Clinical application of 5-hydroxytryptophan

 People in West Africa have used the Griffoniasimplicifolia plant since ancient times as a treatment for diseases. The leaves and its juice are used to treat wounds and kidney diseases. 



They are also used as enemas and aphrodisiacs: the mashed bark can be used as an ointment for chancroid. Wait. Its main active ingredient is 5-hydroxytryptophan (5-hydroxytryptophan), which is a natural aromatic amino acid Griffoniasimplicifolia. The 5-hydroxytryptophan content in the seeds is as high as 10-12%. 


Further research on modern medicine has shown that 5-hydroxytryptophan also has a variety of obvious pharmacological effects, such as: regulating mood, treating depression, reducing aggression in patients; shortening the time to fall asleep, improving sleep quality; reducing appetite, treating obesity; treating fiber Myalgia Syndrome; Relief of Chronic Headache Symptoms, etc. 


5-Hydroxytryptophan has been widely used in the pharmaceutical and health food industries. At present, the extraction and preparation process of 5-hydroxytryptophan mostly adopts: slag pressing or petroleum ether deoiling → water/solvent extraction → activated carbon decolorization → filtration → concentration → recrystallization. Since raw seeds contain more than 35% of fat-soluble substances (fat and fat-soluble pigments, etc.). 


The general pressing method not only cannot effectively remove oils and pigments, but also the slag cake after pressing is extremely inconvenient for subsequent pulverization, thus greatly affecting the subsequent extraction and separation effect; 


the use of organic solvent degreasing method not only has low degreasing rate, slow speed, The cost is high, and it has the disadvantages of being unsafe in production and unfriendly to the environment. In addition, the extract usually contains a lot of impurities such as water-soluble macromolecular pigments, sugar, protein and pectin. 


These impurities are not only difficult to control with general methods such as activated carbon decolorization and impurity removal, but also the product loss is serious. Therefore, the recovery rate of the final product using the above process route is generally only 40-45%, the product cost is high, and the raw material waste is large.


Physiological effect

5-Hydroxytryptamine is a hormone secreted by the human brain, which can affect people's mood, sleep and appetite. 

Too low content can lead to depression, anxiety and sleep disorders. 5-Hydroxytryptophan is a precursor to serotonin, which aids in the production of this hormone in the human brain. 


5-Hydroxytryptophan is needed to keep the body in a normal state when there is an imbalance of serotonin in the brain. Taking 5-hydroxytryptophan can be converted into serotonin in the body, but serotonin is a large molecule and cannot enter the brain through the blood-brain barrier, so 5-hydroxytryptophan must first pass through the blood-brain barrier, and then enter the brain. 


Partly converted into serotonin, can really play a role in stabilizing mood and promoting sleep quality. In animal and human experiments, 5-hydroxytryptophan can promote the metabolism of catecholamines, especially dopamine and norepinephrine, which are other "happy" neurotransmitters. 


Clinical studies have also found that taking 5-hydroxytryptophan can significantly improve the mood of patients with depression; in addition, 5-hydroxytryptophan can also promote sleep quality and improve mild insomnia. 


There is also clinical research evidence that 5-hydroxytryptophan has analgesic effects, can improve the discomfort of some patients with fibromyalgia, and also has a role in the improvement of chronic pressure headaches. 


Taking 5-hydroxytryptophan will reduce the frequency of frequent headaches and increase the concentration of enkephalins in the body. Enkephalins are naturally secreted by the human body to relieve pain and happiness. 


The concentration of enkephalins increases, which can make the human body feel comfortable and happy.


In addition, the eating test of overeating rats found that 5-hydroxytryptophan can increase the blood concentration of leptin (leptin), improve appetite control, and avoid overeating. 


A clinical study of 19 obese women found that taking 5 mg of 5-hydroxytryptophan per kilogram of body weight per day, without a dietary prescription, resulted in an average weight loss of 5% after 5 weeks, similar to The results were also reported in other longer and non-insulin-dependent diabetic patients, so 5-hydroxytryptophan could indeed be used to aid appetite control in obese people.


