Tetrandrine Derivatives as Promising Antibacterial Agents.
Viviana I Calvillo-Páez, Maribel Plascencia-Jatomea, Adrián Ochoa-Terán, Carmen L Del-Toro-Sánchez, Ricardo I González-Vega, Sandra M González-Martínez, Karen Ochoa Lara
Author Information
Viviana I Calvillo-Páez: Centro de Graduados e Investigación en Química, Tecnológico Nacional de México, Campus Tijuana, CP 22444 Tijuana, B.C., México. ORCID
Maribel Plascencia-Jatomea: Departamento de Investigación y Posgrado en Alimentos, Universidad de Sonora, Rosales y Encinas s/n, Col. Centro, CP 83000 Hermosillo, Sonora, México.
Adrián Ochoa-Terán: Centro de Graduados e Investigación en Química, Tecnológico Nacional de México, Campus Tijuana, CP 22444 Tijuana, B.C., México.
Carmen L Del-Toro-Sánchez: Departamento de Investigación y Posgrado en Alimentos, Universidad de Sonora, Rosales y Encinas s/n, Col. Centro, CP 83000 Hermosillo, Sonora, México.
Ricardo I González-Vega: Departamento de Investigación y Posgrado en Alimentos, Universidad de Sonora, Rosales y Encinas s/n, Col. Centro, CP 83000 Hermosillo, Sonora, México.
Sandra M González-Martínez: Departamento de Investigación en Polímeros y Materiales, Universidad de Sonora, Rosales y Encinas s/n, Col. Centro, CP 83000, Hermosillo, Sonora, México. ORCID
Karen Ochoa Lara: Departamento de Investigación en Polímeros y Materiales, Universidad de Sonora, Rosales y Encinas s/n, Col. Centro, CP 83000, Hermosillo, Sonora, México. ORCID
This work reports on the antibacterial activity of two tetrandrine derivatives, with acridine () and anthracene () units, against Gram-positive and Gram-negative bacteria of clinical importance by the broth microdilution method as well as their antioxidant activity against ABTS and DPPH radicals. Unlike natural tetrandrine, its derivatives inhibited bacterial growth, showing selectivity against with notable activity of (MIC = 0.035 μg/mL); this compound also has good activity against the ABTS radical (IC = 4.59 μg/mL). Cell membrane integrity studies and reactive oxygen species (ROS) detection by fluorescent stains helped to understand possible mechanisms related to antibacterial activity, while electrophoretic mobility assays showed that the derivatives can bind to bacterial DNA plasmid. The results indicate that can induce a general state of oxidative stress in and , while induces an oxidative response in . Complementary electrochemical studies were included.
References
J Enzyme Inhib Med Chem. 2009 Jun;24(3):715-21
[PMID: 18951284]
