Anabolic Yogurt? Study shows it builds muscle - even in women By Jerry Brainum

A study presented at the 2007 International Society of Sports Nutrition (ISSN) conference included some interesting information on eating yogurt. Previous studies point to a connection between eating dairy foods and adding lean mass while losing bodyfat. The active ingredients in the process are calcium, for aiding fat loss, and vitamin D, for a boost in muscle mass. The new study examined the effects of eating yogurt while engaged in a weight-training program (though not at the same time!).
Thirty-five untrained women, average age 19, all of whom were considered calcium deficient because they got less than the minimum suggested daily intake of 800 milligrams of calcium, trained with weights for eight weeks. They were placed in three groups based on diet: yogurt, protein and carb.
The yogurt group ate three servings of yogurt containing 200 milligrams of calcium and 40 units of vitamin D per serving. The other two groups continued to follow their usual low-calcium diet.
Immediately after they trained, the yogurt group ate a serving of fat-free yogurt; the protein group drank a commercial sports drink that didn’t contain any calcium or vitamin D, just 19 grams of carbs and five grams of protein; and last group drank a carb-only beverage containing 25 grams of carbs. The yogurt serving and the drinks contained the same number of calories, 100 per serving.
As expected, the yogurt group boosted levels of calcium and vitamin D above the daily recommended allowances. While the groups were all getting similar amounts of protein in their diets, those in the yogurt group showed the greatest lean-mass gains. Though all the women lost bodyfat during the study (proving that weight training does stimulate fat loss), those in the yogurt group again came out on top. Finally, the yogurt group experienced the greatest strength gains, even though all of the subjects used the same exercise program.
Since all the groups got the same amount of protein, the greater progress made by those in the yogurt group indicates that the yogurt provided something that the others weren’t getting, namely added calcium and vitamin D.
Jerry Brainum

White, K., et al. (2007). Yogurt consumption during resistance training increases muscle mass and strength in young women. Presented at the 2007 ISSN conference, Las Vegas, Nevada.

ENERGY

Real-World Supplement Test

In a study presented at the 2007 International Society of Sports Nutrition conference, researchers tested the effects of having a preworkout energy drink on eight men who had weight-training experience. The study had a double-blind placebo-controlled crossover design, the gold standard for scientific studies.
The subjects reported to the lab on five separate occasions. During the first visit they were tested for one-rep-maximum strength in the squat. During the second and third visits they familiarized themselves with the training protocol used in the study, which required doing six sets of 10 reps with 75 percent of their one-rep-maximum weight in the squat, taking a two-minute rest between sets.
The subjects then began a creatine-loading phase for one week, taking 20 grams a day—four teaspoons—of creatine while training on their usual routines. They then returned to the lab for their final two workouts. At that point, however, the subjects were randomly divided into groups that would get either a placebo or a supplement. The supplement consisted of a combination of branched-chain amino acids, creatine, taurine, caffeine and glucuronolactone, which is a common additive in many energy drinks. Ten minutes after downing the drinks, the subjects began the experimental training session. Blood was drawn from the subjects before, immediately following and 15 and 30 minutes after the workout.
The results were significantly different only during the fifth set, although the total number of reps and training volume were higher in the supplement group. The supplement group also showed higher levels of growth hormone and insulin immediately and 15 minutes after the workout than those in the placebo group. The researchers concluded that consuming an energy supplement enhances exercise performance while augmenting anabolic hormone responses.

Hoffman, J.R., et al. (2007). Effect of a pre-exercise energy supplement on the acute hormonal response to resistance exercise. Presented at the 2007 ISSN conference, Las Vegas, Nevada.


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What's your poison? by Jerry Brainum

