Disruption of motor behavior and injury to the CNS induced by 3-thienylboronic acid in mice.

The scarcity of studies on boron containing compounds (BCC) in the medicinal field is gradually being remedied. Efforts have been made to explore the effects of BCCs due to the properties that boron confers to molecules. Research has shown that the safety of some BCCs is similar to that found for boron-free compounds (judging from the acute toxicological evaluation). However, it has been observed that the administration of 3-thienylboronic acid (3TB) induced motor disruption in CD1 mice. In the current contribution we studied in deeper form the disruption of motor performance produced by the intraperitoneal administration of 3TB in mice from two strains (CD1 and C57BL6). Disruption of motor activity was dependent not only on the dose of 3TB administered, but also on the DMSO concentration in the vehicle. The ability of 3TB to enter the Central Nervous System (CNS) was evidenced by Raman spectroscopy as well as morphological effects on the CNS, such as loss of neurons yielding biased injury to the substantia nigra and striatum at doses ≥200mg/kg, and involving granular cell damage at doses of 400mg/kg but less injury in the motor cortex. Our work acquaints about the use of this compound in drug design, but the interesting profile as neurotoxic agent invite us to study it regarding the damage on the motor system.

Effects of succinic acid derivatives on ex vivo acetylcholinesterase activity.

In the present study the acetylcholinesterase (AChE) inhibition and acute toxicity of two succinic acid derivatives were compared with tacrine. Administration of a single dose of each of two succinic acid derivatives produced a time and dose-dependent inhibition of brain AChE activity. Although the magnitude of the cholinergic effects observed with the two succinic acid derivatives was similar to that seen with tacrine and other AChE inhibitors, the toxicity study showed that the new inhibitors have less adverse side effects.

[Toxicity and hypotensive effect of L-arginine oxoborolidinone and its modulation by methylene blue. Comparison with L-arginine, nitrite, and nitrate]. / Toxicidad y efecto hipotensor de oxoborolidinona de L-arginina y su modulación por azul de metileno. Comparación con L-arginina, nitrito y nitrato.

Nitric oxide is synthesized by constitutive oxide nitric synthase from the guanidine group of L-arginine. L-arginine, oxoborolidinone of L-arginine, nitrite and nitrate showed dose-dependent hypotensive effects after injection via the femoral vein in Wistar rats. The hypotensive effects were shifted to the right after treatment with methylene blue, which is a synthetic phenothiazine inhibitor of guanylate cyclase. Oxoborolidinone of L-arginine had high hypotensive effects with an effective half dose of 10 eta moles kg-1 and of mumoles kg-1 for methylene blue. Methylene blue also attenuated the toxic effects of all the tested compounds.