BRAIN RESEARCH
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2023
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IF 2.9
Fankai Gao,Rui Chen,Shuo Li,An Li,Bo Bai,Rulin Mi,Guofang Xue
Neuroinflammation plays a crucial role in the development of epilepsy, and suppressing neuroinflammation can delay epileptogenesis. Recent reports have demonstrated that (+)-borneol has neuroprotective effects in several brain disorders by reducing neuroinflammation. However, its effects on epilepsy have not been reported. In this research, we first studied the effect of different doses of (+)-borneol (3, 6, and 12 mg/kg) on neuroinflammation in a pilocarpine model of epileptogenesis by detecting IL-1β, TNF-α, and COX-2 expression. We demonstrated that different doses of (+)-borneol decreased IL-1β, TNF-α, and COX-2 levels, with 12 mg/kg having the most substantial effect. Furthermore, we examined the effects of 12 mg/kg (+)-borneol on neuronal damage, glial cell activation, and apoptosis in the hippocampus at different time points (1, 3, and 7 days) after SE . We found that (+)-borneol significantly ameliorated neuronal injury, decreased glial cell activation, and attenuated apoptosis. We also found that (+)-borneol inhibited the NF-κB pathway activation induced by SE. In conclusion, our results indicated that (+)-borneol reduces neuroinflammation by inhibiting the NF-κB pathway activation, exerts neuroprotective effects, and may have an inhibitory effect in epileptogenesis.
研究领域:
神经科学
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药理学
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神经炎症
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癫痫
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2023
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IF 5.8
Shangmin Yu,Xinying Wang,Linlin Lv,Tongyan Liu,Qingxiang Guan
Depression is a chronic mental disorder which threatens human health and lives. However, the treatment of depression remains challenging largely due to blood brain barrier (BBB), which restricts drugs from entering the brain, resulting in a poor distribution of antidepressants in the brain. In this work, a novel brain-targeted drug delivery system was developed based on borneol-modified PEGylated graphene oxide (GO-PEG-BO). GO-PEG-BO was characterized and proved to possess excellent biocompatibility . By incorporating borneol , GO-PEG-BO could penetrate BBB efficiently by opening tight junctions and inhibiting the efflux system of BBB. The targeted distribution of GO-PEG-BO in the brain was observed by an in vivo biodistribution study. Moreover, GO-PEG-BO exhibited a neuroprotective effect, which is beneficial to the treatment of depression. Ginsenoside Rg1 (GRg1), which can relieve depressive symptoms but difficult to cross BBB, was loaded to GO-PEG-BO for the therapy of depression. In depressive rats, GRg1/GO-PEG-BO improved stress-induced anhedonia, despair and anxiety, and comprehensively relieved the depressive symptoms. In conclusion, GO-PEG-BO could serve as a promising nanocarrier for brain-targeted drug delivery, and provide a new strategy for the therapy of depression.
研究领域:
药学
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纳米技术
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神经科学
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药物递送系统
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DOI
PubMed
高影响因子
MATERIALS & DESIGN
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2026
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IF 8.2
Yue Peng,Cuiman Tang,Mingcong Niu,Tianyi Xu,QingYu Meng,Xinran Li,Rongheng Ma,Huimin Yu
A traditional medicine-inspired strategy provides a logical framework for constructing carrier-free hybrids. • Precise structural modifications successfully circumvent the inherent bioaccessibility limitations of natural products. • The covalent integration of diverse functional modules enables synergistic therapeutic efficacy against arthritis. • The therapeutic action is closely associated with the modulation of protein kinase B and hypoxia-inducible factor signaling. Curcumin (Cur) possesses potent anti-inflammatory activity but faces clinical challenges due to poor aqueous dispersibility, insufficient membrane affinity, and low bioavailability. Borneol (Bor), a classic “envoy” component in Traditional Chinese Medicine (TCM), exhibits prominent membrane-penetrating properties. Inspired by the “monarch-envoy” compatibility theory, we rationally designed carrier-free hybrids by covalently conjugating Cur (“monarch”) with Bor (“envoy”). Systematic