Kurt-Celep Inci, Zheleva-Dimitrova Dimitrina, Gevrenova Reneta, Uba Abdullahi Ibrahim, Zengin Gokhan, Yıldıztugay Evren, Picot-Allain Carene Marie Nancy, Lorenzo José Manuel, Mahomoodally Mohamad Fawzi, Montesano Domenico
Department of Pharmacognosy, Faculty of Pharmacy, Yeditepe University, 34755 Istanbul, Turkey.
Department of Pharmacognosy, Faculty of Pharmacy, Medical University-Sofia, 1000 Sofia, Bulgaria.
Antioxidants (Basel). 2022 Jul 15;11(7):1377. doi: 10.3390/antiox11071377.
The biological activity of the aerial part and rhizomes of were assessed for the first time. The biological activities (antioxidant properties, enzyme inhibition, and AGE inhibition) as well as the phenolic and flavonoid contents of the ethyl acetate, ethanol, hydro-ethanol and water extracts of aerial parts and rhizomes were determined. Cell viability assays and gelatin zymography were also performed for MMP-2/-9 to determine the molecular mechanisms of action. The gene expression for MMPs was described with RT-PCR. The levels of various proteins, including phospho-Nf-κB, BCL-2, BAX, p-53, and cyclin D1 as well as RAGE were measured using Western blot analysis. The hydro-ethanol extract of the aerial part possessed the highest phenolic (56.81 mg GAE/g) and flavonoid (63.92 mg RE/g) contents. In-depth profiling of the specialized metabolites by ultra-high-performance liquid chromatography-high-resolution mass spectrometry (UHPLC-HRMS) allowed for the identification and annotation of 65 compounds, including phenolic acids and glycosides, flavones, flavonols, chalcones, dihydrochalcones, and saponins. The hydro-ethanol extract of the aerial parts (132.65, 180.87, 172.46, and 108.37 mg TE/g, for the DPPH, ABTS, CUPRAC, and FRAP assays, respectively) and the ethanol extract of the rhizomes (415.06, 638.30, 477.77, and 301.02 mg TE/g, for the DPPH, ABTS, CUPRAC, and FRAP assays, respectively) exhibited the highest free radical scavenging and reducing activities. The ethanol and hydro-ethanol extracts of both the aerial part and rhizomes exhibited higher inhibitory activity against acetylcholinesterase, while the hydro-ethanol extracts (1.16 mmol ACAE/g, for both the aerial part and rhizomes extracts) were more active in the inhibition of α-glucosidase. After the treatment of an HT-29 colorectal cancer cell line with the extracts, the apoptosis mechanism was initiated, the integrity of the ECM was remodeled, and cell proliferation was also taken under control. In this way, extracts were shown to be potential drug sources in the treatment of colorectal cancer. They were also detected as natural MMP inhibitors. The findings presented in the present study appraise the bioactivity of , an understudied species. Additional assessment is required to evaluate the cytotoxicity of as well as its activity in ex vivo systems.
首次对[植物名称]地上部分和根茎的生物活性进行了评估。测定了[植物名称]地上部分和根茎的乙酸乙酯、乙醇、水-乙醇和水提取物的生物活性(抗氧化性能、酶抑制和晚期糖基化终产物抑制)以及酚类和黄酮类含量。还进行了细胞活力测定和明胶酶谱分析以确定基质金属蛋白酶-2/-9的分子作用机制。用逆转录聚合酶链反应(RT-PCR)描述基质金属蛋白酶的基因表达。使用蛋白质免疫印迹分析测量了包括磷酸化核因子κB、B细胞淋巴瘤/白血病-2(BCL-2)、Bax、p53和细胞周期蛋白D1以及晚期糖基化终产物受体(RAGE)在内的各种蛋白质的水平。地上部分的水-乙醇提取物具有最高的酚类(56.81毫克没食子酸当量/克)和黄酮类(63.92毫克芦丁当量/克)含量。通过超高效液相色谱-高分辨率质谱(UHPLC-HRMS)对特殊代谢产物进行深入分析,鉴定并注释了65种化合物,包括酚酸及其糖苷、黄酮、黄酮醇、查耳酮、二氢查耳酮和皂苷。地上部分的水-乙醇提取物(在二苯基苦味酰基自由基(DPPH)、2,2'-联氮-双-3-乙基苯并噻唑啉-6-磺酸(ABTS)、铜离子还原抗氧化能力(CUPRAC)和铁离子还原抗氧化能力(FRAP)测定中,分别为132.65、180.87、172.46和108.37毫克 Trolox 当量/克)和根茎的乙醇提取物(在DPPH、ABTS、CUPRAC和FRAP测定中,分别为415.06、638.30、477.77和301.02毫克 Trolox 当量/克)表现出最高的自由基清除和还原活性。地上部分和根茎的乙醇和水-乙醇提取物对乙酰胆碱酯酶均表现出较高抑制活性,而水-乙醇提取物(地上部分和根茎提取物均为1.16毫摩尔乙酰胆碱酯酶当量/克)对α-葡萄糖苷酶的抑制活性更高。用提取物处理人结肠癌细胞系HT-29后,启动了凋亡机制,细胞外基质的完整性得到重塑,细胞增殖也得到控制。通过这种方式,[植物名称]提取物被证明是治疗结直肠癌的潜在药物来源。它们还被检测为天然的基质金属蛋白酶抑制剂。本研究中的发现评估了一种研究较少的物种[植物名称]的生物活性。需要进一步评估[植物名称]的细胞毒性及其在体外系统中的活性。