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Gut microbiota: The pivotal conduit in the onset of constipation and its alleviation by tea flower polysaccharides (TFP) in a mouse model.
IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-04-01 Epub Date: 2025-02-07 DOI: 10.1016/j.ijbiomac.2025.140808
Tingbo Wu, Fanfen Song, Jiahong Huang, Shumao Cui, Linlin Wang, Qin Yang, Yuanyuan Wu, Bo Li, Youying Tu, Xiaochun Wan, Junsheng Liu

Plant-derived bioactive components, such as polysaccharides, provide promising alleviating effects on constipation with minimal side-effects compared to pharmacological interventions. This study aimed to explore the therapeutic potential of tea flower polysaccharides (TFP) on constipation and the involved mechanisms. In a loperamide-induced constipation mouse model, TFP administration significantly increased fecal water content from 54.23-57.30 % to 63.70-79.36 %, enhanced intestinal transit rate from 30.80 % to 38.81 %, and reduced gastrointestinal (GI) transit time from 234.4 min to 186.2 min. TFP restored levels of both excitatory and inhibitory hormones related to GI motility. Transcriptomic analysis of colonic epithelial cells revealed that TFP restored expression of 544 genes involved in various pathways, including the NF-κB and JAK-STAT signaling pathways, which are associated with the improvement of constipation. Gut microbiota analysis demonstrated that TFP mitigated dysbiosis by normalizing the Firmicutes/Bacteroidota ratio, inhibiting pathogenic genera (e.g., Helicobacter), and promoting beneficial genera (e.g., Muribaculaceae, Bacteroides, Parabacteroides). The mediating role of gut microbiota in the onset of constipation and its alleviation was confirmed through fecal microbiota transplantation (FMT). Furthermore, TFP and its combination with anti-constipation drugs alleviated constipation-induced hepatorenal damage. This study highlights TFP's potential in treating constipation and underscores the essential role of gut microbiota in its therapeutic effects.

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引用次数: 0
Selectively oxidized chitin as a degradable and biocompatible hemostat for uncontrolled bleeding and wound healing.
IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-04-01 Epub Date: 2025-02-10 DOI: 10.1016/j.ijbiomac.2025.140906
Ruochen Ding, Zhan Shu, Jian Yang, Ren Chen

Chitin (CT), one of the most abundant biopolymers, is insoluble in both dilute aqueous solutions and common organic solvents. In traditional hemostatic applications, chitin must be either converted into acid-soluble chitosan by removing acetyl groups or dissolved in an alkaline aqueous solution at -20 °C. However, acetyl groups are more advantageous than amino groups in promoting hemostasis, biocompatibility, biodegradability, and wound healing. A significant challenge remains in retaining acetyl groups while directly preparing a hemostatic agent from chitin without requiring its dissociation. In this study, we have successfully applied oxidized chitin (OCT) as a hemostatic material, which is directly derived from chitin through a TEMPO-mediated selective oxidation of C6 primary hydroxyl groups to carboxyl groups. Due to its significantly higher hydrophilicity compared to chitin, OCT rapidly forms a gel upon contact with blood, efficiently sealing broken blood vessels and facilitating wound healing. Among OCTs with varying carboxylate contents and the commercial chitosan hemostat Celox™, OCT-24 demonstrated not only the best hemostatic performance in some injury models but also excellent biocompatibility and biodegradability, effectively preventing tissue adhesion and promoting wound healing. The selective oxidation offers a straightforward method for developing a highly effective hemostatic material from chitin to address uncontrolled massive bleeding.

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引用次数: 0
Inhibitory activity and mechanisms of chitosan against Fusarium avenaceum, a pathogen causing Angelica root rot disease.
IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-04-01 Epub Date: 2025-01-27 DOI: 10.1016/j.ijbiomac.2025.140249
Yaya Cheng, Saimai Ma, Jianmei Dong, Wenwen Zhang, Yanjun Ma, Aimei Zhang, Hai Peng, Fujun Han, Weibao Kong

