Article
Biochemistry & Molecular Biology
Mustafa T. Ardah, Nabil Eid, Tohru Kitada, M. Emdadul Haque
Summary: Parkinson's disease is characterized by dopamine neuron loss and protein misfolding. The polyphenol Ellagic acid can reduce α-syn aggregation and toxicity, enhance cell viability by activating autophagy and suppressing apoptosis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Sangeun Han, Min Hyung Seo, Sabina Lim, Sujung Yeo
Summary: This study suggests a potential association between reduced ITGA7 expression and increased alpha-syn expression and apoptosis of dopaminergic cells in an MPTP-induced PD mouse model. This is the first study to show a link between ITGA7 and PD.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Cell Biology
Tianen Zhou, Meng Zhang, Yingyu Xie, Ying Chen, Sudan Peng, Xiuna Jing, Ming Lei, Enxiang Tao, Yanran Liang
Summary: In this study, we found that GFP-SNCA Exo decrease autophagy in microglia through carrying miRNAs, which then activate the MAPK signaling pathway and induce inflammation.
CELLULAR SIGNALLING
(2022)
Article
Biochemistry & Molecular Biology
Tsendsuren Tungalag, Dong Kwon Yang
Summary: Parkinson's disease is a neurodegenerative disorder with limited treatment options. Sinapic acid has shown potential as a neuroprotective agent against oxidative stress, mitochondrial dysfunction, and apoptosis, suggesting promising effects in the prevention and treatment of PD.
Article
Biochemistry & Molecular Biology
Anna Sannino, Maria Rosaria Scarfi, Melody Dufossee, Stefania Romeo, Loredana Poeta, Valerie Prouzet-Mauleon, Muriel Priault, Olga Zeni
Summary: Recent studies have shown that radiofrequency (RF) can reduce DNA damage induced by chemical or physical agents, similar to the adaptive response observed in radiobiology. This effect has been reported in vitro and in vivo, and possible cellular mechanisms activated by RF pre-exposure include perturbation of the cell redox status, DNA repair mechanisms, and stress response machinery. This study found that autophagy contributes to the RF-induced adaptive response in human neuroblastoma cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Neurosciences
Xin Liu, Le Qu, Na Zhang, Xiaoqi Yu, Zhixin Xiao, Limei Song, Junxia Xie, Huamin Xu
Summary: Our study demonstrated that Ndfip1 could protect against rotenone-induced neurotoxicity by antagonizing the increase in alpha-syn protein levels and inhibiting the upregulation of caspase-3 and decrease in tyrosine hydroxylase caused by rotenone. Ndfip1 may serve as a potential new drug target for the prevention and treatment of Parkinson's disease.
FRONTIERS IN MOLECULAR NEUROSCIENCE
(2021)
Article
Biochemistry & Molecular Biology
Christina Feng, Marisol Flores, Christina Dhoj, Adaly Garcia, Sheehan Belleca, Dana Abou Abbas, Jacob Parres-Gold, Aimee Anguiano, Edith Porter, Yixian Wang
Summary: By using scanning ion conductance microscopy (SICM), this study monitored the membrane changes induced by alpha-Syn preformed fibrils (PFFs) in neuroblastoma cells. The results showed that as the concentration of PFFs increased, the roughness of the cell membranes significantly increased, and noticeable protrusions with a more crystalline appearance were observed. Cell viability was slightly reduced, but not dependent on the dose.
ACS CHEMICAL NEUROSCIENCE
(2022)
Article
Cell Biology
Xin He, Wei Yuan, Chun-Qing Yang, Lu Zhu, Fei Liu, Juan Feng, Yi-Xue Xue
Summary: Ghrelin exerts neuroprotective effects against 6-OHDA-induced Parkinson's disease via the lincRNA-p21/TGIF1/alpha-synuclein pathway.
NEURAL REGENERATION RESEARCH
(2022)
Article
Biochemical Research Methods
Samiksha Sardana, Anneroos E. Nederstigt, Marc P. Baggelaar
Summary: S-palmitoylation is a lipid modification that plays a role in neuronal development and neurodegenerative diseases. In this study, two methods were used to identify S-palmitoylated proteins and sites during neuronal differentiation. A subset of high-confidence S-palmitoylated proteins were identified, suggesting an important role for S-palmitoylation in neuronal differentiation.
JOURNAL OF PROTEOME RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Noelia Carballeda Sangiao, Susana Chamorro, Sonia de Pascual-Teresa, Luis Goya
Summary: The study confirms the significant protective effect of phenolic compounds and epicatechin in aqueous extract of cocoa powder against oxidative stress on neuronal-like cells under physiological conditions.
