查找使用阿拉丁产品的科研文献

Opposite effects of vitamin C and vitamin E on the antifungal activity of honokiol.

Sun L,Ye X,Ding D,Kai L.

The aim of the present study was to evaluate the effects of two well-known natural antioxidants vitamin C (VC) and vitamin E (VE) on the antifungal activity of honokiol against Candida albicans . The broth microdilution method was employed to test the antifungal activities of honokiol with or without antioxidants in the medium against C . albicans strain. Intracellular reactive oxygen species (ROS) and lipid peroxidation were determined by fluorescence staining assay. Mitochondrial dysfunction was assessed by detecting the mitochondrial DNA and the mitochondrial membrane potential. We observed that VC could significantly potentiate the antifungal activities of honokiol while VE reduced the effectiveness of honokiol against C . albicans . In addition, VC accelerated honokiol-induced mitochondrial dysfunction and inhibited glycolysis leading to a decrease in cellular ATP. However, VE could protect against mitochondrial membrane lipid peroxidation and rescue mitochondrial function after honokiol treatment. Our research provides new insight into the understanding of the action mechanism of honokiol and VC combination against C . albicans .

Effect of Honokiol on culture time and survival of Alzheimer’s disease iPSC-derived neurons

Duong Thi Thuy Le,Cuong Manh Vu,Thuy Thi Bich Ly,Nam Trung Nguyen,Phuong Thi Mai Nguyen,Ha Hoang Chu

Honokiol@PF127 crosslinked hyaluronate-based hydrogel for promoting wound healing by regulating macrophage polarization

Qingcong Wei,Ziming Jin,Weiwei Zhang,Yanfei Zhao,Yaxing Wang,Yixing Wei,Xing He,Guanglei Ma,Yuming Guo,Yuqin Jiang,Zhiguo Hu

Bacterial infection, oxidative stress and inflammation are the main obstacles in wound healing. Hydrogels with moist and inherent properties are beneficial to wound healing. Here, we fabricated a honokiol-laden micelle-crosslinked hyaluronate-based hydrogel by simply mixing honokiol-laden PF127-CHO micelles, 3,3′-dithiobis(propionohydrazide) grafted hyaluronic acid and silver ions. PF127 could not only effectively load hydrophobic small molecules but also be macromolecular crosslinker for preparing hydrogels. Hyaluronic acid plays an essential role in wound healing processes including regulating macrophage polarization towards M2 phenotype. The chemical dynamic acylhydrazone crosslinking and physical crosslinking among PF127-CHO micelles constructed hydrogel's networks, which endowed hydrogel with excellent self-healing properties. PF-HA-3 hydrogel also exhibited outstanding antioxidant and antibacterial capabilities. In a full-thickness skin defect model, this degradable and biocompatible hydrogel could promote wound healing by remodeling wound tissues, regulating M2 polarization and angiogenesis . In summary, this inherent multifunctional hydrogel will provide a promising strategy for designing bioactive compounds-based wound dressings.

Honokiol ameliorates silica-induced lung fibrosis by inhibiting macrophage pyroptosis via modulating cGAS/STING signaling

Qiang Zhou,Meiyu Chang,Shuhan Guo,Yiming Zhang,Qiufang Qu,Qingnan Zhou,Zhiheng Li,Sanqiao Yao

Silicosis is a life-threatening occupational disease because of inhaling silica dust, leading to chronic inflammation, pyroptosis, and fibrosis. Unfortunately, it is still lacking effective pharmacological intervention currently. Honokiol ( HKL ), a natural extract with biological activity from Magnolia bark, is known for its antioxidant and anti-inflammatory biological effects. The current work aimed to investigate the therapeutic potential of HKL in mitigating silica-induced lung fibrosis and pyroptosis, particularly focusing on the cGAS/STING signaling pathway. The pulmonary pathological results shown in H&E and Masson’s trichrome staining images confirmed the protective effects of HKL on lung tissue structure. In addition, HKL significantly reduced lung inflammation, collagen deposition, and oxidative stress compared to mice in the silicosis group. HKL treatment also alleviated silica-induced pyroptosis by suppressing the activation of the cGAS/STING signaling pathway in lung tissues. Moreover, the in vitro experiments using J774A.1 macrophages demonstrated that HKL reduced pyroptosis and improved cell viability under exposure to silica combined lipopolysaccharide (LPS). These were attributed to HKL downregulating the activation of the cGAS/STING signaling pathway in pyroptotic J774A.1 cells induced by silica combined with LPS. Meanwhile, inhibition of STING signaling induced by DNase I significantly enhanced the protective effects of HKL on the inflammatory and pyroptotic processes induced by silica. Overall, HKL could attenuate silica-induced pyroptosis by modulating the cGAS/STING signaling pathway against pulmonary fibrosis. The current study offers a promising approach for treating silicosis and related inflammatory responses.

