MATERIALS & DESIGN
·
2023
·
IF 8.4
Dongshi Liang,Meiqian Yu,Shuaishuai Huang,Jinglin Wang,Zijin Xu,Daai Li,Zhongyu Li,Huamin Wang
Magnolol shows promise as an effective anti-tumor therapeutic agent. Nevertheless, the clinical application of this agent is constrained by its inherent water insolubility and diminished stability. In the present investigation, we have developed a new approach to address these limitations by creating an acid-responsive amphiphilic polymeric prodrug (PMag) that contains acetal bonds and magnolol, and can self-assemble into polymeric micelles (PMag-Ms) in aqueous solutions. We conducted in vitro release studies and observed that the micelles rapidly released magnolol at an acidic pH of 5.0, but only released minimal amounts of magnolol at a neutral pH of 7.4. In vitro investigations performed on gastric cancer cells elucidated that PMag-Ms selectively induced cell apoptosis and G1 phase cell cycle arrest, exhibiting higher efficacy than magnolol alone. Furthermore, in vivo studies confirmed that PMag-Ms exhibited superior inhibition of tumor growth, favorable biocompatibility with organs, increased accumulation in tumor tissues, and enhanced targeting efficiency compared to magnolol. Pharmacokinetic analysis also revealed that PMag-Ms had a longer half-life and extended duration of action in vivo . These results highlight the potential of the synthesized acid-degradable PMag-Ms as a promising therapeutic option for gastric cancer.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2022
·
IF 6.51
Yanzhi Wang,Cancan Sun,Leaf Huang,Mengqian Liu,Lu Li,Xiping Wang,Linchao Wang,Shanshan Sun,Haiwei Xu,Gege Ma,Lei Zhang,Jiaxin Zheng,Hongmin Liu
The potential of combination therapy using nanoparticle delivery systems in improving triple-negative breast cancer treatment efficacy remains to be explored. Here, we report a novel nanoparticle system using a cholesterol biguanide conjugate hydrochloride (CBH) as both a drug and carrier to load magnolol (MAG). Poly(ethylene glycol)-poly(lactic-co-glycolic acid) (mPEG-PLGA) and aminoethyl anisamide-poly(ethylene glycol)-poly(lactic-co-glycolic acid) (AEAA-PEG-PLGA) were added to form nanoparticles. Nanoparticles accumulated most in tumor tissues when the weight ratio of AEAA-PEG-PLGA to mPEG-PLGA was 4:1. MAG and CBH exerted a synergistic inhibitory effect on 4 T1 cells. An in vitro study showed that nanoparticles displayed the highest tumor cell uptake rate, highest apoptosis rate, and strongest inhibitory effect on tumor cell migration and monoclonal formation. CBH might promote nanoparticle uptake by cells and lysosomal escape. After intravenous administration to mice with 4 T1 breast tumors in situ , the nanoparticles inhibited tumor growth without obvious toxicity. Western blot results showed that nanoparticles altered the levels of p53, p-AKT, and p-AMPK in the tumor tissue. Moreover, cell apoptosis was found in the same area of H&E-stained and TUNEL-stained tumors treated with the nanoparticles. Collectively, this nanoparticle system provides a novel combination drug delivery strategy for treating triple-negative breast cancer.
研究领域:
肿瘤学
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药学
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纳米技术
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癌症治疗
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PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2024
·
IF 4.5
Yangfan Zheng,Jiali Deng,Lewei Li,Jing Cao,QinYan Xie,Yangfen Fu
Malignant neoplasms, which are related closely to epithelial-mesenchymal transition (EMT) pathway, are one of the greatest risks threatening human health today. Magnolol (MAG), a traditional Chinese herbal extract, which has been proved to inhibit EMT pathway of solid tumors in previous studies. In this study, we first verified that MAG reduced metastasis and enhanced chemosensitivity to doxorubicin (DOX) in A549 cells, a non-small cell lung cancer (NSCLC) cell. An adenosine monophosphate (AMP) modified nanomicelles (APD@MAG NMs) was further prepared using the appropriate feeding ratio, loading with synergistic DOX and MAG. APD@MAG NMs with high positive charged surface reduced drug release of negative charged MAG, and achieved continuous cellular uptake. APD@MAG NMs significantly reduced the cell viability and enhanced the cell apoptosis of A549 cells. Moreover, the APD@MAG NMs significantly inhibited the mRNA levels and the protein expression of EMT related pathway. Overall, these APD@MAG NMs provide an effective therapeutic strategy for clinical chemo-therapy in NSCLC.
