EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
·
2024
·
IF 4.4
Lixin Liu,Yuning Wang,Jiuyi Sun,Yunan Zhang,Xiangyu Zhang,Lili Wu,Yingli Liu,Xuan Zhang,Yidi Xia,Qiumei Zhang,Ning Gao
To improve the solubility of the fluoroquinolone drug fleroxacin (FL), based on the previous experience of our research group in synthesizing co-crystals/salts of quinolone drugs to improve the physicochemical properties of drugs, Fleroxacin-D-tartaric acid dihydrate salt (FL-D-TT, C 17 H 19 F 3 N 3 O 3 ·C 4 H 5 O 6 ·2(H 2 O)), was synthesized for the first time using fleroxacin and D/L-tartaric acid (D/L-TT). Structural characterization of FL-D-TT was carried out using single-crystal X-ray diffraction, infrared spectral analysis (FT-IR) and powder X-ray diffraction (PXRD). Molecular electrostatic potential analysis showed that D-tartaric acid interacted more readily with FL than L-tartaric acid. The solubility of FL-D-TT (9.71 mg/mL, 1.82 mg/mL) was significantly higher compared to FL (0.39 mg/mL, 0.71 mg/mL) in water and buffer solution at pH 7.4. This may be attributed to the formation of charge-assisted hydrogen bonds (CAHBs) between FL and D-TT that facilitates the dissociation of FL cations in the dissolution medium, leading to an increase in FL solubility. This also led to some improvement in the in vitro antimicrobial activity of FL-D-TT against E. coli , S. typhi , and S. aureus. In addition, the hygroscopic stability of FL has been improved. Surprisingly, FL-D-TT had better photostability than FL, which could be attributed to the introduction of D-TT to make the photosensitizing moiety of FL more stable, which led to the improvement of the photostability of FL.
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Materials
·
2018
·Vol. 11
·期 10
·2063
·
IF 2.467
Xuejing Song,Lingqian Kong,Hongmei Du,Xiangyu Li,Hanlin Feng,Jinsheng Zhao,Yu Xie
Pyrazine derivatives quinoxaline and pyridopyrazine were selected as the acceptors, and benzocarbazole was used as the donor to synthesize four different D–A–D compounds. The results showed that 2,3-bis(decyloxy)pyridine[3,4-b]pyrazine (DPP) exhibited stronger electron-withdrawing ability than that of 2,3-bis(decyloxy)quinoxaline (DPx), because DPP possesses one more nitrogen (N) atom, resulting in a red-shift of the intramolecular charge transfer (ICT) absorption bands and fluorescent emission spectra for compounds with DPP as the acceptor compared with those that use DPx as the acceptor. The band-gap energy (Eg) of the four D–A–D compounds were 2.82 eV, 2.70 eV, 2.48 eV, and 2.62 eV, respectively, for BPC-2DPx, BPC-3DPx, BPC-2DPP, and BPC-3DPP. The solvatochromic effect was insignificant when the four compounds were in the ground state, which became significant in an excited state. With increasing solvent polarity, a 30–43 nm red shift was observed in the emissive spectra of the compounds. The thermal decomposition temperatures of the four compounds between 436 and 453 °C had very high thermal stability. Resistor-type memory devices based on BPC-2DPx and BPC-2DPP were fabricated in a simple sandwich configuration, Al/BPC-2DPx/ITO or Al/BPC-2DPP/ITO. The two devices showed a binary non-volatile flash memory, with lower threshold voltages and better repeatability.Keywords:pyrazine;quinoxaline;benzocarbazole;donor-acceptor-donor;photoelectric properties;electromemory
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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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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2026
·
IF 6.7
Zhihong Zhu,Liqun Shen,Cheng Yu,Yang Li,Bo Zhang,Lingfei Hua,Zhibo Leng,Zijie Li
D-Tagatose is a low-calorie rare sugar with glycemic control and obesity prevention benefits, making it a promising functional sweetener. One-step epimerization of D-fructose to D-tagatose by D-tagatose 4-epimerase (T4E) is an attractive approach, but current T4Es suffer from low activity and poor thermostability. To address this, a novel T4E from the Thermoproteales archaeon (TaDt4e) was identified and engineered. A truncation variant Δ104–123 increased activity by 76.9%, and directed evolution produced the double mutant S46A/I113M with a 153.8% increase over wild-type enzyme. Using 100 g/L D-fructose, whole-cell biotransformation with S46A/I113M achieved 12.1% conversion within 10 min, and the purified enzyme reached 23.8% within 90 min. These results show that coordinated engineering of noncatalytic and active-site regions can substantially improve the catalytic performance of TaDt4e. This study not only identifies TaDt4e as a promising candidate for D-tagatose production, but also provides insights into the semirational or rational engineering of T4Es and related enzymes.
