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Bodybuilding's Best Muscle-Building Supplements
Being a bodybuilder or strength athlete today puts you at an extreme advantage over those who were on an equal quest for size in days gone by. Instead of relying on crude protein concoctions and severe overeating to gain mass, like they did in the old days, we now have a remarkable array of mass building compounds to choose from. As good as this is, however, it also creates more possibilities to go in the wrong direction. We need to be smart about our choices, not fall for the hype, and look for science-based ingredients from reputable companies to be sure you are getting only the best. Some compounds are pure garbage, some show potential but are unproven, some are fairly effective, and a handful are enormously effective mass-building powerhouses. This article separates the meat from the potatoes, by highlighting in great detail what most experts consider to be the top 5 science-based muscle-building compounds our industry has to offer. They appear in no particular order, but starting out with the most potent protein source out there seems like a good start.

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The number one supplement to have in your arsenal is high quality whey protein. You may be saying, "wow tell me something I don't know", however, you would not believe the number of bodybuilding newbies who would rather buy some new and expensive "miracle formula," when whey protein has been proven time and time again as a no-fail anabolic support agent. The importance of high quality protein in bodybuilding cannot be overstated.  As we know, whey protein is available in a number of different forms (e.g., whey concentrate, isolate, hydrolysate, etc.). There's no sense going into each of these because my main focus is the extremely anabolic benefits of Whey Protein Hydrolysate (WPH). Whey protein hydrolysate is commonly processed from another very potent protein, whey protein isolate (WPI), whereby enzymatic degradation (hydrolysis) of the WPI is carried out to "pre-digest" the protein so that it contains peptide fractions (short chains of amino acids). The result is a product that contains a large number of low molecular weight (MW) peptide fractions. High-quality products have been well hydrolyzed and have an average MW of around 500 Daltons. It should be noted that these di- and tri-peptides make for very rapid absorption and have scientifically proven to shunt more water into muscle cells (cell volumizing effect), speed recovery, support anabolism, and support immune function. Users of high quality hydrolyzed whey protein report almost immediate muscle hardness, a result of the powerful cell volumizing effect that is unique to this form of protein. The di- and tri-peptides in WPH makes it more readily absorbed than free-form amino acids and non-hydrolyzed proteins. Whey is an ideal starter protein for hydrolysis because it is a concentrated source of essential amino acids. This results in a superior profile of di- and tri-peptides, producing the greatest hyperaminoacidaemia, which means a rapid increase in branched-chain amino acids into the blood, scientifically proven to augment protein synthesis and recovery. The remarkably greater rate of absorption of di- and tri-peptides compared to amino acid cocktails is a unique result of the body being a better transporter of small peptides than an amino acid carrier system, thus minimizing competition between substrates. It is well established that the ingestion of hydrolyzed whey protein immediately after exercise results in the highest levels of blood amino acids, which are associated with augmented nitrogen utilization and elevated anabolic state. Additionally, when whey protein hydrolysate is ingested along with high-glycemic (i.e., fast) carbohydrates, the result is a synergistic increase in the rate of insulin release, again augmenting the anabolic cascade. A recent study investigated whether the hormonal response to feeding with protein solutions is influenced by the nature and degree of protein fractionation, and examined insulin and glucagon responses after intake of protein solutions containing the same amount of nitrogen in human subjects. They observed that peptide hydrolysates elicited a peak insulin response that was two and four times greater than that evoked by milk protein and glucose solutions respectively. Furthermore, the insulin response correlated to how fast the amino acids entered the blood, especially leucine, isoleucine, valine, phenylalanine and arginine. Thus, whey protein hydrolysate-based supplements with high amounts of these amino acids are superior anabolic activators. It should be stressed that timing is key when using WPH supplements. Being the fastest absorbed protein product available, whey protein hydrolysate ingestion results in the most abundant increase in circulating amino acids over a two-hour window compared to "intact proteins". Thus, drink 25-30 grams of high-quality WPH as soon as you finish your workout, this will enable you to immediately take advantage of the post-exercise anabolic environment and truly maximize muscle growth.

