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1.
J Pharm Biomed Anal ; 62: 79-86, 2012 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-22305080

RESUMO

Strategies to control diffusion of malaria needs to account for the increase of resistance of the parasite to the conventional antimalarial drugs. It has been proposed that a traditional aqueous preparation from Artemisia annua, with a low content of the active compound, artemisinin, may reduce the risk of resistance of the protozoa and be relatively more effective in the treatment of the disease. The solubility properties of the molecule have been the matter of concern about the therapeutic usefulness of herbal teas from A. annua. The present study aimed at analysing the chemical profile of a tea infusion from A. annua. Tea from A. annua was prepared through infusion of the plant aerial parts in water for 1, 24 and 48 h. Content of artemisinin was determined by HPLC-ELSD. Overall chemical characterization of the extracts was carried out by a combination of metabolomic techniques. The artemisinin content varied only slightly in the three different extracts (about 0.12%). A series of mono-caffeoyl- and mono-feruloyl-quinic acids, di-caffeoyl- and di-feruloyl-quinic acids was identified as main components of the tea infusion, together with some flavonoids. Reconstitution of the same extracts in less polar or apolar solvents resulted in a different composition with no phenolics and a much lower concentration of artemisinin.


Assuntos
Artemisia/química , Chá/química , Cromatografia Líquida de Alta Pressão , Limite de Detecção , Espectroscopia de Ressonância Magnética , Reprodutibilidade dos Testes , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em Tandem
2.
Bioorg Med Chem ; 18(16): 5903-14, 2010 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-20667739

RESUMO

Several members of a new family of non-sugar-type alpha-glucosidase inhibitors, bearing a phthalimide moiety connected to a variously substituted phenoxy ring by an alkyl chain, were synthesized and their activities were investigated. The efficacy of the inhibition activity appeared to be governed by the chain length of the substrate. Substrates possessing 10 carbons afforded the highest levels of activity, which were one to two orders of magnitude more potent than the known inhibitor 1-deoxynojirimycin (dNM). Furthermore, structure-activity relationship studies indicated a critical role of electron-withdrawing substituents at the phenoxy group for the activity. Derivatives bearing a chlorine atom along with a strong electron-withdrawing group, such as a nitro group, were the most potent of the series.


Assuntos
Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Inibidores de Glicosídeo Hidrolases , Ftalimidas/química , Ftalimidas/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Inibidores Enzimáticos/síntese química , Humanos , Ftalimidas/síntese química , Saccharomyces cerevisiae/enzimologia , Relação Estrutura-Atividade , alfa-Glucosidases/metabolismo
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