MOLECULES
·
2023
·Vol. 28
·期 14
·5496
·
IF 4.6
Ting Li,Chaoyue Yang,Houkang Cao,Siyi Mo,Bo Li,Zhipeng Huang,Ruobing Zhang,Jianzhao Wu,Kefeng Zhang,Ya Gao
Bergenin (BER), a natural component of polyphenols, has a variety of pharmacological activities, especially in improving drug metabolism, reducing cholestasis, anti-oxidative stress and inhibiting inflammatory responses. The aim of this study was to investigate the effects of BER on liver injury induced by isonicotinic acid hydrazide (INH) and rifampicin (RIF) in mice. The mice model of liver injury was established with INH (100 mg/kg)+RIF (100 mg/kg), and then different doses of BER were used to intervene. The pathological morphology and biochemical indicators of mice were detected. Meanwhile, RNA sequencing was performed to screen the differentially expressed genes and signaling pathways. Finally, critical differentially expressed genes were verified by qRT-PCR and Western blot. RNA sequencing results showed that 707 genes were significantly changed in the INH+RIF group compared with the Control group, and 496 genes were significantly changed after the BER intervention. These differentially expressed genes were mainly enriched in the drug metabolism, bile acid metabolism, Nrf2 pathway and TLR4 pathway. The validation results of qRT-PCR and Western blot were consistent with the RNA sequencing. Therefore, BER alleviated INH+RIF-induced liver injury in mice. The mechanism of BER improving INH+RIF-induced liver injury was related to regulating drug metabolism enzymes, bile acid metabolism, Nrf2 pathway and TLR4 pathway.Keywords:bergenin;isonicotinic acid hydrazide;rifampicin;liver injury;RNA sequencing
研究领域:
药理学
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分子生物学
·
毒理学
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DOI
PubMed
高影响因子
JOURNAL OF APPLIED POLYMER SCIENCE
·
2015
·Vol. 132
·期 27
·
IF 1.768
Lijing Teng,Wangyan Nie,Yifeng Zhou,Linyong Song,Pengpeng Chen
The purpose of this study was to investigate the suitability of a six-arm star-shaped poly( l -lactide)s (s-PLLA) as controlled drug carriers for hydrophobic drug molecules. First, s-PLLA was synthesized by ring-opening polymerization of l -lactide using sorbitol as initiator and stannous octoate as catalyst. The structure and molecular weight ( M w ) of s-PLLA was characterized with 1 H NMR, 13 C NMR, and GPC. Second, rifampicin (RIF) used as a model drug was encapsulated within the microspheres of s-PLLA via oil-in-water emulsion/solvent evaporation technique. The morphology, drug encapsulation efficiency (EE), and in vitro release behavior of the prepared microspheres were studied in details. Results indicated that the average diameters of s-PLLA microspheres can be controlled between 8 and 20 µm by varying the copolymer's concentration or M w . The EE of RIF was mainly determined by the concentration of s-PLLA. The in vitro study showed that the burst release behavior can be depressed by increasing the M w of the s-PLLA. Present work suggests that the synthesized s-PLLA could be used as a new material for drug delivery. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132 , 42213.
研究领域:
材料科学
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药学
·
生物医学工程
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产品关联
DOI
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2022
·
IF 4.831
Yi Zhang,Qingbo Deng,Chang Tang,Minglu Zhang,Zilong Huang,Zhifeng Cai
Development of excellent sensors to determine trace concentrations of rifampicin is of intense importance for medicine analysis and human health. Herein, a facile and green fluorescent probe was established for the determination of rifampicin by using folic acid protected copper nanoclusters (FA-Cu NCs). Many characterization methods were applied for the analysis of the as-prepared FA-Cu NCs including UV–visible absorption spectra, fluorescence spectra, Fourier-transform infrared spectroscopy (FT-IR), transmission electron microscope (TEM), fluorescence lifetime and X-ray photoelectron spectroscopy (XPS). The TEM image suggested that the as-prepared FA-Cu NCs were highly dispersed. The as-synthesized FA-Cu NCs emerged blue fluorescence under UV light and demonstrated maximum emission wavelength at 446 nm under the maximum excitation wavelength of 358 nm. After the addition of rifampicin, the FL intensities of FA-Cu NCs were uncommonly quenched. The related experimental data intimated that the quenching mechanisms were assumed to the inner filter effect (IFE) and static quenching. The as-proposed probe platform displayed an obvious linear relationship with rifampicin concentrations varying from 0.5 to 100 µM, and the corresponding detection limit (LOD) was 0.073 µM (S/N = 3). Finally, the as-established detection platform was successfully employed to analyze trace concentrations of rifampicin in real samples.
