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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Structural characterizations and anti-aging activities of a homogeneous polysaccharide derived from Coix seed-lactic acid bacteria fermentation

Yating Cheng,Shanshan He,Zhihui Wei,Yuxuan Meng,Dun Su,Xiaomin Li,Shu Zhang,Rong-Rong He,Zifei Qin,Qi Xiang

Coix seed, a well-known traditional Chinese medicine, has been extensively used for its anti-aging properties. However, the biological mechanism of its polysaccharides remains unclear. This study systematically investigated the anti-aging effects and mechanism of purified Coix seed polysaccharide (CP1) for the first time. The structural analysis revealed that CP1 mainly consists of glucose linked by α-(1 → 4) and α-(1 → 6) glycosidic bonds and has an average molecular weight of 8.855 kDa. Further, CP1 exhibited strong scavenging activity of approximately 55.85 % against 1,1-diphenyl-2-trinitrobenzohydrazine, 71.30 % against 2,2′-bis-(3-ethylbenzothiazolin-6-sulfonic acid) diammonium salt, and 68.40 % against hydroxyl radicals. In Caenorhabditis elegans , CP1 significantly extended the lifespan by 3–5 days ( p  < 0.001) and increased the survival by 78 % under oxidative stress condition ( p  < 0.001). In addition, CP1 suppressed the activity of senescence-associated β-galactosidase in zebrafish ( p  < 0.001) and reduced DNA damage in human skin fibroblasts ( p  < 0.001). Mechanistically, CP1 mainly activates the p -AMPK/RICTOR/CREB3 pathway by interacting with PARP-1. Taken together, this study performs the structural characterization of a glucan polysaccharide from Coix seed and its anti-aging effects in different models. These findings can provide a theoretical basis and candidate molecule for anti-aging therapies.

CAS / MDL: 573-58-0
研究领域: 天然产物化学 · 药用植物学 · 分子生物学 · 抗衰老研究 · 糖生物学 · 中医药学
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2023 · IF 6.1

Bioavailability of Coix Seed Polyphenols in a MKN28/Caco-2 Continuous Transport Model and Their Lipid-Lowering Effects via Modulating Adipocyte Differentiation of 3T3-L1 Cells

Bowen Qin,Yijun Yao,Jing Zhang,Lifeng Wang

At present, most of the research on coix seed polyphenols (CSPs) focuses on the separation, purification, structure analysis, and biological functions of specific components, and few studies have considered the overall bioavailability and the metabolites that play a role after digestion and absorption and their biological functional activities. In this study, we constructed a MKN28 and Caco-2 cell monolayer continuous transport model (MCTM) to study the bioavailability of CSPs in the digestion and absorption stages of the stomach and small intestine. Using this model, we innovatively divided CSPs into easy-to-digest and hard-to-digest polyphenols and studied their intracellular lipid-lowering function and their influence on human intestinal flora. Transwell experiments showed that ferulic acid, rutin, naringin, arbutin, and syringetin had high transmembrane transport efficiency, especially syringetin. The methylation reaction in the monolayer membrane of Caco-2 cells may be the reason for the higher transport rate of syringetin. Further experiments showed that CPL reduced TG accumulation by more than 50% during 3T3-L1 differentiation and promoted the transformation of adipocytes into brown cells (p < 0.05). Finally, in vitro fermentation experiments showed that CSP_AP can increase the abundance of Lactobacillus and Bifidobacterium of human gut microbiota at the genus level (p < 0.05).

CAS / MDL: 16009-13-5 84-80-0
研究领域: 药理学 · 营养学 · 细胞生物学 · 胃肠生理学 · 微生物学
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International Journal of Nanomedicine · 2024 · IF 6.6

Sequentially Released Liposomes Enhance Anti-Liver Cancer Efficacy of Tetrandrine and Celastrol-Loaded Coix Seed Oil

