INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2025
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IF 5.2
Yuning Wang,Lixin Liu,Yunan Zhang,Yufeng Jiao,Lili Wu,Ji Zhao,Qiumei Zhang,Xinyu Tian,Huiyi Yang
To improve the physicochemical properties and biological activities of the nonsteroidal anti-inflammatory drug tolfenamic acid (TA) and the fluoroquinolone enrofloxacin (ENR). Based on the previous experience of our group in designing and synthesizing quinolone pharmaceutical co-crystals/salts single crystals by non-covalent bonding to improve their physicochemical properties, a drug-drug salt single crystal of tolfenamic acid-enrofloxacin was prepared for the first time using TA and ENR(TA-ENR, C 19 H 23 FN 3 O 3 ·C 14 H 11 ClNO 2 ·C 2 H 3 N). Single-crystal X-ray diffraction (SCXRD) analysis indicated that TA and ENR interacted predominantly through charge-assisted hydrogen bonds (CAHBs) within non-covalent bonds to form asymmetric units. Subsequently, the formation of dimers between ENR + cations in adjacent asymmetric units was promoted, leading to the formation of a stable crystalline structure through C6-H6···O2 and π···π stacking. Solubility experiments demonstrated that the solubility of TA-ENR was notably increased compared to TA. This can be ascribed to the CAHBs formed between TA and ENR, which facilitated the dissociation of TA in the dissolution medium, thereby enhancing TA’s affinity for the dissolution medium. Permeability experiments also revealed that the permeability of TA-ENR was significantly improved compared to both TA and ENR. The in vitro antimicrobial activity and anti-inflammatory activity of TA-ENR were also somewhat improved compared to TA and ENR. The success of this work implies that we may provide new ideas for designing and synthesizing solid drugs with better physicochemical properties and bioactivity, as well as for the treatment of septic arthritis, through the formation of drug-drug co-crystals/salts.
研究领域:
药学
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化学
·
生物学
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DOI
PubMed
高影响因子
MEDICINAL CHEMISTRY RESEARCH
·
2017
·Vol. 26
·期 3
·672-679
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IF 1.277
Liu Zhenbao,Wang Xiaohong,Zhang Hang,Zhang Shanshan,Li Yiqian,Liu Yanfei,Peng Dongming
Berberine owns multiple pharmacological activities, especially anti-inflammatory activity. To enhance the anti-inflammatory therapeutic efficiency of berberine, a series of novel 9- O -substituted berberine derivatives ( 5a – 5d ) were synthesized and their anti-inflammatory activities were evaluated. 13 C-NMR, 1 H-NMR, IR and high resolution mass spectrum (HRMS) results indicated that these derivatives were successfully synthesized. The xylene-induced inflammatory mice model demonstrated that these derivatives showed dose-dependent inhibition of ear inflammatory swelling. Comparing to berberine, ibuprofen and naproxen-modified berberine derivatives enhanced anti-inflammatory activities, while aspirin and nicotinic acid-modified berberine derivatives showed lower anti-inflammatory effects at the same dosages. This could be attributed to the enhanced inhibition of secretion of cytokines, including interleukin-6 and tumor necrosis factor-α, by ibuprofen and naproxen berberine derivatives, while aspirin and nicotinic acid berberine derivatives showed lower inhibition of tumor necrosis factor-α than berberine. These results suggest that ibuprofen and naproxen-modified berberine derivatives are promising new anti-inflammatory drug candidates.
