485-19-8 牛心果碱

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名称和标识

中文名: 牛心果碱
英文名: (S)-Reticuline
CAS号: 485-19-8
分子式: C19H23NO4
分子量: 329.39
中文别名: (S)-1-(3-羟基-4-甲氧基苄基)-6-甲氧基-2-甲基-1,2,3,4-四氢异喹啉-7-醇; 牛心果鹼; 牛心果; 瑞枯灵; 网状番荔枝碱; 网脉番荔枝碱; 化合物 T4243
英文别名: (S)-1-(3-Hydroxy-4-methoxybenzyl)-6-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-ol; (S)-1,2,3,4-tetrahydro-1-[(3-hydroxy-4-methoxyphenyl)methyl]-6-methoxy-2-methylisoquinolin-7-ol; (1S)-1-[(3-hydroxy-4-methoxy-phenyl)methyl]-6-methoxy-2-methyl-3,4-dihydro-1H-isoquinolin-7-ol; reticuline; [1S,(+)]-1,2,3,4-Tetrahydro-1-[(3-hydroxy-4-methoxyphenyl)methyl]-6-methoxy-2-methylisoquinolin-7-ol; [1S,(+)]-1,2,3,4-Tetrahydro-1-[(3-hydroxy-4-methoxyphenyl)methyl]-6-methoxy-2-methylisoquinoline-7-ol; 2-Methoxy-5-[[(1S)-2-methyl-6-methoxy-7-hydroxy-1,2,3,4-tetrahydroisoquinoline]-1-ylmethyl]phenol; 1-(3-Hydroxy-4-methoxybenzyl)-6-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-ol; 1,2,3,4-Tetrahydro-1-[(3-hydroxy-4-methoxyphenyl)methyl]-6-methoxy-2-methyl-7-isoquinolinol; 2-Methyl-7-hydroxy-6-methoxy-1-(3-hydroxy-4-methoxybenzyl)-1,2,3,4-tetrahydroisoquinoline; 1-(3-Hydroxy-4-methoxybenzyl)-6-methoxy-2-methyl-1,2,3,4-tetrahydro-7-isoquinolinol; Coclanoline; (±)-Reticuline

用途与制备

生物活性 Reticuline 分离自 Litsea cubeba，通过 JAK2/STAT3 和 NF-κB 信号通路显示抗炎作用。Reticuline 还可抑制 TNF-α 和 IL-6 的 mRNA 表达，并降低 JAK2 和 STAT3 的磷酸化水平。Reticuline 具有心血管作用。
靶点 JAK2 STAT3 NF-κB
体外研究 Reticuline (3 μM, 30 μM, 300 μM, 900 μM and 1.5 mM) inhibits in a concentration-dependent manner the contractions induced by Phenylephrine (1 μM), KCl (80 mM) and KCl (30 mM), (IC 50 =40±10, 240±40 and 300±40 μM, respectively) in isolated rat aortic rings with intact endothelium. Reticuline (3 μM, 30 μM, 300 μM, 900 μM and 1.5 mM) antagonizes CaCl 2 -induced contractions, and also inhibits the intracellular calcium dependent transient contractions induced by Norepinephrine (1μM), but not those induced by Caffeine (20 mM).
体内研究 Reticuline (5, 10 and 20 mg/kg, i. v., randomly) injections produced an intense hypotension in normotensive rats. The hypotensive effect of Reticuline is probably due to a peripheral vasodilation in consequence of: 1) muscarinic stimulation and NOS activation in the vascular endothelium, 2) voltage-dependent Ca 2+ channel blockade and/or 3) inhibition of Ca 2+ release from norepinephrine-sensitive intracellular stores.
化学性质白色粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于印防己，山胡椒，凹叶厚朴。
瑞枯灵具有抗血小板聚集，抑制子宫平滑肌收缩的作用。

医药