Central nervous system agents in medicinal chemistry最新文献

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Antidepressant-like Properties of Melatonin and Atorvastatin Combination following the Restraint Stress in Mice: A Study of Oxidative Stress Factors. 褪黑素和阿托伐他汀联合使用抑制应激小鼠抗抑郁样特性:氧化应激因子的研究。
Central nervous system agents in medicinal chemistry Pub Date : 2023-01-01 DOI: 10.2174/1871524923666221121111501
Vahid Nikoui, Azam Hosseinzadeh, Solmaz Javadi Khotab, Seyyedeh Zahra Mousavi, Meysam Abolmaali, Saeed Mehrzadi
{"title":"Antidepressant-like Properties of Melatonin and Atorvastatin Combination following the Restraint Stress in Mice: A Study of Oxidative Stress Factors.","authors":"Vahid Nikoui,&nbsp;Azam Hosseinzadeh,&nbsp;Solmaz Javadi Khotab,&nbsp;Seyyedeh Zahra Mousavi,&nbsp;Meysam Abolmaali,&nbsp;Saeed Mehrzadi","doi":"10.2174/1871524923666221121111501","DOIUrl":"https://doi.org/10.2174/1871524923666221121111501","url":null,"abstract":"<p><strong>Background: </strong>Antidepressant properties of melatonin and atorvastatin have been reported by clinical and experimental studies. Since both melatonin and atorvastatin possess antioxidant properties and considering the involvement of oxidative stress factors in depression, the aim of the present investigation was to study the possible role of oxidative stress factors in the antidepressant- like effect of melatonin and atorvastatin combination in mice forced swimming test.</p><p><strong>Methods: </strong>Following the induction of restraint stress, mice were randomly divided into eight groups including the non-stressed and stressed vehicle-treated groups, melatonin- and atorvastatintreated groups, a combination of melatonin and atorvastatin-treated group, and fluoxetineadministrated group. The open field test (OFT) and forced swimming test (FST) were carried out, and the hippocampus and prefrontal cortex were removed for the measurement of oxidative stress factors.</p><p><strong>Results: </strong>Induction of restraint stress increased the immobility time in FST, and melatonin (10 mg/kg) significantly reduced it. Atorvastatin at both doses of 1 and 10 mg/kg could not alter the immobility time, significantly. Co-administration of melatonin and atorvastatin (10 mg/kg) exerted a significant antidepressant-like response and decreased the immobility time compared with melatonin or atorvastatin (10 mg/kg), alone. Induction of restraint stress elevated the malondialdehyde (MDA) levels in mice's hippocampus, while pretreatment of animals with atorvastatin (10 mg/kg) could reverse it. The co-administration of melatonin and atorvastatin (10 mg/kg) increased the cortical superoxide dismutase (SOD) activity compared with atorvastatin alone, but could not alter the catalase (CAT) activity.</p><p><strong>Conclusion: </strong>It is concluded that atorvastatin might augment the antidepressant-like properties of melatonin in FST.</p>","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9732245","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
Evaluation of Nootropic Potential of Aerva persica Roots against D-galactose-induced Memory Impairment. 白叶根对抗D-半乳糖诱导的记忆损伤的嗜面潜能评估。
Central nervous system agents in medicinal chemistry Pub Date : 2023-01-01 DOI: 10.2174/1871524923666230822100016
Mohammad Asif, Kaneez Fatima, Sadaf Jamal Gilani, Mohamad Taleuzzaman, Syed Salman Ali, Samera Ali Siddiqui
{"title":"Evaluation of Nootropic Potential of <i>Aerva persica</i> Roots against D-galactose-induced Memory Impairment.","authors":"Mohammad Asif,&nbsp;Kaneez Fatima,&nbsp;Sadaf Jamal Gilani,&nbsp;Mohamad Taleuzzaman,&nbsp;Syed Salman Ali,&nbsp;Samera Ali Siddiqui","doi":"10.2174/1871524923666230822100016","DOIUrl":"10.2174/1871524923666230822100016","url":null,"abstract":"<p><strong>Background: </strong>The primary phytoconstituents reported to have neuroprotective effects are flavonoids and phenolic compounds. Aerva persica roots are reported to be rich in flavonoids and phenolic compounds. Therefore, this study aimed to explore the nootropic potential of Aerva persica roots.</p><p><strong>Objective: </strong>The objective of this study was to evaluate the nootropic potential of Aerva persica roots against D-galactose-induced memory impairment.