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Zinc(II) mineral increased the in vitro, cellular and ex vivo antihyperglycemic and antioxidative pharmacological profile of p‐hydroxybenzoic acid upon complexation
Journal of Food Biochemistry ( IF 3.5 ) Pub Date : 2021-01-17 , DOI: 10.1111/jfbc.13609 Lindah S L Tshane 1 , Samson S Mashele 1 , Godfrey R Matowane 1 , Susanna L Bonnet 2 , Tshepiso J Makhafola 3 , Anwar E M Noreljaleel 2 , Shasank S Swain 4 , Mamello Sekhoacha 5 , Chika I Chukwuma 3
Journal of Food Biochemistry ( IF 3.5 ) Pub Date : 2021-01-17 , DOI: 10.1111/jfbc.13609 Lindah S L Tshane 1 , Samson S Mashele 1 , Godfrey R Matowane 1 , Susanna L Bonnet 2 , Tshepiso J Makhafola 3 , Anwar E M Noreljaleel 2 , Shasank S Swain 4 , Mamello Sekhoacha 5 , Chika I Chukwuma 3
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In this study, zinc was complexed with p‐hydroxybenzoic acid to synthesize a complex with improved pharmacological profile. Proton NMR and FTIR analysis were used to characterize the complex. Several in vitro, cellular and ex vivo antihyperglycemic and antioxidative assays were used to evaluate the potency of the complex, relative to its precursors, while molecular docking was used to investigate interactions with insulin signaling targets (GLUT‐4 and PKB). Also, the cytotoxicity of the complex was evaluated in Chang liver cells and L‐6 myotubes using MTT assay. Complexation was through a Zn(O4) coordination. This afforded the complex two moieties of p‐hydroxybenzoic acid, which influenced its activities. While the complex retained the α‐glucosidase and α‐amylase inhibitory activity of its phenolic acid precursor, complexation increased in vitro and ex vivo antioxidant activity of the phenolic acid by 1.4 to 10.5‐folds. Complexation, further, conferred a potent antiglycation activity and L‐6 myotube and psoas muscle glucose uptake properties (2.1 to 3.5‐folds more than p‐hydroxybenzoic acid) on the phenolic acid, without notably inhibiting or reducing the viability of Chang liver cells (IC50 = 5,120 μM) and L‐6 myotubes (IC50 = 2,172 μM). Docking studies showed the complex had better interactions with insulin signaling targets (GLUT‐4 and PKB) than p‐hydrobenzoic acid, which may influence its glucose uptake effects. Data suggest that Zn(II) complexation improved and/or broadened the pharmacological profile of p‐hydroxybenzoic acid, thus, may be further studied as a promising adjuvant for phenolic acids.
中文翻译：
锌（II）矿物质在络合后可增强对羟基苯甲酸的体外，细胞和体外抗高血糖和抗氧化药理作用
在这项研究中，锌与对羟基苯甲酸络合以合成具有改善药理作用的络合物。使用质子NMR和FTIR分析来表征该配合物。相对于其前体，几种体外，细胞和离体的降血糖和抗氧化测定法被用来评估该复合物的效力，而分子对接则被用来研究与胰岛素信号传导靶标（GLUT-4和PKB）的相互作用。此外，使用MTT分析法评估了复合物在Chang肝细胞和L-6肌管中的细胞毒性。络合是通过Zn（O 4）协调。这提供了对羟基苯甲酸的两个部分，影响了它的活性。尽管该复合物保留了其酚酸前体的α-葡萄糖苷酶和α-淀粉酶抑制活性，但复合物使酚酸的体外和离体抗氧化活性提高了1.4到10.5倍。络合物进一步赋予酚酸强效的抗糖化活性以及L-6肌管和腰大肌的葡萄糖摄取特性（比对羟基苯甲酸高2.1到3.5倍），而不会显着抑制或降低Chang肝细胞的活力（ IC 50 = 5,120μM）和L‐6肌管（IC 50 = 2,172μM）。对接研究表明，该复合物与胰岛素信号传递靶标（GLUT-4和PKB）的相互作用要好于对羟基苯甲酸，这可能会影响其葡萄糖的吸收作用。数据表明，Zn（II）络合物改善和/或拓宽了对羟基苯甲酸的药理作用，因此，可以进一步研究它作为酚酸的有前途的佐剂。
更新日期：2021-02-22
中文翻译：
锌（II）矿物质在络合后可增强对羟基苯甲酸的体外，细胞和体外抗高血糖和抗氧化药理作用
在这项研究中，锌与对羟基苯甲酸络合以合成具有改善药理作用的络合物。使用质子NMR和FTIR分析来表征该配合物。相对于其前体，几种体外，细胞和离体的降血糖和抗氧化测定法被用来评估该复合物的效力，而分子对接则被用来研究与胰岛素信号传导靶标（GLUT-4和PKB）的相互作用。此外，使用MTT分析法评估了复合物在Chang肝细胞和L-6肌管中的细胞毒性。络合是通过Zn（O 4）协调。这提供了对羟基苯甲酸的两个部分，影响了它的活性。尽管该复合物保留了其酚酸前体的α-葡萄糖苷酶和α-淀粉酶抑制活性，但复合物使酚酸的体外和离体抗氧化活性提高了1.4到10.5倍。络合物进一步赋予酚酸强效的抗糖化活性以及L-6肌管和腰大肌的葡萄糖摄取特性（比对羟基苯甲酸高2.1到3.5倍），而不会显着抑制或降低Chang肝细胞的活力（ IC 50 = 5,120μM）和L‐6肌管（IC 50 = 2,172μM）。对接研究表明，该复合物与胰岛素信号传递靶标（GLUT-4和PKB）的相互作用要好于对羟基苯甲酸，这可能会影响其葡萄糖的吸收作用。数据表明，Zn（II）络合物改善和/或拓宽了对羟基苯甲酸的药理作用，因此，可以进一步研究它作为酚酸的有前途的佐剂。
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