CORDOBA, Spain, June 22, 2018 /PRNewswire/ -- Phytoplant
Research S.L. participated in a first-ever pioneering collaborative
project to investigate the ability of cannabinoid cannabigerol
(CBG), the molecular precursor of Δ9-tetrahydrocannabinol (Δ 9-THC)
and cannabidiol (CBD). The study investigated the ability of the
above to modulate the affinity and functionality of type-1 and
type-2 cannabinoid receptors (CB1 and CB2,
respectively) and CB1–CB2 heteroreceptor
complexes. It concluded that CBG significantly modulates
CB2R- and CB1R/CB2R-mediated
endocannabinoid action, while the effects are weak in
CB1R-expressing cells.
The results of this research, published in the journal
Frontiers in Pharmacology, show that CBG, a non-psychotropic
phytocannabinoid, at nanomolar concentrations, is capable of acting
as a competitive partial agonist of the CB2R. Regarding
its action on CB1R, it is not possible to rule out a
potential allosteric action, since the blocking of intracellular
signalling of CB1R agonists occurs at concentrations of
CBG lower than those necessary for its binding to the orthostatic
site of the receptor.
These findings reopen the discussion about the ability of other
phytocannabinoids, whose mechanism of action was unknown, to bind
directly to cannabinoid receptors as Δ 9-THC does. In
the study, researchers obtained results using different approaches
that include the classic radioligand ligand binding, new
fluorescent-based binding techniques and the measurement of
signalling pathways. In these assays, CBG was able to modify the
affinity and activity of selective CB1R and
CB2R agonists at concentrations with physiological
relevance (nanomolar).
The results also suggest that the partial agonism on the
CB2R is regulated by the presence of the
CB1R. However, more complex alternative scenarios cannot
be ruled out as CBG may act on the orthosteric site of the
CB1R protomer and as protean agonist of the CB1R
protomer within the CB1R/CB2R heteromer.
The Molecular Neurobiology Laboratory at the University of Barcelona, directed by Rafael Franco, is a pioneer in Europe in the research of the biochemical,
pharmacological and functional aspects of G protein-coupled
receptors (GPCRs), including cannabinoid receptors, as well as
the expression and differential function of cannabinoid receptors
during neurodegeneration. One of its main achievements has been the
characterization of these receptors as possible therapeutic targets
for the design and development of new drugs to treat diseases that
affect the central nervous system.
"Natural compounds present in Cannabis sativa L. and
acting on cannabinoid receptors are guiding the search for novel
drugs to combat neurodegenerative diseases," said Professor
Rafael Franco of the Department of
Biochemistry and Molecular Biomedicine of the University of Barcelona.
"With these findings, we demonstrate clearly that CBG is active
at the cannabinoid receptors CB1 and CB2 and that it exerts its
effects through those receptors. We have deepened the knowledge
about phytocannabinoids and reopened the discussion about the
interaction between the Cannabis plant compounds," said Dr.
Xavier Nadal, Director of the R
& D - Extraction Department at Phytoplant Research
S.L.
The results of the study indicate that CBG is indeed effective
as a regulator of endocannabinoid signalling and may exert
beneficial actions with therapeutic potential via cannabinoid
receptors.
About the University of
Barcelona:
The Molecular Neurobiology Laboratory directed by Prof.
Rafael Franco belongs to the
Department of Biochemistry and Molecular Biomedicine at the
University of Barcelona, which is the
Spanish institution with the highest score in biomedical research
rankings. His research activity is devoted to deciphering the
structure and function of GPCRs and their association into
heteroreceptor complexes, with the aim of identifying therapeutic
targets to combat various neurodegenerative diseases, especially
Parkinson's and Alzheimer's disease. Among GPCR research,
cannabinoid receptors are very challenging due to the lipidic
nature of endocannabinoids. Through a variety of technological
strategies, the group has been able to discover allosteric binding
sites in these receptors and get insight into their pharmacology,
specially that related to cannabis components.
Media Contact:
Name: Rafael Franco
Phone: +34 610 30 61 23
Email: 197610@email4pr.com
About the University of Ferrara:
The Cellular and Molecular Pharmacology Laboratory of the
University of Ferrara, directed by Prof. Katia Varani, focuses on research on
ligand-receptor interaction. The group focuses on identifying new
pharmacological targets related to different pathologies such as
neurodegenerative disorders, chronic inflammatory diseases,
ischemia and cancer. It has at its disposal the most advanced
instruments to study the cellular and molecular mechanisms of
pathogenicity and its modulation by means of a receptor-based
approach. For several years, the research group has also
specialized in functional and binding assays for the evaluation of
the affinity, selectivity and potency of new candidate ligands, for
GPCRs in particular.
About Phytoplant Research S.L:
Phytoplant Research SL is a Spanish private company founded in
2008 dedicated to conducting research in herbal medicine. It
specializes in the development of the industrial chain of medicinal
plants, from the selection and breeding, to the registration and
cultivation of varieties and obtaining derived products. The
company focuses on R&D products that contain plant material and
extracts, as well as essential oils and oils from seeds. These
products represent a relevant economic potential for the
pharmaceutical, nutraceutical and dermocosmetic industries. They
also guarantee the industrial supply of raw materials of
phyto-pharmaceutical quality through the cultivation of medicinal
plants and the extraction of plant material, with the aim of
isolating, purifying and manufacturing naturally active ingredients
(psychoactive and non-psychoactive), semi-synthetic,
biotransformed, pharmaceutically acceptable salts and
derivatives.
More information about the company is available here.
Media Contact:
Name: Stefan Martin Meyer
Phone: (0034) 957 10 16 29
Email: 197610@email4pr.com
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SOURCE Phytoplant Research SL