Article
Multidisciplinary Sciences
Amal F. F. Soliman, Mohamed A. A. Sabry, Gehad Abdelwahab
Summary: The essential oil isolated from Araucaria heterophylla resin was analyzed, and 24 components were identified, accounting for 99.89% of the total detected constituents. The oil exhibited inhibitory activity against aldose reductase and BuCHE enzymes, possibly due to compounds containing epoxide and hydroxyl groups. This study provides preliminary screening for the oil as potential therapeutic agents for antidiabetic cataract and Alzheimer's disease.
SCIENTIFIC REPORTS
(2023)
Article
Biochemistry & Molecular Biology
Anna Stasilowicz-Krzemien, Natalia Rosiak, Andrzej Miklaszewski, Judyta Cielecka-Piontek
Summary: To improve the bioavailability of caffeic acid, delivery systems were developed using ball milling and freeze-drying techniques to prepare solid dispersions of caffeic acid and magnesium aluminometasilicate. The 1:1 mass ratio solid dispersion obtained from ball milling was the most effective, and its identity was confirmed using X-ray powder diffraction and Fourier-transform infrared spectroscopy techniques. Screening tests demonstrated the improved anti-neurodegenerative activity of caffeic acid with enhanced solubility, inhibiting acetylcholinesterase, butyrylcholinesterase, tyrosinase, and showing antioxidant potential. In silico studies identified the domains of caffeic acid that interacted with enzymes relevant to neuroprotective activity. Furthermore, improved permeability through gastrointestinal tract and blood-brain barrier mimicking membranes validated the in vivo screening tests for anti-neurodegenerative activity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Muhammad Taha, Fazal Rahim, Nizam Uddin, Ihsan Ullah Khan, Naveed Iqbal, El Hassane Anouar, Mohammed Salahuddin, Rai Khalid Farooq, Mohammed Gollapalli, Khalid Mohammed Khan, Ameeduzzafar Zafar
Summary: Indole-based thiadiazole derivatives were synthesized and evaluated for their inhibition of AChE and BChE. Compounds with para, ortho, and meta-fluoro substitutions on the phenyl ring attached to thiadiazole showed the highest activity. Characterization was done using NMR, MS, and molecular docking studies were conducted.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Food Science & Technology
Rares Birsan, Peter Wilde, Keith W. Waldron, Dilip K. Rai
Summary: The study indicates that polyphenol-rich brewer's spent grain (BSG) fractions have the potential to act as natural anti-cholinesterase agents. The diethyl ether fraction of the saponified extract showed the best inhibitions of cholinesterases.
Review
Biochemistry & Molecular Biology
Anna Bubley, Alexaner Erofeev, Peter Gorelkin, Elena Beloglazkina, Alexander Majouga, Olga Krasnovskaya
Summary: Alzheimer's disease (AD) is a neurodegenerative disorder characterized by Aβ aggregation, tau hyperphosphorylation, and loss of cholinergic neurons. AD is also associated with oxidative stress, metal dyshomeostasis, inflammation, and cell cycle dysregulation. In this review, THA-based hybrids are summarized as potential anti-AD agents, highlighting strategies for drug design that have led to cognitive improvements and reduced hepatotoxicity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Ginson George, Vishal Payyalot Koyiparambath, Sunitha Sukumaran, Aathira Sujathan Nair, Leena K. Pappachan, Abdullah G. Al-Sehemi, Hoon Kim, Bijo Mathew
Summary: This review highlights the recent evidence of chalcones as a privileged structure in the development of drugs for Alzheimer's disease. Different classes of chalcone-derived analogs and the importance of certain functionalities in exhibiting pharmaceutical activity are summarized.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
Jing-Jing Liang, Tian-Ming Lv, Zhi-Yong Xu, Ning-Ning Du, Bin Lin, Xiao-Xiao Huang, Shao-Jiang Song
Summary: Two undescribed split-ring iridoids (1-2) along with six known triterpenes (3-8) and one steride (9) were isolated from Viburnum chingii. Compound 2 exhibited a novel split-ring iridoid skeleton formed by electrocyclic reaction and split ring. The structures and absolute configurations of the new iridoids were determined using NMR, HRESIMS, and ECD calculations. All the isolated compounds were tested for their AChE inhibitory activity, with compounds 1, 2, 3, 4, and 7 showing significant effects compared to the positive control donepezil. Molecular docking studies were also conducted for these compounds.
