authors issued a sincere apology to the readers and co-authors for any inconvenience caused by the errors.
Article
Chemistry, Medicinal
Jing Liang, Dejuan Sun, Yueying Yang, Mingxue Li, Hua Li, Lixia Chen
Summary: This review explores the clinical potential of organometallic compounds as antimicrobial agents, summarizing common scaffolds and discussing therapeutic targets and risks to be aware of in future studies.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Yongzhi Chen, Hongxia Li, Jiayong Liu, Rongcui Zhong, Haizhou Li, Shanfang Fang, Shouping Liu, Shuimu Lin
Summary: The emergence of bacterial multidrug resistance and the lack of new antimicrobial agents have led to the urgent need for the discovery and development of novel antibacterials. Antimicrobial peptidomimetics have shown promise in overcoming antibiotic resistance and are effective in rapidly killing bacteria without inducing resistance. Specific compounds have demonstrated potent activity against Gram-positive bacteria, low toxicity to mammalian cells, good stability, and high efficacy in treating bacterial infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Rongcui Zhong, Haizhou Li, Hongxia Li, Shanfang Fang, Jiayong Liu, Yongzhi Chen, Shouping Liu, Shuimu Lin
Summary: Compound 25, a newly designed amphiphilic coumarin derivative, showed potent antibacterial activity against Gram-positive bacteria, including MRSA, with low hemolytic activity and toxicity. It can quickly kill bacteria by disrupting cell membranes and demonstrated excellent efficacy in a murine corneal infection caused by Staphylococcus aureus. This suggests that compound 25 has great potential as a potent antimicrobial agent for treating drug-resistant Gram-positive bacterial infections.
ACS INFECTIOUS DISEASES
(2021)
Article
Chemistry, Multidisciplinary
Maochao Zheng, Xiaolei Wu, Chao Lu, Wancong Zhang, Shijie Tang, Ying Luo, Daojun Liu
Summary: The development of alternative antimicrobial therapeutics is needed due to the emergence of antibiotic resistance in bacterial pathogens. Polypept(o)ide-based bactericides, which mimic antimicrobial host defense peptides, have shown promise in the treatment of antibiotic-resistant and recurring infections. This review summarizes recent advances in membrane-active polypept(o)ide-based bactericides, focusing on their ability to disrupt bacterial cell walls/membranes and combat acquired antibiotic resistance and biofilm formation.
MATERIALS TODAY CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Jia Li, Leli Zeng, Zheng Wang, Hengxing Chen, Shuo Fang, Jinquan Wang, Chao-Yun Cai, Enming Xing, Xinxing Liao, Zhi-Wei Li, Charles R. Ashby, Zhe-Sheng Chen, Hui Chao, Yihang Pan
Summary: RuZ, a cycloruthenated complex, self-assembles into nanoaggregates in cell culture medium, leading to high intracellular concentrations in multi-drug resistant (MDR) cancer cells. It decreases oxygen consumption, inhibits glycolysis, lowers ATP levels, increases retention in MDR cells, induces oxidative stress and apoptosis. Proteomic analysis shows RuZ decreases glycolysis and mitochondrial respiration proteins while increasing apoptosis-related proteins. It inhibits proliferation of 35 cancer cell lines, including drug-resistant ones, and is effective in doxorubicin-resistant mouse tumor xenografts.
ADVANCED MATERIALS
(2022)
Article
Chemistry, Multidisciplinary
Mirela Mihaila, Camelia Mia Hotnog, Marinela Bostan, Alexandra Cristina Munteanu, Ileana Adela Vacaroiu, Lorelei Irina Brasoveanu, Valentina Uivarosi
Summary: Our study focused on the anticancer activity of several ruthenium (Ru) complexes with quinolone antibiotics in colon tumor cell cultures. The results showed dose-dependent increased levels of cell lysis and induction of apoptosis in LoVo cancer cells treated with the Ru(III) complexes. Additionally, a major decrease in cell proliferation, with a G0/G1 cell arrest and modulation of cell cycle phases, was observed, indicating the potential for the Ru(III) complexes in future chemotherapeutic approaches.
APPLIED SCIENCES-BASEL
(2021)
Review
Nursing
Pheona van Huizen, Lisa Kuhn, Philip L. Russo, Clifford J. Connell
Summary: Nurses play a crucial role in antimicrobial stewardship, yet there is limited research on best practices for preparing, administering, and disposing of intravenous antibiotics. Support through education and evidence-based guidelines is needed to enhance nurses' role in antimicrobial stewardship.
