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标准提取物、 fractions 以及葫芦巴种子中单个次级代谢产物对 SKOV-3、HeLa 和 MOLT-4 细胞系的细胞毒性活性。

Cytotoxic activity of standardized extracts, a fraction, and individual secondary metabolites from fenugreek seeds against SKOV-3, HeLa and MOLT-4 cell lines.

机构信息

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

Department of Pharmacognosy with Medicinal Plants Garden, Medical University of Gdańsk, Gdańsk, Poland.

出版信息

Pharm Biol. 2021 Dec;59(1):424-437. doi: 10.1080/13880209.2021.1903047.

Abstract

CONTEXT

L. (Fabaceae) has many therapeutic properties and anticancer potential.

OBJECTIVE

The cytotoxic activities of standardized extracts and a fraction from fenugreek seeds and their compounds (sapogenins, flavone C-glycosides, alkaloid trigonelline) against human cancer SKOV-3, HeLa and MOLT-4 cells were evaluated.

MATERIALS AND METHODS

Fenugreek seeds were extracted with 70% methanol (A) or water (B). Furthermore, the seeds were purified with petroleum ether and chloroform and next extracted with methanol to obtain fraction (C). The quantitative analysis of saponins and flavonoids in the extracts was done with HPLC methods. The extracts (5-120 µg/mL) and compounds (1-50 µg/mL) were tested on the cells by MTT assay and RTCA system. The effect of a fraction on ROS production, mitochondrial membrane potential and caspase-3/7 activity in HeLa and SKOV-3 cells was also evaluated by flow cytometry.

RESULTS

The strongest cytotoxic activity on cancer cells showed the fraction C (IC was 3.91 ± 0.03 for HeLa, 3.97 ± 0.07 for SKOV-3, and 7.75 ± 0.37 for MOLT-4) with the highest content of steroidal saponins (163.18 ± 11.03 μg/mg) and flavone C-glycosides (820.18 ± 0.05 μg/mg). The fraction significantly increased ROS production (up to four times higher than in keratinocytes as control) and caspases activity in the cells. The examined flavonoids did not exhibit the cytotoxic activity in contrast to yamogenin, tigogenin, and diosgenin.

CONCLUSIONS

The obtained results complement the data on the cytotoxic activity of and synergistic effect of flavonoids and saponins complex contained in the plant.

摘要

背景

葫芦巴(豆科)具有多种治疗特性和抗癌潜力。

目的

评估标准化提取物和葫芦巴种子的一个馏分及其化合物(皂角苷、黄酮 C-糖苷、生物碱三六磷)对人癌症 SKOV-3、HeLa 和 MOLT-4 细胞的细胞毒性活性。

材料与方法

用 70%甲醇(A)或水(B)从葫芦巴种子中提取。此外,用石油醚和氯仿对种子进行纯化,然后用甲醇提取以获得馏分(C)。用 HPLC 方法对提取物中的皂角苷和黄酮进行定量分析。用 MTT 测定法和 RTCA 系统在细胞上测试提取物(5-120μg/ml)和化合物(1-50μg/ml)。还通过流式细胞术评估馏分对 HeLa 和 SKOV-3 细胞中 ROS 产生、线粒体膜电位和 caspase-3/7 活性的影响。

结果

馏分 C 对癌细胞的细胞毒性最强(IC 在 HeLa 为 3.91±0.03,在 SKOV-3 为 3.97±0.07,在 MOLT-4 为 7.75±0.37),其甾体皂角苷(163.18±11.03μg/mg)和黄酮 C-糖苷(820.18±0.05μg/mg)含量最高。该馏分显著增加了细胞中的 ROS 产生(比作为对照的角质形成细胞高四倍)和 caspase 活性。所检查的黄酮类化合物与 yamogenin、tigogenin 和 diosgenin 相反,没有表现出细胞毒性活性。

结论

获得的结果补充了关于和植物中含有的黄酮类和皂角苷复合物的协同细胞毒性活性的数据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/beb8/8057092/f42beed48485/IPHB_A_1903047_F0001_C.jpg

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