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Therapeutic potential and bioactive compounds of Apium graveolens: A phytopharmacological review 荆芥的治疗潜力和生物活性成分:植物药理学综述
Pharmacological Research - Reports Pub Date : 2025-03-01 Epub Date: 2025-04-29 DOI: 10.1016/j.prerep.2025.100039
Ghadi Daoud , Farogh Ahsan , Tarique Mahmood , Shahzadi Bano , Vaseem Ahamad Ansari , Syed Mehdi Hasan Zaidi , Jamal Akhtar Ansari
{"title":"Therapeutic potential and bioactive compounds of Apium graveolens: A phytopharmacological review","authors":"Ghadi Daoud ,&nbsp;Farogh Ahsan ,&nbsp;Tarique Mahmood ,&nbsp;Shahzadi Bano ,&nbsp;Vaseem Ahamad Ansari ,&nbsp;Syed Mehdi Hasan Zaidi ,&nbsp;Jamal Akhtar Ansari","doi":"10.1016/j.prerep.2025.100039","DOIUrl":"10.1016/j.prerep.2025.100039","url":null,"abstract":"<div><div><em>Apium graveolens</em> (<em>A. graveolens</em>), often referred to as celery, is a widely consumed vegetable with a long history of use in traditional medicine. It offers numerous health advantages, such as anti-inflammatory, antioxidant, and antihypertensive properties. Celery is used in both traditional medicine and modern pharmacology for its therapeutic effects. This review is justified to consolidate recent research on its medicinal properties. Emphasizing its therapeutic potential can steer future research and practical applications in pharmaceuticals, enhancing comprehension of its health benefits and encouraging its use in various treatments. Phytochemical studies have discovered numerous bioactive compounds in <em>A. graveolens</em>, such as flavonoids, phenolic acids, coumarins, and essential oils, all of which play a role in its extensive pharmacological effects. Studies have demonstrated that <em>A. graveolens</em> exhibits antioxidant, anti-inflammatory, antimicrobial, antihypertensive, antidiabetic, hepatoprotective, and other pharmacological effects. The presence of compounds such as apigenin, luteolin, and phthalides plays a pivotal role in these therapeutic effects by modulating various biological pathways, including oxidative stress, inflammatory cascades, and lipid metabolism. These compounds also exhibit diuretic effects, promoting urine production and aiding in toxin removal, thereby alleviating stress on the kidneys. The clinical evidence supporting the efficacy of <em>A. graveolens</em> in humans is still limited; its abundant phytochemical profile and new preclinical findings indicate its promise as an adjunctive therapeutic agent. This review provides a scientific basis for the continued exploration and use of <em>A. graveolens</em> in modern medicine, highlighting its role in promoting its pharmacological aspects through its diverse bioactive components.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100039"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143898640","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Designing of potential siRNA molecules for African norovirus gene silencing: A computational approach 设计非洲诺如病毒基因沉默的潜在siRNA分子:一种计算方法
Pharmacological Research - Reports Pub Date : 2025-03-01 Epub Date: 2024-11-15 DOI: 10.1016/j.prerep.2024.100021
Oluwakemi Ebenezer , Abel Kolawole Oyebamiji , Adesoji Alani Olanrewaju , Omowumi Temitayo Akinola , Samson Olusegun Afolabi , Ayodeji Arnold Olaseinde , Jack Tuszynski
