DRUG DELIVERY
·
2017
·
IF 6.402
Hongmei Yan,Jie Song,Xiaobin Jia,Zhenhai Zhang
Baohuoside I is an effective but a poorly soluble antitumor drug. In this study, we prepared baohuoside I-loaded mixed micelles with didecyldimethylammonium bromide (DDAB) and d-a-tocopheryl polyethylene glycol succinate (TPGS) (DTBM) and active targeting mixed micelles (HDTBM) with hyaluronic acid (HA) as the targeting ligand on the surface of the mixed micelles. We performed a systematic comparative evaluation of the antiproliferative effect, cellular uptake, antitumor efficacy, and in vivo tumor targeting of these micelles using A549 cells. HDTBM showed improved cellular uptake and had a greater hypersensitizing effect on A549 cell lines than baohuoside I; half-maximal inhibitory concentration (IC50) was 8.86 versus 20.42 μg/mL, respectively. Results of the antitumor efficacy study and the imaging study for in vivo targeting showed that the mixed-micelle formulation had higher antitumor efficacy and achieved effective and targeted drug delivery. Therefore, our results indicate that HA/baohuoside I-M may be used as a potential antitumor formulation.
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NEW JOURNAL OF CHEMISTRY
·
2025
·
IF 2.5
Tiantian Wang,Jianhong Wei,Furong Shi,Hejie Wang,Jinye He,Xudong Lv,Yuan Zhou,Pengzhi Guo,Chenglong Wang,Yangjun Xia
In recent years, polymerized small molecule acceptors (PSMAs) have emerged as a promising strategy that combines the strong absorption of small molecules with the film-forming ability and stability of polymers, thereby greatly boosting the performance of all-polymer solar cells (all-PSCs). We designed a non-fused acceptor, DTBT-IC, and its polymeric counterpart, PDTBT-Br-T, by selecting DTBT as the core, bithiophene as the π-bridge, and IC as the terminal group. PDTBT-Br-T was synthesized via Stille coupling and used with PM6 as the donor to fabricate organic solar cells. The PDTBT-Br-T-based device delivered superior performance, with a VOC of 1.050 V, JSC of 9.32 mA cm−2, FF of 45.33%, and a PCE of 4.44%, outperforming the DTBT-IC-based counterpart. Morphological and structural analyses revealed that PDTBT-Br-T exhibits more ordered backbone stacking and defined phase separation, enhancing exciton dissociation and charge transport, and suppressing energy loss. The study highlights that polymerization of DTBT-IC enhances intermolecular packing and microstructure, offering critical design insights for efficient all-PSCs.
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ANALYTICAL CHEMISTRY
·
2025
·
IF 6.7
Daoqing Fan,Shuai Qin,Chuanping Li,Yujia Ren,Lilin Hao,Hengqian Zhang,Jiawen Han,Jingyu Hou,Juan Wang,Shaojun Dong
Rational design of high-performance nanozymes with multiple enzyme-mimicking activities for biochemical sensing is one of the most promising directions in this area. D-PA is a kind of S-containing pharmaceutical for treating various diseases; the side effects caused by its unreasonable intake/residual have posed severe threats to human health and the living environment, making its accurate analysis gradually significant. However, most previous works exhibited the drawbacks of complicated synthesis of nanomaterials, unreliable single-modal results, and limited portable sensing ability. Herein, we prepared a low-cost MoCu-2MI MOF nanozyme via a simple hydrothermal method and revealed its excellent peroxidase/laccase dual-enzyme-mimicking properties that might benefit from a bimetallic valence modulation strategy via multifaceted experiments (EIS, EPR, ROS probes, and Michaelis-kinetic tests). Initially, MoCu-2MI MOF worked as a POD mimic and catalyzed the oxidation of TMB into blue-colored Ox-TMB. By synergistically harnessing the visual/photothermal effect of Ox-TMB and the effective reduction and ROS-scavenging abilities of D-PA, we constructed the first colorimetric-RGB-photothermal trimodal D-PA sensor with the assistance of portable devices, bringing evidently strengthened cost-effectiveness, reliability, and portable sensing ability. The LODs for D-PA under the three modes were 0.24, 7.88, and 7.98 μM, which could compete with most previous works. Moreover, the trimodal sensor presented satisfactory applicability in human serum and milk samples. More surprisingly, taking 2,4-DP as the model target (LOD = 0.11 μM), we further achieved the visual analysis of phenolic pollutants based on the excellent LAC-like activity of MoCu-2MI MOF. This work not only offered an effective approach for the exploration and controllable modulation of nanozymes with multiple enzyme-like properties but also opened up unique horizons for the design of multimodal portable biosensors.
