Schizonticidal antimalarial sesquiterpene lactones from Magnolia champaca (L.) Baill. ex Pierre: microwave-assisted extraction, HPTLC fingerprinting and computational studies.

Abstract:

:The present study explored the schizonticidal potential of traditionally used Magnolia champaca (L.) Baill. ex. Pierre flowers, identifying constituents of interest. The extraction of phytoconstituents was carried out by microwave-assisted technique, isolated via column chromatography, and characterised by various physicochemical, spectral (IR, 1H-NMR and Mass) and chromatographic (HPTLC) techniques. Both the isolated compounds (parthenolide and costunolide diepoxide) exhibited potent schizonticidal antimalarial activity during primary screening in rodent models, with maximum parasitaemia suppression (85.18% and 83.65%, respectively) at a dose of 20 mg/kg body weight when compared to the standard drugs chloroquine and artesunate. In silico techniques were employed to identify the probable biological target and mechanism of action of these isolated compounds. Molecular docking studies also predicted the binding orientations and multi-targeted action of these compounds, in particular costunolide diepoxide with maximum affinity towards SERCA and DHFR proteins. Additionally, favourable in silico ADMET parameters were envisaged through various computational programmes.

journal_name

Nat Prod Res

journal_title

Natural product research

authors

Mehrotra E,Vishwakarma J,Tripathi AC,Sonar PK,Saraf SK

doi

10.1080/14786419.2017.1396595

subject

Has Abstract

pub_date

2019-02-01 00:00:00

pages

568-572

issue

4

eissn

1478-6419

issn

1478-6427

journal_volume

33

pub_type

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