Article
Medicine, Research & Experimental
Elif Sahin, Neslihan Saglam, Seniz Erdem, Elif Alvuroglu, Ismail Abidin, Esin Yulug, Ahmet Alver
Summary: This study investigated the effect of 7,8-Dihydroxyflavone (7,8-DHF) on Endoplasmic Reticulum Stress (ERS) in liver and pancreas tissues. The findings showed that 7,8-DHF significantly reduced metabolic abnormalities and suppressed ERS-induced metabolic disorders in both liver and pancreas.
Article
Biochemistry & Molecular Biology
Rajib Paul, Joyobrato Nath, Satinath Paul, Muhammed Khairujjaman Mazumder, Banashree Chetia Phukan, Rubina Roy, Pallab Bhattacharya, Anupom Borah
Summary: 7,8-dihydroxyflavone (DHF) is a naturally-occurring flavone with neuroprotective properties that can combat various neurological disorders, exhibiting antioxidant and anti-inflammatory effects.
NEUROCHEMISTRY INTERNATIONAL
(2021)
Review
Food Science & Technology
Marco Emili, Sandra Guidi, Beatrice Uguagliati, Andrea Giacomini, Renata Bartesaghi, Fiorenza Stagni
Summary: Flavonoids, especially 7,8-Dihydroxyflavone (7,8-DHF), have shown potential as a treatment for brain and body pathologies. A comprehensive review of more than 180 preclinical studies reveals promising results, suggesting the usefulness of 7,8-DHF supplementation as therapy or adjuvant for these conditions.
CRITICAL REVIEWS IN FOOD SCIENCE AND NUTRITION
(2022)
Article
Endocrinology & Metabolism
Zhenlei Zhao, Fan Xue, Yanpei Gu, Jianxin Han, Yingxian Jia, Keqiang Ye, Ying Zhang
Summary: This study showed that 7,8-DHF can protect the function of the female HPO axis and activate tissue-specific ERa, highlighting its potential as a therapeutic strategy for managing MetS in women.
MOLECULAR METABOLISM
(2021)
Article
Medicine, General & Internal
Aihua Yu, Shun Wang, Yiqiao Xing, Mengyao Han, Kun Shao
Summary: This study investigated the protective role of a selective TrkB agonist DHF in retinal ischemia-reperfusion injury (RIRI). The results showed that DHF administration reduced apoptosis and inflammation induced by RIRI through activating TrkB signaling pathway and downstream Akt and Erk signaling pathways. DHF may serve as a promising drug candidate for RIRI related ophthalmopathy.
INTERNATIONAL JOURNAL OF MEDICAL SCIENCES
(2022)
Article
Neurosciences
Maddison R. Johnstone, Rhys D. Bradyz, Jarrod E. Church, David Orr, Stuart J. McDonald, Brian L. Grills
Summary: The study revealed that treatment with 7,8-DHF had a negative impact on fracture healing in mice, leading to decreased tissue volume and biomechanical properties post-fracture. However, in cell experiments, 7,8-DHF did not affect gene expression or mineralization of osteoprogenitor cells.
JOURNAL OF MUSCULOSKELETAL & NEURONAL INTERACTIONS
(2021)
Article
Biology
Fan Xue, Zhenlei Zhao, Yanpei Gu, Jianxin Han, Keqiang Ye, Ying Zhang
Summary: The study demonstrates that both BDNF and 7,8-DHF promote the proliferation, differentiation, and mineralization of osteoblasts through the activation of the Wnt/beta-catenin signaling pathway. Additionally, 7,8-DHF inhibits osteoclast differentiation and improves bone mass and structure in an OVX rat model, indicating its dual regulatory effects on bone remodeling.
Article
Clinical Neurology
Annunziata Guarino, Barbara Bettegazzi, Nimra Aziz, Mario Barbieri, Daniela Bochicchio, Lucia Crippa, Pietro Marino, Maddalena Sguizzato, Marie Soukupova, Silvia Zucchini, Michele Simonato
Summary: Temporal lobe epilepsy often appears after an initial epileptogenic insult and may be preventable. This study tested the antioxidant agent 7,8-dihydroxyflavone (7,8-DHF) as an anti-epileptogenic drug and found that low-dose 7,8-DHF effectively reduced the frequency of seizures in the experimental model.
Article
Engineering, Biomedical
Wenbi Wu, Yinchu Dong, Haofan Liu, Xuebing Jiang, Ling Yang, Jing Luo, Yu Hu, Maling Gou
Summary: In this study, an elastic hydrogel conduit encapsulating with drug-releasable nanoassemblies was fabricated using a 3D printing technique, showing potential for promoting nerve regeneration. The conduit sustainedly released the drug and facilitated axon elongation, resulting in axon regeneration, remyelination, and function recovery. These findings suggest that the drug-loaded hydrogel conduit has potentials for the treatment of long-gap peripheral nerve injury.
