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鉴定伽蓝菜属植物中的类黄酮和蟾蜍二烯内酯成分及其提取物对人癌细胞系的细胞毒性作用。

Identification of Flavonoids and Bufadienolides and Cytotoxic Effects of Kalanchoe daigremontiana Extracts on Human Cancer Cell Lines.

机构信息

Department of Biology and Pharmaceutical Botany, Medical University of Gdańsk, Gdańsk, Poland.

Institute of Physical Chemistry of the Polish Academy of Sciences, Warsaw, Poland.

出版信息

Planta Med. 2020 Mar;86(4):239-246. doi: 10.1055/a-1099-9786. Epub 2020 Jan 28.

Abstract

species are well-known medicinal plants used in traditional medicine as anti-inflammatory and analgesic remedies. Recently, it has been reported that plants have cytotoxic properties; however, data on traditional use of these plants in tumor treatment are extremely limited. is one of the most popular species cultivated in Europe, and it is used, among other things, as a remedy in treating skin injuries and wounds. Studies on the biological activity of this species are scarce, and there is a lack of data on the cytotoxic activity of extracts on epithelial cancer cells in the literature. In our present study, we analyzed the phytochemical composition of ethanol extract and fractions-water and dichloromethane-by the HPLC-DAD-ESI-MS method and estimated cytotoxic activity of the extracts on human adenocarcinoma (HeLa), ovarian (SKOV-3), breast (MCF-7), and melanoma (A375) cell lines by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay, real-time cell analyzer (RTCA), and flow cytometry. We identified 6 bufadienolide compounds and 19 flavonoids, mostly kaempferol, quercetin, isorhamnetin, and myricetin glycosides, of which only 3 flavonoids have been identified in to date. Other flavonoids that were characterized in our study have not yet been found in this plant. The ethanol extract and water fraction of did not show significant cytotoxic activity on the tested cell lines. In contrast, the dichloromethane fraction showed the strongest activity against all cell lines with IC values of ≤ 10 µg/mL. The results indicated that this activity is mainly due to the presence of bersaldegenin-1,3,5-orthoacetate.

摘要

该物种是著名的药用植物,在传统医学中被用作抗炎和镇痛药物。最近,有报道称该植物具有细胞毒性;然而,关于这些植物在肿瘤治疗中的传统用途的数据极为有限。是欧洲最受欢迎的栽培物种之一,除其他外,它还被用作治疗皮肤损伤和伤口的药物。关于该物种的生物活性研究很少,文献中缺乏该植物提取物对上皮癌细胞的细胞毒性活性的数据。在我们目前的研究中,我们通过 HPLC-DAD-ESI-MS 方法分析了 乙醇提取物及其水和二氯甲烷馏分的植物化学成分,并通过 MTT(3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四唑溴盐)测定法、实时细胞分析仪 (RTCA) 和流式细胞术评估了提取物对人腺癌 (HeLa)、卵巢 (SKOV-3)、乳腺 (MCF-7) 和黑素瘤 (A375) 细胞系的细胞毒性。我们鉴定了 6 种蟾毒配基化合物和 19 种类黄酮,主要为山奈酚、槲皮素、异鼠李素和杨梅素糖苷,其中迄今为止仅在 中鉴定出 3 种类黄酮。我们在研究中鉴定的其他类黄酮尚未在该植物中发现。乙醇提取物和 的水馏分对测试的细胞系没有显示出显著的细胞毒性活性。相比之下,二氯甲烷馏分对所有细胞系显示出最强的活性,IC 值均≤10μg/mL。结果表明,这种活性主要归因于 bersaldegenin-1,3,5-orthoacetate 的存在。

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