Sirimangkalakitti_2015_Nat.Prod.Commun_10_1945

Reference

Title : Bromotyrosine Alkaloids with Acetylcholinesterase Inhibitory Activity from the Thai Sponge Acanthodendrilla sp - Sirimangkalakitti_2015_Nat.Prod.Commun_10_1945
Author(s) : Sirimangkalakitti N , Olatunji OJ , Changwichit K , Saesong T , Chamni S , Chanvorachote P , Ingkaninan K , Plubrukarn A , Suwanborirux K
Ref : Nat Prod Commun , 10 :1945 , 2015
Abstract :

Twenty bromotyrosine alkaloids, including a new compound, 13-oxosubereamolline D (5), were isolated from the Thai sponge Acanthodendrilla sp. Their structures were determined by analyses of 1D- and 2D-NMR, high-resolution mass, and circular dichroism data. The complete 1H and 13C NMR assignments of 5,7beta-dichlorocavernicolin (19) and 5,7alpha-dichlorocavernicolin (20) are described herein for the first time. The acetylcholinesterase (AChE) inhibitory activity of all isolated compounds was evaluated. Only homoaerothionin (7) and fistularin 1 (10) exhibited inhibitory activity against human recombinant AChE (hrAChE) with IC50s of 4.5 and 47.5 microM, respectively. The hrAChE inhibition kinetics of 7, the most potent alkaloid, showed increased Km and unchanged Vmaxvalues, suggesting its competitive mode of inhibition. The spirocyclohexadienylisoxazole and the length of the alkyl diamine linkage were proposed as the crucial parts for its strong inhibitory activity. This finding indicates a therapeutic potential for 7 in acetylcholine-related diseases, most importantly Alzheimer's disease.

PubMedSearch : Sirimangkalakitti_2015_Nat.Prod.Commun_10_1945
PubMedID: 26749833

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Citations formats

Sirimangkalakitti N, Olatunji OJ, Changwichit K, Saesong T, Chamni S, Chanvorachote P, Ingkaninan K, Plubrukarn A, Suwanborirux K (2015)
Bromotyrosine Alkaloids with Acetylcholinesterase Inhibitory Activity from the Thai Sponge Acanthodendrilla sp
Nat Prod Commun 10 :1945

Sirimangkalakitti N, Olatunji OJ, Changwichit K, Saesong T, Chamni S, Chanvorachote P, Ingkaninan K, Plubrukarn A, Suwanborirux K (2015)
Nat Prod Commun 10 :1945