Article
Cell Biology
Claudia Magrin, Martina Bellafante, Martina Sola, Ester Piovesana, Marco Bolis, Luciano Cascione, Sara Napoli, Andrea Rinaldi, Stephanie Papin, Paolo Paganetti
Summary: In this study, we performed a bioinformatics analysis to better understand the possible role of Tau in regulation of chromatin compaction and gene expression. Our findings suggest that Tau depletion leads to deregulation of transcripts involved in the polycomb repressive complex 2, leading to decreased levels of core components of the complex and lower histone 3 trimethylation. These changes are associated with increased senescence induction in Tau-deficient cells.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Heng Lin, Ri Tang, Lijun Fan, Ersong Wang
Summary: In this study, we found that exogenous TN can alleviate synucleinopathies in PD cellular models by promoting the degradation of SYN through plasmin. Furthermore, PD leads to aggregation of extracellular SYN, which decreases the expression of TN and increases the expression of PAI-1, resulting in reduced plasmin activity.
NEUROCHEMICAL RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Pooja Gangras, Valentina Gelfanova, Graham D. Williams, Samuel K. Handelman, Ryan M. Smith, Marjoke F. Debets
Summary: This study identifies high-confidence surface proteins expressed on the brain and DRG neurons using a bioinformatic workflow and demonstrates significant overlap between the SH-SY5Y cell surfaceome and the surface proteome of human brain and DRG neurons. It also finds that alternative splicing of specific isoforms in 32% of shared surface proteins allows them to maintain their protein-coding ability and localize to the cell surface. Validation of one of these isoforms confirms its presence in neuroblastomas, making it a receptor of interest for neuroblastoma-specific therapeutics.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Applied
Amanda Mota Vieira, Farrah Zahed, Alessandre Carmo Crispim, Edson de Souza Bento, Rafael de Freitas Oliveira Franca, Irapuan Oliveira Pinheiro, Luis A. Pardo, Bruno Melo Carvalho
Summary: The study found that high yield of levan was obtained through sucrose fermentation, and treatment with 1000 ug/mL of levan induced apoptosis in neuroblastoma cells without reducing proliferation or causing cytotoxic effects.
CARBOHYDRATE POLYMERS
(2021)
Article
Biochemistry & Molecular Biology
Andrila E. Collins, Tarek M. Saleh, Bettina E. Kalisch
Summary: This study aimed to assess the cytoprotective effects of the novel antioxidant compound VANL-100 in a cellular model of beta-amyloid (A beta)-induced toxicity. The results demonstrate that VANL-100 significantly attenuated A beta-induced cell death, indicating its cytoprotective effects against A beta-induced toxicity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Javier Garcia-Carceles, Elena Caballero, Carmen Gil, Ana Martinez
Summary: Viral infections are a significant health issue that requires novel therapeutic strategies. Targeting viral proteins encoded by the viral genome with antivirals usually leads to drug resistance. One potential solution is to target host-based proteins and phosphorylation events that play crucial roles in the viral life cycle. Repurposing existing kinase inhibitors could help in terms of cost and effectiveness, but specific medicinal chemistry programs are still needed for better results.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Cell Biology
Guadalupe Martinez-Chacon, Marta Paredes-Barquero, Sokhna M. S. Yakhine-Diop, Elisabet Uribe-Carretero, Ariadna Bargiela, Maria Sabater-Arcis, Jose Morales-Garcia, Jesus Alarcon-Gil, Eva Alegre-Cortes, Saray Canales-Cortes, Mario Rodriguez-Arribas, Pedro Javier Camello, Jose Manuel Bravo-San Pedro, Ana Perez-Castillo, Ruben Artero, Rosa A. Gonzalez-Polo, Jose M. Fuentes, Mireia Niso-Santano
Summary: QBA is a novel autophagy inducer that triggers autophagy in various neuronal cell lines and mouse and fly models. The beclin-1 (BECN1) and mTOR pathways participate in the regulation of QBA-induced autophagy. Moreover, QBA stimulates SIRT1, which promotes autophagy by the deacetylation of critical ATG proteins. QBA-mediated autophagy promotes neuroprotection in Parkinson's disease in vitro and in a mouse model and extends the lifespan of Drosophila melanogaster.
