Biomass Conversion and Biorefinery
·
2022
·
IF 4.05
Wang Lei,Hu Yang,Guo Guoqing,Li Jie,Fang Xianying,Zhao Linguo
The green extraction and separation of natural produce is a significant part in pharmaceutical industry which has received extensive attention. Comparing with the extraction of hydrophilic products, hydrophobic natural products are further challenging. An extraction means depended in high efficiency hydrophobic deep eutectic solvent (HDES, TCP) was screened by designing ternary HDES. Utilizing the established method, the hydrophobic compound betulin was successfully extracted and recovered from Celtis sinensis leaves. The results showed that HDESs were further productive in extracting hydrophobic compounds than hydrophilic DES. The extractions of TPC were statistically optimized by response surface methodology and central composite design. Under the optimum conditions, the extraction rate of betulin was increased by 125.00% compared with the initial yield. At the same time, it was proved that among the six resins, D-101 macroporous resin had the highest recovery rate of 71.12% for betulin, which was the most effective enrichment and purification method. To sum up, HDES has obvious advantages in the extraction of hydrophobic natural products due to its mild extraction conditions, high yield, and environmental friendliness. At the same time, limitless feasibilities of HDES compositions and their associations furnish a plentiful selection space for the extraction about hydrophobic compounds.
研究领域:
植物化学
·
药用植物学
·
天然产物化学
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DOI
高影响因子
Cell Death Discovery
·
2025
·Vol. 11
·期 1
·1-17
·
IF 7
Wei Guojiang,Huang Ying,Li Wenya,Xie Yuxin,Zhang Deyi,Niu Yuanjie,Zhao Yang
Metabolic reprogramming in prostate cancer has been widely recognized as a promoter of tumor progression and treatment resistance. This study investigated its association with ferroptosis resistance in prostate cancer and explored its therapeutic potential. In this study, we identified differences in the epithelial characteristics between normal prostate tissue and tissues of various types of prostate cancer using single-cell sequencing. Through transcription factor regulatory network analysis, we focused on the candidate transcription factor, SREBF1. We identified the differences in SREBF1 transcriptional activity and its association with ferroptosis, and further verified this association using hdWGCNA. We constructed a risk score based on SREBF1 target genes associated with the biochemical recurrence of prostate cancer by combining bulk RNA analysis. Finally, we verified the effects of the SREBPs inhibitor Betulin on the treatment of prostate cancer and its chemosensitization effect. We observed characteristic differences in fatty acid and cholesterol metabolism between normal prostate tissue and prostate cancer tissue, identifying high transcriptional activity of SREBF1 in prostate cancer tissue. This indicates that SREBF1 is crucial for the metabolic reprogramming of prostate cancer, and that its mediated metabolic changes promoted ferroptosis resistance in prostate cancer in multiple ways. SREBF1 target genes are associated with biochemical recurrence of prostate cancer. Finally, our experiments verified that SREBF1 inhibitors can significantly promote an increase in ROS, the decrease in GSH, and the decrease in mitochondrial membrane potential in prostate cancer cells and confirmed their chemosensitization effect in vivo. Our findings highlighted a close association between SREBF1 and ferroptosis resistance in prostate cancer. SREBF1 significantly influences metabolic reprogramming in prostate cancer cells, leading to ferroptosis resistance. Importantly, our results demonstrated that SREBF1 inhibitors can significantly enhance the therapeutic effect and chemosensitization of prostate cancer, suggesting a promising therapeutic potential for the treatment of prostate cancer.