</p><p><strong>Methods: </strong>In this study, the roots of Aerva persica were extracted with 70% ethanol. The obtained extract was evaluated for total phenolic content using the Folin-Ciocalteu method and total flavonoid content using the aluminium chloride colorimetric assay. Afterward, the acute oral toxicity of the extract was determined following the Organisation for Economic Co-operation and Development (OECD) guideline 423. Additionally, two doses of Aerva persica (100 and 200 mg/kg body weight (BW)) were evaluated for their nootropic potential against D-galactose-induced memory impairment. The nootropic potential of the crude extract was assessed through a behavioural study and brain neurochemical analysis. Behavioural studies involved the evaluation of spatial reference- working memory using the radial arm maze test and the Y-maze test. Neurochemical analysis was performed to determine the brain's acetylcholine, acetylcholinesterase, glutathione (GSH), and malondialdehyde (MDA) levels.</p><p><strong>Results: </strong>The total phenolic content and total flavonoid content were found to be 179.14 ± 2.08 μg GAE/mg and 273.72 ± 3.94 μg QE/mg, respectively. The Aerva persica extract was found to be safe up to 2000 mg/kg BW. Following the safety assessment, the experimental mice received various treatments for 14 days. The behavioural analysis using the radial maze test showed that the extract at both doses significantly improved spatial reference-working memory and reduced the number of total errors compared to disease control groups. Similarly, in the Y-maze test, both doses significantly increased the alteration percentage and the percentage of novel arm entry (both indicative of intact spatial memory) compared to disease control. In neurochemical analysis, Aerva persica at 200 mg/kg significantly normalised the acetylcholine level (p<0.0001) and GSH level (p<0.01) compared to disease control. However, the same effect was not observed with Aerva persica at 100 mg/kg. Additionally, Aerva persica at 200mg/kg BW significantly decreased the acetylcholinesterase level (p<0.0001) and decreased the brain's MDA level (p<0.01) compared to the disease control, whereas the effect of Aerva persica at 100 mg/kg BW in reducing acetylcholinesterase was non-significant.</p><p><strong>Conclusion: </strong>Based on the results, it can be concluded that the nootropic potential of Aerva persica was comparable to that of the standard drug, Donepezil, and the effect might be attributed to","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10051370","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
Novel molecular targets and mechanisms for neuroprotective modulation in neurodegenerative disorders. 神经退行性疾病中神经保护调节的新分子靶点和机制。
Central nervous system agents in medicinal chemistry Pub Date : 2022-06-16 DOI: 10.2174/1871524922666220616092132
Aala Azari, Amin Goodarzi, Behrouz Jafarkhani, M. Eghbali, Zohreh Karimi, Seyed Sajad Hosseini Balef, H. Irannejad
{"title":"Novel molecular targets and mechanisms for neuroprotective modulation in neurodegenerative disorders.","authors":"Aala Azari, Amin Goodarzi, Behrouz Jafarkhani, M. Eghbali, Zohreh Karimi, Seyed Sajad Hosseini Balef, H. Irannejad","doi":"10.2174/1871524922666220616092132","DOIUrl":"https://doi.org/10.2174/1871524922666220616092132","url":null,"abstract":"BACKGROUND\u0000Neuronal death underlies the symptoms of several human neurological disorders, including Alzheimer's, Parkinson's and Huntington's diseases, and amyotrophic lateral sclerosis that their precise pathophysiology have not yet been elucidated. According to various studies the prohibition is the best therapy with neuroprotective approaches which are advanced and safe methods.\u0000\u0000\u0000METHODS\u0000This review summarizes some of the already-known and newly emerged neuroprotective targets and strategies that their experimental effects have been reported. Accordingly, literature was studied from 2000 to 2021 and appropriate articles were searched in Google Scholar and Scopus with the keywords given in the Keywords section of the current review.