{"title":"Designing of potential siRNA molecules for African norovirus gene silencing: A computational approach","authors":"Oluwakemi Ebenezer ,&nbsp;Abel Kolawole Oyebamiji ,&nbsp;Adesoji Alani Olanrewaju ,&nbsp;Omowumi Temitayo Akinola ,&nbsp;Samson Olusegun Afolabi ,&nbsp;Ayodeji Arnold Olaseinde ,&nbsp;Jack Tuszynski","doi":"10.1016/j.prerep.2024.100021","DOIUrl":"10.1016/j.prerep.2024.100021","url":null,"abstract":"<div><div>Introducing siRNAs into cells could degrade specific messenger RNA (mRNA) molecules, reducing the expression of the corresponding protein encoded by those mRNA molecules. Norovirus is the leading cause of both epidemic and pandemic acute gastroenteritis, which is inflammation of the stomach and intestine worldwide, and, as of present, no efficient vaccine is available to combat this norovirus disease. Since siRNA, therapeutics have gained significant attention for their potential to target and silence disease-causing genes. Our study utilizes different computational tools to design siRNA agents against the polyprotein of norovirus without causing off-target effects. According to the results of GC (guanine-cytosine) content, fold-free energy, binding energy, melting temperature, efficacy predictions, and molecular docking against human argonaute 2 protein (AGO2), two siRNA molecules are expected to exert the most effective action. The effectiveness and efficiency of siRNAs against norovirus need to be further examined in vivo before their use as alternative and practical molecular therapeutic agents.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100021"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144279195","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The role of interleukin-1 beta in inflammation and the potential of immune-targeted therapies 白细胞介素-1 β在炎症中的作用和免疫靶向治疗的潜力
Pharmacological Research - Reports Pub Date : 2025-03-01 Epub Date: 2025-01-09 DOI: 10.1016/j.prerep.2025.100027
Syed Ali Wijdan , Syed Muhammad Nasir Abbas Bokhari , Jenelle Alvares , Varisha Latif
{"title":"The role of interleukin-1 beta in inflammation and the potential of immune-targeted therapies","authors":"Syed Ali Wijdan ,&nbsp;Syed Muhammad Nasir Abbas Bokhari ,&nbsp;Jenelle Alvares ,&nbsp;Varisha Latif","doi":"10.1016/j.prerep.2025.100027","DOIUrl":"10.1016/j.prerep.2025.100027","url":null,"abstract":"<div><div>Interleukin-1 beta (IL-1β) has emerged as an important therapeutic target, due to its key role in mediating inflammation and tissue damage in different disorders. This study presents a thorough review of the conditions in which (IL-1β) is playing an important role and a summary of the new and ongoing treatments aimed at suppressing its activity. Furthermore, we explored currently available IL-1β targeted treatments, such as IL-1 inhibitors like Canakinumab and Anakinra, and also explained their work at molecular level in reducing inflammation. IL-1β is targeted in inflammatory illnesses in treatment that are beneficial, but there are drawbacks as well which includes the requirement for customized treatment plans, drug resistance, and unpleasant effects. This study also underlines the recent advancements in IL-1β targeted therapies, shedding light on novel approaches.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100027"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143152927","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Therapeutic potentials of trihydroxylflavonone-7-rhamnoglucoside against hepatocellular Lesch-Nyhan Syndrome induced by mixture of caffeine and KBrO3 via NOS/cAMP/PKA and DARPP-32, BDNF/TrkB signaling cascades 三羟基黄酮-7-鼠李糖甙通过NOS/cAMP/PKA和DARPP-32、BDNF/TrkB信号级联对咖啡因和KBrO3混合诱导的肝细胞Lesch-Nyhan综合征的治疗潜力
Pharmacological Research - Reports Pub Date : 2025-03-01 Epub Date: 2025-05-06 DOI: 10.1016/j.prerep.2025.100040
J.K. Akintunde , P. Adeyemi , O.H. Alonge , S.O. Salami , A.D. Ate , T.E. Oladele , O.A. Akinbode , D.A. Fadare
