Boldine –The New Yohimbine - PES Alphamine Advanced
Boldine – The New Yohimbine
Boldine is a novel alpha-2 adrenergic receptor antagonist that, unlike its widely marketed counterparts (e.g. Yohimbine), does not possess attributes that predispose users to anxiety or cardiovascular side effects1,2,3.
The alpha-2-adrenergic receptor is found throughout the body and functions chiefly to limit the amount of norepinephrine that is released at the site of the receptor. In fat cells, norepinephrine is a powerful signaling molecule that, along with epinephrine, initiates a cascade of reactions that result in fat loss. Therefore, when the alpha-2 receptor is functional, norepinephrine release is reduced and fat loss gets halted. This has been shown in receptor studies, wherein it was found that there is an excess of over 50% of alpha-2 adrenergic receptors in fat cells4, meaning that the human body was genetically designed to preserve energy, and thus, it refuses to let go of this “stubborn fat” by creating more alpha 2 receptor than are necessary for normal function. Indeed, regional obesity, otherwise known as the “stubborn fat” that just doesn’t go despite how hard you try, may be due to local variations in alpha-2 receptor density4.
The authors of the study offered a solution: a prolonged fasting period decreased the number of alpha-2 adrenergic receptors on the fat cells4. But for most of us, prolonged fasts are neither plausible nor optimal for our goals. The solution is boldine, a natural alkaloid which deactivates/antagonizes the alpha-2 receptor, allowing fat loss to proceed undisturbed. This may again be of particular importance when attempting to lose fat in stubborn areas like the midsection, love handles, and thighs.
Unlike the well-known alpha-2 antagonist Yohimbine, Boldine does not possess the profound anti-serotonergic activity that gives yohimbine users anxiety1,2,3, and furthermore, rather than vasoconstricting and increasing blood pressure, Boldine actually vasodilates and reduces blood pressure5. In fact, boldine has been shown to possess an array of health benefits in the murine model, including protection against hypertension6, reduced LDL oxidation7, and other antioxidant/general health properties7,8. This makes boldine the ideal candidate for both safe and effective fat loss.
Also unlike yohimbine, boldine possesses fat loss benefits that are independent of its alpha-2 antagonistic effects. Boldine has the unique ability to induce adiponectin release from fat cells9. As a brief background, adiponectin is released from fat cells that are “empty” due to lipolysis of their stored triglycerides. In very lean people, adiponectin levels are high due to the empty fat cells, while in obese people, adiponectin levels are low. This presents a problem to people with high bodyfat levels, because adiponectin is a hormone that burns fat and prevents the proliferation of fat cells, and since they have low levels already, they’re at an extremely large disadvantage for weight loss. Interestingly, boldine manages to “trick” fat cells into thinking they are empty, resulting in far increased adiponectin release9. This will be beneficial for anyone, because everyone possesses some degree of bodyfat (and hence, adiponectin suppression), and boldine may help optimize adiponectin levels to keep fat loss moving forward.
Finally, boldine is a potent inducer of calcium release from the sarcoplasmic reticulum of skeletal muscle10. You don’t have to know what this means, but you should be aware that calcium release is the key dictator of muscular strength output. By increasing calcium release in a manner very similar to another compound named Amentoflavone. Boldine possesses the ability to enhance strength output, making it of further benefit to your fitness junkie.
With combined alpha-2 antagonism (“stubborn fat” loss), adiponectin release enhancement (enhanced fat burning and suppression of fat gain), and increased calcium release from the SR (improved strength output), Boldine is the ultimate cutting agent for anyone, be it the lean individual looking to lose those last few stubborn pounds, the overweight individual looking to overcome the disadvantage that fat gain has put them at, or your average fitness junkie/gym rat who wants to lose fat while gaining strength and muscle.
Without the side effects that held its predecessors back, Boldine will finally enable you to enjoy round-the-clock fat fighting.
1. De Las Heras, B., et al. "A Study of the Adrenergic Activity of the Alkaloids Boldine and Glaucine." Pharmazie 45.6 (1990): 443-44. Web.
2. Eltze, M., et al. "Affinity Profile at Alpha(1)- and Alpha(2)-adrenoceptor Subtypes and in Vitro Cardiovascular Actions of (+)-boldine." Eur J Pharmacol 443.1-3 (2002): 151-68. Web.
3. Chulia, S., et al. "The Effect of S-(+)-boldine on the Alpha 1-adrenoceptor of the Guinea-pig Aorta." Br J Pharmacol 119.7 (1996): 1305-312. Web.
4. Arner, P. "Adrenergic Receptor Function in Fat Cells." Am J Clin Nutr. 55.1 (1992): 228S-36S. Web.
5. Chen, Keh-Shaw, Feng-Nien Ko, Che-Ming Teng, and Yang-Chang Wu. "Antiplatelet and Vasorelaxing Actions of Some Aporphinoids." Planta Medica 62.02 (1996): 133-36. Web.
6. Lau, Y.-S., A. Machha, F. I. Achike, D. Murugan, and M. R. Mustafa. "The Aporphine Alkaloid Boldine Improves Endothelial Function in Spontaneously Hypertensive Rats." Experimental Biology and Medicine237.1 (2012): 93-98. Print.
7. Santanam, N., M. Penumetcha, H. Speisky, and S. Parthasarathy. "A Novel Alkaloid Antioxidant, Boldine and Synthetic Antioxidant, Reduced Form of RU486, Inhibit the Oxidation of LDL In-vitro and Atherosclerosis in Vivo in LDLR−/− Mice." Atherosclerosis 173.2 (2004): 203-10. Web.
8. O’Brien, Peter, Catalina Carrasco-Pozo, and Hernán Speisky. "Boldine and Its Antioxidant or Health-promoting Properties." Chemico-Biological Interactions 159.1 (2006): 1-17. Print.
9. Yu, Bangning, Carla Cook, and Nalini Santanam. "The Aporphine Alkaloid Boldine Induces Adiponectin Expression and Regulation in 3T3-L1 Cells."Journal of Medicinal Food 12.5 (2009): 1074-083. Web.
10. Kang, Jaw-Jou, and Yu-Wen Cheng. "Effects of Boldine on Mouse Diaphragm and Sarcoplasmic Reticulum Vesicles Isolated from Skeletal Muscle."Planta Medica 64.01 (1998): 18-21. Web.