Scheme of the production of pituitary steroid hormones from cholesterol. A

The synthesis of various steroid hormones from cholesterol is carried out by successive enzymatic reactions. The main pathway of steroidogenesis, leading to the formation of mineralocorticoids, glucocorticoids, androgens and estrogens. The first step in the conversion of cholesterol to pregnenolone is a reaction that occurs in all steroid-producing tissues. This stage limits the rate of synthesis of steroid hormones. Subsequent enzymatic reactions of steroidogenesis occur only in certain tissues.

In the human body, there is no mechanism that contributes to the accumulation of steroid hormones in cells. Only the hormonal precursor in the form of cholesterol esters accumulates in significant amounts in steroid-producing cells. The steroid hormones synthesized in them quickly enter the bloodstream through the cell membrane, and, exercising their hormonal regulation, are gradually excreted from the body (in the active form, steroid hormones have a relatively short half-life).

Regulation of the synthesis of steroid hormones is carried out with the help of peptide hormones produced by the hypothalamus and pituitary gland. Corticotropin, produced by the pituitary gland, stimulates the secretion of corticosteroids (mineralcorticoids and glucocorticoids). Gonadotropins (follitropin and luteotropin), produced by the anterior pituitary gland, stimulate the synthesis of androgens and estrogens. In turn, gonadoliberin produced by the hypothalamus controls the synthesis and release of pituitary gonadotropins.

The production of peptide hormones by the hypothalamus and pituitary gland depends on the concentration of controlled hormones in the blood and is regulated by the feedback principle. The ingestion of exogenous steroid hormones into the body at a rate exceeding the rate of synthesis of the corresponding endogenous steroid hormones almost completely suppresses the production of stimulating peptide hormones, which leads to the suppression of the mechanisms of synthesis of the corresponding endogenous hormones, and as a result, the overall hormonal balance in the body is disturbed.

One of the types of chemical synthesis of steroid hormones was proposed by I. V. Torgovym in 1984 and is used for industrial production in our time. The method is based on the condensation of bicyclic vinylcarbinols with cyclic 1,3-diketones into steroidal diketones:

Depending on the starting components, the reaction proceeds in methanol with or without an alkaline catalyst.

Type VII steroid dienones are the starting compounds for the production of hormonal steroids, primarily estrone and estradiol, as well as their derivatives, many of which have a physiological effect. Moreover, the path of complete synthesis made it possible to obtain various stereoisomers of natural hormones of the estran series, which is important for studying the relationship between spatial structure and hormonal activity.

For the transition from compound VII to estrone derivatives, it is necessary to carry out the reduction of double bonds. This problem is solved by catalytic hydrogenation in the presence of a palladium or nickel catalyst with the formation of 14a-epimers with a reduced d14 double bond (XI).

The formation of XII results in a racemic mixture of isomers, which are converted into the optically active L-form by the culture of S. cervisiae immobilized on a polyacrylamide gel.

Based on the available estran derivatives, it was possible to obtain numerous 19-norsteroids with anabolic and histogenic effects. Thus, 19-nortestosterone (XX) is obtained from the 3-methyl ester of estradiol (XII) through the intermediate product carbinol (XIX).

Nandrolone (Nortestosterone)

Pharmacological action - androgenic, anabolic. It binds to specific receptor proteins on the surface of cells of target organs, forms a receptor-nandrolone complex and, penetrating into the cell nucleus, causes the activation of regulatory genes. Androgenic properties consist in the activation of a cascade of reactions that stimulates the synthesis of nucleic acids (DNA, RNA), structural proteins, increased tissue respiration and oxidative phosphorylation in skeletal muscles with the accumulation of macroergs (ATP, creatine phosphate); increases muscle mass and reduces the amount of adipose tissue. Accelerates the growth of male genital organs and the formation of secondary sexual characteristics according to the male type. Stimulates the secretory activity of the male sex glands (activation of the process of spermatogenesis), in large doses reduces the synthesis of endogenous sex hormones by inhibiting the production of FSH and LH by the pituitary gland (negative feedback). The anabolic effect is manifested by the activation of reparative processes in the epithelium, bone and muscle tissues as a result of stimulation of protein synthesis and structural components of cells. Increases the complete absorption of amino acids from the small intestine (on the background of a diet rich in proteins), creating a positive nitrogen balance. Stimulates the production of erythropoietin. Undergoes biotransformation in the liver, excreted mainly in the urine.

