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COMPOSITES PART A-APPLIED SCIENCE AND MANUFACTURING · 2024 · IF 8.1

Tunable impact resistant materials: Synergistic enhancement of paraffin/MRP/re-entrant structures

Yaping Li,Longyu Bai,Jie Fu,Shixu Li,Huijun Liang,Zhiyang Yin,Song Qi,Miao Yu

In the realm of safety protection, there is a critical demand for materials capable of superior energy absorption and adaptability across diverse application scenarios. Here, this study presents integrated two-phase negative Poisson’s ratio (NPR) composites with adjustable mechanical properties sensitive to magnetic field, temperature and impact load. It is achieved by substituting the vacancy of re-entrant structures (frame phase) with soft paraffin/magnetorheological plastomer (MRP) fillers (matrix phase). The paraffin/MRP exhibits temperature-sensitive properties, enhanced magnetorheological (MR) effect (up to 4178%) and shear thickening (ST) effect (up to 2365%). Through quasi-static compression and dynamic impact tests, the composites demonstrate remarkable adaptability in impact resistance. Specifically, the first peak force exhibits responsiveness to changes in magnetic flux density, temperature, and impact velocity, with respective variations of 80.6%, 68.2%, and 30.3%. The design strategy paves the way for tunable impact resistant materials with potential for extreme environment buffering applications.

CAS / MDL: 8042-47-5
研究领域: 材料科学 · 力学 · 工程学
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ARCHIVES OF PHARMACAL RESEARCH · 2014 ·Vol. 37 ·期 12 ·1617-1623 · IF 1.751

Effect of Sophora flavescens on the pharmacokinetics of carbamazepine in rats

Shi Lei,Dang Xue-Liang,Liu Xin-You,Wei Hua-Mei,Yang Meng-Meng,Zhang Yan

Carbamazepine (CBZ), an antiepileptic with narrow therapeutic window, is a substrate of CYP 3A4 which metabolizes CBZ to carbamazepine-10,11-epoxide (CBZE). CBZE is an active and toxicity metabolite, and it is a substrate of MRP-2. Using CBZ for a long time can cause hepatic injury. Sophora flavescens (SF) is a medicinal herb used for the protected hepatic injury. This study investigated the acute and chronic effects of SF on the pharmacokinetics of CBZ in rats. The concentrations of CBZ and CBZE in plasma and tissues were determined by HPLC method. The results showed that SF which significantly decreased the AUC 0-t of CBZ, increased CBZE conversely. Tissue analysis showed that the concentrations of CBZ and CBZE in brain and liver were decreased by SF. In addition, the distribution of CBZE in kidney was reduced significantly, which influenced the CBZE excretion and increased the drug toxic potentially. Results in the current study suggest that patients using CBZ might be cautioned in the use of SF extract or Sophora -derived products. Meanwhile, patients receiving drugs which are substrates of CYP 3A4 and/or MRP-2 should be advised of the potential herb–drug interaction to reduce the risk of therapeutic failure or increased toxicity of conventional drug therapy.

研究领域: 药理学 · 中药学
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FOOD AND CHEMICAL TOXICOLOGY · 2021 · IF 6.025

Glycated peptides obtained from cultured crocodile meat hydrolysates via Maillard reaction and the anti-aging effects on Drosophila in vivo

Yin Li,Dongyi Hu,Jianlian Huang,Shaoyun Wang

With the aging problems increasing, the discovery of anti-aging compounds has become a popular research direction. Accumulation of free radicals and the consequent oxidative stress are the chief culprit of aging. Given this, cultured crocodile meat peptides-Maillard reaction product (CMP-MRP) with remarkable antioxidant activity was obtained via Maillard reaction of cultured crocodile meat hydrolysates and xylose . The antioxidant activity in vitro and anti-aging activity in vivo of CMP-MRP were investigated. Results indicated that the lifespan and the athletic ability of Drosophila were significantly improved after the administration of CMP-MRP in natural aging, H 2 O 2 - and paraquat-induced models. Furthermore, the antioxidant enzyme activities of Drosophila treated with CMP-MRP were enhanced while the levels of malondialdehyde (MDA) and protein carbonyl (PCO) were reduced in three Drosophila models. With the supplement of 5 mg/mL CMP-MRP in natural aging Drosophila model, the maximum lifespan increased from 61 days to 73 days, athletic ability raised by 95.45%, MDA and PCO reduced by 52.72% and 47.43%, respectively. Taken together, CMP-MRP exhibited outstanding antioxidant and anti-aging capacities in Drosophila models, suggesting that CMP-MRP possesses great potential in the health food and biomedicine fields as a food-derived anti-aging agent.

研究领域: 营养学 · 分子生物学 · 食品科学
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Evidence-based Complementary and Alternative Medicine · 2018 · IF 2.064

Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco-2 Cell Model

Renjie Xu,Yichu Yuan,Jia Qi,Jia Zhou,Xiaowen Guo,Jian Zhang,Ruanjuan Zhan

Loganin, iridoid glycosides, is the main bioactive ingredients in the plant Strychnos nux-vomica L. and demonstrates various pharmacological effects, though poor oral bioavailability in rats. In this study, the intestinal absorption mechanism of loganin was investigated using the human intestinal Caco-2 cell monolayer model in both the apical-to-basolateral (A-B) and the basolateral-to-apical (B-A) direction; additionally, transport characteristics were systematically investigated at different concentrations, pHs, temperatures, and potential transporters. The absorption permeability (AB) of loganin, which ranged from 12.17 to 14.78 × 10−6cm/s, was high at four tested concentrations (5, 20, 40, and 80μM), while the major permeation mechanism of loganin was found to be passive diffusion with active efflux mediated by multidrug resistance-associated protein (MRP) and breast cancer resistance protein (BCRP). In addition, it was found that loganin was not the substrate of efflux transporter P-glycoprotein (P-gp) since the selective inhibitor (verapamil) of the efflux transporter exhibited little effects on the transport of loganin in the human intestinal Caco-2 cells. Meanwhile, transport from the apical to the basolateral side increased 2.09-fold after addition of a MRP inhibitor and 2.32-fold after addition of a BCRP inhibitor. In summary, our results clearly demonstrate, for the first time, a good permeability of loganin in the human intestinal Caco-2 cell model and elucidate, in detail, the intestinal absorption mechanism and the effects of transporters on iridoid glycosides compounds.

研究领域: 药理学 · 生物医学
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Pharmacology Research & Perspectives · 2022 ·Vol. 10 ·期 1 ·e00928 · IF 2.963

The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco-2 monolayer model by interacting with UDP-glucuronosyltransferases and efflux transport proteins

Siyuan Cao,Min Zhang,Minyan Yuan,Dan Yang,Mei Zhao,Shuo Zhang,Pengjiao Wang,Rongping Zhang,Xiuli Gao

The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP-glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco-2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco-2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco-2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the K m value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the V max value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein.

CAS / MDL: 27061-78-5
研究领域: 药学 · 药理学 · 药物代谢 · 药物递送系统
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