{"title":"Therapeutic potentials of trihydroxylflavonone-7-rhamnoglucoside against hepatocellular Lesch-Nyhan Syndrome induced by mixture of caffeine and KBrO3 via NOS/cAMP/PKA and DARPP-32, BDNF/TrkB signaling cascades","authors":"J.K. Akintunde ,&nbsp;P. Adeyemi ,&nbsp;O.H. Alonge ,&nbsp;S.O. Salami ,&nbsp;A.D. Ate ,&nbsp;T.E. Oladele ,&nbsp;O.A. Akinbode ,&nbsp;D.A. Fadare","doi":"10.1016/j.prerep.2025.100040","DOIUrl":"10.1016/j.prerep.2025.100040","url":null,"abstract":"<div><div>The management of Lesch-Nyhan Syndrome (LNS) associated with hepatocellular toxicosis has remained in the speculative phase. Also, due to numerous pharmacological capacities of 4,5,7-Trihydroxylflavonone-7-rhamnoglucoside popularly known as naringin, it may be a potent therapeutic flavonoid against hepatic LNS. We therefore studied the effect of 4,5,7-Trihydroxylflavonone-7-rhamnoglucoside on rats’ hepatic cells exhibiting LNS through NOS/cAMP/PKA/DARPP-32 and BDNF/TrkB signaling pathways. Sixty-seven male rats were divided into nine (n = 7) groups. Group I received distilled water only. Group II and III were exposed to 100 mg/kg KBrO<sub>3</sub> and 250 mg/kg caffeine, respectively. Group IV was co-exposed to 100 mg/kg KBrO<sub>3</sub> and 250 mg/Kg caffeine. Group V and VI were exposed to 100 mg/kg KBrO<sub>3</sub> each plus 100 mg/kg haloperidol and 50 mg/kg naringin, respectively. Group VII received 250 mg/kg caffeine + 50 mg/kg naringin. Group VIII received 100 mg/kg KBrO<sub>3</sub> + 250 mg/kg caffeine + 50 mg/kg naringin. Group IX received 50 mg/kg naringin. Exposure to KBrO<sub>3</sub> and/or caffeine for 21 days induced hepatocellular damage with alterations of ATP hydrolytic enzymes, neurotransmitter enzymes, arginase, PDE-5<sup>1</sup>, MDA and NO levels. Also, genes associated with hepatic LNS were up-regulated and characterized by periportal inflammation and vascular congestion. Post-treatment with 4,5,7-Trihydroxylflavonone-7-rhamnoglucoside for 14 days reverted the hepatic LNS in an <em>in vivo</em> model. We therefore concluded that bio-stimulation of TrKB/BDNF and DARPP-32 levels by 4,5,7-Trihydroxylflavonone-7-rhamnoglucoside may prolong the functionality of liver among individuals suffering from LNS.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100040"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143922084","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Oxidative imbalance induced by dithiocarbamate fungicide, Mancozeb aborts Nrf2 anti-oxidant signaling pathway protection in Vero cell line 二硫代氨基甲酸酯杀菌剂Mancozeb诱导的氧化失衡破坏了Vero细胞株Nrf2抗氧化信号通路保护
Pharmacological Research - Reports Pub Date : 2025-03-01 Epub Date: 2025-05-17 DOI: 10.1016/j.prerep.2025.100041
Shilpa T, Vaishnavi A, Aswati Ravindranathan Nair
{"title":"Oxidative imbalance induced by dithiocarbamate fungicide, Mancozeb aborts Nrf2 anti-oxidant signaling pathway protection in Vero cell line","authors":"Shilpa T,&nbsp;Vaishnavi A,&nbsp;Aswati Ravindranathan Nair","doi":"10.1016/j.prerep.2025.100041","DOIUrl":"10.1016/j.prerep.2025.100041","url":null,"abstract":"<div><div>Indiscriminate use of the dithiocarbamate fungicide mancozeb (MZB) presents serious risks to both human health and environment. These risks are exacerbated during xenobiotic detoxification in kidneys, where glomerular filtration and excretion can lead to the accumulatation of degradation products in renal cells, rendering them more susceptible to toxic effects. Present study examined cytotoxicity of MZB (1–14 μM) in Vero cells, a sensitive model for nephrotoxicity assessment, over different time periods (6–48 h) and detected EC<sub>50</sub> of 11 μM. MZB cytotoxicity was dose- and time-dependent, as shown by a 29 ± 0.02 % cell viability at 14 μM and an EC<sub>50</sub> of 9 ± 1 μM at 48 hours. DNA damage at 11 μM MZB (EC<sub>50</sub>) was evidenced as increased tail length (89 ± 9 μm), tail moment (62 ± 10 a.u.), and tail DNA content (60 ± 6 %). Cytotoxic effects of MZB were associated with the generation of reactive oxygen species (13 ± 0.1 RFU), upregulation of the pro-apoptotic <em>Bax</em> gene, activation of <em>Caspase</em>-3, and downregulation of the anti-apoptotic <em>Bcl</em>-2 gene. The study identified MZB induced redox imbalance and oxidative stress in Vero cells through the disruption of <em>Nrf</em>2-mediated antioxidant signaling pathways.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100041"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144116853","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Levetiracetam produces anxiolytic-like effects and attenuates the adverse consequences of stress exposure in mice 左乙拉西坦产生抗焦虑样作用,减轻小鼠应激暴露的不良后果
