OBJECTIVE: The goal of the present study was to assess the antiproliferative and apoptosis-inducing effects of stem parts of Elytranthe parasitica (L.) Danser (EP) on colorectal cancer and identify the bioactive phytochemicals.
MATERIAL AND METHODS: EP methanol extract (EP.M) and its subsequent fractions were screened for antiproliferative activity in human colorectal carcinoma HCT 116 cell line. Phytocomposition of the bioactive fraction was analyzed by GC-MS. Further, apoptotic induction and cell cycle arrest was assessed in the most bioactive fractions.
RESULTS: EP.DEE (Diethyl Ether) fraction and a subsequent fraction derived by column chromatography, Fraction 3A (FR 3A) significantly inhibited the proliferation of HCT 116 cells (P cell cycle checkpoints. GC-MS analysis of FR 3A revealed the presence of 24 phytochemicals, the most prominent of which was pinocembrin (70.67%), a flavonoid.
CONCLUSION: Hence, it could be speculated that pinocembrin and its related derivatives may be the chief phytochemicals involved in apoptosis - mediated cytotoxicity of the enriched fraction. Our findings indicate the enriched fraction is a promising candidate which could be developed into a natural chemotherapeutic product for colorectal cancer therapy.
METHOD: Young MP leaves were dried, powdered and extracted sequentially using hexane (HX), ethyl acetate (EA), methanol (MeOH) and water (W). Antioxidant activity was evaluated using ferric reducing antioxidant power (FRAP), 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 1,1-Diphenyl-2-picryl-hydrazyl (DPPH) radicals scavenging and cellular antioxidant activity (CAA) assays. Anti-proliferative activity was evaluated through cell viability assay, using the following four human cancer cell lines: breast (HCC1937, MDA-MB-231), colorectal (HCT116) and liver (HepG2). The anti-proliferative activity was further confirmed through cell cycle and apoptosis assays, including annexin-V/7-aminoactinomycin D staining and measurements of caspase enzymes activation and inhibition.
RESULT: Overall, MP-HX extract exhibited the highest antioxidant potential, with IC50 values of 267.73 ± 5.58 and 327.40 ± 3.80 μg/mL for ABTS and DPPH radical-scavenging assays, respectively. MP-HX demonstrated the highest CAA activity in Hs27 cells, with EC50 of 11.30 ± 0.68 μg/mL, while MP-EA showed EC50 value of 37.32 ± 0.68 μg/mL. MP-HX and MP-EA showed promising anti-proliferative activity towards the four cancer cell lines, with IC50 values that were mostly below 100 μg/mL. MP-HX showed the most notable anti-proliferative activity against MDA-MB-231 (IC50 = 57.81 ± 3.49 μg/mL) and HCT116 (IC50 = 58.04 ± 0.96 μg/mL) while MP-EA showed strongest anti-proliferative activity in HCT116 (IC50 = 64.69 ± 0.72 μg/mL). The anticancer potential of MP-HX and MP-EA were also demonstrated by their ability to induce caspase-dependent apoptotic cell death in all of the cancer cell lines tested. Cell cycle analysis suggested that both the MP-HX and MP-EA extracts were able to disrupt the cell cycle in most of the cancer cell lines.
CONCLUSIONS: MP-HX and MP-EA extracts demonstrated notable antioxidant, anti-proliferative, apoptosis induction and cancer cell cycle inhibition activities. These findings reflect the promising potentials of MP to be a source of novel phytochemical(s) with health promoting benefits that are also valuable for nutraceutical industry and cancer therapy.
METHODS: Six different extracts (hexane, chloroform, ethyl acetate, ethanol, methanol and water) were obtained from each plant or algae sample using sequential solvent extraction. The antidermatophytic activity for the extracts was assessed using a colourimetric broth microdilution method. The viability of Vero cells was measured by Neutral Red uptake assay.
RESULTS: All the extracts (except the water extracts of V. amygdalina, C. sertularioides and K. alvarezii) showed antidermatophytic activity against Trichophyton spp. The minimum fungicidal concentration (MFC) ranges for the plant extracts against T. rubrum and T. interdigitale are 0.0025-2.50 and 0.005-2.50mg/mL, respectively. The algae extracts exhibited lower potency against both species, showing MFC ranges of 0.08-2.50 and 0.31-2.50mg/mL, respectively. The ethanol and methanol extracts from the leaves of R. excelsa, and the methanol and water extracts from the leaves of S. myrtifolium were highly active (MFC<0.1mg/mL) and with high selectivity indices (SI>2.8) against reference strains of T. rubrum and T. interdigitale, and most of the clinical isolates of T. tonsurans. Phytochemical analysis indicates the presence of alkaloids, anthraquinones, flavonoids, saponins, tannins, phenolics and triterpenoids in the extracts.
CONCLUSIONS: The medicinal plant extracts exhibited stronger antidermatophytic activity compared to the algae extracts. The leaves of R. excelsa and S. myrtifolium are potential sources of new antidermatophytic agents against Trichophyton spp.