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FOOD CHEMISTRY
·
2023
·
IF 8.8
Wei Jia,Xin Wang
The potential mechanisms about the health risks of endogenous 3-MCPD remain elusive. Here, we researched the influences of 3-MCPD on the metabolic landscape of digested goat infant formulas via integrative UHPLC-Q-Orbitrap HRMS-MS/MS-based peptidomics and metabolomics (%RSDs ≤ 7.35 %, LOQ 2.99–58.77 μg kg −1 ). Digested goat infant formulas under 3-MCPD-interference caused metabolic perturbation by down-regulating levels of peptides VGINYWLAHK (5.98–0.72 mg kg −1 ) and HLMCLSWQ (3.25–0.72 mg kg −1 ) pertained to health-promoting bioactive components, and accelerated the down-regulation of non-essential amino acids (AAs, l -tyrosine 0.88–0.39 mg kg −1 , glutamic acid 8.83–0.88 μg kg −1 , and d -aspartic acid 2.93–0.43 μg kg −1 ), semi-essential AA ( l -arginine 13.06–8.12 μg kg −1 ) and essential AAs ( l -phenylalanine 0.49–0.05 mg kg −1 ) that provide nutritional value. Peptidomics and metabolomics interactions elucidated that 3-MCPD altered the stability of α-lactalbumin and d -aspartate oxidase in a dose-dependent manner, and affected the flavor perception of goat infant formulas, leading to a decline of nutritional value of goat infant formulas.
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Food & Function
·
2019
·Vol. 10
·期 9
·6009-6019
·
IF 3.241
Yun Yu,Xiu-Yuan Lang,Xi-Xi Li,Run-Ze Gu,Qing-Shan Liu,Rongfeng Lan,Xiao-Yan Qin
The major bioactive ingredient THSG of Polygonum multiflorum is well established for its anti-oxidation, anti-aging and anti-inflammation properties. Increasing evidence supports the capacity of THSG to ameliorate the biochemistry of neurotrophins and their downstream signaling axis in mouse models to attenuate neurodegenerative diseases such as Alzheimer's and Parkinson's disease. In this study, the neuroprotective effects of THSG were studied in vitro and in vivo. In cultured mesencephalic dopamine neurons and SH-SY5Y cell line, it was found that THSG protected the integrity of the cell body and neurite branching from MPP+-induced toxicity by restoring the expression of FGF2 and BDNF and their downstream signaling pathways to inhibit apoptosis and promote cell survival. The inhibition of Akt signaling by LY294002 or TrkB activity by K252a eliminated the neuroprotective effects of THSG. In the MPTP-induced mouse models of Parkinson's disease, THSG ameliorated the animal behaviors against MPTP-induced neurotoxicity, which was demonstrated by the pole test and the tail suspension test. Biochemical and immunohistochemical analysis verified the THSG-mediated restoration of the FGF2-Akt and BDNF-TrkB signaling axis in the substantia nigra and corpus striatum and the recovery of dopaminergic neurons. These results establish the neuroprotective effects of THSG in vitro and in vivo and unravel the underlying mechanism against toxin-induced neural atrophy, providing a new avenue for the use and pharmacological research of edible medicine for anti-neurodegenerative diseases.
