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JOURNAL OF BIOMATERIALS APPLICATIONS · 2023 · IF 2.9

Co-Delivery of paclitaxel and doxorubicin in folate-Targeted pluronic/ploy (D,L-lactide-b-glycolide) polymersomes

Tian Yi Wu,Wen Jie Cao,Zi Ling Li,Yan Chun Gong,Xiang Yuan Xiong

Drugs with different solubility can be selectively embedded into polymersomes with the hydrophilic core and hydrophobic bilayer. Novel folate-targeted Pluronic/poly (D,L-lactide-b-glycolide) polymersomes were constructed and used for the co-delivery of paclitaxel (PTX) and doxorubicin (DOX) to improve their inhibitory effect over cancer cells. The particle size of blank polymersomes was mainly distributed below 125 nm. The release of PTX and DOX from polymersomes showed an initial burst release followed by a sustained and slow release. The in vitro cytotoxicity data showed that the targeted co-loaded polymersomes (PTX&DOX FA-Ps) exhibited better inhibitory effect than single-loaded polymersomes and free drugs did. Furthermore, PTX&DOX FA-Ps showed the synergistic therapeutic effect over OVCAR-3 cancer cells. The cellular uptake results also showed that folate modified polymersomes had excellent targeting performance. Therefore, the folate-targeted Pluronic/poly (D,L-lactide-b-glycolide) polymersomes have potential application value as novel drug carriers to co-deliver PTX and DOX.

✓ 已验证 DOI PubMed 高影响因子
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Journal of Ovarian Research · 2025 ·Vol. 19 ·期 1 ·8 · IF 4.2

Oviductus Ranae alleviates D-galactose-induced ovarian aging by inhibiting ferroptosis and regulating the GPX4/ACSL4 pathway

Ling Xiaomei,Xie Cong,Li Ming,Li Jie,Liu Shun,Sun Liyue,Zeng Xinxin,Zhang Zhen,Zhang Xuhui,Liang Lei

Background Ovarian dysfunction caused by aging restricts female reproductive capacity and causes age-related health problems. Ferroptosis is an important mode of cell death during accelerated aging. Oviductus Ranae (OR), a traditional Chinese medicine, has been used to treat ovarian age-related diseases in women. However, the mechanisms through which OR mitigates ovarian aging, especially ferroptosis regulation, remain unclear. This study investigated the pharmacological effects and mechanisms of OR for ovarian aging in rats. Methods Sprague–Dawley female rats were divided into six groups: aging group induced with D-galactose; experiment groups treated with OR at low, middle, and high concentrations; positive control treated with estradiol valerate; and control group with no treatment. After 42 d, ovarian tissue and serum were collected for biochemical determination, hematoxylin and eosin staining, immunohistochemistry, enzyme-linked immunosorbent assay, reverse transcription-quantitative polymerase chain reaction, western blotting, and RNA sequencing analysis. To elucidate the mechanism underlying the effects of OR on ferroptosis in ovarian granulosa cells (OGCs), in vitro experiments were conducted. Results Treatment with OR improved ovarian follicular development and serum hormone levels, reduced iron deposition, enhanced cell proliferation, and inhibited apoptosis in D-galactose-induced ovarian aging rats. Ferroptosis was alleviated in the ovaries and serum by elevated glutathione and decreased lipid peroxidation production. RNA-seq showed that OR induced changes in 2,768 genes that were involved in ovarian steroidogenesis, glutathione metabolism, lipid metabolism, and ferroptosis pathways. Notably, OR downregulated ACSL4, LPCAT3, and ALOX12 mRNA and protein expressions, while upregulating FTH1, FTL, SLC7A11, GSS, and GPX4, which serve as critical regulators in ferroptosis. OGCs pretreated with OR-containing serum before erastin exposure exhibited enhanced viability, reduced ferrous iron, total iron, and lipid peroxidation levels, improved antioxidant activity, and stabilized mitochondrial function, indicating effective ferroptosis inhibition. Furthermore, OR-containing serum pretreatment inhibited ferroptosis in OGCs by regulating the GPX4/ACSL4 axis. Conclusions OR resists ovarian damage and prevents aging through antiferroptosis mechanisms by regulating the GPX4/ACSL4 axis in OGCs and aging rats. These results highlight the potential of OR as a therapeutic agent for the prevention and treatment of ovarian aging.

