Kavalactone
Kavalactones are a class of lactone compounds mainly contained in the kava kava plant (Piper methysticum). In addition, they can also be found in the plant Alpinia Zerumbet [1]. This class of compounds is the reason for the psychoactive properties of kava, which Europe learned about in the 18th century [2]. I first learned information about this plant from the works of the American chemist Alexander Shulgin, who was one of the pioneers in the study of the properties of this plant.
There are 6 main kavalactones in total:
- Kavain, 7,8-dihydrokavain
- Methylsticin
- 7,8-dihydromethystycin
- Yangonin
- Desmethoxyangonin.
Properties
The active compounds have been studied for their analgesic properties. When administered orally, kavaine and dihydrokavaine show the shortest absorption time, the peak of the effect reaching a maximum of 10 minutes after consumption. Methysticin and dihydromethysticin are stronger, but the maximum effect is not seen until 45 minutes after ingestion. Together, these substances have a synergistic effect [3]. In addition to the analgesic properties, antifungal and anticonvulsant effects were also found in a 1973 study by Alexander Shulgin.
But what does modern science tell us about kava? Scientists have shown that the main effect of kavalactones comes from the fact that they are ligands of GABA-A receptors [4, 5, 6]. However, a 2007 study suggests that GABA is not limited to GABA alone. It turned out to be. In a 2012 article, staff from the Italian National Research Council showed that one of the kava compounds, yangonin, is a CB-1 ligand of the endocannabinoid receptor (not as strong as THC, but still). However, it is worth noting that this work was done only in vitro, so more research is needed to confirm that psychoactive cannabimimetic effects occur in humans as well. In practice, people consume about 10 times as much yangonin as has been studied at one time, so still the effects on CB-1 can be considered quite plausible [7]. Another interesting thing is that kavalactones are MAO inhibitors comparable in potency to curcumin, which was chosen as the reference in the study [8]. This may explain their activity against depression.
Applications
In addition to recreational use, kava has established itself as a medicinal agent. While there have been some uncertainties in studies on the mechanism of action of this alkaloid, there is already some interesting and confirmed information in studies of the effects of kava kava on certain diseases. As you noticed in the previous section, kavalactones have anti-anxiety effects. Why not use this for a real disease that comes with anxiety? The earliest work I found dates back to 2009. It shows that kava extract is a safe and effective treatment for depression and generalized anxiety disorder (when consumed no more than 250 mg of kavalactones per day) [9]. Subsequent studies (including a double-blind, placebo-controlled study) have confirmed the therapeutic efficacy of this plant, with mentions that this efficacy is comparable to that of buspirone and opipramol [10, 11, 12].
Restrictions
Despite the positive properties of kava, there are also negative effects of this plant. Since some kavalactones are MAO inhibitors, they cannot be used together with antidepressants because of the risk of serotonin syndrome, which can be fatal. Also, kava should not be consumed together with cheese, as there is a risk of tyramine syndrome. In addition, kavalactones are bad for the liver. In rare cases, kava extract can have a strong hepatotoxic effect [13, 14, 15]. Cultivars recommended for traditional use contain fewer flavokavines that are toxic to the liver. Collection of roots from plants younger than 5 years old is not recommended.
Traditional use
Alexander Shulgin reports that kava was used as a stimulating drink that was a normal part of social life, like coffee in our culture. During the ceremony, people crossed their legs in front of them and sat in an intoxicated state. Two methods of making the drink are well documented [16].
Tonga Method
Using this method, people first chewed the roots of the plant so as to crush it, while avoiding saliva contact with the pulp as much as possible and avoiding swallowing it. Next, the chewed material was soaked in water and infused. After that, the liquid was decanted and was ready for consumption. The person chewing the plant experienced numbness of the tongue and a prolonged loss of taste. The description of the effects after consumption was similar to a strong alcoholic intoxication.
However, missionaries forbade this method because of its unhygienic nature. The most important part of the ritual is adding water to the mass. The finished drink is served to each person individually, calling everyone by name; in Samoa special names are used for this purpose, which are not used outside of this ceremony. After receiving the drink, the person claps his hands and spills a small amount of kava to the gods and then drinks the rest.
Fiji Method
This procedure is more common nowadays. It involves the mechanical grinding of the root, during which it is moistened with water. The resulting mush is then infused in water. When using this method, the psychoactive effects are felt less, with tonic and anti-anxiety effects predominating. Shulgin suggests that saliva enzymes may cause a transformation of the active substances of kava kava, which would contribute to the psychoactive effects described when using the method used in the kingdom of Tonga.