MATERIALS TODAY BIO
(2023)
Article
Biotechnology & Applied Microbiology
Pragya Prasanna, Prakash Kumar, Saptarshi Mandal, Tanvi Payal, Saurabh Kumar, Sk Ugir Hossain, Prolay Das, V Ravichandiran, Debabrata Mandal
Summary: Gold nanoparticles synthesized with 7,8-dihydroxyflavone exhibit high biological activity against Leishmania donovani, inhibiting the activity of the parasite's enzyme. Additionally, a Th1/Th2-mediated cytokine response in macrophages indicates cell death in response to the nanoparticles.
Article
Biochemistry & Molecular Biology
Peng-Zhou Hang, Feng-Qin Ge, Man-Ru Zhang, Qi-Hang Li, Hua-Qing Yu, Yu-Chen Song, Dan-Dan Guo, Jing Zhao, Hua Zhu
Summary: The mimetic of brain-derived neurotrophic factor, 7,8-DHF, improves mitochondrial function and cardiac function in cardiovascular disease. It effectively prevents cell death induced by mitochondrial dysfunction and enhances mitochondrial membrane potential, reducing reactive oxygen species. Furthermore, it restores respiratory function and ATP production in cardiomyocytes.
FREE RADICAL BIOLOGY AND MEDICINE
(2023)
Article
Biochemistry & Molecular Biology
Jing Zhao, Peifeng Li, Hua Zhu, Fengqin Ge, Jie Liu, Jingjun Xia, Pengzhou Hang
Summary: Recent studies have shown that 7,8-dihydroxyflavone (7,8-DHF) can inhibit the development of osteosarcoma by regulating Akt/Bad and MAPK signaling pathways. This study demonstrated that 7,8-DHF reduced cell viability, promoted apoptosis, inhibited migration, and induced oxidative stress in osteosarcoma cells. The findings suggest potential pharmacological effects of 7,8-DHF for improving drug therapy in osteosarcoma patients.
ACTA BIOCHIMICA ET BIOPHYSICA SINICA
(2021)
Article
Neurosciences
Sarah Otzkan, Walter E. Muller, W. Gibson Wood, Gunter P. Eckert
Summary: The study showed that 7,8-DHF restored levels of Rho proteins Rac1 and Rab3A in membrane preparations from brains of aged mice, without affecting BDNF and TrkB levels. Additionally, Tiam1 levels were restored by 7,8-DHF treatment in aged mice brains.
NEUROMOLECULAR MEDICINE
(2021)
Article
Pharmacology & Pharmacy
Peng-Zhou Hang, Jie Liu, Jia-Pan Wang, Feng-Feng Li, Pei-Feng Li, Qing-Nan Kong, Jing Shi, Hong-Yu Ji, Zhi-Min Du, Jing Zhao
Summary: 7,8-DHF attenuates cardiac fibrosis and regulates circadian rhythmic signals, at least partly, by inhibiting the Bmal1/Akt pathway.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Nutrition & Dietetics
Priyanka Sharma, Camila Silva, Sarah Pfreundschuh, Hong Ye, Harini Sampath
Summary: This study establishes for the first time the requirement for the gut microbiome in mediating the metabolic effects of DHF in female mice and uncovers a novel target tissue that may mediate these sexually-dimorphic protective effects.
FRONTIERS IN NUTRITION
(2022)
Article
Behavioral Sciences
Anthony L. Riley, Katharine H. Nelson, Peter To, Raul Lopez-Arnau, Peng Xu, Dan Wang, Youmei Wang, Hao-wei Shen, Donald M. Kuhn, Mariana Angoa-Perez, John H. Anneken, Dawn Muskiewicz, F. Scott Hall
NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS
(2020)
Article
Clinical Neurology
Leticia Duart-Castells, Lidia Cantacorps, Raul Lopez-Arnau, Sandra Montagud-Romero, Brigitte Puster, Paula Mera, Dolors Serra, Jorge Camarasa, David Pubill, Olga Valverde, Elena Escubedo
Summary: The study found that feeding young female mice with a high-fat diet increased triglyceride levels in the blood, while prenatal and lactation alcohol exposure affected female responses to the high-fat diet and cocaine. There was an interaction between these effects.
INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Mireia Casanovas, Irene Reyes-Resina, Alejandro Lillo, Jaume Lillo, Raul Lopez-Arnau, Jorge Camarasa, Elena Escubedo, Gemma Navarro, Rafael Franco
Summary: The study found that methamphetamine affects the function of A(2A) and CB1 receptors, blocking the activation of the MAPK pathway.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Neurosciences
L. Duart-Castells, N. Nadal-Gratacos, M. Muralter, B. Puster, X. Berzosa, R. Estrada-Tejedor, M. Niello, S. Bhat, D. Pubill, J. Camarasa, H. H. Sitte, E. Escubedo, R. Lopez-Arnau
Summary: The study highlights the role of amino terminal substitution in the pharmacological profile of novel synthetic cathinones, including their potency in inhibiting dopamine uptake and inducing psychostimulant and rewarding effects in mice. The results demonstrate a significant correlation between predicted binding affinities by molecular docking and affinity constants for human dopamine transporter, indicating the importance of amino substitutions in determining the biological activity of these compounds.
Article
Biochemistry & Molecular Biology
Laia Alegre-Zurano, Raul Lopez-Arnau, Miguel A. Lujan, Jordi Camarasa, Olga Valverde
Summary: Experimental results show that CBD has a mitigating effect on MDPV-induced conditioned place preference, but exacerbates drug-seeking and taking behaviors in high-responders during MDPV self-administration. CBD exhibits an anxiolytic-like effect exclusively in mice treated with MDPV.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Substance Abuse
Antonio Verdejo-Garcia, Lauren Hanegraaf, Maria Carmen Blanco-Gandia, Raul Lopez-Arnau, Marina Grau, Jose Minarro, Elena Escubedo, David Pubill, Marta Rodriguez-Arias
Summary: The study revealed that individuals with methamphetamine dependence who started using the drug during adolescence exhibited higher antisocial beliefs and poorer emotion recognition compared to those who started using during adulthood. Experiments on mice showed that exposure to methamphetamine during adolescence specifically decreased social investigation during social interaction and had neurochemical effects on the striatal dopaminergic system. These findings suggest heightened sensitivity to methamphetamine effects on social cognition during adolescence.
DRUG AND ALCOHOL DEPENDENCE
(2022)
Article
Biochemistry & Molecular Biology
Nuria Nadal-Gratacos, Esther Lleixa, Monica Gibert-Serramia, Roger Estrada-Tejedor, Xavier Berzosa, Xavier Batllori, David Pubill, Jordi Camarasa, Elena Escubedo, Raul Lopez-Arnau
Summary: Changes in the molecular structure of synthetic cathinones have led to an increase in the number of novel emerging drugs in the illicit drug market. This study investigates the effects of para- and meta-halogen substitutions on the in vivo, in vitro, and in silico effects of alpha-PVP derivatives. The study provides evidence of the rewarding and anxiety-like properties of halogenated alpha-PVP derivatives.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Maria Espinosa-Velasco, Marina D. Reguilon, Marina Bellot, Nuria Nadal-Gratacos, Xavier Berzosa, Pol Puigseslloses, Cristian Gomez-Canela, Marta Rodriguez-Arias, David Pubill, Jordi Camarasa, Elena Escubedo, Raul Lopez-Arnau
Summary: The research demonstrates that acute use of NEP can lead to anxiolytic effects, aggressive behavior, and social exploration deficits, which persist during withdrawal. Furthermore, repeat use of NEP can result in hyperthermia and depressive symptoms, possibly due to decreases in serotonin and noradrenaline levels. Additionally, the long-term increase in Delta FosB levels in the striatum after chronic NEP use indicates a high risk of dependence.
JOURNAL OF NEUROCHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Nuria Nadal-Gratacos, Ana Sofia Alberto-Silva, Miriam Rodriguez-Soler, Edurne Urquizu, Maria Espinosa-Velasco, Kathrin Jaentsch, Marion Holy, Xavier Batllori, Xavier Berzosa, David Pubill, Jordi Camarasa, Harald H. Sitte, Elena Escubedo, Raul Lopez-Arnau
Summary: The study investigated the structure-activity relationships of six novel synthetic cathinones, revealing potent dopamine uptake inhibition and varying effects on serotonin transporters. These synthetic cathinones exhibited different psychostimulant effects and rewarding properties in mice, providing valuable information for understanding their mechanisms of action in addiction.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Juliette Bedrossiantz, Marina Bellot, Pol Dominguez-Garcia, Melissa Faria, Eva Prats, Cristian Gomez-Canela, Raul Lopez-Arnau, Elena Escubedo, Demetrio Raldua
Summary: This study successfully established a zebrafish model of METH-induced neurotoxicity, demonstrating a concentration- and time-dependent decrease in dopamine, norepinephrine, and serotonin levels in METH-exposed fish. Behavioral changes included hyperactivity, positive geotaxis, and negative scototaxis, as well as social isolation, while transcriptional changes indicated alterations in gene expression related to neuronal injury.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Chemistry, Analytical
Marina Bellot, Maria Espinosa-Velasco, Raul Lopez-Arnau, Elena Escubedo, Cristian Gomez-Canela
Summary: This study evaluated the performance of liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) for the determination of multi-class monoamine neurotransmitters in mouse brain, and found significant differences in concentration levels of catecholamine neurotransmitters between brain regions.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2022)
Article
Clinical Neurology
Maria Espinosa-Velasco, Marina D. Reguilon, Marina Bellot, Nuria Nadal-Gratacos, Xavier Berzosa, Cristian Gomez-Canela, Marta Rodriguez-Arias, Jordi Camarasa, Elena Escubedo, David Pubill, Raul Lopez-Arnau
Summary: NEPD is a synthetic cathinone derivative with significant effects on behavior and neurochemistry in mice. Acute use induces anxiolytic effects, while withdrawal after repeated use leads to increased aggressiveness and locomotor activity.
PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
(2022)
Review
Psychiatry
Raul Lopez-Arnau, Jordi Camarasa, Marcel Li Carbo, Nuria Nadal-Gratacos, Pol Puigseslloses, Maria Espinosa-Velasco, Edurne Urquizu, Elena Escubedo, David Pubill
Summary: The utility of classical drugs used to treat psychiatric disorders is often limited, and psychoactive substances have shown potential as alternative treatments for certain disorders. The use of new psychoactive substances has expanded the options for treating these disorders.
FRONTIERS IN PSYCHIATRY
(2022)
Article
Pharmacology & Pharmacy
Paola Orlandi, Marta Banchi, Francesca Vaglini, Marco Carli, Stefano Aringhieri, Arianna Bandini, Carla Pardini, Cristina Viaggi, Michele Lai, Greta Ali, Alessandra Ottani, Eleonora Vandini, Patrizia Guidi, Margherita Bernardeschi, Veronica La Rocca, Giulio Francia, Gabriella Fontanini, Mauro Pistello, Giada Frenzilli, Daniela Giuliani, Marco Scarselli, Guido Bocci
Summary: This study investigates the role of MC4R in melanoma and the use of the selective antagonist ML in combination with vemurafenib. The results show that ML can inhibit melanoma cell proliferation and induce apoptosis through the inhibition of ERK1/2 phosphorylation and reduction of BCL-XL expression. The combination of vemurafenib and ML exhibits a synergistic effect in vitro and inhibits tumor growth in vivo without causing adverse effects.
BIOCHEMICAL PHARMACOLOGY
(2024)
Article
Pharmacology & Pharmacy
Conor J. Bloxham, Katina D. Hulme, Fabrizio Fierro, Christian Fercher, Cassandra L. Pegg, Shannon L. O'Brien, Simon R. Foster, Kirsty R. Short, Sebastian G. B. Furness, Melissa E. Reichelt, Masha Y. Niv, Walter G. Thomas
Summary: Bitter taste receptors (T2Rs) are a type of G protein-coupled receptors that allow humans to detect aversive and toxic substances. This study characterized the functional properties of previously identified T2Rs in human cardiac tissues and their naturally occurring polymorphisms. The results showed differences in signaling among different T2R variants, and revealed a potential association between the T2R50 Tyr203 variant and cardiovascular disease.
BIOCHEMICAL PHARMACOLOGY
(2024)
Article
Pharmacology & Pharmacy
Lu Chen, Huanying Shi, Wenxin Zhang, Yongjun Zhu, Haifei Chen, Zimei Wu, Huijie Qi, Jiafeng Liu, Mingkang Zhong, Xiaojin Shi, Tianxiao Wang, Qunyi Li
Summary: This study demonstrates that Carfilzomib exhibits potent anti-tumor activity against esophageal squamous cell carcinoma (ESCC) by triggering mitochondrial apoptosis and reprogramming cellular metabolism. It has been identified that activating transcription factor 3 (ATF3) plays a crucial role as a cellular target in ESCC cells treated with Carfilzomib. Overexpression of ATF3 effectively counteracts the effects of Carfilzomib on ESCC cell proliferation, apoptosis, and metabolic reprogramming. Furthermore, ATF3 mediates the anti-tumor activity of Carfilzomib, suggesting its potential as a therapeutic agent for ESCC.
BIOCHEMICAL PHARMACOLOGY
(2024)
Review
Pharmacology & Pharmacy
Xing Zhang, Xiang Li, Ran Xia, Hong-Sheng Zhang
Summary: This review summarizes recent progress on the mechanisms of ferroptosis resistance in cancer and highlights the role of redox status and metabolism. Combination therapy for ferroptosis has great potential in treating resistant malignant tumors.
BIOCHEMICAL PHARMACOLOGY
(2024)