Alpha-glucosidase inhibitory activity of cannabidiol, tetrahydrocannabinol and standardized cannabinoid extracts from Cannabis sativa. - GreenMedInfo Summary

Two major cannabinoids of cannabis, namely cannabidiol (CBD) and tetrahydrocannabinol (THC) have been reportedly used as alternative medicine for diabetes treatment in both pre-clinical and clinical research. However, their mechanisms of action still remain unclear. Therefore, this study aimed to evaluate theα-glucosidase inhibitory activity of THC, CBD and the standardized cannabinoid extracts. Based onstudies, THC generated hydrogen bonding and Van der Waals interactions, while CBD exhibited only Van der Waals interactions with functional residues of targetα-glucosidase protein, with good binding energies of -7.5 and -6.9 kcal/mol, respectively. In addition, both of them showed excellent pharmacokinetic profiles with minor toxicity in terms of tumorigenic and reproductive effects. In addition, the enzyme basedassay onα-glucosidase revealed that THC and CBD exhibited good inhibitory activity, with the ICvalues of 3.0 ± 0.37 and 5.5 ± 0.28 μg/ml, respectively. These were better than the standard drug, acarbose (ICof 488.6 ± 10.23 μg/ml). Furthermore, two standardized cannabinoid extracts, SCE-I (leaf extract) and SCE-II (inflorescence extract) exhibited stronger inhibitory activity than THC and CBD, with the ICvalues of 1.2 ± 0.62 and 0.16 ± 0.01 μg/ml, respectively. The present study provides the first evidence that the standardized cannabinoid extracts containing THC and CBD have greater potential than CBD and THC in application as an α-glucosidase inhibitor.