Mesembrenone is an
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 ...
constituent of ''
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 ...
'' (Kanna) and minor constituent of
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 ...
aureus and Lampranthus spectabilis
Similar to modern synthetic
antidepressants
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, heada ...
, it is a potent (IC
50 < 1 μM) selective inhibitor of the
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 tha ...
(SERT) (that is, a
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 extracell ...
; K
i = 27 nM) and also a
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 ...
(PDE4)
inhibitor
Inhibitor or inhibition may refer to:
In biology
* Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity
* Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotra ...
(K
i = 470 nM).
See also
*
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 phosp ...
another alkaloid constituent of Kanna.
References
{{Reflist
Serotonin
PDE4 inhibitors
Alkaloids