研究领域:
肿瘤学
·
药剂学
·
分子生物学
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COMPOSITES PART B-ENGINEERING
·
2022
·
IF 11.322
Wenwen Guo,Fuwei Liang,Shun Chen,Kejing Yu,Jie Sun,Zengyuan Pang,Bin Fei
In this study, a phosphorus-containing bio-based monomer (MBDPP) was first synthesized from renewable magnolol, and subsequently photo-cured with tri-thiol (TPTMP) or tetra-thiol (PETMP) monomers via thiol–ene polymerization. The synthesized MBDPP/TPTMP and MBDPP/PETMP membranes exhibited high char residues at 700 °C in the TGA tests, which were 19.8 wt% and 24.2 wt% for nitrogen while 16.5 wt% and 20.2 wt% for air, respectively, indicating superior charring capacity of both membranes. DMA results indicated that both the higher stiffness and the T g of the cured MBDPP/PETMP membrane was ascribed to its higher cross-linking density than that of the cured MBDPP/TPTMP owing to the tetra-functional groups of PETMP. In the open flame test, both MBDPP/TPTMP and MBDPP/PETMP membranes self-extinguished immediately when removing the flame source, manifesting excellent intrinsic anti-flammability. The cone calorimeter results further demonstrated that MBDPP/TPTMP and MBDPP/PETMP membranes showed lower PHRR (419 and 388 kW/m 2 , respectively) and THR (41.38 and 38.98 MJ/m 2 , respectively) values than most of the thiol-ene photo-polymerized counterparts previously reported. The excellent anti-flammability of MBDPP/TPTMP and MBDPP/PETMP membranes originated from the formation of expandable char residues that played an efficient role in hampering the transfer of flammable pyrolysis products to flame zone as well as insulating the heat irradiation during combustion. Additionally, both MBDPP/TPTMP and MBDPP/PETMP membranes showed excellent transparency (transmittance >85% in the visible region) and flexibility (breaking elongation around 40%). Taking the intrinsic anti-flammability, exceptional transparency and high flexibility into account, the MBDPP/TPTMP and MBDPP/PETMP systems are suitable as intumescent flame retardant coating materials .
研究领域:
材料科学
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化学工程
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高影响因子
Foods
·
2023
·Vol. 12
·期 6
·1149
·
IF 5.2
Feixu Mo,Wenzhi Li,Youhua Long,Rongyu Li,Yi Ding,Ming Li
Magnolol is a natural compound extracted from the traditional Chinese medicineMagnolia officinalis, which exhibits antimicrobial properties. However, magnolol is insoluble in water and consists of a phenolic hydroxyl group, which is volatile; these factors hinder its application. In this study, a safe and environmentally friendly method to improve the microbial resistance and storability of harvested fruits is developed using the water-soluble carrier carboxymethyl chitosan (CMCS) and magnolol. Magnolol was loaded on CMCS particles to form[email protected]antimicrobial particles, a preservation coating agent.[email protected]particles effectively solved the problems of water insolubility and agglomeration of magnolol and reduced the size distribution D50 value of magnolol from 0.749 to 0.213 μm.[email protected]particles showed greater toxicity againstStaphylococcus aureus,Escherichia coli, andBotryosphaeria dothideathan that of magnolol alone, with effective medium concentration (EC50) values of 0.9408, 142.4144, and 8.8028 μg/mL, respectively. Kiwifruit treated with the[email protected]solution showed delayed changes in fruit hardness and soluble solid and dry matter contents and significantly higher ascorbic acid (vitamin C) and soluble total sugar contents and sugar:acid ratios compared with that of the control fruit. In addition, no disease spots were observed on fruit treated with the[email protected]solution within 7 days after inoculation withB. dothidea. In conclusion,[email protected]particles showed antimicrobial activity on harvested fruits, effectively delayed the hardness and nutritional changes of fruits during storage, and improved the storability of kiwifruit.Keywords:[email protected]particles;foodborne pathogen;preservation coating agent;Staphylococcus aureus;kiwifruit
研究领域:
食品科学
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微生物学
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农业科学
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药学
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PubMed
高影响因子
FOOD RESEARCH INTERNATIONAL
·
2025
·
IF 8
Fangyuan Wei,Caihong Shi,Hongyue Wang,Wanxuan Li,Xindi Zhang,Xiangrong Zhang
