|
Kavalactone
Kavalactones are a class of lactone compounds found in kava roots and ''Alpinia zerumbet'' (shell ginger) and in several Gymnopilus, Phellinus and Inonotus fungi. Some kavalactones are bioactive. They are responsible for the psychoactive, analgesic, euphoric and sedative effects of kava. Bioactivity Kava extract interacts with many pharmaceuticals and herbal medications. In human volunteers, in vivo inhibition includes CYP1A2 and CYP2E1 through use of probe drugs to measure inhibition. Research Its anxiolytic and hepatotoxic properties have been investigated. The major kavalactones (except for desmethoxyyangonin, desmethoxyyangonin) potentiate GABAA receptor, GABAA receptors, which may underlie the anxiolytic and sedative properties of kava. Further, Reuptake inhibitor, inhibition of the reuptake of norepinephrine, norepinephrine and dopamine, binding to the CB1 receptor, CB1 receptor, inhibition of voltage-gated sodium channel, sodium and voltage-gated calcium channel, calciu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kava
Kava or kava kava (''Piper methysticum'': Latin 'pepper' and Latinized Ancient Greek, Greek 'intoxicating') is a plant in the Piperaceae, pepper family, native to the Pacific Islands. The name ''kava'' is from Tongan language, Tongan and Marquesan language, Marquesan, meaning 'bitter'. Kava can refer to either the plant or a Psychoactive drug, psychoactive beverage made from its root. The beverage is a traditional ceremonial and recreational drink from Polynesia, Micronesia, and Melanesia. Nakamals and kava bar (establishment), bars exist in many countries. Traditional kava is made by grinding fresh or dried kava root, mixing it with water or coconut milk, and straining it into a communal bowl. Outside the South Pacific, kava is typically prepared by soaking dried root powder in water and straining it. It is Social lubricant, consumed socially for its sedative, hypnotic, muscle relaxant, anxiolytic, and euphoric effects, comparable to those produced by alcohol (drug), alcohol. K ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Yangonin
Yangonin is one of the six major kavalactones found in the kava plant. It acts as a selective agonist at the CB1 receptor, CB1 cannabinoid receptor, inhibits monoamine oxidase (particularly MAO-B), and modulates GABAA receptor activity. Yangonin significantly reduces nociception and inflammatory hyperalgesia via spinal CB1 receptors in rats, highlighting its potential as a promising treatment for pain. It is the strongest COX-II inhibitor among the six major kavalactones. Yangonin also exhibits neuroprotective, antifungal, and antimicrobial properties, though it has shown toxicity to human hepatocytes ''in vitro''. Pharmacology Yangonin has been shown to bind selectively to the cannabinoid receptor CB1 receptor, CB1, with a binding affinity (Ki) of 0.72 μM, and demonstrates low affinity for the CB2 receptor (Ki > 10 μM). It acts as an agonist at the CB1 receptor. This affinity suggests that the endocannabinoid system may play a role in the complex psychopharmacology, psychopharm ... [...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. It is a reversible inhibitor of monoamine oxidase B (MAO-B), likely contributing to increased dopamine levels in the brain’s nucleus accumbens and supporting kava’s attention-enhancing effects. Unlike other kavalactones, it does not modulate GABAA receptors. It also strongly induces the liver enzyme CYP3A23. It is an active compound in '' Alpinia pricei'' with anti-inflammatory and liver-protective effects that improve survival in mice with endotoxin-induced hepatitis. 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, desmethoxyyango ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpinia Zerumbet
''Alpinia zerumbet'', commonly known as shell ginger among other names, is a perennial species of ginger native to East Asia. The plants can grow up to tall and bear colorful funnel-shaped flowers. They are grown as ornamentals and their leaves are used in cuisine and traditional medicine. Names ''Alpinia zerumbet'' is called a "shell ginger" or "shell flower" most commonly, because its individual pink flowers, especially when in bud, resemble sea shells. Other common names in English include "pink porcelain lily", "variegated ginger, "butterfly ginger", and "light galangal". In Japan, ''A. zerumbet'' is called ''gettō'' () in standard Japanese. In the languages of the Ryukyu Islands, it is known as ''sannin'' () on Okinawa, ''shanin'' () on Tanegashima in the Ōsumi Islands, ''sa'nen'' () on Amami Ōshima, ''sani'' () on Okinoerabujima, ''samin'' () on Miyako-jima, ''samin'' (), ''sa'nin'' () and ''sami'' () on Ishigaki Island, ''sami'' () on Taketomi Island and ''sa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methysticin
