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Sci. Pharm., Volume 88, Issue 1 (March 2020) – 5 articles

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Open AccessReview
Antioxidants in Cancer Therapy: Recent Trends in Application of Nanotechnology for Enhanced Delivery
Sci. Pharm. 2020, 88(1), 5; https://doi.org/10.3390/scipharm88010005 - 21 Jan 2020
Viewed by 96
Abstract
Recently, the occurrence of cancer has significantly increased; it represents the second-most frequent cause of death after cardiovascular diseases. Many dietary antioxidants have shown large impact as effective agents for cancer prevention by reducing oxidative stress, which has been a part in the [...] Read more.
Recently, the occurrence of cancer has significantly increased; it represents the second-most frequent cause of death after cardiovascular diseases. Many dietary antioxidants have shown large impact as effective agents for cancer prevention by reducing oxidative stress, which has been a part in the development of many diseases, including cancer. One of the obstacles in the delivery of antioxidant therapies into the required domain lies in the inadequate delivery of these agents to their intended site of action. Using nanotechnology in delivery of antioxidants leads to increased therapeutic index and higher drug concentration in tumor tissues, thus enhancing anticancer treatment. In this review, we discuss the role of different antioxidants in cancer therapy and their improved therapeutic effect through their formulation using nanotechnology. Full article
(This article belongs to the Special Issue Advances in Nanoparticle-Mediated Drug Delivery)
Open AccessEditorial
Acknowledgement to Reviewers of Scientia Pharmaceutica in 2019
Sci. Pharm. 2020, 88(1), 4; https://doi.org/10.3390/scipharm88010004 - 16 Jan 2020
Viewed by 149
Abstract
The editorial team greatly appreciates the reviewers who have dedicated their considerable time and expertise to the journal’s rigorous editorial process over the past 12 months, regardless of whether the papers are finally published or not. [...]
Full article
Open AccessCommunication
Effect of N-Amide Substitution on Antioxidative Activities of Melatonin Derivatives
Sci. Pharm. 2020, 88(1), 3; https://doi.org/10.3390/scipharm88010003 - 08 Jan 2020
Viewed by 206
Abstract
Five N-amide substituted melatonin (MLT) derivatives were synthesized and evaluated for antioxidative activities, and compounds 912 showed higher electron spin resonance (ESR) response than MLT. 4-Bromobenzoyl and naphthoyl derivatives (10 and 11) presented stronger hydroxyl radical inhibitory effect [...] Read more.
Five N-amide substituted melatonin (MLT) derivatives were synthesized and evaluated for antioxidative activities, and compounds 912 showed higher electron spin resonance (ESR) response than MLT. 4-Bromobenzoyl and naphthoyl derivatives (10 and 11) presented stronger hydroxyl radical inhibitory effect than MLT in Fenton reaction. The substitution at the N1-position on the MLT core structure with acetyl (8), benzoyl (9), 4-bromobenzoyl (10), and naphthoyl (11) and N2-substitution with 4-bromobenzoyl (12) decreased the reducing power of the derivatives in ferric reducing antioxidant power (FRAP) assay. Compounds 811 also presented lower antioxidant capacity than their parent compound in 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) disodium salt (ABTS) assay; whereas, compound 12 presented radical scavenging activity similarly to MLT. All aryl derivatives (912) showed higher ability to quench peroxyl radicals than MLT about three times, especially the benzoylated derivatives (9 and 10) that presented the highest ability in oxygen radical absorbance capacity (ORAC) assay. Full article
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Open AccessArticle
Multiple Virtual Screening Strategies for the Discovery of Novel Compounds Active Against Dengue Virus: A Hit Identification Study
Sci. Pharm. 2020, 88(1), 2; https://doi.org/10.3390/scipharm88010002 - 19 Dec 2019
Viewed by 348
Abstract
Dengue infection is caused by a mosquito-borne virus, particularly in children, which may even cause death. No effective prevention or therapeutic agents to cure this disease are available up to now. The dengue viral envelope (E) protein was discovered to be a promising [...] Read more.
Dengue infection is caused by a mosquito-borne virus, particularly in children, which may even cause death. No effective prevention or therapeutic agents to cure this disease are available up to now. The dengue viral envelope (E) protein was discovered to be a promising target for inhibition in several steps of viral infection. Structure-based virtual screening has become an important technique to identify first hits in a drug screening process, as it is possible to reduce the number of compounds to be assayed, allowing to save resources. In the present study, pharmacophore models were generated using the common hits approach (CHA), starting from trajectories obtained from molecular dynamics (MD) simulations of the E protein complexed with the active inhibitor, flavanone (FN5Y). Subsequently, compounds presented in various drug databases were screened using the LigandScout 4.2 program. The obtained hits were analyzed in more detail by molecular docking, followed by extensive MD simulations of the complexes. The highest-ranked compound from this procedure was then synthesized and tested on its inhibitory efficiency by experimental assays. Full article
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Open AccessArticle
Crystal Habits and Biological Properties of N-(4-Trifluoromethylphenyl)-4-Hydroxy-2,2-Dioxo-1H-2λ6,1-Benzothiazine-3-Carboxamide
Sci. Pharm. 2020, 88(1), 1; https://doi.org/10.3390/scipharm88010001 - 18 Dec 2019
Viewed by 249
Abstract
In order to study polymorphic modifications of N-(4-trifluoromethylphenyl)-4-hydroxy-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide, which is of interest as a promising analgesic, its three colorless crystal forms with different habitus have been obtained: sticks of ethyl acetate, plates of meta-xylene and blocks of [...] Read more.
In order to study polymorphic modifications of N-(4-trifluoromethylphenyl)-4-hydroxy-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide, which is of interest as a promising analgesic, its three colorless crystal forms with different habitus have been obtained: sticks of ethyl acetate, plates of meta-xylene and blocks of ortho-xylene. However, the X-ray diffraction analysis has shown that all the forms studied have the identical molecular and crystal structure in spite of such significant differences in appearance. Moreover, pharmacological tests have revealed significant differences in the analgesic activity in these samples (a total of five experimental models were used: “acetic-acid-induced writhing”, “hot plate”, “thermal irritation of the tail tip” (tail-flick), “tail electric stimulation” and “neuropathic pain”), acute toxicity and the ability to cause gastric damage. As a result, only the plate crystal form of N-(4-trifluoromethylphenyl)-4-hydroxy-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide is recommended for further studies. Thus, it has been proven that the habitus of crystals is an important characteristic of the drug substance and is able to have a noticeable effect on its biological properties. Changes in habitus should be considered as a guide to the mandatory verification of at least the basic pharmacological parameters of the new form regardless of whether the molecular and crystal structure changes. Full article
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