Pharmacological Reports
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2017
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IF 2.587
Ting Wu,Haixin Li,Jiasheng Chen,Ying Cao,Weimin Fu,Pingzheng Zhou,Jianxin Pang
Background Apigenin is a flavonoid compound, widely distributed in natural plants. Various studies have suggested that apigenin has inhibitory effects towards several drug transporters, such as the organic anion transporting (OAT) polypeptides , 1B1 and 1B3 (OATP1B1 and OATP1B3). However, the mechanism by which apigenin interacts with OAT1 has not been well studied. Methods MDCK cells stably-expressing OAT1 were used to examine the inhibitory effects of apigenin on OAT1. UPLC–MS/MS was used to evaluate the in vitro and in vivo effects of apigenin on the uptake of acyclovir by OAT1. Cytotoxicity was determined by the cell viability , MTT assays . Results Apigenin effectively inhibited the activity of OAT1 in a dose-dependent manner with an IC50 value of 0.737 μM. Pre-incubation of cells with apigenin caused a time-dependent inhibition (TDI) of OAT1. Additionally, we examined the interactions between apigenin and acyclovir or adefovir . Data showed that apigenin (1 μM) significantly blocked the uptake of acyclovir by OAT1 in vitro with an inhibition rate of 55%. In vivo , apigenin could increase the concentration of acyclovir in plasma when co-administered with acyclovir. Importantly, the MTT assays showed that, at a dose of 50 μM, apigenin significantly reduced the cytotoxicity of adefovir and substantially increased cell viability from 50.6% to 112.62%. Conclusion Our results demonstrate that apigenin regulates OAT1, and can cause TDI or herb-drug interaction (HDI) when used in combination with acyclovir or adefovir. Therefore, apigenin could be used as a nephroprotective agent when used in combination with the substrates of OAT1.
研究领域:
药理学
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分子生物学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2020
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IF 5.162
Mehdihasan I. Shekh,Jhaleh Amirian,Florian J. Stadler,Bing Du,Yanxia Zhu
Developing a novel scaffold carrier with a sustained and controllable release profile of drug is essential to promote the effective transdermal delivery for acyclovir (ACY). In this work, electrospun polyacrylonitrile nanofibers (PAN NFs) was chemically modified with oxidized chitosan (OC). The modified fibrous scaffold was further loaded with the ACY for drug released investigation. FT-IR and NMR results revealed that the conversion of the functional group for each step has successfully occurred on the surface of the fibers. Through the in-vitro drug release and kinetic study, it demonstrated that ACY could be sustainably and controlled released from the OC modified scaffold following the Korsmeyer-Peppas model with a Fickian diffusion mechanism. The human adipose-derived stem cells and the blood combability evaluation confirmed the obtained scaffold possessed excellent cell biocompatibility and hemocompatibility. It could be concluded that the resultant OC modified scaffold based on electrospun PAN NFs opened a new potential option for the topical/transdermal drug delivery of ACY.
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LIFE SCIENCES
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2022
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IF 6.78
Zhuozhou Hu,Jing Zhou,Liang Han,Xiangxiang Li,Chun Li,Tongyu Wu,Jingjing Liu,Wenyang Zhao,Jia Kang,Xinping Chen
Aims Diabetes mellitus (DM) is a major global health threat characterized by insulin resistance. A new tactic to ameliorate insulin resistance, thereby reversing the exacerbation of DM, is urgently needed. The work is aiming to provide a new strategy for DM treatment as well as to identify new targets. Main methods C57BL/6 N mice were raised with high-fat diet (HFD) and infused with streptozotocin (STZ) to induce diabetes. The blood glucose, serum insulin, blood lipid and oxidative stress were detected. In vitro insulin resistance model experiment has been made to examine the molecular mechanisms underlying anti-diabetic effect of potential active chemicals in human hepatocellular carcinoma cells (HepG2). Key findings Acyclovir, an antiviral nucleotide analog, alleviates insulin resistance by reducing blood lipids as well as oxidative stress and elevating insulin sensitivity on diabetic mice, which is in accord with results in the insulin resistance model of HepG2 cells. Mechanically, acyclovir stimulates pyruvate kinase M1 (PKM1) directly to activate adenosine 5′-monophosphate (AMP)-activated protein kinase (AMPK)/Sirtuin1 (SIRT1) signaling pathway, thus improving insulin resistance. Significance The present study supports that acyclovir should be translated to remedy DM, and PKM1 might be a valuable target to develop new medicines.