研究领域:
肿瘤学
·
分子生物学
·
生物信息学
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DOI
PubMed
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
·
2023
·
IF 5.9
Yuhang Zhang,Fengrui Li,Guanhua Guo,Yue Xiu,Honglei Yan,Lixia Zhao,Shuang Gao,Fei Ye,Ying Fu
Betulin is a kind of pentacyclic triterpenoid extracted from the bark of Betula platyphylla, which has the characteristics of anti-inflammatory, antibacterial, antioxidant and so on. However, its poor water solubility limits its application. Betulin/MβCD inclusion complex nanofibers (Betulin/MβCD-IC-NF) were prepared by Methyl-beta cyclodextrin (MβCD) inclusion of betulin and electrospinning techniques. Scanning electron microscopy (SEM) showed that the independent Betulin/MβCD-IC-NF surface was bead-free and smooth. The findings from X-ray diffraction, nuclear magnetic resonance hydrogen spectroscopy, and Fourier transform infrared spectroscopy displayed that an inclusion complex was synthesized containing betulin and MβCD. The results of thermogravimetric analysis displayed that Betulin/MβCD-IC-NF has better stability. The phase solubility study proved that MβCD had the effect of increasing the solubility of betulin. In addition, the DPPH free radical scavenging test and the antibacterial test showed good antioxidant properties and antibacterial properties of Betulin/MβCD-IC-NF, respectively. In conclusion, Betulin/MβCD-IC-NF with high water solubility was obtained by electrospinning, and its thermal stability, antibacterial and antioxidant activity were improved.
研究领域:
材料科学
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药学
·
纳米技术
·
化学
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产品关联
DOI
高影响因子
ACS Applied Materials & Interfaces
·
2018
·
IF 8.097
Ye Chen,Qilei Song,Junpeng Zhao,Xiangjun Gong,Helmut Schlaad,Guangzhao Zhang
Multiblock-like amphiphilic polyurethanes constituted by poly(ethylene oxide) and biosourced betulin are designed for antifouling and synthesized by a convenient organocatalytic route comprising tandem chain-growth and step-growth polymerizations. The doping density of betulin (DB) in the polymer chain structure is readily varied by a mixed-initiator strategy. The spin-coated polymer films exhibit unique nanophase separation and protein resistance behaviors. Higher DB leads to enhanced surface hydrophobicity and, unexpectedly, improved protein resistance. It is found that the surface holds molecular-level heterogeneity when DB is substantially high due to restricted phase separation; therefore, broad-spectrum protein resistance is achieved despite considerable surface hydrophobicity. As DB decreases, the distance between adjacent betulin units increases so that hydrophobic nanodomains are formed, which provide enough landing areas for relatively small-sized proteins to adsorb on the surface.
研究领域:
高分子化学
·
材料科学
·
生物界面工程
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防污涂层
·
可持续聚合物
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DOI
高影响因子
Materials Advances
·
2023
·Vol. 4
·期 9
·2127-2137
·
IF 5
Lusi Zhang,Zhiyuan Ma,Ruili Wang,Weiwei Zuo,Meifang Zhu
Secondary caries is the most common reason for restoration failures in general dental practices, resulting from tooth-adherent cariogenic bacteria in the oral environment. The application of polymerizable quaternary ammonium monomers (QAMs), which are capable of copolymerizing with methacrylate monomers and immobilizing antimicrobials in dental materials simultaneously, is expected to be an attractive anticaries strategy. In this work, three types of bis-quaternary ammonium betulin-based dimethacrylate derivatives (Bis-QADM-Bet) were synthesized via a Menschutkin reaction. Their chemical structures mainly differ for alkyl chain lengths of 4, 8, and 12 carbons (namely C4, C8, and C12). We focused on the fabrication of dental resins with 10 wt% Bis-QADM-Bet and a conventional dimethacrylate-based resin (bisphenol A glycerolate dimethacrylate/tri(ethyleneglycol) dimethacrylate, Bis-GMA/TEGDMA). The relationship between the Bis-QADM-Bet structure and the antibacterial activity, physicochemical properties, and cytotoxicity of dental resins were systematically investigated. The results indicated that regulating the alkyl chain length of Bis-QADM-Bet to C8 led to the formulated resin with superior effectiveness in terms of S. mutans inhibition (p < 0.05). Interestingly, this optimal resin exhibited better flowability and lower cytotoxicity in comparison with the Bis-GMA/TEGDMA based resin without compromising the mechanical properties (p > 0.05). Additionally, the potential antibacterial mechanism of contact-killing was proposed to illustrate the structural–morphological changes of S. mutans. In summary, this work shows that dental restorative resins containing Bis-QADM-Bet with the appropriate alkyl chain length are beneficial toward inhibiting the growth of S. mutans without sacrificing physicochemical performance.
