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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY · 2020 · IF 5.573

Semisynthesis of novel magnolol-based Mannich base derivatives that suppress cancer cells via inducing autophagy

Ting Xu,Zhiyuan Zheng,Yong Guo,Li-Ping Bai

Magnolol , a natural bioactive neolignan , was found in the bark of a traditional Chinese medicine Magnoliae officinalis (“Hou Po” in Chinese). In this study, thrity-two magnolol-based Mannich base derivatives 3a – p and 4a – p were synthesized, and evaluated for their anti-proliferative activities against a panel of human tumor cell lines (T47D, MCF-7, Hela and A549). Among all derivatives, compound 3p displayed the most potent antiproliferative activity against T47D, MCF-7 and Hela cell lines with IC 50 values of 0.91, 3.32 and 1.71 μM, respectively. Compared with the parental magnolol and the positive drug cisplatin , 3p exhibited up to 76.1-fold and 10.3-fold enhancement of cytotoxic effect on T47D cancer cells, respectively. Mechanism study revealed that the most potent derivative 3p suppressed cancer cells via inducing autophagy. Moreover, 3p also possessed suppressive effects on migration of T47D and Hela cancer cells. In addition, some interesting structure-activity relationships (SARs) were also summarized.

CAS / MDL: 528-43-8
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ACS Applied Materials & Interfaces · 2025 · IF 8.2

Functional Wound Dressing Based on Natural Compounds from Traditional Chinese Medicines─Magnolol for Accelerating Wound Healing

Huawang Zhao,Naidan Zhang,Jincheng Zhang,Bekezela Matshazi,Yawen Shi,Minyuan Feng,Weilin Xu,Guangming Cai,Hongjun Yang

Traditional petroleum-based foam dressings offer limitations due to poor biocompatibility, long preparation cycle, and serious environmental pollution. In addition, free small molecules of incomplete polymers and residual toxic cross-linkers pose a threat to the health of patients and hinder the rapid repair of wounds. Recently, natural compounds extracted from plants have gained a lot of interest in the field of wound repair due to their good biocompatibility, biodegradability, and therapeutic effects. In this study, we successfully prepared magnolol-based porous foams by a simple one-pot method using magnolol herbal exhibiting good mechanical properties, hydrophobicity, and biocompatibility, and meets the requirements of wound dressings. The Janus composite dressing was prepared using a magnolol-based porous foam as the inner layer, PVA nonwoven fabric as the middle layer, and polyacrylate as the outer layer. The three-layer structure of magnolol-based porous foam/PVA nonwoven fabric/polyacrylate (MPF/PVA/PAAS) has the capacity to realize unidirectional diversion and rapid water locking of liquid. In vivo experimental data showed that MPF/PVA/PAAS dressing significantly promoted collagen deposition and angiogenesis, and could shorten the wound healing cycle from 14 days to 10 days, significantly accelerating the wound healing process compared to traditional wound dressings. Hence, magnolol-based foam dressings show great application potential in the field of wound treatment.

研究领域: 生物材料学 · 药理学 · 医学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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POLYMER · 2025 · IF 4.5

Magnolol-based active ester modified cycloaliphatic epoxy resins with improved flame retardancy, dielectric and mechanical property

Yonghao Lv,Hongyan Li,Zhubao Shao,Zhiming Jiang

Cycloaliphatic epoxy resins exhibit excellent dielectric properties but are often harder to be flame retarded. To address this issue, a magnolol-derived active ester DDA was synthesized and employed to prepare flame-retardant cycloaliphatic epoxy resins through the intrinsic incorporation of a phosphaphenanthrene moiety (DOPO). Compared with anhydride MHHPA-cured resins, DDA demonstrated superior char-forming capability and enhanced the compactness of carbon residues. Under equivalent phosphorus loadings, the DDA-cured resin (CFDAP) exhibited a significantly higher limiting oxygen index (LOI) value of 30.2 %, notably surpassing the 26.7 % LOI of the MHHPA-cured counterpart. CFDAP effectively achieved reductions of 44 % in peak heat release rate and 50 % in total heat release during combustion. Importantly, ether bonds instead of ester bonds in the main chain of CFDAP enhanced the thermal stability and tensile strength relative to MHHPA-cured system. The chemical integration of DOPO moiety further improved the dielectric properties of epoxy resins at high frequencies by increasing free volume within the matrix. Collectively, the active ester curing agent DDA enables simultaneous enhancements in flame retardancy, thermal stability, mechanical properties, and dielectric performance of epoxy resins, presenting an efficient strategy for designing advanced electronic packaging materials suitable for high-frequency and high-speed electronic communication.