研究领域:
药物化学
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炎症研究
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生物合成
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DOI
高影响因子
BMC Complementary Medicine and Therapies
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2025
·Vol. 25
·期 1
·1-13
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IF 3.4
Yang Tian,Yan YiFan,Xu YiYing,Chen YiLong,Zhi DaLong,Zhang Yan,Xiao ChaoNi
Background Loquat (Eriobotrya japonica Lindl.) fruit has been used as a heath food and folk medicine for preventing and treating the respiratory tract inflammation diseases, however, the active compounds responsible for anti-inflammation effects remain unclear.Methods Cysteinyl leukotriene receptor-1 (CysLTR1) has become an important target protein for developing therapeutics to manage the inflammation-associated diseases. Herein, a rapid approach was established by immobilizing CysLTR1 onto microspheres for the column packing, and it was applied in screening the active compounds from Loquat fruit.Results The screened compounds targeting CysLTR1 were identified as corosolic acid, ursolic acid and oleanolic acid in combination with Mass Spectrum. The high-dose combination of the three ones exhibited the stronger anti-inflammatory activity than triterpene acid alone and the Loquat extract, which can significantly decrease the counts of inflammatory cells and inhibit the production of pro-inflammatory mediators as well as increase the secretion of anti-inflammatory mediator in the LPS-inflamed mice. It was proved that three triterpene acids exhibited anti-inflammatory activities by the attenuation of CysLTR1 expression.Conclusion sOur results indicated that CysLTR1-immobilized column was a rapid and effective tool to seek out the target-specific components from herbal extract, and the screened triterpene acids could serve as alternative anti-inflammatory agents to Loquat fruit.
研究领域:
药理学
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植物化学
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分子生物学
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DOI
PubMed
高影响因子
MACROMOLECULAR BIOSCIENCE
·
2019
·Vol. 19
·期 8
·1900112
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IF 2.895
Zehong Xiang,Yanming Wang,Zhifang Ma,Zhirong Xin,Runhai Chen,Qiang Shi,Shing-Chung Wong,Jinghua Yin
Inflammation-associated thrombosis is a non-negligible source of mortalities and morbidities worldwide. To manipulate inflammation-associated coagulation, nanoparticles that contain anti-inflammatory polymer (copolyoxalate containing vanillyl alcohol, PVAX) and anti-thrombotic heparin derivative deoxycholic acid (Hep-DOCA) are prepared. The strategy takes advantage of the reducted side effects of heparin through heparin conjugation, achievement of long-term anti-inflammation by inflammation-trigged release of anti-inflammatory agents, and formation of PVAX/heparin-DOCA nanoparticles by co-self-assembly. It is demonstrated that the Hep-DOCA conjugate and PVAX are synthesized successfully; PVAX and Hep-DOCA nanodrugs (HDP) are obtained by co-assembly; the HDP nanoparticles effectively reduce the inflammation and coagulation without inducing lethal bleeding both in vivo and in vitro. The method provided here is versatile and effective, which paves new way to develop nanodrugs to treat inflammation-associated thrombosis safely.
研究领域:
药学
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纳米技术
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治疗学
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产品关联
DOI
PubMed
高影响因子
MICROCHEMICAL JOURNAL
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2025
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IF 5.1
Meng-ling Peng,Ying-ying Zhan,Li-fen Cao,Anastassiya V. Gadetskaya,Kai-jing Yu,Jing Zhang,Xiao-hui Qiu,Zhi-hai Huang,Wen Xu
Naturally aged GCP (peel of Citrus reticulata ‘ChaChi’) is a traditional medicine and food ingredient in China. Extensive studies have explored how the aging process affects the chemical and biological properties. In the present study, we used a rigorous sample collection protocol in which GCP were annually collected from a single citrus orchard and aged for 1 to 6 years in a sample warehouse for natural aging. A global chemical investigation was conducted using GC–MS and UHPLC-Orbitrap-MS, identifying 37 volatile and 112 non-volatile chemicals. Volatile terpenes and flavonoid glycosides metabolized into other constituents during aging via oxidation and hydrolysis. The contents of 55 major targets and pseudotargeted metabolomics analysis revealed distinct variation trends in polymethoxyflavones (PMFs) and limonoids. Antioxidant assays of volatile and non-volatile extracts indicated that four-year GCP samples exhibit the best antioxidant activity. The accumulation of terpenoid alcohols and sesquiterpenes, but not terpenes, presented significant positive correlations with antioxidant activity. For non-volatile constituents, PMFs and limonoids displayed significant positive correlations with antioxidant activity. RAW 264.7 cell test showed that all samples demonstrated moderate anti-inflammatory effects, and total PMFs correlated positively with anti-inflammatory activity. This study enhances understanding of the aging mechanism of GCP and establishes a rationale for its practical application.