Sodium carboxymethyl cellulose (CMC)-based films integrated with zein and magnolol complexes were prepared for food packaging with antimicrobial and antioxidant properties. The results showed that the secondary structure of zein changed upon complexation with magnolol. The scavenging ability of the complexes on 1, 1-diphenyl-2-picrylhydrazyl (DPPH) and 2, 2′-azinobis-(3-ethylbenzthiazoline-6- sulphonate) (ABTS) radicals was significantly higher than that of zein alone. The zein-magnolol complexes (ZMC) were then loaded into CMC to form a hydrogel film. The radical sca v enging rates of DPPH and ABTS of CMC/0.5 ZMC (the proportion of ZMC in film solution at 0.5, v /v) were 32.24 % and 91.30 %, respectively, which were significantly higher than CMC film. The incorporation of the complexes also improved the mechanical properties, with a more than 3-fold increase in elongation at break (EB) value. In addition, the complexes-loaded hydrogel film also inhibited the growth of S. aureus , a common bacterium that can cause food poisoning. Cytotoxicity tests have revealed that the studied films are non-toxic, presenting good compatibility. The film also successfully maintained the nutrients in fresh-cut jackfruit by mitigating lipid peroxidation and the increase in malondialdehyde content during 8-day storage. Overall ZMC loaded CMC film provides a promising approach for food preservation against ultra-violet light, oxidation and microbial growth.
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2025
·
IF 5.9
Ying Wang,Jie Zhang,Yehong Tan,Siran Jiang,Meiyi Tong,Xiaoyong Wang
Mitochondria play a critical role in energy production and cell death regulation, rendering them the important targets for anticancer drugs. Magnolol exhibits weak antiproliferative effects on cancer cells through mediating mitochondrial apoptosis pathway. To enhance its anticancer potency, three derivatives of magnolol, MT1, MT2, and MTP, were synthesized by modifying the parent compound with mitochondrion-targeting triphenylphosphonium and other groups. Among them, MTP bearing a pyridyl demonstrated remarkable anticancer activity both in vitro and in vivo. MTP promoted the production of reactive oxygen species, disrupted the structure and energy metabolism of mitochondria, and induced endoplasmic reticulum stress, thus triggering mitophagy and apoptosis in cancer cells. More unusually, MTP induced immunogenic cell death and promoted the maturation of dendritic cells. Consequently, MTP upregulated the expression of major histocompatibility complex I and activated T cells, boosting the secretion of tumor necrosis factor- α , interferon- γ , and other cytokines to elicit antitumor immune responses. This study demonstrates that mitochondrion-targeted MTP is far more effective than magnolol to kill cancer cells. Aside from direct cytotoxic effect, regulating immunity is a distinctive feature that distinguishes MTP from other natural product derivatives.
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高影响因子
Biomaterials Advances
·
2025
·
IF 6
Zhengzhou Sha,Mingqian Hao,Xi Xue,Feihong Zhuo,Xuting Zhou,Tingmei Lyu,Yuting Cui,Yaqin Gao,Chenqi Zhu,Baoping Jiang,Zhipeng Chen,Liu Xu
Diabetic peripheral neuropathy (DPN) remains a prevalent and challenging complication of diabetes with limited therapeutic options. Magnolol (Mag), a natural multi-target agent, demonstrates significant potential in managing DPN through synergistic anti-inflammatory, antioxidant, and neurorestorative properties. However, its poor oral bioavailability and limited skin penetration hinder clinical application. To address these challenges, we developed a novel topical nanogel system for enhanced transdermal delivery of Mag. Borneol (Bor), a potent penetration enhancer, was co-assembled with Mag via antisolvent precipitation to form self-assembled nanoparticles (Mag-Bor NPs), which were further encapsulated into a carbomer hydrogel matrix to construct the Mag-Bor nanogel (Mag-Bor NPs Gel). The resulting formulation exhibited markedly improved skin permeability and sustained drug retention. Upon topical administration, Mag-Bor NPs Gel effectively alleviated neuropathic impairments in DPN rats through a “transdermal enhancement – anti-inflammatory – nerve repair” mechanism. This therapeutic strategy comprehensively improved key pathological indicators, including plantar thermal, mechanical pain sensitivity, motor nerve conduction velocity (MNCV), intraepidermal nerve fiber density (IENFD), sciatic nerve myelin structure, and inflammation levels in dorsal root ganglia (DRG). This study is the first to report a nanogel system combining efficient transdermal delivery and neurorestorative functions, offering a novel and promising strategy for topical DPN treatment.