 In 2007, pet owners were horrified to learn that many commercial pet foods were contaminated. The culprit turned out to be malamine, a substance that was added to wheat gluten, a common ingredient in pet food. Metamine was surreptitiously added because of its rich nitrogen content (67%), and since protein is the only macronutrient that contains nitrogen, adding melamine to the food made it appear to be higher in protein that it actually was. This ingredient wasn't listed on pet food labels, but was added to the food by Chinese food processors. Sadly, many pets died from kidney failure after eating the contaminated pet food.    
     You might think that scenario is unlikely to occur in human food, but you’d be dangerously naive. In recent years several food supplements, mainly aimed at the bodybuilding market, have contained ingredients that weren’t listed on the labels. Analyses of several pro-hormone products showed that they contained not just pro-hormones but full-fledged hormones, including anabolic-steroid drugs. As the products were synthetic, the drugs had to be added.
     The good news is that nobody died from tainted supplements, although athletes may have failed drug tests. A few people who ingested the supplements suffered such problems as liver failure. Other supplements may contain ingredients that can lead to serious health problems.
       Take, for example, a reported case of arsenic poisoning in a 54-year-old woman who took kelp tablets.¹ Kelp is a rich source of trace minerals, especially iodine. Two-thirds of thyroid hormone, which controls basal metabolic rate, is iodine. The other third is the amino acid tyrosine.In the ’60s and ’70s kelp was a popular supplement among bodybuilders. They had few choices when it came to fat-burning supplements, and the theory was that a daily dose of kelp would boost thyroid hormone production, thus helping burn excess bodyfat and increase overall muscularity. Some bodybuilders took 30 to 50 kelp tablets every day.
     What the bodybuilders didn’t realize, however, was that iodine worked in what statisticians call a bell curve. Simply put, while a certain amount of iodine is indeed required for thyroid hormone synthesis, too much of the trace mineral leads to a slowing of thyroid function, or hypothyroidism. Conversely, in those with pre-existing thyroid illness, it can cause overactivity of the thyroid, or hyperthyroidism. That’s been observed in cultures where forms of kelp are a food staple, such as in China and Japan. Fortunately, even though taking in large amounts of iodine shuts the thyroid down, the condition is reversible when people stop getting so much iodine.²
    The 54-year-old woman complained of hair loss, memory loss and fatigue. Doctors initially attributed her symptoms to menopause and adjusted her hormone supplements. The woman took various supplements to treat the symptoms, including kelp tablets, fish oil, ginkgo biloba and grapeseed extract, but the only supplement she used consistently was the kelp. It turned out that her symptoms emanated from arsenic poisoning.
    She began with two kelp tablets daily, then gradually increased the dose to four a day. In due course she developed additional symptoms, including diarrhea, nausea and vomiting and had pressure headaches, feeling as if there was a band around her head. Weakness and fatigue followed, requiring additional sleep. Within a few months she noticed a skin rash on her legs. Her toenails began falling out.
     Her doctor realized that her symptoms indicated toxicity, and a spot urine test showed an elevated arsenic level. Analysis of her food supplements revealed that the kelp tablets were rich in arsenic. As soon as she quit taking them, her symptoms abated, and eventually the arsenic disappeared from her body.
    Arsenic is a poison that’s found naturally in the environment and as a result of industrial contamination. Soils rich in arsenic can yield foods with higher content of the toxin. Because of the high concentration of arsenic in algae and microorganisms eaten by fish, seafood averages four to five parts per million compared to the 0.02 PPM found in grains and cereals, which is below toxic levels.
     The authors of the kelp case study purchased nine samples of kelp supplements from health food stores. Arsenic was detected in eight of them, and the concentration in seven exceeded the Food and Drug Administration’s tolerance level of 2 PPM. As it happens, kelp isn’t that popular among bodybuilders these days.
    Then again, that may not help if you eat chicken. It seems that an arsenic compound called Roxarsone is mixed into the diet of about 70 percent of the 9 billion chickens produced annually in the United States.
 The intent is to promote growth, kill parasites that cause diarrhea and improve the pigmentation of the chicken meat. While relatively benign, Roxarsone converts in the chicken’s body to inorganic arsenic. According to the Environmental Protection Agency, long-term exposure to inorganic arsenic can cause bladder, lung, skin, kidney and colon cancers and adversely affects immune function, the nervous system and hormone release. Low-level exposure is linked to paralysis and diabetes.
    A 2004 report from the United States Department of Agriculture showed that most people eat 1.3 to 5.2 micrograms per day of inorganic arsenic from chicken alone. Those who eat large amounts of chicken (such as bodybuilders) consume 21 to 31 micrograms daily. An analysis of 151 samples of raw chicken obtained from markets in Minnesota and California revealed that 55 percent contained inorganic arsenic ranging from 1.6 to 21.2 PPM. Three-fourths of the samples taken from conventional poultry farms showed detectable levels of arsenic, but only one-third of samples from certified organic and premium farms had detectable levels. Chickens from Tyson and Foster Farms, which had both stopped adding Roxarsone to chicken feed, had no arsenic. The doctor who released the report commented, “As a physician, I find it ludicrous that we continue feeding arsenic to chickens now that we know it increases our cancer risk and is unnecessary for raising chickens.”
   The National Chicken Council responded by saying that the report wasn’t “scientific” and that there was no reason to fear the use of arsenic-based feed additives. Chickenspeak translation: “Pluck you!”
                                                        
                                                         References

1 Amster, E., et al. (2007). Case report: Potential arsenic toxicosis secondary to herbal kelp supplement. Environ Health Perspect. 115:606-608.
2 Kasagi, K., et al. (2003). Effect of iodine restriction on thyroid function in patients with primary hypothyroidism. Thyroid.
3 Hileman, B. (2007). Arsenic in chicken production. Chem Engin News. 85:34-35.

   

Want more evidence-based information on exercise science, nutrition and food supplements, fat-loss, ergogenic aids, and anti-aging research? Check out Applied Metabolics Newsletter at www.appliedmetabolics.com.

 

 

 

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The Ultimate Guide to Prohormones by Jerry Brainum

If you’re confused about the benefits of prohormones, don’t feel alone. When the United States Congress passed the Food Supplement act of 1994, it opened the door for formerly esoteric food supplements, including prohormones. The term “prohormones” doesn’t refer to any secret drugs used by professional athletes. Instead, it refers to steroidal compounds that can be converted into hormones in the body, including both testosterone and estrogen, as well as various hormonal byproducts and metabolites.

