Pharmaceutics
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2023
·Vol. 15
·期 7
·2010
·
IF 5.4
Fengming Tan,Huan Li,Kai Zhang,Lulu Xu,Dahan Zhang,Yang Han,Jing Han
Background: Hydroxy-α-Sanshool (HAS) possesses various pharmacological properties, such as analgesia and regulating gastrointestinal function. However, the low oral bioavailability of HAS has limited its oral delivery in clinical application. Methods and Results: To enhance its oral bioavailability, a nanocomposite delivery system based on chitosan (CH, as the polycation) and sodium alginate (SA, as the polyanion) was prepared using a layer-by-layer coating technique. The morphology, thermal behavior and Fourier transform infrared spectrum (FTIR) showed that the obtained sodium alginate/chitosan-coated HAS-loaded liposomes (SA/CH-HAS-LIP) with core-shell structures have been successfully covered with polymers. When compared with HAS-loaded liposomes (HAS-LIP), SA/CH-HAS-LIP displayed obvious pH sensitivity and a sustained-release behavior in in vitro studies, which fitted well to Weibull model. In vivo, the half-life of HAS from SA/CH-HAS-LIP remarkably extended after oral administration compared to the free drug. Additionally, it allowed a 4.6-fold and 4.2-fold increase in oral bioavailability, respectively, compared with free HAS and HAS-LIP. Conclusions: SA/CH-HAS-LIP could be a promising release vehicle for the oral delivery of HAS to increase its oral bioavailability.Keywords:hydroxy-α-sanshool;modified liposome;pH-response
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2023
·
IF 6.1
Jie Chen,Qin Liu,Longyu Yuan,Wenzhong Shen,Qingxing Shi,Guojun Qi,Ting Chen,Zhenfei Zhang
The brown planthopper (BPH) is the most serious pest causing yield losses in rice. MicroRNAs (miRNAs) are emerging as key modulators of plant–pest interactions. In the study, we found that osa-miR162a is induced in response to BPH attack in the seedling stage and tunes rice resistance to the BPH via the α-linolenic acid metabolism pathway as indicated by gas chromatography/liquid chromatography-mass spectrometry analysis. Overexpression of osa-miR162a inhibited the development and growth of the BPH and simultaneously reduced the release of 3-hexenal and 3-hexen-1-ol to block host recognition in the BPH. Moreover, knockdown of OsDCL1, which is targeted by osa-miR162a, inhibited α-linolenic acid metabolism to enhance the resistance to the BPH, which was similar to that in miR162a-overexpressing plants. Our study revealed a novel defense mechanism mediated by plant miRNAs developed during the long-term evolution of plant–host interaction, provided new ideas for the identification of rice resistance resources, and promoted a better understanding of pest control.
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CHEMICAL ENGINEERING JOURNAL
·
2023
·
IF 15.1
Jiani Lu,Yinan Wang,Hongda Li,Wei Hu,Guowei Zhou,Bin Sun,Shaonan Gu
Amorphous α-CoS, which has abundant unsaturated active sites, was used to construct Bi 2 MoS x O 6-x /α-CoS crystalline/amorphous S-scheme heterojunction on the crystalline surface of Bi 2 MoS x O 6-x to decompose amoxicillin. Amorphous surface adsorbed amoxicillin and activated it through elongating C−N and C=O bonds. Meanwhile, using S to partial substitute O in the MoO 6 octahedron to tune the band structure of Bi 2 MoS x O 6-x for increasing the visible-light utilization and optimizing the redox capability. Accordingly, the visible light absorbance range was extended to 735 nm with outstanding photo-electronic capabilities. The degradation rate catalyzed by Bi 2 MoS x O 6-x /α-CoS was promoted by two orders of magnitude, much higher than that of most of the reported photocatalysts. Furthermore, LC−MS/MS was employed to precisely track the amoxicillin degradation pathways. It was discovered that by attacking the reactive atoms of S7, N13, O21, C23, and O24 in amoxicillin, free radicals generated a series of intermediates with no apparent toxicity assessed by ecological structural activity relationships.