CELL BIOLOGY AND TOXICOLOGY
(2023)
Article
Chemistry, Medicinal
Vanesa Nozal, Loreto Martinez-Gonzalez, Marta Gomez-Almeria, Claudia Gonzalo-Consuegra, Paula Santana, Apirat Chaikuad, Eva Perez-Cuevas, Stefan Knapp, Daniel Lietha, David Ramirez, Sabrina Petralla, Barbara Monti, Carmen Gil, Angeles Martin-Requero, Valle Palomo, Eva de Lago, Ana Martinez
Summary: Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease characterized by the aggregation of protein TDP-43. In this study, TTBK1 inhibitors were identified as a promising therapeutic strategy for ALS. The novel pyrrolopyrimidine derivatives demonstrated their ability to reduce TDP-43 phosphorylation and preserve motor neurons in mouse models, suggesting their potential for future ALS therapy.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Microbiology
Miguel Angel Cuesta-Geijo, Isabel Garcia-Dorival, Ana del Puerto, Jesus Urquiza, Inmaculada Galindo, Lucia Barrado-Gil, Fatima Lasala, Ana Cayuela, Carlos Oscar S. Sorzano, Carmen Gil, Rafael Delgado, Covadonga Alonso
Summary: The inner viral membrane proteins of African swine fever virus (ASFV) interact with endosomal proteins, potentially playing a crucial role in the viral entry process. Silencing or knockout of these proteins affects different stages of ASFV infection, and in some cases, prevents the virus from entering the cytoplasm from endosomes. These findings provide new insights into the role of endosomal proteins in ASFV infection.
Article
Biochemistry & Molecular Biology
Andrea Bagan, Jose A. Morales-Garcia, Christian Grinan-Ferre, Caridad Diaz, Jose Perez del Palacio, Maria C. Ramos, Francisca Vicente, Belen Perez, Jose Brea, Maria Isabel Loza, Merce Pallas, Carmen Escolano
Summary: The research indicates that modulating imidazoline I-2 receptors can improve cognitive impairment and behavioral condition in patients with neurodegenerative diseases, with representative compound B06 showing potential as a drug candidate for advancing in drug discovery.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Victor Sebastian-Perez, Paula Martinez de Iturrate, Montserrat Nacher-Vazquez, Luis Novoa, Concepcion Perez, Nuria E. Campillo, Carmen Gil, Luis Rivas
Summary: A study has identified novel inhibitors of Leishmania GSK-3 with strong antiparasitic activity and in vitro enzyme inhibition, laying the foundation for the development of potential drugs for leishmaniasis.
Article
Microbiology
Tiziana Ginex, Clara Marco-Marin, Mitosz Wieczor, Carlos P. Mata, James Krieger, Paula Ruiz-Rodriguez, Maria Luisa Lopez-Redondo, Clara Frances-Gomez, Roberto Melero, Carlos Oscar Sanchez-Sorzano, Marta Martinez, Nadine Gougeard, Alicia Forcada-Nadal, Sara Zamora-Caballero, Roberto Gozalbo-Rovira, Carla Sanz-Frasquet, Rocio Arranz, Jeronimo Bravo, Vicente Rubio, Alberto Marina, Ron Geller, Inaki Comas, Carmen Gil, Mireia Coscolla, Modesto Orozco, Jose Luis Llacer, Jose-Maria Carazo
Summary: This article investigates the impact of the S:A222V mutation on viral infection, and finds that it promotes the opening of RBD and slightly increases ACE2 binding, while not affecting vaccine effectiveness.
Article
Pharmacology & Pharmacy
Melissa Alegria-Arcos, Tabata Barbosa, Felipe Sepulveda, German Combariza, Janneth Gonzalez, Carmen Gil, Ana Martinez, David Ramirez
Summary: The COVID-19 pandemic has accelerated the development of drugs/vaccines by integrating scientists globally. In this study, researchers collected information on the interactions between proteins from SARS-CoV-2 and humans, as well as information on protein-drug interactions from public databases. By representing this data as networks, they were able to gain insights into the interactions between proteins from both organisms. Through data analysis, they identified important proteins and drugs from a network pharmacology perspective, suggesting potential therapeutic options for COVID-19. This study also revealed the potential importance of human proteins in drug repurposing campaigns.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Pedro Gonzalez-Naranjo, Concepcion Perez, Marina Gonzalez-Sanchez, Adrian Gironda-Martinez, Eugenia Ulzurrun, Fernando Bartolome, Marcos Rubio-Fernandez, Angeles Martin-Requero, Nuria E. Campillo, Juan A. Paez
Summary: This study describes a new family of 5-substituted indazole derivatives with a multitarget profile including cholinesterase and BACE1 inhibition, which is a promising therapeutic approach against Alzheimer's disease. The compounds were synthesized and evaluated, and the results showed that some of them have antioxidant, anti-inflammatory, and neuroprotective properties.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Medicine, General & Internal
Maria Luz Vila Mendez, Carmen Anton Sanz, Alicia del Rocio Cardenas Garcia, Amparo Bravo Malo, Francisco Javier Torres Martinez, Jose Maria Martin Moros, Maria Real Torrijos, Jose Francisco Javier Vendrell Covisa, Olga Guzman Sierra, Veronica Molina Barcena, Nuria Viejo Pinero, Carlos Fernandez Diaz, Purificacion Arroyo Burguillo, Ana Maria Blanco Gallego, Carmen Guirao Sanchez, Aranzazu Montilla Bernabe, Maria del Pilar Villanueva Moran, Salvador Juarez Anton, Angela Fernandez Rodriguez, Maria angeles Somoza Calvo, Ernesto Cerrada Cerrada, Gemma Perez Manas, Antonio Sanchez Calso, Frida Vallejo Somohano, Carmen Cauqui Diaz, Gloria Vinas Fernandez, Jesus Molina Paris, Marina Gonzalez Godoy, Gonzalo Lumbreras Garcia, Javier Rosado Martin, Aida Rodriguez Hernandez, Sara Lopez Antunez, Gabriel Vazquez Perfecto, Maria Concepcion Marcello Andres, Nieves Marina Puente Garcia, Carmen Gil, Ana Martinez, Begona Soler Lopez
Summary: This 28-day study compared the efficacy of bromhexine plus standard of care (SOC) to SOC alone in mild-to-moderate COVID-19 outpatients in primary health care settings. The results showed that bromhexine treatment was associated with a reduction in viral load on day 4, but there was no significant difference compared to SOC alone. Therefore, bromhexine may not be an effective antiviral in patients with COVID-19.
