Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)

BACKGROUND: Limonoids are highly oxygenated compounds with a prototypical structure. Their occurrence in the plant kingdom is mainly confined to plant families of Meliaceae and Rutaceae. Owing to their wide range of pharmacological and therapeutic properties, this study was aimed at investigating th...

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Autores principales:	Dzoyem,Jean P., Tsamo,Armelle T., Melong,Raduis, Mkounga,Pierre, Nkengfack,Augustin E., McGaw,Lyndy J., Eloff,Jacobus N.
Lenguaje:	English
Publicado:	Sociedad de Biología de Chile 2015
Materias:	Trichilia welwitschii Cytotoxicity Acetylcholinesterase Nitric oxide Limonoids
Acceso en línea:	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0716-97602015000100057
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spelling	oai:scielo:S0716-976020150001000572016-02-16Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)Dzoyem,Jean P.Tsamo,Armelle T.Melong,RaduisMkounga,PierreNkengfack,Augustin E.McGaw,Lyndy J.Eloff,Jacobus N. Trichilia welwitschii Cytotoxicity Acetylcholinesterase Nitric oxide Limonoids BACKGROUND: Limonoids are highly oxygenated compounds with a prototypical structure. Their occurrence in the plant kingdom is mainly confined to plant families of Meliaceae and Rutaceae. Owing to their wide range of pharmacological and therapeutic properties, this study was aimed at investigating the potential nitric oxide (NO) and acetylcholinesterase (AChE) inhibitory activity and the cytotoxicity of three limonoids: trichilia lactone D5 (1), rohituka 3 (2) and dregeanin DM4 (3), isolated from Trichilia welwitschii C.DC RESULTS: Results indicated that the three limonoids had low cytotoxicity towards Vero cells with LC50 values ranging from 89.17 to 75.82 (μg/L. Compounds (2) and (3) had lower cytotoxicity compared to puromycin and doxorubicin used as reference cytotoxic compounds. Compound (1) (LC50 of 23.55 (μg/L) had good antiproliferative activity against RAW 264.7 cancer cells. At the lowest concentration tested (0.5 μg/mL), compound (2) and (3) released the lowest amount of nitric oxide (2.97 and 2.93 μM, respectively). The three limonoids had anti-AChE activity with IC50 values ranged of 19.13 (μg/L for (1), 34.15 (μg/L for (2) and 45.66 (μg/L for (3), compared to galantamine (IC50 of 8.22 ( g/mL) used as positive control CONCLUSION: The limonoid compounds studied in this work inhibited nitric oxide production in LPS-stimulated macrophages and had anti-AChE activity. Trichilia lactone D5 had potential antiproliferative activity against RAW 264.7 cancer cells. The limonoids had low cytotoxicity towards Vero cells lines. This study provided further examples of the importance of limonoids compounds as potential AChE inhibitors and anti-inflammatory agents targeting the inhibition of NO productioninfo:eu-repo/semantics/openAccessSociedad de Biología de ChileBiological Research v.48 20152015-01-01text/htmlhttp://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0716-97602015000100057en10.1186/S40659-015-0049-0
institution	Scielo Chile
collection	Scielo Chile
language	English
topic	Trichilia welwitschii Cytotoxicity Acetylcholinesterase Nitric oxide Limonoids
spellingShingle	Trichilia welwitschii Cytotoxicity Acetylcholinesterase Nitric oxide Limonoids Dzoyem,Jean P. Tsamo,Armelle T. Melong,Raduis Mkounga,Pierre Nkengfack,Augustin E. McGaw,Lyndy J. Eloff,Jacobus N. Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)
description	BACKGROUND: Limonoids are highly oxygenated compounds with a prototypical structure. Their occurrence in the plant kingdom is mainly confined to plant families of Meliaceae and Rutaceae. Owing to their wide range of pharmacological and therapeutic properties, this study was aimed at investigating the potential nitric oxide (NO) and acetylcholinesterase (AChE) inhibitory activity and the cytotoxicity of three limonoids: trichilia lactone D5 (1), rohituka 3 (2) and dregeanin DM4 (3), isolated from Trichilia welwitschii C.DC RESULTS: Results indicated that the three limonoids had low cytotoxicity towards Vero cells with LC50 values ranging from 89.17 to 75.82 (μg/L. Compounds (2) and (3) had lower cytotoxicity compared to puromycin and doxorubicin used as reference cytotoxic compounds. Compound (1) (LC50 of 23.55 (μg/L) had good antiproliferative activity against RAW 264.7 cancer cells. At the lowest concentration tested (0.5 μg/mL), compound (2) and (3) released the lowest amount of nitric oxide (2.97 and 2.93 μM, respectively). The three limonoids had anti-AChE activity with IC50 values ranged of 19.13 (μg/L for (1), 34.15 (μg/L for (2) and 45.66 (μg/L for (3), compared to galantamine (IC50 of 8.22 ( g/mL) used as positive control CONCLUSION: The limonoid compounds studied in this work inhibited nitric oxide production in LPS-stimulated macrophages and had anti-AChE activity. Trichilia lactone D5 had potential antiproliferative activity against RAW 264.7 cancer cells. The limonoids had low cytotoxicity towards Vero cells lines. This study provided further examples of the importance of limonoids compounds as potential AChE inhibitors and anti-inflammatory agents targeting the inhibition of NO production
author	Dzoyem,Jean P. Tsamo,Armelle T. Melong,Raduis Mkounga,Pierre Nkengfack,Augustin E. McGaw,Lyndy J. Eloff,Jacobus N.
author_facet	Dzoyem,Jean P. Tsamo,Armelle T. Melong,Raduis Mkounga,Pierre Nkengfack,Augustin E. McGaw,Lyndy J. Eloff,Jacobus N.
author_sort	Dzoyem,Jean P.
title	Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)
title_short	Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)
title_full	Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)
title_fullStr	Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)
title_full_unstemmed	Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)
title_sort	cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from trichilia welwitschii (meliaceae)
publisher	Sociedad de Biología de Chile
publishDate	2015
url	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0716-97602015000100057
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Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)

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