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DOI: 10.1055/s-0036-1596425
Anti-platelet activity studies on compounds of neolignan from Myristica fragrans
Publication History
Publication Date:
14 December 2016 (online)
Platelets play a critical role in pathogenesis of cardiovascular disorders and strokes. The inhibition of platelet function is beneficial for the treatment and prevention of these diseases. A kind of neolignan, erythro-(7S,8R)-7-acetoxy-3,4,3′,5′-tetramethoxy-8-O-4′-neolignan (EATN), has already known activity of inhibition for thrombin- and platelet-activating factor (PAF)-induced platelet aggregation without affecting platelet damage [1]. Furthermore study, we investigated the anti-platelet activity a series of neolignans isolated from Myristica fragrans, using human platelets. The chemical constituents were isolated by various column chromatographic methods and HPLC, structurally elucidated by 1D, 2D NMR [2]. A series of neoligans: Erythro-(7S,8R)-7-acetoxy-3,4,3',5'-tetramethoxy-8-O-4'-neolignan (1), Erythro-2-(4-allyl-2',6'-dimethoxyphenoxy)-1-(3, 4-dimethoxyphenyl) propan-1-ol (2), Erythro-2-(4-allyl-2, 6-dimethoxyphenoxy)-1-(4-hydroxy-3-methoxyphenyl)-propan-1-ol (3), Erythro-2-(4-allyl-2, 6-dimethoxyphenoxy)-1-(3, 4, 5-trimethoxyphenyl) propan-1-ol (4), Threo-2-(4-allyl-2, 6-dimethoxyphenoxy)-1-(3-methoxy-5-hydroxy-phenyl) propan-1-ol (5). Their anti-platelet activity were evaluated. Of them, compound 1 showed the strong IC50 value of 3.2 ± 0.4, so it has bio-activity for anti-platelet.
R1 |
R2 |
R3 |
R4 |
|
1 |
OMe |
OMe |
H |
OAc |
2 |
OMe |
OMe |
H |
OH |
3 |
OMe |
OH |
H |
OH |
4 |
OMe |
OMe |
OMe |
OH |
5 |
OMe |
H |
OH |
OH |
Compound |
1 |
2 |
3 |
4 |
5 |
IC50 |
3.2 ± 0.4 |
> 20 |
> 20 |
> 20 |
> 20 |
Acknowledgements: This research was supported by the National Research Foundation of Korea (NRF), funded by the Ministry of Science, ICT and Future Planning (NRF-2015M3A9A5031271).
Keywords: Myristica fragrans, neolignan, anti-platelet, thrombin, platelet-activating factor.
References:
[1] Kang JW, Min BS, Lee JH. Anti-platelet Activity of Erythro-(7S,8R)-7-acetoxy-3,4,3′,5′-tetramethoxy-8-O-4′-neolignan from Myristica fragrans. Phytother Res 2013; 27: 1694 – 1699
[2] Yang XW, Huang X, Ahmat M. New neolignan from seed of Myristica fragrans. Zhongguo Zhong Yao Za Zhi 2008; 33: 397 – 402