characterization confirmed the successful synthesis and controllable optimization of key properties, including enhanced dispersibility, improved cellular uptake, and favorable biocompatibility. Using rheumatoid arthritis (RA) as a disease model, we identified SCBMS as the optimal formulation owing to its superior dispersibility and uptake, which directly translated into the most potent anti-RA efficacy. The hybrids exerted synergistic multifunctional effects—including robust anti-inflammatory and antioxidant activities—effectively reducing the arthritis index and ameliorating synovial hyperplasia and joint destruction in vivo . Mechanistically, our results indicate a close correlation between the therapeutic effects and the downregulation of the AKT/mTOR/HIF-1α signaling pathway, supporting the involvement of this pathway in the observed anti-RA activity. This study provides a generalizable framework for developing functional hybrids guided by TCM principles and validates their translational potential. Download: Download high-res image (152KB) Download: Download full-size image
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DOI
高影响因子
JOURNAL OF NATURAL PRODUCTS
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2026
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IF 3.7
Yuling Zeng,Jing Nie,Haiyan Lan,Yichao Zhang,Yufang Dai,Xiaojie Cao,Liang Zhang,Jianjian Hu
Camphor is a key quality determinant of lavender oil. Bornyl dehydrogenase (BDH) catalyzes the final camphor biosynthesis step, yet its gene family and mechanism in lavender remain uncharacterized. We phylogenetically classified 154 short-chain dehydrogenase/reductase (SDR) genes into six clades and screened 17 BDH genes. Integrated transcriptomic and metabolomic analyses revealed that camphor biosynthesis primarily occurs via the plastidic 2-C-methyl-D-erythritol 4-phosphate (MEP) pathway, with coordinated expression of geranyl diphosphate synthase (GPPS), bornyl diphosphate synthases (BPPS), bornyl-diphosphate diphosphatase (BDD), and BDH genes. Most biosynthetic genes, especially BDH and BPPS, were significantly upregulated in L. × intermedia “Xinxun 4”, correlating with its highest camphor content. Subcellular localization showed BDH1 resides in the cytoplasm, suggesting plastid-cytoplasm collaboration. In vitro assays demonstrated that BDH1 and BDH2 both oxidize (+)- and (−)-borneol to camphor. Molecular dynamics simulations revealed that BDH1’s active site exhibits conformational flexibility, accommodating both enantiomers with similar binding affinities, which was confirmed by enzyme kinetics. Asn90 was identified as a key catalytic residue. These findings reveal BDH family expansion, coordinated gene expression driving camphor accumulation, and BDH1’s catalytic flexibility, offering key genetic resources and mechanistic insights for optimizing lavender camphor content via metabolic engineering and molecular breeding.
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DOI
PubMed
高影响因子
CATALYSIS TODAY
·
2025
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IF 5.3
Yaoyi Hu,Xiqiang Yuan,Zhengquan Zhang,Yu Zhang,Han Ma,Yunfei He,Shaoyun Shan,Tianding Hu
Natural borneol has enormous medicinal value (like clearing heat, detoxifying, relieving pain, and other effects) but has a low yield and high price. Compared with the natural extraction method to obtain borneol, a synthetic method has significant advantages such as high yield, environmental protection, and high economic benefits. In the synthesis method, the catalyst is the most key factor. In this study, two catalysts (SO 4 2- /ZrO 2 -TiO 2 and Al 2 (SO 4 ) 3 /ZrO 2 -TiO 2 ) with high catalytic performance and high positive selectivity were synthesized by impregnation method to synthesize borneol from α-pinene. The optimum synthesis conditions of SO 4 2- /ZrO 2 -TiO 2 were as follows: n(Zr): n(Ti) = 3: 1, sulfuric acid concentration 2 mol/L, calcination temperature 550 °C, the yield of borneol was 68.14 %. Based on the preparation of catalyst SO 4 2- /ZrO 2 -TiO 2 , the optimum synthesis conditions of Al 2 (SO 4 ) 3 /ZrO 2 -TiO 2 were as follows: the concentration of aluminum sulfate was 0.4 mol/L, the calcination temperature was 600 °C, and the yield of borneol was 74.58%, Compared with the highest yield of 59.89% reported in the existing literature, the performance is improved by 13.96%. In addition, the mechanism of the esterification and saponification reaction of borneol has been in the blank stage. We used the density functional theory (DFT) to explore the reaction mechanism.
