Article
Chemistry, Multidisciplinary
Seong Gi Lim, Sung Eun Seo, Seongjae Jo, Kyung Ho Kim, Lina Kim, Oh Seok Kwon
Summary: In this study, a fast and convenient approach for screening lead vanilloid compounds targeting TRPV1 was proposed. A graphene field-effect transistor with human TRPV1 receptor protein as the bioprobe was fabricated and verified using various analyses. Simulations and experimental analyses confirmed the binding affinity of the ligands with TRPV1.
Article
Biochemistry & Molecular Biology
Joanna K. Bujak, Daria Kosmala, Kinga Majchrzak-Kuligowska, Piotr Bednarczyk
Summary: The study confirmed the expression of the TRPV1 ion channel on both mRNA and protein levels in canine PBMC, and indicated that the ion channel is functional.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Dmytro Isaev, Keun-Hang Susan Yang, Waheed Shabbir, Frank Christopher Howarth, Murat Oz
Summary: Capsaicin, a natural alkaloid derived from chili pepper, has various pharmacological effects and can affect cardiovascular function by inhibiting ion currents in cardiac myocytes. Therefore, caution should be exercised when administering capsaicin to individuals with cardiac channelopathies or arrhythmia-prone conditions.
Review
Chemistry, Medicinal
Murat Oz, Dietrich E. Lorke, Frank C. Howarth
Summary: Capsaicin, derived from chili pepper, has various pharmacological actions, including analgesic, anticancer, anti-inflammatory, antiobesity, and antioxidant effects. It acts on not only TRPV1 receptor, but also other ion channels and enzymes. This study categorizes the non-TRPV1 targets of capsaicin and discusses the cellular and molecular mechanisms of its TRPV1-independent effects.
MEDICINAL RESEARCH REVIEWS
(2023)
Article
Gastroenterology & Hepatology
Lin Chang, Brian E. Lacy, Baha Moshiree, Amy Kassebaum, Jessica L. Abel, Jennifer Hanlon, Wilmin Bartolini, Ramesh Boinpally, Wieslaw Bochenek, Susan M. Fox, Madhuja Mallick, Ken Tripp, Nicholas Omniewski, Elizabeth Shea, Niels Borgstein
Summary: Linaclotide significantly improved abdominal symptoms related to constipation-predominant irritable bowel syndrome (IBS-C) compared to placebo, including bloating, discomfort, and pain. The study found that linaclotide had a higher overall change from baseline in abdominal score (AS) and a higher responder rate for abdominal symptoms improvement, with diarrhea being the most common side effect. The use of a novel multi-item AS derived from the Diary for IBS Symptoms-Constipation may be valuable in future clinical studies for IBS-C to measure meaningful improvements beyond traditional endpoints.
AMERICAN JOURNAL OF GASTROENTEROLOGY
(2021)
Article
Cell Biology
Ya-Kai Xie, Hao Luo, Shan-Xin Zhang, Xiao-Ying Chen, Ran Guo, Xiao-Yun Qiu, Shuai Liu, Hui Wu, Wen-Bo Chen, Xing-Hua Zhen, Qiang Ma, Jin-Lan Tian, Shun Li, Xinzhong Chen, Qingjian Han, Shumin Duan, Chengyong Shen, Fan Yang, Zhen-Zhong Xu
Summary: This study reveals the mechanisms underlying the development of DNP in patients with diabetes and identifies a potential therapeutic target. The researchers found that GPR177 in A-fiber neurons mediates the secretion of WNT5a, which in turn activates the TRPV1 ion channel and causes pain. These findings contribute to the search for therapies to relieve neuropathic pain.
SCIENCE TRANSLATIONAL MEDICINE
(2022)
Article
Cell Biology
Parisa Vahidi Ferdowsi, Kiran D. K. Ahuja, Jeffrey M. Beckett, Stephen Myers
Summary: Capsaicin activates CAMKK2 and AMPK, leading to increased glucose oxidation and elevated ATP levels, independent of insulin, in differentiated C2C12 cells. Furthermore, capsaicin inhibits the phosphorylation of ERK1/2 in mouse myotubes. Pharmacological inhibition of TRPV1 attenuates these effects. These findings suggest that targeting the TRPV1 channel activation by capsaicin may offer a novel therapeutic approach for managing insulin resistance and T2DM.
