Article
Biochemistry & Molecular Biology
Stephane Fraga de Oliveira Tosta, Mariana Santana Passos, Rodrigo Kato, Alvaro Salgado, Joilson Xavier, Arun Kumar Jaiswal, Siomar C. Soares, Vasco Azevedo, Marta Giovanetti, Sandeep Tiwari, Luiz Carlos Junior Alcantara
Summary: Yellow fever is a re-emerging major health issue causing recent outbreaks with high mortality rates, mainly affecting tropical countries in Africa and South America. The development of a multi-epitope vaccine for Yellow fever virus using immunoinformatics approaches shows potential in stimulating both humoral and cellular immune responses, making it a candidate for further experimental validation.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Virology
Ashley E. Strother, Jill K. Thompson, Steven G. Widen, Alan D. T. Barrett
Summary: The yellow fever disease was prevented by two live attenuated vaccines, strains 17D and French neurotropic vaccine (FNV), derived from wild-type strains Asibi and French Viscerotropic virus (FVV) through serial passage. The genome sequence of FVV was determined after five passages in HeLa cells, and it was found that the FVV HeLa p5 virus had five amino acid substitutions compared to the parental strain. Surprisingly, the genetic diversity and Ribavirin resistance of the FVV HeLa p5 virus were not statistically different to the parental strain.
Article
Virology
Eneida Santos Oliveira, Naiara Clemente Tavares, Stella Garcia Colombarolli, Izabella Cristina Andrade Batista, Camila Sales Nascimento, Philip Louis Felgner, Rafael Ramiro de Assis, Carlos Eduardo Calzavara-Silva
Summary: Yellow Fever disease caused severe outbreaks in the Americas in recent years. In this study, peptides were designed and tested with sera collected from infected individuals, and one peptide was found to differentiate vaccinated individuals from naturally infected individuals.
Article
Virology
Kyoko Saito, Kentaro Shimasaki, Masayoshi Fukasawa, Ryosuke Suzuki, Yuko Okemoto-Nakamura, Kaoru Katoh, Tomohiko Takasaki, Kentaro Hanada
Summary: This study established and characterized Vero cell lines carrying YFV replicons, and investigated the effects of various drugs on the persistent replication of the replicons. The results showed that several drugs could inhibit the replication of the replicons, providing evidence for the screening of antiviral drugs.
Review
Microbiology
Awadalkareem Adam, Christian Jassoy
Summary: Arbovirus infections are prevalent in Africa due to the lack of established epidemiological surveillance systems and accurate differential diagnosis. Studies indicate these infections are endemic in most African countries, highlighting the need for improved monitoring to enhance diagnostic accuracy. Healthcare providers should be informed about prevalent arboviral diseases to better identify and manage possible cases.
Article
Microbiology
Julia C. LeCher, Keivan Zandi, Vivian Vasconcelos Costa, Franck Amblard, Sijia Tao, Dharmeshkumar Patel, Sujin Lee, Felipe Rocha da Silva Santos, Matheus Rodrigues Goncalves, Celso Martins Queroz-Junior, Fernanda Martins Marim, Katie Musall, Shu Ling Goh, Tamara McBrayer, Jessica Downs-Bowen, Ramyani De, Niloufar Azadi, James Kohler, Mauro Martins Teixeira, Raymond F. Schinazi
Summary: This study reports potential antiviral drugs against yellow fever virus, showing low toxicity, high intracellular metabolism, and strong anti-YFV activity in different models. The findings provide a new therapeutic option for treating yellow fever virus infections.
Review
Pharmacology & Pharmacy
Ivo C. C. Martins, Rafaela C. C. Ricardo, Nuno C. C. Santos
Summary: Dengue, West Nile, and Zika viruses are vector-borne flaviviruses that cause disease outbreaks with potentially severe symptoms and socioeconomic repercussions. Currently, there are no specific treatments available, and only generic symptom relief is possible. The effectiveness of the first dengue vaccine, Dengvaxia, is limited. Prophylactic approaches against other viruses are even more restricted. Therefore, there is a need for therapeutic strategies.