研究领域:
植物化学
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药理学
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食品科学
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
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IF 8.5
Xiaotong Xu,Xiaoshuang Yan,Xuerong Jin,Juyi Li,Qiaoxia Hu,Dong-Hyun Ahn,Chao Zhong
Colanic acid (CA), an exopolysaccharide synthesized by bacteria, is known for its potential to extend the lifespan of nematodes. However, its high viscosity poses practical application challenges, which can be mitigated by employing colanic acid-degrading enzymes (CAEs). This study presents the expression and characterization of a novel CAE from Escherichia phage phi92, used for the production of CA oligosaccharides (CAOSs). Optimal CAE expression conditions were identified as induction at 20 °C for 24 h with 0.1 mM IPTG. The enzyme showed maximal activity at 55 °C and pH 6.0, with stability in the range of 4–50 °C and pH 4.0–7.0. Structural characterization of CAOSs was performed using GC–MS, LC–MS and NMR spectroscopy, revealing the composition of hexasaccharide and dodecasaccharide units, with CAE cleaving the β-1,4 glycosidic linkage between glucose and fucose. CAOSs were found to mitigate oxidative stress and inflammation induced by H 2 O 2 in RAW 264.7 macrophages, inhibiting NO and MDA production while enhancing CAT activity. Additionally, CAOSs modulated the mRNA expression of pro-inflammatory (IL-1β, COX-2) and anti-inflammatory (IL-10, HO-1) factors. This study deepens the understanding of CAE and facilitates the preparation of CA oligomers for applications in food, cosmetics, and pharmaceuticals.
研究领域:
微生物学
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生物化学
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医药科学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2018
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IF 3.115
Hongyan Ma,Qi Huang,Wenshan Qu,Linyuan Li,Min Wang,Shao Li,Fujiang Chu
Ethnopharmacological relevance The dried roots of Sophora flavescens Ait. (Leguminosae) is traditionally used as antipyretic medicine to reduce inflammation. It is well known that alkaloids and flavonoids are the main constituents of S. flavescens . However, the clinical researches and applications of S. flavescens is mainly based on its water-extracted alkaloids, its flavonoids may still remain in residues and have been underused. With development and manufacturing of S. flavescens in recent years, more herb residues are being produced. Since they are typically treated as waste and dumped openly in landfill sites, which can cause pollution, there is a great need to explore these wastes as recyclable resources and increase their added value. To date, whether other bioactive components would be found in the residues of S. flavescens is still unknown. If the extraction method of these active ingredients was established, the residues of S. flavescens could be turned from the harm to a benefit and make great sense of the comprehensive utilization of S. flavescens resources. This study aimed to establish an extraction method of the residues of S. flavescens and investigate the anti-inflammatory effect of it both in vivo and in vitro . Materials and methods Dried S. flavescens were decocted with distilled water firstly, then the residues were powdered and extracted with ethyl acetate by using ultrasonic wave. HPLC was utilized to analyze the chemical constituents of the water extracts of S. flavescens (WSF) and the ethyl acetate extracts of residues of S. flavescens (RSF). In vivo , the anti-inflammatory effect of WSF and RSF were evaluated using the xylene-induced auricle edema, acetic acid-induced peritoneal permeability and carrageenan-induced hind paw edema methods. In vitro, the inhibitory activities of WSF and RSF on NO, TNF-α, IL-6 and MCP-1 production of LPS-treated RAW264.7 cells were measured. Results The major ingredients of RSF were flavonoids, while WSF almost had no flavonoids. In vivo , WSF and RSF (200 mg/kg) could significantly inhibit the edema in the xylene-induced mice auricle edema and carrageenan-induced hind paw edema as well as the peritoneal permeability increased by acetic acid. They can also lower production levels of PGE 2 in inflamed paw tissues. In vitro experimental results showed that RSF (25-100 μg/mL) could significantly inhibit the release of pro-inflammatory cytokines NO, TNF-α, IL-6 and MCP-1 on LPS-induced RAW264.7 cells. The in vitro suppress effect of WSF had no dose-response relationship. Conclusions The residues of S. flavescens had obvious flavonoids with anti-inflammatory activity. This study provided evidence for the reuse of residues from S. flavescens in the food additive , medicine and cosmetic industries.
