What is the effect of the strongest Coleus Forskohlii extract (95% Forskolin) on the human body?

Coleus forskohlii, also known as Indian coleus, is an herb with a long history of use in traditional Ayurvedic medicine, and is widely used to treat a variety of conditions, including heart disease, pain, and seizures.
Because of this, a lot of research has been done to explore the benefits of these plants, and some other benefits have also been found.
ForsLean® is the only patented Coleus forskohlii root extract that can be used to reduce fat, improve lean body mass, and relieve mood disorders. Multiple clinical studies support the effects and safety of ForsLean.
ForsLean is standardized to contain 10% to 95% of the active ingredient forskolin. It is developed and produced by Sabinsa in the United States and has been on the market for more than two decades.

Focus of this article: Sports nutrition

This article will not cover the pharmacological potential of this herb, as this is beyond the scope of this public account. Instead, we will focus on the use of forskolin, the active ingredient in Coleus forskohlii, in sports nutrition and weight loss.
This means that we will study whether this herb can help users lose weight, increase testosterone, and increase strength and muscle mass. [7]Yes – all of these seemingly contrasting effects are possible – it just depends on your diet and exercise regime.

How Coleus Forskohlii Extract Works

Forskolin is actually the name of the bioactive component of the Coleus Forskohlii plant – it’s called labdan diterpenoid glucosides. This is a class of natural compounds known to have antibacterial, antifungal and anti-inflammatory activity.

What’s unique about forskolin is that it does much more than that.

ForsLean® Forskolin Stimulates Adenylate Cyclase

While its exact mechanism of action is still unclear, we do know that forskolin is a potent stimulator of cellular adenylate cyclase (AC).

When this enzyme (adenylate cyclase) is stimulated, it activates a secondary messenger in hormone signaling, cyclic adenosine monophosphate (3,5-cyclic AMP) or commonly known as cAMP,

which is a crucial biological messenger involved in many of our “energy transactions”. In one study, researchers found that forskolin was able to increase cAMP levels 4.82 times more than a placebo.

In fact, forskolin’s ability to increase cAMP levels is well established, and researchers often use it when studying the effects of increased cAMP in cells.
There is no doubt that forskolin is a very reliable and effective cAMP increaser, but what does this mean for our sports and fitness activities?
cAMP is a cell regulatory compound that is required to regulate a variety of cellular activities. We are most interested in the following effects of forskolin:

Stimulates anabolic and anti-catabolic effects
Promotes oxidation of fatty acids
Increases the body’s basal metabolic rate (BMR)
Increases testosterone levels
Promotes the increase of lean body mass.
Exercise also increases cAMP, so what is so special about forskolin?
If you’ve ever taken an exercise physiology class before, you know that this sounds similar to simple exercise, which can also achieve the same effects mentioned above through cAMP. [17]
There are many ways to activate cAMP (hormones, neurotransmitters, adrenergic receptors, etc.), so what makes forskolin so unique?
While cAMP can indeed be activated in a variety of ways, the pathways used to achieve cAMP stimulation can result in negative feedback effects. This means that after long-term or chronic expression of these hormones (or stimulation of these agonists), downregulation of the receptor or hormonal agent may eventually occur.
Essentially, your body fights back to achieve homeostasis and stay on an even keel - it will eventually adapt to whatever influences you throw at it (good or bad).
But Forskolin supplementation is different - its cAMP process is not hormone or receptor dependent! [13] Forskolin has the unique ability to stimulate cAMP completely independently!

Effect of Forskolin on cAMP levels in intact cells: "Forskolin adenine-labeled cerebral cortical slices increased cAMP accumulation by up to 35-fold." [10] Forskolin is located on the right side of this figure (D), and its efficacy is nearly universal among the other compounds tested.

In addition to this, it may also enhance cAMP increases when combined with hormone or receptor signaling responses, making it an excellent workout supplement.
In short, Forskolin is a great way to increase cAMP without the risk of hormone or receptor downregulation, producing all of the benefits listed above. It is believed that the increase in cAMP is the mechanism by which Forskolin is able to promote fat loss, act as an anabolic agent, and increase thyroid activity and thermogenesis. Let’s take a look at the studies now.

Fat Loss Effects of Forskolin

Weight loss occurs in two phases. First there is lipolysis, which is the release of stored fatty acids, and then there is fat oxidation, which is the “burning” of those fatty acids.

