ACTA PHARMACOLOGICA SINICA
·
2024
·
IF 6.9
He Rong-rong,Ma Chuan-rui,He Xin,Dong Yan-xi,Li Hui,Chu Zi-xuan,Yang Xi-he,Wang Jia-qi,Wang Ting,Wang Feng-qing,Du Fei-fei,Rao Ying,Yu Wen-xuan,Gao Xiu-mei,Fan Guan-wei,Cheng Chen,Li Chuan
Translational pharmacological research on traditional medicines lays the foundation for precisely understanding how the medicines function in the body to deliver therapeutic benefits. Borneolum syntheticum (Bingpian) is commonly used in Chinese herbal medicines for coronary heart disease, but its specific cardiovascular impact remains poorly understood. Isoborneol, a constituent of Bingpian, has been found to reduce lipid accumulation in macrophages in vitro, but its oral bioavailability is limited. This investigation aimed to evaluate anti-atherosclerotic effects of Bingpian, based on understanding its first-pass metabolism. Human subjects orally received an herbal medicine containing Bingpian and their plasma samples were analyzed to identify the major circulating compounds of Bingpian, with the metabolism that was also characterized in vitro and in mice. The identified compounds were evaluated for their ability to inhibit macrophage foam-cell formation induced by oxidized low-density lipoprotein. Furthermore, the anti-atherosclerotic effect of repeatedly dosed Bingpian was assessed in ApoE −/− mice fed a high-fat diet. In human subjects, the major circulating compounds of Bingpian were metabolites, rather than their precursor constituents borneol and isoborneol. These constituents were efficiently absorbed in the intestinal tract but underwent significant first-pass metabolism, involving UGT2B7-mediated glucuronidation into borneol-2- O -glucuronide and isoborneol-2- O -glucuronide, respectively, and CYP2A6/2B6/3A-mediated oxidation both into camphor. Despite their poor membrane permeability, hepatic efflux of borneol-2- O -glucuronide and isoborneol-2- O -glucuronide into the systemic circulation was enhanced by MRP3/4. The circulating metabolites, particularly their combinations, markedly inhibited macrophage foam-cell formation induced by oxidized low-density lipoprotein in vitro. Sub-chronic administration of Bingpian (30 mg·kg −1 ·d − 1 , i.g.) for 12 weeks significantly decreased atherosclerotic lesion size and enhanced plaque stability in ApoE −/− mice. Systemic exposure to Bingpian metabolites in mice closely resembles that in humans, suggesting that the pharmacodynamic effects of Bingpian in mice are likely applicable to humans. Overall, the cardiovascular benefits of Bingpian involve reducing atherosclerosis by inhibiting foam-cell formation through its metabolites. This investigation supports that oral Bingpian could be a druggable agent for reducing atherosclerosis.
研究领域:
药理学
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心血管疾病
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传统中药
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代谢
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转化研究
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DOI
PubMed
高影响因子
MACROMOLECULES
·
2025
·
IF 5.2
Xiangbin Sun,Yuanyuan Xie,Xiaobing Ma,Yufeng He,Pengfei Song,Rongmin Wang
Bacterial biofilm contamination poses a substantial threat to public health and safety while also leading to considerable economic losses. In this study, a series of both offensive and defensive poly(quaternary phosphonium salt-borneol) copolymers (P(QPx-BOy)), utilizing stereochemically structured borneol as the membrane breaking arrow and quaternary phosphonium salt cations as the electrostatic driving force, were successfully synthesized. Notably, this work exemplifies a novel integration of natural borneol with quaternary phosphonium cations. Subsequently, the molecular structure, molecular weight distribution, microstructure, and corresponding physicochemical properties of the P(QPx-BOy) were characterized using NMR, FT-IR, GPC, SEM, EDS, CA, and DLS. Leveraging the electrostatic interaction between the phosphonium cation and the stereochemical antibacterial mechanism of borneol, P(QPx-BOy) exhibited remarkable antibacterial efficacy against both E. coli and S. aureus, achieving a 100% antibacterial rate with MIC value as low as 30 μg/mL. Furthermore, crystal violet staining assays revealed that borneol’s unique antibiofilm mechanism exerts a significant inhibitory effect on bacterial biofilm formation. Finally, the biocompatibility and antibacterial potential of P(QPx-BOy) were evaluated through cytotoxicity assays and fabric antibacterial tests. Specifically, the integration of borneol essential oil with hydrophilic quaternary phosphonium salt cations effectively addresses the hydrophobic nature of borneol essential oil while mitigating the cytotoxic effects associated with quaternary phosphonium salts. This synergistic combination leverages the strengths of both components, thereby enhancing their suitability for applications in healthcare and public health sectors.
