School of Medical Engineering, Hefei University of Technology, Hefei, P. R. China.
Curr Med Chem. 2012;19(16):2652-64. doi: 10.2174/092986712800493020.
The bryostatins, powerful protein kinase C (PKC) agonists, are a family of complex macrolactone natural products. They are originally isolated from the marine bryozoan Bugula neritina. So far tweenty bryostatins have been obtained naturally and exhibit a remarkable range of biological activities, including antineoplastic activity, synergistic chemotheoreputic activity, cognition and memory enhancement, etc. Of the 20 known members, the most extensively studied is bryostatin 1. The effects of bryostatin 1 are mainly linked to its ability of selectively modulating the function of various individual protein kinase C (PKC) isozymes. Moreover, bryostatin 1, or in combination with other agents, has been proposed for phase I and phase II clinical trials. The bryostatins have excellent biological properties, but are scarce in nature. Therefore, it has attracted considerable interests in structural modification over the past two decades. In this review, we will attempt to summarize the main developments that have occurred in the structure-activity relationship and biology of bryostatins over the period 1982-2011.
岩沙海葵毒素是一组强大的蛋白激酶 C（PKC）激动剂，属于复杂大环内酯类天然产物。它们最初是从海洋苔藓虫 Bugula neritina 中分离得到的。迄今为止，已从自然界中获得了 20 种岩沙海葵毒素，它们具有广泛的生物学活性，包括抗肿瘤活性、协同化疗活性、认知和记忆增强等。在 20 种已知成员中，研究最多的是岩沙海葵毒素 1。岩沙海葵毒素 1 的作用主要与其选择性调节各种单个蛋白激酶 C（PKC）同工酶功能的能力有关。此外，岩沙海葵毒素 1 或与其他药物联合使用，已被提议用于 I 期和 II 期临床试验。岩沙海葵毒素具有优异的生物学特性，但在自然界中却很稀缺。因此，在过去的二十年中，对其结构修饰引起了相当大的关注。在本文中，我们将尝试总结 1982 年至 2011 年间岩沙海葵毒素在结构-活性关系和生物学方面的主要进展。
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