Cyperus articulatus is widely distributed in Indian subcontinent and its rhizome has been used as folk
medicine in different geographical regions for treatment of diseases like malaria, epilepsy and dysentery.
In present study the rhizome extracts were studied to identify the natural inhibitor compounds for
α-amylase and α-glucosidase. Among six different solvent extracts of the rhizome, the acetone extract
which showed to have highest phenolics and flavonoids exhibited α-glucosidase inhibition (IC50 9.1
μg/mL). Different fractions were collected using column chromatography and flash chromatography
to analyze the active fractions. Two major fractions significantly showed high enzyme inhibitory
activity. In HRLC-MS/MS phenolic as well as non-phenolic class of compounds were identified such
as quercetrin, dihydroquercetin, mycophenolic acid, koparin-2-methylether, C16-sphinganine, embelin,
phytosphingosine, colforsin, 7,8-dihydroxystearic acid and palmitic acid derivative. The two active
fractions having IC50 8.38 and 7.65 μg/mL, were shown to exhibit competitive and mixed type inhibition,
respectively. Molecular docking analysis of the compounds with the α-glucosidase active site showed
that the phenolic class of compounds have efficient binding with one of the aspartate (Asp66, Asp349
and Asp212) residues whereas there was non-polar contacts with other residues in case of non-phenolic
compounds such as long chain hydroxyl acids. The results suggest that Cyperus articulatus rhizome
is a potential source of drug ingredients for the management of type-II diabetes.
The present study investigated the phytochemical constituents from Canna indica rhizome acetone extract,
which was earlier reported to possess α-glucosidase inhibiting potential. Different fractions were collected
from column chromatography of the acetone extract and the in vitro enzyme inhibition and the kinetic
study was performed with the active fraction. The active fraction exhibited competitive inhibition of
α-glucosidase. HRLC-MS/MS technique was used to identify the lead compounds from the active
fraction. The major compounds were psoromic acid, usnic acid and rosmarinic acid. Molecular docking
study of the compounds with the crystal structure of α-glucosidase was performed using ParDOCK.
Psoromic acid and usnic acid exhibited strong binding affinity with the active site nucleophiles Asp349
and Asp212, respectively. Usnic acid also stabilized the catalytic residue Glu274. Rosmarinic acid
formed multiple hydrogen bonds with the catalytic residue Glu274 and also bonded to non-catalytic
residues Gln276, Arg312 and Glu408. The study illustrated informative data on the phytochemical
constituents from Canna indica rhizome as α-glucosidase inhibitor and as potential candidates for the
development of antidiabetic drugs.
Introduction: Cyperus articulatus rhizome has been used in folk medicine by different inhabitants belonging to tropical and subtropical regions. But its metabolite profile and potential pharmacological and food applications were hardly explored. Evaluation of biological activities of Cyperus articulatus metabolites was the objective of the present study. Materials and Methods: In vitro biological studies concerning radical scavenging, reducing activity, food (meat and β-carotene) protection, biomolecule (DNA and Protein) protection and Acetylcholinesterase inhibitory activity were carried out for the rhizome extracts. Chemical constituents of the bioactive rhizome extract were analyzed through HRLC-MS/MS. Results: The rhizome acetone extract showed the highest antioxidant activity and protected DNA and protein from degradation at the lowest concentrations compared to all the six different solvent extracts tested. It significantly inhibited β-carotene bleaching, controlled the TBARS values during meat oxidation and significantly inhibited the Acetylcholinesterase enzyme. The major compounds detected in HRLC-MS/MS were dihydroquercetin, mycophenolic acid, embelin, quercetrin, meptazinol, koparin-2-methyl ether, venpocentine along with other phenolics and polyhydroxy compounds.
Conclusion:The study explored Cyperus articulatus rhizome as a pharmacologically important source for nutraceuticals and drug ingredients and suggested further safety and efficacy studies of the detected metabolites.
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