研究领域:
材料科学
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微生物学
·
生物医学工程
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产品关联
DOI
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
·
2024
·
IF 5.6
Wen Wang,Tom Coenye,Jianyu Su,Sheng-Xiang Qiu
Biofilms growing on food surfaces, packaging, equipment and processing environments bring huge risks to food safety and result in economic losses. Natural components are receiving increasing interest as “green” antimicrobial agents due to their biocompatibility, broad-spectrum antimicrobial properties, and antibiofilm potential. As a traditional adjuvant in Chinese medicine, borneol has the potential to enhance citral’s antibiofilm efficacy. In this study, the antibiofilm activities of citral, borneol, and the combination citral and borneol (BC) against various foodborne bacteria were evaluated using multiple techniques. Light microscopy, crystal violet (CV) staining, and the 2,3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5-[(phenylaminocarbonyl]-2H-tetrazolium hydroxide (XTT) assay were employed to monitor biofilm formation. Additionally, biofilm eradication was assessed against Staphylococcus aureus and Escherichia coli biofilms grown on polycarbonate membranes. Protein leakage was measured, and field emission scanning electron microscopy (FESEM) was used to examine cell membrane integrity. Results showed that borneol and citral acted synergistically to inhibit biofilms. Borneol, citral, alone or together inhibited biofilm formation in a concentration dependent manner, and they have the ability to inactivate or kill at least 90.7 ± 1.9 % bacteria in preformed biofilms. Both borneol and citral disrupted the membrane integrity of the bacteria, increased permeability, and ultimately led to cell death. These findings suggest that the combination citral and borneol has the potential to be developed as a food preservative or bactericidal agent for controlling foodborne bacterial contamination.
研究领域:
微生物学
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食品安全
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天然产物研究
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产品关联
DOI
高影响因子
EUROPEAN POLYMER JOURNAL
·
2023
·
IF 6
Susu Zhao,Dejin Zhang,Yujie Jiang,Chuanhui Gao,Lei Liu,Yuetao Liu
Nowadays, the development of sustainable nontoxic antifouling coatings is urgent. In this work, the isobornyl as antifouling groups and dodecfluoroheptyl were introduced into the silicone side chains to prepare the environment-friendly silicone antifouling coatings. The synergistic effect of natural borneol and dodecfluoroheptyl improved the static antifouling ability of silicone coating. The coatings exhibited good optical clarity (>92%, 400–800 nm), high adhesion (>2 MPa, steel plates) and excellent fouling release and self-cleaning ability. For example, PDMS-F-PIBO-23 coating had excellent antibacterial and antifouling activities. It’s antibacterial resistance to marine bacteria (Pseudomonas sp.) reached 95.6%, which reduced the coverage area of biofilm by 86.9%, and effectively prevented the adhesion of diatoms. This remarkable antibacterial and antifouling performance was attributed to the complex molecular structure of natural non-toxic borneol and the enrichment of fluoropolymers. Field tests at Yellow Sea showed that the coating had good antifouling ability and could be used for >6 months. Most importantly, compared with traditional coatings containing toxic fungicides, the coating is less harmful to the marine ecological balance. This research provides more possibilities for marine antifouling coatings design and preparation which is expected to be applied in marine, medical and other antipollution fields.
研究领域:
材料科学
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海洋生物学
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环境科学
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产品关联
DOI
高影响因子
Frontiers in Plant Science
·
2022
·
IF 6.627
Zhang Jianyun,Zhao Ziyi,Liang Wenyu,Bi Jingyi,Zheng Yuguang,Gu Xian,Fang Huiyong
Sabina chinensis is a woody plant with important ecological functions in different regions of China, but its essential oils (EO) against plant pathogenic fungi remain largely undetermined. The purpose of our study was to assess the chemical composition and antifungal activity of S. chinensis EO based on optimization of the extraction process. In this study, an actionable and effective model with the experimental results and identified optimum conditions (crushing degree of 20 mesh, liquid–solid ratio of 10.1:1, immersion time of 9.1 h) was established successfully to achieve an extraction yield of 0.54%, which was basically consistent with the theoretical value. A total of 26 compounds were identified using headspace gas chromatography–mass spectrometry (GC–MS) and showed that the major constituent was β-phellandrene (26.64-39.26%), followed by terpinen-4-ol (6.53-11.89%), bornyl acetate (6.13-10.53%), etc. For Petri plate assays, our experiments found for the first time that S. chinensis EO revealed high and long-term antifungal activity against the tested strains, including Fusarium oxysporum and Fusarium incarnatum, at EC50 values of 1.42 and 1.15 µL/mL, which especially reached approximately 76% and 90% growth inhibition at a dose of 0.2 µL/mL, respectively. Furthermore, the antifungal activity of EO from different harvest periods showed remarkable variation. The orthogonal partial least-squares discriminant analysis (OPLS-DA) method revealed 11 metabolites with chemical marker components, and 5 of its potential antifungal activities, terpinen-4-ol, α-terpineol, α-elemol, γ-eudesmol, and bornyl acetate, were strongly correlated with the mycelial inhibition rate. In total, this study explored the antifungal activity of EO against root rot fungus as a potential fungicide and provided valuable information into developing potential products from natural agents.