CAS / MDL: 35948-25-5
研究领域: 高分子科学 · 材料工程 · 阻燃材料 · 介电材料 · 电子封装材料
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PROGRESS IN ORGANIC COATINGS · 2023 · IF 6.6

A low dielectric polysiloxane with hydro-oleophobicity and improved mechanical properties based on magnolol derivative crosslinker

Guoming Yuan,Hui Yang,Kunxin Wang,WenJie Diao,Enxiang Jiao,Zhijun Liu,Zhao Li,Kun Wu,Jun Shi

With the development of the microelectronics industry and the increasing concern for sustainability, there is an urgent need to prepare low dielectric materials from bio-based feedstocks . In this work, an allylated-magnolol (A-M) was synthesized as a crosslinker for fluorinated polymethylhydrosiloxane (F-PMHS) to obtain a low dielectric polysiloxane (M/F-PSO). M/F-PSO exhibited excellent dielectric properties with a dielectric constant of 2.73 and a dielectric loss of 0.0074 at 100 MHz. This was mainly attributed to the synergistic effect of the hard-polarization C F bond and the hindering molecular stacking structure of biphenyl. In addition, M/F-PSO had good hydro-oleophobicity (θ water  = 108° and θ glycol  = 105°), which is brought about by the low surface energy CF 3 and the rigid hydrophobic structure of A-M. The water absorption of M/F-PSO was only 0.13 % after 48 h immersion in deionized water . Owing to the introduction of rigid structure and good dispersion of A-M in F-PMHS, the tensile strength of M/F-PSO was up to 5.00 MPa, which is 432 % higher than that of pure polysiloxane (PSO). Moreover, the thermal stability of M/F-PSO was comparable to that of PSO, with an initial decomposition temperature (T d, 5% ) as high as 440.30 °C. These results demonstrated the feasibility of introducing renewable bio-resource magnolol into polysiloxane to prepare low dielectric materials with excellent hydro-oleophobicity and mechanical properties .

研究领域: 材料科学 · 化学工程 · 可持续发展
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Frontiers in Oncology · 2020 · IF 4.848

Magnolol Suppresses Pancreatic Cancer Development In Vivo and In Vitro via Negatively Regulating TGF-β/Smad Signaling

Chen Shuo,Shen Jiaqi,Zhao Jing,Wang Jiazhong,Shan Tao,Li Junhui,Xu Meng,Chen Xi,Liu Yang,Cao Gang

Magnolol, a hydroxylated biphenyl extracted from Magnolia officinalis, has recently drawn attention due to its anticancer potential. The present study was aimed to explore the effects of Magnolol on restraining the proliferation, migration and invasion of pancreatic cancer in vivo and in vitro. Magnolol showed significant anti-growth effect in an orthotopic xenograft nude mouse model, and immunohistochemical staining of the xenografts revealed that Magnolol suppressed vimentin expression and facilitated E-cadherin expression. The cytoactive detection using CCK-8 assay showed Magnolol inhibited PANC-1 and AsPC-1 concentration-dependently. Scratch healing assay and the Transwell invasion assay proved the inhibiting effects of Magnolol on cellular migration and invasion at a non-cytotoxic concentration. Western blot and rt-PCR showed that Magnolol suppressed epithelial-mesenchymal-transition by increasing the expression level of E-cadherin and decreasing those of N-cadherin and vimentin. Magnolol suppressed the TGF-β/Smad pathway by negatively regulating phosphorylation of Smad2/3. Moreover, TGF-β1 impaired the antitumor effects of Magnolol in vivo. These results demonstrated that Magnolol can inhibit proliferation, migration and invasion in vivo and in vitro by suppressing the TGF-β signal pathway and EMT. Magnolol could be a hopeful therapeutic drug for pancreatic malignancy.

