4.2. Cholinergic nervous

Nucific Bio X4. Cholinergic nervous

Stock Koleos appear to have the characteristics of acetylcholinesterase inhibition with the value of IC50 1.02 +/- 0.02 mg / ml in vitro [15] [6], which seems to survive the digestion in the stomach simulation [15], and it was observed valid after oral ingestion 600 mg / kg in mice. [14]

It is believed that these effects to be secondary to acid rosmarinic, the presence of IC 50 value of 0.44mg / ml, inhibition appears to be reversible. [14] [6] was detected in the brain rosmarinic acid (20.4-24.1μM 30- 60 minutes after intraperitoneal injection of 1 g / kg) after eating tea leaves and Coleus activity was noted that acetylcholine fell by 5.5 to 10% (60 minutes and 30 minutes, respectively). As it characterized [14] Acetylcholineasterase inhibition with the acid level rosmarinic isolated from 12.8 to 13.5% after taking 550μmol / kg. [14]

Koleos securities forskohlii show (not usually be completed on behalf of containing many dietary supplements root) that have inhibitory properties of acetylcholine, because of rosmarinic acid content. And confirmed these effects in vivo


5. Interaction with obesity

5.1. Humanities

As for the human in vivo studies that show promise, but are limited in number and strength. Study of obese women and found that two doses of 250 mg extract 10% reduction in weight gain. [32] was not significant weight loss in the experimental group, but no significant difference between the experimental group (loss of light) and control (overweight). [32] In the men are overweight, and it seems that a single dose of positive changes in body composition over a period of 12 weeks. [33] testosterone increased bone mass and also in a range of Koleos forskohlii. Do not study to investigate weight changes observed mainly during the period of 2 months with 500-700mg forskohlii Koleos there was a decrease of 2.6% up to 2.38 in the body mass index. [3. 4]

There may be significant differences between human beings are obese and normal weight, obese since they have shown low enzyme activity flying aloft in fat cells, which partly corrects in weight loss by reducing calories. [35] In addition, men may be more benefits women, testosterone can serve as an agent to burn fat / muscle portfolio, although it is only one study has been conducted on men so far. [33]


5.2. Metabolic rate

A study of men are overweight who consumed 250mg of Koleos Forskohlii twice daily does not have a significant impact on increasing the metabolic rate. [33]



6. interact with skeletal muscle

6.1. The synthesis of muscle protein

Forskolin is able to increase adenylate flying activity in skeletal muscle. [36] by increasing the camp, and it has been suggested that forskolin can increase muscle protein synthesis through the activation of PI3K and AKT, independent of insulin receptors [37] and that this interaction is subject to allergies. [38]

Bio X4. Muscle contraction

Forskolin, in vitro at concentrations of 1 or has been shown, in order to increase muscle contraction and structure Alazemi- electical stimulation in rat diaphragm. Assumed [39] [40] and mechanims camp this increase levels of PKA activity that drives the work on the ryanodine receptor and increases the CA2 + efflux from the sarcoplasmic reticulum. [41]

Although there is biological plausibility, no studies have been conducted on the Koleos forskohlii and muscle contraction in vivo.


63. Food and muscle cells

Forskolin has been involved live in reducing the effects of insulin on mTOR Q / AKT in skeletal muscle. [42] Specifically, Forskolin appeared to limit the ability of insulin to phosphorylated AKT (AKT total vacuum) and similar results were observed when considering 4EBP1 with Q mTOR and S6K1 affected all transactions. [42]

Forskolin is also able to inhibit myocytes GLUT4 translocation in the laboratory, and to a lesser extent GLUT1. [43] This may also be downstream from the camp, as shown in the fat cells known as Camp negatively affect GLUT4 translocation through its promoter [44] [45] and also in muscle cells. [46]

As for the process of fat metabolism, / PKA in myocytes seems to activate the camp to improve fat metabolism, [47] and is one of the intersections of exercise and health in muscle cells. [48] ​​[49] [50] possibly through Myokine Myonectin call. [51]



7. interaction with heart health

7.1. blood pressure

forskohlii Koleos active compound Forskolin, Well relax the blood vessels and blood pressure or depression does not have an overall effect on blood pressure.

It seems to reduce blood pressure through the media cholinergic or histamine, [24] and provides a continuous drop in blood pressure in the body 0.1-1mg / kg in cats anathesized. More significant decline in those with high blood pressure core [24] Higher doses do not enhance the strength of low blood pressure, but rather to extend the time that can work; and in parallel with the effects of forskolin on intraocular pressure. [24]

This ability may be forskohlii vasorelaxant synergies with prostaglandin E1. [52]


7.2. Heart tissue

Forskolin is able to activate flying aloft in the heart muscle, and making a positive impact inotropic which can be useful for lack of heart. [53] This has been observed in vivo with a cat and a rabbit hearts. [24]

Bio X4 Peripheral Systems

8.1. Eyes

One study has checked in reducing the intraocular pressure (IOP) in human material forskolin as eye drops containing compound (1% solution 50 liter) [54] through its effects as an aphrodisiac cyclate aloft. [55] [56] It has been suggested that the role of forskolin in improving the retinal ganglion cell response (RGC) to stimulate BDNF, as BDNF refers through the camp in these cells [57] [58], but the increase in the levels of extracellular of highly effective BDNF in the renewal of these cells [59] but faced downregulation of TrkB receptors. [60] [61]