Article
Biochemistry & Molecular Biology
Hyun Myung Lee, Rudolf Andrys, Jakub Jonczyk, Kyuneun Kim, Avinash G. Vishakantegowda, David Malinak, Adam Skarka, Monika Schmidt, Michaela Vaskova, Kamil Latka, Marek Bajda, Young-Sik Jung, Barbara Malawska, Kamil Musilek
Summary: The designed and synthesised pyridinium-2-carbaldoximes with quinolinium carboxamide moiety showed intermediate-to-high inhibition of both cholinesterases compared to standard oximes. In vitro evaluation revealed their reactivation ability on human recombinant acetylcholinesterase (hrAChE) and human recombinant butyrylcholinesterase (hrBChE), with one compound showing reactivation of all used organophosphates on hrAChE, and two novel compounds able to reactivate NIMP/NEMP-hrBChE. The molecular modelling results highlighted the importance of creating a pre-reactivation complex for better reactivation of both cholinesterases.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Raquel B. M. de Almeida, Deyse B. B. Barbosa, Mayra R. R. do Bomfim, Jessika A. O. Amparo, Bruno S. S. Andrade, Silvia L. L. Costa, Joaquin M. Campos, Jorddy N. Cruz, Cleydson B. R. Santos, Franco H. A. Leite, Mariana B. B. Botura
Summary: The compound ZINC390718 was found to exhibit inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), and showed low cytotoxicity in vitro. Molecular dynamics (MD) simulation revealed that ZINC390718 interacted with the catalytic residue sites of both enzymes. These findings suggest that ZINC390718 could be a potential chemotype for the development of new dual cholinesterase inhibitors.
Article
Chemistry, Medicinal
Tuan Xu, Shuaizhang Li, Andrew J. Li, Jinghua Zhao, Srilatha Sakamuru, Wenwei Huang, Menghang Xia, Ruili Huang
Summary: In this study, machine learning models were developed to predict novel AChE and BChE inhibitors. The models showed good performance in virtual screening and increased the hit rate of assay. A total of 88 novel AChE and 126 novel BChE inhibitors were identified, with significant inhibitory effects. Structure-activity relationship analysis revealed scaffolds for chemistry design and optimization.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2023)
Article
Toxicology
Edward C. Meek, Russell L. Carr, Janice E. Chambers
Summary: The mechanism of toxic action for organophosphates involves persistent inhibition of acetylcholinesterase, leading to hyperstimulation of the nervous system. Differences in their chemistries result in varied metabolism and toxicity. Age-related differences in sensitivity to organophosphates in mammals are primarily influenced by detoxication capacities.
TOXICOLOGY IN VITRO
(2021)
Article
Chemistry, Applied
Halise Yalazan, Didem Akkaya, Gokce Seyhan, Burak Barut, Halit Kantekin
Summary: There is currently no specific treatment for Alzheimer's disease, which is a significant public health concern, especially in developed countries with an aging population. Acetylcholinesterase and butyrylcholinesterase inhibitors have been used to treat this disease. Tyrosinase inhibitors are used preventively for Parkinson's disease, pigmentation disorders, and skin aging. Therefore, there is a need for novel enzyme inhibitors with desirable properties for the treatment of these diseases.
APPLIED ORGANOMETALLIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Saira Naseem, Ahmed Temirak, Aqeel Imran, Saquib Jalil, Shamool Fatima, Parham Taslimi, Jamshed Iqbal, Mussarat Tasleem, Muhammad Nawaz Tahir, Zahid Shafiq
Summary: In this study, new 1,3,4-oxadiazole derivatives were synthesized and tested as novel inhibitors of monoamine oxidase and cholinesterase enzymes. Several compounds showed promising inhibitory effects on these enzymes, with some compounds displaying multitargeting activity. These newly synthesized analogues represent potential lead compounds for the development of neurological disease treatments.
Article
Chemistry, Medicinal
Suat Sari, Seda Onder, Didem Akkaya, Suna Sabuncuoglu, Merve Zengin, Burak Barut, Arzu Karakurt
Summary: This study examined the inhibitory effects of a class of compounds called Azoles on AChE and BChE, and discovered two derivatives with strong inhibition against both wildtype and mutant BChE. Kinetic analysis and molecular modeling further supported these findings and provided insights into the inhibitory behavior of these compounds against mutant BChE forms.
DRUG DEVELOPMENT RESEARCH
(2023)
Article
Integrative & Complementary Medicine
Majid Balaei-Kahnamoei, Mina Saeedi, Arezoo Rastegari, Mohammad Reza Shams Ardekani, Tahmineh Akbarzadeh, Mahnaz Khanavi
Summary: The study demonstrated that Lawsonia inermis L. (henna) seeds can be utilized for memory improvement in Iranian Traditional Medicine, with certain fractions and compounds showing selective inhibition of butyrylcholinesterase, good metal chelating ability, and antioxidant activity.
EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
(2021)
Article
Chemistry, Medicinal
Niels Heise, Sander Friedrich, Veronika Temml, Daniela Schuster, Bianka Siewert, Rene Csuk
Summary: The study demonstrated that the acetylated triterpenoic acids could effectively inhibit the enzyme butyrylcholinesterase (BChE) while showing weak inhibition for acetylcholinesterase (AChE). Enzyme kinetics evaluation revealed hyperbolic inhibition for BChE, and molecular modeling explained the selectivity between AChE and BChE for these compounds.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Organic
Jixing Lai, Chen Yang, Rene Csuk, Baoan Song, Shengkun Li
Summary: The first palladium-catalyzed asymmetric addition of arylboronic acids to coumarins has been successfully developed, providing a straightforward and asymmetric approach for the synthesis of pharmaceutically important 4-aryl-3,4-dihydrocoumarins. This methodology employs easily accessible and stable ligands, has a broad substrate scope, can be conducted under mild reaction conditions, and allows for the accommodation of electron-withdrawing arylboronic acids.
Article
Chemistry, Medicinal
Andreia Fortuna, Rita Goncalves-Pereira, Paulo J. Costa, Radek Jorda, Veronika Vojackova, Gabriel Gonzalez, Niels Heise, Rene Csuk, M. Conceicao Oliveira, Nuno M. Xavier
Summary: This study describes the synthesis and biological evaluation of novel guanidino sugars as isonucleoside analogs. Some of the compounds showed selective inhibition of acetylcholinesterase and moderate antiproliferative effects in chronic myeloid leukemia and breast cancer cells. The most potent compound also exhibited low toxicity in human fibroblasts.
Article
Chemistry, Physical
Satya Kumar Avula, Saeed Ullah, Sobia Ahsan Halim, Ajmal Khan, Muhammad U. Anwar, Rene Csuk, Ahmed Al-Harrasi
Summary: In this study, 26 compounds of substituted quinoline derivatives were synthesized and their alpha-glucosidase inhibition activity was investigated. Most of the synthesized compounds showed good inhibitory activity against alpha-glucosidase, and some exhibited very promising results. Compound 12's structure was confirmed through single crystal X-ray diffraction. The study revealed a new series of substituted quinoline derivatives as potential inhibitors of alpha-glucosidase.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Toni C. Denner, Niels Heise, Julian Zacharias, Oliver Kraft, Sophie Hoenke, Rene Csuk
Summary: Acetylated triterpenoids were transformed into succinyl-spacered acetazolamide conjugates and tested for their inhibitory actvity on carbonic anhydrase II and cytotoxicity on human tumor cell lines and non-malignant fibroblasts. The conjugates derived from betulin and glycyrrhetinic acid showed the strongest inhibition, while those derived from ursolic or oleanolic acid were weaker inhibitors but had lower cytotoxicity. A betulin-derived conjugate displayed a Ki value of 0.129 μM and an EC50 value of 8.5 μM for human A375 melanoma cells.
Article
Chemistry, Medicinal
Najeeb Ur Rehman, Saeed Ullah, Tanveer Alam, Sobia Ahsan Halim, Tapan Kumar Mohanta, Ajmal Khan, Muhammad U. Anwar, Rene Csuk, Satya Kumar Avula, Ahmed Al-Harrasi
Summary: A series of 24 new 1H-1,2,3-triazole hybrids of 3-O-acetyl-11-keto-beta-boswellic acid and 11-keto-beta-boswellic acid were synthesized using click chemistry. These compounds exhibited potent α-glucosidase inhibitory activity and showed interactions with amino acids in the active site.
Article
Chemistry, Multidisciplinary
Niels Heise, Julia Heisig, Linda Ho Hoehlich, Sophie Hoenke, Rene Csuk
Summary: 36 substituted benzylamides were synthesized from maslinic acid, bredemolic acid, and augustic acid, and their cytotoxicity was evaluated in various human tumor cell lines and non-malignant fibroblasts. The benzylamides derived from maslinic acid exhibited higher cytotoxicity compared to those derived from augustic acid or bredemolic acid. The most effective compound (compound 18, derived from maslinic acid) showed an EC50 value of 1.3 μM against A375 melanoma cells. Further staining experiments revealed that this compound primarily induced apoptosis rather than necrosis.
