IPN leads publication on boron drugs

IPN leads publication on boron drugs

Adda Avendaño

A group of researchers from Spain, Romania, the United States, and Uruguay, led by Dr. Marvin Antonio Soriano Ursúa, a professor and researcher at the Escuela Superior de Medicina (ESM) of the Instituto Politécnico Nacional (IPN), combined their efforts to provide a comprehensive overview of research conducted on boron for therapeutic purposes. They generated an international scientific publication, which was published in the specialized journal Chemical Reviews.

It is worth noting that this is the most important chemistry journal worldwide, published by the American Chemical Society (ACS) since 1924, entirely dedicated to the field of multidisciplinary chemistry, covering organic, inorganic, physical, analytical, theoretical, and biological chemistry. Its articles undergo meticulous peer review, and its prestige places it among the top 10 global scientific journal rankings and at the forefront in terms of citations or Impact Factor (IF).

Fifteen years of relentless boron study

IPN researcher Soriano Ursúa explained that he has dedicated 15 years to studying this element found in nature. During this time, he has discovered that when combined with other molecules, compounds can be formed that may support the treatment of neurodegenerative diseases with high economic and social impact.

"We started with bronchodilators, and then we found that organoborane substances can be developed into drugs capable of reaching the central nervous system, particularly the brain. So, we began evaluating them, first in silico, that is, through computational simulation, and then in animal models to observe how they behave in conditions such as Parkinson's, Alzheimer's, and even SARS-CoV-2, obtaining very promising results," stated the polytechnic professor.

The head of the Neurophysiology Laboratory at ESM added that with his research group and undergraduate and graduate students, they have found some boron-containing substances that can modify metabolism, which can be used to modulate body mass and treat people with obesity or possibly diabetes as well. Furthermore, other research indicates that these compounds can also be beneficial for people with epilepsy.

Boron research had been limited compared to that of other elements; however, researchers worldwide have shown that integrating it into other molecules has advantages over currently available medications in preventing and treating complex conditions such as cancer and some fungal infections. They are safe and effective potential drugs for treating multiple diseases in the future, including neurodegenerative and metabolic diseases.

The international group

To comprehensively address the panorama and explore the frontier of knowledge on boron and organoboron compounds, the recipient of the 2022 Boron in the Americas Award tasked himself with forming a group of nine internationally renowned specialists led by him, dedicated to the study of the "fifth element" of nature.

Justin Grams, Ann Rosenblum, and Webster Santos from the Department of Chemistry and the Drug Research Center at Virginia Tech University, USA, have studied boronated peptides; Ion Romulus Scorei and Andrei Bita from the Department of Pharmacognosy and Phytotherapy at the Faculty of Pharmacy, University of Medicine and Pharmacy in Krakow, Romania, have studied boronates found in nature.

Also involved were Dr. Hugo Cerecetto from the Center for Nuclear Research and the Faculty of Sciences at the University of the Republic, Uruguay, and Dr. Clara Viñas from the Institute of Materials Science in Barcelona, Spain, who are experts in the design and study of boron geometrical complexes or clusters. From Mexico, Antonio Abad García and Dr. Marvin Antonio Soriano Ursúa, both from the Physiology Academy and the Graduate Studies and Research Section (SEPI) of ESM at IPN, have studied boron-containing molecules with structural similarity to available medications.

"It took us two years to mature the article and edit it to address all the comments made by our colleagues from the specialized journal during the review process. So, we delved into historical documents, the first research on boron, the probable side effects with scientific evidence, how the new molecules would act in the body, advances in synthesizing boronated substances, and trends in generating new molecules and their effects on humans, each in their field of expertise," he detailed.

The emerging pharmacology of boron

Recipient of the 2013 National Youth Science and Technology Award, Dr. Soriano Ursúa explained that in more than 100 pages, the authors managed to combine their knowledge and research to generate a document containing a comprehensive review of the role of boron in emerging pharmacology.

They described how boron exists in nature and how 50 years ago, compounds containing boron first emerged as pharmacophores, molecules of interest in drug design, as it was found that they produced physiological effects specific to certain drugs, sometimes with better effects.

He noted that after years of research, five boron-derived drugs have been approved by the Food and Drug Administration (FDA) - an agency of the United States Department of Health and Human Services - for cancer, infections, and inflammatory conditions.

The drugs approved and used commercially are: bortezomib and ixazomib citrate, one injectable and the other oral, both used against multiple myeloma; tavaborol, a topical antifungal treatment for nails; crisaborol, a topical ointment for eczema; and vaborbactam, which in combination with meropenem is a new antibiotic indicated for complicated urinary and intra-abdominal infections and in-hospital pneumonia in adults, including that associated with mechanical ventilation.

The rise of boron-containing compounds in medicinal chemistry and their use in some treatments is based on the multifaceted and unique characteristics of natural and synthetic boron-containing compounds and the diversity of their applications. Therefore, it is expected that research on boron chemistry in conjunction with various biological objectives will continue to explore new drugs with equal or greater effectiveness than current ones. The article has been assigned the digital identifier (DOI): 10.1021/acs.chemrev.3c00663 and will be available this year.

Publications from the American Chemical Society are leaders in accessing information and research related to chemistry through peer-reviewed journals and e-books, where Nobel Prize winners in Chemistry and Medicine and the best authors from around the world have published. This exclusive group now includes researchers from the School of Medicine at IPN as well.

According to the polytechnic teacher, Level II, of the National System of Researchers (SNII), this publication is a recognition of the trajectory of each of the authors, particularly the research work carried out at IPN, and is also a valuable contribution that can pave the way for the exploration of new boron molecules that are effective in creating new drugs aimed at alleviating the ailments of the national and global population.

Selección Gaceta Politécnica #171. (February 29th, 2024). IPN Imagen Institucional: Read the full magazine in Spanish here.