BDNF refers to the functions of the retina cells and growth factor used the camp as an intermediate in the course of its signals. It is believed the chronic exposure of BDNF and its simulators can reduce the expression of the future that stimulation of downstream (by forskolin) may have similar efficacy without the risk tolerance
Studies have been confused by mouth using forskolin with other vehicles. There was a decrease IOP with oral ingestion of Koleos forskohlii (200 mg of 10% forskolin) alongside of 200mg routine and a couple of vitamins B (thiamine and vitamin B2 to 550μg and 700 μg, respectively) in about 20% after 40 days in subjects with primary open-angle glaucoma (POAG) [1], while other studies using this formula to repeat their findings [2] seems effective when given in addition to standard therapy (topical), where more than one month extension reduces the IOP at a rate of 10%. [3]

Forskolin studies more than 40 days of finding durable solutions to be effective in reducing intraocular pressure when oral doses complementary. There is a need to conduct further studies using forskolin alone (as the above studies have confused) longer periods of time to evaluate and possibly correct the problem tolerance

8.2. Liver

Coleus forskohlii extract 0.5% of food intake in mice results in the induction of several enzyme systems in the liver, along with an increase in liver weight. It has been observed dose-dependent increase in copies Cyp2b10, Cyp2c29, Cyp3a11 and GSTM2. And seen [62] These changes after 1 week and stopped after stop eating Coleus. And it estimated the calories in 740 mg / kg of body weight daily Koleos; 24 mg total for mice. [62] and CYP2C induction is clinically relevant, because it is warfarin metabolizing enzyme.

forskolin isolated has a weaker incentive CYP3A enzymes and glutathione, and any increase in liver weight 0.05% of the diet. [62] This can be mediated induction transformational Bregnan X receptor, which is independent of its activities in the adenylate cyclase. [63]



9. interact with hormones

9.1. Testosterone

Intervention in men are overweight testosterone increase observed with 250 mg Koleos Forskohlii (10% Forskolin by weight) for 12 weeks. [33] Although there is no statistically significant differences in the basis (5.06 versus 4.12 +/- 1.21ng +/- 0.82 ng full test, 15.90 +/- 13.28 + 13.39pg T / 7.26pg came top in Group values) increases Koleos in 6 weeks and 12 weeks of Coleus, while there was no change in control; Free Test -. Total test rose 33.77% and 16.77 +/- 8.10 free trial +/- 3.47 after 12 weeks, with high interindividual variation. [33]

The mechanism is supposed to work by increasing the levels of camp within the testis, that mimic the action mechanisms of the hormone in the testes. [64] LH usually more than the same camp but avoid LH to increase the camp can increase the generation of steroid itself. [65] [66] and even some other research studies of herbs such as Cordyceps testicles forskolin used as a benchmark to compare the effectiveness of new drugs. [67]

Can extract Koleos also induce CYP3A4 in the liver, which in theory should lead to increased testosterone metabolism [62] However, no testosterone is measured in this study on mice; forskolin was isolated much smaller effect.


9.2. Insulin

Forskolin has been shown, in vitro, to be able to release insulin release (and glucagon and somatostatin) when incubated in the cells of the pancreas. [68]



10. interactions elements nutritious food

10.1. Beta-adrenergic agonists

It strengthens the effects of beta-adrenergic agonist isoproterenol, and appears to be highly effective for isoproterenol concentrations of 1 or up (which then noticed diminishing returns), showed [21] forskolin dose dependent increase in profits camp with isoproterenol.

In cases where the beta-adrenergic agonists do not encourage (hyporesponsiveness), low doses of forskolin able to rescue the effectiveness of beta-adrenergic receptors. [69] In addition, the 0.1 or forskolin (but not small concentrations) are able to save the beta-adrenergic sensitivity. [70]

This synergy has been observed in vivo using isoproterenol and forskolin through IV. [71]

Beta-adrenergic agonists on incluce synephrine, ephedrine, headlamp and ketone may berries. And the secretion of adrenaline self.


10.2. Methyl

Forskolin is harmonious with, such as methyl bromide has the ability to reduce the suppressive effect of adenosine levels in the camp is high in fat cells through as adenosine inhibitors. [72] [21] This combination of Forskolin and aminophylline methyl beyond synergistically with the addition of beta-adrenergic agonist, such as ephedrine.

Some methyl, such as caffeine and theophylline, as Vosfodestraz owns inhibition properties. PDE inhibition results in increased degradation and mitigate the camp forskolin does not affect PDE. [21] The combination of methyl and forskolin can increase production and alleviate the deterioration of the camp to strengthen cooperation in the laboratory.

Forskolin has also been shown to increase the sarcoplasmic calcium and load modules calcium tops sarcoplasmic network (via phospholambin) [73], which increases the ability of caffeine to induce calcium release. [74]

Bromide, including theophylline, theobromine and caffeine. These can be found in large quantities in tea, chocolate and coffee. Consecutive.


10.3. Alpha-adrenergic antagonists

When coincubated (in the cell at the same time), and transformational or insulin alpha-adrenergic agonists can prevent the increase seen camp forskolin. [75] Co-deductible and alpha-adrenergic agonist forskolin incubation can save some of the negative effects on the inhibition. [75]

Interestingly, sensitization cells (in this study, the cells of colon cancer) before incubation with alpha-adrenergic [75] agonist after exposure to agonist for more than 30 minutes, and the cells 20 times increases forskolin stimulated the camp for a short time (20-40 minutes). [75] [76]



11. The safety and toxicity

11.1. Public

It can cause Koleos Forskohlii supplements stomach acid levels increased, and can be a bad idea for those who are currently suffering from stomach ulcers. [77]

In cats, and it appears that LD50 68 mg / kg of body weight forskolin. [24]


11.2. Tolerance

Aortic cells normally increase the absorption of calcium in response to the camp, although it appears that incubation of 20 hours of 25μM forskolin can desensitize these cells to stimulate the camp despite the lack of sensitive adenylyl aloft, suggesting smelting adapt to another level. [78] Other cells have noted Harran level of protein synthesis, and can mimic by isoproterenol (β2-adrenergic agonist). [79]