CAS / MDL: 59-23-4
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JOURNAL OF MEDICINAL CHEMISTRY · 2025 · IF 6.8

Optimization of Ascidian-Derived Herdmanine D: Targeting Gouty Arthritis via the PPAR-γ/NF-κB/NLRP3 Pathway

Xinlin Zhu,Yi Dong,Ya Zhang,Chenghai Gao,Lijian Ding,Yonghong Liu,Zhiran Ju

Gouty arthritis, driven by monosodium urate (MSU) crystal deposition and dysregulated inflammation, remains a therapeutic challenge due to the limitations of current treatments. Here, we investigate Herdmanine D (HDD), a marine-derived alkaloid from the ascidian Herdmania momus. It was optimized via structure–activity relationship (SAR) studies and computational modeling to enhance its binding to peroxisome proliferator-activated receptor γ (PPAR-γ), which regulates the PPAR-γ/NF-κB signaling pathway in gout pathogenesis. The optimized HDD derivative 9a demonstrated potent PPAR-γ binding affinity and pharmacokinetic properties, effectively suppressing NF-κB-driven pro-inflammatory cytokines in vitro. In murine MSU-induced gouty arthritis models, 9a alleviated synovial inflammation and tissue damage. Mechanistically, 9a activated PPAR-γ to inhibit NF-κB and attenuate NLRP3 inflammasome assembly. This work highlights HDD as a unique marine scaffold for next-generation antigout therapeutics, merging marine natural product safety with rational design to address unmet clinical needs.

✓ 已验证 DOI PubMed 高影响因子
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Journal of Materials Chemistry C · 2024 ·Vol. 12 ·期 39 ·15903-15914 · IF 5.7

Chiral self-assembled (β,D)-RIB-TPE micron vesicles with AIE characteristics used as targeting-drug carriers

Mengyuan Niu,Yuliang Yang,Yue Sun,Yu Hu,Kaiyue Song,Xiaoxia Sun

A novel chiral fluorescent probe, tetraphenylvinyltriazole-ribosyl ribose derivative (β,D)-RIB-TPE, was prepared by Click reaction. It can self-assemble into amphiphilic micron vesicles in methanol solution. (β,D)-RIB-TPE has good AIE properties with a large Stokes shift (redshift 61.8 nm), self-assembles into J-aggregates in a mixed solution with 98% water content, and exhibits a relative fluorescence intensity αAIE = 24, emitting bright blue fluorescence. In addition to the micron vesicles, (β,D)-RIB-TPE self-assembled into J-aggregates in different mixtures, showing different morphologies, such as a cross-linked network structure and an irregular bulk stacking structure. The fluorescent probe (β,D)-RIB-TPE could achieve high efficiency and rapid multi-channel detection of clopidogrel S-(+)-sulfate by fluorescence chromatography and CD spectroscopy. Infrared, nuclear magnetic titration, scanning electron microscopy and DFT calculations confirmed that the probe (β,D)-RIB-TPE recognized S-(+)-clopidogrel sulfate by an ICT mechanism. (β,D)-RIB-TPE and S-(+)-clopidogrel sulfate were co-assembled in methanol to form single-target drug-carrying micron vesicles with a smaller particle size than the self-assembled (β,D)-RIB-TPE vesicles and good drug embedding capacity.

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JOURNAL OF MOLECULAR STRUCTURE · 2024 · IF 4

Discovery of novel thiophene [2,3-D] pyrimidine–thiazole derivative as promising MNK inhibitor to treat breast cancer

Peng Zhu,You Yang,Jianqiang Qian,Jun Han,Dairui Kong,Bo Sun,Jian Zhang,Jingtao Wei,Qulian Guo,Sihui Nian,Lixiang Zhou,Guodong Wang,Shaohua Hou

Mitogen-activated protein kinase–interacting kinases (MNKs) play a key role in the occurrence and migration of tumors and have become promising targets for tumor therapy. Nevertheless, the development progress on the MNKs inhibitors against cancer was relatively slow. In this study, compound 4s (MNK1/2 half-maximal inhibitory concentration [IC 50 ] = 987/1048 nM), a promising MNKs inhibitor was discovered based on virtual screening. After the structural optimization of compound 4s , 18 novel thiophene [2,3-D] pyrimidine–thiazole derivatives were designed and prepared, and their inhibitory effect on MNKs was determined. Among which, compound 5l exhibited the best inhibitory activity on MNKs (MNK1/2 IC 50 = 23/62 nM) and relatively high selectivity among 125 kinases. Results from in vitro experiments indicated that compound 5l could significantly inhibit the in vitro proliferation (IC 50 = 0.8 ± 0.1 μM) and migration of breast cancer cells, which demonstrated that compound 5l is a promising MNK inhibitor to treat breast cancer and need further study.