\u0000\u0000\u0000RESULTS\u0000Lewy bodies are the histopathologic characteristics of neurodegenerative disorders and are protein-rich intracellular deposits in which Alpha-Synuclein is its major protein. Alpha-Synuclein's toxic potential provides a compelling rationale for therapeutic strategies aimed at decreasing its burden in neuronal cells through numerous pathways including ubiquitin-proteasome system and autophagy-lysosome Pathway, proteolytic breakdown via cathepsin D, kallikrein-6 (neurosin), calpain-1 or MMP9, heat shock proteins, and proteolysis targeting chimera which consists of a target protein ligand and an E3 ubiquitin ligase (E3) followed by target protein ubiquitination (PROTACs). Other targets that have been noticed recently are the mutant huntingtin, tau proteins and glycogen synthase kinase 3β that their accumulation proceeds extensive neuronal damage and up to the minute approach such as Proteolysis Targeting Chimera promotes its degradation in cells. As various studies demonstrated that Mendelian gene mutations can result into the neurodegenerative diseases, additional target that has gained much interest is epigenetics such as mutation, phosphodiesterase, RNA binding proteins and Nuclear respiratory factor 1.\u0000\u0000\u0000CONCLUSION\u0000The novel molecular targets and new strategies compiled and introduced here can be used by scientists to design and discover more efficient small molecule drugs against the neurodegenerative diseases. And also the genes in which their mutations can lead to the α-synuclein aggregation or accumulation are discussed and considered a valuable information of epigenetics in dementia.","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-06-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46957936","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: 1
Erythroxylum cuneatum prevented cellular adaptation in morphine-induced neuroblastoma cells. 楔红抑制吗啡诱导的神经母细胞瘤细胞的细胞适应。
Central nervous system agents in medicinal chemistry Pub Date : 2022-05-16 DOI: 10.2174/1871524922666220516151121
Noor Azuin Suliman, M. Moklas, C. N. M. Taib, Mohamad Taufik Hidayat Baharuldin, S. M. Chiroma
{"title":"Erythroxylum cuneatum prevented cellular adaptation in morphine-induced neuroblastoma cells.","authors":"Noor Azuin Suliman, M. Moklas, C. N. M. Taib, Mohamad Taufik Hidayat Baharuldin, S. M. Chiroma","doi":"10.2174/1871524922666220516151121","DOIUrl":"https://doi.org/10.2174/1871524922666220516151121","url":null,"abstract":"BACKGROUND\u0000Chronic morphine stimulates prolonged stimulation of opioid receptors, especially µ-opioid subtype (MOR), which in turn signals cellular adaptation. However, the sudden termination of morphine after chronic intake causes withdrawal syndrome.\u0000\u0000\u0000OBJECTIVES\u0000Hence, this study was designed to find an alternative treatment for the morphine withdrawal using the alkaloid leaf extract of Erythroxylum cuneatum (E. cuneatum), done on morphine-exposed neuroblastoma cell lines.\u0000\u0000\u0000METHODS\u0000SK-N-SH, a commercialised neuroblastoma cell line, was used in two separate study designs; the antagonistic and pre-treatment of morphine. The antagonistic treatment was conducted through concurrent exposure of the cells to morphine and E. cuneatum or morphine and methadone for 24 h. The pre-treatment design was carried out by exposing the cells to morphine for 24 h, followed by 24 h exposures to E. cuneatum or methadone. The cytosolic fraction was collected and run for protein expression involved in cellular adaptation; mitogen-activated protein (MAP)/extracellular signal-regulated (ERK) kinase 1/2 (MEK 1/2), extracellular signal-regulated kinase 2 (ERK 2), cAMP-dependent protein kinase (PKA) and protein kinases C (PKC).\u0000\u0000\u0000RESULTS\u0000The antagonistic treatment showed the normal level of MEK 1/2, ERK 2, PKA and PKC by the combination treatment of morphine and E. cuneatum, comparable to the combination of morphine and methadone. Neuroblastoma cells exposed to morphine pre-treatment expressed a high level of MEK 1/2, ERK 2, PKA and PKC, while the treatments with E. cuneatum and methadone normalised the expression of the cellular adaptation proteins.\u0000\u0000\u0000CONCLUSION\u0000E. cuneatum exerted anti-addiction properties by lowering the levels of cellular adaptation proteins, and its effects are comparable to that of methadone (an established anti-addiction drug).","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-05-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47242409","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: 1
