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Dihydromethysticin
Dihydromethysticin is one of the six major kavalactones found in the kava plant. Pharmacology Dihydromethysticin has marked activity on the induction of CYP3A23, as does the related chemical desmethoxyyangonin. Both dihydromethysticin and methysticin induce the hepatic enzyme CYP1A1, which increases the amount of the very highly carcinogenic benzo 'a''yrene-7,8-dihydrodiol-9,10-epoxide in the body (via the metabolism of benzo 'a''yrene) and may be responsible for some of the toxic effects associated with kava consumption. ''In vitro'', dihydromethysticin possesses analgesic, anticonvulsant, and anxiolytic effects. It has been found to act as a GABAA receptor positive allosteric modulator and as an reversible inhibitor of monoamine oxidase B Monoamine oxidase B, also known as MAOB, is an enzyme that in humans is encoded by the ''MAOB'' gene. The protein encoded by this gene belongs to the flavin monoamine oxidase family. It is an enzyme located in the outer mitochondrial ... [...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] |
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] |
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] |
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] |
Kavalactone
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 gr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
C15H16O5
The molecular formula C15H16O5 (molar mass: 276.28 g/mol, exact mass: 276.099774 u) may refer to: * Dihydromethysticin, a kavalactone found in the kava plant * Lactucin, a bitter sesquiterpene lactone found in lettuce * Vernolepin, a sesquiterpene lactone found in ''Vernonia amygdalina'' {{molFormDisambig Molecular formulas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and an innate response of the body to the environmental stimuli. Mild to moderate anxiety would increase level of performance. However, when anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses such as defensive behaviors, high levels of alertness and negative emotions, without external stimuli which induce anxiety within an individual. Those with anxiety disorders are also often found to have concurrent psychological disorders, most commonly depression. Anxiety disorders are divided into 6 types in clinical recognition. They are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cytochrome P450 Inhibitors
Cytochromes are redox-active proteins containing a heme, with a central Fe atom at its core, as a cofactor. They are involved in electron transport chain and redox catalysis. They are classified according to the type of heme and its mode of binding. Four varieties are recognized by the International Union of Biochemistry and Molecular Biology (IUBMB), cytochromes a, cytochromes b, cytochromes c and cytochrome d. Cytochrome function is linked to the reversible redox change from ferrous (Fe(II)) to the ferric (Fe(III)) oxidation state of the iron found in the heme core. In addition to the classification by the IUBMB into four cytochrome classes, several additional classifications such as cytochrome o and cytochrome P450 can be found in biochemical literature. History Cytochromes were initially described in 1884 by Charles Alexander MacMunn as respiratory pigments (myohematin or histohematin). In the 1920s, Keilin rediscovered these respiratory pigments and named them the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Oxidase B
Monoamine oxidase B, also known as MAOB, is an enzyme that in humans is encoded by the ''MAOB'' gene. The protein encoded by this gene belongs to the flavin monoamine oxidase family. It is an enzyme located in the outer mitochondrial membrane. It catalyzes the oxidative deamination of biogenic and xenobiotic amines and plays an important role in the catabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (such as dopamine). This protein preferentially degrades benzylamine and phenethylamine. Similarly to monoamine oxidase A (MAOA), it also degrades dopamine hough some new research contradicts this, suggesting that MAOB does ''not'' directly degrade dopamine, but is responsible for GABA synthesis Structure Monoamine oxidase B has a hydrophobic bipartite elongated cavity that (for the "open" conformation) occupies a combined volume close to 700 Å3. hMAO-A has a single cavity that exhibits a rounder shape and is larger in volume t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enzyme Inhibitor
An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which substrate molecules are converted into products. An enzyme facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the most difficult step of the reaction. An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. Enzyme inhibitors may bind reversibly or irreversibly. Irreversible inhibitors form a chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. By contrast, reversible inhibitors bind non-covalently and may spontaneously leave the enzyme, allowing the enzyme to resume its function. Reve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Positive Allosteric Modulator
In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimulus. Some of them, like benzodiazepines, are drugs. The site that an allosteric modulator binds to (i.e., an ''allosteric site'') is not the same one to which an endogenous agonist of the receptor would bind (i.e., an ''orthosteric site''). Modulators and agonists can both be called receptor ligands. Allosteric modulators can be 1 of 3 types either: positive, negative or neutral. Positive types increase the response of the receptor by increasing the probability that an agonist will bind to a receptor (i.e. affinity), increasing its ability to activate the receptor (i.e. efficacy), or both. Negative types decrease the agonist affinity and/or efficacy. Neutral types don't affect agonist activity but can stop other modulators from binding to an allosteric site. Some modulators also work as allosteric agonists. The term "allosteric" derive ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAA Receptor
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Upon opening, the GABAA receptor on the postsynaptic cell is selectively permeable to chloride ions (Cl−) and, to a lesser extent, bicarbonate ions (HCO3−). Depending on the membrane potential and the ionic concentration difference, this can result in ionic fluxes across the pore. If the membrane potential is higher than the equilibrium potential (also known as the reversal potential) for chloride ions, when the receptor is activated Cl− will flow into the cell. This causes an inhibitory effect on neurotransmission by diminishing the chance of a successful action potential occurring at the postsynaptic cell. The reversal potential of the GABAA-mediated inhibitory postsynaptic potential (IPSP) in normal solution is −70 mV, contrasting the GABAB IPSP (-100 mV). T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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