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PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY · 2022 · IF 3.915

Hyperoside-loaded TPGs/mPEG-PDLLA self-assembled polymeric micelles: preparation, characterization and in vitro/in vivo evaluation

Xiaoli Xia,Jian Zhang,Michael Adu‑Frimpong,Xiaoxiao Li,Xinyi Shen,Qing He,Wanjing Rong,Hao Ji,Elmurat Toreniyazov,Ximing Xu,Jiangnan Yu,Qilong Wang

Hyperoside (Hyp) self-assembled polymeric micelles (Hyp-PMs) were purposely developed to enhance aqueous solubility, in vivo availability and anti-oxidative effect of Hyp. In preparing Hyp-PMs, we employed the thin film dispersion method with the micelles consisting of TPGs and mPEG2000-PDLLA3000. The particle size, polydispersity index and zeta potential of Hyp-PMs were 67.42 ± 1.44 nm, 0.229 ± 0.015 and −18.67 ± 0.576 mV, respectively, coupled with high encapsulation efficiency (EE)of 90.63 ± 1.45% and drug loading (DL) of 6.97 ± 1.56%. Furthermore, the value of critical micelle concentration (CMC) was quite low, which indicated good stability and improved self-assembly ability of Hyp-PMs. Also, trend of in vitro Hyp release from Hyp-PMs demonstrated enhanced solubility of Hyp. Similarly, in comparison with free Hyp, oral bioavailability of Hyp-PMs was improved (about 8 folds) whilst half-life of Hyp-PMs was extended (about 3 folds). In vitro anti-oxidative effect showed obvious strong scavenging DPPH capability of Hyp-PMs, which may be attributed to its smaller size and better solubility. Altogether, Hyp-PMs may serve as a possible strategy to potentially enhance aqueous solubility, bioavailability and anti-oxidative effect of Hyp, which may play a key role in Hyp application in the pharmaceutical industries.

CAS / MDL: 298-93-1
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Foods · 2023 ·Vol. 12 ·期 2 ·321 · IF 5.2

Reduction in Five Harmful Substances in Fried Potato Chips by Pre-Soaking Treatment with Different Tea Extracts

Weitao Wang,Huaixu Wang,Zhongjun Wu,Tingting Duan,Pengzhan Liu,Shiyi Ou,Hani El-Nezami,Jie Zheng

Thermally processed food always contains various types of harmful substances. Control of their levels in food is important for human health. This work used the extracts from green tea dust, old green tea, yellow tea, white tea, oolong tea, and black tea to simultaneously mitigate diverse harmful substances in fried potato chips. The six tea extracts (30 g/L) all showed considerable inhibitory effects on the formation of 5-hydroxymethylfurfural (reduced by 19.8%–53.2%), glyoxal (26.9%–36.6%), and methylglyoxal (16.1%–75.1%). Green tea and black tea extracts exhibited better inhibitory abilities than the other three teas and were further investigated for other harmful compounds by various concentration treatments. Finally, pre-soaking of fresh potato slices in 50 g/L extracts of green tea dust displayed, overall, the most promising inhibitory capacity of HMF (decreased by 73.3%), glyoxal (20.3%), methylglyoxal (69.7%), acrylamide (21.8%), and fluorescent AGEs (42.9%) in fried potato chips, while it exhibited the least impact on the color and texture. The high level of catechins in green tea dust may contribute most to its outstanding inhibitory effect, whereas the distinguished inhibitory effect of black tea extract was speculated to be attributable to the high levels of theaflavins and amino acids in the fully fermented tea. This study indicated that green tea dust, a predominant waste of the tea industry, had great potential to be exploited to improve food quality and safety.Keywords:potato chips;tea extract;5-hydroxymethylfurfural;acrylamide;dicarbonyl compounds;advanced glycation end-products

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ANALYST · 2023 ·Vol. 148 ·期 7 ·1492-1499 · IF 4.2

A nanopore counter for highly sensitive evaluation of DNA methylation and its application in in vitro diagnostics

Jiahai Wang,Lanfang Chen,Cenlin Gui,Jianji Zhu,Baian Zhu,Zhuobin Zhu,Yunhui Li,Daqi Chen

DNA methylation has been considered an essential epigenetic biomarker for diagnosing various diseases, such as cancer. A simple and sensitive way for DNA methylation level detection is necessary. Inspired by the label-free and ultra-high sensitivity of solid-state nanopores to double-stranded DNA (dsDNA), we proposed a nanopore counter for evaluating DNA methylation by integrating a dual-restriction endonuclease digestion strategy coupled with polymerase chain reaction (PCR) amplification. Simultaneous application of BstUI/HhaI endonucleases can ensure the full digestion of the unmethylated target DNA but shows no effect on the methylated ones. Therefore, only the methylated DNA remains intact and can trigger the subsequent PCR reaction, producing a large quantity of fixed-length PCR amplicons, which can be directly detected through glassy nanopores. By simply counting the event rate of the translocation signals, the concentration of methylated DNA can be determined to range from 1 aM to 0.1 nM, with the detection limit as low as 0.61 aM. Moreover, a 0.01% DNA methylation level was successfully distinguished. The strategy of using the nanopore counter for highly sensitive DNA methylation evaluation would be a low-cost but reliable alternative in the analysis of DNA methylation.

