Acta Biomaterialia
·
2017
·
IF 6.319
Benkai Qin,Lei Liu,Xiaohe Wu,Fengguang Liang,Tian Hou,Yangyang Pan,Shiyong Song
We prepared an amphiphilic redox-responsive conjugate based on mPEGylated solanesol, solanesyl poly(ethylene glycol) dithiodipropionate (SPDP), along with its inert counterpart solanesyl poly(ethylene glycol) succinate (SPGS), which self-assembled in aqueous solution to form redox-responsive micelles . Used as efficient drug carriers for doxorubicin (DOX), the micelles acted as synergistic agents for cancer therapy. Dynamic light scattering (DLS) measurements showed that the SPDP micelles had average diameters of 111 nm, which decreased to 88 nm after the encapsulation of DOX. The mean diameters and size distribution of the disulfide-containing micelles changed obviously in the presence of the reducing agent glutathione (GSH), whereas no changes occurred in the case of redox-insensitive SPGS micelles. DOX could be loaded into both types of micelles, with drug loading content of about 4.0%. A significantly accelerated release of DOX was triggered by GSH for DOX-loaded SPDP micelles, compared with DOX-loaded SPGS micelles. Blank SPGS and SPDP micelles displayed higher inhibition of HeLa and MCF-7 cell proliferation but less cytotoxicity to normal L-02 cells at similar concentrations. Confocal microscopic observation indicated that a greater amount of DOX was delivered into the nuclei of cells following 9 or 12 h incubation with DOX-loaded micelles. In vivo studies on H22-bearing Swiss mice demonstrated the superior anticancer activity of DOX-loaded SPDP micelles over free DOX and DOX-loaded SPGS micelles. All of the data presented here suggested that these SPDP micelles may have a dual function, as they are preferentially toxic for tumor cells alone and are efficient and safe carriers for anticancer drugs. Statement of Significance Various nanoscale drug carriers were used to enhance therapeutic effect of many drugs. While, the metabolites of high quantities of carriers may cause additional short- or long-term toxicities. In this study, a new systems based on solanesol derivatives was developed for anticancer drug delivery. There are two features for this system. One is solanesol originated bioactivity of the carrier, which will synergistically facilitate therapeutic effect of the encapsulated drug. The other is the redox-responsive drug release behavior adaptable to the glutathione-rich atmosphere of tumor cell. All the hypothesis have been elucidated in this work through in vitro and in vivo studies. It was found that this drug delivery system may have a dual function, as they are preferentially toxic for tumor cells alone and are efficient and safe carriers for anticancer drugs.
研究领域:
药剂学
·
肿瘤学
·
纳米医学
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DOI
PubMed
高影响因子
Food & Function
·
2025
·
IF 5.4
Xiaqing Wu,Huan Chen,Yushan Tian,Hongjuan Wang,Hongwei Hou,Qingyuan Hu,Congyi Wang
Obesity and obesity-related metabolic diseases are causally linked to inflammatory activation. Proinflammatory macrophage infiltration and NLRP3 inflammasome activation contribute to chronic inflammation and insulin resistance. Alleviating inflammatory responses is a reliable method to restore insulin sensitivity and reduce the severity of metabolic syndrome. Solanesol, rich in anti-inflammatory foods (potato, tomato, eggplant, chili peppers), has demonstrated anti-inflammatory properties, but whether it plays a beneficial role in obesity-induced chronic inflammation remains poorly understood. In this study, we investigated the effects of solanesol on the NLRP3 inflammasome and inflammatory responses both in vitro and in high-fat diet (HFD)-fed mice. We found that oral administration of solanesol reduced weight gain, insulin resistance, and inflammation in epididymal white adipose tissue (eWAT) in both HFD-fed obese mice and mice concurrently treated with HFD. This effect was involved with reducing macrophage inflammation and inactivating the NLRP3 inflammasome by reducing K+ efflux and ROS production in macrophages. Solanesol also reprogrammed the phenotype of inflammatory macrophages. Taken together, our study suggests that solanesol may be a promising candidate for treating obesity and obesity-related metabolic diseases.
