I. What is Brassisterone®?
◎ Brassisterone® is the branded product of Brassaiopsis glomerulata extract.
◎ Brassisterone® helps balancing a favorable Testosterone:Estrogen ratio in a botanical modulator way.
◎ Brassisterone® helps promoting gains in lean mass.
◎ Brassisterone® supports improvements on exercise performance.
II. Story of Brassaiopsis glomerulata
Brassaiopsis glomerulata is a member of the Araliaceae that occurs in south and southeast Asia. B. glomerulata is a large shrub or small tree with thorns on the stems, palmate leaves with 5–7 leaflets.
This species has several reported traditional medicinal uses. In Vietnam, the plant is used to treat rheumatism and back pain. In India, a group of indigenous tribes called the Nagas drank a juice extract of Brassaiopsis glomerulata bark to aid in digestion and to alleviate constipation. The Nagas also used a paste of the bark of Brassaiopsis glomerulata to treat bone fractures and sprains. This species is also used medicinally in China as one of several kinds of “tongcao”, which means unblocking herbs used to promote urination and assist in lactation. Owing to its use as a “tongcao”, Brassaiopsis glomerulata was then tested using in vivo anti-inflammatory, antipyretic, and diuretic models.
The past history of medicinal use by human populations of Brassaiopsis glomerulata may be indicative of being safe when consumed. With the development of modern science, the strong aromatase inhibition of Brassaiopsis glomerulata extract was discovered by both enzyme- and cell-based assays, coupled with the possibility of a favorable safety profile, which both point to the potential for use of Brassaiopsis glomerulata for the hormone modulation.
III. Extract of Brassaiopsis glomerulata
Interested by the traditional use and novel discovery of Brassaiopsis glomerulata, several researchers investigate the components of it. Its compositions are mainly:
• Acankoreoside A
• 3α-hydroxy-lup-20(29)-en-23,28-dioic acid
• 3α,11α-dihydroxy-23-oxo-lup-20(29)-en-28-oic acid
• Stigmasterol, 6β-hydroxystimasta-4-en-3-one, 7β-hydroxy-4,22-stigmastadien-3-one
• N-benzoyl-L-phenylalaninyl-N-benzoyl-L-phenylalaninate, N-acetyl-L-phenylalaninyl-N-benzoyl-L-phenylalaninate,
and N-benzoyl-L-phenylalanine methyl ester
• Spinasterone and spinasterol
• Oleanolic acid
• Linoleic acid (fatty acid)
Because little was known about the components of Brassaiopsis glomerulata, American researchers subjected it to examination. They discovered that extracts of Brassaiopsis glomerulata leaves have an anti-oestrogenic effect. They isolated the ingredients in the extract and determined the anti-oestrogenic effect of each one. The researchers looked at whether the compounds could inhibit the aromatase that converting androstenedione into female hormones in test tubes trials, and whether they inhibited the conversion in live human cells. The researchers tested the plant ingredients at a concentration of 20ug/ml and meanwhile researchers compared their anti-oestrogenic effect with standard aromatase inhibitors: cytadren (AG) and letrozole (LET).
As the right figure show, the researchers isolated 13 compounds. Among them:
N-benzoyl-L-phenylalanine methyl ester
showed the most significant aromatase inhibition properties. (−)-dehydrololiolide was found to be as effective as Letrozole, which is approved by FDA as non-steroidal aromatase inhibitor.it showed activity in the cell-based AI assay.
IV. Aromatase Inhibition: a Favorable Property for Anabolism
As mentioned above, the attractive effect of Brassaiopsis glomerulata extract is due to its aromatase inhibition property. Aromatase is the enzyme responsible for catalyzing the last steps of biosynthesis of estrogens (estrone and estradiol) from androgens (androstenedione and testosterone). Inhibition of aromatase has been shown to reduce estrogen production throughout the body to nearly undetectable levels.
Bodybuilders that take anabolic ingredients often use aromatase inhibitors in order to minimize or avoid estrogenic effects. Aromatase inhibitors can prevent elevated levels of testosterone from being converted to excess estrogen and have also been shown to reverse age-related decline in testosterone.
V.Cell-based aromatase bioassay
Samples found to be active using the noncellular assay were further tested at various concentrations in SK-BR-3 human breast cancer cells that overexpress aromatase, using a previously described method (Balunas et al., 2006;Natarajan et al., 1994; Richards and Brueggemeier, 2003). Cells were treated in triplicate with samples or 0.1% DMSO (negative control) or 10 nM letrozole (positive control). Results are initially determined as picomoles of3H2O formed per hour incubation per million live cells (pmol/h/106 cells), with PCA calculated by comparison with the negative control, DMSO.
VI. Noncellular, enzyme-based aromatase bioassay
This assay was performed as described in earlier publications (Balunas et al., 2006; Kellis and Vickery, 1987;O’Reilly et al., 1995). Human placental microsomes were obtained from human term placentas that were processed at 4 °C immediately after delivery from The Ohio State University Medical Center [OSU Institutional Review Board (IRB) protocol number 2002H0105, last approved in December 2006]. Extracts and compounds were originally screened at 20 μg/mL in DMSO using a noncellular microsomal radiometric aromatase assay. Samples [extracts or compounds, DMSO as negative control, or 50 μM (±)-aminoglutethimide (AG) as positive control] were tested in triplicate. Each reaction mixture included sample, 100 nM [1β-3H]androst-4-ene-3,17-dione (400,000 – 450,000 dpm), 0.1 M potassium phosphate buffer (pH 7.0), 5% propylene glycol, and an NADPH regenerating system (containing 2.85 mM glucose-6-phosphate, 1.8 mM NADP+, and 1.5 units glucose-6-phosphate dehydrogenase). Microsomal aromatase (50 μg) was added to initiate the reactions, which were then incubated in a shaking water bath at 37 °C, and quenched after 15 min using 2 mL CHCl3. An aliquot of the aqueous layer was then added to 3a70B scintillation cocktail for quantitation of the formation of 3H2O. Percent control activity (PCA) was determined as previously described (Balunas et al., 2006; Kellis and Vickery, 1987; O’Reilly et al., 1995).
VII. Testosterone Boosting Supporter: Brassisterone®
If you’re taking testosterone boosting supplements or if you want to make the most out of your testosterone levels, using Brassisterone® will be a very good choice. The elevation on testosterone also can support you to promote lean mass and exercise performance. Also aromatase inhibition increases serum bioavailable and total testosterone levels to the youthful normal range in older men with mild hypogonadism.
There is currently insufficient evidence to support an oral dose of Brassaiopsis glomerulata. According to the recommended dosages of other similar products in the market, the oral dose of Brassisterone® per serving may be no more than 500mg.This ingredient have not been evaluated by the Food and Drug Administration.
Common side effects from aromatase inhibitors are decreased rate of bone maturation and growth, infertility, aggressive behavior, adrenal insufficiency, kidney failure, and liver dysfunction. Consumers with liver, kidney, adrenal, or prostate abnormalities are at higher risk for developing adverse events.