The polysaccharide chitosan possesses broad-spectrum antimicrobial properties and has proven effective in controlling various postharvest diseases in fruits. Nevertheless, the fundamental mechanisms underlying its action remain unclear. In this study, the antifungal effects of chitosan with different molecular weights against Fusarium avenaceum, a pathogen causing root rot in Angelica sinensis, were evaluated. Additionally, the potential mechanisms of these effects were explored at the microstructural and transcriptomic levels. Notably, low-molecular-weight chitosan (20 kDa) exhibited superior antifungal activity when compared to high-molecular-weight chitosan (500 kDa and 1000 kDa). The half-maximal inhibitory concentration (IC50) of 20, 500, and 1000 kDa chitosan were 0.2103, 0.2183, and 0.2707 g/L, respectively. Morphological and physiological experiments demonstrated that chitosan can inhibit the growth of F. avenaceum by decreasing spore germination, destroying mycelial morphology and microstructure, and promoting the release of intracellular electrolytes. RNA sequencing revealed considerable changes in the transcriptomic profile of F. avenaceum after chitosan treatment, with 2030 genes being differentially expressed. Subsequent KEGG pathway analysis demonstrated that genes associated with translation, human diseases, and transcription were upregulated in F. avenaceum after chitosan treatment. In contrast, genes associated with carbohydrate and amino acid metabolism, cellular processes, exogenous substance degradation and metabolism, and the metabolism of cofactors and vitamins were downregulated. Collectively, these results indicated that chitosan may influence the growth of F. avenaceum by disrupting protein biosynthesis and key metabolic pathways. These findings highlight the substantial potential of chitosan as an alternative agent for the management of fungal diseases in plants used in Chinese herbal medicine.

甲壳素多糖具有广谱抗菌特性,已被证明可有效控制水果的各种采后病害。然而,其作用的基本机制仍不清楚。本研究评估了不同分子量的壳聚糖对引起当归根腐病的镰刀菌(Fusarium avenaceum)的抗真菌作用。此外,还从微观结构和转录组水平探讨了这些作用的潜在机制。值得注意的是,与高分子量壳聚糖(500 kDa 和 1000 kDa)相比,低分子量壳聚糖(20 kDa)表现出更高的抗真菌活性。20 kDa、500 kDa 和 1000 kDa 壳聚糖的半最大抑制浓度(IC50)分别为 0.2103、0.2183 和 0.2707 g/L。形态学和生理学实验表明,壳聚糖能通过降低孢子萌发率、破坏菌丝形态和微结构以及促进细胞内电解质的释放来抑制venaceum蝇的生长。RNA 测序显示,壳聚糖处理后,venaceum 的转录组概况发生了很大变化,有 2030 个基因表达不同。随后的 KEGG 通路分析表明,壳聚糖处理后,与翻译、人类疾病和转录相关的基因在 F. avenaceum 中上调。相反,与碳水化合物和氨基酸代谢、细胞过程、外源物质降解和代谢以及辅助因子和维生素代谢相关的基因则出现了下调。总之,这些结果表明壳聚糖可能会通过破坏蛋白质的生物合成和关键代谢途径来影响酵母菌的生长。这些发现凸显了壳聚糖作为中药植物真菌疾病防治替代药物的巨大潜力。
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引用次数: 0
Mechanism of dsDNA binding, enzyme inhibition, antioxidant activities, and molecular docking studies of taxifolin, daidzein, and S-equol.
IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-04-01 Epub Date: 2025-01-27 DOI: 10.1016/j.ijbiomac.2025.140314
Derya Kılıçaslan

This study investigated the binding mechanism of taxifolin (TA), daidzein (DA), and S-equol (SQ) flavonoids with fish sperm double helix DNA (dsDNA) under the simulated physiological pH condition using UV-Vis and photoluminescence spectroscopy, as well as viscometric methods. Binding constants (Kb) for the flavonoids to dsDNA were determined as 1.8 × 104 M-1 for SQ, 1.6 × 104 M-1 for DA and 1.7 × 104 M-1 for TA, indicating moderate affinity. The groove binding mode was confirmed by competitive binding studies with ethidium bromide or rhodamine B, UV-Vis spectrophotometry and viscosity evaluation. Additionally, the compounds showed high cholinesterase (ChE) inhibitory activity, with TA being the most potent, particularly against BChE (IC₅₀ = 2.93 μM) and AChE (IC₅₀ = 6.42 μM). Antioxidant activities were also evaluated using DPPH and ABTS assays, with TA showing the lowest IC₅₀ values. Additionally, molecular docking studies were performed to assess the interactions and binding affinities of all compounds with AChE and BChE enzymes. As a result, the studied compounds were found to prefer minor groove binding. This research analyzed the contribution of the structure-activities of natural flavones in terms of their biological properties, which is important for their future application against diseases.