✓ 已验证 DOI 高影响因子
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FOOD CHEMISTRY · 2018 · IF 4.946

Synthesis and antibacterial activity of C2 or C5 modified and D ring rejiggered canthin-6-one analogues

Jiangkun Dai,Wenjia Dan,Nian Li,Ruixue Wang,Yao Zhang,Nannan Li,Ruizhi Wang,Junru Wang

Thirty-one canthin-6-one analogues, mainly including C 2 or C 5 or D ring modified canthin-6-ones, were designed and synthesized in order to study their antibacterial activity and structure-activity relationships. The analogue 28 with the highest bioactivity had a peak minimum inhibitory concentration of 4 μg/ml and showed low cytotoxicity against L02 cells and good “drug-like” properties. The antibacterial effect of 28 was characterized further by scanning electron microscopy, cytoplasmic β -galactosidase leakage assay, molecular docking evaluation, UV–visible analysis and isothermal titration calorimetry (ITC) measurement. The results showed that 28 may exert its bactericidal effect by damaging bacterial cell membranes and disrupting the function of DNA topoisomerases, both of which could lead to rapid cell death.

✓ 已验证 DOI 高影响因子
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APPLIED ENERGY · 2020 · IF 8.848

D-mannitol@silica/graphene oxide nanoencapsulated phase change material with high phase change properties and thermal reliability

Lijuan He,Songping Mo,Pengcheng Lin,Lisi Jia,Ying Chen,Zhengdong Cheng

Sugar alcohols have considerable potential for usage in medium-temperature thermal energy storage applications; however, they suffer from poor thermal reliability and low thermal conductivity . Nanoencapsulation is an effective approach to improve the thermal energy storage performance of the phase-change materials. Until now, nanoencapsulation of sugar alcohols with a high phase-change performance has been rarely reported. The objective of this study is to develop a method for the nanoencapsulation of sugar alcohols with an enhanced phase-change performance. D-mannitol nanocapsules with a silica–graphene oxide composite shell were synthesized and investigated to demonstrate the validity of this novel method. The morphology, size distribution, and core–shell microstructure of the nanocapsules were observed using a scanning electron microscope, particle size and zeta potential analyzer, and transmission electron microscope. In addition, the phase-change performance of the nanocapsules was studied using a differential scanning calorimeter, a thermogravimetric analyzer, and weight loss and appearance investigation. The results demonstrate that the melting and solidifying latent heat of the nanocapsules are 216.7 and 174.4 kJ/kg, respectively. The energy storage efficiency of the nanocapsules was 75.8% and its 96.1% was maintained after repeated thermal cycling. Compared with pure D-mannitol, the thermal conductivity of the nanocapsules was observed to increase by up to 128.6%. The novel nanocapsules exhibited good medium-temperature thermal energy storage prospects.

✓ 已验证 DOI 高影响因子
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RSC Advances · 2015 ·Vol. 5 ·期 86 ·70139-70146 · IF 3.84

Catalytic dehydration of D-xylose to furfural over a tantalum-based catalyst in batch and continuous process

Xing-Long Li,Tao Pan,Jin Deng,Yao Fu,Hua-Jian Xu

Furfural is a biomass-based bulk chemical and its derivatives have potential applications as renewable fuels and chemicals. A water-tolerant and stable solid acid catalyst modified hydrated tantalum oxide (TA-p) was developed for catalytic conversion of D-xylose to furfural in water–organic solvent biphasic system. This process was performed both in a batch reactor and a continuous fixed-bed reactor. In the batch process, D-xylose conversion and furfural yield were significantly affected by the organic solvent, reaction temperature and reaction time. 1-Butanol, which could be obtained through the fermentation of biomass-based carbohydrates, was selected as organic phase and the highest furfural yield of 59% was achieved with D-xylose conversion of 96% at 180 °C in the continuous process. Moreover, the long-time stability test for 80 h under the optimal conditions showed the excellent stability of TA-p catalyst.

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ORGANOMETALLICS · 2020 · IF 3.804

Bimetallic Bis-NHC-Ir(III) Complex Bearing 2-Arylbenzo[d]oxazolyl Ligand: Synthesis, Catalysis, and Bimetallic Effects

Shuang Huang,Xi Hong,He-Zhen Cui,Bing Zhan,Zhi-Ming Li,Xiu-Feng Hou

Herein, an unprecedented bimetallic bis-NHC Cp*Ir complex 1 bearing 2-arylbenzo[d]oxazolyl and NHC ligands is reported. A significant increase in activity was observed for N-methylation of amines and reduction of aldehydes with MeOH catalyzed by 1 compared to the monometallic analogues (2–11). Under the optimal conditions, it showed to be highly effective in N-methylation of nitroarenes with MeOH as both C1 and H2 source. Substrates, including aromatic amines, ketones, and nitro compounds with various functional groups, can be well-tolerated. Mechanistic studies and DFT calculation highlight the significance of bimetallic centers cooperativity.

