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Kavalactones
Kavalactones are a class of lactone compounds found in kava roots and Alpinia zerumbet (Shell ginger). Kavalactones are under research for potential to have various psychotropic effects, including anxiolytic and sedative/hypnotic activities. Enzyme inhibition Kava extract has been shown in vitro to potentially inhibit a wide range of hepatic enzymes, suggesting a possible potential for interactions with many pharmaceuticals and herbal medications. In human volunteers in vivo inhibition is currently limited to CYP1A2, and CYP2E1 through use of probe drugs to measure inhibition. Research Several preliminary studies are assessing potential effects of kava, including its anxiolytic actions and hepatotoxicity, but the role specifically of kavalactones among many other kava compounds for these effects remains under study. Kavalactone type compounds may help protect against high glucose induced cell damage. Toxicity Several kavalactones (e.g. methysticin and yangonin) affect a group ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kava
Kava or kava kava (''Piper methysticum'': Latin 'pepper' and Latinized Greek 'intoxicating') is a crop of the Pacific Islands. The name ''kava'' is from Tongan and Marquesan, meaning 'bitter'; other names for kava include ''ʻawa'' (Hawaiʻi), ''ʻava'' (Samoa), ''yaqona'' or ''yagona'' (Fiji), ''sakau'' (Pohnpei), ''seka'' (Kosrae), and ''malok'' or ''malogu'' (parts of Vanuatu). Kava is consumed for its sedating effects throughout the Pacific Ocean cultures of Polynesia, including Hawaii and Vanuatu, Melanesia, some parts of Micronesia, such as Pohnpei and Kosrae, and the Philippines. The root of the plant is used to produce a drink with sedative, anesthetic, and euphoriant properties. Its active ingredients are called kavalactones. A systematic review done by the British nonprofit Cochrane concluded it was likely to be more effective than placebo at treating short-term anxiety. Moderate consumption of kava in its traditional form, i.e., as a water-based suspension of kav ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Desmethoxyyangonin
Desmethoxyyangonin or 5,6-dehydrokavain is one of the six main kavalactones found in the ''Piper methysticum'' (kava) plant. Pharmacology Desmethoxyyangonin is a reversible inhibitor of monoamine oxidase B (MAO-B). Kava is able to increase dopamine levels in the nucleus accumbens and desmethoxyyangonin likely contributes to this effect. This, along with several other catecholamines, may be responsible for the purported attention-promoting effects of kava. Unlike the other major kavalactones, desmethoxyyangonin does not appear to act as a GABAA receptor positive allosteric modulator. Desmethoxyyangonin has marked activity on the induction of CYP3A23. See also *Kavain Kavain is the main kavalactone found mostly in the roots of the kava plant. Pharmacology Kavain has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent and channels. How this ef ... References {{Dopaminergics Monoamine oxidase inhibitors ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kavain
Kavain is the main kavalactone found mostly in the roots of the kava plant. Pharmacology Kavain has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent and channels. How this effect is mediated and to what extent this mechanism is involved in the anxiolytic and analgesic effects of kavalactones on the central nervous system is unknown. The recent finding that kavain can reversibly inhibit both monoamine oxidase A and monoamine oxidase B suggests that kavain may exert some of its effects by modulating serotonin, norepinephrine, and dopamine signaling. However, the precise mechanisms underlying the psychotropic, sedative, and anxiolytic actions of kavain and related kavalactones are still debated. Direct binding to the benzodiazepine/flumazenil binding site of the GABA-A receptor does not occur with kavain enantiomers. Many studies involved kava extracts from different plant parts and are, therefore, not applica ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Yangonin