In the beginning, the prohormone market was simple. You had Mexican yam supplements that were wrongly thought to convert into active hormones (they do, but only with the assistance of certain enzymes not found in the human body); and dehydroepiandrosterone (DHEA). DHEA, still a popular supplement, acts as a precursor for both testosterone and estrogen, as well as a formerly little known intermediate in the steroid biosynthesis pathway called “androstenedione.”

DHEA may provide health benefits related to antiaging properties, but as a testosterone precursor, it left much to be desired. For example, in women, it nearly always converts into testosterone, but in men it’s fate isn’t as certain. In most cases, males convert DHEA into androstenedione, and from there it can take numerous pathways--including the undesirable estrogen route. While it would appear that androstenedione, which has a far more direct conversion into testosterone is a better choice than DHEA, only one man initially recognized this fact.

That man was Patrick Arnold, 33, a Seymour, Illinois-based chemist with an extensive knowledge of both chemistry and particularly, prohormones. Arnold has a bachelors degree in chemistry and 3 years of graduate study in chemistry from the University of Connecticut. When the public furor over baseball slugger Mark McGwire’s use of androstenedione peaked, Arnold was a sought-after expert on the effects of androstenedione. To provide a pure source of this prohormone, and subsequently others, Arnold formed a company called LPJ, with which he continues to pursue both prohormone sales and development.

But recent negative studies published about the effects of androstenedione have cast a pall over the use of prohormones for bodybuilding purposes. Add to this the ever increasing roster of various prohormones introduced since androstenedione hit the market a few years ago, and you can’t help getting confused about both the effects and benefits of these supplements.

The latest types of prohormones even feature allegedly superior delivery systems, such as cyclodextrins and liposomes--words familiar to some scientists, but likely to draw a blank with the hoi polloi of bodybuilding. Both refer to special delivery systems designed to optimize prohormone absorption. Cyclodextrins use a carbohydrate-enveloping effect with prohormones, while liposomes act in a similar manner using a fat-envelope. The effect is somewhat like a “Trojan horse,” allowing prohormones to bypass initial near-complete destruction in the liver. But this isn’t as simple as it appears. Are some cyclodextrin products better than others? How does liposome delivery compare with cyclos? Let’s clear up the confusion here and now by going to the guru of prohormones himself--Pat Arnold.
Q: A new type of delivery system for prohormones is about to emerge called “liposomes,” what are they, and how does this type of prohormone supplement compare with cyclodextrin prohormone delivery?
A: Liposomes are bi-layered shells made from certain kinds of lipids. These particular kinds of lipids, i.e., fatty acids, phospholipids, have a fattylike or non-polar end to them, combined with a more waterlike or polar end, and a long-chain structure. What these lipids can do in water under the right conditions is line-up in such as fashion that all the polar ends are sticking out from a center in which the non-polar ends are anchored.

The whole thing folds upon itself, giving a shell with a water-soluble exterior and a oil soluble interior (somewhat similarly to cyclodextrins). Non-polar drugs, such as steroids, can be trapped in the non-polar tails of the lipid chains in the interior of the liposome. These shells can also be formulated to have many layers, like an onion. The non-polar drugs, including steroid prohormones, can be trapped in the non-polar portions in each layer.

Some manufacturers have made prohormone liposome products, mainly for oral consumption. When a prohormone liposome is ingested, it passes through the stomach into the small intestine. In the small intestine, the liposomes come into contact with the non-polar intestinal cell lining, merging with it. Picture two soap bubbles merging together. When this happens, the prohormone trapped in the interior of the liposome is efficiently transferred into the intestinal lining. From there, it travels into the portal circulation to the liver.

Multi-layered liposomes take longer to completely merge with the intestinal lining cells and deliver their contents. So these are used to provide a more sustained delivery compared to single-layered liposomes. A product that contains different sized liposomes of various layer amounts should theoretically provide a time-released delivery of prohormones.

A single-layered liposome encapsulated prohormone should work similarly to a cyclodextrin (hydroxypropyl-beta-cyclodextrin) complexed prohormone. In other words, put the steroid in a water-soluble shell, then deposit it in the lipidlike surface of the oral or intestinal mucosa. However, the flux between the cavity of the cyclodextrin molecule and the mucosa is far more efficient and faster than liposomes. A liposome must first merge and dissolve into the mucosal cell membrane before its contents are delivered. In contrast, the cyclodextrin molecule undergoes no such interaction at the mucosal membrane, and does not disintegrate; it simply instantaneously delivers its prohormone payload.

A possible advantage of liposome delivery over cyclodextrins is that liposomes may provide a time-released delivery effect through using multilayered liposomes. However, I don’t believe that prohormones should be given in a time-released fashion, because doing is relatively ineffective.

