JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2020
·
IF 4.192
Niu Zhang,Jun-Peng Zeng,Yan-Ping Wu,Meng Wei,Hong Zhang,Liufeng Zheng,Ze-Yuan Deng,Jing Li
The digestion and absorption of different structural lipids in human milk may be different. Hence, by simulating in vitro infant digestion and Caco-2 cells to explore the effects of 1-oleoyl-2-palmitoyl-3-linoleoylglycerol (OPL)/1,3-dilinoleoyl-2-palmitoylglycerol (LPL)/1,3-dioleoyl-2-palmitoylglycerol (OPO) and their mixtures (M) (OPL/LPL/OPO in M1, M2, and M3 were 1.5/0.5/1, 1.2/1.2/1, and 0.5/0.2/1, respectively) on digestion and absorption. The digestibility of the OPO group was higher than those of the OPL and LPL groups, and the M3 group was higher than the M1 and M2 groups. The synthesis and transport of triglycerides in Caco-2 cells in OPL and LPL groups were higher than the OPO group, and the M1 group was significantly higher than that of M3. The expression of FABP1, PPARα, and MTT protein in OPL and M1 groups was significantly higher than OPO and M3, respectively. There are differences in the digestion and absorption of differently structured lipids from this study.
研究领域:
营养学
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生物化学
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儿科
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产品关联
DOI
PubMed
高影响因子
Journal of Environmental Sciences
·
2023
·
IF 6.9
Xiang Zhang,Yunpeng Huang,Jikun Wang,Jie Tang,Yang Mei,Nali Zhu,Zhigang Li,Lingxiangyu Li,Yawei Wang
The nanoscale zinc oxide (n-ZnO) was used in food packages due to its superior antibacterial activity, resulting in potential intake of n-ZnO through the digestive system, wherein n-ZnO interacted with saliva. In recent, facet engineering, a technique for controlling the exposed facets, was applied to n-ZnO, whereas risk of n-ZnO with specific exposed facets in saliva was ignored. ZnO nanoflakes (ZnO-0001) and nanoneedles (ZnO-1010) with the primary exposed facets of {0001} and {1010} respectively were prepared in this study, investigating stability and toxicity of ZnO-0001 and ZnO-1010 in synthetic saliva. Both ZnO-0001 and ZnO-1010 partially transformed into amorphous Zn 3 (PO 4 ) 2 within 1 hr in the saliva even containing orgnaic components, forming a ZnO-Zn 3 (PO 4 ) 2 core-shell structure. Nevertheless, ZnO-1010 relative to ZnO-0001 would likely transform into Zn 3 (PO 4 ) 2 , being attributed to superior dissolution of {1010} facet due to its lower vacancy formation energy (1.15 eV) than {0001} facet (3.90 eV). The toxicity of n-ZnO to Caco-2 cells was also dependent on the primary exposed facet; ZnO-0001 caused cell toxicity through oxidative stress, whereas ZnO-1010 resulted in lower cells viability than ZnO-0001 through oxidative stress and membrane damage. Density functional theory calculations illustrated that ·O 2 − was formed and released on {1010} facet, yet O 2 2− instead of ·O 2 − was generated on {0001} facet, leading to low oxidative stress from ZnO-0001. All findings demonstrated that stability and toxicity of n-ZnO were dependent on the primary exposed facet, improving our understanding of health risk of nanomaterials.
研究领域:
纳米技术
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毒理学
·
材料科学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
Food & Function
·
2019
·Vol. 10
·期 5
·2906-2913
·
IF 3.241
Yanlong Li,Xudong Tian,Shengcai Li,Lijun Chang,Ping Sun,Yubei Lu,Xiaoyan Yu,Shiwang Chen,Zhengquan Wu,Zhong Xu,Wanrong Kang
Dysfunction of the intestinal epithelial barrier plays an important role in the pathogenesis of several intestinal diseases, including celiac disease, inflammatory bowel disease, and irritable bowel syndrome. The present research was carried out to investigate the protective effect of total polysaccharides of adlay bran (TPA) on TNF-α-evoked epithelial barrier dysfunction in Caco-2 cells. Caco-2 cells were treated with or without TPA in the absence or presence of TNF-α, and transepithelial electrical resistance (TEER) and Phenol Red flux were assayed to evaluate the intestinal epithelial barrier function. The results indicated that TPA suppressed the TNF-α-induced release of pro-inflammatory factors. Furthermore, TPA obviously assuaged both the increased paracellular permeability and the decrease of TEER in TNF-α-challenged Caco-2 cells. Furthermore, TPA obviously assuaged TNF-α-evoked up-regulation of IL-8 and IL-6 expression, down-regulation of occludin and ZO-3 expression, and markedly suppressed the activation and protein expression of NF-κB p65. Our results indicated that TPA assuages the TNF-α-evoked dysfunction of the intestinal epithelial barrier by inhibiting the NF-κB p65-mediated inflammatory response.
