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
RESULTS: Aqueous extracts of the leaves and rhizomes of Cyathea latebrosa, Dicranopteris curranii, Gleichenia truncata, and Phymatopteris triloba were analysed. P. triloba leaf extract had the highest contents of total flavonoids (118.6 mg/g dry matter), hydroxycinnamic acids (69.7 mg/g dry matter), and proanthocyanidins (29.4 mg/g dry matter). P. triloba leaf and rhizome extracts as well as G. truncata leaf extract inhibited the growth of both Gram-positive and Gram-negative bacteria. P. triloba leaf extract produced a minimum inhibitory concentration (MIC) value of 0.78 mg dry matter/mL when tested against Pseudomonas aeruginosa, which is 2.5-fold higher than that of ampicillin. Among all extracts, P. triloba leaf extract had the highest anti-glucosidase activity (EC50 = 56 μg dry matter/mL) and also the highest antioxidant potential based on DPPH radical scavenging and Ferric Reducing Antioxidant Power assays. Antioxidant activities of both the leaf and rhizome extracts correlated positively with total flavonoid and hydroxycinnamic acid contents (R(2) = 0.80-0.95). On the other hand, anti-glucosidase activity correlated with total proanthocyanidin contents in both the leaf and rhizome extracts (R(2) = 0.62-0.84).
CONCLUSIONS: In conclusion, highland ferns are potential sources of antibacterial agents, glucosidase inhibitors, and antioxidants.
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.