Chinese Journal of Natural Medicines
·
2026
·Vol. 24
·期 1
·59-72
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IF 4.9
Yang Lin,Zhengmeng Jiang,Zhilu Yu,Tianqing Huang,Wanyu Gui,Ziyuan Wang,Fei Li,Pingting Xiao,Changyin Li,Ehu Liu
Diabetes mellitus (DM) is a chronic disease influenced by gut microbiome disturbances. Honokiol (HON), a low oral bioavailability compound from Magnolia officinalis bark, has demonstrated potential as a treatment for DM. This research investigates the effects of HON on gut microbiota and host metabolism to elucidate its mechanism of action in DM. After 8 weeks of intervention through fecal microbiota transplantation (FMT) or antibiotic treatment, HON improved glucose tolerance and lipid metabolism in a gut microbiota-dependent manner. Specifically, HON administration significantly increased Akkermansia muciniphila (AKK) abundance and modulated tryptophan (TRP) metabolism, as evidenced by 16S ribosomal ribonucleic acid (rRNA) gene sequencing and untargeted/targeted metabolomics analysis. Notably, research revealed that AKK metabolized TRP into tryptamine (TA) and other metabolites in vitro . Both AKK and TA activated the aryl hydrocarbon receptor (AHR) pathway, increasing circulating glucagon-like peptide-1 (GLP-1) levels and ameliorating diabetes-related symptoms in DM mice. These findings indicate that HON’s hypoglycemic effect primarily stems from AHR-GLP-1 pathway activation through targeted modulation of AKK and microbial TRP metabolite TA, potentially enhancing HON’s clinical applications.
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Materials Today Bio
·
2025
·
IF 10.2
Shouli Yi,Hongjuan Zhang,Zhen Yang,Di Wu,Dan Shao,Jiongjie He,Yu Liu,Baocheng Hao,Shengyi Wang
Methicillin-resistant Staphylococcus aureus (MRSA) infections and the formation of associated biofilms often lead to refractory and recurrent bacterial infections, posing a serious threat to public health. Herein, a pH-responsive antibiotic-free nanoparticle (HNK@RHL-COS NPs) was prepared by encapsulating the natural antimicrobial agent honokiol (HNK) with rhamnolipid-modified chitosan, enabling targeted disassembling at the acidic infection site, destruction of the biofilm by rhamnolipid, thereby enhancing the penetration of honokiol and chitosan, thus achieving their synergistic bactericidal effect. HNK@RHL-COS NPs exhibited enhanced antimicrobial effects against MRSA, with a minimum inhibitory concentration (MIC) value of 2 μg/mL, significantly inhibited the formation of biofilm and eradicated the mature biofilm. Furthermore, HNK@RHL-COS NPs efficiently accelerated the healing of wounds in MRSA-infected mice, alleviated bacterial peritonitis in mice, and demonstrated excellent biocompatibility in vitro and in vivo . Collectively, this study provides a novel and safety solution for the clinical treatment of MRSA infections.
研究领域:
纳米医学
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抗菌治疗
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生物医学工程
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传染病
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药物递送
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COLLOIDS AND SURFACES B-BIOINTERFACES
·
2020
·
IF 4.389
Weiwei Wu,Wei Xue
Honokiol (HK), an active compound derived from Magnolia officinalis Rehd. et Wils , possesses many beneficial biological activities for human beings. However, its poor solubility and low bioavailability severely limits its application. In this way, to improve the pharmaceutical properties, the HK was complexed in hydroxypropyl-β-cyclodextrin (HP-β-CD) and its oral bioavailability and antitumor effects were evaluated. The HK/HP-β-CD inclusion complex (1:1) was prepared by saturated aqueous solution method. The inclusion complex (HK-HP-β-CD) obtained had a higher solubility, about 1497 times that of the free HK. The dissolution rate and the oral bioavailability of HK was also significantly higher from inclusion complex than from free HK. Furthermore, the HK-HP-β-CD exhibited higher antitumor activity against Human Hepatoma Cell Line (HepG2) than free HK. More cells were arrested in the sub-G1 phase of the cell cycle and were induced to undergo late apoptosis when treated with the HK-HP-β-CD than when treated with free HK.