研究领域:
药理学
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内分泌学
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分子生物学
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糖尿病研究
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JOURNAL OF PHARMACEUTICAL SCIENCES
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2023
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IF 3.8
Shuang Shan,Jie Hu,Zhiyun Zheng,Shuangying Gui,Yanqiu Long,Danqing Wu,Ning He
Acyclovir is an acyclic purine nucleoside analog that is highly effective in inhibiting the herpes simplex virus . However, topical acyclovir has poor efficacy because of its low skin permeability. This study aimed to develop an acyclovir gel plaster containing sponge spicules (AGP-SS) to achieve synergistic improvements in skin absorption and deposition of acyclovir. The process of preparing the gel plaster was optimized by orthogonal experiments, while the composition of the formulation was optimized using the Plackett-Burman and Box–Behnken experimental designs. The selected formula was tested for physical properties, in vitro release, stability, ex vivo permeation, skin irritation , and pharmacokinetics . The optimized formulation exhibited good physical characteristics. In vitro release and ex vivo permeation studies showed that acyclovir release from AGP-SS was dominated by diffusion with significantly higher skin permeation (20.00 ± 1.07 μg/cm 2 ) than that of the controls ( p < 0.05). Dermatopharmacokinetic analyses revealed that the maximum concentration (78.74 ± 11.12 μg/g), area under the curve (1091.81 ± 29.05 μg/g/h) and relative bioavailability (197.12) of AGP-SS were higher than those of the controls. Therefore, gel plaster containing sponge spicules show potential for development as transdermal delivery systems to achieve higher skin absorption and deposition of acyclovir, especially in deep skin layers.
研究领域:
药剂学
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药物递送系统
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药理学
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ACS Applied Bio Materials
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2018
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IF 0
Lantao Liu,Nan Li,Meijun Chen,Hailin Yang,Qian Tang,Chengbin Gong
The phototoxicity of UV light limits the application of conventional azobenzene-based photoresponsive molecularly imprinted polymers in the biomedical field. This paper reports a tetra-ortho-methoxy-substituted azobenzene, N-(4-((4-amino-2,6-dimethoxyphenyl)diazenyl)-3,5-dimethoxyphenyl)methacrylamide (ADDDM), whose photoswitching is induced by all visible-light irradiation (440 nm for trans form to cis form and 630 nm for cis form to trans form) in N,N-dimethylformamide and tetrahydrofuran (1:9, v/v). Using ADDDM as the monomer, a visible-light-responsive surface molecularly imprinted polymer (VSMIP) on silica microspheres was fabricated for acyclovir (ACV). VSMIP showed a higher drug loading capacity, better specificity, faster drug release rate, and faster photoisomerization rate constant to ACV than the corresponding visible-light-responsive surface molecularly nonimprinted polymer (VSNIP). The selectivity of VSMIP to ACV and competing materials (ganciclovir and triacetylganciclovir) was examined by ultraviolet–visible spectroscopy, and the VSMIP showed excellent specificity of recognition toward ACV. The VSMIP can realize a visible-light-triggered (440/630 nm) release and uptake of ACV through chicken skin tissue (1 mm in thickness).
研究领域:
材料科学
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生物医学工程
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CHEMOSPHERE
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2023
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IF 8.8
Chunsheng Ding,Zhiyue Cai,Chenkai Hu,Jia Lei,Lei Wang,Qingsong Li,Xueyan Li,Jing Deng
Pharmaceutical and personal care products (PPCPs) pose a great threat to water environment security. In this study, acyclovir (ACV) was efficiently degraded by thermally activated persulfate (TAP) system. The ACV degradation increased with rising reaction temperature and persulfate dosage. With the existence of inorganic anions and humic acid , ACV removal was retarded to varying degrees. Under strong alkaline condition, it was observed that the degradation of ACV was significantly inhibited. In addition, Kintecus software was employed to simulate ACV removal and achieved a good fit with the experimental results. The contribution rates of main reactive radicals under acidic, neutral, and alkaline conditions were investigated, and the contribution of hydroxyl radical (⋅OH) increased significantly under alkaline condition. The main active species were identified as sulfate radical (SO 4 ⋅ - ) and ⋅OH through quenching experiment, and the second-order reaction rate constants of SO 4 ⋅ - and ∙OH reacted with ACV were calculated to be 9.17 × 10 9 M −1 s −1 and 2.74 × 10 9 M −1 s −1 , respectively. The main degradation pathways included addition of free radicals, oxidation of branch chain and ring opening. The acute and chronic toxicity of intermediates to organisms predicted by ECOSAR were significantly reduced compared with that of ACV.
