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NATURAL PRODUCT RESEARCH · 2018 · IF 1.928

New anthraquinone and eurotinone analogue from the seeds of Senna obtusifolia and their inhibitory effects on human organic anion transporters 1 and 3

Xu Pang,Li-Ming Wang,You-Cai Zhang,Li-Ping Kang,He-Shui Yu,Guan-Wei Fan,Li-Feng Han

A continuous phytochemical study on the seeds of Senna obtusifolia (Syn.: Cassia obtusifolia) led to the isolation of a new anthraquinone analogue, obtusifolin-2-O-β-D-(6’-O-α,β-unsaturated butyryl)-glucopyranoside (1) and a new eurotinone analogue, epi-9-dehydroxyeurotinone-β-D-glucopyranoside (2). Their structures were established mainly by NMR and MS experiments as well as the necessary chemical evidences. Their inhibitory effects on two organic anion transporters (OAT1 and OAT3) were investigated and the results showed that 1 exhibited a strongly specific inhibitory effect on OAT1 at 100 μM.

CAS / MDL: 3301-79-9
研究领域: 药理学 · 化学 · 分子生物学
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BIOTECHNOLOGY LETTERS · 2015 ·Vol. 38 ·期 4 ·619-627 · IF 1.591

Synthesis of rosmarinic acid analogues in Escherichia coli

Zhuang Yibin,Jiang Jingjie,Bi Huiping,Yin Hua,Liu Shaowei,Liu Tao

Objectives To produce rosmarinic acid analogues in the recombinant Escherichia coli BLRA1, harboring a 4-coumarate: CoA ligase from Arabidopsis thaliana (At4CL) and a rosmarinic acid synthase from Coleus blumei (CbRAS). Results Incubation of the recombinant E. coli strain BLRA1 with exogenously supplied phenyllactic acid (PL) and analogues as acceptor substrates, and coumaric acid and analogues as donor substrates led to production of 18 compounds, including 13 unnatural RA analogues. Conclusion This work demonstrates the viability of synthesizing a broad range of rosmarinic acid analogues in E. coli , and sheds new light on the substrate specificity of CbRAS.

研究领域: 生物化学 · 合成生物学
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Catalysts · 2022 ·Vol. 12 ·期 10 ·1140 · IF 4.501

Single-Phase θ-Fe3C Derived from Prussian Blue and Its Catalytic Application in Fischer-Tropsch Synthesis

Wei Zhang,Caiping Ma,Xingwu Liu,Yong Yang,Yongwang Li,Xiaodong Wen

Elucidation of the intrinsic catalytic principle of iron carbides remains a substantial challenge in iron-catalyzed Fischer-Tropsch synthesis (FTS), due to possible interference from other Fe-containing species. Here, we propose a facile approach to synthesize single-phase θ-Fe3C via the pyrolysis of a molecularly defined Fe-C complex (Fe4[Fe(CN)6]3), thus affording close examination of its catalytic behavior during FTS. The crystal structure of prepared θ-Fe3C is unambiguously verified by combined XRD and MES measurement, demonstrating its single-phase nature. Strikingly, single-phase θ-Fe3C exhibited excellent selectivity to light olefins (77.8%) in the C2-C4hydrocarbons with less than 10% CO2formation in typical FTS conditions. This strategy further succeeds with promotion of Mn, evident for its wide-ranging compatibility for the promising industrial development of catalysts. This work offers a facile approach for oriented preparation of single-phase θ-Fe3C and provides an in-depth understanding of its intrinsic catalytic performance in FTS.Keywords:θ-Fe3C;single phase;Fischer-Tropsch synthesis;Prussian blue analogue

研究领域: 催化 · 材料科学 · 化学工程
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Chemical Biology & Drug Design · 2015 ·Vol. 86 ·期 4 ·753-763 · IF 2.485

Synthesis and Anti-Inflammatory Evaluation of Novel C66 Analogs for the Treatment of LPS-Induced Acute Lung Injury

Jianpeng Feng,Bing Xiao,Wenbo Chen,Ting Ding,Lingfeng Chen,Pengtian Yu,Fengli Xu,Huajie Zhang,Zhiguo Liu,Guang Liang

We previously reported a symmetric monocarbonyl analog of curcumin (MACs), C66, which demonstrated potential anti-inflammatory activity and low toxicity. In continuation of our ongoing research, we designed and synthesized 34 asymmetric MACs based on C66 as a lead molecule. A majority of the C66 analogs effectively inhibited LPS induction of TNF- α and IL-6 expression. Additionally, a preliminary SAR was conducted. Furthermore, active compounds 4a11 and 4a16 were found to effectively reduce the W/D ratio in the lungs and the protein concentration in the bronchoalveolar lavage fluid (BALF). Meanwhile, a histopathological examination indicated that these two analogs significantly attenuate tissue injury in the lungs with LPS-induced ALI rats. 4a11 and 4a16 also inhibited mRNA expression of several inflammatory cytokines, including TNF- α , IL-6, IL-1 β , COX-2, ICAM-1 and VCAM-1, in the Beas-2B cells after LPS challenge. Altogether, the data exhibit a series of new C66 analogs as promising anti-inflammatory agents for the treatment of LPS-induced ALI.

