ABSTRACT
Lyophilized aqueous extract (LAE) from Lychnophora pinaster Mart (Asteraceae) aerial parts was evaluated in the search of possible biological activities. LAE exhibited trypanocidal activity (113.62 mg/mL), but could not inhibit 5-lipoxygenase in vitro (17 percent of inhibition). LAE chemical characterization by HPLC with UV-Diode Array Detector showed the presence of caffeic acid, isochlorogenic acid, vitexin, isovitexin and quercetin, in comparison with authentic samples.
ABSTRACT
O fitoterápico Ierobina®, comercializado no mercado nacional há 67 anos, tem uso indicado para o tratamento de dispepsias. O fitoterápico é constituído pelos extratos fluidos de três espécies nativas (Solanum paniculatum, Remijia ferruginea e Jacaranda caroba) e uma exótica (Erythraea centaurium). O presente estudo descreve a identificação de marcadores químicos para os extratos das espécies constituintes da Ierobina® e a obtenção de perfis cromatográficos de referência para os mesmos, os quais contribuirão para o estabelecimento de protocolos para o controle de qualidade do fitoterápico.
ABSTRACT
Do extrato hexânico das raízes de Zeyheria montana M., uma Bignoniácea conhecida como bolsa‑de‑pastor, empregada popularmente contra doenças de pele, foram isolados os seguintes compostos: lapachol, α‑lapachona, desidro‑α‑lapachona, 4‑hidróxi-α‑lapachona, β‑sitosterol, ácido esteárico e uma mistura de ácidos graxos. Estas substancias foram identificadas por métodos espectrométricos usuais e/ou comparação com amostras autênticas. No cromatograma do extrato etanólico, obtido por CLAE, foram identificados os picos correspondentes às naftoquinonas isoladas e ao ácido esteárico. A ocorrência de naftoquinonas nas raizes de Z. montana e a atividade antimicrobiana comprovada para o lapachol e a α‑lapachona justificam o uso popular desta espécie.
Zeyheria montana M. (Bignoniaceae) is a widespread species in the Cerrado area of Minas Gerais, Brazil, and is popularly known as bolsa‑de‑pastor. In the Brazilian tradicional medicine its roots are used for the treatment of skin diseases. Several species of Bignoniaceae contain naphthoquinones, and lapachol was previously reported in the stem wood of Z. digitalis. This paper describes the isolation of three naphtoquinones from Z. montana stem barks, namely α‑lapachone, dehydro‑α‑lapachone and 4‑hydroxy‑α‑lapachone, besides lapachol, stearic acid and β‑sitosterol. Furthermore, we report the HPLC fingerprint for the species, which allowed the identification of the isolated compounds, except β‑sitosterol. Since the in vitro antimicrobial activity of lapachol and α‑lapachone has been previously described, the presence of these naphthoquinones in the roots of Z. montana corroborates its popular use for the treatment of skin diseases.
ABSTRACT
Ammonium salt derivatives of natural allylphenols were synthesized with the purpose of obtaining potential peripheral analgesics. These drugs, by virtue of their physicochemical properties, would not be able to cross the blood brain barrier. Their inability to enter into the central nervous system (CNS) should prevent several adverse effects observed with classical opiate analgesics (Ferreira et al., 1984). Eugenol (1) O-methyleugenol (5) and safrole (9) were submitted to nitration, reduction and permethylation, leading to the ammonium salts 4, 8 and 12. Another strategy applied to eugenol (1), consisting in its conversion to a glycidic ether (13), opening the epoxide ring with secondary amines and methylation, led to the ammonium salts 16 and 17. All these ammonium salts showed significant peripheral analgesic action, in modified version of the Randall-Sellito test (Ferreira et al. 1978), at non-lethal doses. The ammonium salt 8 showed an activity comparable to that of methylnalorphinium, the prototype of an ideal peripheral analgesic (Ferreira et al., 1984).