Biomedical Applications of Polyurethane Hydrogels, Polyurethane Aerogels and Polyurethane-Graphene Nanocomposite Materials. 聚氨酯水凝胶、聚氨酯气凝胶和聚氨酯-石墨烯纳米复合材料的生物医学应用。
Central nervous system agents in medicinal chemistry Pub Date : 2022-04-29 DOI: 10.2174/1871524922666220429115124
S. Saganuwan
{"title":"Biomedical Applications of Polyurethane Hydrogels, Polyurethane Aerogels and Polyurethane-Graphene Nanocomposite Materials.","authors":"S. Saganuwan","doi":"10.2174/1871524922666220429115124","DOIUrl":"https://doi.org/10.2174/1871524922666220429115124","url":null,"abstract":"BACKGROUND\u0000Increasing new emerging ill-healths have posed therapeutic challenges in modern medicine. Hence polyurethane hydrogels that comprise polyol, copolymer and extender could be prepared from diverse chemical compounds with adjuvants such as ascorbic acid, sorbitol among others. Their mechano-physicochemical properties are functions of their biological activities. Therefore there is need to assess their therapeutic potentials.\u0000\u0000\u0000METHODS\u0000literature were searched on synthesis and medical uses of polyurethane - hydrogels, polyurethane - aerogels and polyurethane - graphene nanocomposite materials, with a view to identifying their sources, synthesis, mechanical and physiochemical properties, biomedical applications, chirality, and the relevance of Lipinski's rule of five in the synthesis of oral polyurethane nanocomposite materials.\u0000\u0000\u0000RESULTS\u0000The prepared hydrogels and aerogels could be used as polymer carriers for intradermal, cutaneous and intranasal drugs. They can be fabricated and used as prosthetics. In addition the strength modulus (tensile stress-tensile strain ratio), biodegradability, biocompatibility and non-toxic effects of the polyurethane hydrogels and aerogels are the highly desirable properties. However, body and environmental temperatures may contribute to their instability, hence there is need to improve on the synthesis of aerogels and hydrogels of polyurethane that can last for many years. Alcoholism, diabetes, pyrogenic diseases, mechanical and physical forces, and physiological variability may also reduce the life span of polyurethane aerogels and hydrogels.\u0000\u0000\u0000CONCLUSION\u0000Synthesis of polyurethane hydrogel-aerogel complex that can be used in complex, rare biomedical cases is of paramount importance. These hydrogels and aerogels may be hydrophobic, hydrophilic, aerophobic-aerophilic or amphiphilic and sometimes lipophilic depending on structural components and the intended biomedical uses. Polyurethane graphene nanocomposite materials are used in the treatment of a myriad of diseases including cancer and bacterial infection.","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46363190","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 effects of vitamin D3 and melatonin combination on pentylenetetrazole-induced seizures in mice. 维生素D3和褪黑素联合使用对戊四唑致小鼠癫痫发作的影响。
Central nervous system agents in medicinal chemistry Pub Date : 2022-04-29 DOI: 10.2174/1871524922666220429121253
A. Hosseinzadeh, Ehsan Dehdashtian, M. Jafari-Sabet, S. Mehrzadi
{"title":"The effects of vitamin D3 and melatonin combination on pentylenetetrazole-induced seizures in mice.","authors":"A. Hosseinzadeh, Ehsan Dehdashtian, M. Jafari-Sabet, S. Mehrzadi","doi":"10.2174/1871524922666220429121253","DOIUrl":"https://doi.org/10.2174/1871524922666220429121253","url":null,"abstract":"BACKGROUND\u0000Epileptic seizures are associated with the overproduction of free radicals in the brain leading to neuronal cell death. Therefore, reduction of oxidative stress may inhibit seizure-induced neuronal cell damage. Current study evaluated the effects of Vit D3 and melatonin and their combination on pentylenetetrazol (PTZ)-induced tonic clonic seizures in mice.