Objective: In this paper, we reported the identification of six differentially expressed proteins isolated from cancer cells, following exposure to the cytotoxic fern extracts.
Materials and Methods: The identities of these cancer proteins were determined by matrix-assisted laser desorption ionization time-of-flight protein sequencing.
Results: The cancer proteins were identified as follows: elongation factor 1-γ, glyceraldehydes-3-phosphate dehydrogenase, heat shock protein 90-β, heterogeneous nuclear ribonucleoprotein-A2/B1, truncated nucleolar phosphoprotein B23, and tubulin-β chain. To the best of our knowledge, this paper represents the first time these cancer proteins are being reported, following exposure to the aforementioned cytotoxic fern extracts.
Conclusion: It is hoped that further efforts in this direction could lead to the identification and development of target-specific chemotherapeutic agents.
SUMMARY: Cytotoxic fern extracts were tested in anti-cancer proteomic works.Six differentially-expressed cancer proteins were identified.Potential anti-cancer protein targets were reported. Abbreviations used: EF: Elongation factor; HRP: Horseradish peroxidase; HSP: Heat shock protein; MALDI: Matrix-assisted laser desorption/ionization.
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.
Results: 3,5-Dinitrosalicylic acid (DNS) method, FTIR, and GC-FID were employed to evaluate the reducing sugar concentration, functional groups of alcohol bonds and concentration of bioethanol, respectively. The two-way ANOVA results (p
OBJECTIVE: The objective of this study is to search for more potent benzimidazole-based cholinesterase inhibitors, through the modification of the 1- and 2-positions of the benzimidazole core.
METHODS: Synthesis of compounds were carried out via a 4-step reaction scheme following a previously reported protocol. Structure-activity relationship of the compounds are established through in vitro cholinesterase assays and in silico docking studies. Furthermore, cytotoxicity and blood brain barrier (BBB) permeability of the compounds were also investigated.
RESULTS: Among the synthesised compounds, three of them (5IIa, 5IIb, and 5IIc) exhibited potent selective butyrylcholinesterase inhibition at low micromolar level. The compounds did not show any significant cytotoxicity when tested against a panel of human cell lines. Moreover, the most active compound, 5IIc, was highly permeable across the blood brain barrier.
CONCLUSION: In total 10 benzimidazole derivatives were synthesized and screened for their AChE and BuChE inhibitory activities. Lead compound 5Iic, represents a valuable compound for further development as potential AD therapeutics.