A New Oleanane Triterpenoid from the Roots of Callerya speciosa

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.

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Augmentation of α-amylase and α-glucosidase inhibitory properties of Callerya speciosa root extracts: An exploration through simulated human gastrointestinal digestion

Quan,

Xuan,

Anh

et al. 2024

IFRJ

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The present work represents the first effort to evaluate the effect of an in vitro simulated human digestion model on the α-amylase and α-glucosidase inhibitory activities of Callerya speciosa root extracts. Through bioguided fractionation, a series of fractions were obtained from hexane (CSH) and ethyl acetate (CSE) extracts. Initial screening identified active fractions (CSH2, CSH3, CSE2, CSE3, and CSE4) for further in vitro digestion evaluation. The results showed a decrease in antioxidant activity across all samples after digestion, while a simultaneous increase in α-amylase and α-glucosidase inhibitory activities was observed during the small intestinal phase. Notably, compared with the undigested fraction, CSE3 demonstrated a 1.7-fold increase in α-amylase inhibition (IC50 = 0.86 mg/mL). Moreover, the α-glucosidase inhibitory activities of CSH3, CSE3, and CSE4 were significantly greater after digestion, with IC50 values of 0.18, 0.05, and 0.02 mg/mL, respectively. Impressively, during the small intestinal phase, the α-glucosidase inhibitory activities of CSH3, CSE3, and CSE4 were substantially greater than those of acarbose by 13.2-, 47.6-, and 119.0-fold, respectively, and greater than those of palmitic acid by 1.7-, 6.0-, and 15.0-fold, respectively. GC-MS and LC-ESI-MS/MS analyses identified isoflavonoids, fatty acids, and triterpenoids as key bioactive compounds in these fractions. The present work provided foundational insights for the future exploration of C. speciosa root extracts for diabetes management.

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A New Oleanane Triterpenoid from the Roots of Callerya speciosa

Cited by 3 publications

References 13 publications

Triterpenoids and saponins in drug discovery

Triterpenoids and saponins in drug discovery

Inhibition of α-Glucosidase, Acetylcholinesterase, and Nitric Oxide Production by Phytochemicals Isolated from Millettia speciosa—In Vitro and Molecular Docking Studies

Augmentation of α-amylase and α-glucosidase inhibitory properties of Callerya speciosa root extracts: An exploration through simulated human gastrointestinal digestion

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