Laboratory of Organic & Medicinal Chemistry, Department of Chemistry, Malaviya National Institute of Technology, Jawaharlal Nehru Marg, Jaipur 302017, India.
Department of Advance Molecular Microbiology, Seminal Applied Sciences Pvt. Ltd., Jaipur 302015, India.
Fitoterapia. 2018 Sep;129:13-19. doi: 10.1016/j.fitote.2018.06.003. Epub 2018 Jun 9.
Cephalandole A 2, a small indole alkaloid isolated from the Taiwanese orchid Cephalanceropsis gracilis (Orchidaceae), exhibits anticancer activity. Surprisingly, this natural product has not been evaluated for any other biological activity so far. To discover other novel potential of Cephalandole A 2, an efficient and economic synthetic protocol for novel Cephalandole A analogues 21a-o has been developed, in only 3 steps from using indole, and applied for their biological activity. Biological testing showed that Cephalandole A 2 and its novel analogues 21a-o exhibited potential antimicrobial and antiplatelet activity in preliminary assay. To the best of our knowledge, this is the first report of Cephalandole A 2 and its novel synthetic analogues 21a-o as a new class of antimicrobial and antiplatelet agents. In this study, 2 and other analogues i.e., 21b, 21d, 21i and 21o showed promising antimicrobial activity against the phytopathogenic bacteria and fungi. Cephalandole A 2, 21c, 21f and 21i, also showed potent antiplatelet activity.
从台湾产兰属植物 Cephalanceropsis gracilis（兰科）中分离得到的小分子吲哚生物碱 Cephalandole A 2 具有抗癌活性。令人惊讶的是，到目前为止，尚未对这种天然产物的其他生物活性进行评估。为了发现 Cephalandole A 2 的其他新的潜在用途，我们开发了一种从吲哚出发的高效、经济的新型 Cephalandole A 类似物 21a-o 的合成方法，仅需 3 步即可完成，并用其进行了生物活性测试。生物测试表明 Cephalandole A 2 及其新型类似物 21a-o 在初步试验中表现出潜在的抗菌和抗血小板活性。据我们所知，这是首次报道 Cephalandole A 2 及其新型合成类似物 21a-o 作为一类新的抗菌和抗血小板药物。在这项研究中，化合物 2 和其他类似物（如 21b、21d、21i 和 21o）表现出对植物病原菌和真菌的良好抗菌活性。Cephalandole A 2、21c、21f 和 21i 也表现出很强的抗血小板活性。