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引用次数: 0
Nanocomposite TiO2/ZnO/chitosan by method sol-gel for self-cleaning application.
IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-04-01 Epub Date: 2025-01-20 DOI: 10.1016/j.ijbiomac.2025.140076
R Novra Gabriela, Heryanto Heryanto, Dahlang Tahir

TiO2/ZnO/Chitosan coated cotton fabric as a self-cleaning, which has been synthesized by various concentrations of TiO2: 0.5 g, 1 g, and 2 g through the sol-gel method at pH 9. The self-cleaning test was conducted on TiO2/ZnO/Chitosan-coated cotton fabric samples by irradiating for 15 h using UVA-UVB lamps with clothing stain dye. TiO2/ZnO/Chitosan composite's structural properties were analyzed from X-ray diffraction (XRD) spectra, chemical bonding by Fourier Transform Infrared (FTIR), and bandgap by quantitative analysis from UV-visible spectroscopy. The XRD diffraction peaks showed a slight shift to the right, except for the sample with the highest TiO2 concentration, which showed a more significant shift. FTIR spectra showed the presence of Ti-O-Ti bonds at wavenumbers 500 cm-1 - 700 cm-1, which identified the presence of TiO2, and at wavenumber 3485 cm-1, which was used for stretching-OH and -NH2 of chitosan. The band gaps were 5.64 eV, 5.63 eV, and 5.58 eV for TiO2: 0.5 g, 1 g, and 2 g, respectively. The self-cleaning test showed that the best results were in the TiO2 sample with a concentration of 2 g at pH 9, where the dye successfully disappeared after exposure to UVA-UVB lamps for 15 h of irradiation.

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引用次数: 0
Preparation of interpenetrating networks from chitosan and poly(hydroxypropyl methacrylate) or p(hydroxyethyl methacrylate) for controlled release of doxorubicin and curcumin: Investigation of potential use in wound dressing.
IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-04-01 Epub Date: 2025-02-11 DOI: 10.1016/j.ijbiomac.2025.140929
Fatemeh Shakouripour, Ali Olad, Gulay Bayramoglu

The IPNs hydrogel films based on chitosan (CS), 2-hydroxyethyl methacrylate (HEMA), and 2-hydroxypropyl methacrylate (HPMA) were prepared, and their potential for drug delivery and wound dressing was evaluated. The characterizations of the IPNs were examined through swelling tests, FTIR, DSC, SEM, mechanical properties, and BET analyses. The percent swelling of the CS/p(HEMA)1 and CS/p(HPMA)1 were obtained as 240 % and 110 %, respectively. The release behavior of prepared hydrogel formulations was investigated in two different pH values for DOX and CUR at pH 5.5 and 7.4, respectively, at varying drug concentrations. In vitro, drug release profiles revealed a time-dependent release pattern, with a maximum release observed at 48 h for all formulations. Among the IPNs, CS/p(HEMA)1 formulation containing CS/HEMA in a 1:1 ratio showed the highest drug release rates of 76.0 % for doxorubicin and 75.5 % for curcumin. MTT assays revealed that the IPNs formulations exhibit enhanced interaction with drugs, leading to an improved drug release rate. A marked decrease in cell viability was observed as the concentration of both drugs increased for testing the ATCC-CRL 2451 leukemia cell line in the prepared formulations. These findings highlight the potential of these composite hydrogels as efficient drug delivery systems for wound dressing applications.

制备了基于壳聚糖(CS)、甲基丙烯酸羟乙酯(HEMA)和甲基丙烯酸羟丙酯(HPMA)的 IPNs 水凝胶薄膜,并评估了它们在药物输送和伤口敷料方面的潜力。通过溶胀试验、傅立叶变换红外光谱、DSC、扫描电子显微镜、机械性能和 BET 分析,考察了 IPNs 的特性。CS/p(HEMA)1 和 CS/p(HPMA)1 的膨胀率分别为 240 % 和 110 %。在两种不同的 pH 值(pH 值分别为 5.5 和 7.4)和不同的药物浓度下,研究了制备的水凝胶配方对 DOX 和 CUR 的释放行为。体外药物释放曲线显示出与时间相关的释放模式,所有制剂在 48 小时内均观察到最大释放。在这些 IPN 中,含有 CS/HEMA 的 CS/p(HEMA)1 制剂的药物释放率最高,多柔比星为 76.0%,姜黄素为 75.5%。MTT 分析表明,IPNs 制剂与药物的相互作用增强,从而提高了药物释放率。在制备的制剂中测试 ATCC-CRL 2451 白血病细胞系时,随着两种药物浓度的增加,观察到细胞活力明显下降。这些发现凸显了这些复合水凝胶作为伤口敷料应用的高效给药系统的潜力。
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引用次数: 0
Targeting JAK/STAT3 in glioblastoma cells using an alginate-PNIPAm molecularly imprinted hydrogel for the sustained release of ruxolitinib. 利用海藻酸盐- pnipam分子印迹水凝胶靶向胶质母细胞瘤细胞中的JAK/STAT3,缓释ruxolitinib。
IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-04-01 Epub Date: 2025-01-17 DOI: 10.1016/j.ijbiomac.2025.140025
Alexandra-Iulia Bărăian, Lajos Raduly, Oana Zănoagă, Bogdan-Cezar Iacob, Lucian Barbu-Tudoran, Elena Dinte, Ioana Berindan-Neagoe, Ede Bodoki