研究领域:
植物科学
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植物病理学
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天然产物化学
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产品关联
DOI
PubMed
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
·
2018
·
IF 3.849
Fu Xiang,Jinhai Bai,Xiaobei Tan,Ting Chen,Wei Yang,Feng He
Essential oil is one of the most important bioactive substances of Artemisia argyi Levl. et Van. var. argyi cv. Qiai, a traditional Chinese herb used in folks for centuries. An essential oil was prepared by steam distillation method. Chemical components of the essential oil were explored by gas chromatography-mass spectrometry. Antimicrobial activities of the essential oil were determined by agar disc diffusion assay and double-broth dilution method. Also, antimicrobial mechanisms were investigated based on cytomembrane permeability, protein and K + leakage and electron microscopy. The results showed that the essential oil yield was (0.7 ± 0.02)% (w/w). A total of 32 components were identified, and thujone was found to be the major compound (14.94%), followed by globulol (11.6%), 1,8-cineole (11.31%), 1-caryophyllene (8.11%), camphor (6.87%), α-terpineol (4.69%), caryophyllene oxide (4.05%), borneol (3.95%), eugenol (3.01%), and germacrene D (2.81%). The oil showed antimicrobial activities against both Gram-positive and Gram-negative bacteria. The minimum inhibition concentrations of the essential oil against Staphylococcus aureus , Bacillus cereus , Bacillus subtilis , Listeria monocytogenes , Escherichia coli , Pseudomonas aeruginosa , and Salmonella Typhimurium were 16.0, 16.0, 32.0, 32.0, 32.0, 64.0, and 32.0 μg/mL, respectively. The minimum bactericidal concentrations of the essential oil against bacteria mentioned above were 32.0, 16.0, 64.0, 64.0, 64.0, 128.0, and 64.0 μg/mL, respectively. Supposedly, the possible antimicrobial mechanism of the essential oil involved simultaneous cytomembrane disruption, leading to the leakage of intracellular substances, such as protein and K + . The results indicated that the cytomembrane might be the target of essential oil.
研究领域:
药理学
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微生物学
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化学
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植物学
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产品关联
DOI
高影响因子
Arabian Journal of Chemistry
·
2023
·
IF 6
Tianming Zhao,Guang Fan,You Tai,Xinhe Shu,Fu Tian,Shuliang Zou,Qin Wu
Illicium lanceolatum is a medicinal and aromatic plant widely distributed in the south of China. The reports on chemical composition and biological activities of its essential oils (EOs) were very limited. In this study, Illicium lanceolatum EOs were extracted by hydro distillation, and analyzed by GC–MS and GC-FID. DPPH radical scavenging assay, ABTS cation radical scavenging assay and ferric reducing/antioxidant power (FRAP) assay were used for antioxidant activity evaluation. Minimum inhibitory concentrations (MICs) and minimum microbiocidal concentrations (MMCs) against 9 microorganisms were determined. The inhibitory effects on tyrosinase, α -glucosidase and cholinesterases were evaluated and cytotoxic activities were evaluated using MTT assay. The results revealed 110 identified compounds, with asaricin, eucalyptol, linalool and caryophyllene oxide as major compounds. Eucalyptol was the most abundant compound in the stem, leaf and fruit EOs while asaricin accounted for 50.52 ± 0.33 % in the root EO. Very weak radical scavenging capacities were noticed for all EOs, but the root EO showed moderate antioxidant activity (176.33 ± 4.52 mg TE/g of EO) in the FRAP assay, which could be attributed to asaricin. The root EO displayed better antimicrobial activities than other three EOs, with MIC values as 3.13 mg/mL against three bacteria including Staphylococcus aureus BNCC 186335, Bacillus cereus BNCC 103930 and Listeria monocytogenes BNCC 336877. Camphor and borneol were found to be important antimicrobial compounds. No inhibitory effect on α -glucosidase was found. The leaf EO displayed better acetylcholinesterase inhibitory activity (17.79 ± 0.32 mg GE/g of EO) while the root EO showed better tyrosinase (30.34 ± 0.40 mg KAE/g of EO) and butyrylcholinesterase (43.25 ± 1.50 mg GE/g of EO) inhibitory activities. Molecular docking between active compounds and enzymes revealed the main interactions as hydrophobic interaction, hydrogen bond and π -stacking. All EOs displayed weak cytotoxicity to HK-2 cells of normal kidney at six tested concentrations. The leaf EO showed strong anticancer activities to HepG2 cells at the concentration of 500 μg/mL. I. lanceolatum EOs showed promising prospects with possible applications in pharmaceutical and cosmetic industries.