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Nano Research
·
2014
·Vol. 8
·期 3
·920-930
·
IF 6.963
Zhang Juan,Liu Ying,Lv Jun,Li Genxi
A colorimetric method has been established for α-glucosidase activity assay and its inhibitor screening. The method is based on the specific recognition between 1,4-phenylenediboronic acid (PDBA) and 4-aminophenyl-α- d -glucopyranoside (pAPG), which may induce aggregation of pAPG-functionalized gold nanoparticles (AuNPs) to achieve color change of the test solution. Because pAPG is the substrate of α-glucosidase, the aggregation of AuNPs will be influenced by α-glucosidase since there is no coordination reactivity between PDBA and 4-aminobenzene, the hydrolyzed product of pAPG catalyzed by the enzyme. Therefore, a simple and easily-operated colorimetric method for the assay of α-glucosidase activity can be developed. Under the optimized experimental conditions, the ratios of absorbance at a wavelength of 650 nm to that at 520 nm vary linearly with the α-glucosidase activity within a range from 0.05 to 1.1 U/mL with a lowest detection limit of 0.004 U/mL. Moreover, using the proposed method, the inhibition effect of gallic acid and quercetin on α-glucosidase activity can be tested with IC 50 values of 1.16 mM and 1.82 μM, respectively. Thus, the method has a great potential not only for the detection of α-glucosidase activity, but also for the screening of its inhibitors.
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Food Analytical Methods
·
2016
·Vol. 10
·期 3
·713-726
·
IF 2.167
Feng Yunzi,Su Guowan,Sun-Waterhouse Dongxiao,Cai Yu,Zhao Haifeng,Cui Chun,Zhao Mouming
The aim of this study was to develop an effective analytical procedure to analyse the aroma-active compounds of soy sauce using headspace solid-phase micro-extraction (HS-SPME) coupled to gas chromatography-mass spectrometry/olfactometry (GC-MS/O). Optimization of SPME focusing on type of fibre, exposure time, extraction temperature and ionic strength was supported by gas chromatography-mass spectrometry (GC-MS). The optimized HS-SPME conditions were as follows: carboxen/polydimethylsiloxane (CAR/PDMS) fibre, NaCl concentration of 270 g/L, extraction temperature of 45 °C and 30-min exposure time. Under these conditions, 25 aroma-active compounds were detected in soy sauce by HS-SPME-GC-O. 2-Methylbutanal (malty), 3-(methylthio)propanal (cooked potato-like), dimethyl trisufide (sulfury, cooked onion), 2-methoxyphenol (smoky) and 2-phenylethanol (flowery) were the most intense. The overall odour impression of the CAR/PDMS-fibre-derived SPME extract detected via human sniffing resembled that of original soy sauce. The intensity of aromas detected by D-GC-O correlated well with the total peak area of GC-MS analysis. Thus, SPME coupled with D-GC-O offers an automated facile method to allow in situ optimization of SPME performance and ultimately effective analysis of aromas.
