Agathadiol, a labdane diterpenoid from juniper berries, is a positive allosteric modulator of CB1R

Stefano Salamone; Giovanni Appendino; Adil Khalili; Federica Pollastro; Eduardo Munoz; Juan D. Unciti-Broceta

doi:10.1016/j.fitote.2021.105059

Agathadiol, a labdane diterpenoid from juniper berries, is a positive allosteric modulator of CB₁R

Stefano Salamone
, Giovanni Appendino
, Adil Khalili
, Federica Pollastro
, Eduardo Munoz
, Juan D. Unciti-Broceta

Research output: Contribution to journal › Article › peer-review

Abstract

The neutral fraction of a juniper (Juniperus communis L.) berries acetone extract could positively modulate the activity of type 1 - cannabinoid receptor (CB₁R). Bioactivity-directed fractionation identified the labdane diterpenoid agathadiol (4) as a positive allosteric modulator of CB₁R, while closely related analogues were inactive. Agathadiol (4) is a minor constituent of juniper, but could be more conveniently obtained by semisynthesis from agathic acid (8), a major constituent of Manila copal.

Original language	English
Article number	105059
Journal	Fitoterapia
Volume	155
DOIs	https://doi.org/10.1016/j.fitote.2021.105059
Publication status	Published - Nov 2021
Externally published	Yes

Keywords

Agathadiol
Allosteric ligands
Cannabinoid receptor-1
Juniperus communis
Labdane diterpenoids

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10.1016/j.fitote.2021.105059

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title = "Agathadiol, a labdane diterpenoid from juniper berries, is a positive allosteric modulator of CB1R",

abstract = "The neutral fraction of a juniper (Juniperus communis L.) berries acetone extract could positively modulate the activity of type 1 - cannabinoid receptor (CB1R). Bioactivity-directed fractionation identified the labdane diterpenoid agathadiol (4) as a positive allosteric modulator of CB1R, while closely related analogues were inactive. Agathadiol (4) is a minor constituent of juniper, but could be more conveniently obtained by semisynthesis from agathic acid (8), a major constituent of Manila copal.",

keywords = "Agathadiol, Allosteric ligands, Cannabinoid receptor-1, Juniperus communis, Labdane diterpenoids",

author = "Stefano Salamone and Giovanni Appendino and Adil Khalili and Federica Pollastro and Eduardo Munoz and Unciti-Broceta, \{Juan D.\}",

note = "Publisher Copyright: {\textcopyright} 2021",

year = "2021",

month = nov,

doi = "10.1016/j.fitote.2021.105059",

language = "English",

volume = "155",

journal = "Fitoterapia",

issn = "0367-326X",

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TY - JOUR

T1 - Agathadiol, a labdane diterpenoid from juniper berries, is a positive allosteric modulator of CB1R

AU - Salamone, Stefano

AU - Appendino, Giovanni

AU - Khalili, Adil

AU - Pollastro, Federica

AU - Munoz, Eduardo

AU - Unciti-Broceta, Juan D.

PY - 2021/11

Y1 - 2021/11

N2 - The neutral fraction of a juniper (Juniperus communis L.) berries acetone extract could positively modulate the activity of type 1 - cannabinoid receptor (CB1R). Bioactivity-directed fractionation identified the labdane diterpenoid agathadiol (4) as a positive allosteric modulator of CB1R, while closely related analogues were inactive. Agathadiol (4) is a minor constituent of juniper, but could be more conveniently obtained by semisynthesis from agathic acid (8), a major constituent of Manila copal.

AB - The neutral fraction of a juniper (Juniperus communis L.) berries acetone extract could positively modulate the activity of type 1 - cannabinoid receptor (CB1R). Bioactivity-directed fractionation identified the labdane diterpenoid agathadiol (4) as a positive allosteric modulator of CB1R, while closely related analogues were inactive. Agathadiol (4) is a minor constituent of juniper, but could be more conveniently obtained by semisynthesis from agathic acid (8), a major constituent of Manila copal.

KW - Agathadiol

KW - Allosteric ligands

KW - Cannabinoid receptor-1

KW - Juniperus communis

KW - Labdane diterpenoids

UR - https://www.scopus.com/pages/publications/85117707318

U2 - 10.1016/j.fitote.2021.105059

DO - 10.1016/j.fitote.2021.105059

M3 - Article

SN - 0367-326X

VL - 155

JO - Fitoterapia

JF - Fitoterapia

M1 - 105059

ER -

Agathadiol, a labdane diterpenoid from juniper berries, is a positive allosteric modulator of CB₁R

Abstract

Keywords

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