Bakana P, Laekeman G M, Totte J, Herman A G, Vlietinck A J
J Nat Prod. 1985 Sep-Oct;48(5):766-71. doi: 10.1021/np50041a008.
Five 2-acylindole alkaloids, isolated from the leaves of Pterotaberna inconspicua, were pharmacologically investigated. The major alkaloids methuenine and 16-epimethuenine showed some interesting pharmacological features, whereas the minor alkaloids including 6-oxomethuenine and methuenine N-oxide were almost devoid of these pharmacological properties. Methuenine, being the most potent, was characterized as a non competitive antagonist against acetylcholine (pD'2=5.10 +/- 0.11) and histamine (pD'2 = 5.13 +/- 0.14) in guinea-pig ileum. Its potency was comparable to that of papaverine. 16-Epimethuenine behaved as a weak antihistaminic (pA2 = 6.55 +/- 0.08). The stereochemistry of both components is discussed in relation to their pharmacological activity.
从隐脉翅子木叶中分离得到的5种2-酰基吲哚生物碱进行了药理研究。主要生物碱甲硫氨酸和16-表甲硫氨酸表现出一些有趣的药理特性，而包括6-氧代甲硫氨酸和甲硫氨酸N-氧化物在内的次要生物碱几乎没有这些药理性质。甲硫氨酸是最有效的，在豚鼠回肠中被表征为对乙酰胆碱（pD'2 = 5.10±0.11）和组胺（pD'2 = 5.13±0.14）的非竞争性拮抗剂。其效力与罂粟碱相当。16-表甲硫氨酸表现为弱抗组胺剂（pA2 = 6.55±0.08）。讨论了两种成分的立体化学与其药理活性的关系。