Article
Chemistry, Analytical
Pei-Shan Tsai, Pin-Xian Du, Batuhan Birol Keskin, Nan-Yao Lee, Shu-Wen Wan, Ya-Lan Lin, Wen-Yu Su, Pei-Chun Lin, Wei-Hsun Lin, Hsi-Chang Shih, Tzong-Shiann Ho, Guan-Da Syu
Summary: This study aims to analyze the humoral immunity and cross-reactivity in dengue patients using a multiplexed protein microarray. The results show that patients with severe dengue have higher levels of IgG antibodies against multiple Flavivirus antigens. Logistic regression analysis identifies groups of markers that can effectively distinguish dengue patients from healthy controls and hospitalized patients from mild cases.
ANALYTICAL CHEMISTRY
(2023)
Article
Microbiology
Seydou Ka, Natacha Merindol, Aissatou Aicha Sow, Amita Singh, Karima Landelouci, Melodie B. Plourde, Genevieve Pepin, Marco Masi, Roberta Di Lecce, Antonio Evidente, Matar Seck, Lionel Berthoux, Laurent Chatel-Chaix, Isabel Desgagne-Penix
Summary: The study found that Amaryllidaceae alkaloids (AAs) from plants of the Amaryllidaceae family have strong antiviral activity, with cherylline specifically inhibiting dengue virus and Zika virus replication. This suggests that AAs, including cherylline, could be a potential source of new antiviral drugs.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Biochemical Research Methods
Idrissa Dieng, Mignane Ndiaye, Moussa Dia, Moufid Mhamadi, Cheikh Talibouya Toure, Aboubacry Gaye, Cheikh Tidiane Diagne, Ahmed El Wahed, Manfred Weidmann, Ousmane Faye, Amadou Alpha Sall, Oumar Faye
Summary: A qRT-PCR system based on TaqMan chemistry was developed to detect Saboya virus (SABV) with high specificity and sensitivity. The system reliably detected SABV strains without cross amplification of other flaviviruses. It can be easily incorporated into existing arbovirus detection assays to study virus prevalence in various samples.
JOURNAL OF VIROLOGICAL METHODS
(2023)
Article
Virology
Carolin Brand, Gabrielle Deschamps-Francoeur, Kristen M. Bullard-Feibelman, Michelle S. Scott, Brian J. Geiss, Martin Bisaillon
Summary: As obligate intracellular parasites, viruses rely heavily on host cells for replication and dysregulate cellular processes for their benefit. The present study used RNA sequencing and mass spectrometry to investigate the complex interactions between viruses and host cells. Changes in the transcriptome and proteome of infected cells were compared to mock-infected cells, revealing significant alterations in mRNA and protein abundance, as well as modulation of alternative splicing. Interestingly, there was a disconnect between the changes in the transcriptome and those in the proteome of infected cells.
Article
Microbiology
Mercedes Viettri, Gerson Caraballo, Maria Elena Sanchez, Aurora Espejel-Nunez, Abigail Betanzos, Vianney Ortiz-Navarrete, Guadalupe Estrada-Gutierrez, Porfirio Nava, Juan E. Ludert
Summary: This study compared the growth and dissemination of Zika virus (ZIKV) with dengue virus (DENV) and yellow fever virus (YFV-17D) in cells. The results showed that ZIKV has a greater ability to infect cells and inhibits the immune and chemical responses of cells.
MICROBIOLOGY SPECTRUM
(2023)
Article
Cell Biology
Sundy N. Y. Yang, Belinda Maher, Chunxiao Wang, Kylie M. Wagstaff, Johanna E. Fraser, David A. Jans
Summary: This study identifies two drugs that can inhibit the replication of dengue virus and other flaviviruses by directly binding to a viral protein.