研究领域: 药理学 · 合成化学 · 免疫学
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2024 · IF 5.7

Hydroxamate-Containing Bisphosphonates as Fosmidomycin Analogues: Design, Synthesis, and Proherbicide Activity

Xin Wu,Zili Yang,Chunlin Song,Mengwei Bu,Weiguo Li,Jiang Duan,Guang-Fu Yang,Aidong Zhang

Fosmidomycin (FOS) is a natural product inhibiting the DXR enzyme in the MEP pathway and has stimulated interest for finding more suitable FOS analogues. Herein, two series of FOS analogue hydroxamate-containing bisphosphonates as proherbicides were designed, with bisphosphonate replacing the phosphonic unit in FOS while retaining the hydroxamate (BPF series) or replacing it with retro-hydroxamate (BPRF series). The BPF series were synthesized through a three-step reaction sequence including Michael addition of vinylidenebisphosphonate, N-acylation, and deprotection, and the BPRF series were synthesized with a retro-Claisen condensation incorporated into the reaction sequence. Evaluation on model plants demonstrated several compounds having considerable herbicidal activities, and in particular, compound 8m exhibited multifold activity enhancement as compared to the control FOS. The proherbicide properties were comparatively validated. Furthermore, DXR enzyme assay, dimethylallyl pyrophosphate rescue, and molecular docking verified 8m to be a promising proherbicide candidate targeting the DXR enzyme. In addition, 8m also displayed good antimalarial activities.

研究领域: 植物学 · 药理学 · 农业科学
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JOURNAL OF THE AMERICAN CERAMIC SOCIETY · 2016 ·Vol. 100 ·期 1 ·333-342 · IF 2.787

A Visible Light Photocatalyst of Carbonate-Like Species Doped TiO2

Linhui Yu,Yangming Lin,Jing Huang,Sen Lin,Danzhen Li

Carbon-doped TiO 2 nanomaterials have been successfully synthesized via an effective two-step procedure involving hydrothermal method and followed by a low-temperature calcination treatment process, through which a controllable amount of carbonate-like species could be incorporated into TiO 2 . First-principles calculations suggest the TiO 2 doped with carbon in form of carbonate-like species can effectively extend the adsorption of the material from ultraviolet region to visible light. And it is experimentally found that carbon-doped TiO 2 nanomaterials exhibit much higher photocatalytic activity than reference P25 and TiO 2− x N x catalysts toward the liquid-phase degradation of organic pollutants under visible light (420 nm < λ < 800 nm) irradiation. The presence of synergic effect between carbonate-like doping and anatase TiO 2 is believed to play an essential role in affecting the photocatalytic reactivity, and the response to the visible light is ascribed to the narrowed band gap energy controlled by carbon doping. Moreover, the roles of active species in the photocatalytic process are compared using different types of active species scavengers. Meanwhile, the degradation mechanism of the photocatalysis is proposed. It is hoped that our work could provide valuable information on the design of carbonate-like doped semiconductor with more excellent properties and set the foundation for the further industrial application.

CAS / MDL: 546-68-9
研究领域: 材料科学 · 环境科学
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International Journal of Nanomedicine · 2024 · IF 6.6

Development of the Curcumin Analog CA7 Liposome and Its Evaluation for Efficacy Against Cervical Cancer in vitro and in vivo

Linjin Xiong,Yumeng Wei,Hui Si,Zheng Li,Jie Wen,Furong Liu,Xiaodong Wang,Hongru Yang,Ligang Chen,Chao Pi,Yunwei Han,Ling Zhao

