FOOD HYDROCOLLOIDS
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2018
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IF 5.089
Fei Zhou,Tao Xu,Yajing Zhao,Huaxin Song,Liuquan Zhang,Xiaodan Wu,Baiyi Lu
The stability and bioavailability of acteoside were improved by encapsulating it with liposomes and chitosan. The liposomes were characterized through transmission electron microscopy , differential scanning calorimetry and Fourier transform infrared spectroscopy , and their particle size, zeta potential , encapsulation efficiency ( EE ), in vitro release, storage stability and oral bioavailability were tested. Results showed that the particles were nanosized and spherical. The average diameter, zeta potential, EE and relative bioavailability ( F rel ) of the acteoside liposome (Ac-Lip) were 78.49 ± 1.44 nm, −4.93 ± 0.79 mV, 81.06 ± 3.48% and 217.62%, respectively. These parameters increased to 92.77 ± 2.99 nm, +19.65 ± 0.90 mV, 88.10 ± 5.36% and 442.84%, respectively, after the surface of Ac-Lip was coated with 2 mg/mL of chitosan (CS-Ac-Lip). In contrast to Ac-Lip, the CS-Ac-Lip showed a reduced in vivo release rate and enhanced storage stability. The chitosan coating increased the diameter, zeta potential, EE , in vivo release time, stability and bioavailability of the Ac-Lip, and the chitosan–liposome is a promising delivery system for transporting acteoside or other bioactive components.
研究领域:
药剂学
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生物医学工程
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF FOOD PROPERTIES
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2018
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IF 1.845
Zhibing Wu,Fengwen Huang,Yutao Chen,Hong Xu,Manjunath D. Meti,Yu Fan,Qingguo G. Han,Haifeng Tang,Zhendan He,Zhangli Hu
The interaction of trypsin with acteoside was studied using ultraviolet visible absorption, fluorescence, synchronous fluorescence, circular dichroism techniques, along with molecular docking method. The fluorescence experiments indicated that acteoside quenched the intrinsic fluorescence of trypsin via a combined quenching process (static and dynamic quenching). The binding constant of acteoside to trypsin obtained was 2.50 × 105 L mol−1 at 298 K and the number of binding site was about one under the same experimental condition. The thermodynamic functions ΔH° and ΔS° of the binding process were 8.79 kJ mol−1 and 132.58 J mol−1 K−1, respectively, which indicated that the hydrophobic force was the main acting force between them. Ultraviolet–visible, synchronous fluorescence together with circular dichroism spectra studies demonstrated that the interaction of acteoside with trypsin lead to a loosening and unfolding of the protein backbone with partial β-sheet structures being transformed into α-helix structures. All these experimental results were validated and explained reasonably by docking studies. And the molecular docking results further illustrated that besides hydrophobic forces, hydrogen bonds also played an important role in the stabilization of the acteoside–trypsin complex. Results from this study should be helpful to make full use of acteoside in the food industry and be useful to the design of the drugs for the diseases related to trypsin.
研究领域:
生物化学
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药物设计
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食品科学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
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IF 8.5
Meng-xiao Wang,Ke-ke Luo,Meng-yao Tian,Wen-ya Gao,Shan Jiang,Yan Zhang,Jian Yang,Nan Si,Shi-lan Ding,Xiao-lu Wei,Yu-yang Liu,Bao-lin Bian,Yan-yan Zhou,Hong-jie Wang
The diagnosis and treatment of chronic glomerulonephritis (CGN) during childhood pose distinct challenges. Acteoside (ACT) is the primary active ingredient extracted from the leaves of Rehmannia glutinosa by our research group, accounting for 2.15 %, which possess multiple biological activities, especially for nephropathy treatment. However, its mechanism intervention on CGN in children remains obscure. In this study, we established a model of purinomycin aminonucleoside (PAN)-induced CGN in childhood rats to assess the potential therapeutic effect and underlying mechanisms of ACT. Leveraging network pharmacology and multi-omics technology, we delved into the effects and mechanisms of ACT intervention on CGN. And these findings were further corroborated through qRT-PCR, western blot and targeted metabolomics. Our results demonstrated that ACT had significantly efficient in the treatment of CGN in childhood rats by improving the key indicators and pathological changes. Further, ACT could significantly regulate differences in endogenous small molecules and genes based on non-target metabolomics and transcriptomics. Meanwhile, target capture analysis found the crucial targets of ACT treatment in CGN. Integrated analysis of multi-omics study indicated that PI3K/Akt signaling pathway and its downstream amino acid metabolism were significantly enriched, hinting at the essential regulatory pathway for ACT in treating of CGN. Finally, through qRT-PCR, western blot and targeted metabolomics, it was verified that ACT could ameliorate CGN through Cxcr4-PI3K-Akt-eNOS signaling pathway, thereby regulating amino acid metabolism. The collective results were consistent with those of multi-omics analysis. Our study illuminated that ACT had notable curative effect on CGN rats, and preliminarily elucidated its mechanism of action. Our research will provide solid basis for the treatment of chronic glomerulonephritis in children with ACT and developing it into innovative traditional Chinese medicine.
