Anti-plasmodial and cholinesterase inhibiting activities of some constituents of Psorospermum glaberrimum.
Glaberianthrone (1), a new bianthrone was isolated from the hexane extract of the stem bark of Psorospermum glaberrimum together with thirteen known compounds: 3-geranyloxyemodin anthrone (2), friedelan-3-one (3), 3-prenyloxyemodin anthrone (4), 3-geranyloxyemodin (5), 3-prenyloxyemodin (6), friedelan-3-ol (7), acetylvismione D (8), betulinic acid (9), 2-geranylemodin (10), bianthrone A2b (11), bianthrone 1a (12), emodin (13) and 2-prenylemodin (14). The structures of the isolated compounds were established by means of spectroscopic methods. The extracts and the isolated compounds were tested in vitro for their anti-plasmodial activity against Plasmodium falciparum (chloroquine resistant strain W2) and for their acetyl- and butyrylcholinesterase inhibitory properties. The n-hexane extract showed good anti-plasmodial activity against P. falciparum W2 strain, with IC(50) of 0.87 microg/ml. It also exhibited 65.5% and 98.2% of acetyl- and butyrylcholinesterase inhibition at 0.2 mg/ml, respectively. Compounds 2 and 8 showed the best potencies against P. falciparum W2 strain with IC(50) of 1.68 microM and 0.12 microM, (0.66 microg/ml and 0.054 microg/ml) respectively. All tested compounds showed good butyrylcholinesterase inhibition activities with compound 12 displaying the best potency (IC(50) 9.25+/-0.25 microM). All the tested compounds showed weak inhibitory activity against acetylcholinesterase.
Ndjakou Lenta
Bruno
B
Department of Chemistry, Organic and Bioorganic Chemistry, Bielefeld University, Bielefeld, Germany. lentabruno@yahoo.fr
Devkota
Krishna Prasad
KP
Ngouela
Silvère
S
Fekam Boyom
Fabrice
F
Naz
Quamar
Q
Choudhary
Muhammad Iqbal
MI
Tsamo
Etienne
E
Rosenthal
Philip Jon
PJ
Sewald
Norbert
N
D000110:Acetylcholinesterase / Q000378:metabolism; D000818:Animals; D000873:Anthracenes / Q000302:isolation & purification* / Q000494:pharmacology*; D000962:Antimalarials / Q000302:isolation & purification* / Q000494:pharmacology*; D002091:Butyrylcholinesterase / Q000378:metabolism; D002163:Cameroon; D002800:Cholinesterase Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology*; D002855:Chromatography, Thin Layer; D028084:Clusiaceae / Q000737:chemistry*; D004912:Erythrocytes / Q000187:drug effects / Q000469:parasitology; D006801:Humans; D006868:Hydrolysis; D009682:Magnetic Resonance Spectroscopy; D024301:Plant Bark / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects / Q000201:enzymology; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet
D000873:Anthracenes; D000962:Antimalarials; D002800:Cholinesterase Inhibitors; C527327:bianthrone A2b; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase