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  • MDPI AG  (52)
  • Pharmacy  (52)
  • 1
    Online Resource
    Online Resource
    Xyloketal B Attenuates Atherosclerotic Plaque Formation and Endothelial Dysfunction in Apolipoprotein E Deficient Mice
    MDPI AG ; 2015
    In:  Marine Drugs Vol. 13, No. 4 ( 2015-04-14), p. 2306-2326
    Details
    In: Marine Drugs, MDPI AG, Vol. 13, No. 4 ( 2015-04-14), p. 2306-2326
    Type of Medium: Online Resource
    ISSN: 1660-3397
    URL: Article
    DOI: 10.3390/md13042306
    Language: English
    Publisher: MDPI AG
    Publication Date: 2015
    detail.hit.zdb_id: 2175190-0
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  • 2
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    A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential
    MDPI AG ; 2022
    In:  Pharmaceutics Vol. 14, No. 2 ( 2022-01-21), p. 249-
    Details
    In: Pharmaceutics, MDPI AG, Vol. 14, No. 2 ( 2022-01-21), p. 249-
    Abstract: Enrofloxacin (EFX) reacting with Ca(II) afforded a new complex, [Ca(EFX)2(H2O)4] (EFX-Ca), which was structurally characterized both in solid and solution chemistry. E. coli and S. typhi were tested to be the most sensitive strains for EFX-Ca. The LD50 value of EFX-Ca in mice was 7736 mg/kg, implying the coordination of EFX to Ca(II) effectively reduced its acute toxicity. EFX-Ca also decreased the plasma-binding rate and enhanced the drug distribution in rats along with longer elimination half-life. EFX-Ca also showed similar low in vivo acute toxicity and higher anti-inflammation induced by H2O2 or CuSO4 in zebrafish, with reactive oxygen species (ROS)-related elimination. The therapeutic effects of EFX-Ca on two types (AA and 817) of E. coli-infected broilers were also better than those of EFX, with cure rates of 78% and 88%, respectively. EFX-Ca showed promise as a bio-safe metal-based veterinary drug with good efficacy and lower toxicity.
    Type of Medium: Online Resource
    ISSN: 1999-4923
    URL: Article
    DOI: 10.3390/pharmaceutics14020249
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2527217-2
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  • 3
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    Emerging Bioactive Agent Delivery-Based Regenerative Therapies for Lower Genitourinary Tissues
    MDPI AG ; 2022
    In:  Pharmaceutics Vol. 14, No. 8 ( 2022-08-17), p. 1718-
    Details
    In: Pharmaceutics, MDPI AG, Vol. 14, No. 8 ( 2022-08-17), p. 1718-
    Abstract: Injury to lower genitourinary (GU) tissues, which may result in either infertility and/or organ dysfunctions, threatens the overall health of humans. Bioactive agent-based regenerative therapy is a promising therapeutic method. However, strategies for spatiotemporal delivery of bioactive agents with optimal stability, activity, and tunable delivery for effective sustained disease management are still in need and present challenges. In this review, we present the advancements of the pivotal components in delivery systems, including biomedical innovations, system fabrication methods, and loading strategies, which may improve the performance of delivery systems for better regenerative effects. We also review the most recent developments in the application of these technologies, and the potential for delivery-based regenerative therapies to treat lower GU injuries. Recent progress suggests that the use of advanced strategies have not only made it possible to develop better and more diverse functionalities, but also more precise, and smarter bioactive agent delivery systems for regenerative therapy. Their application in lower GU injury treatment has achieved certain effects in both patients with lower genitourinary injuries and/or in model animals. The continuous evolution of biomaterials and therapeutic agents, advances in three-dimensional printing, as well as emerging techniques all show a promising future for the treatment of lower GU-related disorders and dysfunctions.
    Type of Medium: Online Resource
    ISSN: 1999-4923
    URL: Article
    DOI: 10.3390/pharmaceutics14081718
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2527217-2
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  • 4
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    Antibacterial Properties of Gold Nanoparticles in the Modification of Medical Implants: A Systematic Review
    MDPI AG ; 2022
    In:  Pharmaceutics Vol. 14, No. 12 ( 2022-11-30), p. 2654-
    Details
    In: Pharmaceutics, MDPI AG, Vol. 14, No. 12 ( 2022-11-30), p. 2654-
    Abstract: The widespread occurrence of bacterial infections and their increased resistance to antibiotics has led to the development of antimicrobial coatings for multiple medical implants. Owing to their desirable properties, gold nanoparticles (AuNPs) have been developed as antibacterial agents. This systematic investigation sought to analyze the antibacterial effects of implant material surfaces modified with AuNPs. The data from 27 relevant studies were summed up. The included articles were collected from September 2011 to September 2021. According to the retrieved literature, we found that medical implants modified by AuNPs have good antibacterial effects against gram-positive and gram-negative bacteria, and the antibacterial effects would be improved by near-infrared (NIR) radiation.
    Type of Medium: Online Resource
    ISSN: 1999-4923
    URL: Article
    DOI: 10.3390/pharmaceutics14122654
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2527217-2
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  • 5
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    Dihydromyricetin Enhances Intestinal Antioxidant Capacity of Growing-Finishing Pigs by Activating ERK/Nrf2/HO-1 Signaling Pathway
    MDPI AG ; 2022
    In:  Antioxidants Vol. 11, No. 4 ( 2022-04-02), p. 704-
    Details
    In: Antioxidants, MDPI AG, Vol. 11, No. 4 ( 2022-04-02), p. 704-
    Abstract: Oxidative stress is one of the main factors affecting animal health and reducing performance. The small intestine is the primary site of free-radical attacks. Dihydromyricetin (DHM) is a flavonoid compound with antioxidant, anti-inflammatory, and other biological activities, which is mainly extracted from Rattan tea. However, the effects of DHM on the intestinal antioxidant function of growing-finishing pigs and related mechanisms remain unclear. The aim of this study was to investigate the effect of dietary DHM supplementation on the intestinal antioxidant capacity of growing-finishing pigs and its mechanism. Our results show that dietary 0.03% DHM increased the activities of the total antioxidant capacity (T-AOC), catalase (CAT), and glutathione peroxidase (GSH-Px), decreased malondialdehyde (MDA) level, and upregulated protein expressions of HO-1, NQO1, nuclear Nrf2, and phospho-ERK (p-ERK) in the jejunum of growing-finishing pigs. Again, we found that 20 μmol/mL and 40 μmol/mL DHM treatment significantly upregulated the protein expression of HO-1 and promoted the nuclear translocation of Nrf2 and ERK phosphorylation in IPCE-J2 cells. ERK inhibitor PD98059 eliminated the DHM-induced upregulation of p-ERK, nuclear Nrf2, and HO-1. Our findings provided the first evidence that DHM enhanced the intestinal antioxidant capacity of growing-finishing pigs by activating the ERK/Nrf2/HO-1 signaling pathway.
    Type of Medium: Online Resource
    ISSN: 2076-3921
    URL: Article
    DOI: 10.3390/antiox11040704
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2704216-9
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  • 6
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    A Mechanism of Isoorientin-Induced Apoptosis and Migration Inhibition in Gastric Cancer AGS Cells
    MDPI AG ; 2022
    In:  Pharmaceuticals Vol. 15, No. 12 ( 2022-12-12), p. 1541-
    Details
    In: Pharmaceuticals, MDPI AG, Vol. 15, No. 12 ( 2022-12-12), p. 1541-
    Abstract: Isoorientin (ISO) is a flavonoid compound containing a luteolin structure, which can induce autophagy in some tumor cells. This study investigated the impact of ISO in gastric cancer AGS cells, and performed an experimental analysis on the main signaling pathways and transduction pathways it regulates. CCK–8 assay results showed that ISO reduced the survival rate of gastric cancer AGS cells, but the toxicity to normal cells was minimal. Hoechst 33342/PI double staining assay results showed that ISO induced apoptosis in gastric cancer AGS cells. Further analysis by flow cytometry and Western blot showed that ISO induced apoptosis via a mitochondria-dependent pathway. In addition, the level of reactive oxygen species (ROS) in gastric cancer AGS cells also increased with the extension of the ISO treatment time. However, cell apoptosis was inhibited by preconditioning cells with N–acetylcysteine (NAC). Moreover, ISO arrested the cell cycle at the G2/M phase by increasing intracellular ROS levels. Cell migration assay results showed that ISO inhibited cell migration by inhibiting the expression of p–AKT, p–GSK–3β, and β–catenin and was also related to the accumulation of ROS. These results suggest that ISO-induced cell apoptosis by ROS–mediated MAPK/STAT3/NF–κB signaling pathways inhibited cell migration by regulating the AKT/GSK–3β/β–catenin signaling pathway in gastric cancer AGS cells.