研究领域:
有机化学
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催化化学
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药物化学
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产品关联
DOI
高影响因子
ACS Applied Materials & Interfaces
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2024
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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
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药理学
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纳米医学
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产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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2024
·
IF 6
Zheren Tong,Xiaolu Jie,Ziwei Chen,Mingtao Deng,Xin Li,Zhiwen Zhang,Faxiang Pu,Zhangfu Xie,Zijin Xu,Ping Wang
Crocetin (CCT), a natural bioactive compound extracted and purified from the traditional Chinese medicinal herb saffron, has been shown to play a role in neurodegenerative diseases , particularly depression. However, due to challenges with solubility, targeting, and bioavailability, formulation development and clinical use of CCT are severely limited. In this study, we used the emulsification-reverse volatilization method to prepare CCT-loaded nanoliposomes (CN). We further developed a borneol (Bor) and lactoferrin (Lf) dual-modified CCT-loaded nanoliposome (BLCN) for brain-targeted delivery of CCT. The results of transmission electron microscope (TEM) and particle size analysis indicated that the size of BLCN (∼140 nm) was suitable for transcellular transport across olfactory axons (∼200 nm), potentially paving a direct path to the brain. Studies on lipid solubility, micropolarity, and hydrophobicity showed that BLCN had a relatively high Lf grafting rate (81.11 ± 1.33 %) and CCT entrapment efficiency (83.60 ± 1.04 %) compared to other liposomes , likely due to Bor improving the lipid solubility of Lf, and the combination promoting the orderly arrangement of liposome membrane molecules. Microplate reader and fluorescence microscopy analysis showed that BLCN efficiently promoted the endocytosis of fluorescent coumarin 6 into HT22 cells with a maximal fluorescence intensity of (13.48 ± 0.80 %), which was significantly higher than that of CCT (5.73 ± 1.17 %) and CN (12.13 ± 1.01 %). BLCN also exhibited sustained function, remaining effective for more than 12 h after reaching a peak at 1 h in cells, while CN showed a significant decrease after 4 h. The uptake mechanisms of BLCN in HT22 cells mainly involve energy-dependent, caveolae-mediated, and microtubule-mediated endocytosis, as well as micropinocytosis. Furthermore, BLCN displayed a significant neuroprotective effect on HT22 cells in glutamate-, corticosterone-, and H 2 O 2 -induced models. Tissue fluorescence image analysis of mice showed that BLCN exhibited substantial retention of fluorescent DiR in the brain after nasal administration for 12 h. These findings suggest that CCT has the potential for cellular uptake, neuroprotection , and targeted delivery to the brain following intranasal administration when encapsulated in Bor and Lf dual-modified nanoliposomes.
研究领域:
药学
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神经科学
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药物递送系统
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生物技术
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DOI
PubMed
高影响因子
ACS Nano
·
2024
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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
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神经科学
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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
FOOD MICROBIOLOGY
·
2024
·
IF 4.5
Zhenlong Zhou,Ruoxin Chen,Pengzhen Li,Penghui Fan,Lin Ma,Xinyu Cai,Yuchao Hou,Binbin Li,Jianyu Su
Photodynamic inactivation (PDI), a non-thermal sterilization method, has attracted considerable attention due to its broad-spectrum antimicrobial activity, environmental friendliness and cost-effectiveness. Curcumin (Cur), a food-grade photosensitizer, exhibits photodynamic antimicrobial activity based primarily on its efficiency in intracellular accumulation. However, Cur's low water solubility and the barriers presented by the outer membrane of Gram-negative bacteria challenge its ability to penetrate the cytoplasm. Natural borneol (NB), a monoterpene food flavoring agent, has also been shown to improve the efficiency of drug absorption. In this study, we demonstrated that NB significantly improved the cellular uptake of Cur, thereby enhancing its photodynamic bactericidal activity against Gram-negative Escherichia coli ( E. coli ) ATCC 8739, a potential alternative to enterohemorrhagic E. coli O157:H7. This effect was attributed to NB's ability to disrupt the integrity of the E. coli bacterial membrane, thereby increasing cellular permeability. Transcriptomic analysis further confirmed that NB dysregulated the expression of genes associated with bacterial membrane structure and function in E. coli . Consequently, the increased accumulation of Cur in E. coli led to excessive production of intracellular reactive oxygen species (ROS) upon exposure to 6.5 J/cm 2 blue light (BL). These ROS, analyzed biochemically and transcriptionally, primarily disrupted bacterial membrane structure and function, the antioxidant system, and ultimately caused bacterial death. Remarkably, this combined strategy not only reduced E. coli contamination in the tested orange juice, but also preserved its nutritional quality. In conclusion, this research provides an innovative and effective approach to maintaining food safety.
研究领域:
微生物学
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食品科学
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药学
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生物技术
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产品关联
DOI
PubMed
高影响因子
International Journal of Nanomedicine
·
2018
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IF 4.37
Hui Song,Man Wei,Nan Zhang,He Li,Xiaochuan Tan,Yujia Zhang,Wensheng Zheng
Introduction The incidence of central nervous system disease has increased in recent years. However, the transportation of drug is restricted by the blood–brain barrier, contributing to the poor therapeutic effect in the brain. Therefore, the development of a new brain-targeting drug delivery system has become the hotspot of pharmacy.Materials and methods Borneol, a simple bicyclic monoterpene extracted from Dryobalanops aromatica, can direct drugs to the upper body parts according to the theory of traditional Chinese medicine. Dioleoyl phosphoethanolamine (DOPE) was chemically modified by borneol as one of the lipid materials of solid lipid nanoparticle (SLN) in the present study.Results The borneol-modified chemically solid lipid nanoparticle (BO-SLN/CM), borneol-modified physically solid lipid nanoparticle (BO-SLN/PM), and SLN have similar diameter (of about 87 nm) and morphological characteristics. However, BO-SLN/CM has a lower cytotoxicity, higher cell uptake, and better blood–brain barrier permeability compared with BO-SLN/PM and SLN. BO-SLN/CM has a remarkable targeting function to the brain, while BO-SLN/ PM and SLNs are concentrated at the lung.Conclusion The present study provides an excellent drug delivery carrier, BO-SLN/CM, having the application potential of targeting to the brain and permeating to the blood–brain barrier.