研究领域:
分析化学
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医学检测
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纳米技术
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产品关联
DOI
PubMed
高影响因子
Journal of Cleaner Production
·
2019
·
IF 6.395
Ze Lin,Xiulan Weng,Gary Owens,Zuliang Chen
Most environmental contaminants exist as a complex mixture of both metallic and organic pollutants and it is thus often a major challenge to remove both components simultaneously. In this paper, due to its low cost and environmentally friendliness, iron nanoparticles (Fe NPs) were successfully prepared using a one-step green synthesis for the simultaneous in-situ remediation of mixed contaminants. Specifically Fe NPs were used for the simultaneous removal of Pb(II) and rifampicin. The removal efficiency for Pb(II) and rifampicin were 100% and 91.6%, respectively. To better understand the mechanism of mixed contaminant removal by Fe NPs various characterization methods and the major conditions impacting removal efficiency were examined. It was concluded that (1) polyphenols and caffeine, both ubiquitous in green tea extracts, acted as both reducing and capping agents during the preparation of Fe NPs, reducing the agglomeration of Fe NPs and increasing their stability and reactivity; (2) the removal mechanism of contaminants involved Pb(II) being adsorbed onto the surface of Fe NPs due to the innate strong adsorption of metal ions onto iron oxides , while rifampicin and Pb(II) both interacted positively with the functional groups on the surface of Fe NPs. Overall, this study demonstrated that green synthesis Fe NPs had potential for use as inexpensive and efficient adsorbent for the simultaneous removal of both Pb(II) and rifampicin from wastewater.
研究领域:
环境科学
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纳米技术
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生物学
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产品关联
DOI
高影响因子
JOURNAL OF LUMINESCENCE
·
2012
·
IF 2.102
Zhengqing Liu,Pengfei Yin,Huiping Gong,Pingping Li,Xiaodan Wang,Youqiu He
Aqueous glutathione (GSH)-capped CdTe / ZnS QDs with the diameter of 3–4 nm were synthesized. The fluorescence of CdTe / ZnS QDs at 577 nm was quenched in the presence of rifampicin (Rfp), with excitation wavelength at 350 nm. The mechanism of the interaction of CdTe / ZnS QDs with Rfp was investigated. Under the optimal conditions, the calibration plot of ln( F 0 /F ) was linear in the range 0.83–56 μg mL −1 with concentration of Rfp, and the detection limit was 0.25 μg mL −1 . The proposed method was successfully applied to the determination of Rfp in its commercial capsules, and satisfactory results were obtained. The recovery of the method was in the range 98.6–103.2%.
研究领域:
分析化学
·
药学
✓ 已验证
DOI
高影响因子
CHEMOSPHERE
·
2021
·
IF 7.086
Chao Xue,Wanling Cai,Xiulan Weng,Gary Owens,Zuliang Chen
The use of biomass for the synthesis of value-added products, such as functional nanomaterial for the removal of contaminants, is a challenge. In this study, hybrid bimetallic Fe/Ni nanoparticles and reduced graphene supported bimetallic Fe/Ni nanoparticles (Fe/Ni-rGO) were prepared via a one-step green synthesis using green tea extract, and thereafter evaluated for the simultaneous removal of rifampicin (RIF) and Pb(II) from aqueous solution. The efficiencies of Pb(II) and RIF removal by Fe/Ni-rGO were 87.5 and 96.8%, respectively. The removal performance of the hybrid Fe/Ni-rGO was better than either n Fe/Ni, rGO, or Fe-rGO. Detailed characterization and analyses of Fe/Ni-rGO indicated that both Fe and Ni nanoparticles were evenly distributed over the surface of rGO and that aggregation of Fe, Ni nanoparticles, and stacking of rGO in the hybrid were decreased. Furthermore, while LC-TOF-MS analysis showed that RIF was degraded into small-molecule fragments, XPS showed that Pb(II) was not reduced to Pb 0 . The major conditions impacting removal efficiency, adsorption kinetics, and fit to adsorption isotherm models were examined to better understand the removal mechanism. While the adsorption of both contaminants fit well a pseudo-second-order kinetic model, the adsorption of RIF fit the Freundlich isotherm model best, while the adsorption of Pb(II) fit the Langmuir isotherm model best. Thus, the removal mechanism of both contaminants firstly being chemical adsorbed onto the surface, while n Fe/Ni continues to participate in the catalytic reduction of RIF. Moreover, Fe/Ni-rGO could be reused and performed well for wastewater treatment , thus suitable as a practical resource recycling technology .