\u0000\u0000\u0000METHODS\u0000Animals were divided into six groups. Group I was administrated with normal saline (0.5 ml, intraperitoneally (i.p.)) on the 15th day of experiment. Group II was injected with PTZ (60 mg/kg dissolved in 0.5 ml normal saline, i.p) on the 15th day. Groups III-IV were treated with diazepam (4 mg/kg/day), Vit D3 (6000 IU/kg/day), melatonin (20 mg/kg/day) and Vit D3 (6000 IU/kg/day)/melatonin (20 mg/kg/day), respectively, and were then injected with PTZ (60 mg/kg) on the 15th day of experiment. Immediately after the injection of PTZ on the 15th day, mice were observed for a 30-min period for the measurement of seizure latency and duration. For determination of oxidative stress markers, malondialdehyde (MDA) level and superoxide dismutase (SOD) activity were measured in mouse brains.\u0000\u0000\u0000RESULTS\u0000Treatment with Vit D3, melatonin, and Vit D3/melatonin significantly increased seizure latency and decreased seizure duration. The brain level of MDA was lower and SOD activity was greater than the PTZ group. Mice treated with Vit D3/melatonin had lower seizure duration compared to other treated groups.\u0000\u0000\u0000CONCLUSIONS\u0000Combination of Vit D3 and melatonin may reduce seizure frequency in epileptic patients; this effect may result from various mechanisms including inhibition of oxidative stress.","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43632977","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: 2
Synthesis and CNS Activity of Phenytoin derivatives. 苯妥英类衍生物的合成及其中枢神经系统活性。
Central nervous system agents in medicinal chemistry Pub Date : 2022-04-29 DOI: 10.2174/1871524922666220429122141
Rahul Chauhan, Shwetank Verma, Alankar Shrivasatava
{"title":"Synthesis and CNS Activity of Phenytoin derivatives.","authors":"Rahul Chauhan, Shwetank Verma, Alankar Shrivasatava","doi":"10.2174/1871524922666220429122141","DOIUrl":"https://doi.org/10.2174/1871524922666220429122141","url":null,"abstract":"BACKGROUND\u0000The derivatives of Phenytoin conjugated with various anilines were synthesized. The synthesized derivatives were evaluated for different physicochemical parameters along with Log P values using different software programs to discover its ability to cross the blood brain barrier. The pharmacological activities such as antianxiety, skeletal muscle relaxant and anticonvulsant were evaluated by using different models.\u0000\u0000\u0000OBJECTIVE\u0000The new Phenytoin derivatives were synthesized and evaluated for different properties to predict its CNS activity. The drugs synthesized by chloroacetylation and then different aniline were added into it. The compounds were evaluated for their different CNS activity by using different methods.\u0000\u0000\u0000METHOD\u0000The compounds were synthesized by firstly chloroacetylating the phenytoin and then different substituted aniline were added into it. The compounds were evaluated for antianxiety activity, Muscle relaxant activity and anticonvulsant activity by using different models.\u0000\u0000\u0000RESULT\u0000The number of derivatives of Phenytoin was synthesized and various physicochemical parameters were optimized which reveal that the compound containing chloro group such as C2 and C5 exhibited significant potential when compared with the standard drug Diazepam.\u0000\u0000\u0000CONCLUSION\u0000It was portrayed that the synthesis, computational studies and evaluation of anticonvulsant, antianxiety and skeletal muscle relaxant activity of new Phenytoin derivatives were carried out. The compounds were productively synthesized and portrayed by molecular docking studies. The compounds also exhibit mild to moderate similarity with respect to standard drug. The synthesized drugs have the potential to be optimized further to engender new scaffolds to treat various CNS disorders.","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45101519","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
Behavioral Pharmacology of Five Uncommon Passiflora Species Indicates Sedative and Anxiolytic-like Potential. 五种不常见西番莲属植物的行为药理学表现出镇静和类似焦虑的潜力。
Central nervous system agents in medicinal chemistry Pub Date : 2022-04-26 DOI: 10.2174/1871524922666220426102650
M. Sakalem, R. Tabach, Miriane de Oliveira, E. Carlini
