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Inhibition of aldose reductase activity by Cannabis sativa chemotypes extracts with high content of cannabidiol or cannabigerol.
Fitoterapia. 2018 Jun; 127:101-108.F

Abstract

Aldose reductase (ALR2) is a key enzyme involved in diabetic complications and the search for new aldose reductase inhibitors (ARIs) is currently very important. The synthetic ARIs are often associated with deleterious side effects and medicinal and edible plants, containing compounds with aldose reductase inhibitory activity, could be useful for prevention and therapy of diabetic complications. Non-psychotropic phytocannabinoids exert multiple pharmacological effects with therapeutic potential in many diseases such as inflammation, cancer, diabetes. Here, we have investigated the inhibitory effects of extracts and their fractions from two Cannabis sativa L. chemotypes with high content of cannabidiol (CBD)/cannabidiolic acid (CBDA) and cannabigerol (CBG)/cannabigerolic acid (CBGA), respectively, on human recombinant and pig kidney aldose reductase activity in vitro. A molecular docking study was performed to evaluate the interaction of these cannabinoids with the active site of ALR2 compared to known ARIs. The extracts showed significant dose-dependent aldose reductase inhibitory activity (>70%) and higher than fractions. The inhibitory activity of the fractions was greater for acidic cannabinoid-rich fractions. Comparative molecular docking results have shown a higher stability of the ALR2-cannabinoid acids complex than the other inhibitors. The extracts of Cannabis with high content of non-psychotropic cannabinoids CBD/CBDA or CBG/CBGA significantly inhibit aldose reductase activity. These results may have some relevance for the possible use of C. sativa chemotypes based preparations as aldose reductase inhibitors.

Authors+Show Affiliations

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98168 Messina, Italy; Foundation Prof. Antonio Imbesi, University of Messina, Messina, Italy. Electronic address: asmeriglio@unime.it.Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98168 Messina, Italy.Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98168 Messina, Italy.Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98168 Messina, Italy.Department of Biomedical and Dental Sciences and Morphofunctional Imaging, University of Messina, 98166 Messina, Italy.Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98168 Messina, Italy.CRA-Research Institute for Industrial Crops (ISCI), 45100 Rovigo, Italy.Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98168 Messina, Italy.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29427593

Citation

Smeriglio, Antonella, et al. "Inhibition of Aldose Reductase Activity By Cannabis Sativa Chemotypes Extracts With High Content of Cannabidiol or Cannabigerol." Fitoterapia, vol. 127, 2018, pp. 101-108.
Smeriglio A, Giofrè SV, Galati EM, et al. Inhibition of aldose reductase activity by Cannabis sativa chemotypes extracts with high content of cannabidiol or cannabigerol. Fitoterapia. 2018;127:101-108.
Smeriglio, A., Giofrè, S. V., Galati, E. M., Monforte, M. T., Cicero, N., D'Angelo, V., Grassi, G., & Circosta, C. (2018). Inhibition of aldose reductase activity by Cannabis sativa chemotypes extracts with high content of cannabidiol or cannabigerol. Fitoterapia, 127, 101-108. https://doi.org/10.1016/j.fitote.2018.02.002
Smeriglio A, et al. Inhibition of Aldose Reductase Activity By Cannabis Sativa Chemotypes Extracts With High Content of Cannabidiol or Cannabigerol. Fitoterapia. 2018;127:101-108. PubMed PMID: 29427593.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inhibition of aldose reductase activity by Cannabis sativa chemotypes extracts with high content of cannabidiol or cannabigerol. AU - Smeriglio,Antonella, AU - Giofrè,Salvatore V, AU - Galati,Enza M, AU - Monforte,Maria T, AU - Cicero,Nicola, AU - D'Angelo,Valeria, AU - Grassi,Gianpaolo, AU - Circosta,Clara, Y1 - 2018/02/07/ PY - 2017/12/04/received PY - 2018/01/22/revised PY - 2018/02/03/accepted PY - 2018/2/11/pubmed PY - 2018/7/18/medline PY - 2018/2/11/entrez KW - Aldose reductase inhibitory activity KW - Cannabis sativa L. chemotypes KW - Molecular docking study KW - Non-psychotropic phytocannabinoids KW - Standardized extracts SP - 101 EP - 108 JF - Fitoterapia JO - Fitoterapia VL - 127 N2 - Aldose reductase (ALR2) is a key enzyme involved in diabetic complications and the search for new aldose reductase inhibitors (ARIs) is currently very important. The synthetic ARIs are often associated with deleterious side effects and medicinal and edible plants, containing compounds with aldose reductase inhibitory activity, could be useful for prevention and therapy of diabetic complications. Non-psychotropic phytocannabinoids exert multiple pharmacological effects with therapeutic potential in many diseases such as inflammation, cancer, diabetes. Here, we have investigated the inhibitory effects of extracts and their fractions from two Cannabis sativa L. chemotypes with high content of cannabidiol (CBD)/cannabidiolic acid (CBDA) and cannabigerol (CBG)/cannabigerolic acid (CBGA), respectively, on human recombinant and pig kidney aldose reductase activity in vitro. A molecular docking study was performed to evaluate the interaction of these cannabinoids with the active site of ALR2 compared to known ARIs. The extracts showed significant dose-dependent aldose reductase inhibitory activity (>70%) and higher than fractions. The inhibitory activity of the fractions was greater for acidic cannabinoid-rich fractions. Comparative molecular docking results have shown a higher stability of the ALR2-cannabinoid acids complex than the other inhibitors. The extracts of Cannabis with high content of non-psychotropic cannabinoids CBD/CBDA or CBG/CBGA significantly inhibit aldose reductase activity. These results may have some relevance for the possible use of C. sativa chemotypes based preparations as aldose reductase inhibitors. SN - 1873-6971 UR - https://www.unboundmedicine.com/medline/citation/29427593/Inhibition_of_aldose_reductase_activity_by_Cannabis_sativa_chemotypes_extracts_with_high_content_of_cannabidiol_or_cannabigerol_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0367-326X(17)31759-8 DB - PRIME DP - Unbound Medicine ER -