研究领域:
胃肠病学
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免疫学
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药理学
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细胞生物学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2024
·Vol. 26
·期 1
·72
·
IF 4.9
Chaoji Li,Min Zhang,Yanni Zhao,Dan Yang,Mei Zhao,Leyuan Shang,Xiaodong Sun,Shuo Zhang,Pengjiao Wang,Xiuli Gao
Mycophenolic acid (MPA) is a commonly used immunosuppressant. In the human body, MPA is metabolized into mycophenolic acid 7-O-glucuronide (MPAG) and mycophenolic acid acyl-glucuronide (AcMPAG) mainly through liver glucuronidation, which involves UDP-glucuronosyltransferase (UGTs) and transfer proteins. Research has indicated that the pharmaceutical excipient PEG400 can impact drug processes in the body, potentially affecting the pharmacokinetics of MPA. Due to the narrow therapeutic window of MPA, combination therapy is often used, and PEG400 is widely used in pharmaceutical preparations. Therefore, investigating the pharmacokinetic influence of PEG400 on MPA could offer valuable insights for optimizing MPA’s clinical use. In this study, we examined the impact of a single oral dose of PEG400 on the blood levels of MPA in rats through pharmacokinetic analysis. We also investigated the distribution of MPA in various tissues using mass spectrometry imaging. We explored the potential mechanism by which PEG400 affects the metabolism of MPA using hepatic and intestinal microsomes and the Caco-2 cellular transporter model. Our findings reveal that the overall plasma concentrations of MPA were elevated in rats following the co-administration of PEG400, with the AUC0-tof MPA and its metabolite MPAG increasing by 45.53% and 29.44%, respectively. Mass spectrometry imaging showed increased MPA content in tissues after PEG400 administration, with significant differences in the metabolites observed across different tissues. Microsomal and transport experiments showed that PEG400 accelerated the metabolism of MPA, promoted the uptake of MPA, and inhibited efflux. In conclusion, PEG400 alters the in vivo metabolism of MPA, potentially through the modulation of metabolic enzymes and transport.
研究领域:
药理学
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免疫抑制剂
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药物代谢
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药用辅料
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体内和体外研究
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产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2021
·
IF 4.384
Wen Fu,Yiping Liang,Zhonghui Xie,Hangyi Wu,Zhenhai Zhang,Huixia Lv
Panax Notoginseng Saponins (PNS) has been widely used in the prevention and treatment of cardiovascular and cerebrovascular diseases such as myocardial infarction, heart failure and cerebral infarction . However, oral administration of PNS showed low bioavailability because of its instability and poor membrane permeability in the gastrointestinal tract. Here, lipoprotein-inspired hybrid nanoparticles of PNS-Lecithin-Zein (PLZ-NPs) were prepared by using a simple phase separation method, which possessed a core-shell structure, where zein was used as protein part to replace the animal origin protein to increase the resistance to acid and enzymes while lecithin was used as the lipid composition to improve the oral absorption of PNS as well as to increase the drug loading capacity of PNS into the nanocarriers . The results of stability test showed that PLZ-NPs had robust enzymolysis resistance ability for acid and digestive enzymes of gastrointestinal environments. The fluorescent resonance energy transfer (FRET) assay confirmed the ability of LZ-NPs to be intactly absorbed by Caco-2 cell monolayer. Cell transport studies demonstrated that the permeability of PLZ-NPs in Caco-2/HT29-MTX co-culture cell model was 1.5-fold that of PNS. Meanwhile, the single-pass intestinal perfusion assay proved the absorption parameter Peff of PLZ-NPs was 1.75 and 1.80 times higher than that of PNS in the ileum and jejunum , respectively. Finally, the in vivo pharmacokinetic experiment showed that the relative oral bioavailability of PLZ-NPs was 1.71-fold that of free PNS in SD rat . In summary, the employment of the Lecithin/Zein hybrid nanoparticles could be considered as a promising approach for PNS analogues.