Yangonin is one of the six major kavalactones found in the kava plant. It has been shown to possess binding affinity for the cannabinoid receptor CB1 (Ki = 0.72 μM), and selectivity vs. the CB2 receptor (Ki >10 μM) where it behaves as an agonist. The CB1 receptor affinity of yangonin suggests that the endocannabinoid system might contribute to the complex human psychopharmacology of the traditional kava drink and the anxiolytic preparations obtained from the kava plant. Like other kavalactones, yangonin has been found to potentiate GABAA receptors. This may contribute to the anxiolytic properties of yangonin and kava as a whole. Further '' in vitro'' studies have also demonstrated yangonin to be an inhibitor of monoamine oxidase, with a moderate preference for isozyme B, which could open the door to a wide range of interactions. Toxicity Yangonin displays marked ''in vitro'' toxicity on human hepatocytes with approximately 40% reduction in viability based on an ethid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methysticin
Methysticin is one of the six major kavalactones found in the kava plant. Research suggests that methysticin and the related compound dihydromethysticin have CYP1A1 inducing effects which may be responsible for their toxicity. Additionally, methysticin has been shown to potentiate GABAA receptor activity, contributing to the overall anxiolytic profile of the kava plant. Toxicity Methysticin induces the function of the hepatic enzyme CYP1A1. This enzyme is involved in the toxification Toxication, toxification or toxicity exaltation is the conversion of a chemical compound into a more toxic form in living organisms or in substrates such as soil or water. The conversion can be caused by enzymatic metabolism in the organisms, as we ... of benzo 'a''yrene into (+)-benzo 'a''yrene-7,8-dihydrodiol-9,10-epoxide, a highly carcinogenic substance. Another related compound is dihydromethysticin, which also induces the function of CYP1A1. No report so far has described enhancement of CYP ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Yangonin
Yangonin is one of the six major kavalactones found in the kava plant. It has been shown to possess binding affinity for the cannabinoid receptor CB1 (Ki = 0.72 μM), and selectivity vs. the CB2 receptor (Ki >10 μM) where it behaves as an agonist. The CB1 receptor affinity of yangonin suggests that the endocannabinoid system might contribute to the complex human psychopharmacology of the traditional kava drink and the anxiolytic preparations obtained from the kava plant. Like other kavalactones, yangonin has been found to potentiate GABAA receptors. This may contribute to the anxiolytic properties of yangonin and kava as a whole. Further '' in vitro'' studies have also demonstrated yangonin to be an inhibitor of monoamine oxidase, with a moderate preference for isozyme B, which could open the door to a wide range of interactions. Toxicity Yangonin displays marked ''in vitro'' toxicity on human hepatocytes with approximately 40% reduction in viability based on an ethid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
10-methoxyyangonin
1 (one, unit, unity) is a number representing a single or the only entity. 1 is also a numerical digit and represents a single unit of counting or measurement. For example, a line segment of ''unit length'' is a line segment of length 1. In conventions of sign where zero is considered neither positive nor negative, 1 is the first and smallest positive integer. It is also sometimes considered the first of the infinite sequence of natural numbers, followed by 2, although by other definitions 1 is the second natural number, following 0. The fundamental mathematical property of 1 is to be a multiplicative identity, meaning that any number multiplied by 1 equals the same number. Most if not all properties of 1 can be deduced from this. In advanced mathematics, a multiplicative identity is often denoted 1, even if it is not a number. 1 is by convention not considered a prime number; this was not universally accepted until the mid-20th century. Additionally, 1 is the s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Elimination Half-life
Biological half-life (also known as elimination half-life, pharmacologic half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration ( Cmax) to half of Cmax in the blood plasma, and is denoted by the abbreviation t_. This is used to measure the removal of things such as metabolites, drugs, and signalling molecules from the body. Typically, the biological half-life refers to the body's natural cleansing through the function of the liver and through the excretion of the measured substance through the kidneys and intestines. This concept is used when the rate of removal is roughly exponential. In a medical context, half-life explicitly describes the time it takes for the blood plasma concentration of a substance to halve (''plasma half-life'') its steady-state when circulating in the full blood of an organism. This measurement is useful in medicine, pharmacology and pharmacokinetics because it helps det ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