研究领域:
药理学
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分子生物学
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肾脏病学
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产品关联
DOI
PubMed
高影响因子
FOOD AND CHEMICAL TOXICOLOGY
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2020
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IF 4.679
Fei Zhou,Weisu Huang,Tao Xu,Lipeng Wu,Qi Chen,Jiyu Peng,Xin Liu,Baiyi Lu
Acteoside is one of the most widespread phenylethanoid glycosides with pharmacological activities , including antioxidant, neuroprotective property, etc. However, its bioavailability is poor due to the low absorption and P-gp efflux. This study aimed to select food derived P-gp inhibitors for promoting the acteoside absorption and investigate whether the inhibitors could increase the bioavailability and stability of acteoside. Results showed that EGCG and quercetin significantly decreased the BL-to-AP efflux and promoted the AP-to-BL influx of acteoside across Caco-2 monolayers with optimum concentrations of 320 μM EGCG or 240 μM quercetin adding to 320 μM acteoside. EGCG increased the bioavailability of acteoside to 1.43-fold, but quercetin had no such effect. Further study showed that EGCG and quercetin had no effects on the storage and digestion stability of acteoside. This work revealed that EGCG could improve the acteoside absorption across the Caco-2 monolayers and enhance the bioavailability of acteoside in rats.
研究领域:
药理学
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营养保健品
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药物递送
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
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2021
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IF 6.165
Helin Xu,Xueqin Li,Yanyan Hao,Xiaoqing Xu,Yan Zhang,Jinli Zhang
Acteoside (ACT) is a bioactive component, which has potential applications in the fields of food, health care, medicine, etc. The development of adsorbents that can efficiently and selectively adsorb ACT is still challenging. Here, polyethyleneimine (PEI) modified heterostructure porous polymer microspheres (HPPM@PEI) were designed and synthesized via a double emulsion interfacial polymerization strategy for efficient adsorption of ACT. HPPM@PEI possessed porous structure with a large pore volume of 1.58 m 3 /g, and PEI moiety was identified on the interior pores and external surface of the microspheres. PEI played two significant roles in the adsorption performance of HPPM@PEI. First, the introduced PEI increased pore volume and specific surface area of HPPM@PEI to provide more adsorption sites. Second, the PEI on interior pores and external surface allowed pH to regulate adsorption capacity and selectivity for ACT on [email protected] /600/2g. The experimental results indicated that [email protected] /600/2g exhibited the highest adsorption capacity of 138.26 ± 8.7 mg/g and selectivity of 6.01 ± 0.16. The adsorption process of ACT can be fitted by pseudo-second-order kinetic and Langmuir isotherm models. The adsorption mechanisms proposed that electrostatic attraction, hydrogen bonding, π-π stacking, and van del Waals were the main interaction forces between [email protected] /600/2g and ACT. This work proposes a novel strategy to synthesize polymer microspheres with large pore volume and high specific surface area for efficient adsorption of bioactive components from plants.