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FITOTERAPIA
·
2026
·
IF 2.9
Hengxing Ran,Yan Wen,Yiebi Qin,Kaiwen Kang,Zhengrong Wu,Yifan Li,Yu Wang,Rihui Wu,Dongli Li,Song Ang,Lishe Gan,Jingwei Jin
This study aims to identify the most primary hepatoprotective compound from Hypericum japonicum and elucidate its underlying mechanisms of liver protection. This study screened 15 compounds from Hypericum japonicum against D-GalN-induced AML12 cell injury, identifying TAX ( Compound 8 , taxifolin 7-rhamnoside) as the most hepatoprotective. This study indicates that TAX reduced AST, ALT, and MDA levels, while enhancing SOD and GSH levels in D-GalN-induced AML12 and LPS/D-GalN -induced liver. In addition, TAX attenuated LPS/D-GalN-induced hepatic injury by lowering inflammatory infiltration and pro-inflammatory cytokines (TNF-α, IL-6 and NO) levels. Network pharmacology analysis revealed common targets between TAX and drug-induced liver injury, forming a protein-protein interaction (PPI) network. Functional enrichment (GO/KEGG) and molecular docking indicated strong binding affinity between TAX and AKT1, confirmed by molecular dynamics simulations. Western blot analyses that TAX ameliorated inflammation and oxidative stress through down-regulating the AKT/NF-κB pathways and up-regulating Nrf2/HO-1 pathways in vivo, TAX inhibited apoptosis via up-regulating Bcl-2 and down-regulating Bax in vitro. Collectively, this study demonstrates that TAX ameliorates LPS/D-GalN-induced ALI by attenuating hepatocyte apoptosis, inflammatory responses, and oxidative stress.
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Food & Function
·
2025
·
IF 5.4
Le Wang,Houzhen Lu,Haitao Gui,Zifu Ni,Zhongke Sun,Zihua Wang,Zhihua Wang,Xuanyan Liu,Qipeng Yuan
Ulcerative colitis (UC) is a prevalent inflammatory bowel disease (IBD) posing a significant health threat. This study explored the protective effects of D-tagatose against DSS-induced colitis in mice and its underlying mechanisms using H&E staining, AB-PAS staining, immunofluorescence, immunohistochemistry, ELISA, qPCR, western blotting, and other assays. D-Tagatose improved colitis by increasing body weight and colon length, with decreased DAI (disease activity index) and histopathological scores. The results showed that D-tagatose inhibited the secretion of myeloperoxidase (MPO), inflammatory enzymes (iNOS and COX-2) and pro-inflammatory cytokines (TNF-α, IL-1β and IL-6) as well as increased the content of anti-inflammatory cytokines (IL-10) in vitro. In addition, D-tagatose enhanced the expression of tight junction proteins (ZO-1 and Occludin) and mucin (MUC-2). Furthermore, D-tagatose was able to modulate the gut microbiota dysbiosis caused by DSS-induced UC and increased the content of short-chain fatty acids (SCFAs). This study indicated that D-tagatose attenuated DSS-induced UC by modulating inflammatory cytokines, restoring intestinal barrier function, maintaining gut microbiota homeostasis, and enhancing SCFA production. These findings provide D-tagatose as a safe and effective novel functional food strategy for the prevention and treatment of UC.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2022
·
IF 5.062
Wan Liu,Meng Cheng,Fangying Yuan,Jiaying He,Yulin Feng,Yi Jin,Jianfang Feng,Shilin Yang,Liangxing Tu
Nanocrystal technology is a common strategy to enhance the oral bioavailability of poorly-soluble drugs, and how to enlarge the enhancing ability on oral absorption via nanocrystals has become a pharmaceutical research field. In this study, we selected andrographolide (ADR), a typical poorly-soluble drug, as the model drug, and employed sodium dodecyl sulfate and D-ɑ-Tocopherol polyethylene glycol 1000 succinate copolymer (SDS-TPGS) to construct novel SDS-TPGS modified andrographolide nanocrystals (S-TANs). We found that the particle sizes of SDS/TPGS physical mixture modified nanocrystals (STANs) were about 553.4 ± 4.1 nm , while that of SDS-TPGS modified nanocrystals (S-TANs) were 604.6 ± 5.7 nm. During the production process of nanocrystals, the crystallinity of ADR was slightly decreased. Nanocrystals enhanced the saturation solubility of ADR, and improved oral absorption, C max and AUC 0-∞ of S-TANs was about 2.10 and 1.24 fold increased, STAN about 2.63, 2.97 fold. In a Real-time distribution study, we found the distribution time of andrographolide, SDS and TPGS in SDS/TPGS physical mixture modified nanocrystals system varies widely, while the distribution times of these materials were similar in SDS-TPGS copolymer modified nanocrystals system. These results indicated that modified with functional stabilizer was an efficient strategy to enlarge the enhancing ability on oral absorption of nanocrystals, and synthesized copolymer containing different functional stabilizers showed higher ability on enhancing oral bioavailability than physical mixtures.
