Abstract
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 IC50 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 IC50 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.
Highlights
Millettia (Leguminosae) is a genus of about 200 species found in tropical and subtropical regions of Africa and Asia [1]
A total of 10 compounds, including six triterpenoids, two flavonoids, and two phenolic compounds were identified from the roots of M. speciosa (Figure 1)
The findings show that the active molecules bind to glucosidase more readily than acarbose (Figure 4)
Summary
Millettia (Leguminosae) is a genus of about 200 species found in tropical and subtropical regions of Africa and Asia [1]. The chemical composition of Millettia is characterized by flavonoids, including chalcones, isoflavones, and triterpenoids [2,3]. Most of these plants are known for their folk medicinal applications. Millettia griffoniana is employed orally for the treatment of boils, inflammation, amenorrhea, menopausal syndromes, sterility, and insect bites [6,7]. Millettia oblata has therapeutic uses for stomachache, cough, and swollen body, while M. usaramensis used as a remedy against snake bites [2]
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