Efficient Synthesis for Altering Side Chain Length on Cannabinoid Molecules and Their Effects in Chemotherapy and Chemotherapeutic Induced Neuropathic Pain

Biomolecules. 2022 Dec 13;12(12):1869. doi: 10.3390/biom12121869.

Abstract

(1) Background: Recently, a number of side chain length variants for tetrahydrocannabinol and cannabidiol have been identified in cannabis; however, the precursor to these molecules would be based upon cannabigerol (CBG). Because CBG, and its side chain variants, are rapidly converted to other cannabinoids in the plant, there are typically only small amounts in plant extracts, thus prohibiting investigations related to CBG and CBG variant therapeutic effects. (2) Methods: To overcome this, we developed an efficient synthesis of corresponding resorcinol fragments using the Wittig reaction which, under acid catalyzed coupling with geraniol, produced the desired side chain variants of CBG. These compounds were then tested in an animal model of chemotherapeutic-induced neuropathic pain and to reduce colorectal cancer cell viability. (3) Results: We found that all side-chain variants were similarly capable of reducing neuropathic pain in mice at a dose of 10 mg/kg. However, the molecules with shorter side chains (i.e., CBGV and CBGB) were better at reducing colorectal cancer cell viability. (4) Conclusions: The novel synthesis method developed here will be of utility for studying other side chain derivatives of minor cannabinoids such as cannabichromene, cannabinol, and cannabielsoin.

Keywords: cannabigerol; cannabinoid synthesis; colorectal cancer; neuropathic pain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cannabinoids* / pharmacology
  • Cannabis* / chemistry
  • Colorectal Neoplasms*
  • Dronabinol
  • Mice
  • Neuralgia* / drug therapy

Substances

  • Cannabinoids
  • Dronabinol

Grants and funding

This project was supported by a NARSAD Young Investigator Award (27364; NMG) and by the Pennsylvania Department of Health using Tobacco CURE Funds (NMG). KEV (and the Penn State College of Medicine) is the recipient of research support from PA Options for Wellness (a state-approved medical marijuana clinical registrant). The funding sources were not involved in: study design, providing any experimental materials, data collection, analysis and interpretation; writing of the report; or the decision to submit the article for publication.