EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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2025
·
IF 5.9
Guoliang Liu,Tao Zhang,Shunmeng Qian,Xiaoshuang Zhang,Hongxiang Lou,Peihong Fan
Mitochondria play a crucial role in cellular processes such as growth, differentiation, and energy conversion. Dysfunctional mitochondria have been implicated in Alzheimer's disease (AD), making mitochondrial improvement a promising therapeutic approach. SIRT3, a mitochondrial deacetylase, modulates mitochondrial function by deacetylating associated proteins. This study aimed to enhance the activity of honokiol, a natural SIRT3 modulator, and improve mitochondrial function for neuroprotective activity, using mitochondria targeting strategy. We synthesized mitochondrial targeting peptide conjugates using XJB as a carrier and found that honokiol conjugates exhibited lower toxicity and higher activity on neuronal injury models in vitro and i n vivo ( Zebrafish model) at lower concentrations compared to honokiol. The neuroprotective mechanism may involve the activation of cellular autophagy-related pathways, promotion of SIRT3 pathway activation, and up-regulation of mitochondrial fusion-associated protein Mfn-1 expression under damaged conditions. This study offers a promising approach for developing anti-Alzheimer's disease (AD) natural product derivatives based on SIRT3 regulation.
研究领域:
药理学
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神经科学
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生物化学
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DOI
PubMed
高影响因子
JOURNAL OF THE ELECTROCHEMICAL SOCIETY
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2025
·Vol. 172
·期 4
·047515
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IF 3.3
Jiajia Lu,Zhiyuan Zheng,Lina Liu,Ningxuan Liu,Yuanyuan You,Xiang Zhou,Ling Lu,Jia Tao,Shaobin Li,Zibin Song,Peng Zhao
Magnolol and honokiol are significant phenolic isomers derived from Magnolia officinalis and are considered promising candidates for potent anticancer drugs. A convenient and rapid method for the simultaneous analysis of magnolol and honokiol is essential for investigating their mechanisms of action and pharmacokinetics. In this study, we developed a composite electrode based on a copper-chelated porous coordination network (PCN-224(Cu)) and carbon nanotubes (CNT). Experimental results demonstrated that the PC-CNT/GCE exhibited a substantial redox potential difference (∼0.14 V) between magnolol and honokiol under differential pulse voltammetry. The modified electrode enabled the simultaneous detection of both compounds in a mixture, showing a linear increase in response current with detection limits (LOD = 3σ/s) of 2.65 μM for magnolol and 11.4 μM for honokiol. Additionally, the sensor exhibited sensitivities of 54.894 μA mM−1 for honokiol and 46.677 μA mM−1 for magnolol. These findings suggest that PCN-224(Cu)-based electrodes hold great potential for the efficient analysis of phenolic isomers in Magnolia officinalis. Furthermore, this study provides a foundation for new applications of porous coordination networks in electrochemical sensing.
研究领域:
分析化学
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药理学
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中药学
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产品关联
DOI
高影响因子
CHEMICAL ENGINEERING JOURNAL
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2021
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IF 13.273
Jingjing Meng,Pengfei Chen,Rui Yang,Linli Dai,Cheng Yao,Zheng Fang,Kai Guo
To produce renewable and functional epoxy resins, novel polymers were fabricated based on naturally available honokiol. The honokiol-derived (DBDBBB) epoxy resin monomer was firstly reported and cured by diamino diphenyl-sulfone (33DDS and 44DDS). The resultant networks were fabricated via both epoxy resin and polyolefin, and showed excellent thermal stability ( T max up to 451 °C), thermal conductivity (~0.743 W/m•K), and high specific heat (5.364 J/g•K) as well as the excellent dielectric constant and loss values (9.74, 0.026) (1 kHz, 25 °C). Moreover, the bio-based networks were low flammable. The high-performing DBDBBB/DDS networks surpass the DGEBA analogs, and hence it will be a promising candidate for DGEBA and has great potential application in the electronics and microelectronics industry.