✓ 已验证 DOI 高影响因子
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JOURNAL OF POWER SOURCES · 2022 · IF 9.794

Modulating the d-p orbital coupling of manganese chalcogenides for efficient polysulfides conversion in lithium–sulfur batteries

Guo Liu,Qi Zeng,Xinyi Sui,Shuhao Tian,Xijuan Li,Qingfeng Wu,Xukun Wang,Kun Tao,Erqing Xie,Zhenxing Zhang

The commercialization of lithium-sulfur battery (LSB) is seriously limited by the shuttling effect and sluggish reaction kinetics. Metal chalcogenides have been widely used as catalysts to enhance electrochemical performance, but the modulation essence of these non-metal anions is unclear. Herein, cubic manganese chalcogenides (MnO, MnS, MnSe) with fixed cation (Mn) and various anions (O, S, Se) are synthesized, and the anion effect on the performance of LSBs is systematically investigated. Based on the complementary experimental characterization and advanced theoretical calculations, it is clear that the interfacial redox reaction dynamics are governed by the catalytic activity of manganese chalcogenides, while the catalytic activity is modulated by the gap between the d-band of cation and p-band of anion (Δd-p). Among these manganese chalcogenides, Se has the largest atom radius and lowest electronegativity , which makes the p-band center of Se move to the Fermi level , thus increasing the electron's energy to react. Consequently, the LSBs based on MnSe catalyst exhibit the best rate (613.5 mAh g −1 at 4C) and cyclic performance (847.5 mAh g −1 after 250 cycles at 0.2C). This comparative study may encourage more effort and provide a new paradigm for developing highly effective catalysts for high-performance LSBs.

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RSC Advances · 2022 ·Vol. 12 ·期 19 ·11967-11973 · IF 4.036

Chiral fluorescent sensor based on H8-BINOL for the high enantioselective recognition of D- and L-phenylalanine

Yafeng Zhang,Huizhen Wang,Hu Yu,Xiaoxia Sun

Phenylalanine an essential aromatic amino acid for humans and animals, cannot be synthesized by humans and animals on their own. However, it synthesizes important neurotransmitters and hormones in the body and is involved in gluconeogenesis and lipid metabolism. Moreover, the two opposite configurations of phenylalanine have different activities. For example, L-phenylalanine is a biologically active optical isomer involved in crucial biological processes, the lack of which will lead to intellectual disability, while D-phenylalanine only acts as a chiral intermediate. In this research, an H8-BINOL chiral fluorescent sensor modified with 1,2,3-triazole was synthesized in high yield (95%) by nucleophilic substitution and click reaction. The chiral fluorescent sensor showed high enantioselectivity toward phenylalanine. L-Phenylalanine enhanced the fluorescence response of the probe significantly, while D-phenylalanine had no obvious fluorescence response change. The enantioselective fluorescence enhancement ratio [ef = (IL − I0)/(ID − I0), where I0 is the fluorescence of the sensor without amino acids] for the highest fluorescence intensity at 20.0 equivalents of amino acids was 104.48. In this way, the probe could be used to identify and differentiate different configurations of phenylalanine.

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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2014 · IF 3.785

Hepatoma-targeting and pH-sensitive nanocarriers based on a novel d-galactopyranose copolymer for efficient drug delivery

Yuanyuan Ding,Jingtian Han,Baocheng Tian,Jian Han,Jing Zhang,Hong Zheng,Yuzhen Han,Meishan Pei

Smart nanoparticles based on the mechanisms of asialoglycoprotein (ASGP)-mediated endocytosis and pH-induced drug release were developed for the efficient treatment of hepatoma using a newly developed copolymer, methoxy-polyethylene glycols (PEG)-b-poly ( d -galactopyranose) (MPEG-b-PMaIPG). The particles exhibited spherical shapes, uniform particle size distribution (100   ±   4.43   nm), negative zeta potential (−32.8   ±   0.23   mV), high drug loading (24.77   ±   2.68%) and encapsulation efficiency (66.12   ±   9.44%). The in vitro drug release was also investigated, resulting that the release of drug from particles depended on different pH value. In vitro cell cytotoxicity and hemolysis assays were conducted to confirm the safety of the MPEG-b-PMaIPG nanoparticles. Anticancer activity showed that DOX-loaded MPEG-b-PMaIPG nanoparticles exhibited a high antitumor activity toward HepG2 cells, which was similar to free DOX, while blank MPEG-b-PMaIPG nanoparticles were non-toxic up to a tested concentration of 1.0   mg/mL. Confocal laser scanning microscopy (CLSM) and flow cytometry (FCM) were used to verify the targeting efficiency of d -galactopyranose-modified nanoparticles. The results clearly demonstrated that d -galactopyranose-modified nanoparticles were taken up quickly by the HepG2 cells, which suggests that MPEG-b-PMaIPG nanoparticles with good biocompatibility and non-toxic for normal cells may be used as an effective cancer-targeting drug delivery system for chemotherapy.

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