Conclusion
Despite all the attractiveness of kavalactones and kava, it is not easy to buy the root of this plant. In some states and countries in Europe, intoxicating peppers are listed as highly potent and poisonous substances, which consequently prohibits their use in dietary supplements. However, you can quite legally go to the ceremony of kava on the islands of Fiji, where it will be held in accordance with all traditions.
But what does modern science tell us about kava? Scientists have shown that the main effect of kavalactones comes from the fact that they are ligands of GABA-A receptors [4, 5, 6]. However, a 2007 study suggests that GABA is not limited to GABA alone. It turned out to be. In a 2012 article, staff from the Italian National Research Council showed that one of the kava compounds, yangonin, is a CB-1 ligand of the endocannabinoid receptor (not as strong as THC, but still). However, it is worth noting that this work was done only in vitro, so more research is needed to confirm that psychoactive cannabimimetic effects occur in humans as well. In practice, people consume about 10 times as much yangonin as has been studied at one time, so still the effects on CB-1 can be considered quite plausible [7]. Another interesting thing is that kavalactones are MAO inhibitors comparable in potency to curcumin, which was chosen as the reference in the study [8]. This may explain their activity against depression.
Applications
In addition to recreational use, kava has established itself as a medicinal agent. While there have been some uncertainties in studies on the mechanism of action of this alkaloid, there is already some interesting and confirmed information in studies of the effects of kava kava on certain diseases. As you noticed in the previous section, kavalactones have anti-anxiety effects. Why not use this for a real disease that comes with anxiety? The earliest work I found dates back to 2009. It shows that kava extract is a safe and effective treatment for depression and generalized anxiety disorder (when consumed no more than 250 mg of kavalactones per day) [9]. Subsequent studies (including a double-blind, placebo-controlled study) have confirmed the therapeutic efficacy of this plant, with mentions that this efficacy is comparable to that of buspirone and opipramol [10, 11, 12].
Restrictions
Despite the positive properties of kava, there are also negative effects of this plant. Since some kavalactones are MAO inhibitors, they cannot be used together with antidepressants because of the risk of serotonin syndrome, which can be fatal. Also, kava should not be consumed together with cheese, as there is a risk of tyramine syndrome. In addition, kavalactones are bad for the liver. In rare cases, kava extract can have a strong hepatotoxic effect [13, 14, 15]. Cultivars recommended for traditional use contain fewer flavokavines that are toxic to the liver. Collection of roots from plants younger than 5 years old is not recommended.
Traditional use
Alexander Shulgin reports that kava was used as a stimulating drink that was a normal part of social life, like coffee in our culture. During the ceremony, people crossed their legs in front of them and sat in an intoxicated state. Two methods of making the drink are well documented [16].
Tonga Method
Using this method, people first chewed the roots of the plant so as to crush it, while avoiding saliva contact with the pulp as much as possible and avoiding swallowing it. Next, the chewed material was soaked in water and infused. After that, the liquid was decanted and was ready for consumption. The person chewing the plant experienced numbness of the tongue and a prolonged loss of taste. The description of the effects after consumption was similar to a strong alcoholic intoxication.
However, missionaries forbade this method because of its unhygienic nature. The most important part of the ritual is adding water to the mass. The finished drink is served to each person individually, calling everyone by name; in Samoa special names are used for this purpose, which are not used outside of this ceremony. After receiving the drink, the person claps his hands and spills a small amount of kava to the gods and then drinks the rest.
Fiji Method
This procedure is more common nowadays. It involves the mechanical grinding of the root, during which it is moistened with water. The resulting mush is then infused in water. When using this method, the psychoactive effects are felt less, with tonic and anti-anxiety effects predominating. Shulgin suggests that saliva enzymes may cause a transformation of the active substances of kava kava, which would contribute to the psychoactive effects described when using the method used in the kingdom of Tonga.
Conclusion
Despite all the attractiveness of kavalactones and kava, it is not easy to buy the root of this plant. In some states and countries in Europe, intoxicating peppers are listed as highly potent and poisonous substances, which consequently prohibits their use in dietary supplements. However, you can quite legally go to the ceremony of kava on the islands of Fiji, where it will be held in accordance with all traditions.
Albizia Julibrissin
The first part of the scientific name, Albizia, comes from the Florentine Filippo del Albizzi, who introduced the plant to Europe in 1745. The species epithet, julibrissin, is a distortion of gul-i abrisham, which means "silk flower" in Farsi. Its leaves slowly close at night and when it rains, the leaves bend downward; thus, its modern Persian name "shabkhosb" means "night sleep. This tendency also explains the common Chinese name "hehuan," which means "happy shutter" and symbolizes a happy couple in bed. The common names in Japan are nemunoki, nemurinoki and nenenoki, which means "sleeping tree. The nemu tree is a partial translation of the word nemunoki.