研究领域:
材料科学
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化学工程
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产品关联
DOI
高影响因子
TOXICOLOGY AND APPLIED PHARMACOLOGY
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2025
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IF 3.4
Xuemin Xian,Xin Zhao,Xingchen Zhou,Hanfang Liu,Changxi Li,Xinquan Wu,Yuhang Chen,Keyue Ye,Hongwei Yang,Mingxi Li,Jianyun Yan,Xiuli Zhang
Vascular calcification (VC) is a common complication of chronic kidney disease (CKD), with oxidative stress identified as a key contributor to VC progression. Honokiol (HKL), a biphenolic compound derived from plants, has been found to be effective in treating various models of cardiovascular disease through the mitigation of oxidative stress. However, its effects on VC remain unexplored. To elucidate the effects of HKL on VC, a CKD rat model, a vitamin D 3 -overload-induced mouse model of vascular calcification, and a high-phosphate-induced human vascular smooth muscle cell (VSMC) calcification model were established. Calcification levels were assessed using Alizarin Red staining, calcium quantification, and Western blotting of osteogenic markers. Oxidative stress was assessed by measuring reactive oxygen species. Furthermore, transcriptome sequencing was employed to identify molecules and pathways affected by HKL. HKL was found to significantly reduce calcification in both in vivo and in vitro models. It also mitigated oxidative stress induced by high phosphate in human VSMCs. Mechanistically, HKL upregulated heme oxygenase-1 (HMOX-1), thereby inhibiting oxidative stress and reducing calcification. Pharmacological inhibition of HMOX-1 counteracted the protective effect of HKL on vascular calcification. In summary, the findings suggest that HKL ameliorates VC by upregulating HMOX-1 and decreasing oxidative stress.
研究领域:
医学
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药理学
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
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2021
·
IF 5.268
Hongyan Zhang,Ji Li,Rong Yuan,Yufen Li,Yue Zhang,Xiaoyun Hu,Jiqiang Qu,Yu Chen,Zheran Wang,Mingyu Xia,Dongkai Wang
Functionally-enabled delivery systems for aggressive lung metastases from breast cancer have been broadly examined, and the simultaneous inhibition of metastasis while fighting tumors persists as a provocative concern. We propose a valid strategy for delivering natural drugs-Honokiol (Hol) to achieve eradication of breast cancer cells and inhibition of pulmonary metastasis. A non-toxic degradable pH-sensitive polymer-PBAE for encapsulated Hol, and the outer layer was wrapped with Folate-DSPE-PEG 2000 (FA/PBAE/Hol-NPs), which have strengthened stability, prolonged in vivo circulation time and efficiently targets tumor sites. FA/PBAE/Hol-NPs displayed dampening the capability of migration and invasion, elevated 4T1 uptake and boosted apoptosis. What’s more, 4T1 breast cancer model mice exhibited marked anti-tumor (Inhibition rate of 62.8 %) and lung metastasis suppression (Inhibition rate of 84.3 %). In parallel, histological immunofluorescence and immunohistochemical assays demonstrate higher apoptosis levels and repression of matrix metalloproteinase expression in mice, all of which are instrumental in inhibiting lung metastasis. Taken together, FA/PBAE/Hol-NPs can as an efficacious intravenous drug delivery system for the curative treatment of metastatic breast cancer.