Article
Microbiology
Izabela Mauricio de Rezende, Gabriela Fernanda Garcia Oliveira, Thais Alkifeles Costa, Aslam Khan, Leonardo Soares Pereira, Tayrine Araujo Santos, Pedro Augusto Alves, Carlos Eduardo Calzavara-Silva, Olindo Assis Martins-Filho, Andrea Teixeira-Carvalho, Angelle Desiree LaBeaud, Betania Paiva Drumond
Summary: Prior studies have shown that yellow fever virus (YFV) RNA can be detected in saliva and urine as an alternative to serum. In this study, urine samples collected from yellow fever (YF) patients during acute and convalescent phases of YF infection were tested for YFV RNA. The results indicated the presence of YFV RNA in both the acute and convalescent phase samples, suggesting a prolonged period of detection beyond the viremic phase. Genotyping analysis revealed the presence of YFV South American I genotype in these samples. The use of urine samples, along with serological tests, epidemiologic inquiry, and clinical assessment, could provide a longer diagnostic window for laboratory YF diagnosis.
JOURNAL OF CLINICAL MICROBIOLOGY
(2022)
Article
Medicine, Research & Experimental
Ruixue Hou, Lewis E. Tomalin, Jessica Pintado Silva, Seunghee Kim-Schulze, Stephen S. Whitehead, Ana Fernandez-Sesma, Anna P. Durbin, Mayte Suarez-Farinas
Summary: Understanding the immune response to dengue virus is crucial for dengue vaccine development. This study showed that the tetravalent vaccine has better protective effects against DENV compared to the trivalent admixture. Additionally, differences in immune responses between Black and White participants were observed.
Article
Biochemistry & Molecular Biology
Saida Lachhab, Az-eddine El Mansouri, Ahmad Mehdi, Indira Dennemont, Johan Neyts, Dirk Jochmans, Graciela Andrei, Robert Snoeck, Yogesh S. Sanghvi, Mustapha Ait Ali, Philippe M. Loiseau, Hassan B. Lazrek
Summary: A new series of 3-acetyl-1,3,4-oxadiazoline hybrid molecules were designed and synthesized, and their activities against pathogens were screened. One of the intermediates exhibited significant antileishmanial activity.
MOLECULAR DIVERSITY
(2023)
Article
Pharmacology & Pharmacy
Winston Chiu, Joost Schepers, Thibault Francken, Laura Vangeel, Kayvan Abbasi, Dirk Jochmans, Steven De Jonghe, Hendrik Jan Thibaut, Volker Thiel, Johan Neyts, Manon Laporte, Pieter Leyssen
Summary: We developed a high-throughput screening method for antiviral drugs against SARS-CoV-2 using a fully automated robot system. This novel dual-reporter virus-cell-based imaging assay proved to be convenient and powerful for screening large compound libraries. The selected host cell subclone showed high expression of the reporter virus, resistance to virus-induced cytopathogenic effects, and strong fluorescent signals, making it suitable for high-throughput screening purposes.
ANTIVIRAL RESEARCH
(2023)
Article
Chemistry, Physical
Az-Eddine El Mansouri, Saida Lachhab, Ali Oubella, Mehdi Ahmad, Johan Neyts, Dirk Jochmans, Winston Chiu, Laura Vangeel, Steven De Jonghe, Hamid Morjani, Mustapha Ait Ali, Mohamed Zahouily, Yogesh S. Sanghvi, Hassan B. Lazrek
Summary: Analogous to pyrimidine and 1,3,4-oxadiazole, the newly synthesized pyrimidine-1,3,4-oxadiazole conjugated hybrid molecules exhibited potential anticancer activity. Specifically, compound 5e demonstrated significant growth inhibition against various cancer cell lines and induced apoptosis through caspase activation and cell-cycle arrest.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Shenghua Gao, Letian Song, Hongtao Xu, Antonios Fikatas, Merel Oeyen, Steven De Jonghe, Fabao Zhao, Lanlan Jing, Dirk Jochmans, Laura Vangeel, Yusen Cheng, Dongwei Kang, Johan Neyts, Piet Herdewijn, Dominique Schols, Peng Zhan, Xinyong Liu
Summary: DF-47 and DF-51 were identified as effective inhibitors of SARS-CoV-2/DENV polymerase through RdRp inhibition screening and in vitro antiviral study. In silico simulation revealed stable binding modes between DF-47/DF-51 and SARS-CoV-2/DENV RdRp, including chelating with Mg2+ near the polymerase active site. These polyphenols have the potential to be developed into broad-spectrum, non-nucleoside RdRp inhibitors with a new scaffold.
