Product Description Product Name: Griffonia Seed Extract
Botanical Name: Griffonia simplicifolia (Vahl ex DC) Baill
Part Used: Seed
Classification: Plant / Herb Extracts
Extract Solvent: Water
Assay: 5-Hydroxytryptophan not less than 98,0 % (HPLC)
L-5-Hydroxytryptophan (5-HTP) is a natural extract from the seeds of the Griffonia simplicifolia tree found principally in the West African countries of Ghana, Ivory Coast and Togo. Traditional African uses for the plant include the use of the stem and roots as chewing sticks, leaves to aid in the healing of wounds, whilst the leaf juice is used as an enema and for the treatment of kidney ailments. A decoction of the steams and leaves is also used to stop vomiting, to treat congestion of the pelvis and as an aphrodisiac. The bark-pulp is applied as a plaster to soft chancres.
From the 1960’s chemical investigations on Griffonia simplicifolia seed resulted in the detection and isolation of several indole derivatives including 5-hydroxy-L-tryptophan, indole-3-acetylaspartic acid and 5-hyrdroxy indole-3-acetic acid (5-HIAA). Research also showed 5-HTP to possess antidepressant activity. 5-HTP was found to be more effective than the tricyclic synthetic drugs which were considered the standard of care at that time. As a consequence during the 1980’s a number of medicinal specialities containing 5-HTP as the active ingredient were registered and launched on the market.
Mechanisms of Action:5-HTP acts primarily by increasing levels of serotonin within the central nervous system. Other neurotransmitters and CNS chemicals, such as melatonin, dopamine, nor-epinephrine, and beta-endorphin have also been shown to increase following oral administration of 5-HTP. This ability to increase not only serotonin levels in the brain, but also dopamine and norepinephrine, allows 5-HTP to produce some significant and unique effects on brain chemistry and on serotonin-related conditions which other substances, including LT, cannot duplicate.
5-Hydroxy-L-tryptophan
Clinical Studies Using 5-HTP:
Depression: Much of the published research on 5-HTP has to do with its use in the treatment of depression. Since the early 1970s, at least 15 studies have evaluated the clinical effects of 5-HTP on depression. These are summarized these studies examined a total of 511 patients with different types of depression. Of these 511 subjects, 285 (56%) showed significant improvement while taking 5-HTP.
In addition, biochemical studies show 5-HTP is closely involved in depressive disorders. In a study employing positron-emission tomography (PET) scanning, eight healthy volunteers and six people diagnosed with major depression received infusions of radiolabelled 5-HTP. The researchers found significantly less 5-HTP crossed the blood-brain barrier into the brains of the depressed subjects than into the brains of the normal controls. The authors suggested the transport of 5-HTP across the blood-brain barrier may be compromised in major depression, which might make the brain dependent on LT to 5-HTP conversion in the brain.
The first large clinical trial using 5-HTP in depression was conducted by Sano in 1972. Using an open trial design, a total of 107 patients with endogenous unipolar or bipolar depression were given daily oral dosages of 5-HTP from 50 to 300 mg. Significant improvement was observed in 74 of the patients (69%), and no significant side effects were reported. The response rate in most of these patients was quite rapid (less than two weeks).
The issue of speed of response was subsequently addressed in a study of 59 patients with eight different types of depression. 5-HTP was administered orally in dosages from 150 to 300 mg daily for a period of three weeks. Thirteen patients (22%) were markedly improved, and another 27 patients (45.8%) showed moderate improvement. Of these 40 patients who improved, 20 (50%) began to show improvement within three days, and 32 patients (80%) improved within two weeks of beginning treatment with 5-HTP.15 In contrast to many conventional antidepressants which may take 4 weeks or longer to achieve therapeutic response in most patients, those taking 5-HTP appear to have a significantly more rapid response.
Japanese researchers administered 5-HTP to 24 patients hospitalized for depression. After two weeks of treatment, a "marked amelioration of depressive symptoms" was observed in seven patients diagnosed with unipolar depression. The administration of 5-HTP was also associated with a 30 percent increase in the levels of 5-hydroxyindolacetic acid, the primary metabolite of serotonin, in the patients' cerebrospinal fluid. This suggested the exogenous 5-HTP was being converted to serotonin within the CNS.
Fibromyalgia: Primary fibromyalgia syndrome is characterized by general musculo-skeletal aching, multiple tender points, fatigue, morning stiffness, and sleep disturbances. Fibromyalgia patients have been found to have low serotonin and tryptophan levels, and some studies have shown symptomatic improvement with the use of tricyclic and SSRI antidepressants. These findings suggest 5-HTP might be useful in the treatment of fibromyalgia, and three clinical trials have demonstrated significant improvement in symptoms, including pain, morning stiffness, anxiety, and fatigue.
Caruso et al conducted a double-blind, placebo-controlled study in 50 fibromyalgia patients, administering 100 mg of 5-HTP three times daily for a period of 30 days. Significant improvements were seen in number of tender points (p<0.001), subjective pain severity (p<0.001), morning stiffness (p=0.017), sleep patterns (p<0.001), anxiety ratings (p<0.001), and fatigue ratings (p=0.003). The incidence of side effects in the 5-HTP group was low (6/25 patients), and no significant laboratory abnormalities were reported during the study.
