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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2018 · IF 2.297

Effect of PI3K/Akt signal pathway inhibitor on docetaxel nanoparticles in cell uptake, cell colony, caspase-3 & caspase-9 expression and pharmacokinetics

Yunzhi Yin,Yiyue Wang,Jun Zhang,Jing Li,Jingjing Chen,Qi Shen

Docetaxel (DTX) is one kind of well-known anticancer drugs against tumors. GDC0941 was used to inhibit PI3K/Akt signal pathway and improve anti-tumor activity. PLGA-PEG-R7 (poly lactic-co-glycolic acid polyethylene glycol bending with cell penetrating peptide R7)/poly sulfadimethoxine-Folate nanoparticles (R7/PSD-Fol NPs) were made to load DTX and GDC0941 simultaneously. In vitro, the release capacity of DTX and GDC0941 inside nanoparticles was determined and both drugs could release from nanoparticles to 70% within 48h. The result of flow cytometry showed that GDC0941 had no interference on cell uptake and R7/PSD-Fol NPs could enhance MCF-7 cells uptake the most significantly. In cell colony study, GDC0941 could further improve the anti-tumor effect of DTX and inhibit the formation of cell clones on the basis of enhancing the uptake of R7/PSD-Fol NPs. The capability of cell colony formation was as follows: DTX > DTX + GDC0941 > R7 NPs > R7/PSD-Fol NPs. The expression of cell apoptosis proteins treated with R7/PSD-Fol NPs was the lowest. The addition of GDC0941 could decrease the full-length content of apoptotic proteins caspase-3 and caspase-9. In vivo, pharmacokinetic parameters results showed us that GDC0941 had no interference on pharmacokinetic study. Main pharmacokinetic parameters of DTX suspension and R7/PSD-Folate NPs suspension showed significant differences.

CAS / MDL: 59-30-3 9002-89-5
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FOOD CHEMISTRY · 2022 · IF 9.231

Development of nonionic nanoemulsions to improve hydrophobic 9′-cis-bixin stability in acidic aqueous medium with in vitro cytosis and nanosafety evaluation

Yuhao Zhu,Chenming Dai,Danyu Lv,Yongguang Guan

Nonionic oil-in-water (O/W) nanoemulsion provides potential to stabilize hydrophobic bio-functional components in aqueous medium. Understanding safety of nanoemulsion droplets via investigating in vitro cell uptake and cellular substructural changes is important to achieve their practical applications. Herein, we developed a nonionic O/W nanoemulsion to stabilize representative bio-functional hydrophobic component of 9′- cis -bixin at pH 3–7 and ultraviolet (UV)-induced degradation at 365, 302, and 254 nm. In vitro cell uptake demonstrated that Caco-2 cells adequately enriched 9′- cis -bixin through fast uptake of nanoemulsion droplets within 15 min. However, excessive nanoemulsion droplets greatly decreased cell survival rate, which was due to the potential destruction of cellular substructures of mitochondria, nuclear membrane, and cell membrane. Lower nanoemulsion concentration provided no significant effects on Caco-2 cell survival. This work provided objective understanding on bio-functional component stability by nanoemulsion with in vitro safety evaluation.

CAS / MDL: 75-05-8 499-75-2 68-12-2
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JOURNAL OF CHROMATOGRAPHY A · 2020 · IF 4.049

9-Plex ultra high performance liquid chromatography tandem mass spectrometry determination of free hydroxyl polycyclic aromatic hydrocarbons in human plasma and urine