Objective The objective of this study was to develop liposomes (LP) containing a curcumin (CU) analog CA7 to enhance its pharmacokinetic profile and anti-cervical cancer (CC) effects.Methods Single-factor and Box-Behnken experiments were conducted to optimize the formulation of CA7-loaded liposomes (CA7-LP). The in vitro release, stability, biocompatibility, and pharmacokinetic of CA7-LP were evaluated. The biological effects of CA7-LP on Hela cells were assessed using MTT assays, colony formation assays, wound healing assays, and flow cytometry. Additionally, the anti-CC efficacy of CA7-LP was tested in mouse models of transplanted tumors.Results The optimal formulation of CA7-LP exhibited a particle size of 92.43 ± 1.52 nm, a polydispersity index of 0.27 ± 0.01, an encapsulation efficiency of 97.79 ± 1.49%, a drug loading of 3.23 ± 0.20%, and a zeta potential of −6.69 ± 0.77 mV. Transmission electron microscopy confirmed that a spherical morphology was exhibited by CA7-LP. The cumulative in vitro release of CA7-LP was found to be 2.84 times greater than that of CA7, and stability at room temperature was maintained for at least 90 d. Furthermore, a significantly higher uptake of CA7-LP by Hela cells was observed compared to curcumin and CA7, leading to enhanced inhibition of cell proliferation, migration and cell cycle, as well as increased apoptosis (p < 0.05). In vivo studies revealed that CA7-LP exhibited superior pharmacokinetic properties compared to CA7 (AUC: 3.58-fold, Cmax: 5.65-fold, t1/2z: 1.2-fold). The anti-CC effects of CA7-LP were found to be comparable to those of Cisplatin injection, with a better safety profile.Conclusion The newly developed CA7-LP is considered a promising candidate for the treatment of CC, demonstrating high potential for clinical application.

CAS / MDL: 8002-43-5
研究领域: 药理学 · 肿瘤学 · 生物医学工程
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Communications Biology · 2024 ·Vol. 7 ·期 1 ·1-14 · IF 5.2

3,4-Dichlorophenylacetic acid acts as an auxin analog and induces beneficial effects in various crops

Tan Chao,Li Suxin,Song Jia,Zheng Xianfu,Zheng Hao,Xu Weichang,Wan Cui,Zhang Tan,Bian Qiang,Men Shuzhen

Auxins and their analogs are widely used to promote root growth, flower and fruit development, and yield in crops. The action characteristics and application scope of various auxins are different. To overcome the limitations of existing auxins, expand the scope of applications, and reduce side effects, it is necessary to screen new auxin analogs. Here, we identified 3,4-dichlorophenylacetic acid (Dcaa) as having auxin-like activity and acting through the auxin signaling pathway in plants. At the physiological level, Dcaa promotes the elongation of oat coleoptile segments, the generation of adventitious roots, and the growth of crop roots. At the molecular level, Dcaa induces the expression of auxin-responsive genes and acts through auxin receptors. Molecular docking results showed that Dcaa can bind to auxin receptors, among which TIR1 has the highest binding activity. Application of Dcaa at the root tip of the DR5:GUS auxin-responsive reporter induces GUS expression in the root hair zone, which requires the PIN2 auxin efflux carrier. Dcaa also inhibits the endocytosis of PIN proteins like other auxins. These results provide a basis for the application of Dcaa in agricultural practices.

研究领域: 植物学 · 分子生物学 · 农业科学
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TALANTA · 2022 · IF 6.556

Tuning the Fe/Co ratio towards a bimetallic Prussian blue analogue for the ultrasensitive electrochemical sensing of 5-hydroxytryptamine

Hao Feng,Fan Wang,Junhua Li,Qian Wu,Ying Cui,Lingzhi He,Xing Liu,Zeng Liu,Dong Qian,Haixia Tong

Lack of highly efficient, inexpensive, and easily available catalysts severely limits the practical applicability of electrochemically sensing assay towards 5-hydroxytryptamine (5-HT). Herein, four kinds of Fe–Co bimetallic Prussian blue analogues (FeCo–PBAs) with different molar ratios of Fe to Co were prepared using a simple coprecipitation method. Interestingly, Fe(III) in K 3 [Fe(CN) 6 ] can be reduced to Fe(II) by adding trisodium citrate dehydrate, which could offer a new clue to synthesize PBAs with Fe(II) core ions. With the optimizational FeCo-PBA synthesized at a 0.5/1 M ratio of Fe to Co as an electrocatalyst , the constructed sensor shows excellent comprehensive performance for the 5-HT assay with a high sensitivity of 0.856 μA μM −1 and an ultralow detection limit of 8.4 nM. Under the optimum conditions, linearity was obtained in the ranges of 0.1–10.0 μM and 10.0–200.0 μM and preferable recoveries ranged from 97.8% to 103.0% with relative standard deviation (RSD) < 4.0%. The integrated properties of FeCo-PBA can be comparable to previously reported electrocatalysts for the 5-HT assay including noble metal-based and expensive carbon (graphene and carbon nanotubes)-based electrocatalysts. The proposed sensor also exhibits outstanding selectivity, reproducibility, and practicality for real sample analyses. This work is the first report on the PBA-based sensor for the 5-HT assay, verifying the practicability of this high-performance sensor for the 5-HT assay.

