Review
Biochemistry & Molecular Biology
Dimitrios Kotsos, Konstantinos Tziomalos
Summary: Nonalcoholic fatty liver disease (NAFLD) is common in the general population and even more prevalent in obese and diabetic patients. NAFLD, especially nonalcoholic steatohepatitis (NASH), increases the risk for liver-related and cardiovascular morbidity. The development and progression of NAFLD involve complex and multifactorial pathogenesis, with potential involvement of microsomal prostaglandin E synthase-1 and -2. Targeting these enzymes may offer a novel therapeutic approach for NAFLD. This review discusses the association between microsomal prostaglandin E synthase-1 and -2 and NAFLD.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Stella Uebbing, Marius Kreiss, Friederike Scholl, Ann-Kathrin Haefner, Duran Sueruen, Ulrike Garscha, Oliver Werz, Devaraj Basavarajappa, Bengt Samuelsson, Olof Radmark, Beatrix Suess, Dieter Steinhilber
Summary: The 5-lipoxygenase enzyme has been identified to modulate miRNA processing in monocytic cells by promoting transcription of specific miRNAs and inhibiting the processing of pre-let-7e, ultimately leading to changes in the miRNA profile. This interaction results in altered expression levels of miRNAs, impacting cell differentiation, proliferation, and the maintenance of leukemic stem cell functions.
Article
Pharmacology & Pharmacy
Verena Krauth, Ferdinando Bruno, Simona Pace, Paul M. Jordan, Veronika Temml, Maria Preziosa Romano, Haroon Khan, Daniela Schuster, Antonietta Rossi, Rosanna Filosa, Oliver Werz
Summary: 5-Lipoxygenase (LO) is a key enzyme in the formation of pro-inflammatory leukotrienes (LT) that are important mediators in allergic reactions and inflammatory disorders. In this study, modifications were made to catechol derivatives to increase their effectiveness as selective 5-LO inhibitors. Two compounds, 3,4-dihydroxy-3 '-phenoxybiphenyl (6b) and 2-(3,4-dihydroxyphenyl)benzo[b]thiophene (6d), showed potent inhibition of human 5-LO in both cell-free and cell-based assays. Furthermore, these compounds were effective in inhibiting 5-LO in human blood and in a murine peritonitis model. These novel catechol derivatives have high selectivity and effectiveness as inhibitors of 5-LO under pathophysiological conditions.
BIOCHEMICAL PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Tarvi Teder, Stefanie Koenig, Rajkumar Singh, Bengt Samuelsson, Oliver Werz, Ulrike Garscha, Jesper Z. Haeggstrom
Summary: This study identified new drugs that can inhibit the expression of LTA(4)H and reduce the activity of 5-LOX in leukocytes, thus suppressing inflammatory responses.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Hsien-Chung Chen, Wen-Chang Chang, Jian-Ying Chuang, Kwang-Yu Chang, Jing-Ping Liou, Tsung- Hsu
Summary: Eicosanoids are bioactive lipids derived from arachidonic acid in the brain, and they play diverse roles in normal physiology, including neuronal signaling, synaptic plasticity, and regulation of cerebral blood flow. Dysregulation of eicosanoids has been implicated in the development and progression of brain tumors, and understanding their role can inform the development of diagnostic, prognostic, and therapeutic approaches.
BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER
(2023)
Article
Chemistry, Medicinal
Ferdinando Bruno, Verena Krauth, Seyed Mohamed Nabavi, Veronika Temml, Florinda Fratianni, Giuseppe Spaziano, Filomena Nazzaro, Fiorita Roviezzo, Jianbo Xiao, Haroon Kahn, Maria Preziosa Romano, Bruno D'Agostino, Oliver Werz, Rosanna Filosa
Summary: Oxidative stress and inflammation coexist in many multifactorial diseases, and the discovery of antioxidants is an appealing approach to target multiple therapeutic pathways in the arachidonic acid cascade.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Izumi Tsukayama, Yuki Kawakami, Asako Tamenobu, Keisuke Toda, Saya Maruoka, Yuki Nagasaki, Yoshiko Mori, Risa Sawazumi, Kensuke Okamoto, Keita Kanzaki, Hideyuki Ito, Yoshitaka Takahashi, Yoshimi Miki, Kei Yamamoto, Makoto Murakami, Toshiko Suzuki-Yamamoto
Summary: In this study, it was found that malabaricone C, a component of nutmeg, strongly inhibited the activity of 5-lipoxygenase, an enzyme involved in leukotriene biosynthesis. Furthermore, malabaricone C was shown to ameliorate psoriasis-like skin inflammation by decreasing the level of leukotriene B4.
