Anti-cancer activity of <em>Fluggea leucopyrus</em> willd (Katupila) against human ovarian carcinoma and characterization of active compounds

Abstract

Fluggea leucopyrus Willd has been used in the treatment for cancers in the traditional system of medicine in Sri Lanka. This study was aimed on evaluation of anti-cancer activity of F.leucopyrus against Human Ovarian carcinoma and identification of active compounds. Anti-cancer activity of ethyl acetate (EtoAc) extract of leaves and two compounds isolated from EtoAc extract were evaluated using MTS and hTERT assays on Human Ovarian carcinoma (A 2780). MTS assay showed a significant anti-proliferation activity giving IC50 (concentration of extract/compound that inhibits 50% of the activity) values of 36.35±0.17µg/mL, 12.36±1.0 µg/mL and 48.53±1.43 µg/mL for EtoAc extract and two compounds (compound-1 & compound-2) respectively. A rapid depletion of hTERT content in Human Ovarian cancer cells was observed for the compound-2 with the concentration range 50-200 µg/mL. The compounds-1 was identified as bergenin, a known compound, whereas the compound-2 was identified as a diastereoisomer of bergenin (at C-9 and C-14,) with the help of NMR and Mass spectral data, and with the comparison of reported data. Brine Shrimp Lethality assay for EtoAc extract showed LC50 (Lethal concentration) values of 2779.63 µg/mL, implying that no toxicity of plant extract towards brine shrimp. As conclusion, anti-cancer activity of leaves of F. leucopyrus against Human Ovarian cancers is confirmed in this study, and bergenin and its isomer were identified as the responsible compounds for the anticancer activity of this plant.

International Journal of KIU

“…Bulugahapitiya et al, 2020 has reported that the leaves of the F. leucopyrus plant contains a Bergenin isomer which is responsible for the anticancer activity (Bulugahapitiya et al, 2020). Anticancer activity also has been detected for the bark and aerial parts of this plant (Bulugahapitiya et al, 2020). Further report suggest that bergenin could be used to develop more potent galectin-3 inhibitors which is a anticancer mechanism (Jayakody et al, 2018, Stegmayr et al, 2019.…”

“…Current study determined that the practitioners used whole plant, roots and leaves. Bulugahapitiya et al, 2020 has reported that the leaves of the F. leucopyrus plant contains a Bergenin isomer which is responsible for the anticancer activity (Bulugahapitiya et al, 2020). Anticancer activity also has been detected for the bark and aerial parts of this plant (Bulugahapitiya et al, 2020).…”

Antimicrobial and Preservative Activity of <em>Plectranthus amboinicus</em> (Lour.) Spreng, <em>Bacopa monnieri</em> (L.) Wettst,<em> Flueggea leucopyrus</em> Willd., and <em>Cymbopogon citratus</em> (DC.) Stapf Plant Extracts against Some Common Milk Pathogens and Their Biocompatibili

“…Consequently, the methanolic extract of B. monnieri dissolved in 0.1% DMSO exhibited the highest toxicity, while P. amboinicus demonstrated the least toxicity. According to [37], the brine shrimp lethality assay for the ethyl acetate extract of F. leucopyrus revealed LC50 values of 2779.63 μg/mL, suggesting no toxicity of the plant extract towards brine shrimp. This implies that LC50 values can vary with differences in plant extraction methods.…”

Chemistry and Pharmacology of Bergenin or Its Derivatives: A Promising Molecule

“…The IC 50 of pure bergenin isolated from different parts of plant species ( Table 2 ) was determined against P. falciparum in vitro, with the following results: 2.41–14.1 µg/mL [ 37 , 38 , 40 , 50 , 58 , 103 ]. The mechanism of action by which bergenin inhibits the growth of the parasite in vitro is not yet well known, but it is suggested that it is triggered by the inhibition of polymerization of the heme group of the parasite in a similar way to the mechanism of action of artemisinin since both are lactones of the same family [ 39 , 104 ].…”

“…Bulugahapitiya et al [ 40 ] reported anticancer activity of ethyl acetate extract (Et O Ac) from F. leucopyrus leaves, bergenin and bergenin diastereomer (at C-9 and C-14) both isolated from Et O Ac, against human ovarian carcinoma. Anticancer activity was evaluated using cell proliferation assays (MTS) and human telomerase reverse transcriptase (hTERT) in human ovarian carcinoma (A 2780).…”