研究领域:
药学
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纳米技术
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药物递送系统
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药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Food & Function
·
2021
·Vol. 12
·期 13
·5949-5958
·
IF 5.396
Lan Mo,Guang-lei Zhao,Xiao-feng Li,Xing-long Xiao,Ning He,Juan-juan Ma,Yi-gang Yu
Acylation has become one of the most widely used methods to improve the lipid solubility and bioavailability of flavonoids. In this study, puerarin acid esters (PAES) with different chain lengths were synthesized via biocatalytic acylation. This was the first study to evaluate the digestion and transport profiles and immunocompetence of PAES. The relationship between the digestion and transport profiles and potential immunocompetence of the acylated derivatives in Caco-2 cell monolayers was also explored. Puerarin and PAES remained stable in gastric phases, whereas different degrees of hydrolysis of PAES were found in the intestine. PAES with less than 12 carbon chains were positively correlated with the degree of hydrolysis, while those with more than 12 carbon chains showed higher resistance to hydrolysis by the artificial human digestive juice. The apparent permeability coefficients of puerarin, puerarin acetate, puerarin propanoate, puerarin butyrate, puerarin hexanoate, puerarin octanate and puerarin laurate were 1.62 ± 0.09, 1.70 ± 0.15, 1.89 ± 0.19, 1.86 ± 0.18, 2.29 ± 0.12, 4.06 ± 1.01 and 2.32 ± 0.88 × 10−6 cm s−1, respectively, in Caco-2 cell monolayers. The results of the immune factor assays indicated that puerarin propanoate, puerarin hexanoate and puerarin myristate could significantly promote the secretion of IL-6, TNF-α and IL-10. These findings suggested that a better absorption could be predicted after oral intake using PAES. Meanwhile, the concentration of esters and their metabolites (puerarin) found in the digestion and transport profiles directly affected their potential immunocompetence.
研究领域:
药理学
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生物化学
·
免疫学
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2021
·
IF 5.279
Yanfang Li,Ming Li,Jiaping Liu,Wenhao Zheng,Yaqiong Zhang,Tongcheng Xu,Boyan Gao,Liangli Yu
The profiles of soluble and insoluble phenolic compounds in 11 commercial red sorghums (B11, B12, B13, B14, J124, J127, J138, J140, J142, J152, and J158) were investigated using ultraperformance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS) analysis. A total of 48 phenolic compounds including 35 phenolic acids and their derivatives, 12 flavonoids, and 1 proanthocyanidin were identified, and 8 phenolic compounds were reported for the first time in sorghums. Four major 3-deoxyanthocyanidins were also quantified, with their soluble forms accounting for 99.75–99.87% of the total contents. Pearson’s correlation analyses indicated that 3-deoxyanthocyanidins significantly contributed to the antioxidant capacities of the red sorghums and that 5-methoxy-luteolinidin showed the strongest correlation. Besides, the soluble phenolic fraction of B13 dose-dependently inhibited the proliferation of Caco-2 cells and the secretion of IL-1β and NO in RAW264.7 macrophages, which might be attributed to its relatively high total phenolic (TPC), flavonoid (TFC), and proanthocyanidin content (TPAC) values and radical scavenging capacities.