In a longer-term study, a total of 50 patients diagnosed with primary fibromyalgia syndrome were given 100 mg 5-HTP three times per day for 90 days in an open study. Patients were assessed at the beginning of the study and after 15, 30, 60, and 90 days of treatment. The clinical variables evaluated included: total number of tender points, pain intensity, sleep quality, morning stiffness, anxiety, and fatigue. All of these measures showed significant improvement throughout the length of the study (p<0.001). A total of 15 patients (30%) reported side effects from the 5-HTP, but in only one case were they severe enough for the patient to be withdrawn from the study.
In a randomized, placebo-controlled study of 200 fibromyalgia patients who were also migraine sufferers, 5-HTP (400 mg/day) was compared to a tricyclic drug (amitriptyline) and a monoamine oxidase inhibitor (MAOI) drug (pargilyne or phenelzine). The combination of 5-HTP (200 mg/day) with an MAOI was also evaluated. Patients were treated for a total of 12 months and kept a daily pain diary by means of a visual analogic scale. At the end of the twelve-month trial period, all treatment regimens showed significant improvement over placebo (p<0.0001), although the combination of 5-HTP with the MAOI was the most effective. 5-HTP alone was as effective as the tricyclic or MAOI drugs. No patients withdrew from the study due to side effects; eight percent of the patients taking 5-HTP alone reported some degree of stomach upset.
Obesity: During dieting, serum tryptophan levels and CNS serotonin levels drop dramatically.These low serotonin levels in obese patients have been associated with carbohydrate cravings and resultant binge eating. It has been theorized that 5-HTP can help prevent this dieting-associated decline in serotonin, thus enhancing weight loss. Three clinical trials in obese patients have demonstrated decreased food intake and subsequent weight loss with 5-HTP supplementation.
Using a placebo-controlled, double-blind protocol, researchers at the University of Rome evaluated the effects of 5-HTP (300 mg three times daily) on the eating habits and weight loss of 20 obese female patients. All patients had a body mass index between 30 and 40, and were determined to consume an excess of food daily, based on calculated energy needs. The twelve-week study period was divided into two six-week sections. During the first six weeks, the patients took either 5-HTP or placebo, but no dietary restrictions were placed on them. In the second six-week period, the patients were placed on a 1200 calorie per day diet, while continuing to take either the 5-HTP or placebo. Subjects compiled detailed 3-day food diaries once every two weeks.
Those in the placebo group did not experience significant weight loss in either of the two periods (94.3 ± 5.6 kg vs. 93.2 ± 5.3 kg ), while the subjects in the 5-HTP group showed significant weight loss in both the first period (99.7 ± 5.9 kg vs. 98.0 ± 5.0 kg, p<0.03) and the second period (98.0 ± 5.0 vs. 94.7 ± 5.1 kg, p<0.02). The placebo group also did not show significant change in their calorie intake, even in the second period when instructed to reduce food intake, while the 5-HTP group had a significant spontaneous dietary intake reduction during the first period, from 3220 calories/day to 1879 calories/day (p<0.001), with carbohydrate intake falling by 50 percent. During the second period, the calorie intake of the 5-HTP group decreased further, to 1268 calories/day (p<0.01), with further reductions in carbohydrates. The researchers interpreted these findings as supporting the theory that 5-HTP decreased carbohydrate cravings and binge eating, even in the absence of a structured diet.
At this high dosage of 5-HTP (900 mg/day), about 80 percent of the subjects initially reported experiencing some nausea. However, this side effect was not severe enough to cause any of the subjects to drop out of the study, and was less frequent during the second six-week period, suggesting that this symptom may be a transitory effect of 5-HTP administration.
Chronic Headaches: Chronic headaches, especially migraines, are considered by some researchers to be the result of low serotonin levels, probably as the result of increased breakdown of serotonin by the enzyme monoamine oxidase. Low serotonin levels are thought to lower pain thresholds in chronic headache sufferers, allowing other headache triggers to more easily "set off" a headache.
5-HTP has been used successfully in the prevention of chronic headaches of various types, including migraine, tension headaches, and juvenile headaches. In a large study of 124 subjects, the ability of 5-HTP to prevent migraines was compared to methysergide, one of the most commonly used migraine drugs. At a dosage of 600 mg daily for six months, 5-HTP totally prevented or substantially decreased the number of migraine attacks in 75 percent of the subjects. However, this difference was not determined to be statistically significant. In a study of 48 elementary and junior high school students, 5-HTP (4.5 mg/kg/day) produced a 70 percent decrease in headache frequency, compared to an 11 percent decrease in the placebo group.
Insomnia: 5-HTP has been shown to be beneficial in treating insomnia, especially in improving sleep quality by increasing REM sleep. Eight normal subjects were monitored to determine the effect of 5-HTP on rapid eye movement (REM) sleep. A total of 600 mg 5-HTP was administered to the subjects in the following manner: 200 mg at 9:15 pm, followed by 400 mg at 11:15 pm. A significant increase in the amount of REM sleep was observed while the subjects were taking 5-HTP (118 ± 14 mins vs. 98 ± 11 mins, p<0.005). A smaller study using a 200 mg dose also showed increases in REM sleep, but to a lesser degree. The smaller dose is probably preferable, since, according to anecdotal reports, higher doses may have a tendency to cause very vivid dreams or nightmares.
Dosage: Initial dosage for 5-HTP is usually 50 mg three times per day with meals. If the clinical response is inadequate after two weeks, dosage may be increased to 100 mg three times per day. For insomnia, the dosage is usually 100-300 mg before bedtime. Because some patients may experience mild nausea when initiating treatment with 5-HTP, it is advisable to begin with 50 mg doses and titrate upward.
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