JOURNAL OF CLINICAL MEDICINE
(2023)
Article
Biochemistry & Molecular Biology
Yang Zheng, Susanne Schroeder, Georgi K. Kanev, Sanaa S. Botros, Samia William, Abdel-Nasser A. Sabra, Louis Maes, Guy Caljon, Carmen Gil, Ana Martinez, Irene G. Salado, Koen Augustyns, Ewald Edink, Maarten Sijm, Erik de Heuvel, Iwan J. P. de Esch, Tiffany van der Meer, Marco Siderius, Geert Jan Sterk, David Brown, Rob Leurs
Summary: This study investigated the potential of Schistosoma mansoni phosphodiesterase SmPDE4A as a new drug target for schistosomiasis. The researchers cloned, isolated, and characterized the full-length and catalytic domains of SmPDE4A. They found that SmPDE4A resembles human PDE4 more than parasite PDEs. Screening of PDE inhibitors identified tetrahydrophthalazinones and benzamides as potential hits, but further evaluation showed that the inhibitors were not effective against S. mansoni, suggesting that SmPDE4A is not a suitable target for anti-schistosomiasis therapy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Alfonso Garcia-Rubia, Fatima Lasala, Tiziana Ginex, Marcos Morales-Tenorio, Catherine Olal, Michelle Heung, Paola Oquist, Inmaculada Galindo, Miguel Aprimengel Cuesta-Geijo, Jose M. Casasnovas, Nuria E. Campillo, Angeles Canales, Covadonga Alonso, Ana Martinez, Cesar Munoz-Fontela, Rafael Delgado, Carmen Gil
Summary: Ebola virus (EBOV), a single-strand RNA virus in the Filoviridae family, has been responsible for significant outbreaks since 2013. In this study, a new series of compounds were synthesized and found to inhibit EBOV infection by acting as virus entry inhibitors. The compounds were evaluated for their inhibitory activity against surrogate models and replicative EBOV, and their biological target was elucidated through various experiments. Additionally, their therapeutic potential was confirmed through in vitro metabolic stability and in vivo pharmacokinetic studies.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Cell Biology
Yaiza Corral Nieto, Sokhna M. S. Yakhine-Diop, Paula Moreno-Cruz, Laura Manrique Garcia, Amanda Gabrielly Pereira, Jose A. Morales-Garcia, Mireia Niso-Santano, Rosa A. Gonzalez-Polo, Elisabet Uribe-Carretero, Sylvere Durand, Maria Chiara Maiuri, Marta Paredes-Barquero, Eva Alegre-Cortes, Saray Canales-Cortes, Adolfo Lopez de Munain, Jordi Perez-Tur, Ana Perez-Castillo, Guido Kroemer, Jose M. Fuentes, Jose M. Bravo-San Pedro
Summary: Using mass spectrometry, this study identified metabolic changes in the liver of mouse models of Parkinson's disease, with the aim of finding new peripheral biomarkers for diagnosis.
Article
Biochemistry & Molecular Biology
Rocio Benitez-Fernandez, Carmen Gil, Carmen Guaza, Leyre Mestre, Ana Martinez
Summary: Multiple sclerosis (MS) is a chronic disease that is difficult to treat. This study found that VP3.15 has the potential to treat primary progressive multiple sclerosis (PPMS) by improving the disease course and motor function in infected mice.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(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)