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ANALYTICAL AND BIOANALYTICAL CHEMISTRY
·
2022
·Vol. 414
·期 4
·1651-1662
·
IF 4.478
Zhang Wei,Zhang Yu,Liu Xin,Zhang Yue,Liu Yibing,Wang Wei,Su Rui,Sun Ying,Huang Yibing,Song Daqian,Wu Yanhua,Wang Xinghua
A sensing platform with both ratiometric fluorescence and colorimetric responses towards copper(II) ions (Cu 2+ ) and D-penicillamine (D-pen) was constructed based on carbon dots (CDs). o -Phenylenediamine (OPD) was employed as a chromogenic development reagent for reaction with Cu 2+ to generate the oxidation product 2,3-diaminophenazine (oxOPD), which not only emits green fluorescence at 555 nm, but also quenches the blue fluorescence of CDs at 443 nm via the inner filter effect (IFE) and Förster resonance energy transfer (FRET). Additionally, oxOPD exhibits obvious absorption at 420 nm. Since the intense chelation affinity of D-pen to Cu 2+ greatly inhibits the oxidation of OPD, the intensity ratio of fluorescence at 443 nm to that at 555 nm ( F 443 / F 555 ) and the absorbance at 420 nm ( A 420 ) were conveniently employed as spectral response signals to represent the amount of D-pen introduced into the testing system. This dual-signal sensing platform exhibits excellent selectivity and sensitivity towards both Cu 2+ and D-pen, with low detection limits of 0.019 μM and 0.092 μM, respectively. In addition, the low cytotoxicity of the testing reagents involved in the proposed sensing platform facilitates its application for live cell imaging. Graphical abstract
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Journal of Materials Chemistry B
·
2022
·Vol. 10
·期 18
·3491-3500
·
IF 7.571
Xiao He,Yannv Qu,Xiaohong Lin,Jiapan Sun,Zhiru Jiang,Chaodong Wang,Yuanfei Deng,Fei Yan,Yansun Sun
Self-assembled amino acid derivatives could form well-defined nanostructures which have great application value for drug delivery systems. In particular, D-amino acid derivatives possess tremendous advantages including anti-degradation and good lysosome escape compared with L-amino acid derivatives. In this work, 9-fluorenylmethyloxycarbonyl (Fmoc) neighboring D-arginine derivatives were replaced by dibenzocyclooctyne (DBCO) to extend the class of functional D-arginine derivatives, which were further reacted with various cross-linkers including azide to construct a library of self-assembled supramolecular nanovehicles and strengthen the stability of nanostructures for disease immunotherapy. Moreover, in vitro studies demonstrated that the combination of DBCO modified D-arginine derivative DR3 and cross-linker C1 not only reinforced the cellular uptake efficiency of ovalbumin (OVA) which was chosen as the model antigen, but also promoted the cytokine TNF-α release of RAW 264.7 cells after the introduction of adjuvant unmethylated cytosine-phosphate-guanine dinucleotides (CpG). Furthermore, the nanovaccine based on DR3C1 could enhance the antigen OVA and adjuvant cytosolic delivery of marrow derived dendritic cells (BMDCs), which improved the antigen-presentation cross efficiency and induced the maturation of BMDCs. Taken together, we believe that D-arginine derivatives functionalized by DBCO provide an effective strategy for disease immunotherapy and act as a great potential delivery tool.
