|Boldione Supplement Review
Boldione for Muscle Mass!
Boldione (1,4-androstadiene-3,17-dione) is the lead innovation to
arise out of the next generation of orally active prohormones. It
is a direct precursor to the anabolic steroid boldenone, and
displays a level of oral bioavailability far superior to any other
compound, including the new 1-androstenes.
If you are unfamiliar with boldenone, it is an anabolic steroid
most often found in injectable form as a veterinary medication
(boldenone undecylenate). It is chemically a derivative of
testosterone, characterized as a strong anabolic and low to
moderately androgenic agent.
As its name indicates, Boldione is simply the “dione”
form of boldenone, activated in the body by the same widely
distributed 17beta-hydroxysteroid dehydrogenase enzyme that
converts androstenedione to testosterone. The chemical structures
of both are:
Boldione (1,4-androstadiene-3,17-dione) Boldenone
Boldione is truly the most advanced and potent anabolic prohormone
ever developed, exhibiting several undeniable advantages over
The Most “Orally Active” Prohormone
Boldione is unquestionably the most orally active prohormone ever
developed. As you probably know, poor oral bioavailability is one
of the most fundamental problems with prohormones. The liver
processes natural steroid hormones so efficiently, that when taken
orally little will make its way all the way through to the blood
stream in active from. All but a small percentage of the steroid
will typically be found as an inactive 17-keto steroid.
Here the 17 beta-hydroxyl group, vital to androgen binding, is
removed and the compound rendered inactive. To solve this problem
with pharmaceutical agents, chemists have synthetically altered
most oral steroids with some form of 17-alpha alkylation (typically
a methyl or ethyl addition), which virtually inhibits
17-ketosteroid reduction by occupying a carbon bond necessary for
this reaction. But this type of alteration is also toxic to the
liver, synthetic, and clearly not possible to use with natural
The structure of Boldione however is intrinsically resistant to
17-ketosteroid deactivation during this first pass through the
liver. The combination of its delta 1 and delta 4 double bond
(1,4-Di Ene) shifts the hepatic metabolism (the 17-keto redox
potential) of this compound far in favor of activation. This is
made clear by studies showing Boldione to produce by far the most
profound excretion of active 17beta-hydroxysteroids we have seen of
any prohormone, as much as 50% of recovered urinary metabolites 
. Surprisingly the 17beta-hydroxyl group survives hepatic
metabolism to an enormous degree. Although this is not the near
100% recovery you would expect with a synthetic agent, it is
amazingly superior (by far) to every other prohormone ever
developed including the 1-androstene’s  .
…by far the most profound excretion of active
17beta-hydroxysteroids of any prohormone, as much as 50% of
recovered urinary metabolites…
Figure 1 compares the 17-beta hydroxysteroid recovery of
4-androstenedione, the new 1-androstenedione, and Boldione
(1,4-androstadienedione). As you can see, the delta 1 bond alone
increases active metabolite recovery considerably. However when we
add the additional delta 4 bond, the recovery is far more
Figure 1. Average percentage of 17beta-hydroxysteroid metabolites
recovered from human urine after 4-Androstenedione injection (J.
Biol Chem 239(1964) 1578-84), 100mg oral 1-androstenedione (J
Steroid Biochem 3 (1972) 933-6) and 100mg oral
1,4-androstadienedione (Steroids 18 (1971) 39-50).
Boldione converts to estrogen at roughly half the rate of
androstenedione and testosterone  . This significantly reduces
the level of estrogen buildup during use compared to that achieved
with testosterone precursors, and similarly also lowers the chance
of noticing strong estrogen related side effects such as increased
body fat, gynecomastia and definition hiding water retention.
It is no coincidence that the best bulking agents are estrogenic
though, as this hormone does offer more than just side effects.
Aside from the basic size increase we would attribute to fluid
retention, estrogen also aids the muscle building process by
enhancing glucose utilization for tissue growth and repair  
, increasing growth hormone secretion  and perhaps even by
increasing androgen receptor concentrations  .
It is clear today that estrogen serves a positive function in
muscle growth, finally allowing us to explain a well known
anecdotal fact: Aromatizable steroids are always the strongest
muscle-builders, and preferred over non-aromatizable steroids when
mass is desired. Boldione coverts to estrogen at a high enough rate
to support excellent muscle gains, yet is typically mild enough to
promote quality, defined growth without unwanted side effects. The
long and fond relationship bodybuilders have had with boldenone is
a clear testament to this fact.