Luping Sun,Shuyun Zhu,Zhenjia Zheng,Jing Sun,Xian-En Zhao,Huwei Liu

Hydroxyl-polycyclic aromatic hydrocarbons (OH-PAHs) are biomarkers for assessing the exposure levels of polycyclic aromatic hydrocarbons (PAHs). A series of stable isotope mass tags (SIMT-332/338/346/349/351/354/360/363/374/377) were firstly designed and synthesized to perform multiplexed stable isotope labeling derivatization (MSILD) of OH-PAHs in human plasma and urine. Their derivatives were enriched and purified by magnetic dispersive solid phase extraction (MDSPE) using prepared Fe 3 O 4 /GO and then determined by ultra high performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) in multiple reaction monitoring mode. 9-Plexed MSILD reagents were prepared using pipemidic acid as core structure with different isotope mass tags, in which carbonyl chloride group was used to label OH-PAHs. The SIMT-346 labeled OH-PAHs standards were used as internal standards, which can greatly increase the quantitative accuracy. 9-Plex labeled nine different real samples can be quantified by UHPLC-MS/MS in a single run. Under optimized MSILD-MDSPE conditions, good linearities of seven OH-PAHs were obtained with satisfactory coefficient of determination R 2  > 0.991. Limits of detection (LODs) of seven OH-PAHs were from 0.1 to 0.5 pg/mL, and limits of quantitation (LOQs) ranged from 0.5 to 2.0 pg/mL. The intra- and inter-day precisions ranged in 2.3–12.4% with accuracies in the range of 91.7–108.4%. Acceptable results of matrix effect (89.7–105.7%) and derivatization efficiency (> 96.4%) were obtained. In short, the developed method has been proved to be high-throughput, sensitive, accurate and easy-handling. This method was applied for the measurement of seven free OH-PAHs in human urine and plasma, and expected to provide technical support for the evaluation of PAHs exposure levels in humans.

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Food & Function · 2020 ·Vol. 11 ·期 7 ·6128-6138 · IF 4.171

Fruiting body polysaccharides of Hericium erinaceus induce apoptosis in human colorectal cancer cells via ROS generation mediating caspase-9-dependent signaling pathways

Xiao-xiao Hou,Jing-yu Liu,Zhuo-yu Li,Ming-chang Chang,Min Guo,Cui-ping Feng,Jiang-ying Shi

The fruiting bodies of Hericium erinaceus (Bull.) Pers. are commonly used in China in the treatment of digestive system diseases. In this work, the polysaccharides from the fruiting bodies of Hericium erinaceus (HEFPs) were extracted, and their effects on human colorectal cancer cells (HCT-116 and DLD1) were investigated in vitro. Our results showed that HEFPs were mainly composed of arabinose, galactose, glucose, and mannose at a molar ratio of 8.99 : 11.15 : 1.2 : 1.97. They significantly inhibited the growth of these cells by inducing apoptosis by the modulation of Bax and Bcl-2 expression, which in turn induced the loss of mitochondrial membrane potential, leading to the activation of cleaved-caspase-9 and cleaved-caspase-3. These results suggested that HEFPs induced apoptosis via the caspase-9-depedent intrinsic mitochondrial pathway. Furthermore, HEFPs increased the level of reactive oxygen species (ROS) in HCT-116 and DLD1 cells. The addition of the antioxidant N-acetyl-L-cysteine reduced the ability of HEFPs to trigger the intrinsic mitochondrial pathway, indicating the role of ROS generation in the upstream pathway of HEFP-induced apoptosis. Therefore, the results described in this study could be of interest for further studies in finding functional foods or alternative therapeutic agents against colorectal cancer.

CAS / MDL: 76-05-1
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ADVANCED FUNCTIONAL MATERIALS · 2024 · IF 18.5

Brain-Targeted 9-Phenanthrol-Loaded Lipid Nanoparticle Prevents Brain Edema after Cerebral Ischemia-Reperfusion Injury by Inhibiting the Trpm4 Channel in Mice

Kewei Liu,Yuqin Peng,Mingheng Xu,Kun Yuan,Yongchuan Li,Chuman Lin,Xiaolin Zhao,Juan Zhu,Yuan Chang,Zhenzhou Lin,Suyue Pan,Huanrong Ma,Xiaorui Wang,Kaibin Huang

Brain edema robustly increases mortality and hinders functional recovery after acute ischemic stroke. However, there are currently no effective therapies available for treating or preventing it. The unchecked opening of the transient receptor potential M4 (TRPM4) channel results in an excessive influx of Na + and water, which contributes significantly to the formation of brain edema after ischemic stroke. 9-phenanthrol (9-Phe), a potent TRPM4 inhibitor, has limited clinical applicability due to its potential cytotoxicity and poor solubility. A brain-targeting T7 (HAIYPRH)-modified lipid nanoparticle (LNP) encapsulated 9-Phe (9-Phe@T7-LNP) is designed and synthesized to improve the physicochemical properties and pharmacokinetic properties of 9-Phe for treating brain edema in vivo. These results demonstrated that 9-Phe@T7-LNP can penetrate the intact blood-brain barrier (BBB) in normal mice and target the brain parenchyma. Moreover, 9-Phe@T7-LNP effectively reduced infarct volume and brain edema, prevented neuronal loss and BBB disruption, improved survival, and facilitated neurological function recovery after transient middle cerebral artery occlusion in mice. Additionally, 9-Phe@T7-LNP scavenged oxygen-free radicals and prevented neuronal apoptosis in cultured neurons subjected to oxygen and glucose deprivation/reperfusion. In summary, these findings showed that 9-Phe@T7-LNP holds strong potential as a promising targeted therapy for brain edema after stroke, providing superior pharmacological neuroprotection against brain edema.