CAS / MDL: 9012-36-6
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2022 · IF 8.025

Gelatin/alginate-based microspheres with sphere-in-capsule structure for spatiotemporal manipulative drug release in gastrointestinal tract

Tao Long,Weiwei Tan,Xiangmin Tian,Zongjian Tang,Keming Hu,Liming Ge,Changdao Mu,Xinying Li,Yongbin Xu,Lei Zhao,Defu Li

Microsphere with sphere-in-capsule structure is a multi-drugs delivery system to achieve the purpose of combination therapy. In this paper, we have prepared gelatin/alginate-based microspheres with sphere-in-capsule structure by a relatively fast, simple, and easily large-scale industrialized emulsification method for spatiotemporal manipulative drug release in gastrointestinal tract. Calcium alginate microspheres encapsulated with bovine serum albumin (BSA) were first prepared as inner microspheres, and then inner microspheres and ranitidine hydrochloride (RH) were co-encapsulated by gelatin microspheres to form double-layer microspheres with sphere-in-capsule structure. The size and distribution of microspheres can be easily controlled by emulsifying conditions. The microspheres with sphere-in-capsule structure displayed desirable encapsulation efficiency of BSA (61.52 %) and RH (56.07 %). The in vitro simulated drug release showed the spatiotemporal release feature of microspheres with sphere-in-capsule structure. In the specific simulated fluid, the release behavior and cumulative release of RH (sustainedly released 95 % in simulated gastric fluid) and BSA (rapidly released 73 % in simulated intestinal fluid) were different. The drug release mechanisms were analyzed to determine RH and BSA's release behavior. Overall, the microspheres with sphere-in-capsule structure have the potential application of spatiotemporal manipulative drug delivery in the gastrointestinal tract.

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Food Chemistry-X · 2023 · IF 6.1

Comprehensive analysis in the nutritional composition, phenolic species and in vitro antioxidant activities of different pea cultivars

Shi-Kang Chen,Hai-Feng Lin,Xin Wang,Yi Yuan,Jun-Yi Yin,Xiao-Xiao Song

In this study, ten pea ( Pisum sativum L.) varieties were compared in their nutrient composition, phenolic compounds, antioxidant properties and their diversity were deciphered by multivariate analysis of correlation analysis and principal component analysis (PCA). The ten pea cultivars are rich in nutrients with different contents in lipid (0.57 to 3.52%), dietary fiber (11.34 to 16.13%), soluble sugar (17.53 to 23.99%), protein (19.75 to 26.48%) and starch (32.56 to 48.57%). Through the UPLC-QTOF-MS and HPLC-QQQ-MS/MS analysis, the ethanol extracts of ten peas mainly included 12 kinds of phenolic substances and showed good antioxidant activities on the 1,1-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, ferric reducing antioxidant power (FRAP) and oxygen radical absorbance capacity (ORAC). The phenolic content and protocatechuic acid showed a positive correlation with antioxidant capacity. All results provide theoretical basis for the development and rational application of different varieties of peas and their related products.

CAS / MDL: 108-95-2
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ACS Biomaterials Science & Engineering · 2023 · IF 5.8

Synthesis, Characterization, In Vitro Cytological Responses, and In Vivo Bone Regeneration Effects of Low-Crystalline Nanocarbonated Hydroxyapatite

