New glycosylated derivatives of versipelostatin, the GRP78/Bip molecular chaperone down-regulator, from Streptomyces versipellis 4083-SVS6
New glycosylated derivatives of versipelostatin, the GRP78/Bip molecular chaperone down-regulator, from Streptomyces versipellis 4083-SVS6
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DOI：
10.1039/b817312e
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发表时间：
2009-01-01
影响因子：
3.2
通讯作者：
Kuzuyama, Tomohisa
中科院分区：
文献类型：
--
作者：
Zhao, Ping;Ueda, Jun-ya;Kuzuyama, Tomohisa
从Streptomyces versipellis 4083-SVS 6发酵液中分离得到4个新的versipelostatin糖基化衍生物（1），即versipelostatins B-E（2-5）。评价了分离的化合物对2-脱氧葡萄糖诱导的分子伴侣GRP 78表达的抑制活性。在5个versipelostatin家族成员中，1和4更有效，IC 50值为3.5和4.3 μ M。这些结果表明，在糖部分的α-L-oleandropyranosyl（1 -> 4）-β-D-digitoxopyranosyl残基可能在下调2-脱氧葡萄糖诱导的GRP 78表达中起重要作用。
Four novel glycosylated derivatives of versipelostatin (1), versipelostatins B-E (2-5), were isolated from the culture broth of Streptomyces versipellis 4083-SVS6. The inhibitory activities of the isolated compounds against the expression of molecular chaperone GRP78 induced by 2-deoxyglucose were evaluated. Of the five versipelostatin family members, 1 and 4 were the more potent with IC50 values of 3.5 and 4.3 mu M. These results suggest that the alpha-L-oleandropyranosyl (1 -> 4)-beta-D-digitoxopyranosyl residue in the sugar moiety may play an important role in down-regulating GRP78 expression induced by 2-deoxyglucose.