Above are excerpts from the description of the action of nandrolone from the drug encyclopedia. To some extent, it is clear that this substance can serve as a good tool for building muscle mass and increasing strength. Moreover, it should be noted that it is practically a safe means. According to its structure, nandrolone has a rather weak androgenic effect, which means a low suppression of endogenous testosterone production and a minimal aromatization effect (conversion of excess testosterone into estrogens - female sex hormones). And as a result, in comparison with androgenic drugs, nandrolone contributes to less fluid retention, which does not create high blood pressure. For the liver, nandrolone is not dangerous even at high dosages. In addition, the highly anabolic nature of the drug contributes to a truly strong weight gain due to muscle mass and an increase in the strength of the user. All this has made nandrolone the most popular steroid used in professional (and not only) sports over the decades.

Nandrolone can be of different actions, it all depends on the ether. If it is phenylpropionate, then the effect of the drug begins quite quickly, already on the 2nd or 3rd day, but it also ends just as quickly, therefore, for effective use, men need at least two injections per week, women need one. Nandrolone phenylpropionate can be used for weight gain and strength gains in combination with many other short and long acting anabolic or androgenic steroids. It is effective to include nandrolone phenylpropionate at the end of the course, in combination with highly anabolic drugs such as Winstrol, you can achieve a smooth exit and the ability to keep the result longer. In Russia, this drug has long disappeared from pharmacy chains, before its name was phenobolin. To date, only the Indian version of nandrolone phenylpropionate can be purchased in dosages of 50 and 200 mg. Of course, an n.f. and in other places, but in Russia mainly "Indian phenyl" is available. Here, it is not faked, ceramic firing, used as a label on vials and ampoules, serves as a kind of protection. Nandrolone decanoate has a long anabolic effect. It is enough to make one injection per week to ensure a permanent working effect. The duration of action of one injection lasts at least two weeks. N. D. is one of the best means for building muscle mass and increasing strength. The most effective use in parallel with other anabolic or androgenic drugs. One of the best combinations is nandrolone decanoate and methandienone. Together, these drugs can work wonders, because. the action of one steroid is enhanced by the action of another. Nandrolone decanoate is equally effective for both advanced steroid users and novice users.

The main disadvantage of nandrolone, like many steroids administered to the human body, is feedback, that is, inhibition of the activity of the glands that are responsible for the synthesis of this hormone in the body. Other steroids (mainly taken orally) have a methyl group at C17, which allows you to prolong the metabolism of the substance in the body, thereby prolonging its action. The breakdown of such anabolics occurs in the liver, and this methyl group harms the cells of the organ, which causes a hepatotoxic effect. Also, steroids are able to aromatize in the liver, forming estrogens, which can lead to various disorders, up to changes in primary sexual characteristics (gynecomastia in men). At the same time, the introduction of male hormones into the female body causes androgenization: active growth of hair on the body, coarsening of the voice.

Structure

They are derivatives of cholesterol - steroids.

The structure of female sex hormones

Synthesis

Female hormones: estrogens synthesized in ovarian follicles progesterone- in the corpus luteum. Partially hormones can be formed in adipocytes as a result of aromatization of androgens.

Scheme of the synthesis of steroid hormones (complete scheme)

Regulation of synthesis and secretion

Activate: estrogen synthesis - luteinizing and follicle-stimulating hormones, progesterone synthesis - luteinizing hormone.

Reduce: sex hormones by a negative feedback mechanism.

1. At the beginning of the cycle, several follicles begin to increase in size in response to FSH stimulation. Then one of the follicles begins to grow faster.
2. Under the influence of LH, the granulosa cells of this follicle synthesize estrogens, which suppress the secretion of FSH and promote the regression of other follicles.
3. The gradual accumulation of estrogens towards the middle of the cycle is a stimulus for the secretion of FSH and LH before ovulation.
4. A sharp increase in the concentration of LH can also be due to the gradual accumulation of progesterone (under the influence of the same LH) and the triggering of the positive feedback mechanism.
5. After ovulation, the corpus luteum is formed, producing progesterone.
6. High concentrations of steroids suppress the secretion of gonadotropic hormones, the corpus luteum degenerates as a result, and the synthesis of steroids decreases. This reactivates FSH synthesis and the cycle repeats.
7. When pregnancy occurs, the corpus luteum is stimulated by chorionic gonadotropin, which begins to be synthesized two weeks after ovulation. The concentrations of estrogens and progesterone in the blood during pregnancy increase tenfold.

