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Ryu, Geon-Seek,Park, Soo-Hee,Kim, Eun-Sook,Choi, Byoung-Wook,Ryu, Shi-Yong,Lee, Bong-Ho The Pharmaceutical Society of Korea 2003 Archives of Pharmacal Research Vol.26 No.10
Two known farnesylacetone derivatives (1 and 2) were isolated from the Korean brown alga Sargassum sagamianum off Jeju Island, Korea. Compounds 1 and 2 were identified as (5E,10Z)-6, 10, 14-trimethylpentadeca-5, 10-dien-2, 12-dione and (5E,9E,13E)-6, 10,4-trimethylpentadeca-5,9,13-trien-2,12-dione, respectively, by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with $IC_{50}$ values of 65.0∼48.0 and 34.0∼23.0 $\muM$, respectively.
Phosphonamidate Compounds for Butyrylcholinesterase Selective Inhibitors
Jintaek Oh,Jung-Youl Park,Kyoung Chan Park,Ji Hyun Hwang,박정호 대한화학회 2020 Bulletin of the Korean Chemical Society Vol.41 No.12
To find a new type of cholinergic drug, phosphonamidate compounds 18?32 were synthesized using a click reaction between propargylated-9,10-Dihydro-9-oxa-10-phosphaphenanthrene-10-oxide (DOPO, 2) and substituted benzyl azide. Their inhibitory activity against butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE) was evaluated. Compound 31 was the most active of the 15 compounds (IC50 = 3.14?±?0.02??M for equine BuChE), whose IC50 value was slightly lower than the IC50 value of galantamine (IC50 = 9.4?±?2.50 for equine BuChE).
Tryptamine–Triazole Hybrid Compounds for Selective Butyrylcholinesterase Inhibition
손민기,이하늘,전철민,강유정,박찬인,이근우,박정호 대한화학회 2019 Bulletin of the Korean Chemical Society Vol.40 No.6
Tryptamine?triazole hybrid compounds (11?18) were synthesized via click reaction between tryptamine azide and propargylated natural compounds. Their cholinesterase inhibitory activity was evaluated. Among the eight compounds, compound 11 showed the most potent inhibitory activity [IC50?=?0.42?±?0.29??M for equine butyrylcholinesterase (BuChE) and 1.96?±?0.15??M for human BuChE]. From the molecular modeling study, compound 11 was bound to the catalytic anionic site, anionic subsite, peripheral anionic subsite, acyl-binding pocket, and oxyanion hole of human or horse BuChE by forming a hairpin or U-shaped structure. The Lineweaver-Burk plot of compound 11 against BuChE suggests a mixed type of inhibition which corresponds well with the molecular modeling study.
Jian-Wei Dong,Le Cai,Xue-Jiao Li,Jia-Peng Wang,Rui-Feng Mei,Zhong-Tao Ding 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.12
Three new monoterpene phenylpropionic acidesters, illigerates A–C (1–3), and one new aporphinealkaloid, illigeranine (4), as well as four known ones,actinodaphnine (5), nordicentrine (6), 8-hydroxy carvacrol(7), and 3-hydroxy-a,4-dimethyl styrene (8), were isolatedfrom the tubers of Illigera aromatica. The structures of 1–4were identified by HRESIMS, 1D and 2D NMR, andelectronic circular dichroism spectra. Compound 1 potentlyinhibited NO production in LPS-stimulated RAW264.7cells with an IC50 value of 18.71 ± 0.85 lM; compound 1,3, and 4 showed moderate butyrylcholinesterase inhibitoryactivities with the IC50 values of 46.86 ± 0.65,53.51 ± 0.71, and 31.62 ± 1.15 lM, respectively. Compound4 showed weak AChE inhibitory activity with anIC50 value of 81.69 ± 2.07 lM, and compounds 5 and 6possessed moderate AChE inhibitory activities with theIC50 values of 47.74 ± 1.66 and 40.28 ± 2.73 lM,respectively. This paper provides a chemical structure andbioactive foundation for using I. aromatica as an herbalmedicine.