研究领域:
药理学
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民族药理学
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化学
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DOI
PubMed
高影响因子
MOLECULES
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2019
·Vol. 24
·期 16
·2906
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IF 3.06
Da-Le Guo,Jin-Feng Chen,Lu Tan,Meng-Ying Jin,Feng Ju,Zhi-Xing Cao,Fang Deng,Li-Na Wang,Yu-Cheng Gu,Yun Deng
Two new terpene glycosides (1–2) along with two known analogs (3–4) were obtained from the root ofSanguisorba officinalis,which is a common traditional Chinese medicine (TCM). Their structures were elucidated by nuclear magnetic resonance (NMR), electrospray ionization high resolution mass spectrometry (HRESIMS), and a hydrolysis reaction, as well as comparison of these data with the literature data. Compounds1–4exhibited anti-inflammatory propertiesin vitroby attenuating the production of inflammatory mediators, such as nitric oxide (NO) as well as tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). An anti-inflammatory assay based on the zebrafish experimental platform indicated that compound1had good anti-inflammatory activity in vivo by not only regulating the distribution, but also by reducing the amount of the macrophages of the zebrafish exposed to copper sulfate.Keywords:terpene glycosides;structural elucidation;Sanguisorba officinalis;zebrafish;anti-inflammatory
研究领域:
药理学
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化学
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生物学
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产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2023
·Vol. 28
·期 5
·2022
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IF 4.6
Ting Zhang,Dingrong Wan,Yuanyuan Li,Sisi Wang,Xiuteng Zhou,Fatemeh Sefidkon,Xinzhou Yang
TheArtemisia argyiLévl. et Van. growing in the surrounding areas of Qichun County in China are called Qiai (QA). Qiai is a crop that can be used both as food and in traditional folk medicine. However, detailed qualitative and quantitative analyses of its compounds remain scarce. The process of identifying chemical structures in complex natural products can be streamlined by combining UPLC-Q-TOF/MS data with the UNIFI information management platform and its embedded Traditional Medicine Library. For the first time, 68 compounds in QA were reported by the method in this study. The method of simultaneous quantification of 14 active components in QA using UPLC-TQ-MS/MS was reported for the first time. Following a screening of the activity of QA 70% methanol total extract and its three fractions (petroleum ether, ethyl acetate, and water), it was discovered that the ethyl acetate fraction enriched with flavonoids such as eupatilin and jaceosidin had the strongest anti-inflammatory activity, while the water fraction enriched with chlorogenic acid derivatives such as 3,5-di-O-caffeoylquinic acid had the strongest antioxidant and antibacterial activity. The results provided the theoretical basis for the use of QA in the food and pharmaceutical industries.Keywords:Artemisia argyiLévl. et Van.;UPLC-MS;quantification;anti-inflammatory;antioxidant
研究领域:
药理学
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分析化学
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传统医学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2025
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IF 4.9
Fan Yang,Jie Wang,Jingjing Wang,Xinyue Yang,Hongyan Zhang
Quercetin (Qc) is a natural flavonoid recognized for its diverse biological activities but is poorly soluble in water. Hydroxypropyl beta-cyclodextrin (HP-β-CD), a cyclodextrin analog, serves as a safe and efficient drug carrier by forming clathrates with therapeutic agents, enhancing their physicochemical and pharmacokinetic properties. This study reports the synthesis of inclusion complexes of HP-β-CD and Qc using ultrasonic magnetic stirring followed by lyophilization. These complexes were analyzed using X-ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and UV–Vis spectroscopy (UV), Fourier-Transform Infrared spectroscopy (FTIR), and Nuclear Magnetic Resonance (NMR) to elucidate their structural and physicochemical properties. The findings validated the successful formation of clathrates between Qc and HP-β-CD, with the resulting inclusion complexes comprising Qc/HP-β-CD demonstrating markedly distinct spectral characteristics compared to unmodified Qc. Moreover, studies revealed a substantial enhancement in the anti-inflammatory and osteogenic activities of Qc upon encapsulation. These findings demonstrate that the Qc/HP-β-CD inclusion complexes markedly enhanced Qc bioavailability while amplifying its therapeutic efficacy in inflammation and bone regeneration.