FREE RADICAL BIOLOGY AND MEDICINE
(2022)
Article
Pharmacology & Pharmacy
Astrid S. Kahnt, Carlo Angioni, Tamara Goebel, Bettina Hofmann, Jessica Roos, Svenja D. Steinbrink, Florian Roersch, Dominique Thomas, Gerd Geisslinger, Kai Zacharowski, Sabine Groesch, Dieter Steinhilber, Thorsten J. Maier
Summary: 5-Lipoxygenase (5-LO) inhibitors show compound-specific pharmacological effects and their efficacy may involve the inhibition of prostaglandin E-2 (PGE(2)) export. Experimental models on the role of 5-LO in inflammation and pain using these inhibitors may be misleading, and their use as pharmacological tools needs to be reevaluated. Additionally, 5-LO inhibitors may serve as new scaffolds for the development of potent prostaglandin export inhibitors.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Cardiac & Cardiovascular Systems
Eva Prescott, Oskar Angeras, David Erlinge, Erik L. Grove, Marja Hedman, Lisette O. Jensen, John Pernow, Antti Saraste, Axel Akerblom, Sara Svedlund, Anna Rudvik, Jane Knochel, Eva-Lotte Lindstedt, Pavlo Garkaviy, Li-Ming Gan, Anders Gabrielsen
Summary: In patients with recent myocardial infarction, AZD5718 exhibited a dose-dependent inhibition of leukotriene biosynthesis and was well tolerated. However, it did not have a significant impact on coronary microvascular function.
INTERNATIONAL JOURNAL OF CARDIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Tugba Gurses, Abdurrahman Olgac, Ulrike Garscha, Tugce Gur Maz, Nur Banu Bal, Orhan Uludag, Burcu Caliskan, Ulrich S. Schubert, Oliver Werz, Erden Banoglu
Summary: The study focused on the role of small heteroaromatic fragments on the scaffold of 4,5-diarylisoxazol-3-carboxylic acid, aiming to produce multitarget inhibitors against mPGES-1, 5-LO and FLAP. Simple structural variations on the scaffold significantly influenced the selectivity against the targets, paving the way for development of new multi-target inhibitors with potential application as anti-inflammatory agents.
BIOORGANIC CHEMISTRY
(2021)
Review
Cell Biology
Mengdie Yan, Siran Zhang, Chengtan Li, Yanyan Liu, Jianbo Zhao, Yanfang Wang, Yi Yang, Lihui Zhang
Summary: Neuroinflammation is a common feature of age-related brain disorders such as Alzheimer's disease, Parkinson's disease, and cerebral ischemia. The proinflammatory enzyme 5-lipoxygenase (5-LOX) plays a crucial role in modulating inflammation by generating leukotrienes, and its abnormal activation and excessive production have been detected in the development of age-related brain pathology. Inhibition of 5-LOX activation may represent a promising therapeutic strategy for AD, PD, and cerebral ischemia.
AGEING RESEARCH REVIEWS
(2021)
Article
Chemistry, Medicinal
Azize Gizem Ergul, Tugce Gur Maz, Christian Kretzer, Abdurrahman Olgac, Paul M. Jordan, Burcu Caliskan, Oliver Werz, Erden Banoglu
Summary: This study reports the identification of new, potent, and selective inhibitors of human mPGES-1, such as compounds 10, 31, and 49, which showed IC50 of 0.03-0.09 mM in a cell-free assay. Compounds 10 and 49 also exhibited inhibitory activity against LTC4S, targeting both inflammatory PGE(2) and cys-LT biosynthesis. Compound 31 showed high selectivity towards mPGES-1 with decreased inhibitory activity on LTC4S, FLAP, and 5-LO.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Medicine, Research & Experimental
Takuto Nosaka, Yosuke Murata, Kazuto Takahashi, Tatsushi Naito, Kazuya Ofuji, Hidetaka Matsuda, Masahiro Ohtani, Katsushi Hiramatsu, Yoshiaki Imamura, Takanori Goi, Yasunari Nakamoto
Summary: This study identified the role of 5-LOX in hepatocellular carcinoma (HCC) progression and demonstrated that inhibition of 5-LOX activity can regulate HCC progression, suggesting it as a potential therapeutic target.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Oncology
Yuka Sasaki, Hiroshi Kuwata, Eri Aida, Tsubasa Ochiai, Daisuke Kamei, Yoshihito Nakatani, Shuntaro Hara
Summary: The study indicates that mPGES-1 plays an important role in skin carcinogenesis, with mPGES-1 deficiency suppressing DMBA/TPA-induced skin carcinogenesis and inhibiting the induction of inflammatory cytokines by TPA.
ANTICANCER RESEARCH
(2021)
Article
Oncology
Qian Wang, Yuanyuan Li, Mengying Wu, Songming Huang, Aihua Zhang, Yue Zhang, Zhanjun Jia
Summary: mPGES-1 inhibitors show promise in blocking the production of PGE2 with better specificity compared to NSAIDs, making them crucial in treating inflammatory diseases. Two inhibitors are undergoing clinical trials, with more novel inhibitors in development.
