天然 calanolides：存在、生物合成和药理学特性，包括治疗潜力。

Naturally Occurring Calanolides: Occurrence, Biosynthesis, and Pharmacological Properties Including Therapeutic Potential.

机构信息

Laboratory of Growth Regulators, Institute of Experimental Botany ASCR & Palacký University, Šlechtitelů 27, 78371 Olomouc, Czech Republic.

Department of Life Science and Bioinformatics, Assam University, Silchar, Assam 788011, India.

出版信息

Molecules. 2020 Oct 28;25(21):4983. doi: 10.3390/molecules25214983.

Calanolides are tetracyclic 4-substituted dipyranocoumarins. Calanolide A, isolated from the leaves and twigs of var. (Whitmore) P. F. Stevens, is the first member of this group of compounds with anti-HIV-1 activity mediated by reverse transcriptase inhibition. Calanolides are classified pharmacologically as non-nucleoside reverse transcriptase inhibitors (NNRTI). There are at least 15 naturally occurring calanolides distributed mainly within the genus but some of them are also present in the genus . Besides significant anti-HIV properties, which have been exploited towards potential development of new NNRTIs for anti-HIV therapy, calanolides have also been found to possess anticancer, antimicrobial and antiparasitic potential. This review article provides a comprehensive update on all aspects of naturally occurring calanolides, including their chemistry, natural occurrence, biosynthesis, pharmacological and toxicological aspects including mechanism of action and structure activity relationships, pharmacokinetics, therapeutic potentials and available patents.

Calanolides 是四环 4 取代的二吡喃香豆素。Calanolide A 从 var. 的叶子和嫩枝中分离出来。（Whitmore）P. F. Stevens，是该类化合物中第一个具有抗 HIV-1 活性的成员，通过逆转录酶抑制介导。Calanolides 在药理学上被分类为非核苷逆转录酶抑制剂（NNRTI）。至少有 15 种天然存在的 calanolides 主要分布在属内，但其中一些也存在于属内。除了具有显著的抗 HIV 特性，这些特性已被开发用于新型 NNRTIs 以用于抗 HIV 治疗外，calanolides 还被发现具有抗癌、抗菌和抗寄生虫的潜力。本文综述了天然 calanolides 的各个方面，包括其化学、天然存在、生物合成、药理学和毒理学方面，包括作用机制和构效关系、药代动力学、治疗潜力和可用专利。