研究领域:
药理学
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材料科学
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骨生物学
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产品关联
DOI
高影响因子
ACS Applied Materials & Interfaces
·
2024
·
IF 8.3
Yue Zhao,Caiqi Cheng,Xinyi Wang,Zhengchao Yuan,Binbin Sun,Mohamed EL-Newehy,Meera Moydeen Abdulhameed,Bing Fang,Xiumei Mo
The increasing aging of the population has elevated bone defects to a significant threat to human life and health. Aerogel, a biomimetic material similar to an extracellular matrix (ECM), is considered an effective material for the treatment of bone defects. However, most aerogel scaffolds suffer from immune rejection and poor anti-inflammatory properties and are not well suited for human bone growth. In this study, we used electrospinning to prepare flexible ZnO-SiO2 nanofibers with different zinc concentrations and further assembled them into three-dimensional composite aerogel scaffolds. The prepared scaffolds exhibited an ordered pore structure, and chitosan (CS) was utilized as a cross-linking agent with aspirin (ASA). Interestingly, the 1%ZnO-SiO2/CS@ASA scaffolds not only exhibited good biocompatibility, bioactivity, anti-inflammation, and better mechanical properties but also significantly promoted vascularization and osteoblast differentiation in vitro. In the mouse cranial defect model, the BV/TV data showed a higher osteogenesis rate in the 1%ZnO-SiO2/CS group (10.94 ± 0.68%) and the 1%ZnO-SiO2/CS@ASA group (22.76 ± 1.83%), compared with the control group (5.59 ± 2.08%), and in vivo studies confirmed the ability of 1%ZnO-SiO2/CS@ASA to promote in situ regeneration of new bone. This may be attributed to the fact that Si4+, Zn2+, and ASA released from 1%ZnO-SiO2/CS@ASA scaffolds can promote angiogenesis and bone formation by stimulating the interaction between endothelial cells (ECs) and BMSCs, as well as inducing macrophage differentiation to the M2 type and downregulating the expression of pro-inflammatory factor (TNF-α) to modulate local inflammatory response. These exciting results and evidence suggest that it provides a new and effective strategy for the treatment of bone defects.
研究领域:
生物材料学
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骨组织工程
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医学
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产品关联
DOI
PubMed
高影响因子
Biomed Research International
·
2021
·
IF 3.411
F. L. Wang,H. Wang,J. H. Wang,D. X. Wang,Y. Gao,B. Yang,H. J. Yang,Y. B. Ji,G. S. Xin
Sophora viciifolia Hance is an edible plant used in traditional Chinese medicine. Sophocarpine, a tetracyclic quinolizidine alkaloid, is one of the most abundant active ingredients in Sophora viciifolia Hance. Here, we study the analgesic and anti-inflammatory effects, as well as the acute toxicity of sophocarpine from Sophora viciifolia Hance in mice. Sophocarpine (20, 40, and 80 mg/kgbw) significantly prolonged the delay period before a hot plate reaction occurred (all ), and the delay before a tail-flick response was induced by a warm bath (; ). Sophocarpine (40, 80 mg/kg) resulted in dose-dependent inhibition of the writhing reaction induced by acetic acid in mice (; , respectively). Sophocarpine (80 mg/kg) reduced the total duration of a formalin-induced pain response (). Sophocarpine prolonged the foot-licking latency of mice after the hot plate reaction, and this effect was antagonized by calcium chloride and enhanced by verapamil. Sophocarpine (20, 40, and 80 mg/kg) significantly inhibited xylene-induced ear edema (; ; , respectively) and the penetration of acetic acid-induced dye into the peritoneal cavity (; ; , respectively). It also reduced the levels of proinflammatory cytokine interleukin (IL)-1β, IL-6, and prostaglandin E2 (, , ) and those of serum nitric oxide (). The results of this study suggest that sophocarpine possesses certain analgesic and anti-inflammatory activities, which may be related to calcium and inhibition of the secretion of inflammatory factors.
研究领域:
药理学
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中药学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）