Article
Chemistry, Medicinal
Jose M. Alonso, Alejandro Escobar-Peso, Israel Fernandez, Alberto Alcazar, Jose Marco-Contelles
Summary: By studying the compound quinolylnitrone QN23 and its related compounds, we have identified promising candidates QN4 and QN15 that show high neuroprotective activity in stroke therapy. These compounds exhibit improved potency, tolerability, and solubility compared to the parent compound. Computational analysis suggests that the antioxidant power contributes to their neuroprotective effects. These findings are important for the design and development of future drugs in this field.
Article
Biochemistry & Molecular Biology
Beatriz Chamorro, Sara Izquierdo-Bermejo, Maria Dolores Martin-de-Saavedra, Francisco Lopez-Munoz, Mourad Chioua, Jose Marco-Contelles, Maria Jesus Oset-Gasque
Summary: Ischemic stroke is a major cause of disability and death worldwide, and current therapeutic strategies are limited in their efficacy. Nitrones, known for their antioxidant and anti-inflammatory effects, show great promise as an alternative treatment. In this study, the neuroprotective effects of two nitrones were further investigated and compared with three reference compounds, showing significant neuroprotective effects.
Article
Cell Biology
Yijie Yang, Ning Wang, Li Xu, Yixin Liu, Lulu Huang, Mengyang Gu, Yue Wu, Wenyi Guo, Hao Sun
Summary: Glaucoma is a leading cause of irreversible blindness, characterized by progressive retinal neurodegeneration and local inflammation. This study explores the involvement of aryl hydrocarbon receptor (AhR) and its agonists tryptophan metabolites in glaucoma development. Findings suggest altered serum tryptophan metabolism and reduced retinal AhR expression in glaucoma patients. Additionally, a tryptophan metabolite called ITE can down-regulate retinal inflammation and protect retinal ganglion cells from ischemia/reperfusion injury through AhR activation. The study identifies a potential mechanism involving the limitation of microglial inflammation through ITE. These findings provide new insights for glaucoma treatment by targeting the disrupted AhR signaling resulting from disturbed tryptophan metabolism.
CELL DEATH & DISEASE
(2023)
Article
Chemistry, Multidisciplinary
Katsuhiko Takeuchi, Ming-Yu Chen, Hao-Yu Yuan, Hiroki Koizumi, Kazuhiro Matsumoto, Norihisa Fukaya, Yoong-Kee Choe, Shinji Shigeyasu, Seiji Matsumoto, Satoshi Hamura, Jun-Chul Choi
Summary: The study successfully isolated and characterized a zinc carbamate complex and proposed an improved catalytic system that can efficiently synthesize various carbamates, including industrially important polyurethane raw materials, using CO2 under atmospheric pressure.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Biophysics
Viktoria Hornok, Keristina Wagdi K. Amin, Alexandra N. Kovacs, Adam Juhasz, Gabor Katona, Gyorgy T. Balogh, Edit Csapo
Summary: The encapsulation possibilities of two neuroprotective drugs, KYNA and SzR72, in BSA nanoparticles were studied to enhance their permeability through the blood-brain barrier. Various preparation conditions were tested, and it was found that successful encapsulation could only be achieved when the drugs were added to pre-prepared BSA nanoparticles. Adjusting the pH to 4.0 increased drug loading and caused significant structural changes, indicating drug insertion into the hydrophobic pockets of BSA. In vitro permeability tests showed three- to fourfold higher BBB penetration for encapsulated KYNA compared to the unformatted drug.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2022)
Article
Chemistry, Multidisciplinary
Arkadiusz Listkowski, Natalia Masiera, Michal Kijak, Roman Luboradzki, Barbara Lesniewska, Jacek Waluk
Summary: The researchers analyzed the structural, spectroscopic, and photophysical data of six porphycenes and found a clear correlation between the strength of intramolecular NH....N hydrogen bonds and the efficiency of the nonradiative depopulation of the lowest-excited singlet state. They proposed a new model based on the delocalization of inner protons in the macrocycle cavity as responsible for nonradiative deactivation, which was confirmed by literature data for other alkyl- or aryl-substituted porphycenes.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Biochemistry & Molecular Biology
Jose David Sanchez-Martinez, Monica Bueno, Gerardo Alvarez-Rivera, Jose Tudela, Elena Ibanez, Alejandro Cifuentes
Summary: Orange by-products are a rich source of health-promoting compounds like terpenes, with ethyl acetate extract showing the most promising neuroprotective and antioxidant activities. The study used bioactivity assays and phytochemical profiling to determine the content and activity of beneficial compounds in orange juice by-products. Hydrocarbons mono- and sesquiterpenoids were found to have high potential to cross the blood-brain barrier in vitro.