研究领域:
牙科学
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材料科学
·
微生物学
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DOI
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2022
·
IF 5.112
Xin Yu Liu,Dan Li,Tian Yang Li,Yan-Ling Wu,Jing shu Piao,Ming Guan Piao
Targeting hepatic stellate cells (HSCs) can improve the therapeutic efficacy of medicines used to treat hepatic fibrosis. The present work aimed to study the feasibility of homing devices with vitamin A(V A ) chemically attached for delivering betulin(Bt)specifically to HSCs. The manufacture and characterisation of V A modified poly (ethylene glycol) -poly (lactide-co-glycolide) block copolymer micelles loaded with Bt (Bt/ V A PPMs) and their potential therapeutic benefits in vitro and in vivo are described in this paper. Bt/V A PPMs were made in a nearly spherical core-shell configuration with diameters under 200nm. In vitro release study showed that Bt/V A PPMs exhibited steady and continuous release for over 168 hours. Bt/V A PPMs had good biocompatibility at the cellular level, according to the safety evaluation, and elicited no inflammatory response in mice. More importantly, as uptake behavior studied in cells and bioimaging experiments in vivo , Bt/V A PPMs exhibited an instinctive liver- targeting capability to focus on activated HSCs. Efficacy tests revealed that administering Bt/V A PPMs effectively inhibits collagen I expression in LX-2 cells in vitro , and this effect was also seen in a mouse model of liver fibrosis. Overall, results demonstrated that Bt/V A PPMs is a promising drug delivery system that possesses specific HSCs targeting ability for treating hepatic fibrosis.
研究领域:
药学
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生物医学工程
·
肝病学
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产品关联
DOI
PubMed
高影响因子
POLYMER JOURNAL
·
2023
·Vol. 55
·期 3
·203-211
·
IF 2.8
Shi Zhichun,Wen Jiaxiang,Zhao Yingnan,Wang Jianjun,Li Jun,Zhao Ming,Teraguchi Masahiro,Aoki Toshiki,Kaneko Takashi
A novel substituted phenylacetylene with a pendant betulin derivative group was designed and synthesized successfully, and the chemical structure of the monomer was confirmed by nuclear magnetic resonance spectroscopy (NMR, 1 H, 13 C), high-resolution mass spectrometry (HRMS) and Fourier transform infrared spectroscopy (FTIR). The obtained monomer was further polymerized in an achiral [Rh(nbd)Cl] 2 /triethylamine (TEA) catalytic system, and the resulting polymer exhibited a strong Cotton effect at the main-chain absorption regions in the circular dichroism (CD) spectra. This one-handed helical backbone was induced by the chiral source on the side chain and maintained by the rigid betulin derivative pendant flats. Furthermore, the rigid betulin derivatives also contributed to the porous morphology and perfect thermal stability of the polymer. This study will provide a new method for preparing porous chiral polymers as efficient separation materials to solve practical issues.
研究领域:
材料化学
·
有机合成
·
高分子科学
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产品关联
DOI
高影响因子
ACS Applied Polymer Materials
·
2023
·
IF 5
Xiaobo Xu,Xiaozhen Ma,Xiaolin Wang,Jin Zhu,Jinggang Wang,Ning Yan,Jing Chen
Using sustainable biomass feedstock to prepare biobased chemical products is attracting increasing attention. Betulin is a natural cyclic aliphatic diol that can be extracted in large quantities from the bark of birch trees. In this study, a series of bio-based polyurethane (PU) elastomers with excellent mechanical properties, solvent resistance, and thermal stability were synthesized under catalyst-free conditions using betulin and castor oil (CO) as the bio-based polyols. The chemical structure and properties of the bio-based PU elastomers were systematically investigated according to the effect of the hydroxyl ratio between betulin and CO. Due to the presence of abundant hydrogen bonds and rigid ring planes in the PU structure, and a higher cross-link density, the obtained PU elastomers had excellent mechanical properties. They achieved a maximum tensile strength of 31.6 MPa with the tensile strain reaching more than 200% and were able to withstand 1 × 105 times their weight. The thermal decomposition temperature of the betulin-derived PUs was over 300 °C. This study showcased a strategy to synthesize sustainable high-performance PU materials with a high biomass content (>75%).