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 The essential amino acids leucine, isoleucine and valine share a unique branched chain structure, and thus, are transported and metabolized by common means. One of the key properties of BCAAs is their catabolism by skeletal muscle after bouts of heavy exercise. Based on this fact alone, it becomes apparent why BCAA supplementation is beneficial to bodybuilders. In skeletal muscle, leucine is key in turning protein synthesis into overdrive through a number of different mechanisms. First, leucine is scientifically proven to increase highly anabolic insulin secretion. At the molecular level, recovery from resistance and endurance exercise primarily relies on supplemental dietary leucine in order to increase the (much needed) intracellular leucine concentration, which activates mTOR and the initiation factors eIF4E and eIF4G. Protein synthesis is dependent on the activation of these molecular factors. Applied research supports supplementation of BCAA's. For example, during prolonged aerobic exercise, leucine is at the mercy of oxidation and there is solid evidence that leucine supplementation promotes anabolism in skeletal muscle long after exercise is completed. In a recent placebo controlled study it was found that six weeks of dietary leucine supplementation significantly improved endurance performance and upper body power in athletes. Recently, there have been numerous reported benefits to BCAA supplementation in bodybuilders. For example, the effect of BCAA supplementation on muscle soreness and fatigue has been recently investigated, whereby, squatting exercise (7 sets of 20 reps) was used to induce delayed onset muscle soreness (DOMS) in males and females. On training day, the subjects ingested either a BCAA cocktail or a placebo approximately 15 min prior to exercise. The authors reported that 5 grams of BCAAs (Ile:Leu:Val = 1:2.3:1.2) significantly reduced the duration and severity of DOMS and fatigue in both males and females for days after exercise. Molecular level support comes from a recent study that illustrated BCAAs ability to activate the anabolic signaling pathways via mTOR and p70 S6 kinase in human muscle in the recovery period after exercise. So it is obvious that BCAAs are not only food for muscles, but also important "switches" for turning on anabolism. In a supporting applied study, investigators observed increases in physical performance in strength athletes due to decreases in muscle damage during training and increases in skeletal muscle protein synthesis. Thus, BCAAs appear to be integral in the modulation of peripheral fatigue. Some very intriguing research has recently illustrated a role for BCAAs in the regulation of central fatigue. Of particular interest, a significant decrease in the rating of perceived exertion (RPE) with leucine supplementation has been reported in strength and endurance athletes. Supporting evidence comes from a recent report that showed increases in the release of 5-hydroxytryptamine (5-HT), which plays a role in fatigue (5-HT affects mood, arousal, and sleepiness). During exercise BCAAs are metabolized (as discussed above) and plasma levels decrease. As exercise progresses, plasma free fatty acids become elevated which promotes increases in free tryptophan (they both competitively bind to plasma albumin). This throws off the free tryptophan to BCAA ratio and enables enhanced tryptophan uptake into the brain. 5-HT synthesis is very sensitive to changes in plasma tryptophan levels and the transport of tryptophan across the blood-brain barrier. It has been hypothesized that ingestion of BCAAs balance the increased levels of tryptophan, thus, decrease the transport across the blood-brain barrier, and subsequently decrease 5-HT synthesis leading to delayed fatigue. This general hypothesis is supported by a study where BCAA supplementation was given during 60 min of heavy cycling exercise. The plasma concentration ratio of free tryptophan to BCAAs increased by 45% during exercise and by 150% 5 min after exercise in the placebo trial but remained unchanged or even decreased when BCAAs were ingested. Subjects reported 7% lower ratings of perceived exertion and 15% lower ratings of mental fatigue at a given work rate, compared to placebo. From these data it should be clear that BCAA supplementation is well supported as a true muscle-builder with major benefits during and post-exercise.

