Pharmacological effects of selenium and its metabolism in rats

 Organoselenium drugs are a new class of compounds. It has antiviral, antitumor, and neurological effects in pharmacological studies. Selenium has a variety of special functions for human health and is classified as one of the essential trace elements. Inorganic selenium compounds have high toxicity and relatively low lethal dose (LC50). 

In contrast, organic selenium has high bioavailability, high bioactivity, low toxicity, and low environmental pollution. In vivo metabolism study of organic selenium in rats is conducted, which can provide a reference for the rational supplementation of organic selenium.

Drug metabolism is one of the most critical factors affecting drug action, and in vivo drug metabolism studies have always been a focal issue in drug research. In vivo drug metabolism study refers to collecting biological samples such as blood, urine, and bile after administering drugs to animals or humans. Then after analysis and separation of drugs and drug metabolites in the models, this method can comprehensively consider the effects of various in vivo factors on drugs and can genuinely and fully reflect the overall in vivo characteristics of drug metabolism. Medicilon offers a broad spectrum of high-quality services involving all micromolecule and macromolecules (protein and antibody), with service contents including in vitro ADME, in vivo pharmacokinetics, and bioanalysis. The test subjects include non-human primates, dogs, rats/mice, rabbits, and guinea pigs. Among them, the non-human primate experimental solution and the isotope solution for protein/antibody have been recognized as essential laboratory solutions by Shanghai Municipal People's Government.

Selenium is vital to human health and can cause many diseases when deficient. Pharmacological research shows that selenium has the following effects.

(1) Cancer prevention and anti-cancer

Selenium has an inhibitory effect on the growth of human tumors and can be used in tumor treatment, such as for the prevention and treatment of colorectal cancer. The mortality rate of cancer in different regions is negatively correlated with the amount of selenium in local food and the level of selenium in whole human blood, meaning that the more selenium in local people's blood, the lower the incidence of cancer. High doses of selenium supplementation can reduce tumors, and cancer incidence can be suppressed by more than 50%.

(2) It has a regulatory effect on immune function

Selenium is an essential trace element, and its critical function is immunomodulation and antioxidant effect. Many studies at home and abroad have confirmed that selenium has precise immunomodulatory functions, including cellular and humoral immunity.

(3) The effect on cardiovascular

Selenium can reduce blood viscosity, lower blood lipids, significantly reduce cholesterol, triglycerides, and LDL levels, reduce thrombosis, and protect the heart muscle. Therefore, selenium is known as the "patron saint of the heart."

(4) The effect on diabetes

Selenium can have a protective effect on the small blood vessels in and around the pancreas, derived from the free radical scavenging function of selenium-containing enzymes, thus exhibiting a hypoglycemic effect. By allowing diabetic patients to take selenium quantitatively, doctors can play a role in protecting and restoring the function of pancreatic islets, which is conducive to improving the symptoms of diabetes and reducing the level of glucosylated hemoglobin in urine. Therefore, some people call selenium the "insulin" of trace elements.

(5) Effect on oxidative damage of tissues

To investigate the effect of selenium on oxidative damage of brain tissues after acute seizures in mice. Sixty healthy mice were selected and divided into an observation group, control A group, and control B group, 20 mice each. 

The results showed that the time of appearance of epilepsy, seizure level, MDA, GSH-Px activity, and water maze escape time was statistically significant (P<0.05) in the three groups of mice. Therefore, acute epilepsy in mice leads to oxidative damage to brain tissue, and selenium supplementation in mice can significantly improve MDA content and GSH-Px activity and reduce the damage caused to brain tissue.

(6) Liver disease

The Chinese Academy of Medical Sciences, after 16 years of research, confirmed that selenium deficiency is one of the important causes of liver cancer. The more obvious selenium deficiency is, the more serious the disease is. Selenium deficiency can reduce the scavenging power of hepatocytes to peroxides, leading to cell membrane lipid peroxidation damage, which in turn causes cell necrosis and mutation, forming a vicious circle. In order to prevent the development and deterioration of the disease, patients with liver disease need to supplement the right amount of selenium as early as possible to improve the blood selenium level, which can help prevent viral hepatitis, liver fibrosis, cirrhosis, and liver cancer. The right amount of selenium supplementation can eventually eliminate about 90% of the hepatitis B virus.

(7) Detoxification of heavy metals and other elements

Selenium antagonizes these heavy metals and is known as a "natural antidote for heavy metals." Clinical trials have shown that the trace element selenium can have antagonistic effects on these heavy metals, effectively blocking the potential harm caused by heavy metals to human health. Many human diseases are caused by pollution in the living environment. The natural detoxifying effect of selenium on harmful heavy metal ions is instrumental in the battlefield of resistance to environmental corrosion with human beings.

Selenium is one of the essential trace elements for the growth and development of animals, with crucial biological functions, and its distribution varies in different tissues and organs. It has been shown that selenium is mainly deposited in animals' livers, kidneys, and pancreas and less in the blood, bones, and muscles.

2, In vivo metabolism study of the organoselenium drug in rats

It used selenium-rich yeast as the carrier of organic selenium, the in vivo metabolism study of drugs in rats treated with different doses of organic selenium in dosage form to provide a theoretical basis for organic selenium intervention and drug use. It was found that after grouping, there was no statistically significant difference in the body weight of rats in each group. After single gavage administration, with the increase of dose, its absorption phase half-life and elimination half-life increased, the peak time was pushed back, and the peak concentration became higher. Still, it was basically eliminated at 24 h in vivo. Therefore, the extravascular oral two-compartment model curve is well-fitted, and the organoselenium is metabolized rapidly in rats. It drops to a lower level at 12 h and is eliminated at 24 h. This can provide a reference for the appropriate supplementation of organoselenium.

Selenium in animals and humans is mainly realized through selenoproteins. So far, 25 kinds of selenoproteins have been found in the human body, which can be divided into two major categories: the first one exists in the free state in cells, i.e., free selenoproteins, there are 16 kinds; the second one is located on cell membrane structure, which is called membrane selenoproteins, there are nine kinds. It was found that the human body mainly absorbs selenium from food through the duodenum's intestinal wall cells. The cells rely on the amino acid transport system and the metabolic system of GSH-Px to complete the absorption of selenium.