研究领域:
材料科学
·
化学工程
·
可持续性
·
聚合物化学
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产品关联
DOI
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
·
2026
·
IF 5.6
Zheyu Fang,Kun Xiang,Xinhuang Lv,Qiyao Li,Conghui Dai,Yao Yang,Yan Lin,Jiaming Liu,Jing Sun
Post-stroke cognitive impairment (PSCI) is characterized by progressive cognitive decline following ischemic stroke, and recent studies have suggested that natural compounds may offer therapeutic benefits; however, the effects and mechanisms of Betulin in PSCI remain unclear. Male C57BL/6 mice were subjected to ischemic stroke surgery to induce PSCI and treated with Betulin (50 mg/kg/day) for 3 weeks, followed by assessments of cognitive impairment, pathological changes, and the production of pro-inflammatory cytokines. Network pharmacology and RNA sequencing were performed to explore potential mechanisms. In vitro, BV2 microglia were stimulated with lipopolysaccharide to examine the anti-inflammatory effects of Betulin. Betulin improved cognitive performance, reduced microglial activation, and attenuated neuroinflammation, as evidenced by decreased levels of TNF-α, IL-1β, and IL-6. Mechanistically, the epidermal growth factor receptor (EGFR)/JAK2/STAT3 pathway was identified as a key pathway potentially involved in these effects. Further experiments with EGFR point-mutation constructs indicated that disrupting the Betulin-EGFR interaction attenuated the inhibitory effect of Betulin on the EGFR/JAK2/STAT3 pathway. Collectively, these findings suggest that Betulin mitigates microglia-driven neuroinflammation by targeting EGFR and may represent a potential therapeutic candidate for PSCI.
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产品关联
DOI
PubMed
高影响因子
Journal of Pharmaceutical Innovation
·
2025
·Vol. 20
·期 6
·1-12
·
IF 2.7
Fu Shihua,Luo Zaiyi,Chen Xin,Yang Lingling,Du Xingjie,Chai Kexin,Zhang Yujie,Liu Zhongbing,Jing Pei,Wang Changguang,Lin Yan,Lu Ruilin,Zhong Zhirong
Betulin (BT) is a pentacyclic triterpene with antibacterial, antiviral, and antitumor activity. However, it is insoluble in water and lacks targeting in the in vivo distribution. To improve this situation, this study aims to formulate betulin into nanoparticles (NPs) and further modify it with folic acid (FA) to develop a novel drug-targeting delivery system (FA-BT@NPs). Based on a single-factor experiment, the central composite design was used to optimize the formulation of BT@NPs which was prepared by an emulsion dispersion method. The conjugate of n-hydroxy succinimide with folic acid was used to decorate BT@NPs to prepare the final formulation of FA-BT@NPs. Further, in terms of the nanoparticles with aqueous form, it is still not as convenient and stable as the dry powder form for application and storage, the lyophilization technique was employed to stabilize the preservation of FA-BT@NPs. The results demonstrated the successful preparation of FA-BT@NPs with uniform spherical shapes and good encapsulation efficiency. The lyophilization formulation could preserve the structural integrity and activity of the nanodrugs and facilitate their long-term storage and immediate usability. Our work may lay a solid foundation for the clinical translation of FA-BT@NPs as a potential therapeutic agent for clinical application, highlighting the crucial roles of prescription optimization and advanced formulation technologies in enhancing nanomedicine efficacy. Graphical Folic acid (FA) was activated to form the conjugate with n-hydroxysuccinmide (FA-NHS). The betulin-loaded nanoparticles (BT@NPs) were prepared by emulsion dispersion method. Finally, BT@NPs was conjugated with FA-NHS to form the novel drug-targeting delivery system FA-BT@NPs.