… estrogen also aids the muscle building process by
enhancing glucose utilization for tissue growth and repair,
increasing growth hormone secretion and perhaps even by increasing
androgen receptor concentrations…
Reduced Androgenic Activity
Boldenone is classified as an anabolic steroid, exhibiting much
less androgenic activity than its analogue testosterone. This is
because unlike testosterone, boldenone is a poor substrate for the
5-alpha reductase enzyme  . This is the enzyme responsible for
converting testosterone to the more potent steroid
dihydrotestosterone in many androgen responsive tissues such as the
skin, scalp, prostate and central nervous system. Consequently the
local potency of testosterone is increased significantly in these
tissues, often allowing it to trigger unwanted side effects such as
oily skin, acne, body/facial hair growth and male pattern hair loss
(for those with a genetic predisposition).
But boldenone tends to interact with the 5-beta reductase enzyme
instead, which reduces this steroid into a very weak binder of the
androgen receptor instead of potentiating its activity.
Consequently boldenone is much milder in terms of androgenic side
effects compared to testosterone, being much more similar to
nandrolone in this regard.
A Naturally Occurring Hormone
In order for any prohormone to be classified as a nutritional
supplement, the compound in question must be “naturally
occurring”. This means that we must isolate a clear source
for it in nature, without human synthesis. Thankfully
1,4-androstadienedione was shown unquestionably to be a natural
androgen in cows. The first study to isolate this compound was
conducted back in 1956, where scientists believed that it was most
likely produced from progesterone in the animal’s
gastrointestinal tract  .
Later studies show the production of this hormone in cow ovarian
tissues however  , suggesting another location and method of
endogenous production. We can also look toward studies in the
agricultural industry, where the natural occurrence of 1,4-dienones
 have caused some difficulty and debate over the screening
processes used for detecting the illegal use of boldenone in
cattle. Many have suggested threshold limits to prevent false
positives due to the low level of 1,4-diene androgens that may be
present naturally in these animals.
100mg 1,4-androstadiene-3,17-dione per capsule, 60 capsules per
 Metabolism of 1-dehydroandrostanes in man. I. Metabolism of
17-beta-cyclopent-1-enyloxyandrosta-1,4-dien-3-one (quinbolone) and
androsta-1,4-dien-3-one (1). Galletti F and Gardi R. Steroids 18
 Metabolism of 1-dehydroandrostanes in man. III.
Metabolism of 17-beta-hydroxy-5a-androst-1-en-3-one,
(mesabolone) and 5a-androst-1-en-3,17-dione. Galletti F and Gardi
R. J Steroid Biochem 3 (1972) 933-6.  Biosynthesis of
Estrogens, Gual C, Morato T, Hayano M, Gut M and Dorfman R.
Endocrinology 71 (1962) 920-25
 Aromatization of androgens to estrogens mediates
increased activity of glucose 6-phosphate dehydrogenase in rat
levator ani muscle. Endocrinol 106(2):440-43 1980
 The pentose phosphate pathway in regenerating
skeletal muscle. Biochem J 170: 17 1978
 Activation of the somatotropic axis by testosterone in adult
males: Evidence for the role of aromatization. Weissberger and Ho.
J Clin Endocrinol Metab 76 (1993) 1407-12.
 Modulation of the cytosolic androgen receptor in striated
muscle by sex steroids. Rance, Max. Endocrinol 115 (1984) 862-6
 Metabolism of Beldenone in Man: gas Chromatographic/Mass
Spectrometric Identification of Urinary Excreted Metabolites and
Determination of Excretion Rates. Schanzer, Donike. Bol Mass Spec.
21 (1992) 3-16
 Identification of C19 Steroids in Bovine Feces. Miller, W.R.,
C.W. Turner, D.K. Fukushima and I.I. Salamon: J. Biol. Chem. 1956
 The in-vitro metabolism of progesterone-c14 to
Delta-1,4-Androstadiene-3,17-dione by a cystic bovine ovary.
Gawienowski A. M., Lee S.L. and Marion G.B.: Endocrinology 69
 C. J. M. Arts, R. Schilt, M. Schreurs and L.a. Van Ginkel, in
Proceedings of the Euroresidue III Conference, Veldenhoven, 6-8 May
1996 ed. N. Haagsma and A. Ruiter, University of Utrecht, Utrecht,
The Netherlands, 1996, p. 212
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