Pharmaceuticals最新文献

{"title":"<i>Lilium brownii</i>/<i>Baihe</i> as Nutraceuticals: Insights into Its Composition and Therapeutic Properties.","authors":"Yong-Fei Wang, Zi-Yi An, Le-Qi Yuan, Ting Wang, Wei-Lin Jin","doi":"10.3390/ph17091242","DOIUrl":"https://doi.org/10.3390/ph17091242","url":null,"abstract":"<p><p>Nutraceuticals are compounds or components in food that offer health benefits. They can be incorporated into food to make it functional or used as supplements or medicine. <i>Lilium brownii</i>/<i>Baihe</i> is one of the classic nutraceuticals. The chemical composition of Lilium is complex and has a variety of pharmacological effects. Moreover, the compound preparation based on Lilium has been used in the treatment of respiratory diseases in traditional Chinese medicine. In addition, Lanzhou lily has become food on the dinner table. Therefore, <i>Lilium brownii</i>/<i>Baihe</i> is a nutraceutical with a long history. Based on the current understanding of Lilium, this review provides an in-depth discussion of the bioactive components and pharmacological effects of Lilium. This is important to provide theoretical reference for the in-depth study of Lilium as well as its development and application in medicine, food, and other industries.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3,"publicationDate":"2024-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11434738/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142352298","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Facile Synthesis of <i>N</i>-(4-Bromo-3-methylphenyl)pyrazine-2-carboxamide Derivatives, Their Antibacterial Activities against Clinically Isolated XDR <i>S. Typhi</i>, Alkaline Phosphatase Inhibitor Activities, and Docking Studies.","authors":"Abdul Hannan Khan, Muhammad Bilal, Abid Mahmood, Nasir Rasool, Muhammad Usman Qamar, Muhammad Imran, Sebastian Ionut Toma, Oana Andreescu","doi":"10.3390/ph17091241","DOIUrl":"https://doi.org/10.3390/ph17091241","url":null,"abstract":"<p><p>The emergence of extensively drug-resistant <i>Salmonella</i> Typhi (XDR-<i>S. Typhi</i>) poses a grave public health threat due to its resistance to fluoroquinolones and third-generation cephalosporins. This resistance significantly complicates treatment options, underscoring the urgent need for new therapeutic strategies. In this study, we synthesized pyrazine carboxamides (<b>3, 5a</b>-<b>5d</b>) in good yields through the Suzuki reaction. Afterward, we evaluate their antibacterial activities against XDR-<i>S. Typhi</i> via the agar well diffusion method; <b>5d</b> has the strongest antibacterial activity with MIC 6.25 (mg/mL). Moreover, in vitro Alkaline Phosphatase inhibitor activity was also determined; <b>5d</b> is the most potent compound, with an IC₅₀ of 1.469 ± 0.02 µM. Further, in silico studies were performed to find the type of interactions between synthesized compounds and target proteins.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3,"publicationDate":"2024-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11434897/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142352444","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Study of Potential Blocking Peptides Targeting the SARS-CoV-2 RBD/hACE2 Interaction.","authors":"Sara M Villada-Troncoso, Jenny Andrea Arévalo-Romero, Vanessa Hernández Rivera, Martha Pedraza-Escalona, Sonia M Pérez-Tapia, Angela Johana Espejo-Mojica, Carlos Javier Alméciga-Díaz","doi":"10.3390/ph17091240","DOIUrl":"https://doi.org/10.3390/ph17091240","url":null,"abstract":"<p><strong>Background/objectives: </strong>Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the causative agent of COVID-19, was declared a public health emergency in early 2020. The infection initiates when the receptor-binding domain (RBD) of the viral spike protein binds to human angiotensin-converting enzyme 2 (ACE2). Despite the success of vaccination efforts, the emergence of new variants highlights the ongoing need for treatments targeting these evolving strains. In silico methods previously identified peptides BP2, BP9, and BP11 as being capable of disrupting the RBD-ACE2 interaction, though their efficacy has not been experimentally validated until now.</p><p><strong>Methods: </strong>In this study, these peptides were recombinantly produced in the yeast <i>Komagataella phaffii</i>, and the activity was assessed in vitro using binding assays with multiple RBD variants and the inhibition of the RBD-ACE2 interaction.</p><p><strong>Results: </strong>The production yield for BP2, BP9, and BP11 was 14.34, 4.01, and 1.35 mg per culture liter, respectively. Noteworthy, the three BPs interacted with the RBD of SARS-CoV-2 variants of concern, with BP2 showing higher recognition. Finally, the BPs showed an RBD/hACE2 interaction blocking capacity with IC₅₀ values between 1.03 and 5.35 nM, with BP2 showing the lowest values among the evaluated peptides.</p><p><strong>Conclusions: </strong>These results demonstrate that BP2, specifically, is a promising candidate for the development of novel therapeutic interventions targeting SARS-CoV-2 and other coronaviruses that use hACE2 for cellular entry.