INTERNATIONAL JOURNAL OF NURSING STUDIES
(2021)
Review
Biotechnology & Applied Microbiology
Anton Du Preez van Staden, Winschau F. van Zyl, Marla Trindade, Leon M. T. Dicks, Carine Smith
Summary: Lanthipeptides are a class of ribosomally synthesized and posttranslationally modified peptides, with diverse modifications that offer bioactive properties for combatting various diseases. Novel bioactive lanthipeptides can be identified through genome mining tools and accelerated through rapid screening and heterologous expression technologies.
APPLIED AND ENVIRONMENTAL MICROBIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Ran Tao, Yin Lu, Wubing Xia, Changwei Zhang, Chengzhang Wang
Summary: This study successfully prepared a ruthenium coordination polymer composite with chitosan quaternary ammonium polymers and shikimic acid. The composite showed good antibacterial properties, with a strong inhibitory effect against S. aureus and the ability to disrupt their biofilm formation. Further mechanism studies revealed that the composite influenced the cell membrane integrity and intracellular Ca2+ levels of S. aureus.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Editorial Material
Microbiology
Stephanie L. L. Egge, James S. S. Lewis, Morgan Hakki
Summary: Multidrug-resistant/extensively drug-resistant (MDR/XDR) Pseudomonas aeruginosa (PA) strains, especially those producing New Delhi metallo-beta-lactamase (NDM), pose a significant challenge in terms of limited treatment options. However, this case study supports the use of cefepime-zidebactam for disseminated infections caused by NDM-producing XDR PA, pending further clinical studies. It is important to test susceptibilities and consider alternative regimens for isolates with alternative metallo-beta-lactamases (MBLs) or increased efflux pump expression, as in vitro data suggest reduced susceptibility to cefepime-zidebactam.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2023)
Article
Pharmacology & Pharmacy
Raphaelle Youf, Adeel Nasir, Mareike Mueller, Franck Thetiot, Tanguy Haute, Rosy Ghanem, Ulrich Jonas, Holger Schoenherr, Gilles Lemercier, Tristan Montier, Tony Le Gall
Summary: Antimicrobial photodynamic therapy (aPDT) is a treatment method that relies on various parameters. In this study, the application of Ruthenium(II) polypyridyl ([Ru(II)]) complexes in the airways of Cystic Fibrosis (CF) patients was investigated, and the influence of different parameters on their properties was studied. The results provide significant evidence for the clinical relevance of [Ru(II)]-based aPDT in CF lung airways.
Review
Chemistry, Physical
Srikanth Gatadi, Y. Madhavi, Srinivas Nanduri
Summary: The rise in drug resistance to conventional antimicrobial agents has become a major healthcare threat globally, while the development of nanoparticle drug conjugates shows promising potential in overcoming challenges posed by traditional medications. Potential multi-functional nanoparticle drug conjugates could revolutionize clinical medicine and play a crucial role in reducing disease burden.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Multidisciplinary
Ting-Ya Li, Shao-Dong Su, Yu-Ying Yang, Yong He, Han Liu, Xin-Tao Wu, Tian-Lu Sheng
Summary: In this study, diruthenium-based cyanido-bridged asymmetrical compounds were used to investigate the electron transfer process. A series of new trinuclear complexes were synthesized and characterized, and their electron transfer properties were analyzed through UV-vis-NIR spectroscopy. The results show that increasing the electron-accepting capability of the electron acceptor is more effective in decreasing the electron transfer energy.
CRYSTAL GROWTH & DESIGN
(2023)
Article
Chemistry, Inorganic & Nuclear
Qin Zhang, Yanshi Xiong, Jianxin Cheng, Yanhui Tan, Xiangwen Liao, Jintao Wang
Summary: Four new ruthenium polypyridine complexes modified with glycyrrhetinic acid derivatives were designed and synthesized, among which Ru2 showed strong antimicrobial activity against Staphylococcus aureus with minimal toxicity to mammalian erythrocytes. The membrane-compromising action mode was suggested as the potential antibactericidal mechanism, and synergism with common antibiotics was observed. In vivo studies demonstrated that Ru2 effectively promoted wound healing in mice infected with S. aureus, indicating its promising potential as an antibacterial agent.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Applied
Yuanyuan Ma, Ming Wei, Xuerong Wang, Li Jiang, Yanshi Xiong, Jianxin Cheng, Yanhui Tan, Xiangwen Liao, Jintao Wang
Summary: In this study, three new ruthenium (II) complexes were designed and synthesized, and their antibacterial activities against Staphylococcus aureus were evaluated. Among them, Ru-2 exhibited the best bacteriostatic and bactericidal effects, as well as the ability to prevent bacterial resistance development. Furthermore, Ru-2 was shown to effectively inhibit bacterial growth and promote wound healing in vivo.