Article
Multidisciplinary Sciences
Nicole N. Scheff, Ian M. Wall, Sam Nicholson, Hannah Williams, Elyssa Chen, Nguyen H. Tu, John C. Dolan, Cheng Z. Liu, Malvin N. Janal, Nigel W. Bunnett, Brian L. Schmidt
Summary: Oral cancer patients experience sensitivity to spicy foods and liquids, but the mechanism behind this sensitivity is not yet understood. In a mouse model of oral cancer, researchers found increased expression of TRPV1 in trigeminal ganglion neurons, indicating an anatomical basis for chemosensitivity. They also discovered that PAR(2) plays a role in mediating the sensitivity induced by TRPV1 in tongue afferents in the oral cancer mouse model.
SCIENTIFIC REPORTS
(2022)
Article
Multidisciplinary Sciences
Tianci Li, Gaoge Wang, Vivian Chin Chin Hui, Daniel Saad, Joao de Sousa Valente, Paolo La Montanara, Istvan Nagy
Summary: Increased activity and excitability of molecules like TRPV1 in pain-sensing neurons are crucial for pathological pain. Two major mechanisms, post-translational changes in TRPV1 induced by inflammatory mediators and TRPV1 activation-induced feed-forward signalling, contribute to TRPV1 sensitisation in injured tissues. Upregulation in COX2 expression and increased synthesis of COX2 products play a role in TRPV1 activation-induced sensitisation in nociceptive neurons.
SCIENTIFIC REPORTS
(2021)
Article
Integrative & Complementary Medicine
Shu Han, Liyuan Bao, Weifei Li, Kaiyang Liu, Ya'nan Tang, Xitao Han, Ziqin Liu, Hongyue Wang, Fengting Zhang, Shuo Mi, Hong Du
Summary: This study aimed to investigate the detoxification effects of gallic acid (GA) from Chebulae Fructus (Hezi) on mesaconitine (MA)-induced cardiotoxicity and the underlying mechanism related to the TRPV1 channel. The results showed that GA exhibited significant detoxification effects on MA-induced cardiotoxicity, possibly by inhibiting intracellular Ca2+ influx, restoring mitochondrial membrane potential, and reducing apoptosis. The detoxification mechanism may be related to the desensitization of the TRPV1 channel.
EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
(2022)
Article
Integrative & Complementary Medicine
Chan Zhu, Meiyuan Wang, Jun Guo, Shu Lan Su, Guang Yu, Yan Yang, Yuan Zhou, Zongxiang Tang
Summary: This study found that Angelica dahurica extract has analgesic effects and can effectively alleviate pain responses in a mouse model of inflammatory pain. Additionally, the extract reduces the activity and protein expression of TRPV1 in the dorsal root ganglion. Therefore, Angelica dahurica extract may be a potential agent for the treatment of chronic inflammatory pain.
EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
(2022)
Article
Neurosciences
Olena A. Petrushenko, Anastasiiya O. Stratiievska, Mariia O. Petrushenko, Elena A. Lukyanetz
Summary: This study investigated the dynamics of calcium transients in DRG neurons associated with TRPV1 channel desensitization and the effect of P2 receptor activation on this process. It was found that TRPV1 channels are mainly present in small nociceptive neurons, while P2 receptors are present in all types of neurons. ATP application can restore the response to capsaicin in these neurons.
FRONTIERS IN CELLULAR NEUROSCIENCE
(2023)
Article
Pathology
Siyuan Xu, Shaochan Liang, Ying Pei, Rui Wang, Yao Zhang, Yifei Xu, Bin Huang, Haiwen Li, Juanjuan Li, Bo Tan, Hongying Cao, Shaoju Guo
Summary: This study suggests that dysfunction of TRPV1 channels may contribute to the impaired gastric relaxation in diabetic gastroparesis (DGP) induced by high-fat diet.
AMERICAN JOURNAL OF PATHOLOGY
(2023)
Article
Multidisciplinary Sciences
Isabel Wank, Lisa Kutsche, Silke Kreitz, Peter Reeh, Andreas Hess
Summary: RTX desensitization of TRPV1-signaling disrupts thermal nociception and affects two distinct brain subnetworks, leading to reduced central nervous system responses to high temperatures in male rats. Resting state and graph-theoretical network analyses provide detailed insight into cerebral processing of noxious temperatures.
