Boron-containing compounds (BCCs) are attractive chemical entities in drug development. Some of these compounds have been used in the treatment of human disease, and studies on their pharmacodynamics suggest that they employ multiple forms of activity. However, less is known about the pharmacokinetic profile of these molecules. Areas covered: The herein compiled reported data is presented in accordance with the classical 'ADME' system for identifying the scope of BCCs in the respective fields. Our analysis suggests that these compounds have several distinct ways to move within the human body, and that the specific structural features of each molecule account for its distinct pharmacokinetic profile. These insights should be useful for designing BCCs with a desired effect. Expert opinion: Increasing knowledge about the pharmacokinetics of BCCs is providing a broader understanding about the design of new release systems and potential drugs, as well as probable protein transporters that could be related to key roles in physiological processes. These transporters may be involved in sodium transport, hormone release and regulation of the cell cycle. The shared features among groups of BCCs are being identified in order to apply these insights to the design of advantageous compounds.
Background:
Boron is considered a trace element that induces various effects in systems of
the human body. However, each boron-containing compound exerts different effects.
Objective:
To review the effects of 2-Aminoethyldiphenyl borinate (2-APB), an organoboron compound,
on the human body, but also, its effects in animal models of human disease.
Methods:
In this review, the information to showcase the expansion of these reported effects through
interactions with several ion channels and other receptors has been reported. These effects are relevant
in the biomedical and chemical fields due to the application of the reported data in developing therapeutic
tools to modulate the functions of the immune, cardiovascular, gastrointestinal and nervous systems.
Results:
Accordingly, 2-APB acts as a modulator of adaptive and innate immunity, including the production
of cytokines and the migration of leukocytes. Additionally, reports show that 2-APB exerts
effects on neurons, smooth muscle cells and cardiomyocytes, and it provides a cytoprotective effect by
the modulation and attenuation of reactive oxygen species.
Conclusion:
The molecular pharmacology of 2-APB supports both its potential to act as a drug and the
desirable inclusion of its moieties in new drug development. Research evaluating its efficacy in treating
pain and specific maladies, such as immune, cardiovascular, gastrointestinal and neurodegenerative
disorders, is scarce but interesting.
Some vegetable oils show beneficial effects in modulating neurodegeneration; in this work, we evaluated the therapeutic potential of corn and olive oils against neurodegenerative processes using the acute parkinsonism murine model induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in C57BL6 mice. The effects of corn and olive oils were quantified by the performance of mice in the open field and rotarod, and grasp strength tests and neuronal survival in the substantia nigra and striatum were determined by immunohistochemistry. Extra-virgin olive oil decreased the toxicity induced by MPTP administration judged by the performance in the behavioral motor tests and the number of total neurons in the analyzed brain regions. In contrast, corn oil only produced discrete changes in the behavioral and histological evaluations. Despite the numerous benefits of olive oil, its active substances that confer desirable effects and their mechanism of action remain unclear. Our observations can help to understand the ameliorative effects of some natural oils on neurodegeneration induced by some toxins, particularly the attenuation of neural damage related to toxin-induced parkinsonism or other pathologies that comprise neuronal death and motor disruption.
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