Bioactive Metabolites from Propolis Inhibit Superoxide Anion Radical, Acetylcholinesterase and Phosphodiesterase (PDE4)

Abd El-Hady, Faten K., Shaker, Kamel H., Imhoff, Johannes F., Zinecker, Heidi, Salah, Nesma M. and Ibrahim, Amal M. (2013) Bioactive Metabolites from Propolis Inhibit Superoxide Anion Radical, Acetylcholinesterase and Phosphodiesterase (PDE4) International Journal of Pharmaceutical Sciences Review and Research, 21 (1). pp. 338-344.

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Cycloartane-triterpenes (cycloartenol, 3α-cycloartenol-26-oic acid and 3β-cycloartenol-26-oic acid) together with α-amyrin acetate
and flavonoids (pinostrobin, tectochrysin and chrysin) were isolated from Egyptian propolis for the first time. Their antioxidant
activity was evaluated with DPPH and superoxide anion radical (O2.-). All compounds possessed both (O2.-) scavenging as well as XOD
inhibitory activity in the range of 50 – 75 %. With DPPH, only the flavonoids showed scavenging activity (48 – 83 %).
Acetylcholinesterase (AChE) and phosphodiesterase type 4 (PDE4) inhibitors are currently considered as intracellular targets for treatment of Alzheimer’s disease and Chronic obstructive pulmonary disease (COPD). 3β-cycloartenol-26-oic acid moderately
inhibited AChE and PDE4 activities in vitro with IC50 values of 0.8±0.2 and 1.9±0.4 μM, respectively, while 3-cycloartenol-26-oic acid
inhibited AChE activity with an IC50 value of 2.1±0.1 μM. The flavonoids pinostrobin and chrysin reduced PDE4 activity by 43 and 40
%, respectively (10 μM) as well as moderately inhibited the growth of the HepG2 cell line, whereas chrysin reduced proliferation of
NIH-3T3 cells at 50 μM. Therefore, our results with 3β- and 3-cycloartenol-26-oic acids can contribute to further research on alternative drugs for the treatment of neurological and neurodegenerative diseases, as well as asthma and COPD.

Document Type: Article
Keywords: Propolis, Acetylcholinesterase (AChE), Phosphodiesterase (PDE4), Cycloartane triterpenes, Radical scavenging activity
Research affiliation: OceanRep > GEOMAR > FB3 Marine Ecology > FB3-MI Marine Microbiology
OceanRep > GEOMAR > Applied R&D > Centre for Marine Substances (KiWiZ)
OceanRep > The Future Ocean - Cluster of Excellence
Refereed: Yes
ISSN: 0976-044X
Projects: KIWIZ, Future Ocean
Date Deposited: 02 Sep 2014 11:02
Last Modified: 27 Jan 2017 13:24

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