JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2025
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IF 6.2
Xiangzhao Ma,Huan Li,Ying Li,Xiaofang Xie,Yiwen Wang,Mengfan Wang,Xin Peng
The inhibitory mechanisms and binding behaviors of nordihydroguaiaretic acid (NDGA) to α-glucosidase/α-amylase were investigated by in vitro multispectroscopic methods and in silico modeling technique. The results demonstrated that NDGA reversibly and uncompetitively inhibited α-glucosidase, exhibiting stronger inhibition than acarbose, while it displayed noncompetitive inhibition against α-amylase. Additionally, NDGA could spontaneously bind to α-glucosidase/α-amylase mainly through hydrogen bonds and hydrophobic forces, thus altering the spatial structure of enzymes and reducing their catalytic activity. The presence of crowding reagents/polysaccharides/undigested milk proteins would decrease the inhibitory ability of NDGA, whereas fatty acids exhibited the opposite phenomenon on α-glucosidase. Furthermore, the antidiabetic activity of NDGA in vivo was evaluated using the diabetic Drosophila model induced by a high-sugar diet. It was found that NDGA significantly reduced the glucose levels of diabetic Drosophila. These findings suggested that NDGA was a potential inhibitor of α-glucosidase/α-amylase and could be used as a nutritional adjuvant to prevent diabetes.
研究领域:
生物化学
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药理学
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营养学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Materials Today Bio
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2025
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IF 10.2
Hongping Wan,Zhengqun Huang,Mingrun Tang,Huirong Tan,Kai Deng,Yingnan Liu,Xinghong Zhao,Hongjun Chen
Enveloped viruses such as coronaviruses are highly transmissible, necessitating effective prevention and inactivation strategies. In this study, we engineered uniform, small-sized (∼57 nm) iron-phenolic nano-networks (NA-Fe) that exhibit high lipoxidase-like activity for the inactivation of enveloped virus, encompassing both DNA virus (Pseudorabies, PRV) and RNA virus (Transmissible Gastroenteritis, TGEV; and Porcine epidemic diarrhea virus, PEDV). Theoretical studies indicate that NA-Fe facilitates the adsorption of pentadiene moieties within the viral envelope through interactions between the d -orbital electrons of iron and the π-electrons of pentadiene. This interaction leads to activation of the C=C bonds, potentially resulting in disruption of the viral envelope. Besides its extracellular antiviral effects, NA-Fe also suppresses intracellular viral replication by stimulating antiviral innate immune responses, and upregulate the expression of interferon-stimulating genes (ISGs). In vivo studies demonstrate that NA-Fe exhibits favorable biosafety, and intranasal administration significantly reduces viral titers while providing effective antiviral protection in PRV-infected mice. Notably, surfaces coated with NA-Fe, such as fences and air purifiers in farm facilities, provide effective antiviral protection. Collectively, these findings demonstrate that NA-Fe exhibits potent broad-spectrum antiviral activity against both extracellular and intracellular viruses, highlighting its potential for application in comprehensive biosecurity and infectious disease control.
研究领域:
纳米技术
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病毒学
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免疫学
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抗病毒治疗
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材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
APPLIED SURFACE SCIENCE
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2015
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IF 2.711
Sen Liao,Wen Zhang,Wei Long,Dan Hou,Xuechun Yang,Ni Tan
In this paper, a new core-shell composite of nordihydroguaiaretic acid (NDGA) molecularly imprinted polymers layer-coated silica gel (MIP@SiO 2 ) was prepared through sol–gel technique and applied as a material for extraction of NDGA from Ephedra. It was synthesized using NDGA as the template molecule, γ-aminopropyltriethoxysilane (APTS) and methyltriethoxysilane (MTEOS) as the functional monomers, tetraethyl orthosilicate (TEOS) as the cross-linker and ethanol as the porogenic solvent in the surface of silica. The non-imprinted polymers layer-coated silica gel (NIP@SiO 2 ) were prepared with the same procedure, but with the absence of template molecule. In addition, the optimum adsorption affinity occurred when the molar ratio of NDGA:APTS:MTEOS:TEOS was 1:6:2:80. The prepared MIP@SiO 2 and NIP@SiO 2 were analyzed by scanning electron microscopy (SEM), thermogravimetric analysis (TGA), and Fourier transform-infrared spectroscopy (FT-IR). Their affinity properties to NDGA were evaluated through dynamic adsorption, static adsorption, and selective recognition experiments, and the results showed the saturated adsorption capacity of MIP@SiO 2 could reach to 5.90 mg g −1 , which was two times more than that of NIP@SiO 2 . High performance liquid chromatography (HPLC) was used to evaluate the extraction of NDGA from the medicinal plant ephedra by the above prepared materials, and the results indicated that the MIP@SiO 2 had potential application in separation of the natural active component NDGA from medicinal plants.
研究领域:
药物化学
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分析化学
✓ 已验证
产品关联
DOI
高影响因子
Frontiers in Pharmacology
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2020
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IF 4.225
Chen Qian,Zhu Min,Xie Jingwen,Dong Zhaojun,Khushafah Fatehi,Yun Di,Fu Weitao,Wang Ledan,Wei Tao,Liu Zhiguo,Qiu Peihong,Wu Jianzhang,Li Wulan
Aberrant fibroblast growth factor receptor-1 (FGFR1), a key driver promoting gastric cancer (GC) progression and chemo-resistance, has been increasingly recognized as a potential therapeutic target in GC. Hereon, we designed and synthesized a series of asymmetric analogues using Af23 and NDGA as lead compounds by retaining the basic structural framework (bisaryl-1,4-dien-3-one) and the unilateral active functional groups (3,4-dihydroxyl). Thereinto, Y14 showed considerable inhibitory activity against FGFR1. Next, pharmacological experiments showed that Y14 could significantly inhibit the phosphorylation of FGFR1 and its downstream kinase AKT and ERK, thus inhibiting the growth, survival, and migration of gastric cancer cells. Furthermore, compared with 5-FU treatment alone, the combination of Y14 and 5-FU significantly reduced the phosphorylation level of FGFR1, and enhanced the anti-cancer effect by inhibiting the viability and colony formation in two gastric cancer cell lines. These results confirmed that Y14 exerted anti-gastric activity and chemosensitizing effect by inhibiting FGFR1 phosphorylation and its downstream signaling pathway in vitro. This work also provides evidence that Y14, an effective FGFR1 inhibitor, could be used alone or in combination with chemotherapy to treat gastric cancer in the future.
研究领域:
肿瘤学
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药物化学
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分子生物学
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癌症研究
✓ 已验证
DOI
PubMed
高影响因子
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