研究领域:
食品科学
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营养学
·
药理学
·
分析化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FITOTERAPIA
·
2014
·
IF 2.216
Yan Xie,Huilin Luo,Jingze Duan,Chao Hong,Ping Ma,Guowen Li,Tong Zhang,Tao Wu,Guang Ji
Aim Total flavones of Hippophae rhamnoides L. (TFH) have a clinical use in the treatment of cardiac disease. The pharmacological effects of TFH are attributed to its major flavonoid components, isorhamnetin , kaempferol , and quercetin . However, poor oral bioavailability of these flavonoids limits the clinical applications of TFH. This study explores phytic acid (IP 6 ) enhancement of the oral absorption in rats of isorhamnetin, kaempferol, and quercetin in TFH. Methods In vitro Caco-2 cell experiments and in vivo pharmacokinetic studies were performed to investigate the effects of IP 6 . The aqueous solubility and lipophilicity of isorhamnetin, quercetin, and kaempferol were determined with and without IP 6 , and mucosal epithelial damage resulting from IP 6 addition was evaluated by MTT assays and morphology observations. Results The P app of isorhamnetin, kaempferol, and quercetin was improved 2.03-, 1.69-, and 2.11-fold in the presence of 333 μg/mL of IP 6 , respectively. Water solubility was increased 22.75-, 15.15-, and 12.86-fold for isorhamnetin, kaempferol, and quercetin, respectively, in the presence of 20 mg/mL IP 6 . The lipophilicity of the three flavonoids was slightly decreased, but their hydrophilicity was increased after the addition of IP 6 in the water phase as the logP values of isorhamnetin, kaempferol, and quercetin decreased from 2.38 ± 0.12 to 1.64 ± 0.02, from 2.57 ± 0.20 to 2.01 ± 0.04, and from 2.39 ± 0.12 to 1.15 ± 0.01, respectively. The absorption enhancement ratios were 3.21 for isorhamnetin, 2.98 for kaempferol, and 1.64 for quercetin with co-administration of IP 6 (200 mg/kg) in rats. In addition, IP 6 (200 mg/kg, oral) caused neither significant irritation to the rat intestines nor cytotoxicity (400 μg/mL) in Caco-2 cells. Conclusions The oral bioavailability of isorhamnetin, kaempferol, and quercetin in TFH was enhanced by the co-administration of IP 6 . The main mechanisms are related to their enhanced aqueous solubility and permeability in the presence of IP 6 . In summary, IP 6 is a potential absorption enhancer for pharmaceutical formulations that is both effective and safe.
研究领域:
药理学
·
药剂学
·
营养保健品
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Foods
·
2025
·Vol. 14
·期 7
·1110
·
IF 5.1
Yuxin Zhang,Zeyuan Deng,Hongyan Li,Zeyin Jiang
Ulcerative colitis (UC) is a chronic inflammatory bowel disease characterized by recurrent episodes and an inability to achieve a complete cure. The spermidine derivative (di- p -coumaroyl-caffeoyl spermidine, SPDD), as a key alkaloid, exhibits unique health benefits. However, it has not yet been reported whether SPDD can improve dextran sulfate sodium (DSS)-induced colitis in mice. Herein, we investigated the effects and mechanisms of SPDD on DSS-induced colitis in mice. SPDD was successfully purified from rose bee pollen and was found to have a protective effect on colitis, evidenced by reduced disease activity index (DAI) scores and colonic inflammation, increased colonic length and upregulated the expression of tight junction proteins (TJs) in the model ( p < 0.05). Importantly, the IL-17 signaling pathway showed significant enrichment by RNA sequencing (RNA-seq) technology with SPDD treatment, which resulted in the downregulation of MAPK4 expression ( p < 0.05). Furthermore, SPDD weakened the interaction between MAPK4 and AKT, resulting in a decrease in the phosphorylation level of AKT, thereby reducing the expression of IL-6, IL-1β, iNOS, and COX-2, and alleviating colitis ( p < 0.05). In addition, SPDD treatment also ameliorated TNF-α-induced inflammation in Caco-2 cells. Overall, our study demonstrated that SPDD reversed colonic inflammation in colitis mice through the MAPK4/AKT pathway and might be a promising candidate for UC intervention.
研究领域:
药理学
·
免疫学
·
胃肠病学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Food Bioscience
·
2026
·
IF 6.2
Yanwei Liu,Yuxin Bao,Junjia Luan,Cikun Liu,Yuanyuan Wang,Jinxiang Wang,Jianrong Li,Xuepeng Li
This study investigated the protective effects of muscle enzymatic hydrolysates from Pacific saury ( Cololabis saira ) on H 2 O 2 -induced oxidative damage, as well as their antioxidant stability. The hydrolysate exhibited a high 1,1-Diphenyl-2-trinitrophenylhydrazine (DPPH) radical scavenging rate and significant reducing power. Meanwhile, it protected HEK-293 cells and Caco-2 cells against H 2 O 2 -induced oxidative damage by maintaining cell membrane integrity, inhibiting lipid peroxidation, and enhancing the levels of cellular antioxidant enzymes. Regarding antioxidant stability, the hydrolysate displayed favorable salt tolerance, retaining 80.33%±1.85% of its reducing power even at 10% NaCl concentration; high-temperature treatment (120°C), glucose addition and simulated gastrointestinal digestion observably enhanced its antioxidant activity, while alkaline environment, high NaCl concentration and ultraviolet irradiation significantly weakened the antioxidant activity. These results indicate that the hydrolysate from Pacific saury has good cell protection effects and is expected to be used in functional foods and nutritional supplements, but its antioxidant stability is easily affected by processing and storage conditions.