研究领域:
药理学
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肿瘤学
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药物化学
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RSC Advances
·
2016
·Vol. 6
·期 60
·54830-54835
·
IF 3.289
Zhen Li,Lan Hao,Pei Yuan,Wenjing Hu,Liangke Zhang
This study aimed to develop a new drug delivery system that combines honokiol-loaded albumin nanoparticles (HKNs) with perfluorocarbon-filled microbubbles (MBs) to improve the target delivery of honokiol (HK). The HKNs were prepared through a desolvation method. The MBs were prepared by mechanical shaking and used to encapsulate the HKNs and perfluorocarbon gas (HKN-MBs). The prepared HKN-MBs displayed a mean diameter of 1447.0 ± 182.4 nm and a drug-loading efficiency of 3.48% ± 0.20%. The HKN-MBs demonstrated good acoustic properties in in vitro and in vivo ultrasound (US) imaging experiments, in which no significant difference to traditional MBs was found. The HKN-MBs had high drug encapsulation and loading efficiency while maintaining the acoustic properties as an US contrast agent. C57BL/6 mice with Lewis lung carcinoma tumor were treated with HKN-MBs through the tail vein and then exposed to an US destruction pulse, resulting in an improved curative effect on the tumor tissues. The experimental group administered with HKN-MBs and exposed to US showed an obvious increase in the rate of tumor growth inhibition (48.78%) compared with those of HKN-MBs (32.85%) and HKNs (29.94%). Encapsulation of HKNs in MBs is expected to improve the therapeutic efficacy of HK and provide a feasible technique for targeted tumor therapy.
研究领域:
药剂学
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肿瘤学
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医学影像学
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INDUSTRIAL CROPS AND PRODUCTS
·
2023
·
IF 5.9
Jingwen Sun,Yu Xie,Zhiyuan Chen,Yipin Fan,Yunfeng Liu,Qi Gao,Jianqiang Li,Jingwen Bai,Yu Yang
Magnolia officinalis root extract was obtained by high-pressure-assisted extraction, and the yield of honokiol (HNK) was 86.97 ± 1.05 mg/g dry power. The purified extracts and HNK inhibited the growth of methicillin-resistant Staphylococcus aureus (MRSA). Assays for alkaline phosphatases , proteins, nucleic acids leakage, and electrical conductivity, along with scanning and transmission electron microscopy measurements, confirmed the damaging effects of HNK on the cell wall and membrane of MRSA. Intake of sugar, protein production, molecular docking , and dynamic simulations revealed that HNK interfered with the transport of mannose-based carbohydrates by binding to VAL196, ILE291, ALA293, PRO294, and MET214 on the mannose transporter (ManP) in the phosphotransferase system, and thereby inhibited the carbohydrate metabolism of MRSA. These results indicated that HNK prevented MRSA from using carbohydrates by cutting off its nutritional process, and ultimately caused bacterial rupture and lysis. Therefore, ManP may be a potential target for HNK to combat MRSA infections.
研究领域:
微生物学
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药理学
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植物化学
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Aging-US
·
2020
·
IF 4.831
Yuan Liu,Peng Cheng,An-Hua Wu
Honokiol is a natural active compound extracted from Chinese herbal medicine, Magnolia officinalis . In this study, the role of honokiol in the development of carotid artery atherosclerotic lesions was evaluated in an ApoE-/- mouse model fed with a normal diet (ND) or a Western-type diet (WD) for ten weeks. After first two weeks, a perivascular collar was surgically placed on the right common carotid arteries of the mice. Then, WD-fed mice were intraperitoneally injected with honokiol (10 or 20 mg/kg) or administrated with 10 mg/kg atorvastatin calcium by gavage once a day for eight weeks. After that, the right common carotid arteries were excised for further experiments. The result showed that honokiol substantially inhibited the development of atherosclerotic lesions. Furthermore, honokiol downregulated the expression of pro-inflammatory markers, like tumor necrosis factor-α, interleukin (IL)-6, and IL-1β. Additionally, honokiol treatment decreased reactive oxygen species level and enhanced superoxide dismutase activity. Nitric oxide level, inducible nitric oxide synthase (iNOS) expression, and aberrant activation of nuclear factor-κB pathway were also significantly inhibited by honokiol treatment. Together, these findings suggest that honokiol protects against atherosclerotic plaque formation in carotid artery, and may be an effective drug candidate for the treatment of carotid artery atherosclerotic stenosis.
