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毛蕊花糖苷、合成衍生物和其他来自阿根廷本土植物物种的糖苷类化合物作为潜在的抗肿瘤药物。

Verbascoside, synthetic derivatives and other glycosides from Argentinian native plant species as potential antitumoral agents.

机构信息

Área de Química Orgánica, INTEQUI-CONICET-UNSL, San Luis, Argentina.

Max Planck Laboratory for Structural Biology, Chemistry and Molecular Biophysics of Rosario (MPLbioR, UNR-MPIbpC), and Instituto de Investigaciones para el Descubrimiento de Fármacos de Rosario (IIDEFAR, UNR-CONICET), Universidad Nacional de Rosario, Rosario, Argentina.

出版信息

Nat Prod Res. 2021 Nov;35(22):4703-4708. doi: 10.1080/14786419.2019.1710701. Epub 2020 Jan 10.

Abstract

A phytochemical study was performed on three native plant species from the central-western zone of Argentina: Grisebach Torr. & A. Gray and L. We could obtain verbascoside () from . From , we could obtain 1, 5, 9--deoxyloganic acid () L. Finally, we could isolate 2--(-rhamnopyranosyl)-3-angeloyloxy-15-acetyloxy-7,13(14)--dien--labdane () and 2--(-rhamnopyranosyl)-3--angeloyloxy-15-hydroxy-7,13(14)--dien--labdane () from . Moreover, three derivatives from , and one semi-synthetic derivative from , were prepared. PCR reaction was used to analyse the activity against DNA polymerase and cell culture to determine cytotoxicity and antitumoral activity. Verbascoside ( was strongly active in the nanomolar scale (IC = 356 nM) against DNA polymerization. Moreover, verbascoside was also strongly active in the nanomolar scale against human melanoma cell line (IC = 256 nM) and human colorectal cell line (IC = 320 nM). Furthermore, derivatives and were cytotoxic against both cancer cell lines.

摘要

对来自阿根廷中西部地区的三种本地植物进行了植物化学研究

Grisebach Torr. & A. Gray 和 L. 我们可以从 中获得毛蕊花糖苷()。从 中,我们可以获得 1,5,9--去氧龙牙草酸()。最后,我们可以从 中分离出 2--(-鼠李吡喃糖基)-3-当归酰氧基-15-乙酰氧基-7,13(14)--二烯--贝壳杉烷()和 2--(-鼠李吡喃糖基)-3--当归酰氧基-15-羟基-7,13(14)--二烯--贝壳杉烷()。此外,还从 中制备了三种衍生物,从 中制备了一种半合成衍生物。通过 PCR 反应分析对 DNA 聚合酶的活性,并通过细胞培养测定细胞毒性和抗肿瘤活性。毛蕊花糖苷(在纳摩尔范围内对 DNA 聚合具有很强的活性(IC = 356 nM)。此外,毛蕊花糖苷对人黑色素瘤细胞系(IC = 256 nM)和人结直肠癌细胞系(IC = 320 nM)也具有很强的活性。此外,衍生物 和 对两种癌细胞系均具有细胞毒性。

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