{"title":"Behavioral Pharmacology of Five Uncommon Passiflora Species Indicates Sedative and Anxiolytic-like Potential.","authors":"M. Sakalem, R. Tabach, Miriane de Oliveira, E. Carlini","doi":"10.2174/1871524922666220426102650","DOIUrl":"https://doi.org/10.2174/1871524922666220426102650","url":null,"abstract":"BACKGROUND\u0000There are over 500 species in the Passiflora genus, and while some of them are very well known in folk medicine for their anxiolytic effects, very little is known for the other genus representants, which could also present medicinal effects.\u0000\u0000\u0000OBJECTIVE\u0000In this study, we performed an interspecific pharmacological comparison of five little investigated Passiflora species, all native to Brazil: P. bahiensis, P. coccinea, P. quadrangularis, P. sidaefolia, and P. vitifolia.\u0000\u0000\u0000METHOD\u0000Extracts were administered to mice before behavioral testing, which included a general pharmacological screening and anxiolytic-like effect investigation.\u0000\u0000\u0000RESULTS\u0000Three of the species [P. coccinea, P. quadrangularis, and P. sidaefolia] induced a decrease in locomotor activity of mice; P. coccinea also reduced the latency to sleep. Importantly, none of the species interfered with motor coordination. Oral administration evoked no severe signs of toxicity even at higher doses. Regarding the anxiolytic-like profile, P. sidaefolia reduced the anxious-like behavior in the Holeboard test in a similar way to the positive control, Passiflora incarnata, while not affecting total motricity.\u0000\u0000\u0000CONCLUSION\u0000These results indicate that P. coccinea, P. quadrangularis, and P. sidaefolia reduced the general activity of mice and confer a calmative/sedative potential to these three species, which must be further elucidated by future investigations.","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42871760","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 Potential and Clinical Evidence of Hesperidin as Neuroprotective Agent. 橙皮苷作为神经保护剂的治疗潜力和临床证据。
Central nervous system agents in medicinal chemistry Pub Date : 2022-04-04 DOI: 10.2174/1871524922666220404164405
S. Joshi, A. Dhingra, B. Chopra, Kumar Guarve, Deepak K Bhateja
{"title":"Therapeutic Potential and Clinical Evidence of Hesperidin as Neuroprotective Agent.","authors":"S. Joshi, A. Dhingra, B. Chopra, Kumar Guarve, Deepak K Bhateja","doi":"10.2174/1871524922666220404164405","DOIUrl":"https://doi.org/10.2174/1871524922666220404164405","url":null,"abstract":"BACKGROUND\u0000Neuroprotection is preserving neural function in various neurodegenerative diseases like Alzheimer's, Huntington's, Parkinson's, and multiple sclerosis. Hesperidin, a flavanone glycoside in citrus fruits such as sweet oranges and lemons, possesses many biological effects, including neuroprotection.\u0000\u0000\u0000OBJECTIVE\u0000To explore the neuropharmacological mechanisms and therapeutic potential of hesperidin in the management of neurodegenerative disorders.\u0000\u0000\u0000METHOD\u0000It emphasizes comparative and clinical trial studies with a number of targets reviewed from the data available on PubMed, Science Direct, Clinicaltrails.gov, and from many reputed foundations.\u0000\u0000\u0000RESULT\u0000Escalating clinical evidence has established the inhibitory effect of hesperidin in the management of neurodegenerative disorders. Neuroprotective potential of hesperidin is characterized through endogenous antioxidant defence functions, improvement of neural growth factors, anti-neuroinflammatory activity, and apoptotic pathways.\u0000\u0000\u0000CONCLUSION\u0000The present study highlights the beneficial neuropharmacological potential of hesperidin including anticonvulsant, antidepressant, antioxidant, anti-inflammatory, memory, and locomotor enhancing activities.","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-04-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48611457","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: 3
Preface 前言
Central nervous system agents in medicinal chemistry Pub Date : 2022-04-01 DOI: 10.2174/187152492201220707105839
Ramón Cacabelos
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