研究领域: 肿瘤学 · 药理学 · 分子生物学
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POLYMER · 2025 · IF 4.5

The forming mechanism and optimizing of natural polymer foam based on magnolol extracted from Chinese herbal medicine

Huawang Zhao,Naidan Zhang,Minyuan Feng,Yu Wang,Bekezela Matshazi,Haofeng Liu,Weilin Xu,Hongjun Yang

Magnolol is a Chinese medicinal herb that has been used for treating cough, phlegm and inflammation for a thousand years. Given its low absorption rate, which limits its use, there is a need to develop porous magnolol foams that are light weight, low density, portable while maintaining tissue integrity to expand its application. This study proposes an innovative method for creating a biocompatible foam through a one-pot process involving the reaction of magnolol with sulfhydryl compounds, using a thiol-ene click reaction to form a foam. Various foams were systematically formulated by adjusting the degrees of cross-linking, concentrations of the foaming agent 2,2'-azobis(2-methylpropionitrile) (AIBN), and the temperature and pressure conditions during the foaming. AIBN acted both as a blowing agent and initiator, triggering cross-linking in the polymer solution by releasing free radicals and nitrogen gas. This initiated rapid expansion when a critical viscosity threshold was reached, ultimately curing the foam. The optimal foaming efficiency was achieved when the molar ratio of allyl to mercapto groups was maintained at 1:1, with pentaerythritol tetrakis(3-mercapto-propionate) (PETMP) identified as the optimal sulfhydryl compound. Increasing the dosage of AIBN enhanced gas generation, further expanding foam volume, pore size and porosity. The foam is lightest when the AIBN content is 7.5%. When magnolol-based foams were prepared under sealed conditions at 100°C, without external pressure, they exhibited large, uniformly distributed pores and excellent water-absorbing properties. Moreover, the resulting foams demonstrated remarkable thermal stability and resilience.Therefore, the magnolol foam prepared in this study is expected to be combined with negative pressure drainage and applied in fields such as wound healing and hemostasis. These findings also offer a new design strategy for engineering high-performance functional magnolol foams with high biomass content.

研究领域: 高分子科学 · 材料工程 · 药物技术 · 生物医学工程 · 天然产物化学
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PHYTOMEDICINE · 2026 · IF 8.3

Magnolol inhibits the resistance of ESBLs E. coli to fourth-generation cephalosporins in vitro and in vivo

Yin-Chao Tong,Huan Lin,Yang Yang,Zhi-fu Zhou,Yi-Ning Zhang,Juan Wang,Wu-ren Ma,Yongsheng Wang,Wei-Min Zhang,Su-Zhu Qing

Background Antimicrobial resistance (AMR) infection is attracting increasing attention, especially superbug infections. As a result, finding ways to reduce AMR is essential. For the time being, natural compound therapy for reducing AMR is an ideal choice. Purpose This study aims to investigate the mechanism of magnolol reducing the AMR of E. coli in vitro and vivo . Methods The morphology and function of E. coli under magnolol treatment were assessed using a scanning electron microscope, qPCR, RNA-seq, and other methods. Moreover, the in vivo treatment effects of magnolol combined with antibiotics were evaluated by HE and IHC staining. Results In this study, we found that magnolol reduced the resistance of ESBL E. coli to the fourth-generation cephalosporin in vitro via two main mechanisms. Firstly, magnolol disrupts iron ion metabolism by increasing environmental iron uptake significantly (P ≤ 0.01), leading to a significant increase in intracellular ROS (P ≤ 0.01) and membrane damage. Secondly, magnolol significantly inhibits the relative mRNA expression of blaCTX-M-1 (P ≤ 0.01) and the CTX-M-1 enzyme activity in ESBL E. coli. Furthermore, we find that magnolol can inhibit ESBL E. coli in vivo by significantly reducing the TLR4-NFκB p65 pathway ( P ≤ 0.01). Conclusion In a word, our results indicate that magnolol is a natural antibacterial adjuvant with potent inhibitory activity against bacterial resistance and exerts this activity through multiple pathways, which has particular significance for the further study of the AMR mechanism.