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You may think that the benefits of creatine supplementation were formed from a 20th century postulate. Amazingly, it has been a known and studied compound as far back as the 1830's. By the early 1900's, scientists began extracting creatine from meat and investigating its potential as a performance enhancing aid. The Soviets were investigating creatine's potential as early as the 1970s, but the real scientific explosion occurred in the 1990's, when creatine monohydrate was introduced to the commercial markets in the US and Great Britain. Creatine is a non-essential substance that is produced by the body and taken in from dietary meat sources. It is synthesized from arginine, methionine, and glycine in two-steps and our predominant creatine pool is in skeletal muscle, where about 40% is free creatine and where phosphocreatine makes up the other fraction. The average 150 lb person has a pool of about 120-140g of creatine on board and loses about 2g of creatine through urination per day. There are reams of well-documented science to back up creatine's muscle building potential, which comes as no surprise because it has been one of the few true powerhouse mass builders used for years now. Here is a more scientific perspective of its actions. First, creatine monohydrate ingestion increases phosphocreatine stores in skeletal muscle, which provides support to rapidly phosphorylate ADP to ATP under repeated powerful and short (<10 sec) duration contractions. This results in better performance with shorter rest periods, an effect that is of primary benefit to bodybuilders and power athletes. Second, creatine monohydrate supplementation leads to increased phosphocreatine stores. The phosphorylation of ADP requires phosphocreatine and stimulates phosphofructokinase (rate limiting enzyme for glycolysis); this increases the rate of glycolysis and more ATP (i.e., energy) is produced. This effect is beneficial for athletic performances that last from 10 seconds to over 2 minutes. Creatine augments the ability for high-energy phosphate to diffuse between mitochondria and myosin heads, thus enhancing cross-bridge cycling and tension production. Creatine supplementation is associated with skeletal muscle hypertrophy and increased protein synthesis, based on its ability to create an osmotic gradient, whereby water is shunted into muscle cells (which is a signal for anabolism).  At this point, you should be convinced that if you are not currently using creatine monohydrtate, then you should start. Creatine comes in many forms, but the tested and true "gold standard" is high-quality premium grade micronized creatine monohydrate. Based on current data, the best way to supplement creatine monohydrate is by including a one-week loading phase at approximately 0.3g/kg (body weight) per day followed by maintenance at approximately 0.1g/kg (body weight) per day. During the loading phase, split the daily dose into approximately 5g servings to be ingested throughout the day, making certain that one dose is ingested 30 minutes before your workout and another 4-6 hours after post-workout. During the maintenance phase, ingest one serving prior to- and post-workout. As with all supplements make sure you use a high quality creatine monohydrate product (preferably German premium grade.) If you want to completely exploit the benefits of creatine supplementation, then look for products that contain maltodextrin, and arginine AKG to increase creatine transport into muscle cells.

Standardized Bulgarian
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Since the prohormone ban, supplement scientists have worked day and night to find compounds that naturally augment testosterone production. Natural testosterone boosters have been around for centuries, but their primary use was to increase libido and virility. One of the most effective herbal formulations comes from extracts of Bulgarian Tribulus terrestris (not to be confused with the crude non-standardized forms of this herb). The steroidal saponins derived from Tribulus terrestris L. (Zygophyllaceae) are considered to be the factor responsible for the biological activity of most value to bodybuilders. This activity depends on the concentration and the composition of active saponins. For our purposes, building mass etc, the most important saponin is called protodioscin. Protodioscin, which is classified as a furostanol saponin, is the active ingredient extracted from Tribulus terrestris that is responsible for its testosterone boosting potential. Research has shown that administration of Tribulus terrestris to humans and animals improves libido and spermatogenesis. More importantly, protodioscin has been shown to augment the levels of testosterone, leutinizing hormone, dehydroepiandrosterone, dihydrotestosterone and dehydroepiandrosterone sulphate. Although research has been somewhat conflicting in the area of Tribulus and its hormone boosting potential, the main issue seems to be a discrepancy in the potencies of Tribulus across studies, and not its androgen boosting capability.