CAS / MDL: 6066-82-6
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CHINESE CHEMICAL LETTERS · 2014 · IF 1.178

Determination of synthetic phenolic antioxidants in essence perfume by high performance liquid chromatography with vortex-assisted, cloud-point extraction using AEO-9

Xiao-Lan Li,Dong-Ling Meng,Jiao Zhao,Ya-Ling Yang

This study aimed to establish a rapid analytical method to determine antioxidants in essence. A simple, efficient and practical, vortex-assisted, cloud-point extraction (VACPE) procedure is proposed for extracting and pre-concentrating four different of synthetic phenolic antioxidants (SPAs), propyl gallate (PG), tert -butylhydroquinone (TBHQ), butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT) in essence prior to high performance liquid chromatography (HPLC) analysis. The non-ionic surfactant, fatty alcohol polyoxyethylene ether-9 (AEO-9), was used as extractant and vortex-mixing was utilized to reduce extraction time and improve extraction efficiency. The effective parameters of the extraction process, such as volume of extraction solvent, pH, vortex-mixing time, equilibration temperature and time, were optimized. Under the optimum conditions, the linear range of PG, TBHQ, BHA and BHT was 8.0–800   ng/mL. All correlation coefficients of the calibration curves were higher than 0.996 and relative standard deviations (RSD, n   =   5) were 2.36%–5.46%. The proposed method was successfully applied to the extraction and determination of antioxidants in essence samples with satisfactory relative recoveries of 89.4%–103.5%. The results confirmed the SPAs of essence could be effectively monitored by this method and also established good reference criteria for essence.

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RAPID COMMUNICATIONS IN MASS SPECTROMETRY · 2015 ·Vol. 29 ·期 14 ·1328-1334 · IF 2.253

Direct detection of the anti-cancer drug 9-phenylacridine in tissues by graphite rod laser desorption vacuum-ultraviolet post-ionization mass spectrometry

Ping Liu,Yongjun Hu,Jiaxin Chen,Qing Yang

Rationale Traditionally, drug analysis in biological tissue by mass spectrometry has required complicated sample pre-treatment, which not only wasted time, but also had adverse effects on the results. In order to assist assessment of potential drugs rapidly and accurately, a direct analytical method for drug detection in tissues is needed. The development of such a method is described in this study. Methods An anti-cancer drug, 9-phenylacridine (ACPH), injected into the kidney of mice, was directly analysed from tissues placed on the surface of a graphite rod by near-infrared (1064 nm) laser desorption single photon ionization mass spectrometry (LD/SPI-MS). Results The LD/SPI-MS method was successfully validated by direct analysis of ACPH in kidney sections of mice, without any complicated and time-consuming sample pre-treatment. The sensitivity of detection was down to about 100 fmol per spot and the wide linear dynamic range allowed quantitative detection of ACPH in complex biological samples. A drug-time curve was acquired of ACPH in the kidney of mice after the drug had been injected into the caudal vein. Conclusions It was demonstrated that the anti-tumor drug ACPH could be directly and rapidly detected by LD/SPI-MS in biological tissues without any time-consuming pre-treatment procedure. This method could potentially be applied to the selective localization and analysis of small molecule drugs in tissues and to the study of the pharmacokinetics of new drugs. Copyright © 2015 John Wiley & Sons, Ltd.