APPLIED ORGANOMETALLIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Liqiang Wang, Lianghong Liu, Xuerong Wang, Yanhui Tan, Xuemin Duan, Chunyan Zhang, Jianxin Cheng, Yanshi Xiong, Guijuan Jiang, Jintao Wang, Xiangwen Liao
Summary: This study designed and synthesized four biphenyl-based antibacterial ruthenium complexes that targeted membrane integrity to mimic the effects of antimicrobial peptides. In vitro screenings demonstrated that these complexes effectively inhibited the growth of Staphylococcus aureus, and also inhibited biofilm formation and hemolysis activity. Furthermore, the combination use of these complexes with traditional antibiotics showed a synergistic effect. In a mouse model, one of the complexes, Ru(II)-1, exhibited significant antibacterial efficacy against S. aureus and showed low toxicity to mouse tissue.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Runbin Wang, Ming Wei, Xuerong Wang, Yushou Chen, Yanshi Xiong, Jianxin Cheng, Yanhui Tan, Xiangwen Liao, Jintao Wang
Summary: Four new ruthenium polypyridyl complexes were synthesized and tested for their antibacterial activity against Staphylococcus aureus. Ru(II)-3 showed significant antibacterial effect, could quickly kill bacteria and inhibit biofilm formation. It also enhanced the susceptibility of S. aureus to different antibiotics and showed no cytotoxicity to mammalian erythrocytes.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Li Jiang, Yuanyuan Ma, Yanshi Xiong, Yanhui Tan, Xuemin Duan, Xiangwen Liao, Jintao Wang
Summary: This study synthesized three new Ru complexes and found that Ru-3 exhibited excellent antimicrobial activity against Staphylococcus aureus with low toxicity to mammalian cells. Furthermore, Ru-3 showed synergistic effects with common antibiotics on Staphylococcus aureus and promoted wound healing in infected mice.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Runbin Wang, Xiaomin Zhou, Jingjing Chen, Yushou Chen, Yanshi Xiong, Xuemin Duan, Xiangwen Liao, Jintao Wang
Summary: Four ruthenium polypyridyl complexes with prenyl groups were synthesized and characterized. Among them, Ru(II)-2 showed the best antibacterial activity against Staphylococcus aureus, with a minimum inhibition concentration (MIC) value of 0.5 μg/mL. It could quickly kill the bacteria and inhibit biofilm formation. The antibacterial mechanism of Ru(II)-2 may be related to depolarization of the cell membrane and generation of reactive oxygen species.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Medicinal
Jing Wang, Yun Song, Ziying Huang, Wenjing Lin, Guangying Yu, Yanshi Xiong, Guijuan Jiang, Yanhui Tan, Jintao Wang, Xiangwen Liao
Summary: This study successfully developed a Ru-based metalloantibiotic, Ru1, which exhibited remarkable bactericidal activity and attenuated bacterial virulence. It can effectively overcome the antibiotic resistance in Staphylococcus aureus.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Yafeng Liu, Chenxi Jiang, Liang Peng, Zhimin Li, Jintao Wang, Xiangwen Liao, Wenying Guo
Summary: This study found that metal complexes in Radix scutellariae (Huangqin) have antibacterial activity. Baicalin, oroxindin, and scutellarin in Huangqin function as ligands with Mn2+ to form complexes, enhancing the antibacterial activity of the aqueous extract. The baicalin-manganese complex can alter the morphological structure of bacteria, disrupt the integrity of their cell membrane and wall, and cause the production of reactive oxygen species. Additionally, the complex can reverse Staphylococcus aureus resistance to amikacin and azithromycin.
