Your browser doesn't support javascript.
loading
Assessment of Novel Curcumin Derivatives as Potent Inhibitors of Inflammation and Amyloid-ß Aggregation in Alzheimer's Disease.
Lakey-Beitia, Johant; González, Yisett; Doens, Deborah; Stephens, David E; Santamaría, Ricardo; Murillo, Enrique; Gutiérrez, Marcelino; Fernández, Patricia L; Rao, K S; Larionov, Oleg V; Durant-Archibold, Armando A.
Afiliação
  • Lakey-Beitia J; Center for Biodiversity and Drug Discovery, Instituto de Investigaciones Científicas y Servicios de Alta Tecnología (INDICASAT AIP), Republic of Panama.
  • González Y; Department of Biotechnology, Acharya Nagarjuna University, India.
  • Doens D; Department of Chemistry, University of Texas at San Antonio, San Antonio, TX, USA.
  • Stephens DE; Department of Biotechnology, Acharya Nagarjuna University, India.
  • Santamaría R; Center for Molecular and Cellular Biology of Diseases, Instituto de Investigaciones Científicas y Servicios de Alta Tecnología (INDICASAT AIP), Republic of Panama.
  • Murillo E; Department of Biotechnology, Acharya Nagarjuna University, India.
  • Gutiérrez M; Center for Molecular and Cellular Biology of Diseases, Instituto de Investigaciones Científicas y Servicios de Alta Tecnología (INDICASAT AIP), Republic of Panama.
  • Fernández PL; Department of Chemistry, University of Texas at San Antonio, San Antonio, TX, USA.
  • Rao KS; Center for Biodiversity and Drug Discovery, Instituto de Investigaciones Científicas y Servicios de Alta Tecnología (INDICASAT AIP), Republic of Panama.
  • Larionov OV; Department of Biochemistry, College of Natural, Exact Sciences and Technology, University of Panama, Republic of Panama.
  • Durant-Archibold AA; Center for Biodiversity and Drug Discovery, Instituto de Investigaciones Científicas y Servicios de Alta Tecnología (INDICASAT AIP), Republic of Panama.
J Alzheimers Dis ; 60(s1): S59-S68, 2017.
Article em En | MEDLINE | ID: mdl-28453488
Alzheimer's disease (AD) is the most common neurodegenerative disorder affecting the elderly population worldwide. Brain inflammation plays a key role in the progression of AD. Deposition of senile plaques in the brain stimulates an inflammatory response with the overexpression of pro-inflammatory mediators, such as the neuroinflammatory cytokine. interleukin-6. Curcumin has been revealed to be a potential agent for treating AD following different neuroprotective mechanisms, such as inhibition of aggregation and decrease in brain inflammation. We synthesized new curcumin derivatives with the aim of providing good anti-aggregation capacity but also improved anti-inflammatory activity. Nine curcumin derivatives were synthesized by etherification and esterification of the aromatic region. From these derivatives, compound 8 exhibited an anti-inflammatory effect similar to curcumin, while compounds 3, 4, and 10 were more potent. Moreover, when the anti-aggregation activity is considered, compounds 3, 4, 5, 6, and 10 showed biological activity in vitro. Compound 4 exhibited a strong anti-aggregation effect higher than curcumin. Monofunctionalized curcumin derivatives showed better bioactivity than difunctionalized compounds. Moreover, the presence of bulky groups in the chemical structure of curcumin derivatives decreased bioactivity.
Assuntos
Palavras-chave
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Peptídeos beta-Amiloides / Citocinas / Curcumina / Anti-Inflamatórios Limite: Animals Idioma: En Revista: J Alzheimers Dis Assunto da revista: GERIATRIA / NEUROLOGIA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Panamá País de publicação: Holanda
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Peptídeos beta-Amiloides / Citocinas / Curcumina / Anti-Inflamatórios Limite: Animals Idioma: En Revista: J Alzheimers Dis Assunto da revista: GERIATRIA / NEUROLOGIA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Panamá País de publicação: Holanda