CAS / MDL: 602-56-2
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Nanoscale · 2024 · IF 5.8

Synergistic nucleation regulation strategy of 4',4'-Tris(carbazl-9-yl)-triphenylamine and moisture for stably air-processed high performance perovskite photodetectors

Guo He,Dezhi Yang,Sizhe Tao,Liqing Yang,Dechao Guo,Jingbo Zheng,Ji Li,Jiangshan Chen,Dongge Ma

Perovskite photodetectors (PPDs) offer a promising solution with low cost and high responsivity, addressing the limitations of traditional inorganic photodetectors. However, there’s still room for improvement in terms of dark current and stability of air-processed PPDs. In this study, 4',4"-Tris(carbazl-9-yl)-triphenylamine (TCTA) is utilized as nucleation agent to enhance the quality of perovskite film. The synergistic effect of TCTA and moisture promotes rapid nucleation of PbI2-PbCl2, resulting in an increased nucleation rate and the elimination of pinholes in the film. By employing additive engineering, we obtain a PbI2-PbCl2 layer with high coverage, leading to a lower density of traps in the corresponding perovskite film. Consequently, the modified PPD exhibits a remarkable reduction in dark current density by over one order of magnitude, reaching 2.4×10-10 A cm-2 at -10 mV, along with a large linear dynamic range (LDR) of 183 dB. Furthermore, the resulting PPD demonstrates remarkable stability, retaining 90% of the initial external quantum efficiency (EQE) value even after continuous operation for over 3200 hours. Due to a fast response time in nanosecond range, the PPD can convert modulated light signals into electrical signals at a speed of 588 Kbit s-1, highlighting great potential in the field of optical communication.

CAS / MDL: 872-50-4
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NEW JOURNAL OF CHEMISTRY · 2019 ·Vol. 43 ·期 16 ·6380-6387 · IF 3.069

Nitrogen-doped hollow carbon spheres functionalized by 9,10-phenanthrenequinone molecules as a high-performance electrode for asymmetric supercapacitors

Wenbin Wang,Yuying Yang,Xiaotong Wang,Yi Zhou,Xinyuan Zhang,Lulu Qiang,Qian Wang,Zhongai Hu

In this study, uniform nitrogen-doped hollow carbon spheres (NHCSs) have been synthesized using sphere-like SiO2 as a template and polydopamine as a carbon source. It is found that NHCSs have an ultrahigh specific surface area of 870.1 m2 g−1 and high porosity. 9,10-Phenanthrenequinone (PQ) molecules are selected to decorate NHCSs to obtain electrode materials (NHCSs/PQ) for supercapacitors, which show a clear capacitance increase in comparison with pure NHCSs when tested in 1 M H2SO4 aqueous solution. In a three-electrode system, the NHCSs/PQ (mass ratio 4 : 2) electrodes exhibit larger specific capacitance (as high as 252 F g−1 at 1 A g−1) and an ultrahigh rate capability (80.8% capacitance retention at 30 A g−1). Furthermore, the asymmetric supercapacitor is assembled using NHCSs/PQ as a positive electrode material and nitrogen-doped porous carbon (NPCs) that has adsorbed anthraquinone as a negative electrode material, respectively. The device exhibits a high energy density of 8.34 W h kg−1 along with a power density of 600 W kg−1.

研究领域: 材料科学 · 电化学 · 能源存储 · 纳米材料 · 功能材料
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Communications Biology · 2025 ·Vol. 8 ·期 1 ·1-15 · IF 5.1

The crosstalk of monocyte-neutrophil in hair follicles regulates neutrophil transepidermal migration in contact dermatitis

Fan Zhan,Xu Yilun,Lu Yafang,Li Xinlin,Xu Mengli,Liu Jinxin,Cai Zhenzhen,Liu Jiayang,Su Jingping,Wang Jialu,Luo Qingming,Zhang Zhihong,Liu Zheng

The excessive accumulation of neutrophils within the epidermis is a significant hallmark of cutaneous diseases; however, the mechanisms governing neutrophil transepidermal migration (NTEM) remain inadequately understood. In this study, we develop trichromatic-fluorescence-labeled chimeric mice by utilizing Cx3cr1 GFP/+ Lyz2 RFP/+ mice as bone marrow donors and Krt14 YFP/+ mice as recipients. This approach enables us to visualize the process of NTEM and the crosstalk between neutrophils and monocytes in a murine model of irritant contact dermatitis (ICD). Intravital imaging reveals a preferential transmigration of neutrophils through hair follicle (HF), where dermal neutrophils exhibit limited mobility and interact with dermal monocytes. Notably, 18 h following hapten exposure, dermal neutrophils continuously migrate toward HF regions and form clusters within 3 h. Importantly, MMP-9 is identified as essential for the NTEM process; the depletion of dermal monocytes results in a significant reduction of MMP-9 expression in the skin and inhibits the NTEM process in ICD. Mechanistically, dermal monocytes are found to be a crucial source of the cytokines TNF-α and CXCL2, which promote the upregulation of MMP-9 in neutrophils. Therefore, our results highlight HF regions as crucial gateways for dermal monocyte-modulated NTEM and provide visual insights into the crosstalk between neutrophils and monocytes in inflammatory skin disorders.