研究领域:
药理学
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生物化学
·
微生物学
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植物科学
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药物化学
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产品关联
DOI
高影响因子
AAPS PHARMSCITECH
·
2024
·Vol. 25
·期 7
·1-19
·
IF 3.4
Long Yanqiu,Lei Fang,Hu Jie,Zheng Zhiyun,Gui Shuangying,He Ning
The compound Salvia Recipe has been shown to have a relatively significant curative effect in management of cardiovascular and cerebrovascular diseases. This work aimed to prepare a thermosensitive in situ gel (ISG) delivery system that utilizes Poloxamer 407, Poloxamer 188, and hydroxypropyl methylcellulose for ocular administration of the compound Salvia recipe to treat cardiovascular and cerebrovascular diseases. The central composite design-response surface method was utilized to improve the prescription of the gel. The formulated gel was characterized and assessed in terms of stability, retention time, in vitro release, rheology, ocular irritation, pharmacokinetics studies, and tissue distribution. The gel was a liquid solution at room temperature and became semisolid at physiological temperature, prolonging its stay time in the eye. Pharmacokinetics and tissue distribution experiments indicated that thermosensitive ISG had enhanced targeting of heart and brain tissues. Additionally, it could lower drug toxicity and side effects in the lungs and kidneys. The compound Salvia ophthalmic thermosensitive ISG is a promising drug delivery system for the management of cardiovascular and cerebrovascular illnesses. Graphical Abstract
研究领域:
药剂学
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生物医学工程
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眼科药物递送
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产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2024
·
IF 8.3
Xiaobang Liu,Jiaqun Du,Junpeng Sun,Han Wang,Jinyu An,Yingqiao Li,Yu Hu,Shuai Cheng,Huicong Feng,He Tian,Xifan Mei,Yang Qiu,Chao Wu
Spinal cord injury (SCI) is a serious neurological disease that can result in paralysis. After SCI occurs, the blood–spinal cord barrier (BSCB) is disrupted, and permeability is transiently elevated. However, the permeability of the BSCB returns to normal over time, which prevents many drugs from being used in subsequent treatments. In this study, we designed a borneol-functionalized macrophage membrane encapsulating mesoporous selenium nanoparticles loaded with resveratrol (MSe-Res-BMMs) for SCI treatment. In vivo animal experiments and in vitro cell experiments demonstrated that MSe-Res-BMMs were able to protect neurons from ferroptosis by reducing ROS levels and increasing glutathione peroxidase-4 (GPx-4) activity. In addition, this treatment also reduced ROS-induced inflammation and apoptosis by decreasing the expression of inflammatory factor IL-1β and apoptotic factor Cleaved Caspase-3 at the site of injury. Therefore, MSe-Res-BMMs are expected to provide new therapeutic options for SCI treatment.
研究领域:
神经科学
·
药理学
·
纳米医学
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产品关联
DOI
PubMed
高影响因子
Bioactive Materials
·
2024
·
IF 18
Yuhsien Lai,Xuesong Wu,Zhuoyu Jiang,Yifei Fang,Xiuting Liu,Dan Hong,Yanyun Jiang,Guozhen Tan,Shiqi Tang,Siyao Lu,David Wei,Sam T. Hwang,Kit S. Lam,Liangchun Wang,Yanyu Huang,Zhenrui Shi
Psoriasis, an immune-mediated inflammatory skin disorder characterized by a chronically relapsing-remitting course, continues to be primarily managed through topical therapy. While oral administration of tyrosine kinase 2 inhibitors (TYK2i) stands as an effective approach for psoriasis treatment, the potential efficacy of topical application of TYK2i remains unexplored. Herein, the carbomer/alginic acid hydrogel is embedded with borneol (BO) as a new topical carrier of TYK2i for achieving enhanced transdermal permeation and anti-psoriasis efficacy. The hydrogel system, i.e., TYK2i-BO-gel, exhibits significantly improved preventative and therapeutic effects in mice models of psoriasiform dermatitis, as evidenced by phenotypical images, psoriasis severity score index (PSI), histology, immunohistochemical staining, and PCR analysis. Remarkably, TYK2i-BO-gel outperforms conventional topical corticosteroid therapy by significantly preventing psoriatic lesion recurrence as measured by a nearly 50 % reduction in ear thickness changes ( p < 0.0001), PSI ( p < 0.0001) and epidermal thickness ( p < 0.05). Moreover, a strengthened anti-inflammatory effect caused by TYK2i-BO-gel is seen in a human skin explant model, implying its potential application for human patients. With the addition of BO, the TYK2i-BO-gel not only increases skin permeability but also inhibits the expression of antimicrobial peptides in keratinocytes and facilitates the anti-Th17 response of TYK2i with suppressed activation of STAT3. Therefore, this work represents the accessibility and effectiveness of TYK2i-BO-hydrogel as a new topical formulation for anti-psoriasis management and shows great potential for clinical application.