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3,"publicationDate":"2024-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11435355/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142352429","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploring Biosurfactants as Antimicrobial Approaches.","authors":"Madalena Lourenço, Noélia Duarte, Isabel A C Ribeiro","doi":"10.3390/ph17091239","DOIUrl":"https://doi.org/10.3390/ph17091239","url":null,"abstract":"<p><p>Antibacterial resistance is one of the most important global threats to human health. Several studies have been performed to overcome this problem and infection-preventive approaches appear as promising solutions. Novel antimicrobial preventive molecules are needed and microbial biosurfactants have been explored in that scope. Considering their structure, these biomolecules can be divided into different classes, glycolipids and lipopeptides being the most studied. Besides their antimicrobial activity, biosurfactants have the advantage of being biocompatible, biodegradable, and non-toxic, which favor their application in several areas, including the health sector. Often, the most difficult infections to fight are associated with biofilm formation, particularly in medical devices. Strategies to overcome micro-organism attachment are thus emergent, and it is possible to take advantage of the antimicrobial/antibiofilm properties of biosurfactants to produce surfaces that are more resistant to the deposition/attachment of bacteria. Approaches such as the covalent bond of biosurfactants to the medical device surface leading to repulsive physical-chemical interactions or contact killing can be selected. Simpler strategies such as the absorption of biosurfactants on surfaces are also possible, eliminating micro-organisms in the vicinity. This review will focus on the physical and chemical characteristics of biosurfactants, their antimicrobial activity, antimicrobial/antibiofilm approaches, and finally on their structure-activity relationship.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11434949/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142352442","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Investigational Study on the Role of <i>CYP2D6</i>, <i>CYP3A4</i> and <i>UGT</i>s Genetic Variation on Fesoterodine Pharmacokinetics in Young Healthy Volunteers.","authors":"Andrea Rodríguez-Lopez, Dolores Ochoa, Paula Soria-Chacartegui, Samuel Martín-Vilchez, Marcos Navares-Gómez, Eva González-Iglesias, Sergio Luquero-Bueno, Manuel Román, Gina Mejía-Abril, Francisco Abad-Santos","doi":"10.3390/ph17091236","DOIUrl":"https://doi.org/10.3390/ph17091236","url":null,"abstract":"<p><p><b><i>Introduction:</i></b> Fesoterodine is one of the most widely used antimuscarinic drugs to treat an overactive bladder. Fesoterodine is extensively hydrolyzed by esterases to 5-hydroxymethyl tolterodine (5-HMT), the major active metabolite. CYP2D6 and CYP3A4 mainly metabolize 5-HMT and are, therefore, the primary pharmacogenetic candidate biomarkers. <b><i>Materials and Methods:</i></b> This is a candidate gene study designed to investigate the effects of 120 polymorphisms in 33 genes (including the CYP, COMT, UGT, NAT2, and CES enzymes, ABC and SLC transporters, and 5-HT receptors) on fesoterodine pharmacokinetics and their safety in 39 healthy volunteers from three bioequivalence trials. <b><i>Results:</i></b> An association between 5-HMT exposure (dose/weight corrected area under the curve (AUC/DW) and dose/weight corrected maximum plasma concentration (C_max/DW)), elimination (terminal half-life (T_1/2) and the total drug clearance adjusted for bioavailability (Cl/F)), and CYP2D6 activity was observed. Poor/intermediate metabolizers (PMs/IMs) had higher 5-HMT AUC/DW (1.5-fold) and C_max/DW (1.4-fold) values than the normal metabolizers (NMs); in addition, the normal metabolizers (NMs) had higher 5-HMT AUC/DW (1.7-fold) and C_max/DW (1.3-fold) values than the ultrarapid metabolizers (UMs). Lower 5-HMT exposure and higher T_1/2 were observed for the CYP3A4 IMs compared to the NMs, contrary to our expectations. <b><i>Conclusions:</i></b> CYP2D6 might have a more important role than CYP3A4 in fesoterodine pharmacokinetics, and its phenotype might be a better predictor of variation in its pharmacokinetics. An association was observed between different genetic variants of different genes of the <i>UGT</i> family and AUC, C_max, and CL/F of 5-HMT, which should be confirmed in other studies.