Daniels M, James R A, Harris P E, Turner S J, Dewar J, Kendall-Taylor P
Department of Medicine, Medical School, Newcastle upon Tyne, UK.
Life Sci. 1991;49(16):1207-12. doi: 10.1016/0024-3205(91)90569-w.
L-363,586 is a cyclic, hexapeptide analogue of somatostatin-14 with potent inhibitory actions on rat growth hormone (GH) release in vitro. The studies reported here investigate the direct effects of L-363,586 on basal and growth hormone-releasing factor (GRF)-stimulated GH secretion from 3 human somatotrophinomas in dispersed cell culture. 1nM and 10nM L-363,586 inhibited both basal and GRF-stimulated GH release from cells of all 3 somatotrophinomas during a 2h treatment period, whilst 100nM L-363,586 had a prolonged inhibitory action on basal GH secretion from cells of 2 of the tumours throughout treatment and recovery periods. Rebound release of GH was observed with cells of 1 tumour following treatment with L-363,586 plus GRF. The actions of L-363,586 were similar to those of somatostatin-14. These data suggest that L-363,586 may have a role in the treatment of acromegaly.
L-363,586是一种环状六肽类似物,它是生长抑素-14的类似物,在体外对大鼠生长激素(GH)的释放具有强大的抑制作用。本文报道的研究探讨了L-363,586对分散细胞培养中3个人生长激素瘤基础分泌以及生长激素释放因子(GRF)刺激的生长激素分泌的直接影响。在2小时的处理期间,1 nM和10 nM的L-363,586抑制了所有3个生长激素瘤细胞的基础分泌以及GRF刺激的生长激素释放,而100 nM的L-363,586在整个处理和恢复期间对其中2个肿瘤细胞的基础生长激素分泌具有延长的抑制作用。在用L-363,586加GRF处理后,在1个肿瘤的细胞中观察到生长激素的反弹释放。L-363,586的作用与生长抑素-14的作用相似。这些数据表明L-363,586可能在肢端肥大症的治疗中发挥作用。