My conclusion about liposome products is that single-layered liposomes featuring good manufacturing standards are a great oral product, and may also be effective sublingually (under the tongue). But I see little or no promise in the multi-layered, controlled release liposome products. In addition, I don’t think even the single-layered liposome products work as well as the cyclodextrin-complexed products.
Q: What happens to standard prohormones in the liver, and could they be toxic to that organ in a manner similar to anabolic steroid drugs?
A: Prohormones in the liver are for the most part metabolized into inactive end products, such as androsterone and etiocholanone. These end products are then usually conjugated with glucuronic acid, which renders them water soluble. They can then be excreted in the urine.
These processes used to metabolize natural steroid hormones are not significantly stressful to the liver. The medical literature shows that non-ankylated steroids such as these do not cause any toxic effects in the liver, even at relatively high doses.

Many doctors and uniformed scientists are lumping all androgenic steroids in with ankylated oral androgens (such as the anabolic steroids methyltestosterone and oxymetholone or Anadrol). Such synthetic ankylated oral steroids feature chemical alterations enabling them to resist certain metabolic deactivations in the liver. As a result of these alterations, a toxic burden is imposed on the liver. Prohormones, which don’t have such alterations, are therefore nontoxic to the liver.
Q) What advantages do cyclodextrin prohormones have over standard prohormones?
A: Cyclodextrin-complexed prohormones, and we are speaking here of the highly soluble hydroxypropyl-beta-cyclodextrin complexed products--not the inferior, poorly soluble beta-cyclodextrins, render prohormones water soluble and are efficiently absorbed into mucosal tissues (mouth, nasal, intestinal lining). This delivery is far more efficient compared to simple prohormone powders in capsules.
A major advantage offered by cyclodextrins is that they have good delivery efficacy through non-gastrointestinal routes, such as under the tongue, thus preventing the usual extensive first-pass liver destruction that happens with most standard prohormones. The result is a far higher blood androgen response per each milligram of prohormone administered. Cyclos will be much less bioavailable when taken orally, but they are still superior to simple encapsulated powdered prohormones.

Q: Are cyclodextrin prohormones (CPH) harmful from a health perspective in any way? For example, can they adversely affect blood lipid levels in manner similar to oral anabolic steroids?
A: Cyclodextrin prohormones, in fact all prohormones, share the same potential health risks associated with prescription testosterone and other steroid drugs. These include possible negative effects on cholesterol (lowered HDL levels); male pattern baldness; acne; gynecomastia (male breast development); prostate gland enlargement; depression of endogenous testosterone production, among others.

On the other hand, cyclodextrin prohormones may present far lower risk of certain side effects. For example, the liver is the site of cholesterol synthesis and lipoprotein production, as well as being quite rich in aromatase enzyme activity (aromatase converts testosterone into estrogen). Since cyclo products avoid first-pass metabolism in the liver, and require lower dosages, I would think that side effects such as HDL depression and gyno should be minimized by this dosage form. In fact, cyclodextrins have been shown to reduce cholesterol when taken orally. They can complex with ingested food cholesterol and inhibit the absorption of such food-contained cholesterol.
Q: What’s the optimal way to take CPH in regard to dosage, timing, with or without meals and so on?
A: CPH are only available in sublingual form now, so I’ll only comment on that. In a study conducted by researchers at East Michigan University, 25 milligrams of cyclo-diol gave similar blood responses to 50 milligrams. However, we never tested anything less than 25 milligrams, so we still don’t know if lower milligram amounts are just as effective as 25 milligram doses.

CPH should probably be taken an hour before meals, since some prohormone may still be unabsorbed in the mouth for some time after the lozenge is dissolved. You should not drink anything for perhaps 10 to 15 minutes after the lozenge is fully dissolved. I think for most young men, these cyclos should be taken at least three times a day. You can take more, but it doesn’t make sense to take more than has been found effective.
Q: Can women use CPH safely, and if so, at what doses?
A: Women can probably take a cyclo-nor-diol prohormone. I know that many fitness competitors love nor-prohormones, and cyclos are the best way to take them.

I won’t make up things just to impress you. I really have not investigated the use of prohormones by women that much, and as such, aren’t secure enough to suggest recommended dosages for them. I plan on doing some interview-type research with women nor users to determine what they are using and finding to be safe. Also, what, if any, side effects they may be experiencing. I have to do this because I think few women would volunteer for a dose-response study on an androgenic product [produces male pattern side effects, including facial hair growth, and so on].

I hope to learn a lot more on the use of nors by women, and then write an article in one of the women’s fitness magazines discussing my findings. I may even decide to market a lower dosage type of prohormone specifically for women. Any female athletes who are reading this and now using prohormones should contact me by mail at parnold8@ix.netcom.com, and discuss their results with me. I would be very appreciative for this feedback, and will certainly respect their anonymity if they wish.
Q:Are slow-release and absorption a desirable aspect of prohormone supplements?
A: I believe that sustained release oral prohormones are probably ineffective for the most part, and that the whole idea of sustained release runs counter to what science has demonstrated concerning the liver metabolism and oral bioavailability of these compounds.
The reasoning behind this assertion is based on bona-fide research showing that compounds easily deactivated in the liver require large amounts to increase blood levels. The reason for this is that large amounts will overwhelm the liver’s degradation capacity and allow undestroyed compound (prohormone) to pass through into the general circulation. In contrast, a time-released product will provide a trickle of prohormone to the liver over a longer time period. As a result, the small trickle is easily metabolized and not much will get into the blood.