Honokiol alleviates monosodium urate-induced gouty pain by inhibiting voltage-gated proton channels in mice

Miao Lurong,Yuan Ziqi,Zhang Shijia,Zhang Guangqin

Objective To investigate whether honokiol (HNK) acted as an analgesic in connection with inhibiting the voltage-gated proton channel (Hv1). Methods The model of gouty arthritis was induced by injecting monosodium urate (MSU) crystals into the hind ankle joint of mice. HNK was given by intragastric administration. Ankle swelling degree and mechanical allodynia were evaluated using ankle joint circumference measurement and von Frey filaments, respectively. Hv1 current, tail current, and action potential in dorsal root ganglion (DRG) neurons were recorded with patch-clamp techniques. Results HNK (10, 20, 40 mg/kg) alleviated inflammatory response and mechanical allodynia in a dose-dependent manner. In normal DRG neurons, 50 µM Zn 2+ or 2-GBI significantly inhibited the Hv1 current and the current density of Hv1 increased with increasing pH gradient. The amplitude of Hv1 current significantly increased on the 3rd after MSU treatment, and HNK dose-dependently reversed the upregulation of Hv1 current. Compared with MSU group, 40 mg/kg HNK shifted the activation curve to the direction of more positive voltage and increased reversal potential to the normal level. In addition, 40 mg/kg HNK reversed the down-regulation of tail current deactivation time constant ( τ tail ) but did not alter the neuronal excitability of DRG neurons in gouty mice. Conclusion HNK may be a potential analgesic by inhibiting Hv1 current.

Nanocomposite biosensor tracks honokiol-induced oxidative stress dynamics in 3D hydrogel-cultured lung cancer cells

Zhu Yuxuan,Huang Zhichao,Tian Shichao,Wang Qi,Wu Fan,Liu Jingwen,Wang Ping,Wan Hao,Zhuang Liujing,Jiang Deming

In cancer cells, higher reactive oxygen species (ROS) than normal cells were observed due to hypermetabolism. The redox balance in cancer cells relies on accordingly upregulated antioxidant capacity. By manipulating oxidation and antioxidant systems, chemotherapeutic drugs can selectively kill cancer cells without hurting normal cells. As three-dimensional (3D) in vitro models, such as spheroids and organoids, have become widely used in cancer research, traditional detection methods (e.g., absorption tests or titration) are inadequate for detecting in 3D environments. Thus, it is crucial to find a new method to detect oxidative stress of 3D in vitro cancer models. Here, a nanocomposite electrochemical biosensor was exploited to evaluate oxidative stress of cancer cells cultured in the 3D environment. The oxidation-regulatory capacity of honokiol, a Magnolia genus-derived anti-cancer molecule, was evaluated. A screen-printed electrode (SPCE) was modified with reduced graphene oxide (RGO) and platinum nanoparticles (Pt NPs) to get Pt NPs/RGO/SPCE. Then the gelatin methacrylate/reduced graphene oxide (GelMA/RGO) hydrogel was applied to immobilized NCI-H1975 in a 3D bionic environment to get NCI-H1975/GelMA/RGO/Pt NPs/RGO/SPCE. After optimizing the experiment condition, the Pt NPs/RGO/SPCE showed a detection threshold of 0.65 μM and a linear field from 1 to 10 μM for H 2 O 2 detection while the NCI-H1975/GelMA/RGO/Pt NPs/RGO/SPCE sensitively responded to H 2 O 2 -induced oxidative stress. By utilizing the NCI-H1975/GelMA/RGO/Pt NPs/RGO/SPCE we found honokiol (a natural polyphenol constituent) inhibits NCI-H1975 by inducing oxidative stress. This simple cell-based electrochemical biosensor can in situ evaluate oxidative stress of 3D cancer models conveniently. It can also be easily extended to the study of the mechanism of action of other drugs and holds broad application prospects in the fields of new drug development and drug repurposing.

Magnolol and honokiol target TRPC4 to regulate extracellular calcium influx and relax intestinal smooth muscle

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.