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产品关联
DOI
高影响因子
FOOD CHEMISTRY
·
2025
·
IF 9.8
Shuang Gao,Yu Zhang,Ruichi Wang,Fengrui Li,Yan Zhang,Siyu Zhu,Hailan Wei,Lixia Zhao,Ying Fu,Fei Ye
Active food packaging made from edible materials was considered as a promising alternative to traditional food packaging. Betulin (BE) is a natural active ingredient extracted from the bark of the birch tree, which has anti-inflammation, antibacterial and antioxidant properties. However, the low solubility of BE in water limits its application in active food packaging. In this research, in order to expand the application range of BE, an innovative potentially antimicrobial and antioxidant packaging material was developed. Betulin/hydroxypropyl- beta -cyclodextrin inclusion complex nanofibers (BE/HP β CD-IC-NF) with a stoichiometric ratio of 1:2 was prepared by electrospinning. Scanning electron microscopy results showed a smooth surface with no beads on the free-standing BE/HP β CD-IC-NF. The results of NMR hydrogen spectroscopy, X-ray diffraction and Fourier transform infrared spectroscopy proved that the BE was successfully encapsulated in the cavity of HP β CD. Meanwhile, the results of thermogravimetric analysis and phase solubility studies proved that the BE/HP β CD-IC-NF enhanced the aqueous solubility and thermal stabilization of BE. Fast dissolving experiment proved that the BE/HP β CD-IC-NF was disintegrated rapidly in water. Furthermore, the free radical scavenging activity and antimicrobial test demonstrated that BE/HP β CD-IC-NF has antioxidant properties and good antimicrobial properties, respectively. Meanwhile, in vivo antimicrobial tests on strawberries proved that BE/HP β CD-IC-NF has an effective effect on the preservation and stabilization of fruits. In conclusion, BE/HP β CD-IC-NF prepared in this study can effectively improve thermal stability, aqueous solubility, antibacterial and antioxidant activity of BE, which provides potential for its application in the field of active food packaging.
研究领域:
食品科学
·
材料科学
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产品关联
DOI
PubMed
高影响因子
ACS Applied Polymer Materials
·
2026
·
IF 5.2
Wen-Wen Li,Zi-Yang Yu,Bo Sun,Jimei Ma,Jing Xu,Qiang Li,Zi-Long Li
Biobased polymers have long been recognized as alternatives to fossil-based counterparts. Although tremendous progress in this field has been witnessed in the last decades, performance-advantaged biobased polymers are still rarely reported. Herein, betulin and betulinic acid-derived high glass transition temperature (Tg) thermoplastics are prepared and preliminarily developed as functional materials. At first, norbornene derivatives (monomers M1 and M2) having betulinic units were obtained by means of esterification. Subsequently, homopolymers P1 and P2 in conjunction with statistical copolymers P3-P6 were synthesized via ring-opening metathesis polymerization (ROMP). In spite of their amorphism, these samples all possess Tgs exceeding 202.5 °C owing to the bulkiness and rigidity of their alicyclic pendent groups. Notably, an increase in Tg is observed as the molar fraction of the M1 unit becomes pronounced within the polymer composition. In particular, homopolymer P1 exhibits an exceptionally high Tg at 241.6 °C among alicyclic biobased polymers. Meanwhile, these specimens show good thermal stability, reprocessability, anticorrosiveness, hydrolysis resistance, and high tolerance to boiling water/nonsolvent given the hydrophobicity and structural rigidity of their frameworks. On the other hand, homogeneous mixing inorganic fillers (e.g., toner, magnetite, and terbium-containing particles) with these polymer matrices readily produce colored, magnetic, and phosphorescent hybrid materials. Furthermore, a postmodification strategy was employed to create fluorescent polymer P7 by anchoring pyrene units on the side chains of pristine polymer P1. This modified polymer can be potentially used in information encryption (optical anticounterfeiting).
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DOI
高影响因子
危险品化学品经营许可证（带存储）