Clinical application

5-Hydroxytryptophan is involved in various activities in the human body, and human depression, sleep, appetite and pain are all related to it. The clinical application of 5-hydroxytryptophan is also becoming more and more mature, and its status in the medical field has attracted more and more attention. 


5-Hydroxytryptophan is available in pure natural herbal formulations, mainly in the form of capsules, tablets and powders. 5-Hydroxytryptophan has been widely used in major pharmaceutical and health care product companies at home and abroad. In foreign countries, antidepressant drugs were launched in Europe in the early 1980s; melatonin health products such as "melatonin" in the domestic market were also converted from 5-hydroxytryptophan. 


The main clinical applications of 5-hydroxytryptophan are as follows.


1. Antidepressants, tranquilizers]


Serotonin is a hormone secreted by the brain, which can affect people's mood, sleep and appetite. Too low levels can lead to depression, anxiety and sleep disorders. 


5-Hydroxytryptophan can increase the production of serotonin in brain cells, thereby increasing its content, which is helpful for normal nerve and brain function. 


5-Hydroxytryptophan antidepressant and selective serum reuptake inhibitor (SSRI) have similar effects, but SSRI antidepressant prescription drugs (such as fluoxetine, etc.) are more expensive and often cause side effects such as dry mouth, anxiety and loss of libido . 


It can be said that 5-hydroxytryptophan is the best substitute for antidepressant prescription drugs, and it has been widely used as an over-the-counter drug in many foreign countries.


2. Pain relief


Serotonin is abundant in mammalian cerebral cortex and synapses. In peripheral tissues, serotonin is a strong vasoconstrictor and a stimulator of smooth muscle contraction. People with chronic headaches are generally deficient in serotonin. Some researchers refer to migraines and chronic headaches as "low serotonin syndrome." 


5-Hydroxytryptophan is effective in relieving the frequency and severity of headaches, including chronic headaches, tension headaches, and migraine attacks.


3. Reduce stress and improve sleep


5-Hydroxytryptophan has also been successfully used to treat sleep disorders. Conventional wisdom holds that because serotonin is a precursor to melatonin, a natural hormone that regulates sleep and wake cycles, when serotonin levels increase, so do melatonin levels, making sleep more sweet . 


However, at the "2013 NPC Natural and Nutritional Health Products China Exhibition", Swanson, a well-known American health care product manufacturer, said that the latest findings confirmed that the product to help sleep is 5-hydroxytryptophan rather than melatonin.


4. Lose weight


5-Hydroxytryptophan can improve the sensitivity of the dietary center and effectively control appetite. It can reduce hunger in the diet control of the weight loss process, make the weight loss process easier and easier, and is a currently popular weight loss food supplement. 


It has been marketed as a dietary supplement for weight loss in developed countries such as the United States.


5. Others


5-Hydroxytryptophan can also be used for the treatment of BH4-deficiency phenylketonuria, and it can also be used for adjuvant treatment of attention-deficit children. Due to the lack of thorough research on 5-hydroxytryptophan, the possible side effects and drug cross-effects are not yet clear. 


Although there are no reports of serious adverse reactions, diarrhea and vomiting are the main causes of diarrhea due to the rapid formation of serotonin in the upper intestinal tract. more common adverse reactions. 


5-Hydroxytryptophan has been reported to cause eosinophilic myalgia syndrome (EMS) in a more severe form, resulting in extreme muscle tenderness, myalgia, and blood abnormalities. 


Subsequent evidence suggested that EMS was caused by contaminants incorporated into the tryptophan process, the raw material for the production of 5-hydroxytryptophan. In addition, the reported drug cross-actions are as follows: when combined with monoamine oxidase inhibitors or SSRI antidepressants, 5-hydroxytryptophan can cause acute hydroxytryptamine syndrome; 


when combined with carbidopa (eg, used in the symptomatic treatment of Parkinson's disease), 5-hydroxytryptophan can cause nausea and vomiting, which can be relieved by taking granisetron.

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