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1.
Eur J Pharmacol ; 976: 176679, 2024 Aug 05.
Article in English | MEDLINE | ID: mdl-38821167

ABSTRACT

To provide a comprehensive framework of the current information on the potency and efficacy of interaction between phyto- and synthetic cannabinoids and their respective receptors, an electronic search of the PubMed, Scopus, and EMBASE literature was performed. Experimental studies included reports of mechanistic data providing affinity, efficacy, and half-maximal effective concentration (EC50). Among the 108 included studies, 174 structures, and 16 targets were extracted. The most frequent ligands belonged to the miscellaneous category with 40.2% followed by phytocannabinoid-similar, indole-similar, and pyrrole-similar structures with an abundance of 17.8%, 16.6%, and 12% respectively. 64.8% of structures acted as agonists, 17.1 % appeared as inverse agonists, 10.8% as antagonists, and 7.2% of structures were reported with antagonist/inverse agonist properties. Our outcomes identify the affinity, EC50, and efficacy of the interactions between cannabinoids and their corresponding receptors and the subsequent response, evaluated in the available evidence. Considering structures' significance and very important effects of on the activities, the obtained results also provide clues to drug repurposing.


Subject(s)
Cannabinoids , Cannabinoids/pharmacology , Cannabinoids/chemistry , Humans , Animals , Structure-Activity Relationship , Receptors, Cannabinoid/metabolism , Ligands , Cannabinoid Receptor Agonists/pharmacology , Cannabinoid Receptor Agonists/chemistry
2.
Mol Biol Rep ; 46(3): 3275-3286, 2019 Jun.
Article in English | MEDLINE | ID: mdl-30993582

ABSTRACT

It was confirmed that several enzymes have anti-cancer activity. The enzymes L-asparaginase, L-glutaminase, and L-arginase were chosen according to amino acids starvation in cancer cells and screened in halophilic and halotolerant bacteria, given probably less immunological reactions of halophilic or halotolerant enzymes in patients. Out of 110 halophilic and halotolerant strains, isolated from different saline environments in Iran and screened, some could produce a variety of anticancer enzymes. A total of 29, 4, and 2 strains produced L-asparaginase, L-glutaminase, and L-arginase, respectively. According to the phenotypic characteristics and partial 16S rRNA gene sequence analysis, the positive strains-strains with the ability to produce these anticancer enzymes-were identified as the members of the genera: Bacillus, Dietzia, Halobacillus, Rhodococcus, Paenibacillus and Planococcus as Gram-positive bacteria and Pseudomonas, Marinobacter, Halomonas, Idiomarina, Vibrio and Stappia as Gram-negative bacteria. The production of anticancer enzymes was mostly observed in the rod-shaped Gram-negative isolates, particularly in the members of the genera Halomonas and Marinobacter. Most of the enzymes were produced in the stationary phase of growth and the maximum enzyme activity was experienced in strain GBPx3 (Vibrio sp.) for L-asparaginase at 1.0 IU/ml, strain R2S25 (Rhodococcus sp.) for L-glutaminase at 0.6 IU/ml and strain GAAy3 (Planococcus sp.) for L-arginase at 3.1 IU/ml. The optimum temperature and pH for L-asparaginase and L-glutaminase activities in selected strains were similar to the physiological conditions of human body and the enzymes could tolerate NaCl up to 7.5% concentration.


Subject(s)
Bacteria/genetics , Salt Tolerance/genetics , Antineoplastic Agents , Asparaginase/metabolism , DNA, Bacterial/genetics , Halobacteriales/genetics , Iran , Phylogeny , RNA, Ribosomal, 16S/genetics , Saline Solution , Sequence Analysis, DNA , Sodium Chloride/metabolism
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