Although Cannabis sativa L. is well known for being prolific in phytocannabinoids, their biosynthetic modular mechanism is ruled by a main enzyme: the geranyltransferase able to pursue the C-isoprenylation of olivetolic acid with the geranyldiphosphate. However, the existence of more than 160 meroterpenoids can be partially explained by a side degree of promiscuity of the geranyltransferase itself, able to recognise different substrate than the ordinary ones. This biological process led to the identification of several unconventional phytocannabinoids with a limited distribution in the plant both for occurrence and concentration. Taking advance of the existing synthetic protocols and using as example the enzymatic promiscuity, we propose a bio-inspired synthesis of naturally occurring minor cannabinoids related to the cannabigerol-type and their preliminary biological inspection in U87, U251 and T98 human glioblastoma cell lines to investigate their potential contribute as supplement in anticancer therapy.
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http://dx.doi.org/10.1016/j.fitote.2024.106354 | DOI Listing |
Acta Neuropathol Commun
January 2025
Sid Faithfull Brain Cancer Laboratory, QIMR Berghofer Medical Research Institute, Brisbane, QLD, 4006, Australia.
Glioblastoma (GBM) is a highly aggressive adult brain cancer, characterised by poor prognosis and a dismal five-year survival rate. Despite significant knowledge gains in tumour biology, meaningful advances in patient survival remain elusive. The field of neuro-oncology faces many disease obstacles, one being the paucity of faithful models to advance preclinical research and guide personalised medicine approaches.
View Article and Find Full Text PDFSci Rep
January 2025
Department of Neurosurgery, Fujita Health University School of Medicine, 1-98 Dengakugakubo Kutsukake-cho, Toyoake, Aichi, 470-1192, Japan.
Karnofsky Performance Status (KPS) is a widely used scale to assess performance status. KPS ≥ 50% implies that patients can live at home. Therefore, maintaining KPS ≥ 50% is important to improve the quality of life of patients with glioblastoma, whose median survival is less than 2 years.
View Article and Find Full Text PDFBioorg Chem
January 2025
N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, Lavrentyev Avenue 9, Novosibirsk 630090, Russia. Electronic address:
Eudesmane-type sesquiterpene lactone isoalantolactone 1 is of great interest due to its availability, biological activity and synthetic application. Respective series of original spirocyclic (11S,5') (1,2,3-triazoline-eudesma-4,15-enolides) and (11S)-aziridine-eudesma-4,15-enolides were efficiently synthesized via a chemoselective 1,3-dipolar cycloaddition reaction of organic azides to the exocyclic double bond of the lactone ring of isoalantolactone or 13E-(aryl)isoalantolactones by heating in DMF or toluene. The thermal reactions of isoalantolactone with benzyl azide, 2-azidoethanol, or n-butyl azide in 2-methoxyethanol afforded 13-(alkyamino)isoalantolactones formed as a mixture of (Z) and (E)-isomers.
View Article and Find Full Text PDFAdv Clin Exp Med
January 2025
Department of Neurosurgery, The Affiliated Children's Hospital of Xi'an Jiaotong University, Xi'an Children's Hospital, China.
Background: Glioblastoma multiforme (GBM) is the most aggressive brain tumor malignancy in adults, accounting for nearly 50% of all gliomas. Current medications for GBM frequently lead to drug resistance.
Objectives: Umbelliferone (UMB) is found extensively in many plants and shows numerous pharmacological actions against inflammation, degenerative diseases and cancers.
Neuro Oncol
January 2025
Department of Pathology, Rady Faculty of Health Sciences, University of Manitoba, Winnipeg, Canada.
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