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2023
·Vol. 103
·期 15
·7381-7392
·
IF 4.1
Qinhao Guan,Lihua Tang,Liangliang Zhang,Lixin Huang,Man Xu,Yuan Wang,Meng Zhang
BACKGROUND Diabetes mellitus poses a substantial threat to public health due to rising morbidity and mortality. α-Glucosidase is one of the key enzymes affecting diabetes. Herein, (−)-epigallocatechin-3-gallate (EGCG) and (−)-epigallocatechin (EGC) were applied to clarify the role of the galloyl moiety of tea polyphenols in the inhibition of glycation and α-glucosidase activity. The structure–activity relationship of the galloyl moiety in EGCG on α-glucosidase was investigated in terms of inhibition kinetics, spectroscopy, atomic force microscopy and molecular docking. A bovine serum protein–fructose model was employed to determine the effect of the galloyl moiety on glycation. RESULTS The results indicated that the introduction of a galloyl moiety enhanced the capacity of EGCG to inhibit glycation and α-glucosidase activity. The IC 50 value of EGC is approximately 2400 times higher than that of EGCG. Furthermore, the galloyl moiety in EGCG altered the microenvironment and secondary structure of α-glucosidase, resulting in a high binding affinity of EGCG to α-glucosidase. The binding constant of EGCG to α-glucosidase at 298 K is approximately 28 times higher than that of EGC. CONCLUSION Overall, the galloyl moiety of EGCG plays a crucial role in inhibiting glycation and α-glucosidase activity, which helps to enhance the molecular understanding of the structure and function of the polyphenol galloyl moiety in the science of food and agriculture. © 2023 Society of Chemical Industry.
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PHYTOCHEMISTRY
·
2023
·
IF 3.8
Qi Hong,Miao-Miao Guo,Jin Yang,Xing Wei,Li Liao,Xiu-Juan Xin,Di Zhang,Fa-Liang An
Four previously undescribed diketopiperazine-type alkaloids including one oxepin-containing diketopiperazine-type alkaloid, oxepinamide L (1), three 4-quinazolinone alkaloids, puniceloids E-G (10–12), together with 12 known analogues, protuboxepin D (2), oxepinamides D-G, J-K and I (3–9), puniceloids B-D (13–15) and protubonine B (16), were isolated from the culture of the marine-derived fungus Aspergillus puniceus FAHY0085. The structures of the previously undescribed compounds were comprehensively elucidated by detailed interpretation of their NMR and HRESIMS data. Their absolute configurations were unambiguously determined by ROESY experiments, Marfey's method, calculated ECD experiments and single-crystal X-ray diffraction analysis. Compounds (3–4, 6–8, 14–15) were evaluated for their cytotoxic activity against HepG2, MCF-7, SW1116 and HeLa cells and compound 6 and 14 showed moderate cytotoxic activity against HeLa cells with IC 50 49.61 ± 2.91 and 28.38 ± 1.57 μM, respectively. Compounds (1–8, 11–15) were screened for their transcriptional activation of liver X receptor α and compound 11 with known compounds 13–15 showed significant transcriptional activation of liver X receptor α with EC 50 values in the range 2–50 μM.
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JOURNAL OF ORGANIC CHEMISTRY
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2022
·
IF 4.198
Hong-Li Huang,Juan Xu,Ya-Xin Fan,Qing-Qiang Su,Ji-Yuan Du,Ru-Fen Zhang,Yan-lan Wang,Honggang Hu,Fei Gao
The visible-light-promoted difunctionalization of alkenyl ketones has been developed for easy access of various tetralones, cyclopropane, or alkenyl migration compounds. With fac-[Ir(ppy)3] as the photocatalyst, alkenyl ketones captured the α-carbonyl alkyl radical and evolved through intramolecular cyclization and the elimination of a proton to give the difunctionalized products. This strategy is characterized by good yields, mild reaction conditions, and outstanding functional group tolerance.
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MACROMOLECULES
·
2022
·
IF 6.057
Xin Ning Zhang,Cong Du,Yan Jie Wang,Li Xin Hou,Miao Du,Qiang Zheng,Zi Liang Wu
The molecular chemical structure has a decisive influence on physicochemical properties of polymer materials, which becomes more complex for hydrogels with dense associative interactions. Recently, we have developed a series of tough supramolecular hydrogels with robust hydrogen-bond associations, and the properties of gels severely depend on the composition of copolymers. Here, we examine the influence of the molecular structure on the mechanical and viscoelastic behaviors of these supramolecular hydrogels synthesized from copolymerization of acrylamide/methacrylamide and acrylic acid/methacrylic acid with a varied α-methyl group on the basic unit. The obtained four kinds of the as-prepared hydrogels exhibit distinct mechanical performances and dynamics, evolving from elastic to glassy state with the increase in the number of α-methyl groups. Rheological dynamic spectra of these hydrogels follow the time–temperature superposition principle, which are used to elucidate the correlation between the chemical structure and the dynamics of gel materials. The incorporation of a hydrophobic α-methyl group effectively improves the chain rigidity and enhances the hydrogen-bond associations. Furthermore, the methyl group on the carboxylic acid unit strengthens the hydrogels more significantly than that on the acrylamide unit, which also results in distinct stability of the hydrogels in water. This comparative study discloses the effect of the α-methyl group on the dynamics of associative copolymers and the performances of supramolecular hydrogels, which should be informative to understand the structure–property relationship of other tough soft materials with associative interactions.
