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Inhibition of α-Glucosidase, Acetylcholinesterase, and Nitric Oxide Production by Phytochemicals Isolated from Millettia speciosa—In Vitro and Molecular Docking Studies
| Content Provider | MDPI |
|---|---|
| Author | Tuan, Nguyen Ngoc Thi, Huong Nguyen My, Chau Le Thi Hai, Tang Xuan Trung, Hieu Tran Kim, Anh Nguyen Thi Tan, Thanh Nguyen Van, Tan Le Nguyen, Cuong Quoc Tran, Quang De Kuo, Ping-Chung Dang, Quang Le Thang, Tran Dinh |
| Copyright Year | 2022 |
| Description | The phytochemical constituents from the roots of Millettia speciosa were investigated by chromatographic isolation, and their chemical structures were characterized using the MS and NMR spectroscopic methods. A total of 10 compounds, including six triterpenoids, two flavonoids, and two phenolic compounds, were identified from the roots of M. speciosa. Out of the isolated compounds, eight showed inhibitory effects on NO production in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, with $IC_{50}$ values ranging from 43.9 to 449.5 µg/mL. Ursane-type triterpenes significantly suppressed NO production compared to the remaining compounds. In addition, these compounds also exhibited remarkable inhibitory effects on α-glucosidase. Among the tested compounds, 4, 5, and 10 exhibited excellent α-glucosidase inhibition, with $IC_{50}$ values ranging from 1.1 to 2.2 µg/mL. Almost all of the test compounds showed little or no acetylcholinesterase inhibition, except for 5, which showed moderate anti-acetylcholinesterase activity in vitro. The molecular docking study of α-glucosidase inhibition by 3–5 and 10 was conducted to observe the interactions of these molecules with the enzyme. Compounds 4, 5, and 10 exhibited a better binding affinity toward the targeted receptor and the H-bond interactions located at the entrance of the enzyme active site pocket in comparison to those of 3 and the positive control acarbose. Our findings evidence the pharmacological potential of this species and suggest that the phytochemicals derived from the roots of M. speciosa may be promising lead molecules for further studies on the development of anti-inflammatory and anti-diabetes drugs. |
| Starting Page | 388 |
| e-ISSN | 22237747 |
| DOI | 10.3390/plants11030388 |
| Journal | Plants |
| Issue Number | 3 |
| Volume Number | 11 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2022-01-30 |
| Access Restriction | Open |
| Subject Keyword | Plants Integrative and Complementary Medicine Millettia Speciosa Molecular Docking No Production Anti-glucosidase Anti-acetylcholinesterase |
| Content Type | Text |
| Resource Type | Article |
