Abstract. The picric acid due to its low pKa value possesses distinct physico-chemical features among all other nitro aromatic derivatives to design fluorescent probes for its’ sensitive and selective detection.The...
Crataegus oxyacantha is an important herbal supplement and famous for its antioxidant potential. The antioxidant in combination with anticholinesterase activity can be considered as an important target in the management of Alzheimer’s disease. The compounds isolated from C. oxyacantha were evaluated for cholinesterases inhibitory activity using Ellman’s assay with Galantamine as standard drug. Total of nine (1–9) compounds were isolated. Compounds 1 and 2 were isolated for the first time from natural source. Important natural products like β-Sitosterol-3-O-β-D-Glucopyranoside (3), lupeol (4), β-sitosterol (5), betulin (6), betulinic acid (7), oleanolic acid (8), and chrysin (9) have also been isolated from C. oxyacantha. Overall, all the compounds exhibited an overwhelming acetylcholinesterase (AChE) inhibition potential in the range 5.22–44.47 μM. The compound 3 was prominent AChE inhibitor with IC50 value of 5.22 μM. Likewise, all the compounds were also potent in butyrylcholinesterase (BChE) inhibitions with IC50s of up to 0.55–15.36 μM. All the compounds, except 3, were selective toward BChE. Mechanism of the inhibition of both the enzymes were further studied by docking procedures using Genetic Optimization for Ligand Docking suit v5.4.1. Furthermore, computational blood brain barrier prediction of the isolated compounds suggest that these are BBB+.
Antimalarial activity of the crude extract of Polygonatum verticillatum rhizomes and its sequentially partitioned fractions were investigated against Plasmodium falciparum. The crude extract possessed notable activity (IC 50 : 21.67 lg/mL) that enhanced reasonably upon fractionation. The antiparasitic potency of the n-hexane fraction was maximum (IC 50 : 2.33 lg/mL) followed by chloroform (IC 50 : 4.62 lg/mL). However, the remaining fractions showed insignificant activity in the assay. The extracts of the plant showed marked scavenging activity on stable free radical, DDPH. The most potent antioxidant was the chloroform fraction (IC 50 : 90 lg/mL) followed by ethyl acetate (IC 50 : 93 lg/mL) and n-butanol (IC 50 : 95 lg/mL) fractions. In the brine shrimps lethality test, the extracts were found nontoxic with the exception of ethyl acetate fraction (LD 50 : 492.846 lg/mL). The bioactivity-guided isolation resulted into 5-hydroxymethyl-2-furaldehyde (HMF) and diosgenin which strongly supports the present experimental findings.
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