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 In other words, the studies that have shown the most impressive anabolic potential were the ones that used legitimate bio-active tribulus with high concentrations of protodioscin. The importance of the standardization of the tribulus simply can not be understated. A tribulus formula with less than 15% protodioscin and 40% total steroidal saponins, just does not have enough bioactive potency to deliver meaningful results. Recent studies really seem to underscore this fact. Recently, a double-blind trial was conducted on ProSource's own AndroTest which is generally considered the most potent tribulus product on the market and the results were nothing short of remarkable. In this study, subjects using AndroTest experienced increases in total testosterone as high as 275% and increases in free testosterone as high as 218% over baseline. This means that some subjects experienced nearly a three fold increase in testosterone levels. To put this in perspective, increases of this magnitude exceed what is seen using straight premium testosterone at therapeutic dosages. Equally impressive is the fact that the increased testosterone levels after two weeks use were maintained at the subsequent measurement points of the study. This is especially important because it is sustained increases in testosterone that can lead to increased muscle gains. Much like virtually all herbal supplements, the key to the effectiveness of tribulus clearly lies within the geographical region it's grown in and the standardization level it is processed to. Unfortunately the vast majority of tribulus products on the market are not standardized, are grown in the wrong regions, and yield negligible active steroidal saponins and thus have little to no effect. The cost of using highly standardized Bulgarian tribulus for manufacturers can be up to 10 times the cost of using the cheaper crude forms of the herb. However, the difference in the end result is truly night and day. A true highly active Bulgarian tribulus such as that used in AndroTest represents one of the most effective natural compounds available today for increasing test levels.

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Beta-alanine is a non-proteinogenic amino acid, meaning that it is "non-protein-building". In meat eaters its presence is speculated to occur from the hydrolysis of di-peptides in the diet. It is also synthesized in the liver as the final metabolite of uracil and thymine degradation. Beta-alanine is one precursor (the other is histidine) to carnosine synthesis, and is said to be rate limiting. Thus, it has garnered much research interest based on its potential to elevate skeletal muscle carnosine levels. Elevating carnosine has been hypothesized as beneficial to performance based on: 1) animals who have a great capacity for prolonged high intensity exercise have high intramuscular carnosine levels; and 2) carnosine levels are relatively higher in fast-twitch versus slow twitch muscle fibers. These two factors bolster the role of carnosine in maintaining normal pH. In fact, the di-peptide carnosine has been unequivocally shown to buffer skeletal muscle pH. Additional support for the importance of carnosine in fast twitch fibers comes from data showing that the carnosine content in vastus lateralis is elevated in resistance-trained bodybuilders. Dietary supplementation with beta-alanine for 2-4 weeks has been shown to increase vastus lateralis carnosine concentration by more than 60%. In a recent performance based study, male subjects underwent periodic cycling capacity (max) tests with either beta-alanine supplementation or a placebo. It was found that muscle carnosine increased 58.8% after 4 weeks and 80.1% after 10 weeks of supplementation. No increase was observed in the control group. Total work completed was 13% greater with 4 weeks beta-alanine ingestion and 16% greater after 10 weeks supplementation. There was no change in total work completed in the control group. The increase in total work done correlated with the increase in vastus lateralis carnosine levels. More support comes from a study illustrating that 4 weeks of beta-alanine supplementation improves power output at lactate threshold. Recent evidence clearly shows that combining creatine and beta-alanine results in significant increases in strength and lean body mass and decreases in body fat percentage.

We hope that this brief update on the current muscle-building supplements aids you in your choices. You should note that we have chosen supplements that stack very well together and provide synergistic benefits when taken simultaneously throughout the day. If you follow the very simple guidelines given herein you will definitely maximize your anabolic potential and get closer to your ultimate goal.

Scientific References

Bemben MG & Lamont HS (2005). Creatine supplementation and exercise performance: recent findings. Sports Med 35, 107-125.
Blomstrand E (2006). A role for branched-chain amino acids in reducing central fatigue. J Nutr 136, 544S-547S.
Blomstrand E, Eliasson J, Karlsson HK, & Kohnke R (2006). Branched-chain amino acids activate key enzymes in protein synthesis after physical exercise. J Nutr 136, 269S-273S.
