天然多环内过氧化物的抗原生动物和抗肿瘤活性：起源、结构和生物活性。
Antiprotozoal and Antitumor Activity of Natural Polycyclic Endoperoxides: Origin, Structures and Biological Activity.
机构信息
Centre for Applied Research, Innovation and Entrepreneurship, Lethbridge College, 3000 College Drive South, Lethbridge, AB T1K 1L6, Canada.
A.V. Zhirmunsky National Scientific Center of Marine Biology, 17 Palchevsky Str., 690041 Vladivostok, Russia.
出版信息
Molecules. 2021 Jan 28;26(3):686. doi: 10.3390/molecules26030686.
Polycyclic endoperoxides are rare natural metabolites found and isolated in plants, fungi, and marine invertebrates. The purpose of this review is a comparative analysis of the pharmacological potential of these natural products. According to PASS (Prediction of Activity Spectra for Substances) estimates, they are more likely to exhibit antiprotozoal and antitumor properties. Some of them are now widely used in clinical medicine. All polycyclic endoperoxides presented in this article demonstrate antiprotozoal activity and can be divided into three groups. The third group includes endoperoxides, which show weak antiprotozoal activity with a reliability of up to 70%, and this group includes only 1.1% of metabolites. The second group includes the largest number of endoperoxides, which are 65% and show average antiprotozoal activity with a confidence level of 70 to 90%. Lastly, the third group includes endoperoxides, which are 33.9% and show strong antiprotozoal activity with a confidence level of 90 to 99.6%. Interestingly, artemisinin and its analogs show strong antiprotozoal activity with 79 to 99.6% confidence against obligate intracellular parasites which belong to the genera Plasmodium, Toxoplasma, Leishmania, and Coccidia. In addition to antiprotozoal activities, polycyclic endoperoxides show antitumor activity in the proportion: 4.6% show weak activity with a reliability of up to 70%, 65.6% show an average activity with a reliability of 70 to 90%, and 29.8% show strong activity with a reliability of 90 to 98.3%. It should also be noted that some polycyclic endoperoxides, in addition to antiprotozoal and antitumor properties, show other strong activities with a confidence level of 90 to 97%. These include antifungal activity against the genera Aspergillus, Candida, and Cryptococcus, as well as anti-inflammatory activity. This review provides insights on further utilization of polycyclic endoperoxides by medicinal chemists, pharmacologists, and the pharmaceutical industry.
多环过氧化物是在植物、真菌和海洋无脊椎动物中发现和分离出来的罕见天然代谢产物。本文旨在对这些天然产物的药理潜力进行比较分析。根据 PASS（物质活性预测系统）的估计，它们更有可能表现出抗原生动物和抗肿瘤的特性。其中一些现已广泛应用于临床医学。本文介绍的所有多环过氧化物都表现出抗原生动物的活性，可分为三组。第三组包括过氧化物，其抗原生动物的活性较弱，可靠性为 70%，这一组只包含 1.1%的代谢物。第二组包括数量最多的过氧化物，占 65%，具有中等抗原生动物的活性，置信度为 70%至 90%。最后，第三组包括过氧化物，占 33.9%，具有很强的抗原生动物的活性，置信度为 90%至 99.6%。有趣的是，青蒿素及其类似物对属于疟原虫、弓形虫、利什曼原虫和球虫属的专性细胞内寄生虫具有很强的抗原生动物活性，置信度为 79%至 99.6%。除了抗原生动物的活性外，多环过氧化物还具有抗肿瘤活性，其比例为：4.6%显示活性较弱，可靠性为 70%以下，65.6%显示活性中等，可靠性为 70%至 90%，29.8%显示活性较强，可靠性为 90%至 98.3%。还应注意的是，一些多环过氧化物除了具有抗原生动物和抗肿瘤的特性外，还具有其他具有 90%至 97%置信度的强大活性。这些活性包括抗真菌活性，针对曲霉属、念珠菌属和隐球菌属，以及抗炎活性。本文为药用化学家、药理学家和制药行业进一步利用多环过氧化物提供了思路。
Zotero 插件