Glioblastoma (GBM) is a notoriously aggressive primary brain tumor characterized by elevated recurrence rates and poor overall survival despite multimodal treatment. Local treatment strategies for GBM are safer and more effective alternatives to systemic chemotherapy, directly tackling residual cancer cells in the resection cavity by circumventing the blood-brain barrier. Molecularly imprinted polymers (MIPs) are promising drug delivery systems due to their high-affinity binding cavities that enable tailored release kinetics. This study reports the development of a semi-synthetic polysaccharide MIP-based hydrogel intended for the post-surgical management of GBM. The biodegradable implant, made of calcium-crosslinked alginate-poly(N-isopropylacrylamide) graft copolymer, was designed for the sustained release of ruxolitinib (RUX) in the resection cavity, targeting the Janus kinase/Signal Transducer and Activator of Transcription-3 signaling pathway. The molecularly imprinted hydrogel demonstrated thermo-thickening and shear-thinning behavior, high entrapment efficiency of RUX (84.59 ± 0.73 %), and sustained release over 14 days, underscoring the advantages that molecular imprinting of the alginate matrix provides compared to conventional MIPs. The dose-dependent inhibitory effects of the imprinted hydrogel against U251 and A172 GBM cells were demonstrated by increased apoptosis, reduced confluence, colony formation, and delayed wound healing, whereas the non-imprinted hydrogel was biocompatible. The MIP hydrogel could be a safe and effective GBM treatment.

胶质母细胞瘤(GBM)是一种众所周知的侵袭性原发性脑肿瘤,其特点是复发率高,尽管采用了多种治疗方法,但总生存率较低。GBM的局部治疗策略是比全身化疗更安全、更有效的替代方案,通过绕过血脑屏障直接处理切除腔内残留的癌细胞。分子印迹聚合物(MIPs)是一种很有前途的药物传递系统,因为它们具有高亲和力的结合腔,可以实现定制的释放动力学。本研究报道了一种半合成多糖mip基水凝胶的开发,用于GBM的术后治疗。生物可降解植入物由钙-交联海藻酸盐-聚(n-异丙基丙烯酰胺)接枝共聚物制成,设计用于ruxolitinib (RUX)在切除腔内的缓释,靶向Janus激酶/信号传感器和转录-3信号通路的激活物。分子印迹的水凝胶表现出热增厚和剪切减薄的行为,RUX的高捕获效率(84.59 ± 0.73 %),持续释放超过14 天,强调了海藻酸盐基质分子印迹与传统mip相比的优势。印迹水凝胶对U251和A172 GBM细胞的抑制作用呈剂量依赖性,表现为细胞凋亡增加、融合减少、集落形成和伤口愈合延迟,而非印迹水凝胶具有生物相容性。MIP水凝胶是一种安全有效的GBM治疗方法。
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引用次数: 0
Effect of bioactive Rosa roxburghii Tratt fruit polysaccharide on the structure and emulsifying property of lactoferrin protein. 活性刺梨果多糖对乳铁蛋白结构及乳化性能的影响。
IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-04-01 Epub Date: 2025-01-19 DOI: 10.1016/j.ijbiomac.2025.140016
Wang Pingping, Du Yutong, Chai Xianghua, Chen Chun, Wu Kegang, Fu Xiong