I believe that oral prohormones should be taken in three relatively massive divided doses throughout the day. I’ve found this technique to be extremely effective, leading to significantly elevated blood androgen levels during most of the day. These oral doses can be given as single layered liposomes or cyclo complexes (the most orally bioavailable), or as micronized (next best, but expensive) formulations or as simple prohormone capsules (best bang for the buck as far as orals).
Q: Besides the recent adverse studies related to androstenedione, one as yet unpublished study showed some good effects related to prohormones--can you tell us about that study and what it found?
A: This study was different, in that the featured prohormone wasn’t androstenedione, but 4-androstenediol (4-AD or Androdiol). The study was done at Eastern Michigan University, and examined the effects of a dose of 450 milligrams a day of 4-AD for 4 weeks. The results showed significant lean mass gains in the study subjects, and also significant strength gains. There were no significant effects on beneficial high density lipoprotein cholesterol (HDL), although this type of “good” cholesterol carrier actually increased in the 4-AD group. In addition, the study found no adverse effects on estrogen levels, luteinizing hormone level (a pituitary hormone that controls testosterone levels in the body), and blood markers for liver toxicity.

I’m starting to sound like a broken record lately, as I have constantly tried to beat into the public mind that there’s a huge difference between 4-AD and androstenedione. 4-AD does not convert directly into estrogens like androstenedione, and is a far more efficient precursor for testosterone. This study could help further my cause, but the study author has experienced difficulty getting it published. Not because of any inherent flaws in the study, but merely for reasons of prejudice against these prohormones.

My company, LPJ, and other companies are co-funding an even more comprehensive safety and efficacy study on 4-AD next year, and I hope the sheer weight of available evidence from these studies finally forces someone to publish the data.
Q: Did the East Michigan Study use the cyclodextrin form of 4-AD?
A: No, I believe they used a simple chewable formulation, which of course involved oral intake.
Q: Would larger doses than what is usually suggested lead to better results with prohormones?
A: Undoubtedly. Dosages under 500 milligrams a day lead to so-so results. Many people have tried this, became disappointed, and then simple wrote off prohormones as ineffective. I am confident enough now, from what I’ve seen in athletes and in myself, to say that oral doses of 1,000 milligrams or even 2,000 milligrams a day of 4-diols (Androdiol or norandrodiol in a stack) lead to impressive results--even dramatic results--with no great increase of side effects. The lack of gyno seen with even mega-doses of 4-diols amazes me, leading me to wonder if the diols themselves in the unconverted form might not impart some kind of antiestrogenic activity. This is a long shot, I guess.

Larger doses produce not only greater blood androgen concentrations at peak, but a far more protracted time in which significant elevations are present in the blood. Three daily doses of 400 milligrams or so should elevate testosterone to the extent that daily blood levels are either far above normal or at least significantly elevated. This kind of cycle, however, should not be done for more than 6 to 8 weeks, and at least that much time should be taken off in between. Remember, you are elevating your androgen levels nearly all the time, so some LH shutdown due to negative feedback inhibition is an unavoidable consequence. As a result, you need to allow your endocrine system time to get going again. The same is true for androgenic/anabolic steroid drugs.
Q: Which is more expensive to produce and sell: hydroxy or beta cyclodextrins?
A: They aren’t too different as far as production costs, but the raw materials for hydroxy complexes are far more expensive.
Q: Since the hydroxypropyl-beta-cyclodextrins (HBC) is more water-soluble compared to the beta-cyclodextrins and is far superior, to your knowledge are there any commercial prohormone products currently marketed that contain the more desirable HBC form?
A: I believe Supertech, OSMO, Kaizen, Sportpharma, and my company, Ergopharm, sell HBC complexed prohormones.
Q: Do you think that the recent adverse publicity related to androstenedione will turn-off consumers considering the use of any type of prohormone supplement?

A: I don’t think, I know. I sometimes end up talking to strangers in gyms and health food stores around the country, and when the subject of prohormones comes up, the general response is “I’m scared of that shit” or “I’ve heard it makes you grow tits” [an objection presumably voiced by males only], or something like “I’ve tried that Andro-6 stuff and it didn’t do anything for me.” The media succeeded in imparting a big scare into consumers regarding prohormones following the publication of those adverse andro studies. That, coupled with the fact that many people tried the stuff at the old recommended dosages that I know to be suboptimal and ineffective, led such people to conclude that prohormones are just a ripoff. This has hurt the industry somewhat. Because of all these misconceptions, I’ve been trying to re-educate people about the differences between diones and diols, and what dosage patterns and forms should be used to see the promised results.
Q:Do you think the Food and Drug Administration (FDA) is trying to remove all prohormone supplements from the market? How would they accomplish this?
A: I don’t think the FDA is trying to get rid of prohormones, but the Drug Enforcement Agency (DEA) is certainly zealous in this regard. The FDA has limited power, and can’t remove prohormones from the market unless they prove clearly toxic in some way. Since, thus far, this toxicity hasn’t emerged, the FDA can’t act yet.