Hormonal changes during the menstrual cycle

Targets and effects

Estrogens

1. At puberty estrogens activate the synthesis of protein and nucleic acids in the genital organs and ensure the formation of sexual characteristics: accelerated growth and closure of the epiphyses of long bones, determine the distribution of fat on the body, skin pigmentation, stimulate the development of the vagina, fallopian tubes, uterus, the development of the stroma and ducts of the mammary glands, axillary and pubic hair growth.

2. In the body of an adult woman:

Biochemical effects

Other effects

activates the synthesis of transport proteins in the liver for thyroxine, iron, copper, etc., stimulates the synthesis of blood coagulation factors - II, VII, IX, X, plasminogen, fibrinogen, inhibits the synthesis of antithrombin III and platelet adhesion, increases the synthesis of HDL, suppresses LDL, increases the concentration of TAG in the blood and lowers cholesterol, reduces the resorption of calcium from bone tissue.

stimulates the growth of the glandular epithelium of the endometrium, determines the structure of the skin and subcutaneous tissue, inhibits intestinal motility, which increases the absorption of substances.

Progesterone

Progesterone is the main hormone of the second half of the cycle and its task is to ensure the onset and maintenance of pregnancy.

Biochemical effects	Other effects
increases the activity of lipoprotein lipase on the capillary endothelium, increases the concentration of insulin in the blood, inhibits sodium reabsorption in the kidneys, is an inhibitor of respiratory chain enzymes, which reduces catabolism, accelerates the excretion of nitrogen from the body of a woman.	relaxes the muscles of the pregnant uterus, enhances the reaction of the respiratory center to CO 2, which reduces the partial pressure of CO 2 in the blood during pregnancy and in the luteal phase of the cycle, causes breast growth during pregnancy, immediately after ovulation, it is a chemattractant for spermatozoa moving through the fallopian tubes.

Pathology

Hypofunction

Congenital or acquired hypofunction of the gonads inevitably leads to osteoporosis. Its pathogenesis is not well understood, although estrogens are known to slow bone resorption in women of childbearing age.

hyperfunction

Women. Raise progesterone can be manifested by uterine bleeding and menstrual irregularities. Raise estrogen may present with uterine bleeding.

Men. High concentrations estrogen lead to underdevelopment of the genital organs (hypogonadism), atrophy of the prostate and spermatogenic epithelium of the testicles, female-type obesity and growth of the mammary glands.

• < Назад

The greatest number of steroid hormones is synthesized in the adrenal cortex, they are called corticosteroids. The most important of these are hydrocortisone, corticosterone and aldosterone. In the sex glands, male and female sex hormones related to steroids are synthesized. (A small amount of sex hormones is also formed in the adrenal cortex.) Male sex hormones are formed in the testes - androgens the most important of which is testosterone. The ovaries produce female sex hormones estrogens And progestins. The main representative of estrogen is estradiol.

Unlike peptide hormones, steroid hormone receptors are located not in the outer cell membrane, but in the cytoplasm of target cells. This difference is determined by the fact that steroid hormones are able to pass through the outer lipid membrane of cells, while peptide hormones are not. When a hormone interacts with a specific receptor, a hormone-receptor complex is formed, which is transported to the cell nucleus. In the nucleus, this complex binds to a specific DNA region, activating its transcription, which leads to the synthesis of certain mRNAs, and then the corresponding proteins responsible for the necessary biological effect (Fig. 12).

Rice. 12. Scheme of the interaction of a steroid hormone with a cell. 1 - hormone, 2 - receptor, 3 - cell, 4 - nucleus, 5 - hormone-receptor complex, 6 - cell membrane

Data on steroid hormones used to assess the functional state of athletes are presented in Table 5.

Physical activity affects the level of steroid hormones, which depends on the degree of fitness of the body and the power of the work performed. In untrained men, short-term exercise causes an increase in testosterone in the blood, and long-term exercise - its decrease. In well-trained athletes, testosterone concentration does not decrease even during prolonged physical work, for example, when running 21 km. The study of estrogen synthesis in men during physical exertion revealed its decrease in trained individuals and an increase in untrained individuals. In women, during hard work, an increase in the concentration of estrogen in the blood is noted.