研究领域:
材料科学
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生物化学
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药物开发
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DOI
高影响因子
FOOD CHEMISTRY
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2023
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IF 8.8
Maiquan Li,Mingzhi Zhu,Wei Quan,Weisu Huang,Xia Liu,Can Zhang,Baiyi Lu,Xing Xiao,Zhonghua Liu
Acteoside, an important phenylethanol glycoside, is the main active component in Osmanthus fragrans flower. Our previous study found that acteoside showed high antiaging effect but its absorption rate was low. We speculated acteoside palliated aging-related cognitive impairment before being absorbed, that was intestinal homeostasis underlie the antiaging effect of acteoside. In this study, acteoside was confirmed to palliate cognitive impairment in d -galactose induced aging mice. Acteoside treatment dramatically reduced oxidative stress, alleviated intestinal inflammation, restored intestinal mucosal barrier, rebuilt gut microbiome structure and upregulated gut microbiome metabolites short-chain fatty acids (SCFAs) and amino acids (AAs). Furthermore, antibiotic treatment revealed that the antiaging ability of acteoside was abolished in microbiota depleted mice, which offered direct evidence for the essential role of gut microbiota in the attenuation of cognitive impairment of acteoside. Together, our study indicated that acteoside palliated cognitive impairment by regulating intestinal homeostasisand acteoside intake might be a promising nutritional intervention in prevention of neurodegenerative diseases.
研究领域:
药理学
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神经科学
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胃肠病学
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微生物学
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DOI
PubMed
高影响因子
Frontiers in Chemistry
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2020
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IF 3.693
Zhao Xiaobin,Cheng Yun,Xu Helin,Hao Yanyan,Lv Yin,Li Xueqin
Acteoside (ACT) belongs to a type of phenylethanoid glycosides (PhGs), and it is worthy of obtaining high-purity due to its significant medicinal functions. In this study, a novel class of MIMs was designed and synthesized with PVDF membranes as the base membrane for high selective separation and enrichment of ACT. The effects of the different functional monomers, the amounts of functional monomers, crosslinking agents, and initiators on the separation properties of MIMs were investigated. Furthermore, adsorption ability, permeation capacity, and reusability of MIMs were discussed for ACT. It indicated that MIM7 was the optimal performance of MIMs. The adsorption ability of MIM7 for ACT was 62.83 mg/g, and the selectivity factor (α) of MIM7 was up to 2.74 and its permeability factor (β) was greater than 2.66. Moreover, the adsorption amount of MIM7 was still more than 88.57% of the initial value after five cycles. As an ACT imprinted layer of MIMs only had recognition sites for ACT molecules, which recombined with the recognition sites in the membrane permeation experiment, ACT molecules penetration was hindered. However, the analogs of ECH successfully passed MIMs. It indicated that the selective MIMs for ACT followed the mechanism of delayed permeation. This work provides an important reference for the high permselective separation of natural products.
研究领域:
药学
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分离科学与技术
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产品关联
DOI
PubMed
高影响因子
MICROPOROUS AND MESOPOROUS MATERIALS
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2022
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IF 5.876
Yu Sun,Yanyan Hao,Xueqin Li,Zhong Wei
In this study, a series of amphiphilic hypercrosslinked β-cyclodextrin polymers (AHβ-CDPs) were synthesized by the hypercrosslinked strategy for acteoside (ACT) separation. Amphiphilic β-cyclodextrin (β-CD) had rigid ring structures, which constructed the rigid networks of AHβ-CDPs. AHβ-CDPs with rigid networks improved adsorption performance for two reasons. On one hand, the hydrophilic ACT was preferentially adsorbed on the hydrophilic outer surface of β-CD, and the hydrophobic molecules were encapsulated in the hydrophobic cavity, improving adsorption selectivity. On the other hand, the constructed rigid networks of AHβ-CDPs with affinity groups provided large specific surface area (1281.16 m 2 /g) and abundant pore structure , increasing additional transport pathways and affinity sites for enhancing adsorption capacity. The experimental results showed the as-prepared AHβ-CDPs-4 had the highest adsorption capacity of 288.36 ± 2.12 mg/g and the selectivity of 4.36 ± 0.11. Therefore, amphiphilic hypercrosslinked adsorbents with rigid networks had potential application for bioactive components separation from natural products.