Pharmacological Research - Reports Pub Date : 2025-03-01 Epub Date: 2025-06-04 DOI: 10.1016/j.prerep.2025.100046
Victor Hadera, Matheus S. Braga, Leonardo B.M. Resstel, Francisco S. Guimarães, Felipe V. Gomes
{"title":"Levetiracetam produces anxiolytic-like effects and attenuates the adverse consequences of stress exposure in mice","authors":"Victor Hadera,&nbsp;Matheus S. Braga,&nbsp;Leonardo B.M. Resstel,&nbsp;Francisco S. Guimarães,&nbsp;Felipe V. Gomes","doi":"10.1016/j.prerep.2025.100046","DOIUrl":"10.1016/j.prerep.2025.100046","url":null,"abstract":"<div><div>Levetiracetam, a second-generation antiepileptic drug, is proposed to regulate neurotransmitter release, including glutamate, by inhibiting the synaptic protein SV2A, as well as modulating voltage-gated calcium channels and reducing excessive synaptic vesicle exocytosis. It may also influence the activity of Kv3.1 channels, which play a critical role in maintaining the fast-spiking activity of parvalbumin-expressing GABAergic interneurons. Through these mechanisms, levetiracetam may help restore the excitatory/inhibitory (E/I) balance, which is often disrupted in psychiatric disorders. Here, we investigated whether acute levetiracetam (50, 100, and 150 mg/kg) produces anxiolytic- and antidepressant-like effects and attenuates the expression and extinction of contextual fear conditioning, as well as cognitive deficits induced by a single footshock exposure in male C57BL/6 mice. Levetiracetam produced an anxiolytic-like effect in the elevated plus-maze, reduced fear expression, and mitigated cognitive impairments in the object recognition test following single footshock exposure. These results suggest that, in addition to its antiepileptic properties, levetiracetam may have therapeutic potential for treating stress-related abnormalities in emotional regulation and cognitive processing.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"3 ","pages":"Article 100046"},"PeriodicalIF":0.0,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144241313","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of novel peptide deformylase inhibitors: Ensemble complex-based pharmacophore modeling, docking and binding affinity studies 发现新型多肽变形酶抑制剂:基于组合复合物的药效学建模、对接和结合亲和力研究
Pharmacological Research - Reports Pub Date : 2024-03-01 Epub Date: 2024-06-13 DOI: 10.1016/j.prerep.2024.100011
Vijaya Bhaskar Baki , Siva Rajesh Sivarathri , Munichandra Babu Tirumalasetty , M.V. Jyothi Kumar , Rammohan Aluru
{"title":"Discovery of novel peptide deformylase inhibitors: Ensemble complex-based pharmacophore modeling, docking and binding affinity studies","authors":"Vijaya Bhaskar Baki ,&nbsp;Siva Rajesh Sivarathri ,&nbsp;Munichandra Babu Tirumalasetty ,&nbsp;M.V. Jyothi Kumar ,&nbsp;Rammohan Aluru","doi":"10.1016/j.prerep.2024.100011","DOIUrl":"10.1016/j.prerep.2024.100011","url":null,"abstract":"<div><p><em>Pseudomonas aeruginosa</em> infections are quickly increasing in association with a variety of illnesses, necessitating the development of novel medications. This study employed an <em>in silico</em> technique to find PDF inhibitors against <em>P. aeruginosa</em> Peptide deformylase (PaPDF). PaPDF's structure is comparable to that of other PDFs; however, binding site studies found that PaPDF has a smaller pocket than <em>Staphylococcus aureus</em>, covering the S1 and S2 sub pockets, and