Honokiol improves cognitive impairment in APP/PS1 mice through activating mitophagy and mitochondrial unfolded protein response

Mingyue Hou,Wenfang Bao,Yuanyuan Gao,Jiayue Chen,Guijun Song

Activated mitophagy and mitochondrial unfolded protein response (UPR mt ) has been reported to protect against mitochondrial dysfunction, which is closely related to the onset of Alzheimer's disease (AD). Honokiol (HKL, C 18 H 18 O 2 ) is a kind of natural extraction from bark of Magnolia offi cinalis with anti-AD effect, and our study aims to explore the effect of HKL on mitophagy and UPR mt in AD. Briefly, male APP/PS1 mice and Aβ oligmer (AβO)-treated primary hippocampal neurons were respectively used to mimic AD in vivo and in vitro. It was determined that HKL significantly ameliorated cognitive impairment and synaptic damages in APP/PS1 mice. Besides, the activated mitophagy and UPR mt together with inhibited oxidative stress and improved mitochondrial dynamic disorder were further validated in hippocampus of HKL-treated APP/PS1 mice. Meanwhile, HKL-treated mice displayed much higher hippocampal expression and activity of mitochondrial sirtuin 3 (SIRT3). Therefore, SIRT3 knockdown was further achieved in primary hippocampal neurons by effective shRNA , and we determined that HKL improved synaptic damage, mitochondrial dysfunction, mitophagy and UPR mt in AβO-treated primary hippocampal neurons in a SIRT3-dependent manner. In summary, our study validates the protective effect of HKL on AD, and highlights that HKL exerts anti-AD effect by activating mitophagy and UPR mt .

Honokiol inhibits endoplasmic reticulum stress‑associated lipopolysaccharide-induced inflammation and apoptosis in bovine endometrial epithelial cells

Wenshu Chen,Jieli Wu,Sisi Zhan,Xiaojie Lu

Honokiol (HKL) has been previously reported to exert anti-inflammatory effects in numerous diseases. However, the role of HKL in endometritis remains unclear. The present study aimed to explore and elucidate the role of HKL in a lipopolysaccharide (LPS)-induced in vitro model of endometritis. Bovine endometrial epithelial cells (bEECs) were pre-treated with HKL at doses of 1, 10 and 20 µM, followed by 1 µg/ml LPS. MTT assay was then used to detect cell viability. ELISA was utilized to measure the levels of the proinflammatory cytokines TNF-α, IL-1β and IL-6 in bEECs culture supernatants. Reverse transcription-quantitative PCR was further performed to examine the mRNA expression levels of these cytokines. Cell apoptosis was observed by TUNEL staining and the levels of Bcl-2, Bax, cleaved caspase 3 and cleaved caspase 9 were assayed by western blotting. Western blotting was also performed to detect the expression levels of endoplasmic reticulum (ER) stress-related proteins activating transcription factor 6, CCAAT-enhancer-binding protein homologous protein, inositol-requiring enzyme 1 and cleaved caspase 12 in bEECs. LPS treatment reduced cell viability and HKL treatment improved the viability of bEECs after LPS treatment. The LPS-induced inflammatory response and apoptosis in bEECs were also inhibited by HKL treatment. Additionally, the increased expression of ER stress-related proteins induced by LPS was reversed by HKL treatment. Following stimulation with the ER stress inducer tunicamycin, it was revealed that HKL attenuated ER stress and inhibited LPS-induced inflammatory response and apoptosis in bEECs. In summary, HKL inhibited ER stress associated with LPS-induced inflammation and apoptosis in bEECs, providing evidence that HKL can serve to be a novel agent for the treatment of endometritis.

Design, synthesis, and optimization of Honokiol-Piperazine derivatives as lung-enriched agents against MRSA pneumonia infection

Ruixue Zhang,Yifan Zhong,Hongzhi Gong,Xinyue Deng,Haibo Peng,Yun He

Methicillin-resistant Staphylococcus aureus ( MRSA ) causes severe bacterial pneumonia; current therapies (e.g., vancomycin) suffer from poor pulmonary bioavailability and dose-limiting safety concerns, demanding precision lung-enriched agents. However, small-molecule lung-enriched antibacterials are relatively rare. Honokiol (HNK), a natural phenolic compound with broad pharmacological activities but moderate antibacterial potency and limited tissue selectivity, was selected as the scaffold. We integrated a piperazine moiety into HNK and synthesized a series of HNK–piperazine derivatives. Among them, 13   f showed potent activity primarily against Gram-positive bacteria, including MRSA (MIC: 2–4 μM; 16–32-fold more potent than HNK) together with preferential lung exposure. 13   f exhibited rapid bactericidal activity and showed minimal MIC shift under sub-MIC selection over 31 serial passages (MICₙ/MIC₀ = 1–2), whereas ciprofloxacin displayed a 256-fold increase over the same period; it also attenuated staphyloxanthin production and reduced biofilm biomass. Mechanistic assays suggested time- and concentration-dependent membrane-associated effects, as reflected by permeability/depolarization readouts, nucleic acid/protein leakage, SEM imaging, and complementary MD analyses, with more pronounced effects at higher exposures. Pharmacokinetic and biodistribution analyses revealed a 13-fold longer half-life and a 147.92-fold higher lung AUC for 13   f than for HNK. In a murine MRSA pneumonia model, 13   f substantially reduced pulmonary bacterial burden and showed in vivo activity in the same overall range as vancomycin under the tested dosing regimen. No obvious histopathological alterations were observed under the tested short-term conditions. Overall, this work demonstrated a small-molecule approach to combine lung enrichment with potent anti-MRSA activity, supporting the further preclinical evaluation of 13   f for MRSA pneumonia.