Review
Biochemistry & Molecular Biology
Awanish Mishra, Pragya Shakti Mishra, Ritam Bandopadhyay, Navneet Khurana, Efthalia Angelopoulou, Yam Nath Paudel, Christina Piperi
Summary: Chrysin, a herbal bioactive molecule, demonstrates various pharmacological effects including antioxidant, anti-inflammatory, neuroprotective, and anti-cancer properties. It has been studied for potential benefits in treating neurological disorders, with a focus on molecular mechanisms and challenges and opportunities in neurotherapeutics.
Article
Dermatology
Young Su Jang, Sugyeong Jeong, A. -ram Kim, Bo Ram Mok, Su Ji Son, Jae-sang Ryu, Woo Sung Son, Seok Kyun Yun, Seunghyun Kang, Hyun Jung Kim, Dong Hyun Kim, Jung U. Shin
Summary: This study investigated the modulation of epidermal differentiation and scavenging of reactive oxygen species by cannabidiol through the aryl hydrocarbon receptor (AhR) in keratinocytes. The results showed that cannabidiol can activate AhR to increase keratinocyte differentiation and antioxidant activity. This suggests the potential use of cannabidiol in improving skin barrier and reducing oxidative stress.
JOURNAL OF DERMATOLOGICAL SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Qing-yu Cui, Xiao-ying Tian, Xi Liang, Zhe Zhang, Rui Wang, Yu Zhou, Hua-xi Yi, Pi-min Gong, Kai Lin, Tong-jie Liu, Lan-wei Zhang
Summary: This study aimed to identify probiotics with the potential to alleviate inflammatory bowel disease and elucidate their mechanism of action. Two strains of Bifidobacterium bifidum, FL-276.1 and FL-228.1, were found to be the most effective in improving body weight loss, colon shortening, and intestinal barrier disruption in mice. It was further discovered that these strains activated the aryl hydrocarbon receptor (AhR) in the intestine, potentially contributing to their anti-inflammatory properties.
Article
Biochemistry & Molecular Biology
ViVi Tang Kang Wee, Hitoshi Shirakawa, Sung-Ling Yeh, Chiu-Li Yeh
Summary: This study investigated the effects of fermented rice bran (FRB) on modulating intestinal aryl hydrocarbon receptor (AhR) expression, innate lymphoid cell (ILC)3 populations, the fecal microbiota distribution, and their associations with dextran sodium sulfate (DSS)-induced acute colitis. The results showed that FRB supplementation can improve gut health, alleviate colitis symptoms, and have anti-colitis effects by enhancing ILC3 and AhR functions.