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INTERNATIONAL JOURNAL OF ONCOLOGY
·
2023
·Vol. 62
·期 5
·1-21
·
IF 5.2
Ting Xue,Yaodong Chen,Jia Xu,Weiqin Du,Pengzhou Kong,Xinri Zhang
Lung cancer is the leading cause of cancer‑related mortality worldwide. Non‑small cell lung cancer (NSCLC) is the most common pathological subtype of lung cancer and is associated with low 5‑year overall survival rates. Therefore, novel and effective chemotherapeutic drugs are urgently required for improving the survival outcomes of patients with lung cancer. Cyclovirobuxine D (CVB‑D) is a natural steroidal alkaloid, used for the treatment of cardiovascular diseases in Traditional Chinese Medicine. Several studies have also demonstrated the antitumor effects of CVB‑D. Therefore, in the present study, the therapeutic effects of CVB‑D in lung cancer and the underlying mechanisms were investigated using the in vivo xenograft model of NSCLC in nude mice and in vitro experiments with the NSCLC cell lines. Bioinformatics analyses of RNA‑sequencing data, and cell‑based functional assays demonstrated that CVB‑D treatment significantly inhibited in vitro and in vivo NSCLC cell proliferation, survival, invasion, migration, angiogenesis, epithelial‑to‑mesenchymal transition and G2/M phase cell cycle. CVB‑D exerted its antitumor effects by inhibiting the KIF11‑CDK1‑CDC25C‑cyclinB1 G2/M phase transition regulatory oncogenic network and the NF‑κB/JNK signaling pathway. CVB‑D treatment significantly reduced the sizes and weights and malignancy of xenograft NSCLC tumors in the nude mice. In conclusion, the present study demonstrated that CVB‑D inhibited the growth and progression of NSCLC cells by inhibiting the KIF11‑CDK1‑CDC25C‑CyclinB1 G2/M phase transition regulatory network and the NF‑κB/JNK signaling pathway. Therefore, CVB‑D is a promising drug for the treatment of NSCLC patients.
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INDUSTRIAL CROPS AND PRODUCTS
·
2020
·
IF 4.244
Yong Guo,Zhiyan Liu,Enhua Hou,Nannan Ma,Jiangping Fan,Cheng-Yun Jin,Ruige Yang
(+)-Nootkatone, a non-food bioactive natural bicyclic sesquiterpene ketone, is isolated from Chamaecyparis nootkatensis [D. Don] Spach as a renewable forest resource. In continuation of our effort to develop synthetic natural derived insecticides from non-food bioactive products, a small library of thirty N -(1,3- thiazol-2-yl)carboxamides fused (+)-nootkatone was prepared by molecular hybridization and characterized by 1 H/ 13 C NMR, HR-MS, and IR spectroscopy. Their insecticidal activities against Mythimna separata Walker and Plutella xylostella Linnaeus were evaluated. Compounds B6 , B7 , B9 , B19 – 21 and B24 showed better insecticidal activity against M. separata than the botanical insecticide azadirachtin , and their LC 50 values ranged from 0.55−0.68 mg/mL. Particularly, compound B9 exhibited 1.87-fold more pronounced insecticidal activity against M. separata than azadirachtin. The insecticidal activity of B21 against P. xylostella was 1.37-fold of that of azadirachtin. Through acetylcholinesterase (AChE) inhibitory activity and molecular docking studies, AChE may be the insecticidal target of B9 against M. separata . In addition, three pronounced compounds B9 , B21 and B24 exhibited low hemolytic and cytotoxic activities on normal mammalian cells. These findings will give insights into the further development of (+)-nootkatone derivatives as potentially synthetic natural derived insecticides for pest management.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2024
·
IF 5.7
Tong Zhou,Meigui Huang,Heping Cui,Shahzad Hussain,Khizar Hayat,Xiaoming Zhang,Chi-Tang Ho
The formation pathway and mechanism of various pyrazines were investigated during the thermal treatment of the alanine-xylose Amadori compound (Ala-ARP) and exogenous alanine (Ala). 15N-labeled Ala was used to coheated with Ala-ARP to clarify the nitrogen sources and the respective contributions of exogenous Ala and the regenerated Ala released from Ala-ARP to different pyrazine formation. It was found that exogenous Ala exhibited a priority in capturing glyoxal (GO) to form pyrazine during the thermal degradation of ARP. Compared to the Ala-methylglyoxal (MGO) model, a lower activation energy was required for the Ala-GO reaction, where the reaction dynamics of Ala-GO followed a zero-order model. In addition to forming pyrazine, the interaction between existing exogenous Ala and GO would accelerate the thermal degradation of Ala-ARP and retro-aldolization reaction of deoxyxylosones (DXs) to α-dicarbonyls. During this process, the release of regenerated Ala and MGO was promoted. Accordingly, as GO was expended by exogenous Ala during the initial stage of ARP-Ala degradation, the condensation between regenerated Ala and MGO became intensified, leading to the generation of methylpyrazine and 2,5-dimethylpyrazine. As a result, in the thermally treated mixture of Ala-ARP and exogenous Ala, 55% of the formed pyrazine originated from exogenous Ala, while 63% of the formed methylpyrazine and 57% of the formed 2,5-dimethylpyrazine were derived from regenerated Ala (120 °C, 30 min).