研究领域:
肿瘤学
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药剂学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
Particuology
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2025
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IF 4.3
Limei Zhang,Huatai Zhu,Peng Ye,Yuting Ren,Hongyu Wang,Jiandu Lei,Jing He
Combining drug delivery technologies with chemotherapeutic drugs is very attractive in terms of enhancing antitumor efficacy and reducing toxicity. Alginate microspheres stand out in the field of drug delivery due to their biocompatibility and high conversion rate. However, there are certain drawbacks in their preparation technology and further research is needed on how to prepare alginate microspheres with uniform particle size using high-viscosity sodium alginate solution. Therefore, this study proposed a novel microfluidic membrane emulsification technique for the preparation of alginate microspheres from high-viscosity sodium alginate solution. A tumor microenvironment-responsive colorectal cancer-targeted oral drug delivery system was constructed using a disulfide-bonded coupling of honokiol and doxorubicin as a model drug to achieve precise targeting, efficiency enhancement and toxicity reduction. The results showed that the prepared microspheres were relatively homogeneous in particle size. The in vitro model showed the high stability of the microspheres in the gastric acid environment and the colon-targeted release characteristic. And the system triggered the breakage of redox bonds and the precise release of the drug, showing good antitumor activity. This study contributes to the construction of drug delivery systems and the study of colon cancer treatment, which has a promising application.
研究领域:
药剂学
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肿瘤学
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生物医学工程
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产品关联
DOI
高影响因子
JOURNAL OF CHROMATOGRAPHY A
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2020
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IF 4.049
Jingwei Zhou,Yaoyao Hu,Peichun Chen,Hongwu Zhang
In the present study, a novel strategy based on unidirectional freezing and atom transfer radical polymerization combined with activator regenerated by electron transfer (ARGET-ATRP) was applied to synthesizing orderly macroporous monolithic column with restricted-access (RA) property in a 1000μL pipette tip. The RA column was composed of hydrophobic inner column (poly(styrene- co -ethylene glycol dimethacrylate) and hydrophilic outer layer (poly-hydroxyethyl methacrylate chain) which was grafted on the hydrophobic surface by means of the second ARGET-ATRP reaction. The as-prepared RA monolithic tip was connected to a 2mL syringe for directly extracting magnolol and honokiol from rat plasma just by manually pushing operation. The surface morphology and chemical composition of the column were characterized by scanning electronic microscope, infrared spectroscopy and X-ray photoelectron spectroscopy respectively. The determined results of evaluation experiments based on the optimized solid phase extraction conditions showed that the RA column possessed good protein exclusion power, extraction recovery and reusability. The constructed RA-SPE-HPLC/UV method for simultaneously analyzing magnolol and honokiol in rat plasma was validated with quality control (QC) samples at four concentration levels. Good precision (RSDs, 3.39~11.16%) and acceptable accuracy (relative recoveries, 89.52%~108.42%) were obtained for intra- and inter-day assays. The determined results of real rat plasma as well as the standard-addition samples demonstrated the developed method with good accuracy and precision. It can be extrapolated from the experimental results that this simple and cost-efficient RA-SPE method is also suitable for directly extracting other hydrophobic constituents in biological body fluid for therapeutic drug monitoring or pharmacokinetic study.