But the DEA, which also monitors illicit anabolic steroid usage, has their sights set on prohormones. Now, the target is just androstenedione; however, if the DEA can get rid of androstenedione, the other prohormones will also go like dominos. Federal drug czar, Barry McCaffrey, has publicly stated that he has an agenda to remove that “dangerous andro” from the market for the sake of our children’s lives.

The plan, as I know it--and this isn’t a secret--is for the government to fund a test (probably on animals) that provides massive amounts of androstenedione, possibly by injection, to prove there is some anabolic activity. Without a doubt, androstenedione is anabolic at megadoses, and when they find this, they can then say that androstenedione fits all the classifications of being an anabolic steroid under the 1990 Anabolic Steroid Control Act. Androstenedione would then be categorized as a class-3 controlled substance, meaning that possession of it will constitute a felony.

Since no one can show that prohormones are overtly dangerous, I can only deduce that our government considers muscle building to be a threat to society. What other explanation can there be?
Q: Considering the recent studies showing adverse effects associated with androstenedione, do you now consider this prohormone ineffective, or still useful for some purpose?
A: I consider androstenedione too weak and too much of an estrogen precursor for chronic bodybuilding use. However, I think it may be quite effective as a libido booster, since both androgens and estrogens are responsible for sex drive.
Q: In terms of anabolic effects, how do prohormone supplements compare to actual anabolic steroid drugs?
A: Anabolic steroid drugs have varied abilities to pack on muscle weight and different propensities for water retention. Regarding prohormones, the 4-diols at high dosages seem to produce gains similar to moderate doses of testosterone and nandrolone. I’m speaking here of doses equal to 1,000 to 2,000 milligrams of 4-AD, nor-4-AD, or a daily combination of both. I realize that people are likely to roll their eyes upon reading this and say,”Here goes the bullshit again,” but I say let them go out and give it a try for a few weeks.
Q: Would the side effects, if any, for CPH be similar to that of anabolic steroid drugs?
A: On a qualitative basis, the side effects from 4-AD are similar to testosterone as far as water retention and androgenic effects go, but the gynecomastia risk seems to be substantially lower. The side effects from nor-4-AD are qualitatively similar to nandrolone.
Q: Should certain people avoid taking any type of prohormone supplement?
A: Anyone who has a medical contraindication to avoid androgen drugs, such as testosterone or nandrolone esters, should not use prohormones. This includes people with prostate cancer, breast cancer, and those who have not yet reached full linear growth (final height, as in teenagers). To find out other examples of people who should avoid using prohormones and associated precautions, as well as possible side effects, check the entry for “testosterone” in the Physician’s Desk Reference.
Q: Since testosterone appears to play a role in prostate gland enlargement, should men with this condition avoid using prohormones?
A: Not necessarily. They may be able to use a 5-alpha-reductase inhibitor [such as finisteride or Proscar] with their 4-AD and still be okay. Or better yet, they may find that a nor-prohormone like nor-4-AD actually helps their prostate by competing with testosterone (more specifically, norDHT competing with dihydrotestosterone, the testosterone metabolite responsible for prostate enlargement) in the prostate, resulting in far less androgenic stimulation and growth. However, I must advise anyone to check with their doctor first--even though their doctor is likely to be clueless about the subject, and too scared to suggest anything but staying away from all prohormones.
Q: Some people have suggested that 19-nor prohormones may cause impotence due to a progestinlike structure--is this possible?
A: This is sheer baloney. Nandrolone does have a weak progestogenic activity, but even so, progestins have never been implicated in reducing libido. The only exception to this is when the progestin in question also had antiandrogenic qualities, due either to cell receptor antagonism or indirectly by suppressing luteinizing hormone from the pituitary gland.

But it’s true that 19-nors may decrease libido or sex drive by competing with testosterone at the level of the central nervous system, i.e., in the brain. This results in less androgenic stimulation in brain centers controlling sex drive.
Q: Are there any specific food supplements or nutrients synergistic with prohormones?
A: I hate that word “synergistic,” because it’s so often misused and abused in the supplement industry. I would say there’s nothing synergistic out there, but a high protein diet that also supplies other ergogens can only help increase gains during a prohormone cycle.
Q: Should people concerned about androgenic side effects, such as male pattern baldness, acne, and prostate enlargement, stick with only 19-nor prohormones?
A: For the most part, yes, if they want to play it smart.
Q: What are the maximum and minimum effective doses for CPH?
A: I have to admit that at this time, I don’t know. What I do know, based in the results of the East Michigan University study discussed earlier, is that taking more than 25 milligrams at one time won’t do any good. The optimal dosage lies somewhere between 5 and 25 milligrams, and I will someday find the precise dose.
Q: Can taking CPH 3 times a day or more lead to a feedback suppression of endogenous testosterone synthesis?
A: Used 3 times a day, I don’t think so. At least I know that cyclodextrin testosterone taken 3 times daily resulted in suppression only while the testosterone levels were elevated, and when they returned to normal, so did LH. I would expect the same to be true for CPH. I don’t know at which level over 3 times a day that you would reach a level of suppression that would not fully return readily to normal testosterone output.
Q: Would using any of the CPH forms of prohormones increase aggression?
A: My view on the entire ‘roid rage thing is that people who are assholes tend to be worse assholes when they build muscles. People with normal temperaments just get more confident for the most part.