研究领域:
心血管疾病
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药理学
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分子生物学
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PubMed
高影响因子
Frontiers in Pharmacology
·
2024
·
IF 4.4
Jiemei Shi,Min Liu,Jiajie Zhao,Ye Tan,Chunhui Jiang
Introduction: Mitochondrial dysfunction and oxidative stress play important roles in diabetic retinal vascular injuries. Honokiol (HKL) is a small-molecule polyphenol that exhibits antioxidant effects and has a beneficial effect in diabetes. This study aimed to explore the potential ability of HKL to ameliorate vascular injury in diabetic retinopathy (DR) and its possible mechanisms of action.Methods: The effect of HKL was evaluated in vascular injury in an in vivo type 2 diabetic (db/db) mouse model. In vitro, retinal microvascular endothelial cells were treated with high glucose (HG) to simulate the pathological diabetic environment. Cell viability, expression of apoptosis-related proteins, cellular reactive oxygen species, mitochondrial membrane potential, and morphological changes in the mitochondria were examined.Results: The diabetic mice exhibited severe retinal vascular damage, including vascular leakage in vivo and capillary endothelial cell apoptosis in vitro. HKL reversed the retinal vascular leakage in the diabetic mice. In vitro, HKL improved retinal capillary endothelial cell viability, decreased apoptosis, and reversed the HG-induced increased cellular oxidative stress and mitochondrial fragmentation. The sirtuin 3 (SIRT3) inhibitor 3-TYP blocked all the in vivo and in vitro protective effects of HKL against diabetic retinal vascular leakage and capillary endothelium and eliminated the decrease in oxidative stress levels and reduction of mitochondrial fragmentation.Discussion: In conclusion, these findings suggest that HKL inhibits vascular injury in DR, which was likely achieved through SIRT3-mediated mitochondrial fusion. This study provides a potential new strategy for the treatment of DR.
研究领域:
药理学
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糖尿病学
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眼科学
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细胞生物学
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COLLOIDS AND SURFACES B-BIOINTERFACES
·
2025
·
IF 5.6
Dandan Liao,Yan Yang,Shuxin Xiong,Jizhou Feng,Cheng Zou,Haibo Peng,Xiaohong Yang,Shao-lin Zhang,Zhi-Peng Wang,Yun He,Chao Huang.
Honokiol (HK), a key bioactive compound extracted from the root and stem bark of Magnolia officinalis , has been a staple in traditional Chinese medicine for over a millennium. Despite its long history of use, HK exhibits low oral bioavailability, which hinders its potential for clinical applications. Herein, we report a GSH-responsive and biodegradable polyphosphazene based Nano-HK particles synthesized via covalent bonding of HK, a disulfide-containing linker, and hexachlorocyclotriphosphazene (HCCP). The Nano-HK particles are uniformly distributed, with an average size of approximately 160 nm. Thanks to the covalent bonding between HK molecules, Nano-HK remains stable in plasma, gradually releasing HK at the tumor site through the reduction of disulfide bonds by the high glutathione (GSH) concentration in cancer cells. This targeted release results in a significantly enhanced inhibitory effect on tumor growth in an A375 xenograft model, outperforming free HK. The results showed no toxic symptoms in mouse or any pathological alterations in major organs. These studies demonstrated that Nano-HK substantially enhanced cytotoxicity against tumor cells compared to free HK, inducing G2/M cell cycle arrest and apoptosis in A375 cells. The conjugated HCCP Nano-HK exhibited both efficacy and safety in mouse, showing promise for further development as a potential treatment for tumors.
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CHEMICO-BIOLOGICAL INTERACTIONS
·
2024
·
IF 4.7
Changfeng Zhong,Changmei Wang,Wei Li,Wenyuan Li,Xuemei Chen,Jieqing Guo,Yifan Feng,Xia Wu
Parkinson's disease (PD) is the fastest growing neurodegenerative disease in the world at present. Neuroinflammation plays an important role in Parkinson's disease. In our study, we initially screened magnolol/honokiol derivatives synthesized by our group for their potential anti-neuroinflammatory properties. This was done using LPS-activated BV-2 microglial cell and MPP + -induced PC-12 cell models. Most of derivatives had increased anti-inflammatory activities and decreased toxicities compared to raw materials. Then, compounds were scored with inflammatory factors IL-1β, TNF-α and IL-6 by molecular docking in silico . Our studies revealed the strongest binding compound HM568 which binds with honokiol and metformin. Furthermore, HM568 showed no acute toxicity in mice through acute toxicity. And it is stable under high temperature, high humidity and strong light irradiation. Combining cell experiments and computer results, HM568 was considered for further in vivo pharmacological validations. Intraperitoneal injection administration of MPTP into C57BL/6 mice was utilized as Parkinson's animal model. Results showed that administration of HM568 for 14 days in MPTP-PD mice led to a significant alleviation in weight loss and movement disorders. Further HM568 could significantly down-regulate the expression levels of inflammatory factors IL-1β, IL-6 and TNF-α in brain tissue of the mouse model, reduce the level of caspase-3 and the ratio of Bcl-2/Bax, and up-regulate the level of transforming factor TGF-β, thus producing anti-apoptosis and anti-neuroinflammatory effects on neuronal cells. In terms of pathological features, HM568 could reduce the infiltration of neuronal cells and alleviate the development of lesions, promote the transformation of microglia from M1 negative phenotype to M2 type, and reverse the reduction of TH-positive immune cells in mouse neurons induced by MPTP. The administration of HM568 could reduce the abnormal accumulation of α-syn, and thus produce neuroprotective effect on MPTP-PD mice. Cell experiments, molecular docking and animal experiments thus depict HM568 as a promising agent to delay neuronal degeneration in PD, and its mechanism is related to anti-neuroinflammation.