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JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
·
2017
·
IF 1.9
Li Xu,Caifeng Wan,Jing Du,Hongli Li,Xuesong Liu,Hong Yang,Fenghua Li
Breast cancer is the leading cause of cancer-related deaths in women and earlier detection can substantially reduce deaths from breast cancer. Polymers with targeted ligands are widely used in the field of molecular ultrasound imaging and targeted tumor therapy. In our study, the nanotheranostic agent was fabricated through filling perfluoropropane (C3F8) into poly(d,l-lactic-co-glycolic acid) nanoparticles (PLGA NPs), followed by the formation of gold nanoshell on the surface, then conjugated with anti p53 antibody which has high specificity with the p53 protein overexpressing in breast cancer. The average diameter of the gold nanoshelled PLGA NPs carrying anti p53 antibody (p53-PLGA@Au NPs) was 247 ± 108.2 nm. The p53-PLGA@Au NPs had well-defined spherical morphology and hollow interiors observed by electron microscope, and had a good photothermal effect under the irradiation of an 808 nm laser. The results of laser scanning confocal microscope (LSCM) and flow cytometer (FCM) indicated the specific targeting of p53-PLGA@Au NPs conjugating with breast cancer MCF-7 cells overexpressing p53 protein in vitro. Also the ultrasound imaging experiments in vitro showed that p53-PLGA@Au NPs were suitable for ultrasound contrast imaging. In conclusion, the p53-PLGA@Au NPs are demonstrated to be novel targeted UCAs and may have potential applications in the early diagnosis and targeted near-infrared (NIR) photothermal therapy of breast cancer in the future.
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FUNCTIONAL & INTEGRATIVE GENOMICS
·
2014
·Vol. 14
·期 3
·603-615
·
IF 2.691
Shi Min,Luo Xiuqin,Ju Guanhua,Yu Xiaohong,Hao Xiaolong,Huang Qiang,Xiao Jianbo,Cui Lijie,Kai Guoyin
Tanshinone is widely used for treatment of cardio-cerebrovascular diseases with increasing demand. Herein, key enzyme genes SmHMGR (3-hydroxy-3-methylglutaryl CoA reductase) and SmDXR (1-deoxy- d -xylulose 5-phosphate reductoisomerase) involved in the tanshinone biosynthetic pathway were introduced into Salvia miltiorrhiza ( Sm ) hairy roots to enhance tanshinone production. Over-expression of SmHMGR or SmDXR in hairy root lines can significantly enhance the yield of tanshinone. Transgenic hairy root lines co-expressing HMGR and DXR (HD lines) produced evidently higher levels of total tanshinone (TT) compared with the control and single gene transformed lines. The highest tanshinone production was observed in HD42 with the concentration of 3.25 mg g −1 DW. Furthermore, the transgenic hairy roots showed higher antioxidant activity than control. In addition, transgenic hairy root harboring HMGR and DXR (HD42) exhibited higher tanshinone content after elicitation by yeast extract and/or Ag + than before. Tanshinone can be significantly enhanced to 5.858, 6.716, and 4.426 mg g −1 DW by YE, Ag + , and YE-Ag + treatment compared with non-induced HD42, respectively. The content of cryptotanshinone and dihydrotanshinone was effectively elevated upon elicitor treatments, whereas there was no obvious promotion effect for the other two compounds tanshinone I and tanshinone IIA. Our results provide a useful strategy to improve tanshinone content as well as other natural active products by combination of genetic engineering with elicitors.
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