研究领域:
皮肤病学
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药剂学
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免疫学
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产品关联
DOI
PubMed
高影响因子
ACS Nano
·
2024
·
IF 15.8
Guanlin Wang,Zizhao Zhai,Wenhao Wang,Xiao Xia,Haihua Guo,Xiao Yue,Xiaoyuan Wang,Bing Zhu,Zhengwei Huang,Xin Pan,Ying Huang,Chuanbin Wu,Xuejuan Zhang
The nanodrug delivery system-based nasal spray (NDDS-NS) can bypass the blood–brain barrier and deliver drugs directly to the brain, offering unparalleled advantages in the treatment of central nervous system (CNS) diseases. However, the current design of NNDS-NS is excessively focused on mucosal absorption while neglecting the impact of nasal deposition on nose-to-brain drug delivery, resulting in an unsatisfactory nose-to-brain delivery efficiency. In this study, the effect of the dispersion medium viscosity on nasal drug deposition and nose-to-brain delivery in NDDS-NS was elucidated. The optimized formulation F5 (39.36 mPa·s) demonstrated significantly higher olfactory deposition fraction (ODF) of 23.58%, and a strong correlation between ODF and intracerebral drug delivery (R2 = 0.7755) was observed. Building upon this understanding, a borneol-modified lipid nanoparticle nasal spray (BLNP-NS) that combined both nasal deposition and mucosal absorption was designed for efficient nose-to-brain delivery. BLNP-NS exhibited an accelerated onset of action and enhanced brain targeting efficiency, which could be attributed to borneol modification facilitating the opening of tight junction channels. Furthermore, BLNP-NS showed superiority in a chronic migraine rat model. It not only provided rapid relief of migraine symptoms but also reversed neuroinflammation-induced hyperalgesia. The results revealed that borneol modification could induce the polarization of microglia, regulate the neuroinflammatory microenvironment, and repair the neuronal damage caused by neuroinflammation. This study highlights the impact of dispersion medium viscosity on the nose-to-brain delivery process of NDDS-NS and serves as a bridge between the formulation development and clinical transformation of NDDS-NS for the treatment of CNS diseases.
研究领域:
药学
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纳米技术
·
神经科学
·
药物递送系统
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药理学
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产品关联
DOI
PubMed
高影响因子
Foods
·
2025
·Vol. 14
·期 4
·682
·
IF 5.1
Huanyan Liang,Feifei Lv,Mengting Xian,Chenghua Luo,Lei Zhang,Meihua Yang,Qian Li,Xiangsheng Zhao
This investigation evaluates the comparative efficacy ofCinnamomum burmanniileaf essential oil (YXYO) and its main active ingredients as a novel preservative to protect stored food commodities from fungal infestations, aflatoxin B1(AFB1) contamination caused byAspergillus flavus. Morphological observations utilizing SEM and TEM revealed significant alterations in treated samples, alongside a decrease in ergosterol content and a dose-dependent disruption of the antioxidant system and energy system. Transcriptomic analysis suggested that differentially expressed genes were predominantly associated with spore growth, the cell wall, the cell membrane, oxidative stress, energy metabolism, and aflatoxin biosynthesis. Solid-phase microextraction–gas chromatography–mass spectrometry (SPME-GC-MS) identified ten active ingredients in YXYO, including borneol,α-terpineol, terpinen-4-ol, etc. Moreover, an effective inhibition ofA. flavusinfection in peanuts was observed with the application of 30 μL/disc of YXYO and a blend of its active compounds.
研究领域:
食品科学
·
微生物学
·
植物化学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）