Produtos naturais como candidatos a fármacos úteis no tratamento do Mal de Alzheimer

Viegas, Cláudio; Bolzani, Vanderlan da Silva; Furlan, Maysa; Fraga, Carlos A. M.; Barreiro, Eliezer J.

doi:10.1590/s0100-40422004000400021

Cited by 29 publications

(13 citation statements)

References 20 publications

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“…But the serum, the teciduals liquid and the cells possess antioxidant mechanisms of protection that annul this toxicity -ceruloplasmine, transferrine, superoxide dismutase, catalase and glutation peroxidase. Many of the protective effects in CNS are related to the presence of poliphenolic constituents of the vegetable extracts, being able to act in different forms, contributing thus for the neuronal tissue integrity inhibiting the activity of the enzyme superoxide dismutase (it acts as blocking of FR's propagator) and monoamine oxidase, that contribute to generate free radical (RL) in the brain and in the body; kidnapping radical that could cause damage to the neurons and, consequently, retarding the changes associated with age in the brain; reducing the liberation of araquidonic acid, a toxic co-product to the lipidic metabolism, that appears on the brain as soon as the ischemic episode (Gold et al 2002;Viegas Junior et al 2004). Auddy et al (2003) presented results with antioxidant plants of the Indian medicine: Sida cordifolia, Cynodon dactylon and Evolvulus alsinoides, that compose rasayanas in the ayurvedic practice for disturbances, neurodegenerations, prevention and treatment, as Parkinson and Alzheimer; as well as renewers, a lot in vogue in cosmetology as anti-aging.…”

Section: Discussionmentioning

confidence: 99%

Behavioral and enzymatic bioassays with Serjania erecta Radlk., Sapindaceae, correlated with cognitive dysfunctions

Broggini¹,

Fernandes²,

Nogueira³

et al. 2010

Rev. bras. farmacogn.

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RESUMO: "Comportamento e ensaios bioenzimáticos com Serjania erecta Radlk., sapindaceae, correlacionados com disfunções cognitivas." O objetivo deste estudo foi pesquisar o extrato bruto de Serjania erecta Radlk., Sapindaceae, e seus bioativos como preventivos ou inibidores de perda de memória em roedores, e outros fatores correlacionados com a síndrome de Alzheimer: atividade antioxidante e anticolinesterásicas, principalmente como planta adaptógena, baixa toxicidade e ação regulatória. A reversão do bloqueador colinérgico (escopolamina) no teste da esquiva passiva foi detectada pela latência mensurada em animais jovens e adultos. Apresentou baixa toxicidade, com efeito protetor na análise bioquímica (hipoglicemia/hipotrigliceridemia). Índices elevados (acima 83%) na atividade antioxidante foram observados. A inibição da AChE e BuChE foi perceptível nas frações cromatográficas, confirmando as ações via oral e diretamente no SNC.Unitermos: Serjania erecta, antioxidante, anticolinesterase, adaptógena, Alzheimer. ABSTRACT:The purpose of this study was to investigate the crude extract of Serjania erecta Radlk., Sapindaceae, and its bioactive agents as preventive or inhibitor of memory loss in rodents, as well as other factors correlated with Alzheimer's syndrome: antioxidant and anticholinesterase activity, mainly as plant adaptogen -low toxicity and regulation action. The blocking cholinergic reversion activity (scopolamine) in the test of the passive avoidance was detected by measuring latency in young and adult animals. It presented low toxicity, with protective effect as shown by biochemical analysis (hypoglycemic/ hypotriglyceridemic). Elevated levels (above 83%) of antioxidant activity were detected. AchE and BuChE inhibition were also detected in the chromatographic fractions, which were active both orally and directly on CNS (ICV).

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Section: Discussionmentioning

confidence: 99%

Behavioral and enzymatic bioassays with Serjania erecta Radlk., Sapindaceae, correlated with cognitive dysfunctions

Broggini¹,

Fernandes²,

Nogueira³

et al. 2010

Rev. bras. farmacogn.

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“…Barbosa-Filho et al (2006) showed in a review that 309 plants belong to 92 botanical families were tested against acetylcholinesterase inhibition whereas 156 of them were active (ca 50%). Presently, the use of inhibitors of acetylcholinesterase still seems to be the most effi cient approach to treat the symptoms of neurodegenerative diseases, such as Alzheimer disease (Viegas et al, 2004).…”

Section: Resultsmentioning

confidence: 99%

Screening for antifungal, DNA-damaging and anticholinesterasic activities of Brazilian plants from the Atlantic Rainforest: Ilha do Cardoso State Park

Lopes¹,

Carreira²,

Agripino³

et al. 2008

Rev. bras. farmacogn.

