Free radicals play a crucial role in the development of tissue damage in various human pathologies such as Alzheimer’s disease (AD).1 In spite of the multi-factorial nature of AD, the only therapeutic approach is based on the so-called cholinergic hypothesis that postulates a deficiency in cholinergic neurotransmission, which seems to play a fundamental role in memory.2 So restore the level of acetylcholine through inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) is a therapeutic useful approach to treat AD and other forms of dementia. This study aimed to investigate the chemical composition, the antioxidant properties and the anticholinesterase activity of the aerial parts of Berberis aetnensis C. Presl. (Berberidaceae). Several Berberis species are used for treating a variety of ailments such as eye and ear diseases, rheumatism, jaundice, diabetes, fever, stomach disorders, skin disease, malarial fever and as tonic.3 Aerial parts were collected in July 2007 in Calabria (Italy) and exhaustively extracted with methanol. The total extract was fractionated to obtain a methanol and a n-hexane fraction. Moreover, in order to obtain the alkaloid fraction, the method reported by Kupeli et al.4 was used. The total phenol and flavonoid contents were determined by the Folin-Ciocalteau method and a method based on the formation of a flavonoid-aluminium complex, respectively.5 The antioxidant activity was screened by DPPH and β-carotene bleaching test.5 Methanol fraction exhibited the most promising radical scavenging activity with an IC50 value of 23.0 μg/mL. In β-carotene bleaching test the total extract showed the highest activity with an IC50 value of 2.8 μg/mL after 30 min of incubation. AChE and BChE inhibition was assessed by Ellman’s method.6 The alkaloid fraction showed the highest anticholinesterase activity with IC50 values of 18.6 and 54.7 μg/mL against AChE and BChE, respectively. GC-MS and GC analyses revealed the presence of berberine, palmatine, ossiberberine, berbamine and oxoglaucine as major components of the alkaloid fraction. n-Hexane fraction, characterized by terpenes, fatty acids and sterols as most common constituents, selectively inhibited BChE (IC50 value of 68.4 μg/mL). References 1 Gutteridge, J.M.C. Chem Biol Interact, 1994, 91, 133-140. 2 Loizzo, M.R., Tundis, R., Menichini, F., Menichini, F. Curr Med Chem, 2008, 15, 1209-1228. 3 Musumeci, R., Speciale, A., Costanzo, R., Annino, A., Ragusa, S., Rapisarda, A., Pappalardo, M.S., Iauk, L. Int J Antimic Agents, 2003, 22, 48-53. 4 E. Küpeli, M. Koᶊar, E. Yeilada, C.H. Baᶊer, C. Baᶊer. Life Sciences, 2002, 72, 645-657. 5 Conforti, F., Marrelli, M., Menichini, F., Tundis, R., Statti, G.A., Solimene, U., Menichini, F. J Enzyme Inhib Med Chem, 2011, 26 , 404-411. 6 Ellman, G.L., Courtney, K.D., Andres, V.Jr, Featherstone R.M. Biochem Pharmacol, 1961, 7, 88-95.
In vitro anticholinesterase and antioxidant properties of Berberis aetnensis C. Presl. (Berberidaceae) aerial parts
Marco Bonesi;TUNDIS, ROSA;LOIZZO, Monica Rosa;CONFORTI, FILOMENA;Nicodemo Passalacqua;
2012-01-01
Abstract
Free radicals play a crucial role in the development of tissue damage in various human pathologies such as Alzheimer’s disease (AD).1 In spite of the multi-factorial nature of AD, the only therapeutic approach is based on the so-called cholinergic hypothesis that postulates a deficiency in cholinergic neurotransmission, which seems to play a fundamental role in memory.2 So restore the level of acetylcholine through inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) is a therapeutic useful approach to treat AD and other forms of dementia. This study aimed to investigate the chemical composition, the antioxidant properties and the anticholinesterase activity of the aerial parts of Berberis aetnensis C. Presl. (Berberidaceae). Several Berberis species are used for treating a variety of ailments such as eye and ear diseases, rheumatism, jaundice, diabetes, fever, stomach disorders, skin disease, malarial fever and as tonic.3 Aerial parts were collected in July 2007 in Calabria (Italy) and exhaustively extracted with methanol. The total extract was fractionated to obtain a methanol and a n-hexane fraction. Moreover, in order to obtain the alkaloid fraction, the method reported by Kupeli et al.4 was used. The total phenol and flavonoid contents were determined by the Folin-Ciocalteau method and a method based on the formation of a flavonoid-aluminium complex, respectively.5 The antioxidant activity was screened by DPPH and β-carotene bleaching test.5 Methanol fraction exhibited the most promising radical scavenging activity with an IC50 value of 23.0 μg/mL. In β-carotene bleaching test the total extract showed the highest activity with an IC50 value of 2.8 μg/mL after 30 min of incubation. AChE and BChE inhibition was assessed by Ellman’s method.6 The alkaloid fraction showed the highest anticholinesterase activity with IC50 values of 18.6 and 54.7 μg/mL against AChE and BChE, respectively. GC-MS and GC analyses revealed the presence of berberine, palmatine, ossiberberine, berbamine and oxoglaucine as major components of the alkaloid fraction. n-Hexane fraction, characterized by terpenes, fatty acids and sterols as most common constituents, selectively inhibited BChE (IC50 value of 68.4 μg/mL). References 1 Gutteridge, J.M.C. Chem Biol Interact, 1994, 91, 133-140. 2 Loizzo, M.R., Tundis, R., Menichini, F., Menichini, F. Curr Med Chem, 2008, 15, 1209-1228. 3 Musumeci, R., Speciale, A., Costanzo, R., Annino, A., Ragusa, S., Rapisarda, A., Pappalardo, M.S., Iauk, L. Int J Antimic Agents, 2003, 22, 48-53. 4 E. Küpeli, M. Koᶊar, E. Yeilada, C.H. Baᶊer, C. Baᶊer. Life Sciences, 2002, 72, 645-657. 5 Conforti, F., Marrelli, M., Menichini, F., Tundis, R., Statti, G.A., Solimene, U., Menichini, F. J Enzyme Inhib Med Chem, 2011, 26 , 404-411. 6 Ellman, G.L., Courtney, K.D., Andres, V.Jr, Featherstone R.M. Biochem Pharmacol, 1961, 7, 88-95.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