研究领域:
材料科学
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天然产物化学
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生物分离技术
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DOI
高影响因子
Applied Biological Chemistry
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2022
·Vol. 65
·期 1
·1-12
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IF 3.206
Zhang Yifan,Shen Jinhuang,Ma Xinhua,Yao Mingshuang,Zhang Yonghong,Cao Dairong
Acanthus ilicifolius var. xiamenensis (Acanthaceae), a mangrove found in southeastern China, is an herb with strong antiinflammatory property. Phytochemical study of the mangrove showed that the plant has a high content of phenylethanol glycoside acteoside (AC). In this research, the anti-inflammatory activity of acteoside on dextran sodium sulphate (DSS)-mediated mouse ulcerative colitis model were studied. For DSS- mediated colitis in mice, AC can reduce weight loss and DAI score in UC mice, suppress colon shortening and alleviate colon pathological injury. Moreover, AC treatment notably up-regulates IL-10, down-regulates the levels of IL-1β and TNF-α, and inhibits the protein expression of JAK2/STAT3, NF-κB p65, IKKα/β and IKB of colon. In addition, after AC treatment, the level of MDA and NO in colonic tissue were remarkably decreased, while the levels of GSH, SOD, and Nrf2 and HO-1 protein expression levels were significantly increased. These results indicate that AC can activate the Nrf2 signaling pathway by inhibiting the JAK/STAT, iNOS/eNOS and NF-κB signaling cascades, enhance the intestinal barrier function, and effectively reduce DSS-induced UC in mice.
研究领域:
药理学
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免疫学
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分子生物学
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DOI
高影响因子
Heliyon
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2022
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IF 3.776
Jing Guo,Qiao-Zhou Liu,Fang-Juan Zhu,Min Li,Jiao Li,Li Guo,Qian-Yun Sun,Qing-Xiong Yang
Background Acteoside, a water-soluble active constituent of diverse valuable medicinal vegetation, has shown strong anti-inflammatory property. However, studies on the anti-inflammatory property of acteoside in complement-induced acute lung injury (ALI) are limited. Therefore, this study aims to evaluate the anti-inflammatory activity of acteoside in cobra venom factor (CVF)-stimulated human microvascular endothelial cells (HMEC) and in ALI mice model. Methods In this study, we investigated the effects of acteoside (20, 10, and 5 μg/mL) in vitro in CVF induced HMECs and the activity of acteoside (100, 50, and 20 mg/kg/day bodyweight) in vivo in CVF induced ALI mice. Each eight male mice were orally administered acteoside or the positive drug PDTC (100 mg/kg/day) for 7 days before CVF (35 μg/kg) injection. After injection for 1 h, the pharmacological effects of acteoside were investigated by spectrophotometry, pathological examination, enzyme-linked immunosorbent assay, and immunohistochemistry. Results In vitro , acteoside (20, 10, and 5 μg/mL) reduced the protein expression of adhesion molecules and pro-inflammatory cytokines and transcriptional activity of NF-κB ( P < 0.01). In vivo studies showed that acteoside dose-dependently alleviated lung histopathologic lesion, inhibited the production of the protein content of BALF, leukocyte cell number, lung MPO activity, and expression levels of IL-6, TNF-α, and ICAM-1, and suppressed the C5b-9 deposition and NF-κB activation in CVF-induced acute lung inflammation in mice ( P < 0.05, 0.01). Conclusion This study demonstrates that acteoside exerts strong anti-inflammatory activities in the CVF-induced acute lung inflammation model and suggests that acteoside is a potential therapeutic agent for complement-related inflammatory diseases.