A. julibrissin is widely grown as an ornamental plant in parks and gardens because of its beautifully textured leaves, flowers and attractive horizontal crown. It is often planted in semi-arid areas such as California's Central Valley, central Texas and Oklahoma.
The wide crown of the adult tree allows for mottled shade. Flower colors range from white to rich yellow with red tips. Variants with cream or pale yellow flowers are also reported.
Using
This plant is used in Asian countries as a stand-alone drug to treat insomnia, as well as in combination with other plants. It is actively in demand. For example, in 2002 in Taiwan, this plant was part of a combination of three medicinal herbs prescribed for patients suffering from insomnia [17]. Either the bark or the flowers of the tree in dried form are most often used to make the dosage form.Three substances are thought to be responsible for the plant's sedative effects:
- Quercitrin
- Isoquercitrin
- Julibroside C1
However, despite the desired sedative effect, the use of the plant may be limited by the fact that its bark contains cytotoxic saponins [21, 22], which, however, may find their use in leukemia therapy because of their activation of caspase-3 [23].
Anadenanthera peregrina
Anadenanthera peregrina, commonly known as yopo or cohoba, is a perennial tree belonging to the Fabaceae family. Indigenous to the tropical regions of South America, particularly the Orinoco River Basin and the Caribbean, this plant has captivated the attention of researchers and enthusiasts alike due to its potent psychoactive effects. The seeds of A. peregrina contain a rich array of alkaloids, including bufotenin, dimethyltryptamine (DMT), and 5-MeO-DMT, which are responsible for its mind-altering properties. Throughout history, various indigenous cultures have utilized this plant for spiritual, medicinal, and recreational purposes, highlighting its cultural significance and versatility.
Botanical Description and growth patterns
Anadenanthera peregrina is a medium-sized tree, typically reaching heights of 15 to 20 meters. Its bark is smooth and grayish, while the leaves are bipinnate, with small, elliptical leaflets. The tree produces fragrant, cream-colored flowers that give way to elongated, woody seed pods. Each pod contains numerous reddish-brown seeds, which are the primary source of the plant's psychoactive compounds.
A. peregrina thrives in tropical and subtropical climates, with a preference for well-drained soils and ample sunlight. The tree is resilient and can tolerate a range of environmental conditions, including periodic flooding and drought. Its natural distribution spans from Venezuela and Colombia to the southern regions of Brazil and Paraguay.
Traditional uses and cultural significance
The use of Anadenanthera peregrina dates back to pre-Columbian times, with archaeological evidence suggesting its consumption by indigenous cultures such as the Taino, Carib, and Yanomami. The seeds were traditionally ground into a fine powder, which was then mixed with a calcined substance, such as snail shells or plant ashes, to create a snuff called yopo or cohoba. This mixture was typically administered through the nostrils using specialized inhalation devices, such as bone or wooden tubes.
The psychoactive effects of A. peregrina were highly valued in ritualistic and shamanic contexts, as they were believed to facilitate communication with the spirit world and promote healing. Additionally, the plant was occasionally employed for recreational purposes, with users seeking its euphoric and hallucinogenic properties.
Psychoactive effects and active constituents
The seeds of Anadenanthera peregrina contain a complex mixture of tryptamine alkaloids, including bufotenin, DMT, and 5-MeO-DMT. These compounds act as agonists at the 5-HT2A receptor, eliciting a range of psychoactive effects that can include visual and auditory hallucinations, altered perception of time and space, euphoria, and heightened introspection.
The intensity and duration of the experience depend on various factors, such as the method of administration, individual sensitivity, and the presence of other alkaloids or additives. Generally, the effects of A. peregrina are characterized by a rapid onset, peaking within 15 to 30 minutes, and subsiding after 1 to 2 hours.
Preparation, consumption, and dosage
To harness the psychoactive properties of Anadenanthera peregrina, the seeds must be properly prepared and consumed. Traditional methods involve grinding the seeds into a fine powder and combining them with a calcined substance to facilitate absorption and reduce potential harm to the nasal mucosa. Modern adaptations may include the extraction and purification of the active alkaloids, which can then be vaporized or ingested orally.
Dosage is a critical factor in determining the intensity and safety of the A. peregrina experience. A typical starting dose for the snuff form ranges from 3 to 5 seeds per nostril, with experienced users sometimes opting for higher amounts. For extracted alkaloids, the dosage should be adjusted accordingly, taking into account the purity and potency of the preparation.
Conclusion
Anadenanthera peregrina is a remarkable plant with a rich history and a diverse array of psychoactive effects. Its unique combination of botanical, cultural, and pharmacological attributes make it a fascinating subject for further research and exploration. By understanding and respecting the traditional uses and practices surrounding A. peregrina, we can gain valuable insights into the plant's potential applications and contributions to the field of ethnobotany.