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Drug Design Development and Therapy
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2022
·
IF 4.319
Wen-Gang Chen,Sa-Sa Zhang,Shu Pan,Zhong-Fang Wang,Jin-Ying Xu,Xue-He Sheng,Qin Yin,Yi-Jin Wu
Background Studies have found that α-mangostin (MG) can relieve experimental arthritis by activating cholinergic anti-inflammatory pathway (CAP). It affects the polarization of macrophages and the balance of related immune cell subpopulations, but the specific mechanism is still unclear. It has been found that silent information regulator 1 (SIRT1) is closely related to macrophage activity. The purpose of this study is to explore the mechanism of MG intervening in macrophage polarization during treatment of early adjuvant-induced (AIA) rats through the CAP-SIRT1 pathway.Methods We investigated the polarization of M1 macrophages and the differentiation of Th1 in AIA rats by flow cytometry. Activity of acetylcholinesterase (AChE) and the level of nicotinic adenine dinucleotide (NAD+) in serum were also detected, and immunohistochemical was used to detect the levels of α7 nicotinic cholinergic receptor (α7nAChR) and SIRT1. Then in macrophages, the molecular mechanism of MG regulating the abnormal activation of macrophages in rats with early AIA through the CAP-SIRT1 pathway was studied.Results MG can significantly inhibit the polarization of M1 macrophages and the differentiation of Th1 in AIA rats in the acute phase of inflammation. MG can significantly inhibit the activity of AChE and increase the level of NAD+, thereby further up-regulated the expression levels of α7nAChR and SIRT1. Meanwhile, MG inhibited nuclear factor-κB (NF-κB)-mediated inflammation by activating the CAP-SIRT1 pathway in macrophages.Conclusion In summary, the stimulation of MG induced CAP activation, which up-regulated SIRT1 signal, and thereby inhibited M1 polarization through the NF-κB pathway, and improved the pathological immune environment of early-stage AIA rats.
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BIOMEDICAL CHROMATOGRAPHY
·
2022
·Vol. 37
·期 2
·e5536
·
IF 1.911
Qi Dong,Na Hu,Huilan Yue,Honglun Wang,Yue Wei
α -glucosidase inhibitors (AGIs) are widely used for the treatment of type 2 diabetes, but their side effects have made it to develop novel and alternative AGIs immediately. In this study, the extract of Hypericum perforatum L. (HPE) has been confirmed to have α -glucosidase inhibitory activity in vitro and in vivo. Seven active compounds, rutin, hyperoside, isoquercitrin, avicularin, quercitrin, quercetin, and biapigenin, were screened based on a bio-affinity chromatography column with α -glucosidase enzyme-conjugated solid phase and UPLC/MS, which exhibited excellent α -glycosidase inhibitory effects by the determined IC 50 values. The mechanism of α -glycosidase inhibitory activity of biapigenin was studied for the first time. The results showed that biapigenin was a high-potential, reversible, and mixed enzyme inhibitor. Analysis by molecular docking further revealed that hydrophobic interactions were generated by interactions between biapigenin and amino acid residues LYS156, PHE303, PHE314, and LEU313. In addition, hydrogen bonding occurred between biapigenin and α -glucosidase amino acid residues ASP307, SER241, and LYS156. This research identified that biapigenin could be a novel AGI and further applied to the development of potential anti-diabetic drugs. Furthermore, our studies established a rapid in vitro screening method for AGIs from plants.