Yunyan Chen,Ziwei Zhang,Zhilei Qian,Rui Ma,Minna Luan,Yu Sun

Background A sequential release co-delivery system is an effective strategy to improve anti-cancer efficacy. Herein, multicomponent-based liposomes (TET-CTM/L) loaded with tetrandrine (TET) and celastrol (CEL)-loaded coix seed oil microemulsion (CTM) were fabricated, which showed synergistic anti-liver cancer activities. By virtue of Enhanced Permeability and Retention (EPR) effect, TET-CTM/L can achieve efficient accumulation at the tumor site. TET was released initially to repair abnormal vessels and decrease the fibroblasts, and CTM was released subsequently for eradication of tumor tissue.Methods TEM (transmission electron microscopy) and DLS (dynamic light scattering) were adopted to characterize the TET-CTM/L. Flow cytometry was adopted to examine the cellular uptake and cytotoxicity of HepG2 cells. The HepG2 xenograft nude mice were adopted to evaluate the anti-tumor efficacy and systemic safety of TET-CTM/L.Results TEM images of TET-CTM/L showed the structure of small particle size of CTM within large-size liposomes, indicating that CTM can be encapsulated in liposomes by film dispersion method. In in vitro studies, TET-CTM/L induced massive apoptosis toward HepG2 cells, indicating synergistic cytotoxicity against HepG2 cells. In in vivo studies, TET-CTM/L displayed diminished systemic toxicity compared to celastrol or TET used alone. TET-CTM/L showed the excellent potential for tumor-targeting ability in a biodistribution study.Conclusion Our study provides a new strategy for combining anti-cancer therapy that has good potential not only in the treatment of liver cancer but also can be applied to the treatment of other solid tumors.

CAS / MDL: 34157-83-0 518-34-3
研究领域: 药学 · 肿瘤学 · 纳米技术
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JOURNAL OF FOOD SCIENCE · 2023 ·Vol. 88 ·期 6 ·2723-2734 · IF 3.9

Preparation of a broad-specificity antibody against zearalenone and its primary analogues and development of immunoassay of Coicis Semen and related products

Jiao Tian,Jiaoyang Luo,Jiaan Qin,Yudan Wang,Xinqi Sun,Jing Zhang,Tongwei Ke,Mengyue Guo,Haonan Ruan,Fang An,Meihua Yang

The purpose of this study was to prepare a highly sensitive and specific zearalenone (ZEN) monoclonal antibody, which was then used to develop an indirect enzyme-linked immunosorbent assay (ic-ELISA) and a colloidal gold immunochromatographic assay (GICA). These techniques were used for the detection of Coicis Semen and related products (Coicis Semen flour, Yimigao, and Yishigao). Immunogens were synthesized by oxime active ester techniques and characterized via ultraviolet spectrophotometry. Immunogens were injected subcutaneously into the abdominal cavities and backs of mice. Using the prepared antibodies, we developed ic-ELISA and GICA rapid detection methods, which were then applied for the rapid detection of ZEN and its analogues from Coicis Semen and related products. For ic-ELISA, the half maximal inhibitory concentration (IC 50 ) values for ZEN, α-zearalenol (α-ZEL), β-zearalenol (β-ZEL), zearalanone (ZAN), α-zearalanol (α-ZAL), and β-zearalanol (β-ZAL) were determined to be 1.13, 1.69, 2.06, 0.66, 1.20, and 0.94 ng•mL −1 , respectively. For GICA, the cutoff values of ZEN, α-ZEL, β-ZEL, α-ZAL, and β-ZAL on test strips were 0.5 ng•mL −1 in phosphate buffer saline (0.01 M, pH 7.4), while ZAN was found to be 0.25 ng•mL −1 . Furthermore, the cutoff values of test strips were between 10 and 20 µg∙kg −1 in Coicis Semen and related products. The results of these two detection methods were in good agreement with results from liquid chromatography-tandem mass spectrometry. This study provides technical support for the preparation of broad-specificity monoclonal antibodies against ZEN and lays the foundation for the simultaneous detection of multiple mycotoxins from food and herbal medicines.

研究领域: 免疫学 · 分析化学 · 食品科学 · 药理学
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FOOD RESEARCH INTERNATIONAL · 2021 · IF 6.475

Coix seed polysaccharides alleviate type 2 diabetes mellitus via gut microbiota-derived short-chain fatty acids activation of IGF1/PI3K/AKT signaling

Ting Xia,Chang-Shun Liu,Yan-Nan Hu,Zhen-Ye Luo,Fei-Long Chen,Li-Xia Yuan,Xiao-Mei Tan