研究领域:
医学
·
免疫学
·
代谢研究
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2017
·
IF 3.154
Benkai Qin,Lei Liu,Yangyang Pan,Yingchun Zhu,Xiaohe Wu,Shiyong Song,Guang Han
Coenzyme Q10 (CoQ10) is widely used in preventive or curative treatment of cardiovascular diseases. However, CoQ10 exhibits an extremely low solubility in aqueous medium as well as a poor oral bioavailability. Therefore, solanesyl poly(ethylene glycol) succinate (SPGS) and CoQ10 were formulated as CoQ10-SPGS micelles with a high content of CoQ10 to improve the bioavailability of CoQ10 in rat. Findings indicate that, in the CoQ10-SPGS micelles, SPGS is self-assembled into stable nanosized micelles with a CoQ10 loading capacity of more than 39%. The CoQ10-SPGS micelles exhibit an enhanced photostability upon exposure to simulated sunlight. In vivo experiments demonstrate that, as compared to that of the coarse suspensions of CoQ10, there was three-fold enhancement of oral bioavailability for CoQ10-loaded SPGS micelles depending on varying molecular weight of SPGS. In the encapsulation of CoQ10 by SPGS micelles, the self-assembled nanocarriers with strong muco-adhesive properties lead to increases in the solubility and oral absorption of lipophilic CoQ10 nanoparticles.
研究领域:
药剂学
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
LANGMUIR
·
2026
·
IF 4.4
Mingze Xu,Yanwei Yang,Gai Liu,Chunyun Wang,Xu Xu,Bohan Ye,Lei Liu,Xiaoyu Wu,Shiyong Song
Pluronic F127 is widely used in micelle formulations, yet its application is limited by its poor stability and low drug loading capacity. Structural modification of F127 is therefore necessary to overcome these drawbacks. Carrier materials with intrinsic pharmacological activity can reduce metabolism-related toxicity and exert synergistic effects with loaded drugs, offering broad application prospects. Solanesol (SOL), a long-chain unsaturated polyisoprenoid, exhibits antitumor activity and favorable lipophilicity. In this study, a solanesol derivative, monosolanesyl succinate (MSS), was synthesized and conjugated via an amide bond to Pluronic F127 as a hydrophobic segment, forming a pH-sensitive therapeutic nanocarrier. The critical micelle concentration (CMC) of F127-MSS was 10-fold lower than that of F127, indicating a significantly improved stability. The resulting doxorubicin-loaded F127-MSS micelles (F127-MSS-DOX) had an average particle size of approximately 130 nm and a drug loading capacity of ∼ 6.2%, which was about 4 times higher than those of F127-DOX micelles. The F127-MSS-DOX micelles exhibited pH-responsive drug release, promoting drug accumulation at tumor sites while reducing the toxicity in normal tissues. They also demonstrated excellent dilution, plasma, and storage stability. Blank F127-MSS micelles showed inherent inhibitory effects on HepG-2 and MCF-7 cells, attributed to the pharmacological activity of MSS. Furthermore, F127-MSS-DOX micelles displayed potent antitumor activity, comparable to that of free DOX at high concentrations. In vivo studies confirmed that blank F127-MSS micelles moderately suppressed tumor growth, while F127-MSS-DOX micelles significantly inhibited tumor progression and markedly reduced the systemic toxicity of free DOX, owing to their high drug loading, superior stability, pH sensitivity, and synergistic antitumor effect. These findings highlight the great potential of F127-MSS-DOX micelles for tumor treatment.
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2022
·
IF 8.025
Mengying Zhang,Huimin Yu,Jinglu Hu,Zhengyu Zhao,Lei Liu,Gaomin Yang,Tingli Wang,Guang Han,Shiyong Song
The administration of nanodrugs can lead to metabolism related systemic toxicity due to the use of inert carriers in large quantities. Carrier materials that offer therapeutic effects are therefore a promising means of addressing this limitation. Herein, a hyaluronate-based nanocarrier was prepared from hyaluronic acid (HA) and solanesol. Solanesyl thiosalicylate (STS) derived from solanesol has certain antitumor effects and was used to modify HA. The conjugate (HA-STS) self-assembled into nanoparticles acting as a drug carrier. The synthesis of the conjugates was confirmed by 1 H NMR spectroscopy. Doxorubicin (DOX) was loaded into the HA-STS nanoparticles with a relatively high content of 6.0%. pH-sensitive drug release behavior was achieved by introducing a hydroazone bond between STS and HA. A cytotoxicity assay indicated that the blank nanoparticles had an antitumor effect, which was enhanced by loading with an additional drug. Moreover, in vivo antitumor experiments indicated that the HA-STS-DOX showed superior tumor inhibition compared with free DOX, as well as lower cardiotoxicity and hepatotoxicity, demonstrating the advantages of the bioactive drug vehicles in cancer therapy.