研究领域:
药学
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神经科学
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产品关联
DOI
PubMed
高影响因子
Journal of Environmental Chemical Engineering
·
2025
·
IF 7.2
Xiaobing Ma,Xiangbin Sun,Yuanyuan Xie,Rongmin Wang,Yaping Zhang,Yufeng He,Pengfei Song
A series of borneol quaternary ammonium copolymer P(BO-StB) was synthesized through emulsion polymerization and characterized using 1H NMR, FT-IR, and scanning electron microscopy (SEM). Characterization results demonstrated that P(BO-StB) copolymers exhibited a favorable microscopic morphology, accompanied by excellent hydrophilicity (minimum water contact angle, θₘᵢₙ = 25.6 ± 3.7°) and a high surface zeta potential (maximum ζ potential, ζₘₐₓ = 31.1 ± 1.4 mV). Among the copolymer series, the optimal P(BO-StB) sample displayed the strongest antibacterial potency: it achieved an antibacterial rate of 99.9% against E. coli and 99.2% against S. aureus , with a minimum inhibitory concentration (MIC) of 6 mg/mL for E. coli and 3 mg/mL for S. aureus. In addition, P(BO-StB) also showed a statistically significant antibiofilm effect (P < 0.001). A proposed mechanism is that the electrostatic interaction between the cation and the bacteria facilitates the permeation of borneol into the cell membrane; furthermore, the stereochemical structure of borneol hinders bacterial adherence. Importantly, the use of polymers in coatings also fully leverages their antimicrobial benefits, offering novel alternatives for the development of antibacterial coatings.
研究领域:
高分子科学
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抗菌材料
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表面涂层
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生物医学工程
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杀菌技术
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2025
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IF 5.2
Shulin Shen,Yanyan Zheng,Yueyue Xie,Xinzi You,Xuechao Chen,Binghui Xie,Jiaqi Weng,Qingqing Huo,Yunxiang Zhang,Meselhy R. Meselhy Zayed,Qinying Yan
Microneedle technology has emerged as a promising transdermal platform for transdermal delivery of Alzheimer’s disease therapeutics. However, conventional passive diffusion approaches face fundamental limitations in overcoming both skin and blood–brain barriers. To address these limitations, we developed a rocket-inspired gas-propelled microneedle system integrating nanostructured lipid carriers for enhanced dual-barrier penetration. The study combined fluid vortex generation with blood–brain barrier endothelial remodeling to achieve efficient drug delivery. Specifically, the system featured a hierarchical cavity design with borneol-modified huperzine A-loaded nanostructured lipid carriers (NLCs) (particle size: 89.6 ± 0.7 nm; zeta potential: –22.5 ± 0.5 mV; Hup A encapsulation efficiency: 83.40 ± 1.51 %; drug loading capacity: 2.63 ± 0.06 %) in primary cavities and a spatially isolated pneumatic initiator (ascorbic acid/sodium bicarbonate) in secondary cavities. Through multiphysics simulation coupled fluid dynamics with chemical reaction kinetics and mass transport phenomena, which revealed that acid-base reactions generate CO 2 microbubbles capable of producing rapid thrust forces. This microbubble-mediated propulsion mechanism achieved a 50 % increase in penetration depth (up to ∼ 1428 µm) relative to conventional microneedle platforms. Remarkably, this innovative hierarchical cavity design achieved a high drug loading capacity of 182 μg/array while preserving spatial isolation between the reactants and therapeutic payload. In vivo studies validated efficient brain delivery, as evidenced by a marked increase (p < 0.001) in cortical acetylcholine concentrations and amelioration of scopolamine-induced spatial memory impairments in rat models. This work established a preclinical proof-of-concept for the enhanced brain delivery of therapeutics in neurodegenerative disease through the synergistic integration of gas-propulsion physics and advanced nanocarrier engineering, offering new possibilities for overcoming biological delivery barriers.
研究领域:
药物递送系统
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神经药剂学
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生物医学工程
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纳米医学
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转化医学
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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）