Department of Biology, Faculty of Science, Princess Nourah Bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi Arabia.
Department of Chemistry, Faculty of Science, King Abdulaziz University, P.O. Box 80203, Jeddah 21589, Saudi Arabia.
Molecules. 2021 Jan 18;26(2):488. doi: 10.3390/molecules26020488.
By the end of the twentieth century, the interest in natural compounds as probable sources of drugs has declined and was replaced by other strategies such as molecular target-based drug discovery. However, in the recent times, natural compounds regained their position as extremely important source drug leads. Indole-containing compounds are under clinical use which includes vinblastine and vincristine (anticancer), atevirdine (anti-HIV), yohimbine (erectile dysfunction), reserpine (antihypertension), ajmalicine (vascular disorders), ajmaline (anti-arrhythmic), vincamine (vasodilator), etc. Monoterpene Indole Alkaloids (MIAs) deserve the curiosity and attention of researchers due to their chemical diversity and biological activities. These compounds were considered as an impending source of drug-lead. In this review 444 compounds, were identified from six genera belonging to the family Apocynaceae, will be discussed. These genera (, , , , and and ) consist of 400 members and represent 20% of Apocynaceae species. Only 30 (7.5%) species were investigated, whereas the rest are promising to be investigated. Eleven bioactivities, including antibacterial, antifungal, anti-inflammatory and immunosuppressant activities, were reported. Whereas cytotoxic effect represents 47% of the reported activities. Convincingly, the genera selected in this review are a wealthy source for future anticancer drug lead.
到 20 世纪末，人们对天然化合物作为可能的药物来源的兴趣下降，取而代之的是其他策略，如基于分子靶点的药物发现。然而，在最近的一段时间里，天然化合物重新成为极其重要的药物先导来源。含有吲哚的化合物已在临床上使用，包括长春碱和长春新碱（抗癌）、阿替韦啶（抗 HIV）、育亨宾（勃起功能障碍）、利血平（抗高血压）、阿马碱（血管疾病）、阿马林（抗心律失常）、长春酰胺（血管扩张剂）等。由于其化学多样性和生物活性，单萜吲哚生物碱（MIAs）值得研究人员的好奇和关注。这些化合物被认为是药物先导的潜在来源。在这篇综述中，从夹竹桃科的六个属中鉴定出了 444 种化合物，将进行讨论。这些属（，，，，和）由 400 个成员组成，占夹竹桃科物种的 20%。只有 30 种（7.5%）被调查，而其余的则有希望被调查。报道了 11 种生物活性，包括抗菌、抗真菌、抗炎和免疫抑制活性。而细胞毒性作用代表了报道的活性的 47%。令人信服的是，本综述中选择的属是未来抗癌药物先导的丰富来源。
