单叶Eugenia叶片黄酮醇苷类及其体外细胞毒性、抗氧化和抗炎活性研究

IF 2.3 Q3 PHARMACOLOGY & PHARMACY Scientia Pharmaceutica Pub Date : 2023-08-24 DOI:10.3390/scipharm91030042
A. Oriola, G. Miya, Moganavelli Singh, A. Oyedeji
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引用次数: 0

摘要

鉴于在传统医学中广泛使用Eugenia uniflora叶子来治疗肿瘤和其他慢性炎症性疾病,对其叶子乙醇提取物进行活性引导分离,分离出两种黄酮醇苷。细胞毒性研究是基于3-(4,5-二甲基噻唑-2-基)-2,5-二苯基- 2h -溴化四唑(MTT)对非致瘤性人胚胎肾(HEK-293)细胞、肝癌(Hep-G2)和宫颈癌(HeLa)细胞系的活力测定。采用2,2-二苯基-1-苦味酰肼(DPPH)、一氧化氮(NO)和过氧化氢(H2O2)自由基清除法进行抗氧化试验,采用鸡蛋白蛋白变性(EAD)法进行体外抗炎试验。综合光谱和光谱测定结果表明,这两个化合物分别为杨梅霉素(1)和新发现的化合物5,7-二羟基-3-(3,4,5-三羟基-6-甲基四氢吡喃-2-氧基)-2-(2,4,5-三羟基苯基)铬-4- 1,命名为“unifloratrin(2)”。杨梅三醇(1)的细胞毒性与5-氟尿嘧啶(标准药物)相当,对HeLa细胞的CC50为8.5±2.2µg/100µL。对DPPH、NO和H2O2自由基的IC50分别为6.23±1.09、22.01±2.59和30.46±1.79µM,具有较好的抗氧化活性。在20µg/mL和2 h的孵育时间下,杨梅三醇的抗炎活性与双氯芬酸(标准药物)相当。这一研究结果可以作为一种民族医学应用的依据,而黄酮醇苷,如杨梅三醇(1),可以进一步开发作为一种候选的细胞毒性药物。
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Flavonol Glycosides from Eugenia uniflora Leaves and Their In Vitro Cytotoxicity, Antioxidant and Anti-Inflammatory Activities
In view of the extensive use of Eugenia uniflora leaves for the management of tumours and other chronic inflammatory diseases in traditional medicine, an activity-guided fractionation of its leaf ethanolic extract led to the isolation of two flavonol glycosides. Cytotoxicity study was based on the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) viability assay against the non-tumourigenic human embryonic kidney (HEK-293) cells, and the cancerous liver (Hep-G2) and cervical (HeLa) cell lines. Antioxidant tests were carried out using 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) and hydrogen peroxide (H2O2) radical scavenging assays, while an in vitro anti-inflammatory test was conducted using egg albumin denaturation (EAD) assay. Based on comprehensive spectroscopic and spectrometric evidence, the compounds were elucidated as myricitrin (1) and a newly described compound, 5,7-dihydroxy-3-(3,4,5-trihydroxy-6-methyltetrahydropyran-2-yloxy)-2-(2,4,5-trihydroxyphenyl)chromen-4-one, named “unifloratrin (2)”. The cytotoxicity of myricitrin (1) was comparable to 5-fluorouracil (standard drug), with a CC50 of 8.5 ± 2.2 µg/100 µL against HeLa cells. It also demonstrated better antioxidant activity, with an IC50 of 6.23 ± 1.09, 22.01 ± 2.59 and 30.46 ± 1.79 µM against DPPH, NO and H2O2 free radicals, respectively. At 20 µg/mL and an incubation time of 2 h, myricitrin was comparable to diclofenac (standard drug) in anti-inflammatory activity. This report may serve as a justification for the ethnomedicinal use of E. uniflora, while flavonol glycosides, such as myricitrin (1), could be further exploited as a candidate cytotoxic agent.
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来源期刊
Scientia Pharmaceutica
Scientia Pharmaceutica Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
4.60
自引率
4.00%
发文量
67
审稿时长
10 weeks
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