研究领域:
环境科学
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药学
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Journal of Environmental Chemical Engineering
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2023
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IF 7.7
Xinghong Qu,Hongxue Zeng,Yongsheng Gao,Dong Xu
In this study, phosphate/thermal activated peroxymonosulfate (PMS) process were applied to degrade the antiviral drug acyclovir (ACV) in water. Both Na 2 HPO 4 and Na 5 P 3 O 10 could effectively enhance ACV removal by thermally activated PMS process and the enhancement of Na 2 HPO 4 was more significant. High reaction temperature favored ACV removal and the best removal can be achieved at a certain PMS dosage in both processes. With increasing Na 2 HPO 4 dosage, the ACV removal first increased and then decreased, while increasing Na 5 P 3 O 10 dosage caused the enhancement of the degradation. The ACV degradation by Na 2 HPO 4 /thermal/PMS system was easily affected by initial solution pH, while Na 5 P 3 O 10 /thermal/PMS system operated in a wider pH range. The addition of Cl - and NO 3 - exerted insignificant effect in Na 2 HPO 4 /thermal/PMS process, while posed complicated impact by Na 5 P 3 O 10 /thermal/PMS process. The presence of HA significantly retarded ACV degradation by Na 2 HPO 4 /thermal/PMS system, while in Na 5 P 3 O 10 /thermal/PMS system, high HA concentration accelerated the degradation. In Na 2 HPO 4 /thermal/PMS system, SO 4 •- and •OH were identified as the main active species. Whereas, the ACV degradation was relied on non-free radicals ( 1 O 2 ) in Na 5 P 3 O 10 /thermal/PMS process. The strengthening effect of Na 2 HPO 4 was reflected in its ability to reduce the reaction energy barrier required for O-O bond cleavage in PMS molecules, while Na 5 P 3 O 10 provided an alkaline condition for the self-decomposition of PMS. 10 and 11 intermediate products were detected in Na 2 HPO 4 /thermal/PMS and Na 5 P 3 O 10 /thermal/PMS systems, respectively. Both processes produced intermediates with higher toxicity than ACV according to software analysis.
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CHEMICAL ENGINEERING JOURNAL
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2026
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IF 12.5
Zijun Dong,Feng Wang,Xiangsheng Chen,Jingyun Fang,Xuechuan Li,Ting Zhou
UV/PAA achieves efficiency ACV removal across a broad pH. • Both •OH and R-C• synergistically drive ACV oxidation. • DFT and LC-MS/MS identify distinct pathways yielding low-toxicity products. • The dual-function system highly inactivates chlorine-resistant B. subtilis . Acyclovir (ACV) is an emerging antiviral contaminant posing risks to aquatic ecosystems. This study proposed the application of the UV/peracetic acid (UV/PAA) process as a novel dual-function technology for simultaneous ACV elimination and water disinfection. The UV/PAA process achieved 97.6% ACV removal within 30 min under the optimized conditions (2.5 mM PAA and 1800 μW/cm 2 UV intensity) while maintaining stable degradation performance across a broad pH range (3.0–11.0). Mechanistic analysis indicated that ACV degradation was governed by the combined action of hydroxyl radicals (•OH) and carbon-centered radicals (R-C•), with •OH serving as the dominant reactive species (57.4–65.6%). Density functional theory (DFT) coupled with LC-MS/MS revealed distinct addition and substitution pathways that structurally transform ACV into low-toxicity products. Furthermore, addressing a critical biosecurity challenge, the process exhibited exceptional biocidal synergy, achieving a 3.79 log inactivation of chlorine-resistant Bacillus subtilis spores. Overall, the results provided mechanistic insight into ACV degradation by UV/PAA and supported its potential application for the simultaneous control of pharmaceutical contaminants and microbial risks in water treatment. Download: Download high-res image (255KB) Download: Download full-size image
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2024
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IF 4.9
Nana Tang,Aiting Chen,Yanping Wei,Shuting Shi,Chuanqin Zhou,Quanguo He,Jun Liu
Acyclovir (Acyclovir, ACV) is an antiviral drug which, despite its favorable safety profile, can have systemic adverse effects, following improper use. This study prepared a clay-like two-dimensional transition metal carbide Ti 3 C 2 by etching Ti 3 AlC 2 with LiF and HCl. Carboxylated multi walled carbon nanotubes (Carboxylated multi-walled carbon nanotubes , MWCNTs-COOH) were combined with Ti 3 C 2 using chitosan (Chitosan, CS) as solvent and ultrasonic treatment . The nanocomposite was then modified onto the surface of a glassy carbon electrode (Glassy carbon electrode, GCE) to develop an electrochemical sensor for the detection of ACV. The Ti 3 C 2 -CS-MWCNTs-COOH/GCE nanocomposite was characterized by X-ray diffractometry (X-ray diffractometry, XRD), scanning electron microscope (Scanning electron microscope，SEM), and cyclic voltammetry (Cyclic voltammetry，CV), as well as the electrochemical impedance method (Electrochemical impedance，EIS). The successful preparation of Ti 3 C 2 -CS-MWCNTs-COOH, and the good electrochemical performance of the electrode were verified. Linear scanning voltammetry (Linear scan voltammetry，LSV) was used to quantify the ACV. The linear range of the method is wider than other works (0.05 ∼ 20.0 and 20.0 ∼ 500.0 μM), with a low detection limit (0.088 μM). The sensor achieves sensitive detection of ACV and can be used for the analysis of ACV in pharmaceutical and urine dosage forms , with recoveries of 95.5∼97.6% and 95.6∼97.5%, respectively. For the first time, this sensor utilizes clay-like Ti 3 C 2 with a larger specific surface area in combination with MWCNTs-COOH for ACV detection, which exhibits excellent immunity to interference, repeatability, reproducibility, and stability. This method provides a rapid and sensitive method for the determination of ACV, and lays foundations for developing miniaturized field rapid test detectors.
