Antidiabetic Micro-/Nanoaggregates from Ge-Gen-Qin-Lian-Tang Decoction Increase Absorption of Baicalin and Cellular Antioxidant Activity In Vitro.

Antidiabetic Micro-/Nanoaggregates from Ge-Gen-Qin-Lian-Tang Decoction Increase Absorption of Baicalin and Cellular Antioxidant Activity In Vitro.
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葛根芩连汤汤中的抗糖尿病微/纳米聚集体可增加黄芩苷的吸收和细胞体外抗氧化活性

DOI:
10.1155/2017/9217912
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发表时间:
2017
影响因子:
--
通讯作者:
Rao P
Rao P
中科院分区:
生物学3区
文献类型:
--
作者:
Lin D;Du Q;Wang H;Gao G;Zhou J;Ke L;Chen T;Shaw C;Rao P

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葛根芩连汤的抗糖尿病作用已被临床证实。在stz诱导的糖尿病大鼠的药理学研究中,葛根芩连汤的组成物/沉淀物比可溶性成分表现出更强的降糖和抗氧化活性。本研究旨在通过测量活性单体植物化学物质(如黄芩苷)在Caco-2细胞单层中的通透性,并测定stz诱导氧化应激后胰腺β细胞系INS-1的细胞活力、细胞内氧化还原状态(MDA和SOD)和胰岛素分泌,来证明GQD衍生聚集体的药理特性。聚集体被分离成三个部分,即“MA(微聚集体)”,“400 g上清”和“MNA(微/纳米聚集体)”,分别在400 ×g和15000 ×g离心。沉积物中的聚集物增加了黄芩苷的吸收,对β细胞毒性较小,细胞内SOD水平升高,并显著抑制氧化损伤对细胞活力和功能的影响。在体外实验中,“MA”组分比“MNA”组分粒径更大,抗氧化细胞保护作用更强,表明其可能是中药汤剂中的有效成分。这些微/纳米聚集体的作用可能为理解中药煎剂的抗糖尿病作用提供新的视角,并有助于解释多种成分之间的协同作用。
The antidiabetic effects of Ge-Gen-Qin-Lian-Tang decoction (GQD) have been proven clinically. In a pharmacological study conducted on STZ-induced diabetic rats, the constitutive aggregates/sediments of Ge-Gen-Qin-Lian-Tang decoction exhibited stronger hypoglycemic and antioxidant activities compared to the soluble compositions. This study aims to demonstrate the pharmacological properties of aggregates derived from GQD by measuring permeability of the active monomer phytochemicals (e.g., baicalin) in a Caco-2 cell monolayer and determine the cellular viability, intracellular redox status (MDA and SOD), and insulin secretion of pancreatic β-cell line, INS-1, following STZ-induced oxidative stress. The aggregates were separated into three fractions, namely, “MA (microaggregates),” “400 g supernatant,” and “MNA (micro-/nanoaggregates),” by centrifugation at 400 ×g and 15000 ×g, respectively. Aggregates in the sediment increased baicalin absorption, showed little toxicity to β-cells, elevated intracellular SOD levels, and significantly suppressed oxidative damage effects on cellular viability and functions. The “MA” fraction had a larger particle size and provided higher antioxidant cellular protection than “MNA” in vitro, implying that the sediments may be the active components in the herbal decoction. The actions of these micro-/nanoaggregates may provide a new perspective for understanding the antidiabetic effects of herbal decoctions and aid in interpretation of synergistic actions between the multiple components.
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