研究领域:
药学
·
纳米技术
·
肿瘤学
·
药物递送系统
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
·
2016
·
IF 2.687
Xiaoqin Ma,Zihui Meng,Lili Qiu,Jing Chen,Yushu Guo,Da Yi,Tiantian Ji,Hua Jia,Min Xue
A novel solanesol extraction method based on molecularly imprinted polymer (MIP) as the Flash chromatography stationary phase was established and evaluated. Spherical MIP particles in a size range of 250–350 μm (d (0.5) = 320 μm) for solanesol were synthesized by suspension polymerization, with imprinting factor of 3.9. The MIP particles (5.5 g) were packed in common Teflon column as the stationary phase while the sample solution and elution solvent were confirmed as methanol and methanol/acetic acid solution (80/20, v/v), loading at 4 ml/min and eluting 8 ml/min, respectively. Under the optimal chromatographic conditions, the adsorption capacity of the MIP-Flash column was determined as 107.3 μmol/g, and in each process, 370.8 mg purified solanesol (98.4%) could be obtained from the extract (20 mM, 40 ml) of tobacco leaves (14.7 g), and the yield of solanesol was 2.5% of the dry weight of tobacco leaves. The results reported here confirm the feasibility to extract highly purified active ingredients directly from natural products on a large scale by MIP-Flash chromatography.
研究领域:
植物化学
·
分析化学
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产品关联
DOI
PubMed
高影响因子
Materials Today Communications
·
2022
·
IF 3.662
Hua Yuan,Liming Zhou,Zhiwen Qi,Changwei Zhang,Chengzhang Wang
This study focuses on the development of a new preparation method of solanesol derivatives for their effective use as drug carriers. The current preparation methods for solanesol derivatives generally suffer from poor accessibility and low yields of the target products, which affect the further development of their products. To address this issue, a solanesol-based poly (glutamic acid) (Sol-PEG-PGA) was first designed on the basis of the click reaction between alkynyl-functionalized solanesol and amino-polyethylene glycol (PEG)-azide, followed by a coupling reaction with poly (glutamic acid). The introduced polyethylene glycol and poly (glutamic acid) conferred amphipathic properties on solanesol. Sol-PEG-PGA possessed a suitable lipid-water partition coefficient of 1.01 and water contact angle of 55° and could self-assemble into spherical micelles with an average diameter of 74.0 ± 3.5 nm to load doxorubicin (DOX) via hydrophobic interaction, with a loading capacity of 27.7 ± 1.2 %. Besides, Sol-PEG-PGA micelle exhibited excellent stability before and after loading DOX under the dilution of 1000 times and could be stored stably at room temperature for 15 days. The DOX loaded into Sol-PEG-PGA could be released by acid induction, with a cumulative release of 84.8 ± 2.5 % at pH 5.0. Furthermore, in vitro cytotoxicity assay, the normal cells NIH/3T3 treated with Sol-PEG-PGA maintained relatively high viability of 95.0% compared to that of free DOX at 320 µg/mL, verifying its good biocompatibility. The DOX loaded into Sol-PEG-PGA possessed a high-efficiency anticancer activity compared to free DOX, with an inhibition rate of 99.2 ± 1.6 % against tumor cells 4T1, suggesting the potentials of Sol-PEG-PGA for drug delivery applications. This new preparation method is expected to provide a new strategy for constructing various functional carriers from solanesol derivatives.
研究领域:
药学
·
纳米技术
·
药物递送系统
·
癌症研究
·
材料科学
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产品关联
DOI
高影响因子
CHEMICO-BIOLOGICAL INTERACTIONS
·
2023
·
IF 5.1
Yiqiu Liu,Musen Lin,Xingrui Mu,Lin Qin,Junyu Deng,Ye Liu,Xingqian Wu,Wenjie He,Huiwen Pang,Felicity Han,Chengxin Sun,Xuqiang Nie
S olanesol is a tetra sesquiterpene enol with various biological activities . Modern medical studies have confirmed that solanesol has the function of lipid antioxidation and scavenges free radicals. This study aimed to investigate the protective effect of solanesol against oxidative damage induced by high glucose on human normal hepatocytes (L-02 cells) and its possible mechanism. The results showed that solanesol could effectively improve the decrease of cell viability induced by high glucose, decrease the contents of alanine aminotransferase (ALT), aspartate aminotransferase (AST), and lactate dehydrogenase (LDH) in the extracellular medium, increased the enzyme activities of glutathione peroxidase (GSH-Px), superoxide dismutase (SOD), catalase (CAT), balanced the level of reactive oxygen species (ROS) in cells, inhibited lipid peroxidation of all kinds of biological membranes, and restored mitochondrial membrane potential (MMP). In addition, Solanesol also inhibited the expression of Keap1, promoted the nuclear translocation of Nrf2 by hydrogen bonding with Nrf2, and activated the expression of downstream antioxidant factors NQO1 and HO-1. Altogether, these findings suggest that solanesol may be a potential protectant against diabetic liver injury.