Methysticin is one of the six major kavalactones found in the kava plant. It enhances the activity of the GABAA receptor, acting as a positive modulator without affecting the benzodiazepine binding site. This effect is attributed to structural features such as its angular lactone ring and is similar in strength to other kavalactones like kavain and dihydromethysticin. Methysticin also induces the liver enzyme CYP1A1, which plays a role in the toxification of benzo yrene into a highly carcinogenic metabolite, although such induction has not been observed in vivo in humans or animals. Additionally, methysticin is a mechanism-based inactivator of CYP2C9, irreversibly inhibiting the enzyme through NADPH-dependent reactive intermediates, suggesting potential interactions with medications metabolized by CYP2C9. Pharmacology It enhances the binding activity of the GABA_A receptor. Specifically, at a concentration of 0.1 micromolar, (+)-methysticin increases the binding of the receptor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enzyme
An enzyme () is a protein that acts as a biological catalyst by accelerating chemical reactions. The molecules upon which enzymes may act are called substrate (chemistry), substrates, and the enzyme converts the substrates into different molecules known as product (chemistry), products. Almost all metabolism, metabolic processes in the cell (biology), cell need enzyme catalysis in order to occur at rates fast enough to sustain life. Metabolic pathways depend upon enzymes to catalyze individual steps. The study of enzymes is called ''enzymology'' and the field of pseudoenzyme, pseudoenzyme analysis recognizes that during evolution, some enzymes have lost the ability to carry out biological catalysis, which is often reflected in their amino acid sequences and unusual 'pseudocatalytic' properties. Enzymes are known to catalyze more than 5,000 biochemical reaction types. Other biocatalysts include Ribozyme, catalytic RNA molecules, also called ribozymes. They are sometimes descr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabolism
Metabolism (, from ''metabolē'', "change") is the set of life-sustaining chemical reactions in organisms. The three main functions of metabolism are: the conversion of the energy in food to energy available to run cellular processes; the conversion of food to building blocks of proteins, lipids, nucleic acids, and some carbohydrates; and the elimination of metabolic wastes. These enzyme-catalyzed reactions allow organisms to grow and reproduce, maintain their Structures#Biological, structures, and respond to their environments. The word ''metabolism'' can also refer to the sum of all chemical reactions that occur in living organisms, including digestion and the transportation of substances into and between different cells, in which case the above described set of reactions within the cells is called intermediary (or intermediate) metabolism. Metabolic reactions may be categorized as ''catabolic''—the ''breaking down'' of compounds (for example, of glucose to pyruvate by c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cytochrome P450
Cytochromes P450 (P450s or CYPs) are a Protein superfamily, superfamily of enzymes containing heme as a cofactor (biochemistry), cofactor that mostly, but not exclusively, function as monooxygenases. However, they are not omnipresent; for example, they have not been found in ''Escherichia coli''. In mammals, these enzymes oxidize steroids, fatty acids, xenobiotics, and participate in many biosyntheses. By hydroxylation, CYP450 enzymes convert xenobiotics into hydrophilic derivatives, which are more readily excreted. P450s are, in general, the terminal oxidase enzymes in electron transfer chains, broadly categorized as P450-containing systems. The term "P450" is derived from the spectrophotometry, spectrophotometric peak at the wavelength of the absorption spectroscopy, absorption maximum of the enzyme (450 nanometre, nm) when it is in the redox, reduced state and complexed with carbon monoxide. Most P450s require a protein partner to deliver one or more electrons to reduc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hepatotoxicity
Hepatotoxicity (from ''hepatic toxicity'') implies chemical-driven liver damage. Drug-induced liver injury (DILI) is a cause of acute and chronic liver disease caused specifically by medications and the most common reason for a drug to be withdrawn from the market after approval. The liver plays a central role in transforming and clearing chemicals and is susceptible to the toxicity from these agents. Certain medicinal agents, when taken in overdoses (e.g. acetaminophen, paracetamol) and sometimes even when introduced within therapeutic ranges (e.g. halothane), may injure the organ. Other chemical agents, such as those used in laboratories and industries, natural chemicals (e.g., alpha-amanitin), and herbal remedies (two prominent examples being kava, though the causal mechanism is unknown, and comfrey, through pyrrolizidine alkaloid content) can also induce hepatotoxicity. Chemicals that cause liver injury are called hepatotoxins. More than 900 drugs have been implicated ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