Blomstrand E, Hassmen P, Ek S, Ekblom B, & Newsholme EA (1997). Influence of ingesting a solution of branched-chain amino acids on perceived exertion during exercise. Acta Physiol Scand 159, 41-49.
Borsheim E, Tipton KD, Wolf SE, & Wolfe RR (2002). Essential amino acids and muscle protein recovery from resistance exercise. Am J Physiol Endocrinol Metab 283, E648-E657.
Crowe MJ, Weatherson JN, & Bowden BF (2006). Effects of dietary leucine supplementation on exercise performance. Eur J Appl Physiol 97, 664-672.
Curzon G, Friedel J, & Knott PJ (1973). The effect of fatty acids on the binding of tryptophan to plasma protein. Nature 242, 198-200.
Demant TW & Rhodes EC (1999). Effects of creatine supplementation on exercise performance. Sports Med 28, 49-60.
Dincheva D, Jandab B, Evstatievac L, Oleszekb W, Aslanid MR & Kostova I. Distribution of steroidal saponins in Tribulus terrestris from different geographical regions. Phytochemistry. 2007 Aug 22; Epub ahead of print.
Gautsch TA, Anthony JC, Kimball SR, Paul GL, Layman DK, & Jefferson LS (1998). Availability of eIF4E regulates skeletal muscle protein synthesis during recovery from exercise. Am J Physiol 274, C406-C414.
Haussinger D, Roth E, Lang F, & Gerok W (1993). Cellular hydration state: an important determinant of protein catabolism in health and disease. Lancet 341, 1330-1332.
Harris RC, Tallon MJ, Dunnett M, Boobis L, Coakley J, Kim HJ, Fallowfield JL, Hill CA, Sale C, & Wise JA (2006). The absorption of orally supplied beta-alanine and its effect on muscle carnosine synthesis in human vastus lateralis. Amino Acids 30, 279-289.
Henderson SA, Black AL, & Brooks GA (1985). Leucine turnover and oxidation in trained rats during exercise. Am J Physiol 249, E137-E144.
Hill CA, Harris RC, Kim HJ, Harris BD, Sale C, Boobis LH, Kim CK, & Wise JA (2006). Influence of beta-alanine supplementation on skeletal muscle carnosine concentrations and high intensity cycling capacity. Amino Acids.
Hoffman J, Ratamess N, Kang J, Mangine G, Faigenbaum A, Stout J. Effect of creatine and B-alanine supplementation on performance and endocrine responses in strength/power athletes. International Journal of Sports Nutrition and Exercise Metabolism. 16, pp. 430-446, 2006.
Layman DK (2002). Role of leucine in protein metabolism during exercise and recovery. Can J Appl Physiol 27, 646-663.
Mesa JL, Ruiz JR, Gonzalez-Gross MM, Gutierrez SA, & Castillo Garzon MJ (2002). Oral creatine supplementation and skeletal muscle metabolism in physical exercise. Sports Med 32, 903-944.
Norton LE & Layman DK (2006). Leucine regulates translation initiation of protein synthesis in skeletal muscle after exercise. J Nutr 136, 533S-537S.
Shimomura Y, Yamamoto Y, Bajotto G, Sato J, Murakami T, Shimomura N, Kobayashi H, & Mawatari K (2006). Nutraceutical effects of branched-chain amino acids on skeletal muscle. J Nutr 136, 529S-532S.
Tallon MJ, Harris RC, Boobis LH, Fallowfield JL, & Wise JA (2005). The carnosine content of vastus lateralis is elevated in resistance-trained bodybuilders. J Strength Cond Res 19, 725-729.
Tipton KD, Ferrando AA, Phillips SM, Doyle D, Jr., & Wolfe RR (1999). Postexercise net protein synthesis in human muscle from orally administered amino acids. Am J Physiol 276, E628-E634.
Zoeller RF, Stout JR, O'kroy JA, Torok DJ, & Mielke M (2006). Effects of 28 days of beta-alanine and creatine monohydrate supplementation on aerobic power, ventilatory and lactate thresholds, and time to exhaustion. Amino Acids.