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MACROMOLECULES
·
2024
·
IF 5.1
Guoming Yuan,Hui Yang,Xiaole Zheng,Kunxin Wang,Zhijun Liu,Yuemiao Zhang,Yanhan Tao,Kun Wu,Peiwei Hong,Jun Shi,Li Yang
In response to the limitations imposed on the microelectronics industry by electronic crosstalk losses and signal delays, as well as the rapid accumulation of heat, intrinsically low dielectric and high thermal conductivity materials are in urgent demand. Here, a self-curable biobased silane precursor (M@KH590) with a biphenyl unit was synthesized. A series of films (magnolol polysiloxane films (MPSOs)) were prepared using simple sol–gel film conversion and annealing and modulated intermolecular forces and molecular structure. The red-shift of the UV–vis absorption indicated that a larger π–π conjugated system was established. As a result, the through-plane thermal conductivity of MPSO-140 was 0.601 W·m–1·K–1, which was more than three times that of the pure polysiloxane material. Meanwhile, MPSO-140 exhibited excellent intrinsic low dielectric properties (Dk = 2.52, Df = 0.000572, and f = 100 MHz). This was mainly attributed to the reduction of highly polar substances and groups as well as the difficulty in polarizing a π–π conjugated system. Based on rigid biphenyl units and high cross-link density, the tensile strength and modulus of MPSO-140 were 17.42 MPa and 2.61 GPa, respectively, showing prominent mechanical properties. In addition, MPSO-140 exhibited excellent water resistance (water contact angle and 72 h water absorption of 104.8° and 0.19%, respectively) and electrical insulation, showing great potential for practical applications. The study broadened the way toward overcoming the contradiction between low dielectric and high thermal conductivity by simultaneously introducing large free volume and modulating the intermolecular forces and molecular structure in a simple and effective way.
研究领域:
材料科学
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电子工程
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高影响因子
Pharmaceuticals
·
2024
·Vol. 17
·期 11
·1416
·
IF 4.3
Ziang Zhou,Yumeng Wang,Yu Xing,Shuman Pan,Wanru Wang,Jie Yang,Wenyuan Wu,Jie Zhou,Luyi Huang,Qiongdan Liang,Dongmei Zhang,Lingdong Kong
Background/Objectives: High fructose has been implicated as an important trigger of kidney inflammation in patients and experimental models. Magnolol, isolated fromMagnolia officinalis, has an anti-inflammatory effect, but its protective role in podocytes remains underexplored. This study explored the protective effects and underlying mechanism of magnolol against high fructose-induced podocyte inflammation. Methods: The effects of magnolol on high fructose-induced podocyte inflammation were assessed in male Sprague Dawley rats administered 10% (w/v) fructose water for 12 weeks and heat-sensitive human podocyte cell lines (HPCs) exposed to 5 mM fructose. Podocyte foot processes were examined using transmission electron microscopy. The expression levels of nephrin, podocin, tumor necrosis factor-α (TNF-α), Notch1 intracellular domain (NICD1), triokinase/FMN cyclase (TKFC), specificity protein 1 (Sp1) and histone deacetylase 4 (HDAC4) were determined by Western blot, immunofluorescence and real-time quantitative polymerase chain reaction (qRT-PCR). The chromatin immunoprecipitation (ChIP) assay was performed to evaluate the interaction between Sp1 and the promoter region of HDAC4. Results: Magnolol mitigated the impairment of glomerular filtration function in high fructose-fed rats. Besides, it significantly alleviated the inflammatory responses in glomeruli and HPCs, evidenced by decreased protein levels of TNF-α and NICD1. Increased protein levels of TKFC, Sp1 and HDAC4 were observed in high fructose-stimulated HPCs and rat glomeruli. TMP195, an HDAC4 inhibitor, reduced TNF-α and NICD1 protein levels in high fructose-exposed HPCs. The increased Sp1 was shown to associate with the promoter region of HDAC4, promoting HDAC4 protein expression in high fructose-exposed HPCs. The knockdown of TKFC in HPCs byTKFCsiRNA decreased Sp1, HDAC4 and NICD1 protein levels, alleviating podocyte inflammatory response. Furthermore, magnolol inhibited TKFC/Sp1/HDAC4/Notch1 activation in vivo and in vitro. Conclusions: Magnolol attenuated high fructose-induced podocyte inflammation possibly through the suppression of TKFC/Sp1/HDAC4/Notch1 activation, providing new evidence for its potential role in podocyte protection.