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ABSTRACT:Crude extracts from 17 plant species collected from an Atlantic Forest region in the State of São Paulo (Brazil) have been screened for antifungal, DNA-damaging and acetylcholinesterase inhibiting activities. Of the 34 extracts obtained from leaves and stems of plants assayed for antifungal activity with Cladosporium sphaerospermum and C. cladosporioides 26.5% were active. However, only the extract of leaves of Cabralea canjerana showed a strong inhibition of both fungi. The DNA-damaging assay with mutant strains of Saccharomyces cerevisiae resulted in 11.7 % of the extracts being active whereas 100% of them showed selectivity for the DNA-repair mechanism of topoisomerase II. Of the 17 species analysed, 12 showed anticholinesterasic activity in TLC assay. However, only extracts from Tetrastylidium grandifolium (stems) and Sloanea guianensis (leaves and stems) inhibited acetylcholinesterase activity more than 50% in quantitative assay.

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“…A atrofia dos núcleos de Meynert ocasiona uma diminuição expressiva na produção de CAT e a consequente diminuição nos níveis de ACh na fenda sináptica. [39][40] Outro alvo terapêutico enzimático, descrito em vários trabalhos na literatura, é a butirilcolinesterase (BuChE). Esta colinesterase está presente principalmente nas células gliais, no tecido endotelial e nos neurônios, atuando juntamente com a AChE na modulação dos níveis de ACh.…”

Section: Fisiopatologia Da Daunclassified

Recent Applications of the MultiTarget Directed Ligands Approach for the Treatment of Alzheimer's Disease

Dias¹,

Paula²,

Riquiel³

et al. 2015

Revista Virtual De Química

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In the last years, Medicinal Chemistry is tracking down for novel tools and alternatives capable to bring to light better agility, safety and a more efficient address in the design and prospection of drug candidates. In this context, strategies for drug discovery focusing the development of ligands that act on specific target have been discussed, considering that they have limited application on multifactorial diseases, where a set of biochemical events and protein targets are involved. During the last decade, a novel polypharmacology based approach has emerged for planning ligands, aiming the discovery of chemical entities capable to act simultaneously on multiple molecular targets. Since 2005, the literature has reported many studies that use this innovative strategy for drug design against Alzhei e s disease (AD). AD is a neurodegenerative illness, characterized by a set of interconnected events involving intra and extracellular protein fragment deposits, the onset of a complex neuroinflammatory process, mitochondrial dysfunction, apoptosis and neuronal death. As a consequence of the disease progress, the patient is affected by memory and cholinergic deficits, motor and functional impairment, and death. In this brief review, our goal was to report the most recent advances (2013-2014) on medicinal chemistry for the design and discovery of novel multi-target drug candidate prototypes potentially useful for AD treatment. This work is complementary to another review recently published by our group covering the early 2005-2012 period. In most of the works discussed herein, the commercial drugs rivastigmine, tacrina, donepezil and galanthamine have been used as models of acetilcolinesterase inhibitors for the design of novel molecular hybrids with multiple action profile. In other cases, natural products such as curcumine, resveratrol, berberine and quercetin have been elected due to their neuroprotective, antiapoptotic, anti-inflammatory and antioxidant characteristics for planning new chemical entities with innovative properties and therapeutic potential for a more effective AD treatment.

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Produtos naturais como candidatos a fármacos úteis no tratamento do Mal de Alzheimer

Cited by 29 publications

References 20 publications

Behavioral and enzymatic bioassays with Serjania erecta Radlk., Sapindaceae, correlated with cognitive dysfunctions

Behavioral and enzymatic bioassays with Serjania erecta Radlk., Sapindaceae, correlated with cognitive dysfunctions

Screening for antifungal, DNA-damaging and anticholinesterasic activities of Brazilian plants from the Atlantic Rainforest: Ilha do Cardoso State Park

Recent Applications of the MultiTarget Directed Ligands Approach for the Treatment of Alzheimer's Disease

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Produtos naturais como candidatos a fármacos úteis no tratamento do Mal de Alzheimer

Cited by 29 publications

References 20 publications

Behavioral and enzymatic bioassays with Serjania erecta Radlk., Sapindaceae, correlated with cognitive dysfunctions

Behavioral and enzymatic bioassays with Serjania erecta Radlk., Sapindaceae, correlated with cognitive dysfunctions

Screening for antifungal, DNA-damaging and anticholinesterasic activities of Brazilian plants from the Atlantic Rainforest: Ilha do Cardoso State Park

Recent Applications of the Multi­Target Directed Ligands Approach for the Treatment of Alzheimer's Disease

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Recent Applications of the MultiTarget Directed Ligands Approach for the Treatment of Alzheimer's Disease