Type 2 diabetes mellitus (T2DM) has become a worldwide concern in recent years. Coix seed (CS) as a homologous substance of traditional Chinese medicine and food, its polysaccharides can improve the symptoms of patients with metabolic disorders. Since most plant polysaccharides are difficult to digest and absorb, we hypothesized that Coix seed polysaccharides (CSP) exert hypoglycemic effects through the gut. In this study, the underlying mechanisms regulating hypoglycemic effects of CSP on a T2DM mouse model were investigated. After treatment with CSP, serum insulin and high-density lipoprotein cholesterol levels were increased, while total cholesterol, triglycerides and low-density lipoprotein cholesterol levels were decreased in T2DM mice. In addition, CSP treatment helped repair the intestinal barrier and modulated the gut microbial composition in T2DM mice, mainly facilitating the growth of short-chain fatty acid (SCFA)-producing bacteria, Spearman’s analysis revealed these bacteria were positively related with the hypoglycemic efficacy of CSP. Colonic transcriptome analysis indicated the hypoglycemic effect of CSP was associated with the activation of the IGF1/PI3K/AKT signaling pathway. Correlative analysis revealed that this activation may result from the increase of SCFAs-producing bacteria by CSP. GC–MS detection verified that CSP treatment increased fecal SCFAs levels. Molecular docking revealed that SCFAs could bind with IGF1, PI3K, and AKT. Our findings demonstrated that CSP treatment modulates gut microbial composition, especially of the SCFAs-producing bacteria, activates the IGF1/PI3K/AKT signaling pathways, and exhibits hypoglycemic efficacy.

研究领域: 药理学 · 内分泌学 · 微生物学 · 分子生物学 · 营养学
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BIOMACROMOLECULES · 2017 · IF 5.246

Oral Nanomedicine Based on Multicomponent Microemulsions for Drug-Resistant Breast Cancer Treatment

Ding Qu,Lixiang Wang,Meng Liu,Shiyang Shen,Teng Li,Yuping Liu,Mengmeng Huang,Congyan Liu,Yan Chen,Ran Mo

The aim of this study is to demonstrate the enhanced therapeutic efficacy of anticancer drugs on drug-resistant breast cancer using multicomponent microemulsions (ECG-MEs) as an oral delivery system. The etoposide-loaded ECG-MEs were composed of coix seed oil and ginsenoside Rh2 (G-Rh2), both of which possess not only the synergistic antitumor effect with etoposide, but also have excipient-like properties. Orally administrated ECG-MEs were demonstrated to be able to accumulate at the tumor site following crossing the intestines as intact vehicles into the blood circulation. The spatiotemporal controlled release characteristics of ECG-MEs brought about the efficient P-gp inhibition by the initially released G-Rh2 and the increased intracellular accumulation of the sequentially released etoposide. The combination antitumor activity of etoposide, G-Rh2 and coix seed oil using ECG-MEs was verified on the xenograft drug-resistant breast tumor mouse models. In addition, the safety evaluation studies indicated that treatment with ECG-MEs did not cause any significant toxicity in vivo. These findings suggest that ECG-MEs as an oral formulation may offer a promising strategy to treat the drug-resistant breast cancer.

研究领域: 药学 · 肿瘤学 · 纳米技术 · 药物递送系统
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2017 · IF 3.671

Structural characteristics and prebiotic effects of Semen coicis resistant starches (type 3) prepared by different methods

Chen Bao,Hongliang Zeng,Yi Zhang,Longtao Zhang,Xu Lu,Zebin Guo,Song Miao,Baodong Zheng

In order to investigate the effects of different preparation methods on Semen coicis resistant starch, the structural properties and prebiotic effects of autoclaving treatment–purified S. coicis resistant starch (GP-SRS3), ultrasonic-autoclaving treatment–purified S. coicis resistant starch (UP-SRS3), enzyme-autoclaving treatment–purified S. coicis resistant starch (EP-SRS3) and microwave-moisture treatment–purified S. coicis resistant starch (MP-SRS3) were studied compared to high-amylose maize starch (HAMS). Fourier transform infrared spectroscopy and Solid-state 13 C NMR spectroscopy showed all of SRS3 displayed B-type crystallite structure, furthermore, MP-SRS3 and UP-SRS3 showed higher degree of ordered structure and degree of double helical structure compared to other samples. Field emission scanning electron microscopy showed MP-SRS3 displayed deeply layered strips and UP-SRS3 exhibited some cavities. Moreover, S. coicis resistant starch could promote the growth of Bifidobacteria adolescentis better compared to high-amylose maize starch, among these samples. MP-SRS3 exhibited best prebiotic effect, which was possible attributed to its rough surface and double helix structure. B. adolescentis displayed a higher survival rate to the simulated gastrointestinal tract environment in SRS3 medium than that in high-amylose maize starch medium, especially MP-SRS3 and UP-SRS3, which partly contributed to its strips and cavities. Overall, MP-SRS3 could be regarded as a potential prebiotic to promote the growth of B. adolescentis for its structural trait.