Editorial Material
Microbiology
Dirk Jochmans, Manon Laporte, Johan Neyts
Summary: Broad-spectrum antiviral drugs should be developed and stockpiled during epidemic/pandemic periods for immediate response to new virus outbreaks, and they will continue to be important tools even after the introduction of vaccines and monoclonal antibodies.
CELL HOST & MICROBE
(2023)
Editorial Material
Gastroenterology & Hepatology
Jerome Gouttenoire, Johan Neyts
Article
Biochemistry & Molecular Biology
Olaia Marti-Mari, Rana Abdelnabi, Dominique Schols, Johan Neyts, Maria-Jose Camarasa, Federico Gago, Ana San-Felix
Summary: AL-471 is a potent inhibitor of HIV and EV-A71 entry, and our research group has made further improvements on it. The antiviral activity of the compounds seems to be largely independent of the Trp stereochemistry and is dependent on both the Trp unit and the distal isophthalic moiety. One derivative, 23 (AL-534), with the shortest alkyl urea linkage, showed subnanomolar potency against different EV-71 clinical isolates.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Medicine, General & Internal
Elise Wouters, Caro Verbrugghe, Rana Abdelnabi, Rosalie Devloo, Dorien De Clippel, Dirk Jochmans, Dominique De Bleser, Birgit Weynand, Veerle Compernolle, Johan Neyts, Hendrik B. Feys
Summary: Convalescent plasma (CP) transfusion is an effective prophylactic for COVID-19, especially when administered within 5 days after symptom onset. Testing on hamsters showed that high-titer CP provided significant protection against viral infection. Therefore, including CP transfusion in future pandemic preparedness plans is crucial.
Article
Pharmacology & Pharmacy
Xinyu Wang, Lisanne Terrie, Guanghui Wu, Els J. M. Van Damme, Lieven Thorrez, Anthony R. Fooks, Ashley C. Banyard, Dirk Jochmans, Johan Neyts
Summary: Infection with the rabies virus is a deadly neurological disease, but post-exposure prophylaxis (PEP) with vaccination and anti-rabies immunoglobulins (RIGs) is 100% effective if administered early. This study found that Urtica dioica agglutinin (UDA), a specific lectin, can prevent the entry of the virus into host cells and effectively stop virus replication in a muscle model. UDA holds promise as a cheap and simple alternative for RIGs in PEP.
Article
Microbiology
Tatiana M. T. Rezende, Gabriella Macera, Leo Heyndrickx, Johan Michiels, Sandra Coppens, Hendrik Jan Thibaut, Kai Dallmeier, Marjan Van Esbroeck, Johan Neyts, Kevin K. Arien, Koen Bartholomeeusen
Summary: This article reports the validation of a new reporter cell line, Hec1a-IFNB-Luc, for the inhibition studies of various flaviviruses relevant to human pathology. The cell line showed high responsiveness to all tested flaviviruses, including dengue virus serotypes. It is comparable to clinically applied assays in measuring neutralizing antibody activity and assessing the antiviral activities of small-molecule compounds.
