FUNGAL METABOLITES .12. POTENT IMMUNOSUPPRESSANT, 14-DEOXOMYRIOCIN, (2S,3R,4R)-(E)-2-AMINO-3,4-DIHYDROXY-2-HYDROXYMETHYLEICOS-6-ENOIC ACID AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF MYRIOCIN DERIVATIVES
FUNGAL METABOLITES .12. POTENT IMMUNOSUPPRESSANT, 14-DEOXOMYRIOCIN, (2S,3R,4R)-(E)-2-AMINO-3,4-DIHYDROXY-2-HYDROXYMETHYLEICOS-6-ENOIC ACID AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF MYRIOCIN DERIVATIVES
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DOI：
10.7164/antibiotics.47.216
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发表时间：
1994-02-01
影响因子：
3.3
通讯作者：
OKUMOTO, T
中科院分区：
文献类型：
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作者：
FUJITA, T;INOUE, K;OKUMOTO, T
为了研究其构效关系，制备了14个肉豆蔻菌素((2S，3R，4R)-(E)-2-amino-3，4-dihydroxy-2-hydroxymethyl-14-oxoeicos-6-enoic酸的衍生物，并在体外检测了它们对小鼠异基因混合淋巴细胞反应的免疫抑制活性。其中，14-脱氧霉素(((2S，3R，4R)-(E)-2-amino-3，4-dihydroxy-2-hydroxymethyl-eicos-6-enoic酸)的药效最强。它还抑制小鼠腹腔注射后产生的同种反应性细胞毒性T淋巴细胞，其效力是Myriocin的10倍。
In order to investigate the structure-activity relationships, fourteen derivatives of myriocin ((2S,3R,4R)-(E)-2-amino-3,4-dihydroxy-2-hydroxymethyl-14-oxoeicos-6-enoic acid) were prepared and examined for immunosuppressive activity on mouse allogeneic mixed lymphocyte reaction in vitro. Among them, 14-deoxomyriocin ((2S,3R,4R)-(E)-2-amino-3,4-dihydroxy-2-hydroxymethyl-eicos-6-enoic acid) was the most potent. It also suppressed the generation of allo-reactive cytotoxic T lymphocytes in mice upon intraperitoneal administration, with a potency 10-fold greater than that of myriocin.