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ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
·
2022
·Vol. 29
·期 52
·78874-78886
·
IF 5.19
Xu Junge,Hu Die,Wang Yingmu,Zhang Ziwei
Ciprofloxacin (CIP) is a third-generation fluoroquinolones (FQs) antibiotic, and the occurrence of CIP in the water environment has raised growing concerns owning to its environmental toxicity. In this paper, a novel α-(Fe, Cu)OOH/RGO nanocomposite was synthesized via a one-step reflux method for CIP degradation through a photo-Fenton-like process. When the RGO content was 1 wt%, CIP degradation ratio by the α-(Fe, Cu)OOH/RGO nanocomposite reached 100% under visible light irradiation within 120 min, and total organic carbon (TOC) removal ratio reached 60% within 180 min. The result of molecular fluorescence spectra highlighted that the loading of RGO on the α-(Fe, Cu)OOH significantly increased the content of hydroxyl radicals (·OH) in the heterogeneous photo-Fenton-like system and simultaneously inhibited the recombination of photogenerated electron and hole, which played critical roles in the enhancement of CIP degradation. In addition, 11 main intermediates were identified as the degradation products of CIP in the α-(Fe, Cu)OOH/RGO/H 2 O 2 /visible light reaction systems using liquid chromatograph–mass spectrometer (LC-MS) analyses. The results demonstrated that three degradation pathways for CIP removal by α-(Fe, Cu)OOH/RGO nanocomposite occurred, including (i) oxidation on the piperazine ring and dealkylation, (ii) defluorination and decarboxylation, and (iii) hydroxylation on the quinolone ring. This work would provide a novel insight of CIP degradation pathways in photo-Fenton-like processes. Graphical abstract
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Catalysis Science & Technology
·
2022
·Vol. 12
·期 20
·6163-6173
·
IF 6.177
Jin Zhang,Mengting Gao,Ruiyi Wang,Xincheng Li,Pengqi Zhu,Yunwei Wang,Zhanfeng Zheng
Selective hydrogenation of α,β-unsaturated aldehydes under mild conditions is a great challenge in the synthesis of the corresponding alcohols. Herein, we report that a series of oxygen vacancy enriched MgAl-LDH coordinated transition metal hydroxide M(OH)x (M = Ru, Pt, Pd, Ag, Rh, Fe, Co, Ni and Cu) photocatalysts were successfully prepared taking advantage of the “memory effect” of MgAl-LDH. A high yield of α,β-unsaturated alcohols was achieved under visible light irradiation. DFT simulations and DRIFTS results show that oxygen vacancies facilitate the adsorption of –CO groups and hinder the adsorption of –CC groups in cinnamaldehyde, which ensures the high selectivity to cinnamyl alcohol. The highly dispersed and electron-rich transition metal hydroxides facilitated the activation of isopropanol to provide active H species under light irradiation and then enhanced the photocatalytic performance. This study demonstrated oxygen vacancy enriched MgAl-LDH supported transition metal hydroxide M(OH)x photocatalysts for efficient selective hydrogenation under visible light irradiation.
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JOURNAL OF LIQUID CHROMATOGRAPHY & RELATED TECHNOLOGIES
·
2022
·
IF 1.467
Yi Zhang,Jing Meng,Shuai Wang,Dongyu Gu,Xingtao Lin,Dezhi Huang,Yi Yang
Toona sinensis is a traditional vegetable with rich nutrition and wide biological activity. In our previous study, an active composition against α-amylase was screened from T. sinensis by ligand fishing. To investigate the effect of T. sinensis on other targets of antidiabetes, in this work, α-glucosidase was immobilized on polydopamine-coated magnetic nanoparticles to further screen the compounds against α-glucosidase by ligand fishing. The enzyme activity test showed that the 70% ethanol extract of T. sinensis (crude sample) had weak α-glucosidase inhibitory activity, but after extraction with different solvents, the ethyl acetate extract showed the highest α-glucosidase inhibitory activity. After immobilization of α-glucosidase on polydopamine (PDA)-coated magnetic nanoparticles, the properties of the enzyme were characterized and determined, and then quercetin-3-O-α-L-rhamnopyranoside was screened by ligand fishing and isolated by high-speed counter-current chromatography using the two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water (1:5:1:5, v/v). The results of enzymes assay showed that the screened compound (IC50 value of 374.94 ± 4.35 μg/mL) possessed moderate α-glucosidase inhibitory activity. The presented results not only proved that ligand fishing based on polydopamine-coated magnetic α-glucosidase was an effective method for the rapid discovery of natural active substances, but also further strengthened the evidence of antidiabetic effect of T. sinensis.
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