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  • Zhang, Jiaojiao  (6)
  • Pharmacy  (6)
  • 1
    In: Fundamental & Clinical Pharmacology, Wiley, Vol. 38, No. 3 ( 2024-06), p. 579-587
    Abstract: It was evidenced that cetylpyridinium‐chloride (CPC) mouthwash could inhibit SARS‐COV‐2 activity and reduce salivary viral load, thus reducing SARS‐CoV‐2 transmission. However, due to insufficient residence time in the oral cavity, CPC‐containing mouthwashes have no prolonged antiviral effect. The duration of action of the CPC buccal tablet is expected to be longer than that of the mouthwash. However, there are currently no reports on the salivary drug concentration of CPC buccal tablets. Objective The study aimed to investigate the salivary drug concentration of CPC buccal tablets and the antiviral effect of CPC on SARS‐CoV‐2 in vitro. Trial design This is a single‐dose, single‐arm clinical trial, involving 10 Chinese healthy subjects who received 2‐mg CPC buccal tablet to collect saliva samples and to detect saliva concentration at different timepoints within 2 h (Clinical Trial Registration Number: NCT05802628, Registration Date: April 6, 2023). Materials and methods CPC concentration in saliva was detected by liquid chromatography tandem mass spectrometry (LC–MS/MS), and pharmacokinetic parameters were calculated based on the non‐compartmental model. With an in vitro antiviral experiment, the activity of CPC buccal tablets against SARS‐CoV‐2 and its cellular toxicity was tested. Results Drug concentrations in saliva at 15 min, 30 min, 1 h, 1.5 h, and 2 h after administration were 8008.33 (1042.25, 41081.11), 2093.34 (373.15, 5759.83), 1016.58 (378.66, 3480.68), 891.77 (375.66, 6322.07), and 717.43 (197.87, 2152.71) ng/mL. PK parameters of saliva concentration: C max = 8008.33 (1042.25, 41081.11) ng/mL, AUC 0‐t = 4172.37 (904.42, 13912.61) ng/mL * h, AUC 0‐∞ = 6712.85 (1856.77, 19971.12) ng/mL * h, T 1/2 = 1.22 (0.59, 2.83) h, T max = 0.25 (0.25, 0.25) h. As determined in in vitro experiment, CPC was active on SARS‐CoV‐2 with cytotoxic and inhibitory activity of CC50 = 35.75 μM (≈12155 ng/mL) and EC50 = 7.39 μM (≈2512.6 ng/mL). Conclusions The comparison between the salivary CPC concentration and EC50/CC50 values from in vitro antiviral experiments suggests that CPC buccal tablets may inhibit SARS‐CoV‐2 activity, and the inhibition may last for approximately 30 min without cytotoxicity.
    Type of Medium: Online Resource
    ISSN: 0767-3981 , 1472-8206
    URL: Issue
    Language: English
    Publisher: Wiley
    Publication Date: 2024
    detail.hit.zdb_id: 2006242-4
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  • 2
    Online Resource
    Online Resource
    Bentham Science Publishers Ltd. ; 2020
    In:  Anti-Cancer Agents in Medicinal Chemistry Vol. 20, No. 5 ( 2020-05-28), p. 559-570
    In: Anti-Cancer Agents in Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 20, No. 5 ( 2020-05-28), p. 559-570
    Abstract: The Hepatocyte Growth Factor Receptor (HGFR) c-Met is over-expressed and/or mutated in various human tumor types. Dysregulation of c-Met/HGF signaling pathway affects cell proliferation, survival and motility, leading to tumor growth, angiogenesis, and metastasis. Therefore, c-Met has become an attractive target for cancer therapy. Objective: This study is aimed to evaluate a new series of 4-phenoxypyridine derivatives containing semicarbazones moiety for its cytotoxicity. Methods: A series of novel 4-phenoxypyridines containing semicarbazone moieties were synthesized and evaluated for their in vitro cytotoxic activities against MKN45 and A549 cancer cell lines and some selected compounds were further examined for their inhibitory activity against c-Met kinase. In order to evaluate the mechanism of cytotoxic activity of compound 24, cell cycle analysis, Annexin V/PI staining assay, AO/EB assay, wound-healing assay and docking analysis with c-Met were performed. Results: The results indicated that most of the compounds showed moderate to good antitumor activity. The compound 28 showed well cytotoxic activity against MKN45 and A549 cell lines with IC50 values of 0.25μM and 0.67μM, respectively. Compound 24 showed good activity on c-Met and its IC50 value was 0.093μM. Conclusion: Their preliminary Structure-Activity Relationships (SARs) studies indicated that electronwithdrawing groups on the terminal phenyl rings are beneficial for improving the antitumor activity. Treatments of MKN45 cells with compound 24 resulted in cell cycle arrest in G2/M phase and induced apoptosis in a dose-dependent manner. In addition, AO/EB assays indicated 24 induced dose-dependent apoptosis of A549 and MKN45 cells. Wound-healing assay results indicated that compound 24 strongly inhibited A549 cell motility.