maintains a conserved hydrophobic nature. The Zn metal binding site of modified PaPDFs was examined using molecular dynamics, and the results revealed that Cys92Ala differed from His134Ala and His138Ala, respectively. Complex-based pharmacophore investigation revealed three significant pharmacophoric characteristics within the pocket: two hydrophobic and one H-bond acceptor. This allows us to perform virtual screening using the ChemBride database to uncover a variety of potential hits with specific inhibitory characteristics. Several restrictions, including docking and molecular mechanics/general born-volume integral implicit solvent (MM/GBVI), were applied, and the top-ranked ligands were tested for inhibitory characteristics against key residues in the active site. Furthermore, the bioavailability and toxicity prediction identified seven potential leads and suggested future research into the design and synthesis of a unique class of PaPDF inhibitors.</p></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"2 ","pages":"Article 100011"},"PeriodicalIF":0.0,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2950200424000119/pdfft?md5=31489a4403fc10c617aba7dc8b969fb5&pid=1-s2.0-S2950200424000119-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141390792","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Bilirubin, a potent and persistent inhibitor of genetic damage induced by gamma rays in D. melanogaster 胆红素--伽马射线诱导黑腹蝇遗传损伤的强效持久抑制剂
Pharmacological Research - Reports Pub Date : 2024-03-01 Epub Date: 2024-11-20 DOI: 10.1016/j.prerep.2024.100022
Elizabeth Jiménez , Emilio Pimentel , Martha P. Cruces , Viviana Valadez-Graham , Zazil Velázquez
{"title":"Bilirubin, a potent and persistent inhibitor of genetic damage induced by gamma rays in D. melanogaster","authors":"Elizabeth Jiménez ,&nbsp;Emilio Pimentel ,&nbsp;Martha P. Cruces ,&nbsp;Viviana Valadez-Graham ,&nbsp;Zazil Velázquez","doi":"10.1016/j.prerep.2024.100022","DOIUrl":"10.1016/j.prerep.2024.100022","url":null,"abstract":"<div><div>The antimutagenic and radioprotective action as well as the persistence of the effects of chlorophyllin, a tetrapyrrole with copper-chelate ring, was demonstrated in our laboratory, using the <em>in vivo</em> system <em>Drosophila melanogaster</em>. The aim of this investigation was to evaluate the inhibitory capacity of bilirubin (BRB) on gamma radiation-induced oxidative genetic damage. For this purpose, the SMART assay on the wing of <em>D. melanogaster</em> was used. Second instar larvae were pretreated with BRB for 24 hours and then groups of them were exposed to gamma ray at 0, 24, 48 or 72 hours after pretreatment. For the antioxidant action, Canton-S strain larvae were pretreated during 2 h with BRB, and after that, they were exposed to gamma rays to measure the activity of the SOD, CAT and GSH-Px enzymes and overexpression of genes <em>Sod</em> and <em>Cat</em>. The results indicated that the group treated with BRB+Gamma rays sharply reduced (56 %) the genetic damage compared to the groups exposed only to gamma rays. Furthermore, this effect was persistent up to 72 h after pretreatment. Bilirubin did not modify CAT nor GSH-Px enzymes activity, neither the transcription of <em>Sod1</em> gene at any time tested, however, the <em>Cat</em> gene only overexpressed 24 h after BRB and BRB+10 Gy treatment. These findings suggest that these porphyrins act as antioxidants probably by itself, which positions BRB as a possible radioprotector.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"2 ","pages":"Article 100022"},"PeriodicalIF":0.0,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142705857","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The synthetic peptide, PnPP-15, derived from the PnTx2-6 toxin of the spider Phoneutria nigriventer, induces peripheral antinociception involving neprilysin, opioid, and cannabinoid systems 从蜘蛛 Phoneutria nigriventer 的 PnTx2-6 毒素中提取的合成肽 PnPP-15 可诱导外周抗痛觉,其中涉及肾蛋白酶、阿片类和大麻素系统
