title: Current data regarding the structure-toxicity relationship of boron-containing compounds.
abstract: Boron is ubiquitous in nature, being an essential element of diverse cells. As a result, humans have had contact with boron containing compounds (BCCs) for a long time. During the 20th century, BCCs were developed as antiseptics, antibiotics, cosmetics and insecticides. Boric acid was freely used in the nosocomial environment as an antiseptic and sedative salt, leading to the death of patients and an important discovery about its critical toxicology for humans. Since then the many toxicological studies done in relation to BCCs have helped to establish the proper limits of their use. During the last 15 years, there has been a boom of research on the design and use of new, potent and efficient boron containing drugs, finding that the addition of boron to some known drugs increases their affinity and selectivity. This mini-review summarizes two aspects of BCCs: toxicological data found with experimental models, and the scarce but increasing data about the structure-activity relationship for toxicity and therapeutic use. As is the case with boron-free compounds, the biological activity of BCCs is related to their chemical structure. We discuss the use of new technology to discover potent and efficient BCCs for medicinal therapy by avoiding toxic effects.
authors.affiliation: Departamento de Bioquímica, Sección de Estudios de Posgrado e Investigación. Escuela Superior de Medicina, Instituto Politécnico Nacional. Plan de San Luis y Díaz Mirón, 11340, México City, México; Departamento de Fisiología, Sección de Estudios de Posgrado e Investigación. Escuela Superior de Medicina, Instituto Politécnico Nacional. Plan de San Luis y Díaz Mirón, 11340, México City, México.
authors.forename: E D
authors.initials: ED
authors.lastname: Farfán-García
authors.affiliation: Departamento de Fisiología, Sección de Estudios de Posgrado e Investigación. Escuela Superior de Medicina, Instituto Politécnico Nacional. Plan de San Luis y Díaz Mirón, 11340, México City, México.
authors.forename: N T
authors.initials: NT
authors.lastname: Castillo-Mendieta
authors.affiliation: Departamento de Bioquímica, Sección de Estudios de Posgrado e Investigación. Escuela Superior de Medicina, Instituto Politécnico Nacional. Plan de San Luis y Díaz Mirón, 11340, México City, México; Departamento de Fisiología, Sección de Estudios de Posgrado e Investigación. Escuela Superior de Medicina, Instituto Politécnico Nacional. Plan de San Luis y Díaz Mirón, 11340, México City, México.
authors.forename: F J
authors.initials: FJ
authors.lastname: Ciprés-Flores
authors.affiliation: Unidad Profesional Interdisciplinaria de Biotecnología, Instituto Politécnico Nacional, Avenida Acueducto s/n, Barrio La Laguna Ticomán, 07340, México.
authors.forename: I I
authors.initials: II
authors.lastname: Padilla-Martínez
authors.affiliation: Departamento de Bioquímica, Sección de Estudios de Posgrado e Investigación. Escuela Superior de Medicina, Instituto Politécnico Nacional. Plan de San Luis y Díaz Mirón, 11340, México City, México.
authors.forename: J G
authors.initials: JG
authors.lastname: Trujillo-Ferrara
authors.affiliation: Departamento de Fisiología, Sección de Estudios de Posgrado e Investigación. Escuela Superior de Medicina, Instituto Politécnico Nacional. Plan de San Luis y Díaz Mirón, 11340, México City, México. Electronic address: msoriano@ipn.mx.
authors.forename: M A
authors.initials: MA
authors.lastname: Soriano-Ursúa
mesh_terms: D000818:Animals; D001896:Boron Compounds / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity*; D015195:Drug Design; D015507:Drugs, Investigational / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D004785:Environmental Pollutants / Q000737:chemistry / Q000633:toxicity*; D006801:Humans; D015394:Molecular Structure; D009153:Mutagens / Q000737:chemistry / Q000633:toxicity; D013329:Structure-Activity Relationship; D023382:Toxicity Tests, Acute; D036401:Toxicity Tests, Chronic
chemical_list: D001896:Boron Compounds; D015507:Drugs, Investigational; D004785:Environmental Pollutants; D009153:Mutagens
keywords: Acute toxicity; Boron; Boron containing compounds; Central nervous system; Eukaryotic and prokaryotic cells