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11435314/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142352315","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Intravitreal Dexamethasone Implant in Anti-Vascular Endothelial Growth Factor Pretreated Diabetic Macular Edema-A Swiss Cohort Study.","authors":"Ferhat Turgut, Gábor M Somfai, Christoph Tappeiner, Katja Hatz, Irmela Mantel, Aude Ambresin, Guy Donati, Viviane Guignard, Dana Nagyová, Isabel B Pfister, Christine Schild, Justus G Garweg","doi":"10.3390/ph17091235","DOIUrl":"https://doi.org/10.3390/ph17091235","url":null,"abstract":"<p><strong>Background/objectives: </strong>Diabetic macular edema (DME) is a significant cause of visual impairment, often treated with anti-vascular endothelial growth factor (anti-VEGF) agents. However, some patients do not respond adequately to this treatment. This study aims to evaluate the contribution of the intravitreal dexamethasone (DEX) implant as a second-line treatment in DME patients with insufficient response to anti-VEGF therapy or with high treatment burden.</p><p><strong>Methods: </strong>This retrospective multicenter cohort study was conducted across seven clinical sites in Switzerland. The study included eyes with active DME that had been pretreated with anti-VEGF for at least six months before receiving DEX therapy. Data were extracted from electronic patient records, focusing on best-corrected visual acuity (BCVA), central subfield thickness (CST), and injection frequency.</p><p><strong>Results: </strong>A total of 95 eyes from 89 patients (38.8% females, mean age 65.6 ± 9.1 years, follow-up time 80.6 ± 38.5 [13.5-166.7] months) were analyzed. Prior to the first DEX implant, eyes had undergone an average of 16.0 ± 13.3 anti-VEGF injections over 32.5 ± 22.4 months. Post-DEX treatment, 22.1% of eyes received DEX monotherapy, 44.2% received a combination of DEX and anti-VEGF, 25.3% continued with anti-VEGF monotherapy, and 8.4% received no further treatment. The number of anti-VEGF injections decreased significantly from 6.4 ± 3.1 in the year before DEX to 1.6 ± 2.4 in the year after DEX (<i>p</i> < 0.001). BCVA remained stable (0.4 ± 0.3 logMAR at baseline, 0.4 ± 0.5 logMAR at 24 months, <i>p</i> = 0.2), while CST improved from 477.7 ± 141.0 to 320.4 ± 125.5 μm (<i>p</i> < 0.001), and the presence of retinal fluid decreased from 98.0% to 61.1% (<i>p</i> = 0.021). During follow-up, 26.3% of eyes required glaucoma medication, 4.2% underwent glaucoma surgery, and 1.1% needed cataract surgery.</p><p><strong>Conclusions: </strong>In real-world clinical settings, the addition of DEX to anti-VEGF therapy in DME patients significantly reduces treatment burden and retinal fluid while maintaining visual function. Treatment decisions should balance anatomical and functional outcomes, considering individual patient needs.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11434786/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142352466","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Mechanisms of NMDA Receptor Inhibition by Biguanide Compounds.","authors":"Arseniy S Zhigulin, Anastasiya O Novikova, Oleg I Barygin","doi":"10.3390/ph17091234","DOIUrl":"https://doi.org/10.3390/ph17091234","url":null,"abstract":"<p><p>N-methyl-D-aspartate (NMDA) receptors are inhibited by many medicinal drugs. The recent successful repurposing of NMDA receptor antagonists ketamine and dextromethorphan for the treatment of major depressive disorder further enhanced the interest in this field. In this work, we performed a screening for the activity against native NMDA receptors of rat CA1 hippocampal pyramidal neurons among biguanide compounds using the whole-cell patch-clamp method. Antimalarial biguanides proguanil and cycloguanil, as well as hypoglycemic biguanide phenformin, inhibited them in micromolar concentrations, while another hypoglycemic biguanide metformin and antiviral biguanide moroxydine were practically ineffective. IC₅₀ values at -80 mV holding voltage were 3.4 ± 0.6 µM for cycloguanil, 9.0 ± 2.2 µM for proguanil and 13 ± 1 µM for phenformin. The inhibition by all three compounds was not competitive. Cycloguanil acted as an NMDA receptor voltage-dependent trapping channel blocker, while proguanil and phenformin acted as allosteric inhibitors. Our results support the potential clinical repurposing of biguanide compounds for the treatment of neurodegenerative disorders linked to glutamatergic excitotoxicity while also providing a better understanding of structural determinants of NMDA receptor antagonism by biguanides.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11434645/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142352471","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Rat Sympathetic Neuron Calcium Channels Are Insensitive to Gabapentin.","authors":"Mallory B Scott, Paul J Kammermeier","doi":"10.3390/ph17091237","DOIUrl":"https://doi.org/10.3390/ph17091237","url":null,"abstract":"<p><p>The gabapentenoids such as gabapentin (GP) and pregabalin are approved for the treatment of chronic pain, but their utility is limited by persistent side effects. These adverse effects result from GPs affecting many types of neurons and muscle cells, not just the pain-sensing neurons that are the intended targets. We have recently discovered a type of peripheral neuron, rat sympathetic neurons from the superior cervical ganglion (SCG), that is uniquely insensitive to GP effects. Currents were