Novel relationship between the antifungal activity and cytotoxicity of marine-derived metabolite xestoquinone and its family
Novel relationship between the antifungal activity and cytotoxicity of marine-derived metabolite xestoquinone and its family
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DOI：
10.1271/bbb.69.1749
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发表时间：
2005-09-01
影响因子：
1.6
通讯作者：
Ojika, M
中科院分区：
文献类型：
--
作者：
Nakamura, M;Kakuda, T;Ojika, M
.雄醌和相关代谢物（雄醌家族）存在于海绵中，已知具有多种生物活性。在这项研究中，第一次全面的抗真菌活性进行了评价雄甾醌和9个天然和非天然类似物的细胞毒性比较。对两种人鳞状细胞癌细胞系A431和Nakata的细胞毒性表明，多环分子的末端醌结构是重要的（xestoquinone等）。并且在相对末端的C-3处酮基的存在显著地降低了活性（卤代喹酮等）。与此相反，在C-3的酮基团增强了对植物病原体辣椒疫霉的抗真菌活性，无论醌部分的存在。雄甾醌类化合物的细胞毒活性与抗真菌活性呈负相关。
. Xestoquinone and related metabolites (the xestoquinone family) occur in marine sponges and are known to show a variety of biological activities. In this study, the first comprehensive evaluation of antifungal activity was performed for xestoquinone and nine natural and unnatural analogues in comparison with their cytotoxicity. The cytotoxicity against two human squamous cell carcinoma cell lines, A431 and Nakata, indicated that the terminal quinone structure of the polycyclic molecules was important (xestoquinone, etc.) and that the presence of a ketone group at C-3 of the opposite terminus dramatically diminished the activity (halenaquinone, etc.). In contrast, a ketone group at C-3 enhanced the antifungal activity against the plant pathogen, Phytophthora capsici, regardless of the presence of a quinone moiety. The cytotoxicity and antifungal activity of the xestoquinone family were negatively correlated with each other.