✓ 已验证 DOI PubMed 高影响因子
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MOLECULES · 2026 ·Vol. 31 ·期 6 · IF 5.1

Magnolia officinalis Rehder & E.H.Wilson. Bark Extract and Magnolol Alleviate Allergic Rhinitis via Modulating NF-κB/MAPK Signaling

Leyuan Huang,Xu Zhou,Guanfeng He,Haixin Li,Xiaoying Chen,Jingwen Xu,Lei Zhou

Magnolia officinalisRehder & E.H.Wilson. bark is famous as a traditional herbal medicine used in prescriptions for treating gastrointestinal discomfort, respiratory and inflammatory disorders. Magnolol, one of its principal bioactive constituents, exhibits potent anti-inflammatory and immunomodulatory properties. However, its therapeutic mechanisms in allergic rhinitis (AR) remain to be elucidated. In this study, the anti-allergic effects and molecular mechanisms ofM.officinalisbark aqueous extract (MOAE) and magnolol were investigated using an ovalbumin (OVA)-induced AR mouse model. Nasal symptoms, histopathological alterations, and serum inflammatory mediators, including histamine and immunoglobulins (IgE, IgG1, IgG2a), were evaluated to assess efficacy. Both MOAE and magnolol significantly alleviated nasal rubbing and sneezing, reduced eosinophil infiltration and mucus hypersecretion, and improved tissue morphology in nasal and lung sections. Moreover, treatment markedly decreased serum levels of histamine and OVA-specific antibodies. Integrative network pharmacology, RNA sequencing, and molecular docking analyses revealed 33 co-regulated target genes mainly involved in the NF-κB and MAPK signaling pathways, suggesting that modulation of these pathways underlies the observed anti-inflammatory effects. These findings demonstrate that MOAE and magnolol exert protective effects against AR through the regulation of key inflammatory signaling cascades. This study provides modern pharmacological evidence supporting the traditional use ofM.officinalisbark and highlights its potential as a natural therapeutic candidate for AR.

CAS / MDL: 528-43-8
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2026 · IF 5.2

Magnolol nanomicelles based on valproic acid-modified hyaluronic acid for the treatment of androgenetic alopecia in mice

Xuedan Fu,Qijie Cheng,Wenda Li,Xiaoxia Zhang,Minyu Sun,Xinnan Wang,Pu Wang,Zeyu Zhang,Huixia Lv,Zhenhai Zhang,Jianming Ju

Magnolol (Mag) exhibits potent antibacterial, anti-inflammatory, and antioxidant effects and is a promising agent for androgenetic alopecia (AGA) treatment, but its poor water solubility limits its clinical application. We thus fabricated modified hyaluronic acid-based follicle-targeted nanomicelles. Hydrophobic valproic acid-modified hyaluronic acid (HA-VPA) was utilized as a nanocarrier for magnolol encapsulation to construct HA-VPA-Mag micelles, followed by systematic characterization of their physicochemical properties. The therapeutic efficacy of HA-VPA-Mag against androgenetic alopecia was assessed in a testosterone propionate-induced AGA mouse model, with a focus on transdermal permeation behavior and hair follicle targeting efficiency. In vitro studies demonstrated sustained magnolol release, enhanced transdermal retention, and selective follicular accumulation. In a testosterone propionate-induced AGA mouse model, enzyme-linked immunosorbent assay (ELISA), Real-time quantitative polymerase chain reaction (RT-qPCR), Western blot (WB), and histopathological analyses revealed that magnolol nanomicelles markedly reversed alopecia symptoms and outperformed free magnolol solution. The hyaluronic acid-valproic acid -based magnolol nanomicelles overcome the drug's poor aqueous solubility, enhance follicular targeting, and significantly improve therapeutic efficacy against AGA. Download: Download high-res image (485KB) Download: Download full-size image

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Pharmaceutics · 2021 ·Vol. 13 ·期 10 ·1725 · IF 6.321

Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

Jiawei Han,Luyuan Li,Meiling Su,Weili Heng,Yuanfeng Wei,Yuan Gao,Shuai Qian

Different from previously reported co-amorphous systems, a co-amorphous curcumin-magnolol (CUR-MAG CM) system, as compared with its crystalline counterparts, exhibited decreased dissolution due to its aggregation during dissolution. The main purpose of the present study is to deaggregate CUR-MAG CM to optimize drug dissolution and explore the deaggregation mechanism involved. Herein, a small amount of polymer (HPMC, HPC, and PVP K30) was co-formulated at 5% (w/w) with CUR-MAG CM as ternary co-amorphous systems. The polymer addition changed the surface properties of CUR-MAG CM including improved water wettability enhanced surface free energy, and hence exerted a deaggregating effect. As a result, the ternary co-amorphous systems showed faster and higher dissolution as compared with crystalline CUR/MAG and CUR-MAG CM. In addition, the nucleation and crystal growth of dissolved CUR and MAG molecules were significantly inhibited by the added polymer, maintaining a supersaturated concentration for a long time. Furthermore, polymer addition increased the Tgof CUR-MAG CM, potentially involving molecular interactions and inhibiting molecular mobility, resulting in enhanced physical stability under 25 °C/60% RH and 40 °C/75% RH conditions. Therefore, this study provides a promising strategy to optimize the dissolution and physical stability of co-amorphous systems by deaggregation and crystallization inhibition via adding small amounts of polymers.Keywords:curcumin;magnolol;co-amorphous;deaggregation;dissolution;physical stability

研究领域: 药剂学 · 药物化学
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INDUSTRIAL CROPS AND PRODUCTS · 2023 · IF 5.9

Using carboxymethyl cellulose and pectin to construct an enzyme-responsive magnolol-release film against plant pathogenic fungi

Feixu Mo,Xianfeng Hu,Yi Ding,Rongyu Li,Youhua Long,Ming Li

This study aimed to realize controlled release of pesticides . Inspired by the characteristics of plant pathogenic fungi that release cell wall-degrading enzymes (CWDEs) to destroy plant cell walls, enzyme-responsive carboxymethyl cellulose , pectin, sodium alginate , and glycerol (CPSG) films were constructed to encapsulate carboxymethyl chitosan (CMCS) particles loaded with magnolol (Mag) to form a [email protected] @CPSG film. The results showed that the amount of Mag released by the [email protected] @CPSG film under cellulase and pectinase stimulation was 43.18% at 7 h, which was 103.87% higher than that in water. After the [email protected] @CPSG film treatment, the diameter of the disease spots on tobacco caused by Rhizoctonia solani decreased by 93.17%. The contact angle of the film on the rice leaf surface was less than 30° and the half-life of magnolol increased to 15.2 d. In conclusion, the CPSG film can realize the controlled release of pesticides and improve their utilization rate.

研究领域: 植物病理学 · 材料科学 · 农业科学
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MATERIALS TECHNOLOGY · 2023 · IF 3.1

Glutathione and acid dual-responsive nanomaterials loaded with methotrexate and magnolol for triple-negative breast cancer treatment

Hongyi Wang,Zhehao Shen,Zehui Fan,Ni Jiang,Guowei Wang,Ziyi Mai,Ziwei Hu,Lingli Mou,Yanjuan He,Xiaojun Tao,Wu Zhong,Xuelong Fan

In this study, we designed and synthesised MTX and PEG‒grafted chitosan copolymer nanoparticles (PsCM) to load MAG. We generated MAG@PsCM nanoparticles according to the effective ratio of dual drugs of 1:2.5, achieving 3.73% and 8.95% drug loading for MTX and MAG, respectively. Drug efficiency experiments were conducted on MDA-MB-231 breast cancer cells, and the results showed that when MTX was used alone, the tumour cell survival rate was 43.66 ± 1.77%and when low-dose MAG and MTX were used in combination, the survival rate of tumour cells was significantly reduced to 29.82% ± 2.22%. The nanoparticles enhanced the synergistic tumour therapeutic effect of the two drugs with the cell survival rate was 21.94 ± 1.43%, significantly lower compared with the free drugs. MAG@PsCM nanoparticles were significantly taken up by cells at 3, 6 and 12 h, and the total amount taken up increased significantly with time.

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