α-Glucosidase inhibitory activity of cannabidiol, tetrahydrocannabinol and standardized cannabinoid extracts from Cannabis sativa
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 ev...
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| Format: | Article |
| Language: | English |
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Elsevier
2022-01-01
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| Series: | Current Research in Food Science |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2665927122001046 |
| _version_ | 1811293777446305792 |
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| author | Wiwit Suttithumsatid Muhammad Ajmal Shah Shabana Bibi Pharkphoom Panichayupakaranant |
| author_facet | Wiwit Suttithumsatid Muhammad Ajmal Shah Shabana Bibi Pharkphoom Panichayupakaranant |
| author_sort | Wiwit Suttithumsatid |
| collection | DOAJ |
| description | 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 the α-glucosidase inhibitory activity of THC, CBD and the standardized cannabinoid extracts. Based on in silico studies, THC generated hydrogen bonding and Van der Waals interactions, while CBD exhibited only Van der Waals interactions with functional residues of target α-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 based in vitro assay on α-glucosidase revealed that THC and CBD exhibited good inhibitory activity, with the IC50 values of 3.0 ± 0.37 and 5.5 ± 0.28 μg/ml, respectively. These were better than the standard drug, acarbose (IC50 of 488.6 ± 10.23 μg/ml). Furthermore, two standardized cannabinoid extracts, SCE-I (C. sativa leaf extract) and SCE-II (C. sativa inflorescence extract) exhibited stronger inhibitory activity than THC and CBD, with the IC50 values 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. |
| first_indexed | 2024-04-13T05:06:25Z |
| format | Article |
| id | doaj.art-81a0e205b25c474db4ff574de6c157ee |
| institution | Directory Open Access Journal |
| issn | 2665-9271 |
| language | English |
| last_indexed | 2024-04-13T05:06:25Z |
| publishDate | 2022-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Current Research in Food Science |
| spelling | doaj.art-81a0e205b25c474db4ff574de6c157ee2022-12-22T03:01:09ZengElsevierCurrent Research in Food Science2665-92712022-01-01510911097α-Glucosidase inhibitory activity of cannabidiol, tetrahydrocannabinol and standardized cannabinoid extracts from Cannabis sativaWiwit Suttithumsatid0Muhammad Ajmal Shah1Shabana Bibi2Pharkphoom Panichayupakaranant3Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, 90112, ThailandDepartment of Pharmacy, Hazara University, Mansehra, PakistanDepartment of Biosciences, Shifa Tameer-e-Millat University, Islamabad, Pakistan; Yunnan Herbal Laboratory, College of Ecology and Environmental Sciences, Yunnan University, Kunming 650091, Yunnan, ChinaFaculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, 90112, Thailand; Phytomedicine and Pharmaceutical Biotechnology Excellence Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, 90112, Thailand; Corresponding author. Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, 90112, Thailand.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 the α-glucosidase inhibitory activity of THC, CBD and the standardized cannabinoid extracts. Based on in silico studies, THC generated hydrogen bonding and Van der Waals interactions, while CBD exhibited only Van der Waals interactions with functional residues of target α-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 based in vitro assay on α-glucosidase revealed that THC and CBD exhibited good inhibitory activity, with the IC50 values of 3.0 ± 0.37 and 5.5 ± 0.28 μg/ml, respectively. These were better than the standard drug, acarbose (IC50 of 488.6 ± 10.23 μg/ml). Furthermore, two standardized cannabinoid extracts, SCE-I (C. sativa leaf extract) and SCE-II (C. sativa inflorescence extract) exhibited stronger inhibitory activity than THC and CBD, with the IC50 values 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.http://www.sciencedirect.com/science/article/pii/S2665927122001046α-GlucosidaseCannabidiolCannabinoidCannabisDiabetes mellitusTetrahydrocannabinol |
| spellingShingle | Wiwit Suttithumsatid Muhammad Ajmal Shah Shabana Bibi Pharkphoom Panichayupakaranant α-Glucosidase inhibitory activity of cannabidiol, tetrahydrocannabinol and standardized cannabinoid extracts from Cannabis sativa Current Research in Food Science α-Glucosidase Cannabidiol Cannabinoid Cannabis Diabetes mellitus Tetrahydrocannabinol |
| title | α-Glucosidase inhibitory activity of cannabidiol, tetrahydrocannabinol and standardized cannabinoid extracts from Cannabis sativa |
| title_full | α-Glucosidase inhibitory activity of cannabidiol, tetrahydrocannabinol and standardized cannabinoid extracts from Cannabis sativa |
| title_fullStr | α-Glucosidase inhibitory activity of cannabidiol, tetrahydrocannabinol and standardized cannabinoid extracts from Cannabis sativa |
| title_full_unstemmed | α-Glucosidase inhibitory activity of cannabidiol, tetrahydrocannabinol and standardized cannabinoid extracts from Cannabis sativa |
| title_short | α-Glucosidase inhibitory activity of cannabidiol, tetrahydrocannabinol and standardized cannabinoid extracts from Cannabis sativa |
| title_sort | α glucosidase inhibitory activity of cannabidiol tetrahydrocannabinol and standardized cannabinoid extracts from cannabis sativa |
| topic | α-Glucosidase Cannabidiol Cannabinoid Cannabis Diabetes mellitus Tetrahydrocannabinol |
| url | http://www.sciencedirect.com/science/article/pii/S2665927122001046 |
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