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Scientists from St. Petersburg State University together with colleagues from the St. Petersburg Research Center for Environmental Safety of the Russian Academy of Sciences have discovered a new organic compound from the group of thiazolotriazoles that changes its activity under the influence of light. It is an inhibitor of a key enzyme of the nervous system-cholinesterase, which is involved in the work of many systems of the human body. Substances with this effect are used, for example, in the treatment of Alzheimer's disease or in ophthalmology. The discovery of chemists will help to "turn off" the biological activity of the drug with a laser, which means that it is safer and more accurate to affect the cells of the human body.

A graphic abstract of the article was published on the cover of the scientific journal Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy.

Most modern medicines can not be "turned on" or "turned off" at the behest of a doctor or patient: once you have taken a pill — it remains biologically active during the entire journey through the body and even after it. Today, for example, there is a problem of decontamination of antibiotics, which after human consumption inevitably enter the environment and lead to the rapid development of antibiotic-resistant strains of microorganisms.

One possible solution to this problem is the development of photopharmacology, a fairly young field of pharmacy that studies substances that can "turn on" and "turn off" under the influence of light. This approach will allow you to" turn on " the drugs when they reach the area of inflammation, or "turn off" the biological activity of the drug in time to achieve the desired therapeutic effect (or if the patient has undesirable side effects). Usually, photopharmacological agents consist of two parts: the drug itself and the photoactive"switch". However, scientists from St. Petersburg State University and the National Research Center of the Russian Academy of Sciences managed to obtain a compound that simultaneously performs both functions. It turned out to be methyl-3-amino-2-methyl-3H-thiazolo [3,2-b] [1,2,4] triazole-7-ylium-6-phosphonate.

"The discovery of this substance was partly accidental: it was first synthesized by our colleagues from the St. Petersburg State Technological Institute when they were solving problems in the field of organic synthesis. Subsequently, we conducted joint studies of this group of substances. At some point, we measured the absorption spectrum and found out that if you shine a laser with a certain wavelength (266 nanometers) into the absorption band of this compound, it will change both the absorption spectrum and its biological activity. As it turned out, the molecule changes its geometry: the phosphonate group rotates, which causes the compound to change its biological activity and reduce its inhibitory ability against cholinesterase. Moreover, after the light "off", the substance remains stable, its biological activity is not restored, " Alina Manshina, Professor of the Department of Laser Chemistry and Laser Materials Science of St. Petersburg State University, Doctor of Chemical Sciences, said about the study.

The chemists demonstrated an unusual transformation in the graphic abstract of their article. The illustration shows a couple dancing a twist (in English, twist means "turn"), and the girl is under the light of a soffit — that is, laser radiation. The editors of the magazine decided to put "laser twist" on the cover of the issue.

Although research in the field of photopharmacology is currently conducted only on laboratory animals, this area still opens up great prospects for human treatment. A "switchable" cholinesterase inhibitor can potentially be used, for example, in ophthalmology: today, similar substances, but without a light "switch", are used to reduce eye pressure. Another potential application of phosphorylated thiazolotriazole is the treatment of Alzheimer's disease and other neurodegenerative diseases.

This discovery allows you to set a lot of new tasks. How can I visualize the area where the drug was absorbed? How to determine the concentration of this drug? How to get enough biological activity? How to find not only "switches", but also "switches" of active substances? By the way, this is the topic of our new research: we are now working with compounds that, on the contrary, begin to show more pronounced biological activity under the influence of light. They are also both a drug and a photoactive component.

Professor of the Department of Laser Chemistry and Laser Materials Science of St. Petersburg State University Doctor of Chemical Sciences Alina Manshina

The team of researchers included scientists from the scientific group "Laser Synthesis" under the leadership of Professor Alina Manshina (Department of Laser Chemistry and Laser Materials Science of the Institute of Chemistry of St. Petersburg State University), scientists from the NITSEB RAS-St. Petersburg FITZ RAS, as well as employees of the resource center "Optical and Laser Methods of Substance Research" of the St. Petersburg State University Science Park.

Image - Under the influence of laser radiation, the phosphonate group rotates inside the molecule of a new organic compound, resulting in a change in its biological activity.
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