Phytochemical investigation of a high potency variety of Cannabis sativa L. resulted in the isolation of six new metabolites, (+/-)-6,7-trans-epoxycannabigerolic acid ( 2), (+/-)-6,7- CIS-epoxycannabigerolic acid ( 3), (+/-)-6,7- CIS-epoxycannabigerol ( 4), (+/-)-6,7-trans-epoxycannabigerol ( 5), 5'-methyl-4-pentylbiphenyl-2,2',6-triol ( 7), and 7-methoxycannabispirone ( 8), along with seven known compounds namely, cannabigerolic acid ( 1), 5'-methoxycannabigerolic acid ( 6), cannabispirone ( 9), beta-cannabispiranol ( 10), dehydrocannabifuran ( 11), cannflavin B ( 12) and cannabigerol ( 13). The antimicrobial as well as the antileishmanial activities were investigated.
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http://dx.doi.org/10.1055/s-2008-1034311 | DOI Listing |
Pharmaceuticals (Basel)
December 2024
Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio®), Instituto Nacional de Ciência e Tecnologia de Fármacos e Medicamentos (INCT-INOFAR), Universidade Federal do Rio de Janeiro, Rio de Janeiro 21941-902, Brazil.
Glioblastoma is a malignant tumor with a poor prognosis for the patient due to its high lethality and limited chemotherapy available. Therefore, from the point of view of chemotherapy treatment, glioblastoma can be considered an unmet medical need. This has led to the investigation of new drugs for monotherapy or associations, acting by synergistic pharmacological mechanisms.
View Article and Find Full Text PDFMolecules
December 2024
NRC Institute of Immunology FMBA of Russia, 115552 Moscow, Russia.
N-Acetylgalactosamine (GalNAc) is an efficient and multifunctional delivery tool in the development and synthesis of chemically modified oligonucleotide therapeutics (conjugates). Such therapeutics demonstrate improved potency in vivo due to the selective and efficient delivery to hepatocytes in the liver via receptor-mediated endocytosis, which is what drives the high interest in this molecule. The ways to synthesize such structures are relatively new and have not been optimized in terms of the yields and stages both in lab and large-scale synthesis.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Institute of Cytology, Russian Academy of Sciences, St. Petersburg 194064, Russia.
G-protein-coupled receptors (GPCRs) have emerged as critical regulators of bone development and remodeling. In this study, we aimed to identify specific GPCR mutations in osteoporotic patients via next-generation sequencing (NGS). We performed NGS sequencing of six genomic DNA samples taken from osteoporotic patients and two genomic DNA samples from healthy donors.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Biosciences and Bioinformatics, School of Science, Xi'an Jiaotong-Liverpool University, 111 Ren'ai Road, Suzhou 215123, China.
The SARS-CoV-2 main protease (Mpro, also known as 3CLpro) is a key target for antiviral therapy due to its critical role in viral replication and maturation. This study investigated the inhibitory effects of Bofutrelvir, Nirmatrelvir, and Selinexor on 3CLpro through molecular docking, molecular dynamics (MD) simulations, and free energy calculations. Nirmatrelvir exhibited the strongest binding affinity across docking tools (AutoDock Vina: -8.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Biochemistry, National Defense Medical Center, Taipei 114, Taiwan.
Local anesthetics are commonly used in various clinical settings for both prevention and symptom relief. Numerous clinical studies have demonstrated that intra-articular injections of local anesthetics achieve high success rates in orthopedic practices. However, several widely used local anesthetics, including bupivacaine, lidocaine, and ropivacaine, have been shown to exhibit toxicity to chondrocytes, with the underlying mechanisms of chondrotoxicity remaining poorly understood.
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