    Type of Medium: Online Resource
    ISSN: 1871-5206
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2020
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  • 3
    Online Resource
    Online Resource
    Bentham Science Publishers Ltd. ; 2021
    In:  Current Medicinal Chemistry Vol. 28, No. 6 ( 2021-02), p. 1251-1268
    In: Current Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 28, No. 6 ( 2021-02), p. 1251-1268
    Abstract: Systemic lupus erythematosus (SLE) is an autoimmune disease characterized by a local or systemic inflammatory response. At present, the increasing research results show that the pathogenesis of the disease is complex, and the methods of clinical treatment also show diversity. This review analyzes and summarizes the existing mechanism research and drug treatment methods in order to provide a reference value for further drug research and development. Method: We carried out a thorough literature search using databases. According to the main purpose of the article, irrelevant articles were excluded after further examination and directly relevant articles were included. Finally, the information related to the article was summarized. Result: In this article, seventy-four articles are included. According to related articles, there are mainly four kinds of drugs, namely antimalarial drugs, glucocorticoids, immunosuppressive agents and biological agents. About fifty-five articles summarized the drugs for the treatment of systemic lupus erythematosus. The rest of the articles were related to the research progress of the mechanism of systemic lupus erythematosus. Conclusion: This article describes the pathogenesis of systemic lupus erythematosus, and summarizes the traditional and new therapeutic drugs, which is not only beneficial to the treatment of lupus erythematosus patients, but also plays a vital reference significance for the future development of new systemic lupus erythematosus drugs.
    Type of Medium: Online Resource
    ISSN: 0929-8673
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2021
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  • 4
    Online Resource
    Online Resource
    Frontiers Media SA ; 2022
    In:  Frontiers in Pharmacology Vol. 13 ( 2022-11-14)
    In: Frontiers in Pharmacology, Frontiers Media SA, Vol. 13 ( 2022-11-14)
    Abstract: Background: In recent years, several clinical trials have focused on oncolytic virus (OVs) combined with chemotherapy or immune checkpoint inhibitors (ICIs) in solid tumor patients, which showed encouraging effects. However, few studies have concentrated on the summary on the safety and efficacy of the combined treatments. Therefore, we conducted this meta-analysis to explore the safety and curative effect of the combined therapy. Methods: We searched the PubMed, Cochrane Library, Embase, and Clinicaltrials.gov databases to comprehensively select articles on OVs combined with chemotherapy or ICIs for the solid tumor treatment. Overall survival (OS), progression-free survival (PFS), 1-year survival rate, 2-year survival rate, objective response rate (ORR), and adverse events (AEs) were the outcomes. Results: Fifteen studies with 903 patients were included in this meta-analysis. The pooled ORR was 32% [95% confidence interval (CI): 27–36%, I 2 = 24.9%, p = 0.239]. Median OS and median PFS were 6.79 months (CI: 4.29–9.30, I 2 = 62.9%, p = 0.044) and 3.40 months (CI: 2.59–4.22, I 2 = 0.0%, p = 0.715), respectively. The 1-year survival rate was 38% (CI: 0.29–0.47, I 2 = 62.9%, p = 0.044), and the 2-year survival rate was 24% (CI: 12–37%, I 2 = 0.0%, p = 0.805). The most common AEs were fever (63%, CI: 57–69%, I 2 = 2.3%, p = 0.402), fatigue (58%, CI: 51–65%, I 2 = 49.2%, p = 0.096), chill (52%, CI: 43–60%, I 2 = 0.0%, p = 0.958), and neutropenia (53%, CI: 47–60%, I 2 = 0.0%, p = 0.944). Conclusion: OVs combined with ICIs showed a better efficacy than OVs combined with chemotherapy, which lends support to further clinical trials of OVs combined with ICIs. In addition, OVs combined with pembrolizumab can exert increased safety and efficacy. The toxicity of grades ≥3 should be carefully monitored and observed. However, high-quality, large-scale clinical trials should be completed to further confirm the efficacy and safety of OVs combined with ICIs. Systematic Review Registration : [ https://www.crd.york.ac.uk/PROSPERO/login.php ], identifier [RD42022348568] .
