alkaloid
Alkaloids are a broad class of natural product, naturally occurring organic compounds that contain at least one nitrogen atom. Some synthetic compounds of similar structure may also be termed alkaloids.
Alkaloids are produced by a large varie ...
found within the plants ''
Nymphaea caerulea
''Nymphaea nouchali'' var. ''caerulea'', is a water lily in the genus '' Nymphaea'', a botanical variety of '' Nymphaea nouchali''.
It is an aquatic plant of freshwater lakes, pools and rivers, naturally found throughout most of the eastern h ...
'' and ''
Nelumbo nucifera
''Nelumbo nucifera'', also known as the pink lotus, sacred lotus, Indian lotus, or simply lotus, is one of two extant taxon, extant species of aquatic plant in the Family (biology), family Nelumbonaceae. It is sometimes colloquially called a ...
''.
Preliminary psychopharmacological research in 1978 was unable to conclusively determine the compound's classification regarding dopamine-receptor activity. On one hand, investigative studies found evidence of behavior traditionally associated with ''dopamine-receptor'' ''stimulation'': stereotypy, increase in spontaneous motor activity, inhibition of conditioned avoidance response, and an increase in pain sensitivity resulting in an inhibition of morphine analgesia. On the other hand, these early investigative studies also found evidence of behavior traditionally associated with ''dopamine-receptor'' ''blockade'': decrease of spontaneous motor activity, chills, catalepsy, trance-like states of consciousness.
Nuciferine exhibits a receptor profile similar to atypical
antipsychotics
Antipsychotics, previously known as neuroleptics and major tranquilizers, are a class of psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizo ...
, demonstrating antipsychotic-like effects in rodent models without inducing catalepsy.
Pharmacology
Nuciferine has been reported to have various
anti-inflammatory
Anti-inflammatory is the property of a substance or treatment that reduces inflammation, fever or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs reduce pain by inhibiting mechan ...
effects, possibly mediated via PPAR delta activation.
According to a newer study from 2016, Nuciferine acts as an
antagonist
An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.5-HT2A, 5-HT2C, and 5-HT2B receptors, an
inverse agonist
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.
A neutral antagonist has no activity in the absence of an agonist or inverse agon ...
partial agonist
In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (bio ...
agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
at 5-HT1A and D4 receptors. Additionally, it inhibits the dopamine transporter ( DAT).
In rodent models relating to antipsychotic drug effects, Nuciferine has shown various actions such as blocking head-twitch responses and discriminative stimulus effects of a 5-HT2A agonist, enhancing amphetamine-induced locomotor activity, inhibiting
phencyclidine
Phencyclidine or phenylcyclohexyl piperidine (PCP), also known in its use as a street drug as angel dust among other names, is a dissociative anesthetic mainly used recreationally for its significant mind-altering effects. PCP may cause hall ...
( PCP)-induced locomotor activity, and restoring PCP-induced disruption of pre-pulse inhibition without inducing
catalepsy
Catalepsy (from Ancient Greek , , "seizing, grasping") is a neurological condition characterized by muscular rigidity and fixity of posture regardless of external stimuli, as well as decreased sensitivity to pain.
Signs and symptoms
Sympt ...
.
Nuciferine may also potentiate
morphine
Morphine, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are ...
analgesia
Pain management is an aspect of medicine and health care involving relief of pain (pain relief, analgesia, pain control) in various dimensions, from acute and simple to chronic and challenging. Most physicians and other health professionals ...
. The
median lethal dose
In toxicology, the median lethal dose, LD50 (abbreviation for " lethal dose, 50%"), LC50 (lethal concentration, 50%) or LCt50 is a toxic unit that measures the lethal dose of a given substance. The value of LD50 for a substance is the dose re ...
in mice is 289 mg/kg. It is structurally related to
apomorphine
Apomorphine, sold under the brand name Apokyn among others, is a type of aporphine having activity as a non- selective dopamine agonist which activates both D2-like and, to a much lesser extent, D1-like receptors. It also acts as an antago ...
and other
aporphine
Aporphine is an alkaloid with the chemical formula . It is the core chemical substructure of the aporphine alkaloids, a subclass of quinoline alkaloids. It can exist in either of two enantiomeric forms, (''R'')-aporphine and (''S'')-aporphine.
...
derivatives.Spess, David L. Errors in Alkaloids of Nelumbo and Nymphaea species, 2011, academia.edu