title: A germination bioassay as a toxicological screening system for studying the effects of potential prodrugs of naproxen.
abstract: A germination bioassay with radish (Raphanus sativus L.) seeds was developed as a toxicological screening system for assessing the effects of new potential prodrugs of naproxen, as an alternative to animals and animal cell toxicity screens. Both enantiomers of naproxen (6-methoxy-α-methyl-2-naphthaleneacetic acid) and naproxol (6-methoxy-β-2-naphthaleneethanol), and their racemic mixtures, inhibited the radicle growth of R. sativus at a concentration of 1mM, while only (R)-(+ )-naproxol and racemic naproxol inhibited the hypocotyl growth of R. sativus at the same concentration. Four novel combinatorial esters, naproxen naproxyl esters (6-methoxy-β-methyl-2-naphthaleneethyl 6-methoxy-α-methyl-2-naphthaleneacetate), resulting from the combinatorial chemistry of the esterification reaction between naproxen and naproxol, were synthesised and then tested in the germination bioassay, at a concentration of 0.5mM. It was found that they did not inhibit either the radicle or the hypocotyl growth of R. sativus.
authors.affiliation: Departamento de Farmacia, Facultad de Quimica, UNAM, CU Mexico, Mexico.
authors.forename: M
authors.initials: M
authors.lastname: Gonzalez-de la Parra
authors.affiliation: Departamento de Sistemas Biologicos, Universidad Autonoma Metropolitana-Xochimilco, Coyoacan, Mexico.
authors.forename: C
authors.initials: C
authors.lastname: Ramos-Mundo
authors.affiliation: Instituto de Quimica, UNAM, CU Mexico, Mexico.
authors.forename: M
authors.initials: M
authors.lastname: Jimenez-Estrada
authors.affiliation: Departamento de Farmacia, Facultad de Quimica, UNAM, CU Mexico, Mexico.
authors.forename: C
authors.initials: C
authors.lastname: Ponce-de Leon
authors.affiliation: Departamento de Farmacia, Facultad de Quimica, UNAM, CU Mexico, Mexico.
authors.forename: R
authors.initials: R
authors.lastname: Castillo
authors.affiliation: Departamento de Farmacia, Facultad de Quimica, UNAM, CU Mexico, Mexico.
authors.forename: V
authors.initials: V
authors.lastname: Tejeda
authors.affiliation: Departamento de Farmacia, Facultad de Quimica, UNAM, CU Mexico, Mexico.
authors.forename: K G
authors.initials: KG
authors.lastname: Cuevas
authors.affiliation: Instituto de Quimica, UNAM, CU Mexico, Mexico.
authors.forename: R G
authors.initials: RG
authors.lastname: Enriquez