Article
Medicine, General & Internal
Weslania Nascimento, Noemi Tomsen, Saray Acedo, Cristina Campos-Alcantara, Christopher Cabib, Marta Alvarez-Larruy, Pere Clave
Summary: The study found that age and gender have an impact on spontaneous swallowing frequency in healthy individuals, with older age associated with lower spontaneous swallowing frequency. Gender did not have a significant effect on spontaneous swallowing frequency. Sensory stimulation with TRPV1 agonist capsaicin significantly increased spontaneous swallowing frequency in patients with post-stroke oropharyngeal dysphagia, suggesting a potential therapeutic strategy for central pattern generator activation in these patients.
Editorial Material
Biochemistry & Molecular Biology
Sergio Marques Borghi, Rubia Casagrande, Waldiceu Aparecido Verri
CURRENT MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Patricia H. R. Martins, Adolfo I. B. Romo, Francisco O. N. da Silva, Otaciro R. Nascimento, Joaquin Rodriguez-Lopez, Izaura C. N. Diogenes, Luiz G. F. Lopes, Eduardo H. S. Sousa
Summary: The role and reactivity of metal complexes in interacting with DNA, especially metallonitrosyl compounds, have been poorly investigated. A nitrosyl compound cis-[Ru(bpy)(2)(SO3)(NO)](PF6)(A) exhibited promising biological activities, while a final product cis-[Ru(bpy)(2)(SO3)(H2O](B) showed important reactivity with H2O2 causing DNA degradation. The aqua product of the nitrosyl ruthenium complex should be further studied for its potential genotoxicity to DNA.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Medicine, Research & Experimental
Pedro Martins da Silva, Iury Araujo Paz, Nilberto Robson Falcao do Nascimento, Dieric S. Abreu, Luiz Gonzaga de Franca Lopes, Eduardo Henrique Silva Sousa, Elisane Longhinotti
Summary: Sodium nitroprusside (SNP), a drug used to treat severe hypertension in hospital emergency settings, has emerged with new clinical uses in recent years. This drug functions by releasing nitric oxide (NO), but due to its short lifetime, NO donor molecules are used for administration. Currently, there are various drug delivery strategies that can overcome the limitations of SNP, providing new opportunities for its use. This Perspective highlights the properties of SNP and emphasizes the potential therapeutic uses arising from the use of drug delivery systems such as silica-based nanoparticles.
MOLECULAR PHARMACEUTICS
(2023)
Article
Public, Environmental & Occupational Health
Rafaela Pires Erthal, Glaucia Eloisa Munhoz de Lion Siervo, Giovanna Fachetti Frigoli, Tiago Henrique Zaninelli, Waldiceu Aparecido Verri, Glaura Scantamburlo Alves Fernandes
Summary: This study found that low doses of malathion can impair sperm quality and function by downregulating gene expression, and can also damage the sperm's antioxidant profile during critical periods of development.
JOURNAL OF DEVELOPMENTAL ORIGINS OF HEALTH AND DISEASE
(2023)
Review
Pharmacology & Pharmacy
Sergio M. Borghi, Tiago H. Zaninelli, Jessica B. Carra, Olivia K. Heintz, Marcela M. Baracat, Sandra R. Georgetti, Fabiana T. M. C. Vicentini, Waldiceu A. Verri, Rubia Casagrande
Summary: Asthma is a chronic disease characterized by allergic inflammatory reactions. Current treatment options have limitations and can have adverse effects, leading to poor management of the disease. Flavonoids, with their antioxidant and anti-inflammatory properties, have shown potential benefits for asthma treatment.
Article
Biochemistry & Molecular Biology
Cristina P. B. Melo, Priscila Saito, Renata M. M. Martinez, Larissa Staurengo-Ferrari, Ingrid C. C. Pinto, Camilla C. A. Rodrigues, Stephanie Badaro-Garcia, Josiane A. A. Vignoli, Marcela M. M. Baracat, Allan J. C. Bussmann, Sandra R. R. Georgetti, Waldiceu A. A. Verri, Rubia Casagrande
Summary: This study investigates the protective effect of AT-RvD1 on UVB-induced inflammation and oxidative stress in hairless mice. The results show that AT-RvD1 can restrict various inflammatory and oxidative stress markers and restore the skin's natural antioxidant defense. AT-RvD1 achieves this by upregulating the Nrf2 pathway and promoting the expression of ARE genes.
