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Antiglycation and enzyme inhibitory potential of salicylalazine isolated from Micromeria biflora (Buch.-Ham.ex D.Don) Benth
South African Journal of Botany ( IF 2.7 ) Pub Date : 2021-01-05 , DOI: 10.1016/j.sajb.2020.12.021
Abdur Rauf , Saud Bawazeer , Umer Rashid , Mohamed A. El-Esawi , Muhammad Humayun Khan , Syed Uzair Ali Shah , Mohammad S. Mubarak , Kannan RR Rengasamy

The aim of the present study was focused on experimental analysis for medicinal use of Micromeria biflora Benth. The plant was collected and subjected to extraction and fractionation; the chloroform fraction resulted in the isolation of a new constituent salicylalazine, using preparative HPLC. The Chemical structure of salicylalazine was confirmed through NMR and high-resolution mass spectrometry. Salicylalazine was evaluated (in vitro) against various biological targets such as urease, phosphodiesterase-1, tyrosinase, and anti-glycation studies. Furthermore, the binding orientation and interaction pattern of salicylalazine with crucial amino acid residues of the respective targets were used to explore the mechanism of enzymes inhibition. Results indicated that salicylalazine caused potent urease inhibition with an IC50 value of 12.4 ± 1.10 µM, in comparison of standard thiourea (IC50 = 21.0 ± 0.21 µM). The compound exhibited excellent inhibition potential against tyrosinase (89.4%), phosphodiesterase-1 (94.7%) compared to the standards kojic acid (86.3%) and EDTA (86.4%), respectively. Besides, salicylalazine possessed good anti-glycation activity with % inhibition of 86% and IC50 value of 248.7 ± 2.09 µM, compared to the standard Rutin (96%, IC50 value of 295 ± 3.14). Thus, it is concluded that salicylalazine, the active constituent Micromeria biflora Benth, exhibited remarkable in vitro inhibition of urease, phosphodiesterase-1, tyrosinase, and anti-glycation.



中文翻译:

抗糖化和分离自salicylalazine的酶抑制潜力姜味(Buch.-Ham.ex D.Don)广藿香

本研究的目的集中在小花m虫药的医学用途的实验分析。收集植物并进行萃取和分离。氯仿馏分使用制备型HPLC分离出新的成分水杨基嗪。水杨基嗪的化学结构通过NMR和高分辨率质谱法确认。评估水杨嘧啶(体外)针对各种生物靶标,例如脲酶,磷酸二酯酶-1,酪氨酸酶和抗糖基化研究。此外,利用水杨基嗪与各个靶标的关键氨基酸残基的结合方向和相互作用模式来探索酶抑制的机理。结果表明,与标准硫脲(IC 50  = 21.0±0.21 µM)相比,水杨基嗪可有效抑制脲酶,IC 50值为12.4±1.10 µM 。与标准曲酸(86.3%)和EDTA(86.4%)相比,该化合物对酪氨酸酶(89.4%),磷酸二酯酶-1(94.7%)表现出优异的抑制潜力。此外,水杨基嗪具有良好的抗糖化活性,抑制率达86%,IC 50相对于标准芦丁(96%,IC 50值为295±3.14),其值为248.7±2.09 µM 。因此,得出的结论是,水杨柳嗪(活性成分美人小粉虱Benth)在体外具有显着的尿素酶,磷酸二酯酶-1,酪氨酸酶抑制作用和抗糖化作用。

更新日期:2021-01-05
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