measured using whole-cell patch-clamp electrophysiology from cells in primary culture from either the SCG or the Nodose Ganglion (NDG) as a positive control for the effects of GP. We find that the calcium current density was dramatically reduced by GP pretreatment in NDG neurons, but that neurons from the SCG were resistant. Further, when GP was cytoplasmically injected into these neurons, the resistance of SCG neurons to GP treatment persisted. These data demonstrate that rat sympathetic neurons appear to be uniquely resistant to GP treatment. These results may help us to better understand the mechanism of action of, and resistance to, GP in altering calcium channel current density, which may help to develop future treatments with fewer side effects.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11435301/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142352410","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Multitarget-Directed Ligands Hitting Serotonin Receptors: A Medicinal Chemistry Survey.","authors":"Imane Ghafir El Idrissi, Angela Santo, Enza Lacivita, Marcello Leopoldo","doi":"10.3390/ph17091238","DOIUrl":"https://doi.org/10.3390/ph17091238","url":null,"abstract":"<p><p>Serotonin (5-hydroxytryptamine, 5-HT) is a ubiquitous neurotransmitter in the human body. In the central nervous system, 5-HT affects sleep, pain, mood, appetite, and attention, while in the peripheral nervous system, 5-HT modulates peristalsis, mucus production, and blood vessel dilation. Fourteen membrane receptors mediate 5-HT activity. In agreement with the crucial roles played by 5-HT, many drugs target 5-HT receptors (5-HTRs). Therefore, it is unsurprising that many efforts have been devoted to discovering multitarget-directed ligands (MTDLs) capable of engaging one or more 5-HTRs plus another target phenotypically linked to a particular disease. In this review, we will describe medicinal chemistry efforts in designing MTDLs encompassing activity for one or more 5-HTRs, starting with atypical antipsychotics and moving to dual 5-HT1AR/serotonin transporter ligands, 5-HT6R antagonists/acetyl cholinesterases inhibitors, and 5-HT4R agonists/acetyl cholinesterases inhibitors. We will also provide an outlook on the most recent efforts made in the field.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142352384","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Anti-Arthritic Potential of the Ethanolic Extract of <i>Salvia Lachnostachys</i> Benth. Leaves and Icetexane Dinor-Diterpenoid Fruticuline B.","authors":"Natália de M Balsalobre, Elisangela Dos Santos-Procopio, Cristhian S Oliveira, Silvia C Neves, Maria H Verdan, Saulo E Silva-Filho, Rodrigo J Oliveira, Maria É A Stefanello, Cândida A L Kassuya","doi":"10.3390/ph17091226","DOIUrl":"https://doi.org/10.3390/ph17091226","url":null,"abstract":"<p><p>The decoction of <i>Salvia lachnostachys</i> Benth. leaves is used in Brazilian folk medicine for anti-spasmodic, antipyretic, and anxiolytic purposes. Some of the biological effects of an <i>S. lachnostachys</i> extract have been shown to be anti-inflammatory, anti-cancer, and antidepressant effects. In addition, this medicinal plant produces several compounds including icetexane diterpenoids, such as fruticuline A and fruticuline B. The aim of the present work was to evaluate the anti-hyperalgesic and anti-inflammatory properties of fruticuline B (FRUT B) and the ethanolic extract obtained from the leaves of <i>S. lachnostachys</i> (EESL) in experimental mouse models. EESL (30, 100, and 300 mg/kg) and FRUT B (1 mg/kg) were evaluated in articular inflammation-induced models in <i>Swiss</i> mice. In articular inflammation induced by Zymosan, EESL (300 mg/kg) and FRUT B (1 mg/kg) significantly reduced mechanical hyperalgesia (83.17% inhibition for EESL and 81.19% for FRUT B); edema (68.75% reduction for EESL and 33.66% for FRUT B); leukocyte migration (81.3% for EESSL and 92.2% for FRUT B), and nitric oxide production (88.3% for EESL and 74.4% for FRUT B). The exposure to fruticuline B significantly inhibited the edema (51.5%), mechanical (88.12%) and cold hyperalgesia (80.8%), and myeloperoxidase (MPO) (63.4%) activity 24 h after CFA injection. In the pleurisy model, FRUT B reduced 89.1% of leukocyte migration and 50.3% in nitric oxide production. Four hours after carrageenan injection, FRUT B (1 mg/kg) diminished 89.11% of mechanical hyperalgesia, 65.8% of paw edema, and 82.12% of the response to cold hyperalgesia. In the MTT test, EESL and fruticuline B caused no cytotoxicity. The present study revealed, for the first time, the anti-arthritic and anti-nociceptive effects of FRUT B, pointing out the therapeutic potential of the species to control inflammation and nociception. Future studies are needed to evaluate other biological properties of fruticuline B and to better understand its mechanism of action.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11435285/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142352449","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}