JOURNAL OF NUTRITIONAL BIOCHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Umapriya Kollu, Vijaya Kumar Reddy Avula, Swetha Vallela, Visweswara Rao Pasupuleti, Grigory Vasilievich Zyryanov, Yugandhar Sreedhar Neelam, Naga Raju Chamarthi
Summary: A new series of urea/thiourea derivatives were efficiently synthesized and characterized for their potential antioxidant activity. Some compounds were found to have blood-brain barrier penetrability and neuroprotective properties for the central nervous system.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Xueyan Liu, Chuanyu Yu, Yuxing Yao, Huifang Lai, Xiaoxia Ye, Jiexin Xu, Jianpeng Guo, Xian Xiao, Chen Lin, Zhihong Huang, Jin Lin, Changxi Yu, Daijun Zha
Summary: We synthesized a series of novel pyromeconic acid-styrene hybrid compounds and evaluated their potential in Alzheimer's disease treatment. The most potent compound, compound 30, exhibited strong inhibitory and disaggregating effects on A beta 1-42 fibril aggregation. It also demonstrated antioxidant, anti-inflammatory, and neuroprotective activities, making it a promising lead candidate for Alzheimer's disease therapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Tamer M. Tamer, Mervat M. ElTantawy, Arina Brussevich, Anna Nebalueva, Alexander Novikov, Ivan Moskalenko, Marwa M. Abu-Serie, Mohamed A. Hassan, Svetlana Ulasevich, Ekaterina Skorb
Summary: In this study, chitosan was modified with 2,2',4,4'-tetrahydroxybenzophenone through Schiff base, resulting in a new derivative with improved biological properties. The structural characterization was done using 1H NMR, FT-IR, and UV-Vis analyses. The thermal analysis showed that the CS-THB derivatives are more stable than chitosan itself. The antioxidant properties were significantly enhanced, and the new derivative showed potential for tissue regeneration applications.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Biochemistry & Molecular Biology
Anna Stasilowicz-Krzemien, Michal Golebiewski, Anita Plazinska, Wojciech Plazinski, Andrzej Miklaszewski, Marcin Zarowski, Zofia Adamska-Jernas, Judyta Cielecka-Piontek
Summary: The preparation of solid dispersions of naringenin with various carriers significantly improved its solubility and biological activity, including enhanced permeability through the gastrointestinal tract and blood-brain barrier, increased antioxidant activity, and enzyme inhibition.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Medicine, Research & Experimental
Miguel M. Garcia, Miguel Molina-Alvarez, Carmen Rodriguez-Rivera, Nancy Paniagua, Ernesto Quesada, Jose Antonio Uranga, Maria Isabel Rodriguez-Franco, David Pascual, Carlos Goicoechea
Summary: Spinal glia plays a crucial role in the development and maintenance of chronic pain. The TLR4 signaling pathway is identified as a key trigger mechanism in pain. By using a CD14/TLR4 antagonist, researchers explored the effects of TLR4 inhibition on pain development and glia activation in different pain models. Their findings suggest that peripheral and central TLR4 have different roles in diverse types of pain.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Biochemistry & Molecular Biology
Beatriz Chamorro, Iwona E. Gtowacka, Joanna Gotkowska, Rafal Gulej, Dimitra Hadjipavlou-Litina, Francisco Lopez-Munoz, Jose Marco-Contelles, Dorota G. Piotrowska, Maria Jesus Oset-Gasque
Summary: This study reports the synthesis, antioxidant, and neuroprotective properties of nucleobase-derived nitrones against an ischemia model. The nitrones with purine and pyrimidine nucleobases showed better neuroprotective effects, while the introduction of methyl or halogen substituents may decrease their neuroprotective activity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Multidisciplinary
Mohammad A. Khasawneh, Ayesha AlKaabi, Abdelouahid Samadi, Priya Antony, Ranjit Vijayan, Lamya Ahmed Al-Keridis, Haythem A. Saadeh, Nael Abutaha
Summary: A series of novel urea and thiourea derivatives of 8-hydroxyquinoline were designed, synthesized, and evaluated for their anticancer activities. The structures of the new compounds were determined using spectroscopic techniques, and their cytotoxicity against breast cancer cell lines was assessed. Molecular docking studies revealed potential interactions between these compounds and proteins associated with breast cancer.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Valeria Kopytina, Lucia Pascual-Anton, Nora Toggweiler, Eva-Maria Arriero-Pais, Lisa Strahl, Patricia Albar-Vizcaino, David Sucunza, Juan J. Vaquero, Sonja Steppan, Dorothea Piecha, Manuel Lopez-Cabrera, Guadalupe-Tirma Gonzalez-Mateo
Summary: This study analyzed the biocompatibility of Steviol glycosides (SG)-based fluids compared to glucose-based fluids and evaluated their impact on the peritoneal membrane. The results showed that SG-based fluids have better ability to protect and maintain the functionality of the peritoneal membrane compared to glucose-based fluids.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Chemistry, Medicinal
Enrique Crisman, Pablo Duarte, Esteban Dauden, Antonio Cuadrado, Maria Isabel Rodriguez-Franco, Manuela G. Lopez, Rafael Leon
Summary: The translation discusses the importance of the transcription factor NRF2 in the antioxidant response and its association with various diseases. The article also explores the innovative strategy of discovering NRF2 activators through KEAP1-NRF2 protein-protein interaction inhibitors and summarizes the known inhibitors and their design features, as well as the preclinical pharmacological properties of these compounds.
