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