Q:Are there any currently available natural estrogen antagonists that are effective?
A: I think indole-3-carbinol and its derivative, diindolymethane, are potentially effective compounds. However, I don’t know how well they are working in the real world at this time. I introduced a flavone called chrysin in 1996. But I always demanded that in-vivo testing be done before it was marketed. Despite the lack of such “in the body” tests, various companies marketed it based solely on hype.

Last year, my company, for a measly $350, funded a simple test on chrysin using rats as subjects. We had several groups, such as those receiving the chrysin as injections, orally, or other rats given a placebo for each of these. The results showed no effects of chrysin on estrogen, but the rats did get fatter after using chrysin.
Q: Regarding DHT, the “bad byproduct” of testosterone linked to male pattern baldness, acne, and prostate enlargement, some people suggest that the herb saw palmetto may reduce DHT synthesis. Would it be a good idea to take saw palmetto concurrently with CPH?
A: No, unless you are taking the herb for some health reason. The problem with saw palmetto is that it may potentially reduce the effectiveness of prohormones.
Q: To your knowledge, are there still untapped possible prohormones that have yet to be marketed?
A: As far as androgenic prohormones, I know of at least one that still isn’t marketed. But it has no advantages over the current best types of prohormones that are available, so there isn’t any actual reason to market this particular substance. I believe the androgen prohormone possibilities have been exhausted as far the best ones go. Someone may place a synthetic (perhaps unknowingly) on the market and call it a prohormone, but that’s breaking the law, and not what we’re talking about.

I do know of a steroidal prohormone that isn’t androgenic, yet may have some valuable athletic benefits. I don’t want to discuss anything more about it now, but this will definitely be a future product of my company.
Q: What type of future effective delivery systems for prohormones do you anticipate; in fact, what do you view as the future of prohormones in general?
A: I think an aqueous solution of cyclo prohormones, taken intranasally, would be quite effective, especially prior to a workout. The nasal passages go high up into the head, right next to the base of the brain. Absorption through these membranes should promote an amplified central nervous system effect. I have, in fact, made these for my own use and found them to be potent enough to feel right away.

I have developed a sustained-release cyclo product made to stick in a particular part of the mouth and dissolve very slowly. This product will provide both the high bioavailability of cyclo prohormones taken through a route that bypasses the liver, as well as a sustained release into the blood. On top of that, with this product there is virtually no bitter taste problem as is the case with sublinguals. I said earlier that sustained release delivery of orals is a bad concept because of liver degradation. However, this new product, being better absorbed through the lining of the mouth, doesn’t undergo first-pass liver metabolism, and thus is very suitable for sustained release. This stuff required extensive research and formulation work to get right, so I would expect that anyone who tries to produce a knock-off product would probably create a crappy and obvious counterfeit.

  

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Resveratrol: lasts longer than believed by Jerry Brainum

Resveratrol is a compound found naturally in such sources as grapes, peanuts, berries, and most famously, in red wine. For years, the various health benefits attributed to a moderate intake of red wine--two glasses a day--have thought to come from the resveratrol content of the wine. But red wine doesn't contain a lot of resveratrol, and more recent research suggests that resveratrol is merely a player in a larger team of nutrients that actually are responsible for the observed health benefits of red wine consumption.
   This is not to say that resveratrol itself doesn't provide significant health benefits, but rather that the studies that have shown such benefits have involved animal studies, in which doses of resveratrol equivalent to drinking thousands of bottles of wine have been provided to the lab animals. These benefits have been considerable, such as helping to offset the metabolic syndrome, a precursor of both cardiovascular disease and diabetes. Other studies suggest that resveratrol may provide anti-aging effects. Some even suggest that resveratrol, through activating a cell protective protein called SIRT-1 can mimic some of the beneficial effects of caloric restriction. Caloric restriction remains the only method established to increase longevity in animals. There is no human evidence that CR would work the same way in humans. Resveratrol is thought to provide some of the same benefits as CR, but without the odious reduction in food intake. What the studies actually show, however, is that resveratrol does appear to boost lifespan in obese rats who consume a very high fat (60% of caloric intake) diet. It didn't provide any significant life extension to leaner rats eating a normal diet.
     Critics of resveratrol have often noted the dearth of human research about its putative health effects. They also note resveratrol appears to be rapidly metabolized when orally ingested. Specifically, within 14 minutes following oral intake, resveratrol is conjugated in the liver. This means that it is combined with either sulfate or glucuronide compounds. Some have hypothesized that this liver-induced change in resveratrol renders resveratrol unavailable to cells, thereby making it useless.Because of this, those who are into various suggested "anti-aging" therapies have opted to go around the suggested resveratrol metabolic roadblock by ingesting huge doses of resveratrol in the hope that ingesting such megadoses will provide the various health benefits of resveratrol. In fact, ingesting such large doses may be hazardous to health, since some research suggests that while resveratrol normally provides antioxidant activity, when you consume it in large doses, it acts as a pro-oxidant, which can paradoxically damage cells. One recent study showed that resveratrol provided to those who suffer from multiple sclerosis may worsen symptoms of the disease.
     But according to a new study from Great Britain, the notion that resveratrol is rendered biologically inert within minutes is wrong. In fact, the study showed that resveratrol complexed with sulfates is reduced by enzymes in the cell that remove the sulfate portion, thus converting the compound into pure resveratrol, which is active in the cell. The study, which involved mice, found that providing the rodents with resveratrol did result in increased blood levels of free or unconjugated resveratrol in the blood, and in various other tissues. When human colon cancer cells were exposed to the resveratrol, resveratrol caused the cancer cells to self-destruct, and also produced a rapid aging effect in the cancer cells, which also led to the destruction of the cells.
   Perhaps the best news is that you don't need to ingest huge doses of resveratrol to obtain the health benefits. Now that it's established that resveratrol is indeed absorbed into cells following oral ingestion, the next studies should determine the precise optimal doses of the nutrient that would provide maximum health benefits with few, if any risks. Also, while these new findings involved lab animals, and also isolated human cancer cells, the mechanisms involved both are known to exist in the human body. This suggests that the findings of the study are likely also applicable to human physiology.