✓ 已验证
DOI
高影响因子
Food Bioscience
·
2026
·
IF 6.2
Hui Ouyang,Jiaying Huo,Xiaojuan Xin,Ying Gao,Ping Wang,Xiongwei Yu,Shugang Li
The transport and absorption of antioxidant peptides are critical for their biological activity. The walnut meal-derived peptide YWSPNDEQFR (YR-10) has been shown to alleviate oxidative stress–induced liver injury, but its absorption mechanisms remain unclear. In this study, we employed a Caco-2 monolayer, DPPC liposomes, and molecular docking to characterize the transepithelial transport of YR-10 across the intestinal epithelium. YR-10 was absorbed through clathrin-mediated endocytosis and paracellular pathway, with significantly promotes the restoration of ZO-1 and closure protein gene expression, indicating its ability to restore the integrity of the epithelial barrier. Further research revealed that YR-10 binding to lipid bilayers was predominantly entropy-driven, involving electrostatic, hydrogen-bonding, and hydrophobic interactions that regulated membrane fluidity and order. These findings collectively elucidate the intestinal absorption mechanism of YR-10 and provide a theoretical basis for improving the bioavailability of walnut powder-derived bioactive peptides in functional food applications.
✓ 已验证
产品关联
DOI
高影响因子
MOLECULAR PHARMACEUTICS
·
2013
·
IF 4.57
Wenjing Li,Xinru Li,Yajie Gao,Yanxia Zhou,Shujin Ma,Yong Zhao,Jinwen Li,Yan Liu,Xinglin Wang,Dongdong Yin
The present study aimed to investigate the effect of monomethoxy poly(ethylene glycol)-block-poly(d,l-lactic acid) (mPEG-PLA) on the activity of P-glycoprotein (P-gp) in Caco-2 cells and further unravel the relationship between PLA chain length in mPEG-PLA and influence on P-gp efflux and the action mechanism. The transport results of rhodamine 123 (R123) across Caco-2 cell monolayers suggested that mPEG-PLA unimers were responsible for its P-gp inhibitory effect. Furthermore, transport studies of R123 revealed that the inhibitory potential of P-gp efflux by mPEG-PLA analogues was strongly correlated with their structural features and showed that the hydrophilic mPEG-PLA copolymers with an intermediate PLA chain length and 10.20 of hydrophilic–lipophilic balance were more effective at inhibiting P-gp efflux in Caco-2 cells. The fluorescence polarization measurement results ruled out the plasma membrane fluidization as a contributor for inhibition of P-gp by mPEG-PLA. Concurrently, mPEG-PLA inhibited neither basal P-gp ATPase (ATP is adenosine triphosphate) activity nor substrate stimulated P-gp ATPase activity, suggesting that mPEG-PLA seemed not to be a substrate of P-gp and a competitive inhibitor. No evident alteration in P-gp surface level was detected by flow cytometry upon exposure of the cells to mPEG-PLA. The depletion of intracellular ATP, which was likely to be a result of partial inhibition of cellular metabolism, was directly correlated with inhibitory potential for P-gp mediated efflux by mPEG-PLA analogues. Hence, intracellular ATP-depletion appeared to be possible explanation to the inhibition mechanism of P-gp by mPEG-PLA. Taken together, the establishment of a relationship between PLA chain length and impact on P-gp efflux activity and interpretation of action mechanism of mPEG-PLA on P-gp are of fundamental importance and will facilitate future development of mPEG-PLA in the drug delivery area.
研究领域:
药学
·
药理学
·
药物递送系统
✓ 已验证
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）