It is the first part – and arguably the most important part – lipolysis that we are going to focus on here.

Releasing Stored Fat Through Lipolysis
Fat is stored in fat cells throughout our bodies. Fatty acids bind to glycerol to form triglycerides, and the accumulation of triglycerides leads to an increase in adipose tissue. Therefore, if your goal is to lose weight, you must first release these fatty acids from the glycerol in order to get rid of the fat.

Forskolin sets off a chain reaction that ultimately leads to fat loss.

Here is a brief breakdown of the steps in lipolysis:

The neurotransmitter NE (norepinephrine) binds to adrenergic receptors (AR) present in the plasma membrane of fat cells.
Binding of NE to AR on the adipocyte triggers the release of G proteins.
The G proteins travel to adenylate cyclase in the cytoplasm.
Adenylate cyclase recruits ATP (the “energy molecule”) from within the cell and produces a secondary messenger protein, our friend cyclic adenylate cyclase (cAMP).
cAMP activates a cytoplasmic enzyme called protein kinase A (PKA).
The now activated PKA goes on to activate hormone-sensitive lipase (HSL).
HSL breaks down triglycerides into free fatty acids.
The released fatty acids can then be oxidized to ATP (burned to generate energy) [15]
In the above steps, adenylate cyclase is activated by hormones, leading to an increase in cAMP and cyclic AMP-dependent protein kinase (PKA), as well as phosphorylation and activation of the downstream enzyme hormone-sensitive lipase (HSL). [18]
Forskolin skips the hormones!
As mentioned earlier, Forskolin has the unique ability to directly activate adenylate cyclase without the need for hormone intervention! As a result, it increases cAMP levels, which in turn increases the release of fatty acids from fat stores, ultimately leading to adipocyte thermogenesis and lipolysis. [9,19,20,21]

This means that Forskolin has the potential to increase lipolysis without the use of stimulants. This is absolutely fantastic for those who don’t want to touch up to stimulants or want to add a bigger boost to their top fat burners.

Boosts Thyroid Function
In addition to the process described above (i.e. Forskolin -> increased cAMP -> increased HSL -> increased release of fatty acids to be burned as energy), Forskolin also has a positive effect on thyroid activity! [23,24]

In this regard, Forskolin has been shown to have the potential to stimulate the production of the thyroid hormones T3 and T4. Essentially, Forskolin enhances thyroid activity (comparable in strength to TSH) by activating adenylate cyclase in the thyroid gland [23,24].

In addition to this, Forskolin can also stimulate the conversion of T4 to T3. This thyroid stimulation helps increase the basal metabolic rate and promotes thermogenesis.

This is probably an area that needs more research, as thyroid boosters are extremely popular but not always well understood. If you are taking thyroid medication, it is imperative that you consult your doctor before starting any new diet or supplementation plan—especially one that boosts thyroid hormone, like forskolin.

Powerful Muscle-Building and Anabolic Effects

As mentioned earlier, the benefits of forskolin extend beyond weight loss. In addition to its ability to boost thermogenesis and increase thyroid activity, forskolin can also stimulate increases in bone mass and serum free testosterone levels in men, meaning that forskolin also has anti-catabolic and anabolic effects. [6,16]

Again, the way it does this is by increasing cAMP.

Remember that cAMP is a secondary messenger. What’s happening here isn’t all that different than what’s happening in fat cells—just the effects are different.

As before, forskolin binds to and increases cAMP production. This, in turn, activates the enzyme protein kinase A, which in turn positively affects androgen receptor binding. Not to mention, cAMP is also the signal for testosterone production (steroidogenesis) in Leydig cells.

On the surface, this may not seem that significant, but it is not. Increased cAMP also increases levels of steroidogenic acute regulatory protein (StAR), which is essential for stimulating the steroidogenic enzyme involved in transferring cholesterol to testosterone.

Essentially, high cAMP leads to a chain of events that starts with increased luteinizing hormone (LH) binding levels and ends with testosterone production.

A general process of the HPTA (hypothalamic pituitary testicular axis). This connection between the endocrine glands controls testosterone production.