    Type of Medium: Online Resource
    ISSN: 1424-8247
    URL: Article
    DOI: 10.3390/ph15121541
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2193542-7
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  • 7
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    Total Synthesis and Anti-Inflammatory Bioactivity of (−)-Majusculoic Acid and Its Derivatives
    MDPI AG ; 2021
    In:  Marine Drugs Vol. 19, No. 6 ( 2021-05-21), p. 288-
    Details
    In: Marine Drugs, MDPI AG, Vol. 19, No. 6 ( 2021-05-21), p. 288-
    Abstract: The first total synthesis of marine natural product, (−)-majusculoic acid (1) and its seven analogs (9–15), was accomplished in three to ten steps with a yield of 3% to 28%. The strategy featured the application of the conformational controlled establishment of the trans-cyclopropane and stereochemical controlled bromo-olefination or olefination by Horner–Wadsworth–Emmons (HWE) reaction. The potential anti-inflammatory activity of the eight compounds (1 and 9–15) was evaluated by determining the nitric oxide (NO) production in the lipopolysaccharide (LPS)-induced mouse macrophages RAW264.7. (−)-Majusculoic acid (1), methyl majusculoate (9), and (1R,2R)-2-((3E,5Z)-6-bromonona-3,5-dien-1-yl)cyclopropane-1-carboxylic acid (12) showed significant effect with inhibition rates of 33.68%, 35.75%, and 43.01%, respectively. Moreover, they did not show cytotoxicity against RAW264.7 cells, indicating that they might be potential anti-inflammatory agents.
    Type of Medium: Online Resource
    ISSN: 1660-3397
    URL: Article
    DOI: 10.3390/md19060288
    Language: English
    Publisher: MDPI AG
    Publication Date: 2021
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  • 8
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    Protective Effect of Flavonoids from a Deep-Sea-Derived Arthrinium sp. against ox-LDL-Induced Oxidative Injury through Activating the AKT/Nrf2/HO-1 Pathway in Vascular Endothelial Cells
    MDPI AG ; 2021
    In:  Marine Drugs Vol. 19, No. 12 ( 2021-12-18), p. 712-
    Details
    In: Marine Drugs, MDPI AG, Vol. 19, No. 12 ( 2021-12-18), p. 712-
    Abstract: Oxidized low-density lipoprotein (ox-LDL)-induced oxidative injury in vascular endothelial cells is crucial for the progression of cardiovascular diseases, including atherosclerosis. Several flavonoids have been shown cardiovascular protective effects. Recently, our research group confirmed that the novel flavonoids isolated from the deep-sea-derived fungus Arthrinium sp., 2,3,4,6,8-pentahydroxy-1-methylxanthone (compound 1) and arthone C (compound 2) effectively scavenged ROS in vitro. In this study, we further investigated whether these compounds could protect against ox-LDL-induced oxidative injury in endothelial cells and the underlying mechanisms. Our results showed that compounds 1 and 2 inhibited ox-LDL-induced apoptosis and adhesion factors expression in human umbilical vein vascular endothelial cells (HUVECs). Mechanistic studies showed that these compounds significantly inhibited the ROS level increase and the NF-κB nuclear translocation induced by ox-LDL. Moreover, compounds 1 and 2 activated the Nrf2 to transfer into nuclei and increased the expression of its downstream antioxidant gene HO-1 by inducing the phosphorylation of AKT in HUVECs. Importantly, the AKT inhibitor MK-2206 2HCl or knockdown of Nrf2 by RNA interference attenuated the inhibition effects of these compounds on ox-LDL-induced apoptosis in HUVECs. Meanwhile, knockdown of Nrf2 abolished the effects of the compounds on ox-LDL-induced ROS level increase and the translocation of NF-κB to nuclei. Collectively, the data showed that compounds 1 and 2 protected endothelial cells against ox-LDL-induced oxidative stress through activating the AKT/Nrf2/HO-1 pathway. Our study provides new strategies for the design of lead compounds for related cardiovascular diseases treatment.