CAS / MDL: 64-19-7 107-92-6 79-09-4
研究领域: 食品科学 · 营养学 · 微生物学
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Food Bioscience · 2022 · IF 5.318

Analysis of metabolites of coix seed fermented by Monascus purpureus

Qi Mei,Zhaona Xu,Quanye Wu,Likang Qin,Haiying Zeng,Yi Zhu

In this study, an untargeted metabolomics method based on LC-MS was used to investigate the differential metabolites of coix seed after fermentation by Monascus purpureus . The compounds with highly correlated variable importance in projection (VIP) values of orthogonal partial least squares discriminant analysis (OPLS-DA) were selected as the important metabolites of coix seed samples. Coix seed was fermented by M. purpureus for 9 d. The color value units (CVU) of pigment in fermented coix seed reached 157.47 CVU/g, and the contents of total phenols and total flavonoids were 0.32 mg/g and 1.2 mg/g, respectively. A total of 270 differential metabolites were detected, including amino acids, peptides, fatty acids, phenols, steroids, and their derivatives, of which the relative contents of 187 metabolites showed a significant upward trend (p < 0.05). Amino acids, peptides and analogues accounted for the largest proportion at 26%, among which most metabolites were enriched. For example, N-alpha-acetyllysine, l -tryptophan and l -arginine exhibited a fold change (FC) of 6200.87, 330.29, and 35.59, respectively. In particular, the detected steroid metabolites accounted for 3% of the total metabolites, and they all participated in the same pathway, in which androsterone, 2-methoxyestrone and etiocholanolone were upregulated. The synthesis of these steroids was related to the precursors and enzymes in the pathway, such as dehydroepiandrosterone, androstenedione, and 3beta-hydroxy-delta5-steroid dehydrogenase (HSD3B). The results of this study reveal M. purpureus fermentation can successfully transform coix seed, improving the functional activities of metabolites. Thus, this process has high development value with important applications in the food industry.

CAS / MDL: 103616-89-3
研究领域: 食品科学 · 代谢组学 · 微生物学 · 药理学
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DRUG DELIVERY · 2020 · IF 4.902

Furin-responsive triterpenine-based liposomal complex enhances anticervical cancer therapy through size modulation

Yunyan Chen,Mengfei Guo,Ding Qu,Yuping Liu,Jian Guo,Yan Chen

The accumulation and penetration of antitumor drugs in tumor tissues are directly related to their antitumor effects. The particle size of the nanodrug delivery system is one of the most important factors for the accumulation and penetration of antitumor drugs within tumor tissues. Generally, nanodelivery systems of intermediate size (100–120 nm) are capable of efficient accumulation owing to prolonged circulation and enhanced permeability and retention (EPR) effect; however, smaller ones (20–40 nm) are effective for deep penetration within tumor tissue. Currently a conventional drug delivery system cannot possess two types of optimal sizes, simultaneously. To solve this and to enhance cervical cancer treatment, a furin-responsive triterpenine-based liposomal complex (PEGcleavable Tf-CTM/L), with Tf-CTM (transferrin-modified tripterine-loaded coix seed oil microemulsion) in core, coated with a thermo-sensitive lipid and a kind of PEG shell modified with a furin-cleavable peptide was developed to improve tumor-specific accumulation and penetration. Herein, PEGcleavable Tf-CTM/L was capable of efficient accumulation because of EPR effect. The PEG shells could timely detach under stimulation of overexpressed furin protein to solve the problem of the steric hindrance dilemma. The small-sized Tf-CTM released under stimulation of tumor microthermal environment in cervical cancer, which was efficient with regards to deep penetration at tumor sites. Notably, compared to the use of triterpenine alone, PEGcleavable Tf-CTM/L promoted anticervical efficacy and displayed diminished systemic toxicity by efficient accumulation and deep penetration of antitumor drugs within tumor tissues. Our study provides a new strategy, and holds promising potential for anticervical cancer treatment.

研究领域: 药学 · 纳米技术 · 癌症研究 · 药物递送系统 · 生物医学工程
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