Article
Chemistry, Medicinal
Tiago H. Zaninelli, Sandra S. Mizokami, Mariana M. Bertozzi, Telma Saraiva-Santos, Felipe A. Pinho-Ribeiro, Gabriele Inacio de Oliveira, Renata Streck, Eduardo J. A. Araujo, Nilton S. Arakawa, Sergio M. Borghi, Rubia Casagrande, Waldiceu A. Verri
Summary: In this study, it was found that kaurenoic acid (KA), extracted from Sphagneticola trilobata, has analgesic properties and can be used for the treatment of neuropathic pain. KA inhibits neuropathic pain induced by chronic constriction injury (CCI) by activating the NO/cGMP/PKG/ATP-sensitive potassium channel signaling pathway. KA also reduces activation of sensory neurons and increases the levels of neuronal nitric oxide synthase (nNOS) and nitric oxide (NO) in dorsal root ganglion (DRG) neurons. These findings suggest that KA inhibits CCI neuropathic pain by activating the nNOS-NO pathway to silence nociceptive signaling.
Article
Biotechnology & Applied Microbiology
Marilia F. Manchope, Mariana M. Bertozzi, Sergio M. Borghi, Cintia L. Handa, Mariana A. Queiroz-Cancian, Camila R. Ferraz, Sandra S. Mizokami, Stephanie Badaro-Garcia, Ketlem C. Andrade, Tiago H. Zaninelli, Wilma A. Spinosa, Sandra R. Georgetti, Elza I. Ida, Waldiceu A. Verri, Rubia Casagrande
Summary: This study evaluates the biological activity of fermented and non-fermented defatted soybean flour (DSF) extracts in pain and inflammation. The results demonstrate that both fermented and non-fermented DSF extracts have analgesic and anti-inflammatory effects, with differences in the mechanism of action depending on the fungi used for fermentation.
FERMENTATION-BASEL
(2023)
Review
Pharmacology & Pharmacy
Tiago H. Zaninelli, Geovana Martelossi-Cebinelli, Telma Saraiva-Santos, Sergio M. Borghi, Victor Fattori, Rubia Casagrande, Waldiceu A. Verri Jr
Summary: Gout arthritis is an intermittent inflammatory disease that affects approximately 10% of the global population. Current therapies are not fully effective and have numerous side effects, highlighting the need for new drug targets and effector molecules in the development of novel treatments for gout arthritis.
EXPERT OPINION ON THERAPEUTIC TARGETS
(2023)
Review
Biochemistry & Molecular Biology
Fernanda S. S. Rasquel-Oliveira, Matheus Deroco Veloso da Silva, Geovana Martelossi-Cebinelli, Victor Fattori, Rubia Casagrande, Waldiceu A. A. Verri Jr
Summary: During infection, inflammation can be harmful when it becomes excessive or chronic. Specialized pro-resolving lipid mediators (SPMs), derived from omega-3 and -6 polyunsaturated fatty acids, play a crucial role in resolving inflammation and promoting a coordinated immune response against pathogens. SPMs regulate leukocyte influx, reduce cytokine and chemokine levels, enhance bacterial clearance, inhibit viral replication, stimulate tissue healing, and decrease antibiotic requirements. Understanding the biosynthesis and effects of SPMs in different infections could have important implications for developing new therapeutic strategies.
Article
Microbiology
Vera Lucia Hideko Tatakihara, Aparecida Donizette Malvezi, Rito Santo Pereira, Bruno Fernando Cruz Lucchetti, Lucas Felipe Dos Santos, Rubens Cecchini, Lucy Megumi Yamauchi, Sueli Fumie Yamada-Ogatta, Katrina M. Miranda, Waldiceu A. Verri, Marli Cardoso Martins-Pinge, Phileno Pinge-Filho
Summary: This study found that a nitric oxide donor called Angeli's salt (AS) can reduce the number of parasites and the severity of Chagas disease in mice. In addition, AS treatment can enhance the antioxidant capacity of infected animals' red blood cells. These results suggest that AS could be a promising therapy for Chagas disease.