MICROBIOLOGY SPECTRUM
(2023)
Article
Microbiology
Jordi Doijen, Koen Temmerman, Christel van den Eynde, Annick Diels, Nick Van den Broeck, Michiel Van Gool, Inha Heo, Steffen Jaensch, Marleen Zwaagstra, Mayra Diosa Toro, Winston Chiu, Steven De Jonghe, Pieter Leyssen, Denisa Bojkova, Sandra Ciesek, Jindrich Cinatl, Lore Verschueren, Christophe Buyck, Frank Van Kuppeveld, Johan Neyts, Marnix Van Loock, Ellen Van Damme
Summary: This article reports the discovery of a small molecule, Z-Tyr-Ala-CHN2, which shows sub-micromolar antiviral activity against SARS-CoV-2, SARS-CoV-1, and human coronavirus 229E. The molecule acts at the early phase of the infection cycle by inhibiting cathepsin L. Although its activity is cell-specific, Z-Tyr-Ala-CHN2 can be a useful tool compound for studying the biology of coronavirus entry and replication.
Article
Pharmacology & Pharmacy
Xin Zhang, Niels Cremers, Stijn Hendrickx, Yannick Debing, Tania Roskams, Lotte Coelmont, Johan Neyts, Suzanne J. F. Kaptein
Summary: Hepatitis E virus (HEV) is a major cause of hepatitis, with an estimated 3.3 million symptomatic cases annually. Currently, there is no specific treatment for HEV, and a vaccine is only available in China and Pakistan. To aid in the development of therapeutic and preventive strategies, convenient HEV infection models in small laboratory animals are needed.
ANTIVIRAL RESEARCH
(2023)
Article
Pharmacology & Pharmacy
Robert Konkel, Aleksandra Milewska, Nguyen Dan Thuc Do, Emilia Barreto Duran, Artur Szczepanski, Jacek Plewka, Ewa Wieczerzak, Sofia Iliakopoulou, Triantafyllos Kaloudis, Dirk Jochmans, Johan Neyts, Krzysztof Pyrc, Hanna Mazur-Marzec
Summary: In this study, fifteen cyanopeptolins (CPs) were isolated from the Baltic cyanobacterium Nostoc edaphicum and tested for their activity against SARS-CoV-2. The results showed that the Arg-containing CP978 exhibited the strongest inhibition of Delta SARS-CoV-2 infection, possibly through direct interaction with the virus. CP978 also showed significant reduction in virus replication in human airway epithelial cells. Among the tested SARS-CoV-2 variants, CP978 had no effect on the Wuhan variant. These findings suggest that CP978 has potential as an antiviral drug candidate.
ANTIVIRAL RESEARCH
(2023)
Article
Chemistry, Medicinal
Bart Kesteleyn, Dorotheie Bardiot, Jean-Francois Bonfanti, Benoit De Boeck, Olivia Goethals, Suzanne J. F. Kaptein, Bart Stoops, Erwin Coesemans, Jeirome Fortin, Philippe Muller, Freideiric Doublet, Gunter Carlens, Mohamed Koukni, Wim Smets, Pierre Raboisson, Patrick Chaltin, Kenny Simmen, Marnix Van Loock, Johan Neyts, Arnaud Marchand, Tim H. M. Jonckers
Summary: The discovery and development of a novel small-molecule antiviral for dengue prevention or treatment is critical due to the absence of approved dengue-specific treatment. This study identified a series of 3-acyl-indole derivatives as potent dengue virus inhibitors and optimized them to improve their effectiveness against all four DENV serotypes. The optimized candidates demonstrated good chiral stability, oral bioavailability, and efficacy in treating DENV-2 infection in mice.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Immunology
Rana Abdelnabi, Patricia Perez, David Astorgano, Guillermo Albericio, Winnie Kerstens, Hendrik Jan Thibaut, Lotte Coelmont, Birgit Weynand, Nuria Labiod, Rafael Delgado, Dolores Montenegro, Eugenia Puentes, Esteban Rodriguez, Johan Neyts, Kai Dallmeier, Mariano Esteban, Juan Garcia-Arriaza
Summary: This study describes the enhanced immunogenicity and efficacy of the MVA-S(3P) vaccine in hamsters. Vaccinated hamsters developed high titers of antibodies that could neutralize different variants of the virus and showed reduced disease symptoms after infection. Additionally, the vaccine reduced lung pathology and proinflammatory cytokine levels.
FRONTIERS IN IMMUNOLOGY
(2023)
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)
