Introduction of Boldenone

General description

Boldenone is a DEA Schedule III controlled substance. Substances in the DEA Schedule III have a potential for abuse less than substances in Schedules I or II and abuse may lead to moderate or low physical dependence or high psychological dependence. Boldenone is an 3-oxo-Delta(1),Delta(4)-steroid substituted by an oxo group at position 3 and a beta-hydroxy group at position 17. It is an anabolic androgenic steroid that has been developed for veterinary use. It is a 17beta-hydroxy steroid, an anabolic androgenic steroid and a 3-oxo-Delta(1),Delta(4)-steroid. Boldenone. is also known to be endogenous in the entire male horse and potentially formed by microbes in voided urine, the gastrointestinal tract, or feed resulting in its detection in urine samples.^[1]

It is an important protein assimilating androgen steroid, which can steadily and continuously increase muscle and strength. Now it is mainly synthesized by 1,4-androstenedione (ADD) through chemical method. Compared with the boldenone chemical synthesis, biotransformation has the advantages of mild transformation conditions, less environmental pollution and less by-products. However, 17β-hydroxysteroid dehydrogenase (17β-HSD) for the synthesis of boldenone, is rarely identified or the identified 17β-HSDs do not have the activity of catalyzing 17β-reduction reaction, resulting in the low utilization rate of the enzyme, so it is necessary to screen 17β-hydroxysteroid dehydrogenase with higher activity.

Application

It is a kind of drugs with the mother nucleus structure of steroids, which can be used to treat skin diseases, endocrine diseases, improve protein metabolism and surgical anesthesia. At present, steroids (steroid hormones) are the main steroids produced. Steroid hormones are fat soluble hormones. Steroid hormone drugs can combine with the receptors of target cells to form complexes, which has very important clinical application value. Steroids have important medicinal value and play an important role in anti-tumor, anti-inflammatory, anti allergy, immune regulation and reproductive development. They are the most important drugs other than antibiotics. According to the different functions of steroid hormones, they can be divided into cortical hormones, sex hormones and protein assimilation hormones.^[2]

1.Boldenone is an anabolic steroid developed for veterinary use, mostly for treatment of horses. It is not indicated for use in humans in the US and is only available through veterinary clinics.Baodanone is an injectable animal steroid with strong anabolism and medium androgen characteristics. Baodanone greatly prolongs the activity of the drug (UNDECYLENOATE is one carbon atom longer than decanoate), so it only needs to be injected once every 3 or 4 weeks. Athletes like the balanced anabolic and androgenic properties of this drug very much. Athletes usually think it is a drug with stronger and slightly higher androgen than deca durabolin. It is also generally cheaper and can replace deca in most cycles without greatly changing the end result. Baodanone is also generally considered to be a drug that can increase erythropoiesis, although it is characteristic of almost all anabolic / androgenic steroids

2.Baodanone is a derivative of testosterone, which will be converted into estrogen and make the body store water. No hepatotoxicity. However, it can increase appetite, have strong protein synthesis ability, improve pump feeling and vascular clarity during training, improve muscle quality and enhance muscle endurance. Suitable for beginners, and also suitable for muscle increasing stage or fat reducing stage

Synthesis

Utilization 17 β- The synthesis of baodanone from 1,4-androstenedione catalyzed by hydroxysteroid dehydrogenase requires a large amount of coenzyme, and the coenzyme price is high and the stability is not good. If coenzyme is added directly to the reaction system, it will cause additional consumption and increase the production cost. Therefore, in production and application, in order to save cost and facilitate operation, the corresponding coenzyme regeneration system is often introduced into the constructed catalytic system to convert the oxidizing (reducing) coenzyme into reducing (oxidizing) coenzyme [55]. Coenzyme circulation can stabilize the level of coenzyme in the catalytic system, and there will be a certain level of coenzyme in living cells due to the normal metabolism of cells. Therefore, only the substrate required for coenzyme transformation needs to be added to achieve coenzyme self-sufficiency, and there is no need to add coenzyme manually.