   Patel, KR, et al. Sulfate metabolites provide an intracellular pool for resveratrol generation and induce autophagy with senescence. Sci Trans Medicine 2013;5:205ra133.      

 ©,2013 Jerry Brainum. Any reprinting in any type of media, including electronic and foreign is expressly prohibited.

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Can melatonin help you lose body fat? by Jerry Brainum

Melatonin is a natural hormone secreted by the pineal gland in the brain. Melatonin is synthesized through a series of enzymatic steps starting with the presence of the essential amino acid, L-tryptophane. The tryptophane is converted into serotonin, which is a brain neurotransmitter, and then converted into melatonin. This happens at night, and melatonin has long been associated with sleep onset. In fact, it's sold as an over the counter food supplement for that purpose. Besides being available in food supplement form, melatonin is also found naturally in small amounts in various foods, such as fruits, vegetables, cherries, almonds, mustard, and other foods. Besides its use as a sleep aid, melatonin also has been shown in various studies to be useful in treating diabetes, elevated glucose levels, and elevated blood fats. It is considered safe when used in moderate amounts. The usual dose for sleep onset purposes is 1-5 milligrams, taken an hour prior to sleep. Any more than this results in extreme morning grogginess. As you might expect, since melatonin promotes the stages of deep sleep, it also promotes growth hormone release during sleep. One study published a few years ago found that when young men ingested melatonin prior to exercise, they showed significant elevations in growth hormone release during exercise. This, however, is not advised, since melatonin will make you feel sleepy, and thus is not conducive to intense training.
     While having excess body fat is considered antithetical to good health for a number of reasons, there is one type of fat that is beneficial. Known as brown adipose tissue or simply, "BAT," this type of fat provides a potent thermogenic action, converting excess calories into heat. This tends to help keep body fat levels lower. While humans were previously thought to express BAT only during infancy, more recent research has found that BAT is more active in adults than previously believed. Some suggest that BAT explains why some people can consume more calories than others, yet not get fat. Another type of fat recently discovered is known as beige adipose tissue. Similarly to regular BAT, this type of fat is thermogenic, but doesn't contain as any mitochondria (where fat is oxidized) as the usual form of BAT. But the beige fat does contain higher amounts of the same thermogenic protein found in BAT, namely uncoupling protein-1 or UCP-1. White adipose tissue or the usual type of fat found in the body, can be converted into beige fat through exposure to cold. But according to a new study, another way to convert white fat into more active beige fat is by providing melatonin.
   The study involved both diabetic fat rats, as well as normal, thin rats. Providing melatonin to the rats increased the sensitivity to cold exposure (thus producing more beige fat), as well as boosting the thermogenic effect produced by exercise. The researchers who conducted this study were surprised to find that melatonin produced these beneficial effects in both the diabetic obese rats as well as the thin normal rats.The amount of melatonin supplied to the rats was 10 milligrams per kilogram of bodyweight, but this would be modified for a human dose, and thus humans would need ingest a far lower dose to get the same effect as the rats. Precisely how much hasn't yet been determined. The levels of UCP-1, the primary thermogenic protein in BAT and beige fat, doubled in the rats provided with melatonin. Melatonin also boosted the levels of another protein called PGC-1A, which promotes the development of additional mitochondria, by 25% in the lean rats, and more than double in the fat rats.
    While this research looks promising, it must be kept in mind that it involved rats, not humans. While the existing mechanisms also occur in humans, whether melatonin will produce similar effects remains to be studied. In addition, the ideal human dose for this purpose also needs to be determined before melatonin can be recommended as a fat-loss aid.

                                                                    Reference

   Jimenez-Aranda, et al.

Melatonin induces browning of inguinal white adipose tissue in Zucker diabetic fatty rats. J Pineal Res 2013: in press.

 ©,2013 Jerry Brainum. Any reprinting in any type of media, including electronic and foreign is expressly prohibited.

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