Actual Results
In a 2015 paper published in the Journal of Obesity Research, researchers gave participants forskolin over a 12-week period and observed an average increase in free testosterone of 33%

A loss of 10 pounds of fat

An increase in lean body mass of 8 pounds [6]

Sound far-fetched? Badmaev observed similar results in a 2001 study! [28]
So, basically, the forskolin-induced increase in cAMP may stimulate the pituitary gland, which in turn increases LH output, which in turn increases testosterone production by stimulating the StAR protein…which plays a fundamental role in testosterone synthesis.
That sounds like a long story, but this is generally how natural supplements work. This mechanism is exactly what natural athletes are looking for—it’s obviously not for those who inject testosterone directly into their bodies.
For that matter, let’s not confuse a 33% testosterone increase with steroids, as they are definitely nowhere near that number. However, considering that this is a natural herbal supplement, the results are pretty impressive.

Anti-catabolic Effects

However, the benefits of forskolin don’t stop at building muscle—the compound also has anti-catabolic effects. This means that it can help prevent muscle breakdown, which is often a physique destroyer.

Whether you’re dieting and don’t want to lose muscle tone (lest you become the dreaded “skinny fat guy”) or you’re working out hard and don’t want to lose recovery, it’s extremely important to prevent catabolism as much as possible.

Like its previous effects, forskolin’s anti-catabolic effects are also cAMP-dependent.

So what happens during the catabolism/breakdown of muscle tissue? When exposed to dietary or physical stress, the proteins in muscle undergo hydrolysis, either partially into peptides or completely into amino acids. This process is called proteolysis.

Fortunately, this process is reversible. Under normal circumstances, our muscle mass is regulated by a balance between protein synthesis and protein degradation, and when this balance is impaired, muscle breakdown occurs. [29]

About Calpain Complications

So what does forskolin do here? To understand this, we must first quickly recap the physiological process of muscle breakdown: calcium-dependent enzymes, the calpains, control the breakdown of muscle tissue.

When these enzymes are activated, they participate in the breakdown of myofibrils (the basic rod-shaped units of muscle cells) and direct the resulting myofibril structures to the ubiquitin-proteasome pathway (UPP). [30]
In short, when these calpains are activated, some of your beloved muscle fibers say goodbye. The activity of these enzymes is regulated by calpain inhibitors. That’s where forskolin comes in.
Forskolin blocks this process
It turns out that calpain inhibitor activation is cAMP-dependent. This means that by supplementing with forskolin and activating cAMP, calpain inhibitor gene transcription will increase, inhibiting calpain activity and ultimately promoting muscle mass maintenance. [31]

Did you get the point? If not, don’t worry: the actual human studies on muscle growth above are what really matter.

Are there any side effects?
The most common side effect of taking forskolin is gastrointestinal discomfort, usually in the form of diarrhea. This is due to an increase in cAMP within the smooth muscle of the GI tract, which leads to increased contractions and motility.

Prevent side effects with highly standardized ingredients
This means that the rate at which substances pass through the digestive system will increase. This problem can be easily avoided by using high-quality, highly standardized extracts such as Sabinsa’s 95% ForsLean®, according to online user reviews. [32]
It uses a patented extraction process. [25] You’re more likely to experience this type of gastrointestinal discomfort with cheaper, less standardized extracts.
Finally, we have this to tell you: Don’t buy Forskolin unless it’s a 95% extract. That means stay away from cheap junk formula products on Amazon or those shady affiliate marketing sites looking for pure profit.
Blood Pressure Effects… Like Lowering Blood Pressure
Forskolin also has an effect on blood pressure. Unlike the above side effects, this side effect is not necessarily considered an adverse reaction. Forskolin does have the potential to lower blood pressure. It has even long been used for this purpose in Ayurvedic medicine.

So there are some inconsistencies to consider. Anyone diagnosed with hypotension or low blood pressure and/or stomach ulcers should avoid taking this supplement.

Individuals who are taking anti-asthma and anti-hypertensive medications should consult their healthcare provider before using this supplement, and warnings about thyroid medications should also come with it.

How to Take Forskolin?

The “optimal” dose is not known, with the recommended dose being 25 mg of Forskolin taken 30-60 minutes before meals, twice daily. Keep in mind, this is the amount of actual active Forskolin, not the total amount of Coleus Forskolin.

What is the best forskolin supplement?

Let’s say you’re taking a “forskolin supplement” that actually contains only 10% forskolin. To get the recommended dose, you’d have to take 250 mg twice a day for a total daily dose of 500 mg, and you’d need to be wary of diarrhea.

Worse still, some cheap forskolin supplements don’t even state how standardized they are. These supplements may not even be worth your time (or money).

Therefore, it’s important to consider