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A unique high-diversity natural product collection as a reservoir of new therapeutic leads
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2020-12-11 , DOI: 10.1039/d0qo01210f Francesca Ghirga 1, 2, 3, 4 , Deborah Quaglio 4, 5, 6, 7, 8 , Mattia Mori 6, 9, 10, 11, 12 , Silvia Cammarone 4, 5, 6, 7, 8 , Antonia Iazzetti 4, 5, 6, 7, 8 , Antonella Goggiamani 4, 5, 6, 7, 8 , Cinzia Ingallina 4, 5, 6, 7, 8 , Bruno Botta 4, 5, 6, 7, 8 , Andrea Calcaterra 4, 5, 6, 7, 8
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2020-12-11 , DOI: 10.1039/d0qo01210f Francesca Ghirga 1, 2, 3, 4 , Deborah Quaglio 4, 5, 6, 7, 8 , Mattia Mori 6, 9, 10, 11, 12 , Silvia Cammarone 4, 5, 6, 7, 8 , Antonia Iazzetti 4, 5, 6, 7, 8 , Antonella Goggiamani 4, 5, 6, 7, 8 , Cinzia Ingallina 4, 5, 6, 7, 8 , Bruno Botta 4, 5, 6, 7, 8 , Andrea Calcaterra 4, 5, 6, 7, 8
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Plants represent a rich source of structurally diverse secondary metabolites, which can be exploited in the development of new clinically important compounds. Indeed, due to their biodiversity, medicinal plants represent the largest library of compounds that has ever existed. To date less than 1% of this vast biodiversity has been exploited in drug discovery, due to several factors, including the lack of an appropriate multidisciplinary perspective. Here we review the successful application of computer-aided methods in screening a unique and high-diversity in house collection library composed of around 1000 individual natural products, isolated mainly from indigenous plants collected in biodiversity-rich countries, especially of the tropics and subtropics, and enlarged with their semi-synthetic and synthetic derivatives, as well as plant material extracts, up to around 2000 components. During the last ten years, the in house library has provided several lead compounds that have been developed, and in some cases patented, as anticancer and antimicrobial agents. The main classes of the library are described, including (but not limited to) alkaloids, terpenoids, Diels–Alder-type adducts, isoflavones, chalcones, and cannabinoids. The main focus is on the chemical characteristics and biological activity of these identified compounds, with particular attention being given to those currently under patent or in the preclinical phase. We also assess the use of computer-aided methods in screening this unique and diverse in house collection of natural products that, over the last ten years, has provided some lead compounds that have been developed, and in some cases patented, as anticancer and antimicrobial agents. Finally, this review highlights the potential use of plant food extracts as a source of nutraceuticals and functional foods. The multidisciplinary approach described herein may further motivate research groups involved in natural product chemistry to potentially benefit from a limitless source of novel bioactive compounds.
中文翻译：
独特的高多样性天然产物收藏品，可作为新治疗线索的储存库
植物代表了结构多样的次级代谢产物的丰富来源，可用于开发具有临床意义的新化合物。确实，由于其生物多样性，药用植物代表了迄今存在的最大的化合物库。迄今为止，由于多种因素，包括缺乏适当的多学科视角，这种广泛的生物多样性中只有不到1％被用于药物开发。在这里，我们回顾了计算机辅助方法在筛选房屋中独特且高度多样性的成功应用馆藏由大约1000种天然产品组成，主要从生物多样性丰富的国家（尤其是热带和亚热带地区）收集的本土植物中分离，并以其半合成和合成衍生物以及植物材料提取物扩大，直至大约2000个组件。在过去的十年中文库提供了几种已开发的先导化合物，并在某些情况下获得了专利，作为抗癌和抗菌剂。描述了该库的主要类别，包括（但不限于）生物碱，萜类化合物，狄尔斯-阿尔德型加合物，异黄酮，查耳酮和大麻素。主要重点是这些鉴定出的化合物的化学特性和生物学活性，尤其要注意那些目前处于专利保护之下或处于临床前阶段的化合物。我们还评估了计算机辅助方法在筛选内部这种独特而多样的情况下的使用在过去十年中，我们提供了一系列天然产物，这些产物提供了一些先导化合物，这些先导化合物已被开发出来，并在某些情况下获得了专利，作为抗癌和抗菌剂。最后，这篇评论强调了植物性食品提取物作为保健食品和功能性食品来源的潜在用途。本文所述的多学科方法可以进一步激发参与天然产物化学的研究小组潜在地受益于无限量的新型生物活性化合物。
更新日期：2021-01-06
中文翻译：
独特的高多样性天然产物收藏品，可作为新治疗线索的储存库
植物代表了结构多样的次级代谢产物的丰富来源，可用于开发具有临床意义的新化合物。确实，由于其生物多样性，药用植物代表了迄今存在的最大的化合物库。迄今为止，由于多种因素，包括缺乏适当的多学科视角，这种广泛的生物多样性中只有不到1％被用于药物开发。在这里，我们回顾了计算机辅助方法在筛选房屋中独特且高度多样性的成功应用馆藏由大约1000种天然产品组成，主要从生物多样性丰富的国家（尤其是热带和亚热带地区）收集的本土植物中分离，并以其半合成和合成衍生物以及植物材料提取物扩大，直至大约2000个组件。在过去的十年中文库提供了几种已开发的先导化合物，并在某些情况下获得了专利，作为抗癌和抗菌剂。描述了该库的主要类别，包括（但不限于）生物碱，萜类化合物，狄尔斯-阿尔德型加合物，异黄酮，查耳酮和大麻素。主要重点是这些鉴定出的化合物的化学特性和生物学活性，尤其要注意那些目前处于专利保护之下或处于临床前阶段的化合物。我们还评估了计算机辅助方法在筛选内部这种独特而多样的情况下的使用在过去十年中，我们提供了一系列天然产物，这些产物提供了一些先导化合物，这些先导化合物已被开发出来，并在某些情况下获得了专利，作为抗癌和抗菌剂。最后，这篇评论强调了植物性食品提取物作为保健食品和功能性食品来源的潜在用途。本文所述的多学科方法可以进一步激发参与天然产物化学的研究小组潜在地受益于无限量的新型生物活性化合物。
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