MEDICINAL RESEARCH REVIEWS
(2023)
Article
Chemistry, Medicinal
Maria J. Matos, Paula Novo, Lucia Mayan, Iria Torres, Eugenio Uriarte, Matilde Yanez, Jose Angel Fontenla, Francesco Ortuso, Stefano Alcaro, Francesca Procopio, Maria Isabel Rodriguez-Franco, Cristina Val, Maria I. Loza, Jose Brea, Fernanda Borges, Dolores Vina
Summary: Psychiatric and neurological disorders affect millions of people worldwide, and current treatments are limited in their effectiveness. New therapeutic solutions are urgently needed to improve the lives of patients.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Damijan Knez, Daniel Diez-Iriepa, Mourad Chioua, Andrea Gottinger, Milica Denic, Fabien Chantegreil, Florian Nachon, Xavier Brazzolotto, Anna Skrzypczak-Wiercioch, Anze Meden, Anja Pislar, Janko Kos, Simon Zakelj, Jure Stojan, Kinga Salat, Julia Serrano, Ana Patricia Fernandez, Aitana Sanchez-Garcia, Ricardo Martinez-Murillo, Claudia Binda, Francisco Lopez-Munoz, Stanislav Gobec, Jose Marco-Contelles
Summary: This study describes the development of quinolylnitrones (QNs) as multifunctional ligands inhibiting cholinesterases and monoamine oxidases for the therapy of neurodegenerative diseases.
ACTA PHARMACEUTICA SINICA B
(2023)
Article
Multidisciplinary Sciences
Beatriz Chamorro, Sara Izquierdo-Bermejo, Julia Serrano, Dimitra Hadjipavlou-Litina, Mourad Chioua, Francisco Lopez-Munoz, Jose Marco-Contelles, Ricardo Martinez-Murillo, Maria Jesus Oset-Gasque
Summary: Cerebral ischemia is a growing global problem and the leading cause of disability. Researchers have focused on finding neuroprotective drugs that target the molecular processes involved in cerebral ischemia. Six new quinolylnitrones (QNs) have been discovered, which show promising neuroprotective and antioxidant properties against ischemia-reperfusion in neuronal cultures. Among these QNs, QN6 demonstrates the highest antioxidant power and neuroprotective effect, making it a potential candidate for cerebral ischemia therapy.
SCIENTIFIC REPORTS
(2023)
Article
Chemistry, Medicinal
Umberto Maria Battisti, Leticia Monjas, Fady Akladios, Josipa Matic, Eric Andresen, Carolin H. Nagel, Malin Hagkvist, Liliana Haversen, Woonghee Kim, Mathias Uhlen, Jan Boren, Adil Mardinoglu, Morten Grotli
Summary: The inhibition of liver pyruvate kinase is a potential strategy for treating or reversing non-alcoholic fatty liver disease (NAFLD). Urolithin C has been identified as a promising scaffold for developing allosteric inhibitors of liver pyruvate kinase. A comprehensive structure-activity analysis of urolithin C and its analogues was conducted, revealing important chemical features for the desired activity. These findings may facilitate the discovery of more potent and selective PKL allosteric inhibitors.