Honokiol-based pH-responsive amphiphilic polymer as an intelligent delivery system for rhizosphere-targeted herbicide application

Yuying Xie,Yangchun Ge,Zhuochao Shen,Yupeng Qiu,Honglei Wang,Haohua Zhang,Qingyue Zhang,Tingting Xiang,Minhui Wo,Xuqiang Peng,Zhongyu Li

BACKGROUND The development of efficient and environmentally friendly herbicide-delivery systems is crucial in modern agriculture. Such systems can achieve precise targeting and controlled release of active ingredients through formulation technologies like slow-release carriers and targeted microcapsules. This study aims to synthesize a novel bio-based polymer through polycondensation of the natural product honokiol with triethylene glycol divinyl ether, and to evaluate its potential as a herbicide carrier. RESULTS This study successfully synthesized an amphiphilic honokiol-based polymer. The resulting polymer micelle suspension, formed via self-assembly, exhibited a particle size of 130.5 nm, a critical micelle concentration of 3.8 × 10 −3 mg/mL, a drug loading capacity of 13.79%, and an encapsulation efficiency of 82.75%. In vitro release studies demonstrated pH-dependent kinetics, with 80.1% cumulative release of diuron at pH 5.0 over 60 h, compared with only 16.35% at pH 7.0. Herbicidal activity tests against Echinochloa crus-galli demonstrated that the polymer micelle suspension achieved higher mortality rates and fresh weight reduction than diuron dispersion systems, attributable to their rhizosphere-triggered release properties, while significantly enhancing crop seedling safety. CONCLUSIONS This study represents the first successful application of honokiol-based polymers in the field of herbicide delivery. The carrier system exhibits excellent controlled-release properties and synergistic effects, significantly enhancing herbicide utilization efficiency while reducing potential environmental risks. These findings provide a promising strategy and material foundation for developing a new generation of green pesticide formulations. © 2025 Society of Chemical Industry.

Honokiol ameliorates hepatic fibrosis by inducing lysosomal membrane permeabilization and impairing lipophagy in hepatic stellate cells

Zhiyi Wang,Zibo Li,Wenlong Yang,Yuyue Li,Ziyang Huang,Zhenzhen Guo,Erping Xu,Ming Bai,Yucheng Li

Lipophagy in HSCs (hepatic stellate cells) is associated with loss of stellate cell retinol storage and increased β oxidation rate, indicating that the increase in lipophagy serves to provide energy for HSC activation, and contributes to hepatic fibrosis. Honokiol (HNK), a bioactive lignan extracted from Houpoea officinalis, shows effective anti fibrotic and anti inflammatory activities in multiple hepatic diseases. In our study, HNK inhibited activation and induced lipid droplet accumulation in HSC-LX2 cells, without affecting hepatocyte lipid droplets. Fluorescence imaging of EGFP-mCherry-LC3B and lipid staining revealed that HNK suppressed the autophagic degradation of lipid droplets. Notably, Galectin-3 overexpression restored lysosomal function, reduced autophagosome and lipid droplet accumulation, and reversed HNK's effects. Mechanistically, HNK activates Cathepsin B (CTSB) mediated lysosomal associated membrane protein 1 (LAMP1) degradation, thereby promoting lysosomal membrane permeabilization (LMP), impairing lipophagy, and promoting HSC-LX2 inactivation. Besides, TFEB activator 1 attenuated the effects of HNK by reversing HNK induced LAMP1 degradation and restoring lysosomal function. In vivo, HNK ameliorated CCl 4 induced hepatic fibrosis, reduced collagen deposition, and decreased expression of HSC activation markers. In conclusion, HNK induces LMP and impairs lipophagy by activating CTSB mediated LAMP1 degradation, thereby inhibiting HSC activation and ultimately reversing hepatic fibrosis. Our research has further elucidated the mechanisms by which HNK exhibits anti liver fibrotic effects, thereby providing therapeutic strategies and potential candidates for hepatic fibrosis treatment.