研究领域:
环境科学
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纳米材料科学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2022
·
IF 8.025
Shumei Zhang,Shaoyun Shan,Heng Zhang,Xin Gao,Xiaoning Tang,Keli Chen
Wound healing is a challenged and complicated process due to the bacterial infections and frequent replacement in healing process. Hydrogels with properties of visibility and biocompatibility provided convenient and effective treatment during the wound healing process. Bamboo parenchyma cells have a great potential utilized on cellulosic materials fabrication for their high specific surface area and accessibility of chemical reagents. Herein, we present a simple and facile manufacture of transparent wound dressing from bamboo parenchymal cellulose via dissolution in DMAc/LiCl system. Rifampicin (RIF) was loaded on the hydrogel through immersion method. The result exhibited that the maximum drug loading efficiency of cellulose hydrogels was 82.13%. Hydrogel loaded RIF (HLR) showed that the inhibition zones against Gram-negative and Gram-positive bacteria were 19.11 mm and 36.93 mm, respectively. It was observed that the wound was healed more than 60% at 11th day in murine wound models. Meanwhile, RIF provided an exceptionally antibacterial property to hydrogels and promoted proliferation of epidermis cells in wound. As a result of observations, HLR demonstrating potential application in visual wound dressing materials for their excellent transparency, antibacterial effect, wound healing, and biocompatibility.
研究领域:
生物医学工程
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材料科学
·
药学
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产品关联
DOI
PubMed
高影响因子
DRUG METABOLISM AND DISPOSITION
·
2014
·Vol. 42
·期 5
·839-843
·
IF 3.334
Ke Li,Sylvia Zhao,Lingling Zhang,Xiaoyun Wu,Pan Shu,Yang Wang,Hao Feng,Zheming Gu,Helen Han Hsu
It has been proposed that in humans 4β-hydroxycholesterol is formed mainly by CYP3A-catalyzed metabolism of cholesterol and thus may serve as an endogenous marker for CYP3A activity. The cynomolgus monkey is widely used as one of the nonrodent preclinical safety species in pharmaceutical research. In the current study, the potential application of 4β-hydroxycholesterol as an endogenous biomarker of CYP3A in response to drug treatment was evaluated in cynomolgus monkeys. Following multiple oral administration of rifampicin (a known CYP3A inducer) at 15 mg/kg/d in cynomolgus monkeys, the mean serum 4β-hydroxycholesterol levels increased 4-fold from the baseline of 55.3 ± 21.7 to 221 ± 53.4 ng/ml. The mean concentration ratios of 4β-hydroxycholesterol to cholesterol increased 5-fold. The data suggest that 4β-hydroxycholesterol formation from cholesterol metabolism was induced by rifampicin treatment in monkeys. This observation correlated with the metabolism of midazolam (a probe substrate of CYP3A activity) monitored in the same study. The serum exposure (area under the curve) of midazolam was markedly decreased by ∼95%, confirming the induction of CYP3A catalytic activity by rifampicin treatment in monkeys. The formation of 4β-hydroxycholesterol from cholesterol was specifically mediated by recombinant cynomolgus CYP3A8 and CYP3A5. The Km values of CYP3A8 and CYP3A5 for 4β-hydroxycholesterol formation from cholesterol were 204 and 104 μM, respectively, and Vmax values were 0.600 and 0.310 pg/pmol/min, respectively. The results suggest that 4β-hydroxycholesterol can be used as an endogenous biomarker to identify strong CYP3A inducers in cynomolgus monkeys, which may help to evaluate drug-drug interaction potential of drug candidates in preclinical settings.
研究领域:
药理学
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毒理学
·
生物化学
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DOI
PubMed
高影响因子
Applied Nanoscience
·
2021
·Vol. 11
·期 8
·2271-2280
·
IF 3.674
Liu Yueqi,Li Chenxi,Chen Jia,Han Yufen,Wei Ming,Liu Jun,Yu Xiaomin,Li Fangjun,Hu Ping,Fu Lulu,Liu Yong
Rifampicin (RIF) and Isoniazid (INH) are two first-line drugs for tuberculosis treatment. Compared to isoniazid, rifampicin has poor water solubility, which results in low bioavailability. Combining the two drugs can improve the treatment effect of tuberculosis, but thier direct contact may accelerate the degradation of rifampicin, which is also considered to be another reason for RIF’s low bioavailability. In this study, the polyvinylpyrrolidone (PVP) was selected as the carrier and mixed with the loaded drug of rifampicin and isoniazid separately. The quick-released rifampicin/isoniazid-polyvinylpyrrolidone mingled fibers (RIPMF) were fabricated by the electrospinning method to promote the absorption of rifampicin. The results showed that isoniazid-polyvinylpyrrolidone (INH-PVP) nanofibers and rifampicin-polyvinylpyrrolidone (RIF-PVP) microfibers were mixed in RIPMF, instead of two drugs coexisting in one fiber. Rifampicin and isoniazid in the fibers changed from crystalline to amorphous states, which facilitated the release of the rifampicin from the fibers. The hydrophilicity of RIF-PVP fibers was not distinct, but that of RIPMF increased with the addition of INH-PVP fibers. The release rate of rifampicin in rifampicin-loaded fibers was twice as fast as rifampicin powder. Additionally, in vitro antibacterial test showed that RIPMF had an obvious inhibition effect on Staphylococcus aureus . Finally, the rifampicin-loaded fibers enhanced the release rate of rifampicin and improved its bioavailability. Increased bioavailability reduces the waste of rifampicin and prevents damage to the kidneys due to the massive metabolism of rifampicin in biomedicine.
