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[髓肽MP-2反向类似物的合成与性质]

[Synthesis and properties of the retro-analogue of myelopeptide MP-2].

作者信息

Fonina L A, Ovchinnikov M V, Gur'ianov S A, Sychev S V, Belevskaia R G, Treshchalina E M

出版信息

Bioorg Khim. 2005 May-Jun;31(3):239-44. doi: 10.1007/s11171-005-0029-1.

DOI:10.1007/s11171-005-0029-1
PMID:16004381
Abstract

The bone marrow myelopeptide MP-2 (Leu-Val-Val-Tyr-Pro-Trp), exhibiting antitumor activity, and its retro-analogue (Trp-Pro-Tyr-Val-Val-Leu) were synthesized, and their properties were studied. The in vitro and in vivo activities of retro-MP-2 were comparable with those of MP-2. Both peptides equally restored the functional activity of T-lymphocytes inhibited by toxins released by HL-60 cells and inhibited by 70-82% the growth of various types of transplantable solid tumors: Ca-755 adenocarcinoma of the mammary gland, Lewis adenocarcinoma of the lung, and S180 sarcoma. The positions and intensities of the Cotton effects in CD spectra of the MP-2 peptide and its retro-analogue in various solvents are almost indistinguishable. The positions of extrema and integral intensities of the amide I and amide A bands in IR spectra of both peptides were practically identical. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2005, vol. 31, no. 3; see also http://www.maik.ru.

摘要

合成了具有抗肿瘤活性的骨髓髓肽MP-2(亮氨酸-缬氨酸-缬氨酸-酪氨酸-脯氨酸-色氨酸)及其反向类似物(色氨酸-脯氨酸-酪氨酸-缬氨酸-缬氨酸-亮氨酸),并对其性质进行了研究。反向MP-2的体外和体内活性与MP-2相当。两种肽均能同等程度地恢复被HL-60细胞释放的毒素抑制的T淋巴细胞的功能活性,并抑制各种类型可移植实体瘤生长的70 - 82%:乳腺Ca-755腺癌、肺Lewis腺癌和S180肉瘤。MP-2肽及其反向类似物在各种溶剂中的圆二色光谱中科顿效应的位置和强度几乎无法区分。两种肽的红外光谱中酰胺I和酰胺A带的极值位置和积分强度实际上是相同的。论文英文版:《俄罗斯生物有机化学杂志》,2005年,第31卷,第3期;另见http://www.maik.ru。

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