红巴西蜂胶的抗锥虫活性、细胞毒性及植物化学评价。

Evaluation of the antitrypanosomal activity, cytotoxicity and phytochemistry of red Brazilian propolis.

机构信息

Clinical Laboratory Sciences Department, College of Applied Medical Sciences, King Saud University, Riyad, Saudi Arabia.

Research and Laboratories Sector, National Drug and Cosmetic Control Laboratories (NDCCL), Saudi Food and Drug Authority, Riyadh, Saudi Arabia.

出版信息

PLoS One. 2024 Nov 19;19(11):e0313987. doi: 10.1371/journal.pone.0313987. eCollection 2024.

DOI:10.1371/journal.pone.0313987

PMID:39561157

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11575780/

Abstract

Recently, the growth in the consumption of functional foods with potential nutritional and health benefits revealed rapid progress in phytochemical analysis to assure quality and profile the chemical composition. Bee propolis, a gummy exudate produced in beehives after harvesting from different plant species and showed to contain bioactive secondary metabolites with biological importance. The main goal of the current study is to profile the chemical composition of red propolis samples from the Brazilian stingless bee Tetragonula biroi for the first time using HPLC-UV-ELSD and NMR analysis for assignment of the abundant metabolites' classes as well as extraction and isolation of the major compounds. Column chromatography and size exclusion chromatography were applied for the purification of the major compounds in red Brazilian propolis. Further, testing the antitrypanosomal and cytotoxic activities against Trypanosoma brucei and human leukemia cell lines (U937) was performed. A total of 29 secondary metabolites were identified as two anthocyanins, 6 flavonoids, 8 isoflavonoids, 10 phenolics, two phenolic acids, and one triterpenoid. Two phenolic compounds were purified and identified using 1D and 2D NMR analysis along with MS analysis as liquiritigenin and calycosin. Red Brazilian propolis FB-3 fraction showed the highest inhibitory activity against T. brucei at 1.6 μg/ml, compared to 12.4 μg/ml of the crude extract. The isolated compounds showed moderate activity with an MIC of 8.5 μg/ml for liquiritigenin and 8.7 μg/ml for calycosin. Moreover, FB-3 fraction and calycosin were showed the potent cytotoxic effect with IC50 = 45.1 and 35.8μg/ml, respectively compared to IC50 = 29.5 μg/ml of the standard diminazen. Hence, red Brazilian propolis is rich source of polyphenols with myriad biological importance. Propolis fractions and purified compounds showed moderate antiprotozoal activity and potent cytotoxic activity against human leukemia cell lines.

摘要

最近，具有潜在营养和健康益处的功能性食品的消费增长，促使植物化学分析取得了快速进展，以确保质量并分析化学成分。蜂胶是一种粘性渗出物，由从不同植物物种中收获的蜜蜂在蜂巢中产生，含有具有生物学重要性的生物活性次生代谢物。目前研究的主要目标是首次使用 HPLC-UV-ELSD 和 NMR 分析来分析巴西无刺蜜蜂 Tetragonula biroi 的红色蜂胶样品的化学成分，以分配丰富代谢物类别的归属以及主要化合物的提取和分离。柱色谱和尺寸排阻色谱用于纯化红色巴西蜂胶中的主要化合物。此外，还对其进行了抗锥虫和细胞毒性测试，以测试其对锥虫和人白血病细胞系（U937）的活性。共鉴定出 29 种次生代谢物，包括两种花色苷、6 种类黄酮、8 种异黄酮、10 种酚类、两种酚酸和一种三萜。两种酚类化合物通过 1D 和 2D NMR 分析以及 MS 分析与 MS 分析一起被鉴定为甘草素和大豆苷元。与粗提取物的 12.4 μg/ml 相比，红色巴西蜂胶 FB-3 馏分对 T. brucei 的抑制活性最高，在 1.6 μg/ml 时。分离得到的化合物显示出中等活性，甘草素的 MIC 为 8.5 μg/ml，大豆苷元的 MIC 为 8.7 μg/ml。此外，FB-3 馏分和大豆苷元对人白血病细胞系显示出较强的细胞毒性作用，IC50 分别为 45.1 和 35.8μg/ml，而标准 diminazen 的 IC50 为 29.5 μg/ml。因此，红色巴西蜂胶是富含多酚的丰富来源，具有多种生物学重要性。蜂胶馏分和纯化的化合物对原生动物表现出中等的抗活性，对人白血病细胞系表现出很强的细胞毒性。