    Type of Medium: Online Resource
    ISSN: 1663-9812
    Language: Unknown
    Publisher: Frontiers Media SA
    Publication Date: 2022
    detail.hit.zdb_id: 2587355-6
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  • 5
    Online Resource
    Online Resource
    Bentham Science Publishers Ltd. ; 2021
    In:  Current Drug Delivery Vol. 18, No. 3 ( 2021-05-17), p. 357-368
    In: Current Drug Delivery, Bentham Science Publishers Ltd., Vol. 18, No. 3 ( 2021-05-17), p. 357-368
    Abstract: The purpose of this study is to develop a new PLGA based formulation for microspheres, which aims to release mometasone furoate for one month, so as to improve compliance. Methods: The microspheres containing mometasone furoate were prepared by oil in water emulsion and solvent evaporation. The microspheres were characterized by surface morphology, shape, size and encapsulation efficiency. The release in vitro was studied in 37°C phosphate buffer, and in vivo, pharmacodynamics and preliminary safety evaluation were conducted in male Sprague Dawley rats. Results: The morphology results showed that the microspheres have a smooth surface, spherical shape and an average diameter of 2.320-5.679μm. The encapsulation efficiency of the microspheres loaded with mometasone furoate was in the range of 53.1% to 95.2%, and the encapsulation efficiency of the microspheres could be greatly affected by the proportion of oil phase to the water phase and other formulation parameters. In vitro release kinetics revealed that drug release from microspheres was through non-Fick's diffusion and PLGA polymer erosion. Pharmacokinetic data showed that the initial release of microspheres was small and then sustained. The results of the pharmacodynamics study fully proved the long-term effectiveness of mometasone furoate microspheres. The results of in vivo safety evaluation showed that the preparation system possessed good in vivo safety. Conclusion: This study shows that the microspheres prepared in this study have sufficient ability to stable drug release at least for 35 days, with good efficacy and high safety. In addition, mometasone furoate can be used as a potential candidate drug for 35 days long-term injection.
    Type of Medium: Online Resource
    ISSN: 1567-2018
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2021
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  • 6
    In: Current Drug Delivery, Bentham Science Publishers Ltd., Vol. 19 ( 2021-09-28)
    Abstract: The article has been withdrawn at the request of the editor of the journal Current Drug Delivery due to incoherent content. The Bentham Editorial Policy on Article Withdrawal can be found at https://benthamscience.com/editorial-policies-main.php Bentham Science Disclaimer: It is a condition of publication that manuscripts submitted to this journal have not been published and will not be simultaneously submitted or published elsewhere. Furthermore, any data, illustration, structure or table that has been published elsewhere must be reported, and copyright permission for reproduction must be obtained. Plagiarism is strictly forbidden, and by submitting the article for publication the authors agree that the publishers have the legal right to take appropriate action against the authors, if plagiarism or fabricated information is discovered. By submitting a manuscript, the authors agree that the copyright of their article is transferred to the publishers if and when the article is accepted for publication.
    Type of Medium: Online Resource
    ISSN: 1567-2018
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2021
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