研究领域:
神经科学
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药理学
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神经退行性疾病
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炎症
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药物发现
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PubMed
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ACS Biomaterials Science & Engineering
·
2024
·
IF 5.4
Chang Liu,Zhengjiang Cao,Li Li,Qingyin Li,Chunle Zhang,Yunbing Wang,Linhua Li,Ping Fu
Sepsis is a severe and complex systemic infection that can result in multiple organ dysfunction. Sepsis-associated acute kidney injury (SAKI), caused by inflammatory response, oxidative stress, and cellular apoptosis, is a common complication that seriously impacts patient survival rates. Herein, a potent and novel metal-polyphenol nanomicelle can be efficiently self-assembled with Pt4+ and honokiol (HK) by the chelation, π–π conjugation, hydrophobic action, and the surfactant properties of Tween-80. These nanomicelles not only enhance drug bioavailability (encapsulation rates: Pt─49%, HK─70%) and reduce drug toxicity (safety dose: <20 μg/g) but also improve targeting toward damaged renal tissues. Furthermore, Pt4+ and HK in the nanomicelles exert a synergistic physiological effect by scavenging free radicals to alleviate oxidative damage, inhibiting macrophage activation and the release of inflammatory factors to regulate inflammation, and displaying broad-spectrum antimicrobial activity to control infection. These actions collectively protect renal tissue and restore its functionality. Here, we constructed metal-polyphenol nanomicelles (Pt/HK-NMs) via ingenious and efficient self-assembly, providing a new strategy to compensate for deficiencies in the hemodialysis and antibiotic treatment of SAKI.
研究领域:
药学
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纳米技术
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感染病学
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肾脏病学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Yilin Li,Yali Song,Na Gan,Lijuan Chen,Si Chen,Yi He,Tingting Zeng,Xinhui Wang,Wei Wang,Di Wu
Owing to the limited availability of biocompatible, edible and natural emulsifiers, the development of Pickering emulsions applicable to the food industry still confronts challenges. Moreover, Honokiol (HNK), due to its poor stability and susceptibility to oxidation, most of the existing delivery systems are centered on injection administration routes and relatively complex in preparation, posing significant challenges for industrialization. In this research, a Pickering emulsion system stabilized by gliadin and konjac glucomannan composite particles (GKPs) was constructed using the pH cycling method and was employed for the delivery of HNK. Under the conditions of a 1:2 mass ratio of the composite particles at pH 4 and an oil phase fraction of 50 %, the storage stability of HNK was effectively enhanced, attaining a retention rate of 84.88 % ± 0.78 % at 4 °C for 14 days. In simulated in vitro digestion, this emulsion system effectively mitigated the degradation of HNK, achieving a bioavailability of 66.94 % ± 4.05 % and increasing the release of free fatty acids. Pickering emulsions stabilized by GKPs may provide a useful means of delivery of bisphenol lignans.
研究领域:
食品科学
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药物递送系统
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高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2026
·
IF 6.7
Yao Wang,Yongxiao Chai,Qisheng Qian,Yue Liang,Xin-xin Chen,Guangxu Xing,Liutao Zhao,Songlin Qiao,Rui Li,Gaiping Zhang
Porcine reproductive and respiratory syndrome (PRRS) is a highly contagious swine disease and poses a severe economic burden to the global swine industry. Owing to the inadequacy of current prevention and control measures, developing effective antiviral strategies for preventing PRRS epidemics is imperative. Honokiol (HNK) is a bioactive component of the dietary supplement magnolia extract. Here, we demonstrated that HNK exhibited potent antiviral effects against different PRRSV strains in vitro. Mechanistically, HNK was shown to interfere with PRRSV replication rather than attachment, internalization, or release. HNK was further determined to target PRRSV RNA-dependent RNA polymerase to impair viral genomic RNA synthesis. In addition, HNK was found to decrease PRRSV-triggered inflammatory responses. More importantly, HNK was revealed to reduce viral loads and alleviate lung damage in vivo. This study highlights the potential of HNK as an inhibitor of PRRSV and provides novel insights into its antiviral properties.
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危险品化学品经营许可证（带存储）