Leishmanicidal and Cholinesterase Inhibiting Activities of Phenolic Compounds from Allanblackia monticola and Symphonia globulifera

Molecules

Bruno Ndjakou Lenta¹  Catherine Vonthron-Sénécheau¹  Bernard Weniger¹  Krishna Prasad Devkota¹  Joseph Ngoupayo¹  Marcel Kaiser¹  Qamar Naz¹  Muhammad Iqbal Choudhary¹  Etienne Tsamo¹ 

[1] ¹Department of Chemistry, Higher Teachers’ Training College, University of Yaoundé 1, P.O. Box 47, Yaoundé, Cameroon

关键词: Allanblackia monticola;    Symphonia globulifera;    Phenolic compounds;    Leishmanicidal;    Anticholinesterase;   

DOI  :  10.3390/12081548

来源: mdpi

【 摘 要 】

In a preliminary antiprotozoal screening of several Clusiaceae species, the methanolic extracts of Allanblackia monticola and Symphonia globulifera showed high in vitro leishmanicidal activity. Further bioguided phytochemical investigation led to the isolation of four benzophenones: guttiferone A (1), garcinol (2), cambogin (3) and guttiferone F (4), along with three xanthones: allanxanthone A (5), xanthone V₁ (6) and globulixanthone C (7) as active constituents. Compounds 1 and 6 were isolated from S. globulifera leaves, while compounds 2-5 were obtained from A. monticola fruits. Guttiferone A (1) and F (4) showed particulary strong leishmanicidal activity in vitro, with IC₅₀ values (0.2 μM and 0.16 μM, respectively) comparable to that of the reference compound, miltefosine (0.46 μM). Although the leishmanicidal activity is promising, the cytotoxicity profile of these compounds prevent at this state further in vivo biological evaluation. In addition, all the isolated compounds were tested in vitro for their anticholinesterase properties. The four benzophenones showed potent anticholinesterase properties towards acetylcholinesterase (AChE) and butylcholinesterase (AChE). For AChE, the IC₅₀ value (0.66 μM) of garcinol (2) was almost equal to that of the reference compound galanthamine (0.50 μM). Furthermore, guttiferone A (1) and guttiferone F (4) (IC₅₀ = 2.77 and 3.50 μM, respectively) were more active than galanthamine (IC₅₀ = 8.5) against BChE.

【 授权许可】

CC BY   
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