Article
Agriculture, Dairy & Animal Science
Suellen Miguez Gonzalez, Marcela Bortoletto Cerezetti, Larissa Zamparone Bergamo, Camila Rodrigues Ferraz, Waldiceu Aparecido Verri Jr, Marcelo Marcondes Seneda
Summary: The aim of this study was to evaluate oxidative stress in ovaries and corpus luteum (CL) of Bos taurus indicus females and the oxidant effect of CL in ovarian tissues. The results showed that luteal tissues had higher antioxidant activity than ovarian tissues, and there was no difference in antioxidant activity and oxidative stress between ovarian fragments obtained from different regions (with or without CL). The presence of CL in the ovaries did not influence oxidative stress or antioxidant potential.
ANIMAL REPRODUCTION
(2023)
Article
Chemistry, Multidisciplinary
Lucas Braganca Carvalho, Isabela Silva Godoy, Ana Cristina Preisler, Patricia Luiza de Freitas Proenca, Telma Saraiva-Santos, Waldiceu Aparecido Verri Jr, Halley Caixeta Oliveira, Giliardi Dalazen, Leonardo Fernandes Fraceto
Summary: In this study, zein nanoparticles associated with the herbicide atrazine were developed and their efficacy in weed control was evaluated. The nanoformulation showed good stability and encapsulation efficiency. It exhibited greater effectiveness against the target plant, Brassica juncea, even at low doses, without causing toxicity to the crop species. The nanoparticles were captured and accumulated in roots but had limited transportation to the shoot. The atrazine nanoencapsulation did not increase the mobility of the herbicide in the soil.
ENVIRONMENTAL SCIENCE-NANO
(2023)
Article
Chemistry, Inorganic & Nuclear
Florencio Sousa Gouveia Junior, Joao Alison de Moraes Silveira, Thais Muratori Holanda, Aline Diogo Marinho, Lisa A. Ridnour, David A. Wink, Rodrigo Jose Bezerra de Siqueira, Helena Serra Azul Monteiro, Eduardo Henrique Silva de Sousa, Luiz Gonzaga de Franca Lopes
Summary: In this study, two new nitrosyl ruthenium complexes were developed and characterized. These complexes showed potential for releasing nitric oxide and nitroxyl, which can be beneficial for cardiovascular diseases. They also demonstrated antioxidant and vasodilating properties.
DALTON TRANSACTIONS
(2023)
Article
Behavioral Sciences
Amine Bahi
Summary: Gestational environmental enrichment (EE) has protective effects on social stress-induced anxiety-like behaviors and excessive ethanol consumption through increasing BDNF levels.
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2024)
Article
Behavioral Sciences
Sarabesh Natarajan, Grant Abass, Lucas Kim, Corinne Wells, Amir H. Rezvani, Edward D. Levin
Summary: Multiple neural systems, including dopamine D1 receptors and glutamate NMDA receptors, are involved in nicotine reinforcement. Acute blockade of D1 receptors decreases nicotine self-administration, while acute blockade of NMDA receptors increases it. Chronic blockade of NMDA receptors decreases nicotine self-administration. Memantine attenuates the decrease in nicotine self-administration caused by chronic D1 antagonist SCH-23390.
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2024)
Article
Behavioral Sciences
David R. Maguire
Summary: The study found that Lorcaserin alone reduces ventilation and enhances the ventilatory-depressant effects of opioids. This suggests that combining a 5-HT2C receptor agonist with opioids may increase the risk of ventilatory depression without reducing abuse.
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2024)
Article
Behavioral Sciences
Fen Liu, Qing Tian, Hui-Ling Tang, Xiang Cheng, Wei Zou, Ping Zhang
Summary: This study demonstrates the attenuating effect of H2S on PD-associated depression by improving hippocampal synaptic plasticity.
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2024)
Article
Behavioral Sciences
Mehrsa Rahimi-Danesh, Mohammad-Ali Samizadeh, Amir-Ehsan Sajadi, Tara Rezvankhah, Salar Vaseghi
Summary: This study investigated the effects of lithium on freezing behavior and pain perception in a fear-conditioning model in rats. The results showed that lithium had no effect on freezing behavior and pain subthreshold in all rats. Extinction training decreased freezing behavior, with more efficacy in females. Gender differences were also observed in the effects of extinction training.
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2024)