研究领域:
药理学
·
细胞生物学
·
分子生物学
·
糖尿病研究
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产品关联
DOI
PubMed
高影响因子
Metabolites
·
2026
·Vol. 16
·期 8
·541
·
IF 4.5
Qian Li,Lutao Xu,Mingyu Zhu,Gaoge Wang,Huan Chen,Hongwei Hou,Yu Bai
Background: Parkinson’s disease (PD) is characterized by a complex interplay of dopaminergic degeneration, glial activation, and lipid metabolic dysregulation. However, accurately describing how natural product interventions remodel these pathologies across distinct brain regions and cellular microenvironments remains a critical challenge.Methods: We established an integrated multi-omics framework to decode the neuroprotective mechanisms of solanesol (Sol) in an MPTP-induced PD mouse model. We combined single-cell eQTL-based Mendelian randomization (scMR), transcriptomic localization, and virtual knockout analyses to prioritize cell-type-specific regulatory nodes across neuronal, glial, and vascular populations, avoiding the limitations of traditional bulk targeting. In vivo behavioral assays were conducted, alongside orthogonal validation via airflow-assisted desorption electrospray ionization mass spectrometry imaging (AFADESI-MSI) and gene–metabolite co-enrichment analysis, to map regional metabolic networks and structural spatial reprogramming.Results: Computational prioritization highlighted cell-type-specific regulatory nodes including PRKCB, PRKCE, PDGFRB, and FABP3/5. In vivo, Sol attenuated motor and cognitive deficits and largely restored the highly compartmentalized spatial distributions of striatal dopamine, L-DOPA, and acetylcholine. Crucially, AFADESI-MSI and co-enrichment analysis revealed that Sol specifically reversed MPTP-induced spatial disruptions by rescuing key neuromodulatory metabolites—including cervonoyl ethanolamide, phosphatidylcholine species, taurine, and NADHX—which were tightly coupled to sphingolipid signaling, fatty-acid transport, mitochondrial translation, and cell-adhesion pathways. Conclusions: Sol ameliorates PD-like pathology not through a singular target, but by choreographing a spatially and cellularly compartmentalized restoration of lipid–inflammatory homeostasis. Furthermore, our integrated single-cell and spatial metabolomic blueprint sets a new methodological paradigm for elucidating the precise execution programs of natural neurotherapeutics.
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产品关联
DOI
高影响因子
JOURNAL OF AOAC INTERNATIONAL
·
2020
·Vol. 104
·期 2
·479-484
·
IF 1.51
Lan Tao,Yu Congcong,Li Ren,Ma Zheng,Xi Xingjun,Chu Qiao
BackgroundSolanesol is an important pharmaceutical intermediate raw material, mainly used to synthesize coenzyme Q10, vitamin K2. It can be found prominent in potato stems and leaves. But now potato stems and leaves are always abandoned or discarded as they are not suitable for use as feed in aquaculture or other purposes. These agricultural waste resources can be reutilized as the corresponding extracts.ObjectiveTo develop a simple and standardized method for the detection of total solanesol in potato leaves and its extracts.MethodsN-hexane was chosen as the extraction solvent for three times in the solanesol extraction from potato leaves. HPLC-MS was used for the detection.ResultsThe LOQ was 0.3 µg/g and the linear range was from 0.1 to 50 µg/mL. The precision and stability were evaluated by the relative standard deviations (RSDs) of three samples (potato leaves, Extract-1, Extract-2) for interday and intraday. The accuracy of the method was evaluated by the recoveries of three different spiked concentrations of solanesol for three samples, and results showed it ranged from 80.7% to 99.0% with RSDs less than 8.7%.ConclusionsThe method we established can provide a simple and standardized way for the extraction and detection of total solanesol.HighlightsThe work laid a foundation for the resource reutilization of potato stem and leaf.
研究领域:
植物化学
·
分析化学
·
药用植物学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）