1. Isolation, Purification and Anti-Cancer Potency of Novel Compound 6-Ethyl-3-Hydroxy-4-Methyl-8aH-Xanthen-9(10aH)-One from Mesua ferrea Linn from Western Ghats of Karnataka.
- Author
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MURTHUZA, S., MANJUNATHA, B. K., VIDYA, S. M., SHAIKH, F. K., MAGARE, V. N., and HALLUR, R. L. S.
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CAMPTOTHECIN , *LIQUID chromatography-mass spectrometry , *DNA topoisomerase I , *TRADITIONAL knowledge , *ANNEXINS , *ANTINEOPLASTIC agents , *DRUG standards - Abstract
Cancer is one of the leading causes of death worldwide. With the help of current scientific developments and traditional knowledge about medicinal plants, great progress could be made in the fight against cancer. The present study attempts to scientifically validate the ethnomedicinal and anticancer effects of Mesua ferrea Linn from the Western Ghats of Karnataka, India. Using preparative HPLC, two main fractions (C1 and C2) were isolated from the methanolic extract of Mesua ferrea and their bioactivity was investigated. Gas chromatography/Mass spectrometry analysis of Mesua ferrea methanol extract revealed the presence of 7 phytocomponents. Fraction C2 shows maximum potency against liver HepG2 cancer cell lines. Fraction C2 was further purified and subjected to spectroscopic analysis by 13C NMR, 1H NMR, FTIR and liquid chromatography-mass spectrometry techniques. The structure is predicted and identified as 6-ethyl-3- hydroxy-4-methyl-8aH-xanthen-9(10aH)-one. This compound was found to have antiproliferative activity with an IC50 value of 352.007 µg/ml compared to the standard drug (camptothecin) with an IC50 value of 52.253 µg/ml and a crude drug of 177.006 µg/ml. Anticancer efficacy of the purified compound assessed by Annexin V apoptosis Study Using HepG2 cell lines. The compound exhibits significant early and late apoptosis of 13.6 % and 15.5 %, respectively, compared to the standard drug camptothecin with 28.7 % and 18.7 % early and late apoptosis and 7.02 % and 11.8 %. Caspase-3 expression analysis using HepG2 cell lines revealed that the purified compound inhibited early apoptosis in HepG2 cells at a concentration of 352 µg/ml, activating the caspase-3 cascade by 15.3 % compared with 17 % of the standard drug CTP. The result of the DNA fragmentation test supported the results of Annexin V and caspase 3 expression and showed significant protection. Our results indicate that 6-ethyl-3-hydroxy-4-methyl-8aH-xanthen-9(10aH)-one isolated from Mesua ferrea may be a new lead molecule for the development of an antiproliferative, DNA-protective and effective anticancer drugs. [ABSTRACT FROM AUTHOR]
- Published
- 2023
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