Article
Chemistry, Organic
Francisco Maqueda-Zelaya, Jose Luis Acena, Estibaliz Merino, Juan J. Vaquero, David Sucunza
Summary: An efficient methodology has been developed for the synthesis of 4-alkoxy- and 4-aryloxybenzo[d][1,2,3]triazines via an intramolecular heterocyclization of 1-azido-2-[isocyano(p-tosyl)methyl]benzenes under basic conditions. DFT calculations were performed to gain a better understanding of the mechanism behind this heterocyclization, which demonstrated good to excellent yields with a broad scope.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Polymer Science
H. M. Abd El-Salam, Ali M. El Shafey, Abdelouahid Samadi, Mahmoud K. Abdel-Latif
Summary: Current research focuses on the removal of iron and ammonia from groundwater using a poly acrylic-poly acrylamide hydrogel grafted with 3-chloroaniline. The effects of agitation time, dosage, and adsorbent temperature on the removal process sensitivity were investigated. The hydrogel showed efficient regeneration and selective removal of iron and ammonia.
Article
Chemistry, Medicinal
Sandra Codony, Jose M. Entrena, Carla Calvo-Tusell, Beatrice Jora, Rafael Gonzalez-Cano, Silvia Osuna, Ruben Corpas, Christophe Morisseau, Belen Perez, Marta Barniol-Xicota, Christian Grinan-Ferre, Concepcion Perez, Maria Isabel Rodriguez-Franco, Anton L. Martinez, M. Isabel Loza, Merce Pallas, Steven H. L. Verhelst, Coral Sanfeliu, Ferran Feixas, Bruce D. Hammock, Jose Brea, Enrique J. Cobos, Santiago Vazquez
Summary: A new benzohomoadamantane-based sEH inhibitor has been developed to improve the drug metabolism and pharmacokinetics properties for pain-related disorders, showing anti-allodynic and analgesic effects in murine models of capsaicin-induced allodynia and cyclophosphamide-induced cystitis.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Tim Keuler, Carina Lemke, Paul W. Elsinghorst, Isabel Iriepa, Mourad Chioua, Maria Angeles Martinez-Grau, Christopher D. Beadle, Tatiana Vetman, Francisco Lopez-Munoz, Timo Wille, Ulrike Bartz, Winnie Deuther-Conrad, Jose Marco-Contelles, Michael Guetschow
Summary: The multifactorial nature of Alzheimer's disease requires the development of drugs that can target different relevant pathways. In this study, we synthesized a series of tailored chromanones and identified compound 19 as a representative compound with balanced pharmacological properties. Compound 19 showed inhibitory activities against human acetyl- and butyrylcholinesterase, monoamine oxidase-B, and high affinity to sigma 1 and sigma 2 receptors.
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE
(2022)
Article
Chemistry, Medicinal
Tim Keuler, Carina Lemke, Paul W. Elsinghorst, Isabel Iriepa, Mourad Chioua, Maria Angeles Martinez-Grau, Christopher D. Beadle, Tatiana Vetman, Francisco Lopez-Munoz, Timo Wille, Ulrike Bartz, Winnie Deuther-Conrad, Jose Marco-Contelles, Michael Gutschow
Summary: The multifactorial nature of Alzheimer's disease necessitates the development of agents that can target multiple relevant pathways. In this study, we synthesized a series of tailored chromanones and evaluated their biological activities. One representative compound (compound 19) was identified, which exhibited balanced pharmacological properties and showed inhibitory activities against acetylcholinesterase, butyrylcholinesterase, monoamine oxidase-B, and high affinity to sigma 1 and sigma 2 receptors. Our findings provide a framework for the development of chromanone-based multineurotarget agents.
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE
(2022)