Lactoferrin protein (LF) is a natural protein with certain emulsifying ability, but is sensitive to be affected by environmental factors and has poor oxidative stability to be used as emulsifier. In this study, the emulsifying ability of LF was significantly improved after conjugation with Rosa roxburghii Tratt fruit polysaccharides (RTFP), and the emulsion stability mechanism of LF-RTFP conjugates (L-R) were elucidated through the utilization of CLSM (confocal laser scanning microscopy), interfacial tension, apparent viscosity, and protein adsorption rate. The emulsion stabilized by L-R showed the smaller particle size (17.17 ± 0.13 μm), which reduced by 51 % compared with that of LF. After conjugation with RTFP, the hydrophobic amino acids that are originally inside the structure of LF would be exposed on the protein surface. In addition, the protein adsorption rate of L-R stabilized emulsion interface was 62.70 ± 0.71 %, 2.4 times higher than that of LF. The optical microscopy and CLSM experiments indicated that the glycosylation with RTFP increased the bridged flocculation and further formed gel network structure in the emulsion stabilized by LF. These findings suggested that the novel emulsifier prepared by the Maillard reaction between LF and RTFP showed potential to stable emulsion.

乳铁蛋白(LF)是一种具有一定乳化能力的天然蛋白,但对环境因素的影响比较敏感,氧化稳定性差,不能作为乳化剂。本研究利用共聚焦激光扫描显微镜(CLSM)、界面张力、表观粘度和蛋白质吸附率等指标,对LF-RTFP偶联物(L-R)的乳化稳定性机理进行了研究。L-R稳定乳状液的粒径较小(17.17 ± 0.13 μm),比LF稳定乳状液减小了51 %。与RTFP结合后,原存在于LF结构内部的疏水氨基酸暴露在蛋白表面。L-R稳定乳状液界面对蛋白质的吸附率为62.70 ± 0.71 %,是LF的2.4倍。光学显微镜和CLSM实验表明,RTFP的糖基化增加了桥式絮凝,进一步形成了LF稳定乳状液中的凝胶网络结构。这些结果表明,由LF和RTFP之间的美拉德反应制备的新型乳化剂具有稳定乳液的潜力。
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引用次数: 0
Corrigendum to "Characterization and functional properties of walnut protein fibrils for enhanced bioaccessibility of CoQ10 and ALA" [International Journal of Biological Macromolecules, Volume 285 (2025), 138171]. “增强辅酶q10和ALA生物可及性的核桃蛋白原纤维的表征和功能特性”[国际生物大分子杂志,285(2025),138171]。
IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-04-01 Epub Date: 2025-01-20 DOI: 10.1016/j.ijbiomac.2025.139960
Xiaoyu He, Li Zhang, Minjie Cao, Yiwen Guo, Jie Mi, Zhu Zhu, Yuehao Song, Ming Chang, Ruijie Liu, Xingguo Wang
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引用次数: 0
Cobalt polygalacturonates and the pharmacological composition based on them: Preparation, properties and cytotoxicity.
IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-04-01 Epub Date: 2025-01-27 DOI: 10.1016/j.ijbiomac.2025.140377
Salima T Minzanova, Evgenii V Chekunkov, Anna V Khabibullina, Lubov G Mironova, Alexandra D Voloshina, Anna P Lyubina, Kirill V Kholin, Guliya R Nizameeva, Airat R Khamatgalimov, Vasili A Milyukov

The aim of the present study was to obtain new metal complexes of citrus pectin with cobalt ions based on potassium polygalacturonate and to prepare a new pharmacological composition (PC) PGKCo: PGNaCo (1:1) with antitumor activity based on potassium cobalt polygalacturonate (PGKCo) and sodium cobalt polygalacturonate (PGNaCo). The study of the effect of PGKCo, PGNaCo and PC on the cell viability of tumor cell lines of different genesis in vitro showed that the obtained compounds are soluble in water and exhibit selective cytotoxic activity against the tumor cell lines of human lung carcinoma A549, breast adenocarcinoma MCF-7 and cervical carcinoma M-HeLa, with no significant toxic effect on normal human cells. The possible mechanism of action of the investigated PC on M-HeLa cancer cells was investigated. The mechanism of action of PC was found to be associated with cell cycle arrest in the G0/G1 phase and the induction of apoptosis through the mitochondrial pathway. The results obtained indicate the potential for the non-toxic compounds (PGKCo, PGNaCo and PC) to be developed as drugs for the complex treatment of oncologic diseases.

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引用次数: 0
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International Journal of Biological Macromolecules
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