Teliang Lu,Siwen Yan,Haishan Shi,Jiandong Ye

Hydroxyapatite (HA) has been commonly used as an alternative bone substitute. But it has drawbacks, such as poor degradation and limited osteogenesis. Low-crystalline carbonated hydroxyapatite (L-CHA), which has greater biodegradability than HA, is suggested as one of the main components of bone minerals, but the exact mechanism behind the roles of carbonate substituted in biological behaviors of low-crystalline HA is still a mystery. In this study, L-CHAs with different carbonate contents were prepared, and the effects of the content on the physicochemical properties, in vitro cytological responses, and in vivo bone defects repair effects of L-CHAs were investigated. The results demonstrated that CO32– had successfully entered the lattice structure of L-CHAs with a maximum content of 9.2 wt %. Both low-crystalline undoped HA (L-HA) and L-CHAs were nanocrystalline (20–30 nm) with significantly higher specific surface areas, protein adsorption capacities, and biodegradability compared to high-crystalline HA (H-HA) with submicron crystalline size (200–400 nm). Besides, the amounts of the adsorbed protein and released Ca2+ ions increased in a carbonate-content-dependent manner. Compared to L-HA and H-HA, L-CHAs promoted the adhesion and proliferation of bone marrow mesenchymal stem cells and significantly upregulated the levels of alkaline phosphatase (ALP) activity and the expression of osteogenesis-related genes. In addition, L-CHA-9 not only showed a faster biodegradation rate but also effectively promoted bone regeneration when implanted in the critical-sized bone defects of rabbit femora. This study provided evidence for the development of L-CHA as a promising biodegradable and bioactive material with great osteoconductivity and osteogenic capability with respect to conventional HA.

CAS / MDL: 9004-34-6 9004-67-5
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FOOD RESEARCH INTERNATIONAL · 2023 · IF 8.1

High Fischer ratio peptide of hemp seed: Preparation and anti-fatigue evaluation in vivo and in vitro

Zhu Ying,Huang Yuyang,Li Meiying,Sun Bingyu,Liu Linlin,Lv Mingshou,Qu Min,Guan Huanan,Zhu Xiuqing

The high Fischer (F) ratio hemp peptide (HFHP) was prepared by enrichment using activated carbon adsorption, ultrafiltration, and Sephadex G-25 gel filtration chromatography. The OD 220 /OD 280 ratio reached 47.1 with a molecular weight distribution from 180 to 980 Da, a peptide yield up to 21.7 %, and the F value was 31.5. HFHP had high scavenging ability of DPPH, hydroxyl free radicals, and superoxide. Mice experiments showed that the HFHP increased the activity of superoxide dismutase and glutathione peroxidase. The HFHP had no effect on the body weight of mice, but prolonged their weight-bearing swimming time. The lactic acid, serum urea nitrogen, and malondialdehyde of the mice after swimming was reduced, and the liver glycogen increased. The correlation analysis indicated that the HFHP had significant anti-oxidation and anti-fatigue properties.

CAS / MDL: 7440-44-0 64365-11-3
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ACS Applied Materials & Interfaces · 2023 · IF 9.5

Microcapsule-Based Autonomous Self-Healing of Electrical Damage in Dielectric Polymers Induced by In Situ Generated Radicals

Jiaye Xie,Lu Han,Zhen Luo,Qi Li,Jinliang He

Dielectric polymers are playing important roles in electrical and electronic industries. However, aging under high electric stress is a main threat to the reliability of polymers. In this work, we demonstrate a self-healing method for electrical tree damage based on radical chain polymerization, which is initiated by in situ radicals that are generated during electrical aging. Acrylate monomers contained in microcapsules will be released and flow into hollow channels after the capsules are punctured by electrical trees. Autonomous radical polymerization of the monomers will heal the damaged regions, which is triggered by radicals resulting from polymer chain scissions. After optimizing the healing agent compositions by evaluating their polymerization rate and dielectric properties, the fabricated self-healing epoxy resins showed effective recovery from treeing in multiple aging–healing cycles. We also expect the great potential of this method to heal tree defects autonomously without the need to switch off operating voltages. This novel self-healing strategy will shed light on building smart dielectric polymers with its broad applicability and online healing competence.

CAS / MDL: 94-36-0
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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY · 2023 · IF 3.4

In vivo and in vitro evaluation of pulmonary administration of itraconazole nanostructured lipid carriers for pulmonary aspergillosis

Yanming Wang,Zhang Chenghao,Zhaoli Wu,Xinran Cui,Jinmei Ren,Jingling Tang

Objective Pulmonary aspergillosis, which is a secondary complication of fungal pneumonia, is widely considered to have an increasing incidence and high mortality. Itraconazole (Itz) can inhibit ergosterol biosynthesis to treat pulmonary aspergillosis. Nevereless, Itz’s clinical application is limited because of its poor water solubility, low oral bioavailability, and systemic hepatotoxicity. In this study, Itz-loaded nanostructured lipid carriers (Itz-NLCs) were developed to improve the in vitro permeability and bioavailability of Itz via pulmonary administration.Methods Itz-NLCs were prepared by the emulsification-evaporation method using oleic acid and glycerol monostearate as liquid and solid lipids, respectively.Results The Itz-NLCs were optimized with tiny particle size, uniform distribution, and excellent entrapment efficiency (EE, 97.57% ± 0.45%). A Xenopus alveolar membrane was used in the permeation study, and the cumulative permeation percentage of Itz was 10% for Itz-NLCs at 8 h, which was 2.50-fold higher than that for Itz suspensions (4%, p < .001). A rabbit pharmacokinetic investigation revealed that Itz-NLCs have an 83.05% absolute bioavailability after intratracheal instillation.Conclusions The purpose of Itz-NLCs is to enhance the bioavailability and permeability of Itz in vitro for administration via the lungs.

