Mesembrenone
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Mesembrenone
Mesembrenone is an alkaloid constituent of ''Sceletium tortuosum'' (Kanna) and minor constituent of Lampranthus aureus and Lampranthus spectabilis Similar to modern synthetic antidepressants, it is a potent (IC50 < 1 μM) selective inhibitor of the (SERT) (that is, a ; Ki = 27 nM) and also a (PDE4)

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Sceletium Tortuosum
Sceletium tortuosum is a succulent plant commonly found in South Africa, which is also known as Kanna, Channa, Kougoed (Kauwgoed/ 'kougoed', prepared from 'fermenting' ''S. tortuosum'')—which literally means, 'chew(able) things' or 'something to chew'. The generally recognised eight ''Sceletium'' species are ''S. crassicaule'', ''S. emarcidum'', ''S. exalatum'', ''S. expansum'', ''S. rigidum'', ''S. strictum'', ''S. tortuosum'' and ''S. varians''. Per Klak et al. (2007), an alternative classification for the ''Sceletium'' group is ''Mesembryanthemum crassicaule'', ''M. emarcidum'', ''M. exalatum'', ''M. expansum'', ''M. archeri'' (''S. rigidum''), ''M. ladismithiense'' (''S. strictum''), ''M. tortuosum'' and ''M. varians''. History The plant has been used by South African pastoralists and hunter-gatherers as a mood-altering substance from prehistoric times. The first known written account of the plant's use was in 1662 by Jan van Riebeeck. The traditionally prepared drie ...
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Phosphodiesterase-4 Inhibitor
A phosphodiesterase-4 inhibitor, commonly referred to as a PDE4 inhibitor, is a drug used to block the degradative action of phosphodiesterase 4 (PDE4) on cyclic adenosine monophosphate (cAMP). It is a member of the larger family of Phosphodiesterase inhibitor, PDE inhibitors. The PDE4 family of enzymes are the most prevalent PDE in immune cells. They are predominantly responsible for hydrolyzing cAMP within both immune cells and cells in the central nervous system. Therapeutic utility The prototypical PDE4 inhibitor is rolipram. PDE4 inhibitors are known to possess procognitive (including long term memory-improving), wakefulness-promoting, neuroprotective, and anti-inflammatory effects. Consequently, PDE4 inhibitors have been investigated as treatments for a diverse group of different diseases, including central nervous system disorders such as major depressive disorder (clinical depression), anxiety disorders, schizophrenia, Parkinson's disease, Alzheimer's disease, multiple scl ...
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Alkaloid
Alkaloids are a class of basic, naturally occurring organic compounds that contain at least one nitrogen atom. This group also includes some related compounds with neutral and even weakly acidic properties. Some synthetic compounds of similar structure may also be termed alkaloids. In addition to carbon, hydrogen and nitrogen, alkaloids may also contain oxygen, sulfur and, more rarely, other elements such as chlorine, bromine, and phosphorus.Chemical Encyclopedia: alkaloids
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Alkaloids are produced by a large variety of organisms including , , Medicinal plant, plants, an ...
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Lampranthus
''Lampranthus'' is a genus of succulent plants in the family Aizoaceae, indigenous to southern Africa. Description The genus name ''"Lampranthus"'' means ''"shining-flowers"'' in Greek, and the species of this genus have unusually large, bright flowers, of a range of colours (sometimes even bi-coloured), that usually appear in summer, and frequently cover the plants entirely. The species of this genus typically have long, smooth, elongated, succulent leaves. These can be triangular or cylindrical, and like all plants in its family, appear in opposite pairs on the shrubs' branches. ''Lampranthus'' can be clearly distinguished from related genera by its seed capsules. The seed capsules of all of these genera have triangular valves, which open when they become wet, exposing the seed chambers ( locules). In contrast to '' Ruschia'', each valve in a ''Lampranthus'' capsule has two wings, on either side of it, but no visible closing body. Unlike in ''Delosperma'', the seeds in ''Lam ...
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Antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, headaches, sexual dysfunction, and emotional blunting. There is a slight increased risk of suicidal thinking and behavior when taken by children, adolescents, and young adults. Discontinuation syndrome may occur after stopping any antidepressant which resembles recurrent depression. Some research regarding the effectiveness of antidepressants for depression in adults has found benefits, whilst other research has not. Evidence of benefit in children and adolescents is unclear. The twenty-one most commonly prescribed antidepressant medications are more effective than placebo for the short-term (acute) treatments of adults with major depressive disorder. There is debate in the medical community about how much of the observed effects of antidep ...