INORGANIC CHEMISTRY FRONTIERS
(2023)
Article
Chemistry, Inorganic & Nuclear
Hai-Yan Huang, Pei Wang, Wei Deng, Li-Xin Dou, Xiang-Wen Liao, Jin-Tao Wang, Xue-Min Duan, Ru-Jian Yu, Yan-Shi Xiong
Summary: Antibiotic abuse has led to the emergence of drug-resistant bacteria, posing a threat to human health. In this study, ruthenium complexes modified with coumarin were synthesized and evaluated for their antibacterial activities against Staphylococcus aureus. Among them, Ru(II)-1 exhibited the best antibacterial activity and could effectively inhibit biofilm formation and the development of drug-resistant bacteria. Mechanism studies suggested that Ru(II)-1 targeted the bacterial cell membrane, inducing oxidative stress and ultimately leading to bacterial death. In vivo tests further demonstrated the potential of Ru(II)-1 in combating S. aureus infection.
DALTON TRANSACTIONS
(2023)
Article
Chemistry, Inorganic & Nuclear
Pei Wang, Hai-Yan Huang, Li-Xin Dou, Wei Deng, Jin-Tao Wang, Xiang-Wen Liao, Ru-Jian Yu, Xue-Min Duan, Yan-Shi Xiong
Summary: Bacterial infection is a serious public health problem that harms human health and is costly. The misuse and overuse of antibiotics have resulted in drug resistance. Therefore, there is an urgent need to develop new antimicrobial agents to address this issue.
DALTON TRANSACTIONS
(2023)
Article
Biochemistry & Molecular Biology
Li Jiang, Yuanyuan Ma, Yiman Chen, Mengcheng Cai, Zhixing Wu, Yanshi Xiong, Xuemin Duan, Xiangwen Liao, Jintao Wang
Summary: In this study, three new Ru(ii) complexes were successfully synthesized and characterized. Among them, Ru-1 showed excellent antimicrobial activity against Staphylococcus aureus, with rapid bactericidal activity and low toxicity. Furthermore, Ru-1 demonstrated comparable anti-infective efficacy to vancomycin in skin infection models and a mouse model of sepsis. Mechanism exploration suggested that the antibacterial behavior of Ru-1 is likely related to targeting the bacterial cell membrane and inhibiting topoisomerase I.
RSC MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
ChunYan Zhang, LiQiang Wang, Wei Deng, HaiYan Huang, JinTao Wang, XiangWen Liao, XueMin Duan, RuJian Yu, YanShi Xiong
Summary: In this study, three complexes Ru1-3 were synthesized and Ru3 was found to exhibit excellent antibacterial activity against S. aureus with low toxicity to red blood cells. Ru3 was shown to disrupt the bacterial cell membrane and alter its permeability, inhibiting the growth of bacteria. In model experiments, Ru3 demonstrated good activity against S. aureus and contributed to attenuating the development of drug resistance. Moreover, Ru3 exhibited a synergistic effect when combined with certain antibiotics.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Yushou Chen, Lianghong Liu, Xuerong Wang, Zhouyuji Liao, Runbin Wang, Yanshi Xiong, Jianxin Cheng, Guijuan Jiang, Jintao Wang, Xiangwen Liao
Summary: This study designed and synthesized a series of ruthenium-based antibacterial agents that target bacterial cell membrane integrity to combat methicillin-resistant Staphylococcus aureus. The study demonstrated that the lipophilicity/hydrophilicity ratio and the biphenyl group are crucial for enhancing antibacterial activity. Through various experiments, it was shown that Ru2 can disrupt bacterial cell membrane integrity and effectively inhibit biofilm formation and hemolysin secretion. Ru2 also exhibited significant antibacterial activity in both mouse and wax worm infection models with low toxicity.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Multidisciplinary
Chun-Yan Zhang, Ru-Jian Yu, Li-Qiang Wang, Hai-Yan Huang, Meng-Qi Xiao, Xue-Min Duan, Jin-Tao Wang, Xiang-Wen Liao, Yan-Shi Xiong
Summary: This study aimed to develop a good antibacterial drug against Staphylococcus aureus that does not easily produce resistance. The researchers synthesized a variety of metal ruthenium polypyridyl complexes and tested their antibacterial activity and toxicity. The results showed that the newly-synthesized ruthenium complex Ru(II)-2 exhibited good antibacterial activity in vivo and in vitro, with lower cytotoxicity.
NEW JOURNAL OF 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)
