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 anti-cancer activity of this plant.
Highlights
Cancer is characterized as uncontrolled cell division caused by mutation of DNA of the cells and invaded into other organs of the body making abnormalities of normal cell functions
3.1 Results of purification of crude extracts using column chromatography Four compounds were isolated in pure stage from EtoAc extract in the repeated flash column chromatography and all the compounds were solid at the room temperature (Table-1)
3.3 Results of Human Telomerase Reverse Transcriptase (hTERT) Assay In hTERT assay, a rapid depletion of hTERT content in Human Ovarian cancer cells was observed in the range of 50-200 μg/mL with the compound-2 (Figure 2)
Summary
Cancer is characterized as uncontrolled cell division caused by mutation of DNA of the cells and invaded into other organs of the body making abnormalities of normal cell functions. The number of cancer cases reported worldwide is tremendously increasing due to various factors, mainly environmental and behavioural. According to WHO reports, cancers are known as the second leading cause for death globally and 9.6 million death reported in 2018, about 70% of deaths occur in low- and middleincome countries [1]. Finding cure for cancers using plant-based treatment has emerged as a promising alternative. At this endeavour, scientific investigation of medicinal plants which are known to have traditional uses in cancer treatment, is considered as prime important in order to prove their anti-cancer activity scientifically and to identify the active compounds
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