Department of Biochemistry, Microbiology and Biotechnology, Biology Faculty, Yerevan State University, 0025 Yerevan, Armenia.
Research Institute of Biology, Yerevan State University, 0025 Yerevan, Armenia.
Discov Med. 2023 Aug;35(177):590-611. doi: 10.24976/Discov.Med.202335177.59.
Herbal medicinal products containing L. (bilberry) fruits and fruit extracts are widely available in the market. Although bilberry leaves and stems are considered as bio-waste, they contain much higher levels of phenolic compounds than fruits. The study aimed to investigate the antimicrobial and anticancer potential of aerial part extracts from L. (, VM) plants harvested at high altitudes in Armenian landscape and characterize the bioactive phytochemicals.
For evaluation of antioxidant properties, chemical-based tests (total phenolic and flavonoid content, and antiradical activity in 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) tests) and cellular antioxidant activity (CAA) assay were applied. Genotoxicity and anticancer properties of the extract alone and in combination with fluorouracil were explored in human cancer and normal cell lines. Antibacterial properties of extract alone and in combination with antibiotics, as well as their effect on proton-flux rate through cell membrane were explored on bacterial strains. The characterization of active phytochemicals was done using Liquid Chromatography-Quadrupole-Orbitrap High-Resolution Mass Spectrometry (LC-Q-Orbitrap HRMS).
The aerial part extract demonstrated promising antioxidant properties in all tests. The selective cytotoxic activity was documented against various cancer cell lines (human colon adenocarcinoma (HT29), human breast cancer (MCF-7) and human cervical carcinoma (HeLa)), while it did not inhibit the growth of tested human normal primary renal mixed epithelial cells (HREC) even at 10-fold higher concentrations. The extract did not have genotoxic properties in comet assay making it a potential source for the development of anticancer preparations. The investigated extract did not directly inhibit the growth of () and () strains at up to 1 mg/mL concentration. However, extract enhanced the kanamycin intake and increased its efficiency against strain. The phytochemical characterization of the extract showed the presence of different groups of phenolics.
Based on obtained data, we suggest the aerial parts of the plant as an alternative source of bioactive natural products for food supplements, nutraceuticals, functional foods and medicine.
含有越橘（bilberry）果实和果实提取物的草药药品在市场上广泛销售。尽管越橘叶和茎被认为是生物废料，但它们所含的酚类化合物含量比果实高得多。本研究旨在调查亚美尼亚景观中高海拔地区收获的 L.（，VM）植物的地上部分提取物的抗菌和抗癌潜力，并对生物活性植物化学物质进行表征。
为了评估抗氧化性能，应用了基于化学的测试（总酚和类黄酮含量以及在 2,2'-偶氮-双（3-乙基苯并噻唑啉-6-磺酸）（ABTS）和 2,2-二苯基-1-吡唑啉-5-肼（DPPH）测试中的抗自由基活性）和细胞抗氧化活性（CAA）测定。单独使用和与氟尿嘧啶联合使用提取物的遗传毒性和抗癌特性在人类癌症和正常细胞系中进行了探索。单独使用和与抗生素联合使用 提取物的抗菌特性以及它们对质子通过细胞膜通量的影响在细菌菌株上进行了探索。使用液相色谱-四极杆轨道阱高分辨率质谱（LC-Q-Orbitrap HRMS）对活性植物化学物质进行了表征。
地上部分提取物在所有测试中均表现出有希望的抗氧化性能。记录了对各种癌细胞系（人结肠腺癌（HT29）、人乳腺癌（MCF-7）和人宫颈癌（HeLa））的选择性细胞毒性活性，而即使在 10 倍更高的浓度下，它也不会抑制测试的人正常原代肾混合上皮细胞（HREC）的生长。提取物在彗星试验中没有遗传毒性，使其成为开发抗癌制剂的潜在来源。在所研究的提取物中，高达 1mg/mL 浓度时，它不能直接抑制 （）和 （）菌株的生长。然而， 提取物增强了庆大霉素的摄取并提高了其对 菌株的效率。提取物的植物化学表征表明存在不同类别的酚类化合物。
根据获得的数据，我们建议将 植物的地上部分作为食品补充剂、营养保健品、功能性食品和药物中生物活性天然产物的替代来源。
