☆ 4.2 Article

HPLC-DAD finger printing, antioxidant, cholinesterase, and α-glucosidase inhibitory potentials of a novel plant Olax nana

BMC COMPLEMENTARY AND ALTERNATIVE MEDICINE (2018)

期刊

BMC COMPLEMENTARY AND ALTERNATIVE MEDICINE

卷 18, 期 -, 页码 -

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BMC

DOI: 10.1186/s12906-017-2057-9

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Olax nana; Phytochemical analysis; HPLC-dad; Acetylcholinesterase (AChE); Butyrylcholinesterase (BChE); DPPH; H2O2; ABTS; alpha-glucosidase inhibitory assays

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Integrative & Complementary Medicine

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Background: The medicinal importance of a novel plant Olax nana Wall. ex Benth. (family: Olacaceae) was revealed for the first time via HPLC-DAD finger printing, qualitative phytochemical analysis, antioxidant, cholinesterase, and alpha-glucosidase inhibitory assays. Methods: The crude methanolic extract of O. nana (ON-Cr) was subjected to qualitative phytochemical analysis and HPLC-DAD finger printing. The antioxidant potential of ON-Cr was assessed via 1,1-diphenyl, 2-picrylhydrazyl (DPPH), 2,2-azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) and hydrogen peroxide (H2O2) free radical scavenging assays. Furthermore, acetylcholinesterase (AChE) & butyrylcholinesterase (BChE) inhibitory activities were performed using Ellman's assay, while alpha-glucosidase inhibitory assay was carried out using a standard protocol. Results: The qualitative phytochemical analysis of ON-Cr revealed the presence of secondary metabolites like alkaloids, flavonoids, tannins, sterols, saponins and terpenoids. The HPLC-DAD finger printing revealed the presence of 40 potential compounds in ON-Cr. Considerable anti-radical activities was revealed by ON-Cr in the DPPH, ABTS and H2O2 free radical scavenging assays with IC50 values of 71.46, 72.55 and 92.33 mu g/mL, respectively. Furthermore, ON-Cr showed potent AChE and BChE inhibitory potentials as indicated by their IC50 values of 33.2 and 55.36 mu g/mL, respectively. In the alpha-glucosidase inhibition assay, ON-Cr exhibited moderate inhibitory propensity with an IC50 value of 639.89 mu g/mL. Conclusions: This study investigated Olax nana for the first time for detailed qualitative phytochemical tests, HPLC-DAD finger printing analysis, antioxidant, anticholinesterase and alpha-glucosidase inhibition assays. The antioxidant and cholinesterase inhibitory results were considerable and can provide scientific basis for further studies on the neuroprotective and anti-Alzheimer's potentials of this plant. ON-Cr may further be subjected to fractionation and polarity guided fractionation to narrow down the search for isolation of bioactive compounds.

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7-Amine-spiro[chromeno[4,3-b]quinoline-6,1′-cycloalkanes]: Synthesis and cholinesterase inhibitory activity of structurally modified tacrines

Leticia B. Silva, Pablo A. Nogara, Paula T. Halmenschelager, Jessica C. Alvim, Fernanda D'A. Silva, Sarah C. Feitosa, Joao B. T. Rocha, Marcos A. P. Martins, Nilo Zanatta, Helio G. Bonacorso

Summary: Five new spirochromeno-quinolines were synthesized using a sequential one-pot two-step cyclocondensation reaction with cyclopentane, cyclohexane, and cycloheptane. The molecule with a spirocyclopentane derivative showed the highest AChE and BChE inhibitory activity. Non-halogenated compounds were found to be better inhibitors of AChE and BChE compared to halogenated molecules. Their inhibitory potency was weaker than that of tacrine, possibly due to the size of the spirocarbocyclic moieties hindering the interaction with cholinesterases. These findings may contribute to the development of new anticholinesterase drugs.

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