AMERICAN JOURNAL OF TRANSLATIONAL RESEARCH
(2021)
Article
Chemistry, Multidisciplinary
Antonia Fruntke, Mira Behnke, Leanne M. Stafast, Tom Trader, Elisabeth Dietel, Antje Vollrath, Christine Weber, Ulrich S. Schubert, Timm Wilke
Summary: This publication presents a series of experiments in the field of nanomedicine for high school chemistry education and student laboratories, developed as a collaborative project between chemistry didactics and chemical research. In this context, polymeric nanocarriers represent a promising approach for drug delivery, acting as smart packaging material to ensure transport to the desired location in the body and a targeted release. All experiments can be performed with simple and harmless chemicals within a time frame of two school lessons.
JOURNAL OF CHEMICAL EDUCATION
(2023)
Article
Biochemistry & Molecular Biology
Victor D. Lechuga-Islas, Melisa Trejo-Maldonado, Ilya Anufriev, Ivo Nischang, Ipek Terzioglu, Jens Ulbrich, Ramiro Guerrero-Santos, Luis E. Elizalde-Herrera, Ulrich S. Schubert, Carlos Guerrero-Sanchez
Summary: This article describes an all-aqueous, surfactant-free, and pH-driven method to generate pH- and temperature-responsive polymer nanoparticles. The nanoparticles were produced by solubilizing copolymers in an acidic buffer and can be stable for at least 28 days in a pH range of 2.0 to 6.0 and a temperature range of 25 to 50 degrees C. These nanoparticles can act as nanocarriers for pH-sensitive drugs, expanding their bioavailability and enabling controlled release.
MACROMOLECULAR BIOSCIENCE
(2023)
Article
Polymer Science
Lisa Ehrlich, Doris Pospiech, Upenyu L. Muza, Albena Lederer, Julia Muche, Dieter Fischer, Petra Uhlmann, Felix Tzschoeckell, Simon Muench, Martin D. Hager, Ulrich S. Schubert
Summary: This study investigates solid electrolytes based on ionic liquid polymers that offer stable ion conduction. Ionic liquid monomers are converted into linear homopolymers or polymer networks by thermally initiated radical polymerization or UV-initiated copolymerization. The materials are confirmed through NMR or Raman spectroscopy, and their ionic conductivities are measured. The results show that these materials have potential as electrolytes for solid-state batteries.
MACROMOLECULAR CHEMISTRY AND PHYSICS
(2023)
Article
Polymer Science
Leanne M. Stafast, Nora Engel, Helmar Goerls, Christine Weber, Ulrich S. Schubert
Summary: In this study, 2-(4-(iodomethyl)benzyl)isoindoline-1,3-dione was used as a protected amine-functionalized initiator for the cationic ring opening-polymerization (CROP) of 2-ethyl-2-oxazoline. The polymerization was well-controlled and terminated with sodium azide. Subsequent deprotection allowed for attachment of targeting ligands to the polymer. The heterotelechelic PEtOx was then coupled to end-functionalized polylactide to form block copolymers for nanomedicine.
EUROPEAN POLYMER JOURNAL
(2023)
Article
Chemistry, Physical
Christian Friebe, Clara Zens, Stephan Kupfer, Ulrich S. Schubert
Summary: We propose an approach to overcome the low intrinsic electrical conductivity of established organic materials by directly electrochemically polymerizing suitable monomers onto the battery electrode. By linking a terthiophene to a TEMPO moiety, we not only achieve successful electropolymerization but also construct additive-free organic batteries. Cell tests demonstrate the system's high rate capabilities (20% capacity retention at 50C) and good long-term stability (0.03% capacity loss per cycle).
JOURNAL OF PHYSICAL CHEMISTRY C
(2023)
Article
Chemistry, Physical
Erik Schroeter, Lada Elbinger, Manon Mignon, Christian Friebe, Johannes C. Brendel, Martin D. Hager, Ulrich S. Schubert
Summary: Aqueous zinc batteries with organic cathode materials have the potential to be sustainable, safe, environmentally friendly, and highly flexible secondary energy storage systems. In this study, we demonstrate the preparation of an oxygen-tolerant, semi-organic setup using an all-aqueous process, from polymerization to coin cell assembly, without the need for intermediate purification steps. The resulting battery exhibits high energy densities and excellent stability, making it a promising candidate for cost-effective and efficient rechargeable zinc-based batteries.
