Masuda M, Nakashima H, Ueda T, Naba H, Ikoma R, Otaka A, Terakawa Y, Tamamura H, Ibuka T, Murakami T
Faculty of Pharmaceutical Sciences, Kyoto University, Japan.
Biochem Biophys Res Commun. 1992 Dec 15;189(2):845-50. doi: 10.1016/0006-291x(92)92280-b.
Tachyplesin and polyphemusin are antimicrobial peptides recently isolated from the hemocytes of horseshoe crabs (Tachypleus tridentatus and Limulus polyphemus). We synthesized them and their analogs and examined their antiviral activity against human immunodeficiency virus (HIV) type 1 in vitro. The infection of human T cells with the virus was markedly inhibited by some of them at low concentrations. In this structure-activity study, we found that [Tyr5,12, Lys7]-polyphemusin II, which was designated as T22, had extremely high anti-HIV activity. Its 50% inhibitory concentration (EC50) was 0.008 micrograms/ml, while its 50% cytotoxic concentration (CC50) was 54 micrograms/ml and these values were comparable to those of AZT. This result indicates that T22 would be a potential candidate for the therapy of HIV infection.
鲎素和鲎血细胞素是最近从鲎（中国鲎和美洲鲎）血细胞中分离出的抗菌肽。我们合成了它们及其类似物，并在体外检测了它们对1型人类免疫缺陷病毒（HIV）的抗病毒活性。其中一些在低浓度下就能显著抑制该病毒对人T细胞的感染。在这项构效关系研究中，我们发现被命名为T22的[酪氨酸5,12，赖氨酸7] - 鲎血细胞素II具有极高的抗HIV活性。其50%抑制浓度（EC50）为0.008微克/毫升，而其50%细胞毒性浓度（CC50）为54微克/毫升，这些值与齐多夫定相当。这一结果表明T22可能是治疗HIV感染的潜在候选药物。
