Sponge-derived neurotoxic substances : Structure, Bioactivity, and their cellular localization.

在本研究中，我们从冲绳海绵Axinissa aculeate中鉴定出新的多胺，这些多胺可以调节配体与NMDA型谷氨酸受体的结合。这些多胺也可能是参与海绵中二氧化硅生物矿化的一个因素。从同一提取物中，我们发现了在亚结构中含有多胺的新肽，并命名为aculeines。这种新型高修饰肽在小鼠中表现出强烈的惊厥作用。我们还从密克罗尼西亚的海绵中分离到了一种新的嘌呤——cribrocharina olemda。cribropriin诱导大鼠海马神经元出现癫痫样自发电流。海绵树ailia sp.的亲脂提取物含有树ailol作为小鼠癫痫诱导因子。从冲绳海绵海绵中分离出蛋白毒素鸟耳脂苷。我们确定了索蒂苷的末端氨基酸序列。我们确定了一个兴奋性氨基酸乙酰索蒂苷定位的细胞。根据其16S rDNA序列鉴定该细胞为蓝细菌Synechosystis sp .，这表明dysiherbine是一种蓝细菌产物，该物种还含有6-磷脂化脱氧诺吉霉素衍生物。对一种表现出AMPAKine样活性的水提取物的研究导致了生物活性组分的分离。其中一种活性组分根据其血凝活性被证明含有凝集素。含有凝集素的部分表现出类似ampakine的活性，而含有小分子的部分则负责诱导小鼠癫痫发作。预先研究表明，诱导小鼠抽搐的有毒提取物是神经元活性化合物的有趣来源，可以成为神经生物学的有用工具。

In the present study, we identified new polyamines from a Okinawan sponge Axinissa aculeate that modulate ligand binding to NMDA type glutamate receptors. These polyamines may also function as a factor involved in silica biomineralization in the sponge. From the same extract, we identified new peptides containing polyamine in the substructure and named aculeines. This novel highly modified peptide showed strong convulsant actions in mice. We also isolated Cribropurine, a new purine from a Micronesian sponge Chribrocharina olemda. Cribroprine elicited a seizure-like spontaneous current in rat hippocampal neuron. A lipophilic extract of the sponge Raspailia sp. contained raspailol as seizure-inducing factor in mice. Okinawan sponge Spongosolites afforded an isolation of protein toxin Soritesidine. A terminal amino acid sequence for sotitesidine was determined We identified a cell where an excitatory amino acid dysiherbaine was localized. The cell was identified to be a cyanobacteria Synechosystis sp based on its 16S rDNA sequence This result suggested that dysiherbaine was a cyanobacterial product This species also contained 6-phospholylated deoxynojirimycin derivatives. Investigation of an aqueous extract that exhibited AMPAKine like activity resulted in separation of bioactive fractions. One of the active fractions was shown to contain lectin based on its hemagglutinating activity. The lectin- containing fraction showed AMPAKine-like activity whereas the fraction containing small molecule was responsible for seizure-induction in mice. The preset study demonstrated that toxic extracts that induce convulsion in mice is a interesting source of neuron active compounds that can be useful tools in neurobiology.