研究领域:
药学
·
材料科学
·
微生物学
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产品关联
DOI
高影响因子
POLYMER BULLETIN
·
2015
·Vol. 73
·期 1
·97-112
·
IF 1.438
Teng Lijing,Nie Wangyan,Zhou Yifeng,Chen Pengpeng
In this paper, a series of star-shaped poly( l -lactide)s (s-PLLA) were synthesized via ring-opening polymerization of l -lactide (LLA) using erythritol as initiator. The structure and properties of s-PLLA were characterized by 1 H NMR, GPC and DSC. Then taking rifampicin (RIF) as the model drug, RIF-loaded s-PLLA microspheres were prepared using an oil-in-water emulsion solvent evaporation method. SEM and size analysis indicated that s-PLLA with high monomer/initiator molar ratios (s-PLLA98 and s-PLLA99) could form regular microspheres with smooth surface and have narrow size distributions, which hold the drugs well. The XRD spectra of the RIF-loaded microspheres demonstrated that s-PLLA and RIF were both in their amorphous state after the encapsulation process, which might be caused by the impediment effect of each other. The in vitro release profiles of the RIF-loaded microspheres showed that the s-PLLA99 microspheres were able to sustain the release of RIF for a considerable period of time (70–80 % within 180 h) and the release profiles of RIF from s-PLLA microspheres followed the Baker–Lonsdale model equation. Therefore, these biodegradable and biocompatible s-PLLA microspheres may find practical applications as drug delivery carriers.
研究领域:
生物材料学
·
药剂学
·
高分子化学
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产品关联
DOI
高影响因子
Journal of Flow Chemistry
·
2018
·Vol. 8
·期 3
·129-138
·
IF 1.658
Li Xin,Liu Zhuang,Qi Hao,Fang Zheng,Huang Siyu,Miao Shanshan,Guo Kai
To reduce the cost and improve the efficiency for rifampicin preparation, a continuous flow synthesis of rifampicin starting from rifamycin S and tert -butylamine was studied in a microreactor. Two reaction steps and one purification step were coupled in a microreactor, and rifampicin was obtained with 67% overall yield. This method used 25% less 1-amino-4-methyl piperazine and got 16% higher overall yield without changing solvent and purification process between steps. This method has a good potential for further industrial application.
研究领域:
制药工程
·
有机化学
✓ 已验证
DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2018
·
IF 3.997
Bowen Yu,Lu Meng,Sirui Fu,Zhiyu Zhao,Yuhang Liu,Ke Wang,Qiang Fu
The applications of Polylactide (PLA) microspheres in biomedical areas are greatly determined by the size, morphology and internal structure. Taking advantage of the formation of stereocomplex (SC) crystallites between poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), we propose a facile strategy to prepare PLA microspheres with tunable morphology and crystalline structure by compounding PLLA and PDLA. With increasing PDLA content, the crystallinity of SC-PLA rose gradually until the ratio of PLLA and PDLA reached 1:1 and then fell. Correspondingly, the morphology of the microspheres were varied (smooth, porous, golf-ball like, guava like) and higher crystallinity of SC-PLA would lead to a more coarse and porous structure. Finally, three typical kinds of Rifampicin-loaded microspheres with different ratio of PLLA and PDLA (7:3, 3:7, 10:0, sorted by porosity from high to low) were prepared and the release behavior was compared. At 30 h, the cumulative release of 7:3, 3:7 and 10:0 microspheres were 32.6%, 17.8% and 6.0% respectively, indicating that the release profiles were generally determined by the porosity of the microspheres. Our findings not only provide a new strategy to prepare PLA microspheres with controllable morphology but offer additional possibilities for the applications of SC-PLA products in biomedical area.
研究领域:
生物医学工程
·
药学
·
材料科学
✓ 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）