CAS / MDL: 61791-12-6
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INVESTIGATIONAL NEW DRUGS · 2023 ·Vol. 41 ·期 1 ·134-141 · IF 3.4

Viscosalactone B, a natural LSD1 inhibitor, inhibits proliferation in vitro and in vivo against prostate cancer cells

Yan Gaobo,Zhang Hongyan,Li Yan,Miao Guoqiang,Liu Xiaolei,Lv Qifan

Lysine-specific demethylase 1 (LSD1) has been a promising target to treat prostate cancer, and discovery of novel LSD1 inhibitors would have great clinical significance. In this work, viscosalactone B was first identified as a novel LSD1 inhibitor. Viscosalactone B isolated from Withania Somnifera displayed antiproliferative activity against PC3, DU145, C42B, PC3/MDVR, DU145/MDVR, and C42B/MDVR cells with IC 50 values of 1.17, 0.72, 3.86, 2.06, 0.96 and 1.15 μM, respectively. In comparison, it was a selective LSD1 inhibitor with an IC 50 value of 970.27 nM and could induce a significant accumulation of LSD1 substrates H3K9me1, H3K9me2, and H3K4me1 in a concentration-dependent manner in DU145 cells. According to docking studies, it formed hydrogen bonds with the Thr11, Lys14, and Arg8 residues of LSD1. Importantly, while it displayed potent antitumor efficacy in vivo, it did not show obvious cytotoxicity on the major organs of nude mice. Therefore, viscosalactone B, as a novel LSD1 inhibitor, is a potential candidate that can be used for the treatment of prostate cancer in clinics.

CAS / MDL: 1330-20-7
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Jove-Journal of Visualized Experiments · 2022 · IF 1.424

Real-Time Detection of Reactive Oxygen Species Production in Immune Response in Rice with a Chemiluminescence Assay

Ying Wang,Zhuo An,Zhifang Zhao,Can Li,Jiangbo Fan

Reactive oxygen species (ROS) play vital roles in a variety of biological processes, including the sensing of abiotic and biotic stresses. Upon pathogen infection or challenge with pathogen-associated chemicals (pathogen-associated molecular patterns [PAMPs]), an array of immune responses, including a ROS burst, are quickly induced in plants, which is called PAMP-triggered immunity (PTI). A ROS burst is a hallmark PTI response, which is catalyzed by a group of plasma membrane-localized NADPH oxidases-the RBOH family proteins. The vast majority of ROS comprise hydrogen peroxide (H2O2), which can be easily and steadily detected by a luminol-based chemiluminescence method. Chemiluminescence is a photon-producing reaction in which luminol, or its derivative (such as L-012), undergoes a redox reaction with ROS under the action of a catalyst. This paper describes an optimized L-012-based chemiluminescence method to detect apoplast ROS production in real-time upon PAMP elicitation in rice tissues. The method is easy, steady, standardized, and highly reproducible under firmly controlled conditions.

CAS / MDL: 7681-52-9
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Food & Function · 2022 ·Vol. 13 ·期 22 ·11652-11663 · IF 6.317

Co-encapsulation of quercetin and resveratrol in zein/carboxymethyl cellulose nanoparticles: characterization, stability and in vitro digestion

Zhongyu Yang,David Julian McClements,Xinwen Peng,Chao Qiu,Jie Long,Jianwei Zhao,Zhenlin Xu,Man Meng,Long Chen,Zhengyu Jin

Oral administration of combinations of specific nutrients and nutraceuticals can provide synergistic health benefits to humans. In this work, zein/carboxymethyl cellulose composite nanoparticles were successfully prepared using antisolvent precipitation methods. Zein/carboxymethyl cellulose nanoparticles with the smallest size (204.6 nm) were formed when the mass ratio of zein to CMC was 2 : 1. Hydrogen bonding and hydrophobic interactions were dominant binding forces to stabilize the composite nanoparticles. Quercetin and resveratrol were then encapsulated within these nanocarriers, which improved their resistance to both light and thermal degradation. Encapsulation of the nutraceuticals was shown to delay their release under simulated gastrointestinal conditions, which may be beneficial for some applications. Moreover, encapsulation increased the in vitro bioaccessibility of the quercetin and resveratrol. Our results indicate that zein/carboxymethyl cellulose nanoparticles can be used to co-deliver combinations of bioactive compounds, which may be useful for the development of functional foods, supplements, and pharmaceuticals.

CAS / MDL: 501-36-0
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