Pharmacological Research - Reports Pub Date : 2024-03-01 Epub Date: 2024-06-23 DOI: 10.1016/j.prerep.2024.100012
Renata Cristina Mendes Ferreira , Edleusa Marques Lima-Batista , Ana Cristina Nogueira Freitas , Xavier Maia Mariano , Marcelo Ferreira Marcondes Machado , Dongchen Na , Adriana Karaoglanovic Carmona , Steve Peigneur , William Gustavo Lima , Brener Cunha Carvalho , Carlos Alberto Tagliati , Jan Tytgat , Igor Dimitri Gama Duarte , Maria Elena de Lima
{"title":"The synthetic peptide, PnPP-15, derived from the PnTx2-6 toxin of the spider Phoneutria nigriventer, induces peripheral antinociception involving neprilysin, opioid, and cannabinoid systems","authors":"Renata Cristina Mendes Ferreira ,&nbsp;Edleusa Marques Lima-Batista ,&nbsp;Ana Cristina Nogueira Freitas ,&nbsp;Xavier Maia Mariano ,&nbsp;Marcelo Ferreira Marcondes Machado ,&nbsp;Dongchen Na ,&nbsp;Adriana Karaoglanovic Carmona ,&nbsp;Steve Peigneur ,&nbsp;William Gustavo Lima ,&nbsp;Brener Cunha Carvalho ,&nbsp;Carlos Alberto Tagliati ,&nbsp;Jan Tytgat ,&nbsp;Igor Dimitri Gama Duarte ,&nbsp;Maria Elena de Lima","doi":"10.1016/j.prerep.2024.100012","DOIUrl":"https://doi.org/10.1016/j.prerep.2024.100012","url":null,"abstract":"<div><h3>Background</h3><p>The PnTx2–6 toxin is isolated from the Phoneutria nigriventer spider venom. The synthetic peptide PnPP-19 is derived from this toxin and induces antinociception. When topically applied, it is cleaved by proteases generating a 15 amino acid residues peptide, PnPP-15. PnPP-15 showed an antinociceptive effect in neuropathic pain developed by streptozotocin-induced diabetic mice. The present work aimed to investigate if PnPP-15 is also effective against the inflammatory pain induced by PGE<sub>2</sub>. We also evaluated its cytotoxicity <em>in vitro</em> and studied its possible action mechanism in the pain pathway.</p></div><div><h3>Methods</h3><p>The nociceptive threshold was assessed using the mechanical paw pressure test. Paw tissue was collected for protein extraction and western blot analyses. The FRET enzymatic assay measured neprilysin activity. The two-electrode voltage clamp technique measured evoked electrical currents in <em>Xenopus laevis</em> oocytes. Cytotoxicity was measured using multiple cell lines.</p></div><div><h3>Results</h3><p>PnPP-15 has peripheral antinociceptive activity <em>via</em> µ-opioid and CB<sub>1</sub> cannabinoid receptors and inhibits neprilysin. In addition, it induced direct activation of mu-opioid receptors expressed in <em>Xenopus laevis</em> oocytes. PnPP-15 was not cytotoxic against mammalian kidney, liver, heart, nerve, or lung cells.</p></div><div><h3>Conclusion</h3><p>This work demonstrated the antinociceptive effect of PnPP-15 in an inflammatory pain model, suggesting its use as a possible tool for developing new analgesic drugs.</p></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"2 ","pages":"Article 100012"},"PeriodicalIF":0.0,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2950200424000120/pdfft?md5=894719be290c29f9baee9c6b92b49796&pid=1-s2.0-S2950200424000120-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141484179","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Reno-protective effect of Roflumilast against kidney injury induced by ischemia/reperfusion in rats: Evidence from biochemical and histological investigations 罗氟司特对大鼠缺血/再灌注引起的肾损伤具有雷诺保护作用:生化和组织学研究的证据
Pharmacological Research - Reports Pub Date : 2024-03-01 Epub Date: 2024-07-30 DOI: 10.1016/j.prerep.2024.100014
Rehab F. Abdel-Rahman , Marawan A. Elbaset , Hany M. Fayed , Tuba Esatbeyoglu , Sherif M. Afifi , Rehab Adel Diab
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