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ADVANCES IN POLYMER TECHNOLOGY
·
2018
·Vol. 37
·期 8
·3038-3044
·
IF 2.073
Wensheng Tan,Renjun Fu,Hong Ji,Datong Wu,Yueguo Xu,Yong Kong
Polyaniline (PANI) is chemically synthesized using two low-molecular-weight organic acids (D-tartaric acid and citric acid) as the dopants, respectively. The doped PANI is characterized by field emission scanning electron microscopy, FT-IR spectra, and X-ray diffraction. The two doped PANIs exhibit different electrochemical properties, especially in the supercapacitive behaviors. Compared with citric acid-doped PANI, D-tartaric acid-doped PANI shows higher specific capacitance (525 F/g at 1 A/g) and cyclic stability. The good electrochemical behaviors of D-tartaric acid-doped PANI might be attributed to the two carboxyl groups of D-tartaric acid, which are beneficial to the oriented growth of PANI chains. The results demonstrate that compared with citric acid, D-tartaric acid is a promising dopant for PANI used in supercapacitors.
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NEW JOURNAL OF CHEMISTRY
·
2017
·Vol. 41
·期 24
·15216-15228
·
IF 3.269
Xiaoqing Zeng,Lei Zhang,Jidong Yang,Yuan Guo,Yunmei Huang,Haiyan Yuan,Yongsheng Xie
In this report, water-soluble carbon dots (CDs) with stable fluorescence (FL) were designed and synthesized by using environment-friendly reduced L-glutathione (GSH) as the precursor and ethylenediamine (EDA) as the passivating agent through a one-step hydro-thermal method. The CDs, with bright blue FL, had the quantum yield (QY) of 40% and showed excellent monodispersity and solubility in water. The FL intensity was remarkably enhanced when a racemic modification of L-/D-arginine (Arg) was added into the CDs solution. Therefore, the CDs could be considered as a sensitive probe for the detection of Arg. Under optimized conditions, the CDs exhibited a linear fluorescence response in the range of 3–124 μM (R2 = 0.9987) Arg with the detection limit of 2.85 × 10−8 M. In addition, no evident difference was observed when comparing the FL results of L-Arg and D-Arg. Therefore, this method could not be used in the chiral recognition of two enantiomers. Under optimum conditions, the mechanism and the reasons for the enhancement of FL were investigated. The developed method exhibited great stability, selectivity and accuracy in determining the Arg content in human urine sample and the recovery range was from 97.0% to 102.2%. Thus, our proposed method has potential application in biological molecular recognition.
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JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
·
2024
·
IF 2.8
Wenchan Deng,Chundan Ye,Wei Wang,Rongrong Huang,Cheng Guo,Yuanjiang Pan,Cuirong Sun
Colorectal cancer (CRC) is a common malignant tumor in the gastrointestinal tract. Changes in amino acid metabolites have been implicated in tumorigenesis and disease progression. Biomarkers on the basis of chiral amino acids, especially D-amino acids, have not been established for early diagnosis of CRC. Quantification of chiral amino acids, especially very low concentrations of endogenous D-amino acids, is technically challenging. We report here the quantification of L- and D-amino acids in urine samples collected from 115 CRC patients and 155 healthy volunteers, using an improved method. The method of chiral labeling, liquid chromatography, and tandem mass spectrometry enabled separation and detection of 28 amino acids (14 L-amino acids, 13 D-amino acids and Gly). Orthogonal partial least squares discriminant analysis identified 14 targeted variables among these chiral amino acids that distinguished the CRC from the healthy controls. Binary logistic regression analysis revealed that D-α-aminobutyric acid (D-AABA), L-alanine (L-Ala), D-alanine (D-Ala), D-glutamine (D-Gln) and D-serine (D-Ser) could be potential biomarkers for CRC. A receiver operating characteristic curve analysis of combined multi-variables contributed to an area under the curve (AUC) of 0.995 with 98.3 % sensitivity and 96.8 % specificity. A model constructed with D-AABA, D-Ala, D-Gln, and D-Ser achieved an AUC of 0.988, indicating important contributions of D-amino acids to the association with CRC. Further analysis also demonstrated that the metabolic aberration was associated with age and the development of CRC, D-methionine (D-Met) was decreased in CRC patients with age over 50, and D/L-Gln in patients at stage IV was higher than patients at stage I. This study provides the signature of D-amino acids in urine samples and offers a promising strategy for developing non-invasive diagnosis of CRC.
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