研究领域:
药理学
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免疫学
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肺科学
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炎症研究
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DOI
PubMed
高影响因子
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
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2021
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IF 4.013
Yuanyuan Wu,Mengnan Zeng,Ruiqi Xu,Beibei Zhang,Shengchao Wang,Benke Li,Yuxuan Kan,Bing Cao,Xiaoke Zheng,Weisheng Feng
Background Melanoma is an aggressive cancer with a rapidly increasing incidence rate worldwide. Acteoside has been shown to have antitumor effects in multiple human cancers; however, the underlying function and mechanisms of acteoside in melanoma remain unclear. Purpose This study explored the inhibitory effect of acteoside on melanoma and the possible mechanisms. Methods Acteoside (15 mg/kg, 30 mg/kg) was administered to mice daily for 21 days. ICI182,780 (0.5 mg/kg) was intraperitoneally injected 30 min before acteoside administration three times a week to evaluate whether the effects elicited by acteoside were mediated via the estrogen receptor . Tumor growth and metabolism, cardiac function, ROS and apoptosis levels in the spleen, serum inflammatory factors, and immune cells in the spleen were monitored. STAT3 , p-STAT3, CD31 , and survivin levels in tumor tissues were measured via immunofluorescence. Ras, Raf1, STAT3, p-STAT3, Bcl-2, Bax, cleaved caspase-3, and cleaved caspase-9 levels in tumor tissues were determined via Western Blotting . Results The results showed that acteoside inhibited melanoma growth, alleviated inflammation levels in mice, attenuated ROS and apoptosis levels in the spleen, downregulated the levels of CD31, survivin, Ras, Raf1, p-STAT3, and Bcl-2, and upregulated the levels of ER β , Bax, cleaved caspase-3, and cleaved caspase-9. Moreover, the effect of acteoside was blocked by ICI182,780. Conclusion Acteoside may promote the apoptosis of tumor cells by regulating the ER β -Ras/Raf1-STAT3 signaling axis, thus inhibiting the occurrence and development of melanoma.
研究领域:
肿瘤学
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药理学
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分子生物学
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免疫学
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DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
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2026
·
IF 5.7
Meng Wang,Che Wang,Zhihao Liu,Xiaoyu Du,Lu Tian,Qi Li,Feng Zhang,Yingxiang Chen,Chengzhi Lu
Acteoside attenuates doxorubicin-induced cardiotoxicity and ferroptosis. • Acteoside preserves mitochondrial function in doxorubicin-exposed cardiomyocytes. • Acteoside promotes KEAP1 degradation and activates NRF2 signaling. • NRF2 inhibition attenuates the cardioprotective and anti-ferroptotic effects of ACT. : Doxorubicin (DOX)-induced cardiotoxicity (DIC) is a major limitation to the clinical use of DOX, highlighting the need for effective cardioprotective strategies. Although acteoside (ACT), a natural compound with antioxidant properties, has shown potential cardioprotective effects, its role in DIC, particularly in the regulation of ferroptosis, remains unclear. This study therefore investigated the protective effects of ACT against DIC and the underlying molecular mechanisms. Using C57BL/6 mice in vivo and H9c2 cells in vitro, we evaluated cardiac function, myocardial injury and histopathological alterations, ferroptosis-related changes, and key regulatory proteins. ACT significantly attenuated DOX-induced cardiac dysfunction, myocardial injury, and fibrosis. These protective effects were accompanied by suppression of ferroptosis, as evidenced by reduced iron accumulation and lipid peroxidation and restored expression of glutathione peroxidase 4 (GPX4) and the cystine/glutamate transporter (xCT). ACT also preserved mitochondrial membrane potential and reduced mitochondrial reactive oxygen species (ROS) levels, thereby alleviating mitochondrial dysfunction. Mechanistically, ACT may interact with Kelch-like ECH-associated protein 1 (KEAP1) and promoted KEAP1 degradation, thereby facilitating the nuclear translocation of nuclear factor erythroid 2-related factor 2 (NRF2) and increasing the expression of downstream antioxidant proteins, including heme oxygenase-1 (HO-1). Moreover, the NRF2 inhibitor ML385 significantly attenuated the protective effects of ACT, supporting the involvement of NRF2 signaling in ACT-mediated cardioprotection. Collectively, these findings suggest that ACT protects against DIC, at least in part, by promoting KEAP1 degradation, activating NRF2 signaling, and suppressing ferroptosis. This figure summarizes the mechanism by which ACT alleviates DOX-induced cardiotoxicity through the suppression of ferroptosis. ACT promotes KEAP1 degradation, reduces KEAP1-mediated NRF2 degradation, and enhances NRF2 nuclear translocation and downstream antioxidant and anti-ferroptotic signaling. These effects upregulate HO-1, xCT, and GPX4, reduce lipid ROS accumulation, improve mitochondrial function, and suppress cardiomyocyte ferroptosis. Collectively, the cardioprotective effects of ACT are mediated, at least in part, through activation of the KEAP1/NRF2 axis. Download: Download high-res image (175KB) Download: Download full-size image
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高影响因子
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