摘要
倍半萜类化合物在自然界中广泛存在,而硝基苯酯倍半萜类化合物较为罕见.迄今发现的12种天然来源硝基苯酯倍半萜均来自于海洋曲霉属Aspergillus真菌,是一类典型的海洋特征天然产物.该类天然产物显示了较好的抗肿瘤、抗病毒和抑制破骨细胞分化活性,特别是在治疗破骨细胞相关疾病中显示较好的药用开发价值.本文对硝基苯酯倍半萜的天然产物来源和化学结构、化学和生物合成、生物活性和药理机制进行了综述,并对其吸收(absorption)、分布(distribution)、代谢(metabolism)、排泄(excretion)及毒性(toxicity)(ADME/T)和类药性进行预测和讨论,为海洋来源硝基苯酯倍半萜类天然产物及其药用开发潜力提供较为全面的认识.
Abstract
Sesquiterpenoids are widely found in nature,while nitrobenzoyl sesquiterpenoids are relatively rare.Twelve natural nitrobenzoyl sesquiterpenoids were all derived from marine Aspergillus fungi,which are typical natural products with marine characteristics.These natural products exhibit good antitumor,antiviral,and inhibition of osteoclast differentiation activity,especially in the treatment of osteoclast-related diseases,showing good medicinal development value.This article reviews the natural product sources,chemical structure,chemical synthesis,biosynthesis,bioactivity,and pharmacological mechanisms of nitrobenzoyl sesquiterpenoids and predicts and discusses their absorption,distribution,metabolism,excretion,toxicity(ADME/T),and drug-likeness,providing a comprehensive understanding of the natural products of nitrobenzoyl sesquiterpenoids from marine sources and their potential for pharmaceutical development.
基金项目
广东特支计划本土创新创业团队项目(2019BT02Y262)
国家自然科学基金(U20A20101)
国家自然科学基金(81973235)