研究领域:
分析化学
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药物分析
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF NANOPARTICLE RESEARCH
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2021
·Vol. 23
·期 5
·1-14
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IF 2.253
Zhu Li,Song Zhimei,Feng Sijia,Xu Hongmei,Chen Shiyu,Feng Runliang
In the study, biotin-modified oligochitosan-F127 conjugate (F127-CS-BIO) was synthesized as a carrier to prepare honokiol-loaded micelles via dialysis method. The encapsulation efficiency and drug loading were 70.79 ± 2.70% and 9.70 ± 0.57%, respectively. The mean particle size and zeta potentials were 210.9 ± 4.65 nm and 12.9 ± 7.22 mV, respectively. In vitro release studies showed that the release of honokiol from the micelles was slow and steady. MTT evaluation and cellular uptake results demonstrated that F127-CS-BIO was more easily absorbed by tumor cells and resulted in low IC 50 value of honokiol due to biotin’s targeting guidance when compared with biotin-unmodified F127-CS. In conclusion, F127-CS-BIO polymer was expected as an effective nanocarrier to encapsulate chemotherapeutic drugs. Graphical abstract
研究领域:
药剂学
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纳米医学
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肿瘤学
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产品关联
DOI
高影响因子
JOURNAL OF NANOPARTICLE RESEARCH
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2018
·Vol. 20
·期 10
·1-11
·
IF 2.127
Feng Runliang,Deng Peizong,Zhou Feilong,Feng Sijia,Song Zhimei
To overcome honokiol’s poor water solubility and investigate its antifungal activity and pharmacokinetic property, Pluronic® F-127 (F127)-cyclodextrin conjugate was synthesized and employed to prepare honokiol-loaded micelles through emulsion-solvent evaporation method. The drug-loaded micelles were obtained with 92.30 ± 3.28% of encapsulation efficiency being higher than that obtained from F127 due to additional cyclodextrin inclusion. Fourier transformation infrared spectrometry and diffraction scanning calorimetry analysis tests demonstrated that honokiol was successfully encapsulated into the conjugate micelles in the amorphous or solid solution state because of their interactions. Meanwhile, in vitro antifungal activity experiment indicated that the MIC 90 of drug-loaded micelles was 64 μg/mL, showing the same antifungal activity as pure honokiol although it obviously retarded honokiol’s release. In vivo pharmacokinetic results confirmed that in vivo area under curve and apparent distribution volume of honokiol in drug-loaded micelles were 2- and 1.69-folds higher than that for pure honokiol, with its obvious prolonged mean retention time and half-life period, respectively. The clearance rate of honokiol was also shortened about 2-fold in comparison with pure honokiol when encapsulated into the micelles. These results suggest that the developed F127-cyclodextrin micellar formulation is a promising drug delivery system for antifungal drugs.
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研究领域:
药剂学
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生物医学
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药物递送系统
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产品关联
DOI
高影响因子
Biomaterials Advances
·
2025
·
IF 6
Zhen Lin,Ruyu Cao,Fan Nie,Lingling Ma,Jing Xu,Yuanqiang Guo
Traditional therapies are inadequate in addressing the escalating threat of cancer, highlighting the urgent need for more effective treatment modalities. Natural products play a crucial role in the development of novel anticancer pharmaceuticals and safe anti-tumor nanomedicines. Honokiol (HK), a naturally occurring compound, has been shown to induce apoptosis in cancer cells and inhibit tumor proliferation, positioning it as a promising candidate for chemotherapeutic applications. While, plant-derived polysaccharides are known to activate anti-tumor immune responses and exhibit favorable properties such as biocompatibility, safety, and modifiability, making them suitable carriers for drug delivery. In this study, golden berries (the fruits of Physalis peruviana ) polysaccharides (PPP), which exhibit immune-stimulating properties, were integrated with the crosslinking agent benzene-1,4-diboronic acid (BDBA) to develop pH-responsive nanoparticles (HK@PPP-BDBA) for synergistic chemo-immunotherapy. We conducted a comprehensive chemical characterization of the nanoparticles and investigated the molecular mechanisms underlying the assembly of HK and polysaccharides through computational simulations. The HK@PPP-BDBA demonstrated significant inhibitory effects on the proliferation of MCF-7 and HeLa cells, reduced tumor growth, and impeded cancer cell migration in vivo . HK promoted the production of reactive oxygen species (ROS) and apoptosis in tumor cells, while PPP facilitated the maturation of dendritic cells, enhanced the expression of costimulatory molecules and histocompatibility complex, and initiated anti-tumor immunity. The advancement of HK@PPP-BDBA expands the potential applications of natural polysaccharides and nanoparticles in cancer treatment, offering a promising platform for the integration of chemotherapy and immunotherapy.