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Serotonin Transporter
The serotonin transporter (SERT or 5-HTT) also known as the sodium-dependent serotonin transporter and solute carrier family 6 member 4 is a protein that in humans is encoded by the SLC6A4 gene. SERT is a type of monoamine transporter protein that transports the neurotransmitter serotonin from the synaptic cleft back to the presynaptic neuron, in a process known as serotonin reuptake. This transport of serotonin by the SERT protein terminates the action of serotonin and recycles it in a sodium-dependent manner. Many antidepressant medications of the SSRI and tricyclic antidepressant classes work by binding to SERT and thus reducing serotonin reuptake. It is a member of the sodium:neurotransmitter symporter family. A repeat length polymorphism in the promoter of this gene has been shown to affect the rate of serotonin uptake and may play a role in sudden infant death syndrome, aggressive behavior in Alzheimer disease patients, post-traumatic stress disorder and depression-suscepti ...
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Selective Serotonin Reuptake Inhibitor
Selective serotonin reuptake inhibitors (SSRIs) are a class of drugs that are typically used as antidepressants in the treatment of major depressive disorder, anxiety disorders, and other psychological conditions. SSRIs increase the extracellular level of the neurotransmitter serotonin by limiting its reabsorption (reuptake) into the presynaptic cell. They have varying degrees of selectivity for the other monoamine transporters, with pure SSRIs having strong affinity for the serotonin transporter and only weak affinity for the norepinephrine and dopamine transporters. SSRIs are the most widely prescribed antidepressants in many countries. The efficacy of SSRIs in mild or moderate cases of depression has been disputed and may or may not be outweighed by side effects, especially in adolescent populations. Medical uses The main indication for SSRIs is major depressive disorder; however, they are frequently prescribed for anxiety disorders, such as social anxiety disorder, ge ...
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Phosphodiesterase 4
At least four types of the enzyme phosphodiesterase 4 (PDE4) are known: * PDE4A * PDE4B * PDE4C * PDE4D See also * 3',5'-cyclic-AMP phosphodiesterase * Phosphodiesterase (PDE) * PDE4 inhibitor A phosphodiesterase-4 inhibitor, commonly referred to as a PDE4 inhibitor, is a drug used to block the degradative action of phosphodiesterase 4 (PDE4) on cyclic adenosine monophosphate (cAMP). It is a member of the larger family of PDE inhibitor ... {{chemistry index Molecular biology ...
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Functional Food
A functional food is a food claimed to have an additional (often one related to health promotion or disease prevention) by adding new ingredients or more of existing ingredients. The term may also apply to traits purposely bred into existing edible plants, such as purple or gold potatoes having increased anthocyanin or carotenoid contents, respectively. Functional foods may be "designed to have physiological benefits and/or reduce the risk of chronic disease beyond basic nutritional functions, and may be similar in appearance to conventional food and consumed as part of a regular diet". The term was first used in the 1980s in Japan, where there is a government approval process for functional foods called Foods for Specified Health Use (FOSHU). Industry The functional food industry, consisting of food, beverage and supplement sectors, is one of the several areas of the food industry that is experiencing fast growth in recent years.Roberts, W. "Benefiting Beverages." ''Prepared ...
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Mesembrine
Mesembrine is an alkaloid present in ''Sceletium tortuosum'' (kanna). It has been shown to act as a serotonin reuptake inhibitor (Ki = 1.4 nM), and more recently, has also been found to behave as a weak inhibitor of the enzyme phosphodiesterase 4 (PDE4) (Ki = 7,800 nM). Still more recently, in an in vitro study published in 2015, scientist concluded that "a high-mesembrine Sceletium extract exerts its anti-depressant effect by acting primarily as monoamine releasing agent, rather than as selective serotonin-reuptake inhibitor." As such, mesembrine likely plays a dominant role in the antidepressant effects of kanna. The levorotatory isomer, (−)-mesembrine, is the natural form. Rat studies have evaluated effects of kanna extract, finding analgesic and antidepressant potential. No adverse results were noted for a commercial extract up to 5000 mg/kg daily in rats. Mesembrine has also been identified in Mesembryanthemum cordifolium, Delosperma ech ...
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Serotonin
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets and is ...
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PDE4 Inhibitors
At least four types of the enzyme phosphodiesterase 4 (PDE4) are known: * PDE4A * PDE4B * PDE4C * PDE4D See also * 3',5'-cyclic-AMP phosphodiesterase * Phosphodiesterase (PDE) * PDE4 inhibitor A phosphodiesterase-4 inhibitor, commonly referred to as a PDE4 inhibitor, is a drug used to block the degradative action of phosphodiesterase 4 (PDE4) on cyclic adenosine monophosphate (cAMP). It is a member of the larger family of PDE inhibitor ... {{chemistry index Molecular biology ...
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