研究领域:
药理学
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分析化学
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2022
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IF 5.518
Yanping Wei,Liangyuan Yao,Yiyong Wu,Xia Liu,Jinxia Feng,Jianhua Ding,Kanghua Li,Quanguo He
An electrochemical sensor based on ferrous molybdate (FeMoO 4 ) loaded graphene oxide composites was prepared and used for the ultrasensitive detection of Acyclovir in nanomolar concentrations. FeMoO 4 nanorods were prepared by hydrothermal method , and loaded with graphene oxide by ultrasonication. The materials were characterized by Scanning Electron Microscopy, X-ray diffractometer and Energy Dispersive Spectroscopy . The electrochemical sensor was fabricated by drop-coating method for the determination of Acyclovir. The sensing performance was investigated by cyclicvoltammetry, electrochemical impedance and linear sweep voltammogram. The results showed that the optimal signals appeared on the electrode. Furthermore, the oxidation peak current was linearly related to the Acyclovir concentration in the range of 0.1–10 μM and 10–100 mM. The limit of detection was 20 nM (S/N = 3). The sensor was used to analyze in process and in situ Acyclovir drug samples with good recoveries of 95.0–100.0% and excellent accuracy in nanomolarity.
研究领域:
分析化学
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药物分析
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电化学传感器
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高影响因子
Frontiers in Chemistry
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2022
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IF 5.545
Lu Xin-Yang,Li Jing,Kong Fen-Ying,Wei Mei-Jie,Zhang Pei,Li Ying,Fang Hai-Lin,Wang Wei
An electrochemical sensor for sensitive sensing of acyclovir (ACV) was designed by using the reduced graphene oxide–TiO2–Au nanocomposite-modified glassy carbon electrode (rGO–TiO2–Au/GCE). Transmission electron microscopy, X-ray diffractometer, and X-ray photoelectron spectroscopy were used to confirm morphology, structure, and composition properties of the rGO–TiO2–Au nanocomposites. Cyclic voltammetry and linear sweep voltammetry were used to demonstrate the analytical performance of the rGO–TiO2–Au/GCE for ACV. As a result, rGO–TiO2–Au/GCE exerted the best response for the oxidation of ACV under the pH of 6.0 PB solution, accumulation time of 80 s at open-circuit, and modifier amount of 7 µl. The oxidation peak currents of ACV increased linearly with its concentration in the range of 1–100 µM, and the detection limit was calculated to be 0.3 µM (S/N = 3). The determination of ACV concentrations in tablet samples also demonstrated satisfactory results.
研究领域:
分析化学
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生物医学工程
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材料科学
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JOURNAL OF THE ELECTROCHEMICAL SOCIETY
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2024
·Vol. 171
·期 1
·013503
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IF 3.1
Lanlan Wei,Lin Wang,Lu Chen,Yifan Ru,Lianzhong Shen,Yu Ye,Zhouwei Li,Qizhou Dai
A three-dimensional porous lead dioxide electrode (3D-PbO2) was developed by the template electrodeposition approach. Polystyrene microspheres were prepared by microemulsion polymerization, and then the polystyrene template was loaded on the PbO2 electrode by electrodeposition. Finally, a porous structure was formed by removing the template. Under these optimized conditions, the degradation of acyclovir could achieve complete removal, while the removal of COD was 29.59%. The electrochemical degradation process of acyclovir was consistent with the proposed primary reaction kinetics. The 3D-PbO2 electrode was comprehensively characterized using SEM, XRD, and XPS techniques. The SEM analysis revealed the presence of well-defined porous structures on the electrode surface, while the XRD results indicated a reduction in electrode crystal sizes. Additionally, the XPS analysis demonstrated a higher proportion of reactive oxygen species on the 3D-PbO2 electrode. The electrochemical properties of the electrode were investigated using CV and EIS. The experimental findings demonstrate that the 3D-PbO2 electrode exhibits a higher oxygen evolution potential and lower charge transfer resistance than the conventional PbO2 electrode. This study presents a viable approach to enhance the electrochemical oxidation performance of lead dioxide.
研究领域:
环境科学
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电化学
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材料科学
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高影响因子
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