研究领域:
肿瘤学
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药剂学
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生物材料学
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产品关联
DOI
PubMed
高影响因子
Scientific Reports
·
2015
·
IF 5.578
Caiao Guo,Liang Ma,Yudan Zhao,Anlin Peng,Biao Cheng,Qiaoqiao Zhou,Ling Zheng,Kun Huang
Amyloid formation is associated with multiple amyloidosis diseases. Human calcitonin (hCT) is a typical amyloidogenic peptide, its aggregation is associated with medullary carcinoma of the thyroid (MTC), and also limits its clinical application. Magnolia officinalis is a traditional Chinese herbal medicine; its two major polyphenol components, magnolol (Mag) and honokiol (Hon), have displayed multiple functions. Polyphenols like flavonoids and their derivatives have been extensively studied as amyloid inhibitors. However, the anti-amyloidogenic property of a biphenyl backbone containing polyphenols such as Mag and Hon has not been reported. In this study, these two compounds were tested for their effects on hCT aggregation. We found that Mag and Hon both inhibited the amyloid formation of hCT, whereas Mag showed a stronger inhibitory effect; moreover, they both dose-dependently disassembled preformed hCT aggregates. Further immuno-dot blot and dynamic light scattering studies suggested Mag and Hon suppressed the aggregation of hCT both at the oligomerization and the fibrillation stages, while MTT-based and dye-leakage assays demonstrated that Mag and Hon effectively reduced cytotoxicity caused by hCT aggregates. Furthermore, isothermal titration calorimetry indicated Mag and Hon both interact with hCT. Together, our study suggested a potential anti-amyloidogenic property of these two compounds and their structure related derivatives.
研究领域:
药理学
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生物化学
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分子生物学
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中医药
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产品关联
DOI
PubMed
高影响因子
Drug Design Development and Therapy
·
2015
·
IF 3.028
Jing Sun,Xueqi Fu,Ye Liu,Yongsen Wang,Bo Huo,Yidi Guo,Xuefeng Gao,Wannan Li,Xin Hu
Background Honokiol is one of the main bioactive constituents of the traditional Chinese herbal drug Magnolia bark (Cortex Magnoliae officinalis , Hou Po). The aim of this study was to probe its anti-type 2 diabetes mellitus effects and the underlying mechanism. Methods Type 2 diabetic mouse model was established by intraperitoneally injecting with streptozotocin. Fasting blood glucose, body weight, and lipid profile were measured. The subcutaneous adipose tissue, skeletal muscle, and liver were isolated as well as homogenized. The phospho-insulin receptor β-subunit (IRβ), IRβ, phospho-AKT, AKT, phospho-ERK1/2, ERK1/2, phosphotyrosine, and actin were examined by Western blot assay. Cell viability or cytotoxicity was analyzed by using MTT method. The inhibitory potencies of honokiol on the protein tyrosine phosphatase 1B (PTP1B) activity were performed in reaction buffer. Molecular docking and dynamic simulation were also analyzed. Results In in vivo studies, oral treatment with 200 mg/kg honokiol for 8 weeks significantly decreases the fasting blood glucose in type 2 diabetes mellitus mice. The phosphorylations of the IRβ and the downstream insulin signaling factors including AKT and ERK1/2 significantly increase in adipose, skeletal muscle, and liver tissue of the honokiol-treated mice. Moreover, honokiol enhanced the insulin-stimulated phosphorylations of IRβ, AKT, and ERK1/2 in a dose-dependent manner in C2C12 myotube cells. Meanwhile, honokiol enhanced insulin-stimulated GLUT4 translocation. Importantly, honokiol exhibited reversible competitive inhibitory activity against PTP1B with good selectivity in vitro and in vivo. Furthermore, using molecular docking and dynamic simulation approaches, we determined the potential binding mode of honokiol to PTP1B at an atomic level. Conclusion These findings indicated the hypoglycemic effects of honokiol and its mechanism that honokiol improved the insulin sensitivity by targeting PTP1B. Therefore, our study may highlight honokiol as a promising insulin sensitizer for the therapy of type 2 diabetes.
研究领域:
药理学
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内分泌学
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分子生物学
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糖尿病研究
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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）