Table 5

Steroid hormones used to assess functional

condition of athletes

	Concentration in 1 ml of blood is normal	Place of synthesis	Biological action
Aldosterone		Adrenal cortex	Regulates water-salt metabolism
Hydrocortisone		Adrenal cortex
Corticosterone		Adrenal cortex	Regulates glycogenesis and protein breakdown in skeletal muscle
Testosterone		Testes and adrenal cortex	Regulates spermatogenesis and has a general anabolic effect

Steroid hormones with anabolic effects, i.e. stimulating processes of biosynthesis are used as biological stimulants. For the first time, these compounds began to be used in medicine for the treatment of certain diseases and recovery in the postoperative period, to increase the rate of anabolic processes, in particular tissue repair.

In sports, anabolic steroids began to be widely used in the 50s. First, weightlifters and bodybuilders began to use them, and then - throwers and pushers. Regular use of anabolic steroids proved to be quite effective and led to a significant improvement in athletic performance.

All steroids have an androgenic effect, so anabolic steroids, when used regularly, have a depressing effect on the activity of the male gonads by a feedback mechanism (the more androgen is introduced into the body, the less it is synthesized in the body itself). Thus, the regular use of anabolic steroids entails a violation of the normal sexual life. Naturally, women are more sensitive to such drugs. It has been shown that the administration of testosterone to newborn female rats causes further male behavior and infertility in them.

Anabolic steroids affect the activity of a number of enzymes, increasing their synthesis and changing metabolism in general, which can lead to serious metabolic disorders. In addition, a number of steroid hormones cause significant suppression of immune responses. The literature has accumulated extensive data on the negative impact of anabolic steroids on the body of athletes.

The widespread use of anabolic steroids in big-time sports has led to the inclusion of these drugs in the doping list, since their use, on the one hand, is not compatible with the ethical principles of sports, and on the other hand, it has a clear negative effect on the body of athletes.

Steroid hormones, or simply steroids, are a group of biologically active substances that regulate many human life processes. Those who monitor their health and take care of the figure should get to know these valuable substances in more detail and be aware of what exactly each hormone is responsible for.

Types of steroids

Steroids include the following types of hormones:

1. Hormones of the adrenal cortex, that is, corticosteroids. They are divided into glucocorticoid hormones (cortisone, cortisol, corticosterone) and mineralocorticoid hormones (deoxycorticosterone, aldosterone).
2. Female sex hormones, that is, estrogens (estriol, estradiol, folliculin (estrol), ethinyl estradiol).
3. Male sex hormones, that is, androgens (androsterone, testosterone, methyltestosterone, androstenedione).

Influence of steroids

If we consider the influence of each of the listed active substances, we can say that:

• glucocorticoids are necessary for the body for the full metabolism of carbohydrates, proteins, fats, as well as the synthesis of nucleic acids. The task of these biologically active substances is to reduce weight by removing toxins from the body with urine;
• Mineralcorticoids are equally important for health. They regulate water-salt metabolism, as well as the exchange of sweat and salivary glands;
• estrogens, which are produced in the ovaries, are responsible for gestation and happy childbirth, and also regulate the woman's menstrual cycle. In addition, these active substances give the fair sex a feminine silhouette, proportionally distributing fat cells in the buttocks and thighs. The work of the sebaceous glands, timely skin hydration and even calcium metabolism also depend on the normal production of estrogen;
• Androgens are male hormones, although they are also produced in small amounts in women. During puberty, such hormones are responsible for the formation of the genital organs, as well as for axillary and pubic hair. By the way, in women, this type of steroid is produced all their lives, maintaining the normal functioning of the ovaries and uterus.

What threatens an overabundance and lack of steroids

High levels of estrogen can also be dangerous. In this case, the menstrual cycle may be disturbed in women, a seal in the mammary glands may appear, the weight may “jump” and the mood may change dramatically. On the contrary, a lack of estrogen often results in a violation of the water exchange process in the female body. In this case, the skin becomes dry and flaky, wrinkles, acne and cellulite appear. In addition, the lack of these active substances leads to vaginal dryness and urinary incontinence. From such a deficiency, bones suffer, which become weak and brittle.

