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大黄素的抗氧化、抗糖尿病、抗胆碱能和抗青光眼作用。

Antioxidant, Antidiabetic, Anticholinergic, and Antiglaucoma Effects of Magnofluorine.

机构信息

Department of Medical Services and Technology, Cayirli Vocational School, Erzincan Binali Yildirim University, Erzincan 24500, Turkey.

Department of Pharmacy Services, Vocational School of Health Services, Van Yuzuncu Yil University, Van 65080, Turkey.

出版信息

Molecules. 2022 Sep 11;27(18):5902. doi: 10.3390/molecules27185902.

Abstract

Magnofluorine, a secondary metabolite commonly found in various plants, has pharmacological potential; however, its antioxidant and enzyme inhibition effects have not been investigated. We investigated the antioxidant potential of Magnofluorine using bioanalytical assays with 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ,-dimethyl--phenylenediamine dihydrochloride (DMPD), and 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging abilities and K[Fe(CN)] and Cu reduction abilities. Further, we compared the effects of Magnofluorine and butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), α-Tocopherol, and Trolox as positive antioxidant controls. According to the analysis results, Magnofluorine removed 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals with an IC value of 10.58 μg/mL. The IC values of BHA, BHT, Trolox, and α-Tocopherol were 10.10 μg/mL, 25.95 μg/mL, 7.059 μg/mL, and 11.31 μg/mL, respectively. Our results indicated that the DPPH· scavenging effect of Magnofluorine was similar to that of BHA, close to that of Trolox, and better than that of BHT and α-tocopherol. The inhibition effect of Magnofluorine was examined against enzymes, such as acetylcholinesterase (AChE), α-glycosidase, butyrylcholinesterase (BChE), and human carbonic anhydrase II (hCA II), which are linked to global disorders, such as diabetes, Alzheimer's disease (AD), and glaucoma. Magnofluorine inhibited these metabolic enzymes with Ki values of 10.251.94, 5.991.79, 25.411.10, and 30.563.36 nM, respectively. Thus, Magnofluorine, which has been proven to be an antioxidant, antidiabetic, and anticholinergic in our study, can treat glaucoma. In addition, molecular docking was performed to understand the interactions between Magnofluorine and target enzymes BChE (D: 6T9P), hCA II (A:3HS4), AChE (B:4EY7), and α-glycosidase (C:5NN8). The results suggest that Magnofluorine may be an important compound in the transition from natural sources to industrial applications, especially new drugs.

摘要

莪术呋喃酮,一种常见于多种植物中的次生代谢产物,具有药理学潜力;然而,其抗氧化和酶抑制作用尚未得到研究。我们使用 2,2-联氮-双(3-乙基苯并噻唑啉-6-磺酸)(ABTS)、1,1-二苯基-2-苦基肼(DPPH)清除能力和 K[Fe(CN)6]3-和 Cu2+还原能力的生物分析测定来研究莪术呋喃酮的抗氧化潜力。此外,我们比较了莪术呋喃酮和丁基羟基甲苯 (BHT)、丁基羟基茴香醚 (BHA)、α-生育酚和 Trolox 作为阳性抗氧化对照物的效果。根据分析结果,莪术呋喃酮清除 1,1-二苯基-2-苦基肼(DPPH)自由基的 IC 值为 10.58 μg/mL。BHA、BHT、Trolox 和 α-生育酚的 IC 值分别为 10.10 μg/mL、25.95 μg/mL、7.059 μg/mL 和 11.31 μg/mL。我们的结果表明,莪术呋喃酮的 DPPH·清除效果与 BHA 相似,接近 Trolox,优于 BHT 和 α-生育酚。我们还研究了莪术呋喃酮对与全球疾病(如糖尿病、阿尔茨海默病(AD)和青光眼)相关的酶(如乙酰胆碱酯酶(AChE)、α-糖苷酶、丁酰胆碱酯酶(BChE)和人碳酸酐酶 II(hCA II))的抑制作用。莪术呋喃酮对这些代谢酶的抑制 Ki 值分别为 10.251.94、5.991.79、25.411.10 和 30.563.36 nM。因此,在我们的研究中,莪术呋喃酮已被证明具有抗氧化、抗糖尿病和抗胆碱能作用,可用于治疗青光眼。此外,我们还进行了分子对接,以了解莪术呋喃酮与靶酶 BChE(D:6T9P)、hCA II(A:3HS4)、AChE(B:4EY7)和 α-糖苷酶(C:5NN8)之间的相互作用。结果表明,莪术呋喃酮可能是从天然来源向工业应用转化的重要化合物,特别是新药。

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