研究领域:
药理学
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肾病学
·
分子生物学
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PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2022
·
IF 5.195
Lin Niu,Jie Wang,Fukui Shen,Jie Gao,Min Jiang,Gang Bai
Ethnopharmacological relevance Magnolia officinalis Cortex ( M. officinalis ) is a classical traditional Chinese medicine (TCM) widely used to treat digestive system diseases . It effectively regulates gastrointestinal motility to improve abdominal pain, abdominal distension and other symptoms. Magnolol (MAG) and honokiol (HON) are the main pharmacodynamic components responsible for the gastrointestinal activity of M. officinalis . Aim of the study The transient receptor potential (TRP) family is highly expressed in the gastrointestinal tract and participates in the regulation of gastrointestinal motility, visceral hypersensitivity, visceral secretion and other physiological activities. In this study, the calcium-lowering mechanisms of MAG and HON contributing to the smooth muscle relaxation associated with TRP are discussed. Materials and methods The relaxation smooth muscle effects of MAG and HON were tested by the isolated intestine tone tests. A synthetic MAG probe (MAG-P) was used to target fishing for their possible target. The distribution of MAG on the smooth muscle was identified by a molecular tracer based on chemical biology. Ca 2+ imaging and dual-luciferase reporter assays were used to determine the effects on the target proteins. Finally, the calcium-mediating effects of MAG and HON on smooth muscle cells and TRPC4-knockdown cells were compared to verify the potential mechanism. Results After confirming the smooth muscle relaxation in the small intestine induced by MAG and HON, the relaxation effect was identified mainly due to the downregulation of intracellular calcium by controlling external calcium influx. Although MAG and HON inhibited both TRPV4 and TRPC4 channels to reduce calcium levels, the inhibitory effect on TRPC4 channels is an important mechanism of their smooth muscle relaxation effect, since TRPC4 is widely expressed in the small intestinal smooth muscle cells. Conclusions The inhibition of MAG and HON on TRPC4 channels contributes to the relaxation of intestinal smooth muscle.
研究领域:
药理学
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胃肠病学
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传统中药
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细胞生物学
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PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2021
·Vol. 22
·期 15
·7769
·
IF 5.924
Xueying Song,Liu Liu,Xiaoxia Wu,Yongfeng Liu,Jialu Yuan
The aims of this study were to develop the magnolol–chitosan films and study the positive effect of the combination of magnolol and chitosan. The addition of magnolol made the magnolol–chitosan films exhibit higher density (1.06–1.87 g/cm3), but the relatively lower water vapor permeability (12.06–7.36 × 10−11·g·m−1·s−1·Pa−1) and water content (16.10–10.64%). The dense and smooth surface and cross-section of magnolol–chitosan films were observed by environmental scanning electron microscopy (ESEM) images. The interaction of magnolol and chitosan was observed by X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy and thermogravimetric analysis (TGA). After the addition of magnolol, the antioxidant capacity of magnolol–chitosan films was increased from 18.99 to 82.00%, the growth ofP. aeruginosawas inhibited and the inhibition percentage of biofilm formation was increased from 30.89 to 86.04%. We further verified that the application of magnolol–chitosan films on chilled pork significantly reduced the increases in pH value, inhibited the growth of microorganisms and extended the shelf life. Results suggest that magnolol had a positive effect on magnolol–chitosan films and could be effectively applied to pork preservation.Keywords:magnolol;chitosan;film;antimicrobial;pork
研究领域:
食品科学
·
生物材料学
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PubMed
高影响因子
危险品化学品经营许可证（带存储）