CAS / MDL: 50-67-9
研究领域: 生物化学 · 分析化学
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Colloids and Interfaces · 2023 ·Vol. 7 ·期 1 ·14 · IF 2.4

Boosting Water Oxidation Activity via Carbon–Nitrogen Vacancies in NiFe Prussian Blue Analogue Electrocatalysts

Meng Zhang,Wenjie Wu,Zhen Wang,Gang Xie,Xiaohui Guo

The development of electrocatalysts for oxygen evolution reactions (OERs) is of great significance for hydrogen production. Defect engineering is an effective strategy to improve the OER performance of electrocatalyst by regulating the local electronic and atomic structures of electrocatalysts. Here, we successfully synthesized defective Prussian blue analogues (PBAs) with rich CN vacancies (D-NiFe PBA) as efficient OER electrocatalysts. The optimized D-NiFe PBA exhibited an overpotential of 280 mV at 10 mA cm−2and a superior stability for over 100 h in KOH electrolytes. The formation of CN vacancies in the NiFe PBA could effectively inhibit the loss of Fe active sites, promote the reconstruction of the NiFe oxygen (hydroxide) active layer in the OER process, and further improve the electrocatalytic activity and stability of the VCN-NiFe PBA. This work presents a feasible approach for the wide application of vacancy defects in PBA electrocatalysts.Keywords:Prussian blue analogues;vacancy;OER;activity;stability

CAS / MDL: 12030-49-8
研究领域: 材料科学 · 电化学
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2025 · IF 9.7

Ameliorating water splitting by entropy regulation and electronic structure engineering on pristine Prussian blue analog

Xuechun Zhou,Xianhao Chen,Boxuan Li,He Zhu,Si Lan,Horst Hahn,Tao Feng

Electrochemical water splitting is the most promising green method for hydrogen production. In this work, the traditional Prussian blue analogs were endowed with the new concept of high entropy to bring a breakthrough in electrocatalytic performance. A classic two-step synthetic strategy was employed to fabricate the high-entropy FeCoNiCr 6 P nanoparticle via phosphating the FeCoNiCr 6, which was prefabricated using a facile coprecipitation method. The phosphides can trap protons by acting as bases to promote the discharge step faster. FeCoNiCr 6 P requires a lower overpotential of only 268.3 mV at a current density of 100 mA cm −2 for OER. The FeCoNiCr 6 P//FeCoNiCr 6 P electrochemical water splitting couple can realize a low voltage of 1.58 V to at 10 mA cm −2 current density. Furthermore, the electronic states and coordination environment of catalyst active sites were investigated to get deeper insight into material design.

CAS / MDL: 1310-58-3
研究领域: 材料科学 · 电化学
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Scientific Reports · 2025 ·Vol. 15 ·期 1 ·1-13 · IF 3.9

Design of a novel long-acting insulin analogs by acetylation modification and compared with insulin Icodec

Yu Min,Zhang Chuanzhi,Xu Hongjiang,Dong Yuanzhen,Zhu Hongxiang,Xia Chunguang,Feng Jun

Insulin is a potent medication for managing diabetes, yet its short half-life requires daily administration. Currently, Novo Nordisk’s icodec is the sole insulin available on the market that requires administration only once a week. Insulin icodec, developed by Novo Nordisk through amino acid mutations and fatty acid side chain modifications, has demonstrated the capability to control blood glucose levels on a once-weekly basis. To improve its efficacy, we modified the acylation side chain of icodec to generate insulin analogs appropriate for weekly dosing. A promising insulin analog, TBE001-A-S033, was synthesized and conjugated, and its efficacy was assessed in ICR and db/db mice. TBE001-A-S033 prolonged blood glucose control in ICR mice and exhibited a comparable blood glucose trend to insulin icodec in db/db mice. These findings suggest that TBE001-A-S033 possesses a favorable hypoglycemic effect and a differential half-life across species compared to insulin icodec, indicating its potential for once-weekly use in humans. This preclinical investigation indicates that TBE001-A-S033 may serve as an effective therapeutic for type 2 diabetes mellitus (T2DM).

CAS / MDL: 693-13-0
研究领域: 药理学 · 糖尿病研究 · 生物化学
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