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Oxidative stress mitigation, kinetics of carbohydrate-enzymes inhibition and cytotoxic effects of flavonoids-rich leaf extract of Gazania krebsiana (Less.): An in vitro evaluation

机译:Gazania krebsiana(Less。)的富含黄酮类叶提取物的氧化应激缓解,碳水化合物酶抑制动力学和细胞毒性作用:体外评估

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摘要

Objective:To investigate the free radical scavenging,antidiabetic,kinetics of enzyme inhibition and cytotoxic potentials of flavonoid-rich extract of Gazania krebsiana leaves using standard methods.Methods:Antioxidant activity of the flavonoids was investigated at scavenging free radicals such as 1,1-diphenyl-2-picryl hydrazyl,nitric oxide,hydroxyl radical,reducing capabilities,2,2-azinobis (3-ethylbenzothiazoline-6) sulphonic acid as well as metal chelating capability at different concentrations (125-1 000 μg/mL) while the antidiabetic activity was evaluated via the inhibition and kinetics of carbohydrate digestive enzymes including α-αmylase,α-glucosidase,sucrase and maltase.Brine shrimp lethality assay was also employed to examine the cytotoxic effects at various concentrations (125-2 000 μg/mL).Results:The study showed the best antioxidant activity in 2,2-azinobis (3-ethylbenzothiazoline-6)sulphonic acid,hydroxyl radical,nitric oxide and metal chelating with IC5o values of (1 089.00±19.29),(719.40±5.35),(633.10±5.31),(1 116.00±22.92) μg/mL,respectively;as compared with butylated hydroxyl anisole (standard) with IC50 of 1 166,747,639 and 1 363 μg/mL,respectively.Similarly,strong inhibition of α-glucosidase as well as moderate inhibition of sucrase and maltase enzyme activities which were significantly (P<0.05) better than acarbose were also observed in the study;though acarobse activity against α-amylase was better than the extract.The kinetics or mode of inhibition of α-amylase by the extract revealed an uncompetitive inhibition,competitive for α-glucosidase and non-competitive inhibitions for both sucrase and maltase,while the result of the lethality assay showed a potent cytotoxic effect with LC50 value of 359 μg/mL.Conclusion:The results obtained from this study are suggestive of the antioxidative,antidiabetic and cytotoxic potentials of flavonoid-rich extract of Gazania krebsiana.
机译:目的:采用标准方法研究富集的杂色菊叶黄酮提取物的自由基清除,抗糖尿病作用,酶抑制动力学和细胞毒性潜力。方法:研究黄酮对清除自由基(例如1,1-二苯基-2-吡啶基肼基,一氧化氮,羟基自由基,还原能力,2,2-叠氮基双(3-乙基苯并噻唑啉-6)磺酸以及不同浓度(125-1 000μg/ mL)的金属螯合能力通过抑制碳水化合物消化酶(包括α-α淀粉酶,α-葡萄糖苷酶,蔗糖酶和麦芽糖酶)的动力学来评估其抗糖尿病活性。还使用盐水对虾的致死率测定来检查不同浓度(125-2 000μg/ mL)的细胞毒性作用。结果:研究表明,在2,2-叠氮基双(3-乙基苯并噻唑啉-6)磺酸,羟基自由基,一氧化氮和金属螯合剂中具有最佳的抗氧化活性,IC 50值为(1089.0) 0±19.29),(719.40±5.35),(633.10±5.31),(116.00±22.92)μg/ mL;与丁基化羟基茴香醚(标准品)的IC50分别为1,166,747,639和1363μg/ mL,同样,在研究中也观察到α-葡萄糖苷酶的强抑制作用以及蔗糖酶和麦芽糖酶活性的中度抑制作用均显着优于阿卡波糖(P <0.05);尽管对α-淀粉酶的青蒿素活性优于α-糖化酶。提取物对α-淀粉酶的抑制动力学或抑制方式显示出无竞争性的抑制作用,与​​α-葡萄糖苷酶的竞争性以及对蔗糖酶和麦芽糖酶的非竞争性抑制作用,而致死性试验的结果显示,LC50具有强的细胞毒性作用值359μg/ mL。结论:本研究获得的结果表明,杂色菊芋富含类黄酮提取物具有抗氧化,抗糖尿病和细胞毒性的潜力。

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    Phytomedicine and Phytopharmacology Research Group, Department of Plant Sciences, University of the Free State, QwaQwa Campus, Private bag x 13, Phuthaditjhaba 9866, South Africa;

    Phytomedicine and Phytopharmacology Research Group, Department of Plant Sciences, University of the Free State, QwaQwa Campus, Private bag x 13, Phuthaditjhaba 9866, South Africa;

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