RESULTS IN CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Marie Kozubek, Toni C. Denner, Marc Eckert, Sophie Hoenke, Rene Csuk
Summary: Maslinic acid was converted to rhodamine conjugates with different alkyl moieties, which showed high cytotoxicity, especially for A2780 cells. Among them, a propyl substituted rhodamine conjugate exhibited low EC50 values of EC50 = 0.01 μM and was approximately 15 times more cytotoxic to cancer cells than non-malignant fibroblasts (NIH 3 T3). The cytotoxicity was correlated with the lipophilicity of the residues, suggesting an interaction of the conjugates with the inner mitochondrial membrane as they acted as mitocanes.
RESULTS IN CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Anastasiya V. Petrova, Oxana B. Kazakova, Ivan S. Nazarov, Rene Csuk, Niels V. Heise
Summary: A series of new lupane, ursane, and oleanane type triterpenic A-seco-derivatives containing various functional groups have been synthesized and evaluated for their acetylcholinesterase inhibitory activities. The results showed that the bromo- and azido-derivatives of 28-oxo-allobetuline and betulinic acid exhibited the most potent inhibitory activity against AChE. Further experiments demonstrated the cyano-derivatives of betulinic acid as mixed-type inhibitors with low Ki values.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Chemistry, Medicinal
Oliver Kraft, Anne-Kathrin Hartmann, Sarah Brandt, Sophie Hoenke, Niels V. Heise, Rene Csuk, Thomas Mueller
Summary: Amides and rhodamine B conjugates of pentacyclic triterpene acids have demonstrated excellent cytotoxicity against human tumor cells. The spacer attached to the carboxyl group at ring E determines the cytotoxicity of these conjugates. One acetylated homopiperazinyl spacered rhodamine B conjugate showed high cytotoxicity against ovarian carcinoma cells. These conjugates act as mitocans and induce apoptosis, and have the ability to overcome resistance to standard chemotherapeutic drugs, making them promising candidates for chemotherapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Plant Sciences
Shengxin Sun, Xia Wang, Renei Csuk, Shengkun Li
Summary: Drimane meroterpenoids have attracted attention for their structural diversity and bioactivity, but the lack of an efficient synthetic route has hindered further development. A nickel-catalyzed decarboxylative cross-coupling method has been established to access a variety of drimane meroterpenoids, featuring mild conditions and tolerance for challenging functional groups. This method enables the scalable synthesis of advanced intermediates for late-stage functionalizations, which has led to the discovery of new antifungal leads against Rhizoctonia solani.
JOURNAL OF NATURAL PRODUCTS
(2023)
Article
Chemistry, Medicinal
Niels Heise, Florian Lehmann, Rene Csuk, Thomas Mueller
Summary: This study focuses on the development of triterpenoic acid-rhodamine conjugates with fluorescence shifted to the near-infrared (NIR) region for theranostic applications in cancer research. Spectral analysis revealed emission wavelengths around λ = 760 nm, enabling stronger signals and deeper tissue penetration. The conjugates were evaluated using SRB assays on tumor cell lines and non-malignant fibroblasts, demonstrating low nanomolar activity and high selectivity, similarly to their known rhodamine B counterparts. Additional staining experiments proved their mode of action as mitocans.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Agriculture, Multidisciplinary
Chen Yang, Shengxin Sun, Wei Li, Yushuai Mao, Qiao Wang, Yabing Duan, Renei Csuk, Shengkun Li
Summary: A novel antifungal scaffold, isoquinoline-3-hydrazides, was identified through a bioassay-guided scaffold subtraction. The compound LW3 showed a broad-spectrum antifungal activity and no cross-resistance to commonly used fungicides. This finding highlights the practical potential of isoquinoline hydrazides as a novel model in fungicide innovation.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Niels V. Heise, Toni C. Denner, Selina Becker, Sophie Hoenke, Rene Csuk
Summary: In this study, Asiatic acid was converted into different types of rhodamine conjugates with piperazinyl, homopiperazinyl, and 1,5-diazocinyl spacers. The compounds were tested for cytotoxic activity, and compound 12 showed the highest cytotoxicity with an EC50 of 0.8 nM. However, compound 18, with a ring expanded 1,5-diazocinyl moiety and n-propyl substituents, exhibited the highest selectivity with a selectivity factor of almost 190 while maintaining high cytotoxicity (EC50 = 1.9 nM for A2780 ovarian carcinoma).
Article
Chemistry, Medicinal
Sophie Hoenke, Benjamin Brandes, Rene Csuk
Summary: A non-cytotoxic aza-BODIPY derivative was designed and synthesized in a few simple steps. It was conjugated to 3-O-acetyl-triterpene carboxylic acids and the resulting conjugates exhibited selective targeting of the endoplasmic reticulum.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY REPORTS
(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)