CAS / MDL: 1405-10-3 1405-20-5
研究领域: 免疫学 · 皮肤病学 · 细胞生物学
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SCIENCE OF THE TOTAL ENVIRONMENT · 2019 · IF 5.589

A novel discovery of a heterogeneous Fenton-like system based on natural siderite: A wide range of pH values from 3 to 9

Fuwei Sun,Haibo Liu,Hanlin Wang,Daobing Shu,Tianhu Chen,Xuehua Zou,Fangju Huang,Dong Chen

Natural iron-bearing minerals have been proven to be effective for activating H 2 O 2 to produce OH, which can be used to degrade organic pollutants . In this study, the performance of siderite to degrade sodium sulfadiazine via catalytic H 2 O 2 degradation was investigated at different solution pH values from 3 to 9. An interesting discovery was made: the performance of the siderite-H 2 O 2 system was excellent under acidic, neutral, and even alkaline conditions. The influence of various factors (e.g. initial concentration, anions, natural organic matters, etc.) on the system under different pH conditions was investigated, which confirmed that siderite exhibited an excellent catalytic performance. By combining EPR characterization with scavenger research, it was proposed that dissolved iron (Fe 2+ ) mainly initiated the homogenous Fenton reaction to degrade pollutants under acidic conditions, while structural Fe 2+ species present in siderite triggered Fenton-like reactions under neutral or even alkaline conditions. From the SEM and XPS characterizations, oxidation and dissolution of Fe 2+ on the surface were also observed, confirming our inference concerning the different reaction mechanisms. The experimental findings show that this siderite-H 2 O 2 system can be used in solutions with pH values from 3 to 9 and that siderite plays a positive role in soil and groundwater remediation when H 2 O 2 is used as an oxidant.

研究领域: 环境科学 · 化学
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Food Bioscience · 2026 · IF 6.2

Screening and functional characterization of purine-degrading Limosilactobacillus fermentum R-9 and its active enhancement effect in the fermentation of Smilax glabra Roxb

Xi Hu,Ruxuan Tan,Xueling Qin,Qingyun He,Zhihua Huang,Lizhong Nong,Junwei Qin,Zhenqiang Wu

Hyperuricemia is associated with dietary purine intake, dysregulated purine metabolism, and impaired uric acid excretion. This study aimed to isolate multifunctional LAB from fermented foods and apply the selected strain to enhance the functional potential of Smilax glabra Roxb. fermentation. Among 79 isolates, 46 were identified as LAB. Limosilactobacillus fermentum R-9 showed efficient degradation of inosine, guanosine, and adenosine, while exhibiting favorable gastrointestinal tolerance and safety-related probiotic properties. Its survival rates after simulated gastric and intestinal digestion were 82.28% and 67.18%, respectively. Genomics revealed genes related to nucleoside hydrolysis, purine/pyrimidine transport, nucleotide salvage, starch utilization, α-glucan metabolism, and β-glucosidase-related glycoside transformation, supporting the dual potential of R-9 for purine metabolism and adaptation to starch-rich S. glabra . L. fermentum R-9 was further used to ferment Smilax glabra Roxb., a starch-rich medicinal and edible plant material containing flavonoid glycosides. After 4 days of fermentation, total phenolics increased from 0.384 to 0.572 mg GAE/mL, and total flavonoids increased from 2.11 to 3.02 mg RE/mL. Xanthine oxidase (XOD) inhibitory activity increased from 16.58% to 70.81%, accompanied by enhanced DPPH and ABTS radical-scavenging activities. Astilbin reached 59.75 μg/mL, increasing by 33.79%. Mechanistically, L. fermentum R-9 fermentation promoted acidification, amylase and β-glucosidase activities, starch matrix disruption, and flavonoid release. These findings highlight L. fermentum R-9 as a promising starter for developing fermented Smilax glabra Roxb. products with enhanced antioxidant and xanthine oxidase inhibitory potential.

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