But the female body is especially sensitive to disruption of androgen production. An excess of these steroids suppresses the production of female sex hormones, as a result of which a woman may develop male sexual characteristics, for example, a deepening of the voice, hairiness, and the cessation of menstruation. If there is a deficiency of androgens, libido decreases in the fairer sex, hot flashes are observed, ladies become over-emotional and may become depressed.

As you can see, steroid hormones are extremely important for women, which means that it does not hurt to periodically be examined and monitor the level of these substances in the body. Health and beauty to you!

Drugs such as steroid hormones, or as they are called in the common people, steroids, are elements that control the processes of vital activity in the human body. It is especially important for people who monitor their health to know the specifics of these drugs.

Where are they applied?

Steroids are a very important link in the body of any person. The more competently the chain of their work is built, the healthier the human body. Such a change in the body is due to their strong influence.

You can hear about steroid drugs in sports circles, most often they are used there. Anabolic steroids are especially popular in such power sports:

• powerlifting;
• Weightlifting;
• crossfit.

Such drugs help to achieve different goals, from gaining muscle mass to getting rid of excess weight.

Adrenal steroids

The modern market is oversaturated with drugs and sports nutrition, and it is sometimes difficult to understand this wealth. The list of steroids includes several groups.

Adrenal steroids are a type of steroid that is generated by the body in the adrenal glands. These organs perform irreplaceable work and produce the following:

• Hydrocortisone, or as it is more commonly called -. It is also called glucocorticoid. It plays one of the key roles in metabolism - metabolism and regulation of blood pressure. This hormone has many names, the most popular among them is "". Cortisol is produced in the body during stressful situations (experiences, excitement, fasting, lack of sleep). Due to the production of cortisol, muscle fibers disintegrate, immunity worsens. Therefore, this substance is considered negative because of its effect on the body, it is worth controlling its production.
• Corticosterone is a substance responsible for the degradation of proteins. It also promotes the processing of amino acids into complex carbohydrates, which serve as fuel for the body and give it energy. It also helps the liver produce glycogen, which is found in the muscles and is also used as an energy source.
• - This hormone is involved in the work of blood pressure. And also this steroid controls the value of potassium and sodium in the human body. It calls on the kidneys to absorb sodium and eliminate potassium from the urine if needed.

sex steroids

No less popular are the sexual substances:

• (androgen - male sex hormone) - the main androgen among the male genital organs is testosterone. Testosterone is produced by the male body in the testicles and performs important functions in the body. Testosterone is directly responsible for the sexual characteristics of a man, and such as hairline on the face, chest and other parts of the body, unlike women. This androgen makes the voice rough, gives it a baritone. And also testosterone is responsible for the development of muscles and sexual desire. All these functions are performed by the androgen.
• Estrogens (female sex hormones) - these substances are produced by women in the ovarian follicular apparatus. The estrogen class includes three types of hormones: estradiol, estriol and estrone. Estrogens contribute to the development of the uterus, fallopian tubes, vagina, pigmentation in the nipples and genitals. They increase the concentration of thyroxine, iron and copper in the blood. If there is a shortage of estrogen in the body of a woman, there is a possibility of developing osteoporosis.

Anabolic steroids are steroids that cause androgenic activity in the human body and are similar in their action to the male hormone testosterone.

Such drugs are densely found in power sports. Athletes use anabolic agents to improve their physical condition and athletic performance. This type of drug has an effect on muscle tissue and increases their volume due to enhanced metabolism and protein synthesis. Means of anabolic action can also be attributed to people suffering from dystrophy.

Known drugs

Proven drugs in sports circles are:

• Hydrocortisone;
• Dexamethasone;
• prednisone;
• Estriol;
• Prednisolone.

Before using these drugs, you should consult your doctor.

Side effects

Steroid hormones (especially androgen) can also have a negative effect on the body:

• suppression of the production of own testosterone;
• liver tissue damage;
• development ;
• acne (acne);
• increase in blood cholesterol levels;
• problems with the cardiovascular system;
• increased blood pressure;
• kidney problems;
• mental disorders;
• growth stop;
• prostate hypertrophy;
• infertility;
• thrombus formation.

The use of steroids requires the utmost attention and scrupulousness from a person. Steroid hormones comprehensively affect the human body. Do not use untested hormonal drugs without consulting a specialist.