In organisms, enzyme catalyzed reduction reactions often require the participation of coenzyme NAD (P) H. with the continuous development of biological preparation of drugs or other compounds, there is an increasing demand for oxidoreductases that need NAD (P) h as reducing agent. About 90% of the known oxidoreductases require coenzyme NAD (P) h or NAD (P) + participation [57]. At present, the discovered methods from oxidized coenzyme NAD (P) + to reduced coenzyme NAD (P) H mainly include enzyme catalysis, chemical method, homogeneous catalysis, electrochemistry, photocatalysis, heterogeneous catalysis, etc. [58]. Among them, enzyme catalysis avoids the problem of difficult separation of by-products and high efficiency of regeneration of NAD (P) h because it does not need to add compounds to provide protonic donors, It is a more widely used coenzyme regeneration method.

History

It is reported that Ciba called it anabolic steroids in 1949. In the 1950s and 1960s, the company developed experimental esters of several drugs, and then issued baodanone as a long-acting agent. It is sold under the brand name parenabol and is known as an parenteral (injectable) anabolic agent because of its characteristics. Parenabol had some clinical applications in the late 1960s and early 1970s, mainly as an anabolic agent for preserving thin tissue under weight loss and preserving bone mass for osteoporosis. Baodanone existed briefly in the human medical market. However, it was discontinued worldwide before the late 1970s. Squibb is famous for launching this drug in the veterinary market and will be sold under the now most famous trade name baodanone.^[3]

Figure Coupled reaction of hydroxylation and NADPH regeneration

Toxicity

1.Anabolic / androgen steroids can have harmful effects on serum cholesterol. This includes the tendency to lower HDL (good) cholesterol and increase LDL (bad) cholesterol, which may convert HDL into LDL balance, resulting in a greater risk of arteriosclerosis. The relative effect of anabolic / androgenic steroids on serum lipids depends on dose, route of Administration (oral and injection), type of steroids (aromatic or non aromatic), and level of resistance to liver metabolism. Anabolic / androgen steroids may also adversely affect blood pressure and triglycerides, reduce endothelial relaxation, and lead to left ventricular hypertrophy, which may increase the risk of cardiovascular disease and myocardial infarction. Compared with oral anabolic steroids, boldenone has little effect on cardiovascular risk factors. This may be partly due to its openness to liver metabolism, which makes it have little effect on liver cholesterol metabolism. The aromatization of estradiol by cholesterol also helps to reduce the negative effect of androgen on serum lipids. To help reduce cardiovascular stress, it is recommended to maintain an active cardiovascular exercise program and always minimize the intake of saturated fat, cholesterol and simple carbohydrates during AAS use. It is also recommended to supplement fish oil (4 g per day) and natural cholesterol antioxidant formulas such as lipid stabil or products with similar ingredients.

2.Use (women): when used for physical or performance enhancement purposes, women take a lower dose than men, usually 50-75 mg per week. Women should use this slow acting preparation carefully, otherwise they will have the symptoms that blood levels are difficult to control and slow decline.^[4]

Storage

1.Keep in dark place,Sealed in dry,Store in freezer.

2.Boldenone was storage into the Ampoule bottle (Latin: ampula) that a kind of glass container, can be fused and sealed. It is generally used to store serum, vaccine, injection medicine, etc. The biggest feature of this kind of container is its sealing property, which stores the essence liquid, which can guarantee the stable storage of various active ingredients in the essence.

Reference

1.Viljanto M., Kicman A. T. & Walker C. J. et al., "Bioformation of boldenone and related precursors/metabolites in equine feces and urine, with relevance to doping control," Drug Testing and Analysis, Vol.12, No.2(2020), pp.215-229.
2.Gomez C., Pozo O. J. & Geyer H. et al., "New potential markers for the detection of boldenone misuse," J Steroid Biochem Mol Biol, Vol.132, No.3-5(2012), pp.239-246.
3.Wu Yuling: 17 β— Functional identification of hydroxysteroid dehydrogenase and its application in the synthesis of baodanone: Jiangnan University, 2020.
4."Reactions 1491, p6 - 8 Mar 2014,".