    Type of Medium: Online Resource
    ISSN: 1660-3397
    URL: Article
    DOI: 10.3390/md19120712
    Language: English
    Publisher: MDPI AG
    Publication Date: 2021
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  • 9
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    A Marine Alkaloid, Ascomylactam A, Suppresses Lung Tumorigenesis via Inducing Cell Cycle G1/S Arrest through ROS/Akt/Rb Pathway
    MDPI AG ; 2020
    In:  Marine Drugs Vol. 18, No. 10 ( 2020-09-27), p. 494-
    Details
    In: Marine Drugs, MDPI AG, Vol. 18, No. 10 ( 2020-09-27), p. 494-
    Abstract: Ascomylactam A was reported for the first time as a new 13-membered-ring macrocyclic alkaloid in 2019 from the mangrove endophytic fungus Didymella sp. CYSK-4 from the South China Sea. The aim of our study was to delineate the effects of ascomylactam A (AsA) on lung cancer cells and explore the antitumor molecular mechanisms underlying of AsA. In vitro, AsA markedly inhibited the cell proliferation with half-maximal inhibitory concentration (IC50) values from 4 to 8 μM on six lung cancer cell lines, respectively. In vivo, AsA suppressed the tumor growth of A549, NCI-H460 and NCI-H1975 xenografts significantly in mice. Furthermore, by analyses of the soft agar colony formation, 5-ethynyl-20-deoxyuridine (EdU) assay, reactive oxygen species (ROS) imaging, flow cytometry and Western blotting, AsA demonstrated the ability to induce cell cycle arrest in G1 and G1/S phases by increasing ROS generation and decreasing of Akt activity. Conversely, ROS inhibitors and overexpression of Akt could decrease cell growth inhibition and cell cycle arrest induced by AsA. Therefore, we believe that AsA blocks the cell cycle via an ROS-dependent Akt/Cyclin D1/Rb signaling pathway, which consequently leads to the observed antitumor effect both in vitro and in vivo. Our results suggest a novel leading compound for antitumor drug development.
    Type of Medium: Online Resource
    ISSN: 1660-3397
    URL: Article
    DOI: 10.3390/md18100494
    Language: English
    Publisher: MDPI AG
    Publication Date: 2020
    detail.hit.zdb_id: 2175190-0
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  • 10
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    Zebrafish Model in Ophthalmology to Study Disease Mechanism and Drug Discovery
    MDPI AG ; 2021
    In:  Pharmaceuticals Vol. 14, No. 8 ( 2021-07-25), p. 716-
    Details
    In: Pharmaceuticals, MDPI AG, Vol. 14, No. 8 ( 2021-07-25), p. 716-
    Abstract: Visual impairment and blindness are common and seriously affect people’s work and quality of life in the world. Therefore, the effective therapies for eye diseases are of high priority. Zebrafish (Danio rerio) is an alternative vertebrate model as a useful tool for the mechanism elucidation and drug discovery of various eye disorders, such as cataracts, glaucoma, diabetic retinopathy, age-related macular degeneration, photoreceptor degeneration, etc. The genetic and embryonic accessibility of zebrafish in combination with a behavioral assessment of visual function has made it a very popular model in ophthalmology. Zebrafish has also been widely used in ocular drug discovery, such as the screening of new anti-angiogenic compounds or neuroprotective drugs, and the oculotoxicity test. In this review, we summarized the applications of zebrafish as the models of eye disorders to study disease mechanism and investigate novel drug treatments.
    Type of Medium: Online Resource
    ISSN: 1424-8247
    URL: Article
    DOI: 10.3390/ph14080716
    Language: English
    Publisher: MDPI AG
    Publication Date: 2021
    detail.hit.zdb_id: 2193542-7
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