JOURNAL OF POWER SOURCES
(2023)
Article
Polymer Science
Nicole Ziegenbalg, Hans F. F. Ulrich, Steffi Stumpf, Philipp Mueller, Jurgen Wiethan, Janette Danner, Ulrich S. S. Schubert, Torben Adermann, Johannes C. C. Brendel
Summary: This study investigated the polymerization of VME monomer in water and found that the resulting polymer could coordinate with silver or gold ions, forming stable dispersions. Polyvinyl alcohol (PVA) was identified as the only surfactant capable of creating stable dispersions. Exposure to sunlight led to controlled reduction of the metal ions and the formation of composite particles. Silver ion-containing dispersions demonstrated strong antibacterial properties.
MACROMOLECULAR CHEMISTRY AND PHYSICS
(2023)
Article
Polymer Science
Natalie E. Goeppert, Michael Dirauf, Phil Liebing, Christine Weber, Ulrich S. Schubert
Summary: A monomer of 3-benzylmorpholine-2,5-dione is synthesized from l-phenylalanine and characterized by various techniques. A well-defined poly(ester amide) homopolymer is then synthesized using a binary catalyst system, showing high controllability of dispersities and molar masses. The resulting polyesteramides have potential as drug delivery vehicles, especially for hydrophobic drugs.
MACROMOLECULAR RAPID COMMUNICATIONS
(2023)
Article
Nanoscience & Nanotechnology
He Jia, Zehan Chen, Shanshan Yan, Fabio Lucaccioni, Zdravko Kochovski, Yan Lu, Christian Friebe, Ulrich S. Schubert, Jean-Francois Gohy
Summary: Nanoreactors with hydrophilic porous SiO2 shells and amphiphilic copolymer cores were prepared, which can adjust their hydrophilic/hydrophobic balance and exhibit chameleon-like behavior depending on the environment. The resulting nanoparticles showed excellent colloidal stability in solvents with different polarities. Importantly, with the help of nitroxide radicals attached to the amphiphilic copolymers, the synthesized nanoreactors exhibited high catalytic activity in both polar and nonpolar environments, and achieved high selectivity for the products of benzyl alcohol oxidation in toluene.
ACS APPLIED MATERIALS & INTERFACES
(2023)
Article
Chemistry, Multidisciplinary
Patrick Endres, Timo Schuett, Julian Kimmig, Stefan Zechel, Martin D. Hager, Robert Geitner, Ulrich S. Schubert
Summary: In this study, online NMR measurements are introduced as a new analytical setup for investigating the synthesis of oxymethylene dimethyl ether (OME). The setup is validated by comparing it with state-of-the-art gas chromatographic analysis. The influence of parameters such as temperature, catalyst concentration, and catalyst type on OME fuel formation based on trioxane and dimethoxymethane is investigated, with Amberlyst(TM) 15 (A15) and trifluoromethanesulfonic acid (TfOH) being used as catalysts. A kinetic model is applied to describe the reaction and calculate the activation energy and catalyst order.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Multidisciplinary
Tugce Gur Maz, H. Burak Caliskan, Irfan Capan, Burcu Caliskan, Berrin Ozcelik, Erden Banoglu
Summary: Chronic gastric infections caused by Helicobacter pylori (H. pylori) urease can be effectively treated with a new series of 1,3,4-oxadiazole-2-thiones compounds as urease inhibitors. Among them, compound 21 displayed the highest efficacy with an IC50 value of 26.6 µM and competitive inhibition pattern. Molecular docking analysis revealed important interactions between compound 21 and amino acid residues in the active pocket of the urease, suggesting the potential for developing improved urease inhibitors as anti-infective agents.
Article
Chemistry, Organic
Tugce Gur Maz, Huseyin Burak Caliskan
Summary: Inhibition of soluble epoxide hydrolase (sEH) is a potential therapeutic approach against inflammatory disorders. Piperidine/piperazine amide derivatives of chromone-2-carboxylic acid were synthesized and evaluated as sEH inhibitors. Compound 7 showed concentration-dependent inhibition of sEH activity with an IC50 of 1.75 μM, making it a novel lead structure for developing improved sEH inhibitors.
ORGANIC COMMUNICATIONS
(2023)
Article
Chemistry, Multidisciplinary
Abdurrahman Olgac, Irfan Capan, Philipp Dahlke, Paul M. Jordan, Oliver Werz, Erden Banoglu
Summary: This study investigates the synthesis and FLAP-antagonistic potential of 1,2,4-triazole derivatives. The results show that structural variations on 4,5-diaryl moieties and the 3-thioether side chain of the 1,2,4-triazole scaffold significantly affect FLAP antagonism. Metabololipidomics analysis reveals that one of the compounds selectively suppresses leukotriene B-4 formation without affecting other branches of the AA pathway. Overall, the 1,2,4-triazole scaffold holds promise as a chemical platform for developing more potent FLAP antagonists as anti-inflammatory agents.
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)