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The Design, Synthesis, and Biological Evaluation of Compounds with Medicinal Value

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Applied Biosciences and Bioengineering".

Deadline for manuscript submissions: closed (20 December 2020) | Viewed by 76952

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Special Issue Editor

Special Issue Information

Dear Colleagues,

In industrialized countries over the last few decades, there has been a significant increase in infectious; cardiovascular, inflammatory, and neurodegenerative diseases; as well as different forms of cancer, diabetes, and so on.

Between them, microbial infections and cancer are still the major causes of death among the world’s population due to increased bacterial resistance phenomena and the development of resistance to chemotherapeutics. For these reasons, there is an urgent need to design and synthesize new antimicrobial agents, particularly those with antibacterial activity, and particularly against Gram _ve pathogens that could be used to fight drug resistance, and also for new antineoplastic drugs with higher selectivity on tumoral cells, which are able to overcome cancer cells’ resistance with minimal side effects.

Recently, some delivery systems have proved particulary effective as antimicrobial and anticancer carriers due to targeted drug delivery at the action sites, reduced drug-resistance and side effects, and an increased therapeutic index.

Potential topics for manuscripts include the following:

  • The design, synthesis, and biological evaluation of anticancer agents;
  • The design, synthesis, and biological evaluation of antimicrobial agents;
  • Delivery systems and nanosystems for targeted cancer and antimicrobial therapy.
Prof. Maria Stefania Sinicropi
Guest Editor

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2400 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • molecular modeling
  • synthesis
  • anticancer compounds
  • antimicrobial compounds
  • targeted therapy
  • delivery systems

Published Papers (14 papers)

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Editorial

Jump to: Research, Review, Other

5 pages, 212 KiB  
Editorial
Special Issue on “The Design, Synthesis and Biological Evaluation of Compounds with Medicinal Value”
by Maria Stefania Sinicropi
Appl. Sci. 2021, 11(4), 1904; https://doi.org/10.3390/app11041904 - 22 Feb 2021
Viewed by 1177
Abstract
During the last few decades, in industrialized countries a significant increase in infectious, cardiovascular, inflammatory and neurodegenerative diseases was registered, as well as different forms of cancer, diabetes, and so on [...] Full article

Research

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14 pages, 3361 KiB  
Article
Nutraceuticals Obtained by SFE-CO2 from Cladodes of Two Opuntia ficus-indica (L.) Mill Wild in Calabria
by Domenico Iacopetta, Noemi Baldino, Anna Caruso, Valentina Perri, Francesca Romana Lupi, Bruno de Cindio, Domenico Gabriele and Maria Stefania Sinicropi
Appl. Sci. 2021, 11(2), 477; https://doi.org/10.3390/app11020477 - 6 Jan 2021
Cited by 4 | Viewed by 2047
Abstract
The aim of the present study was to evaluate the possibility to extract, by supercritical fluids, nutraceuticals as polyphenolic compounds, able in the prevention and in the treatment of a series of chronic-degenerative diseases, from plant matrices like the cactus pear. Supercritical fluid [...] Read more.
The aim of the present study was to evaluate the possibility to extract, by supercritical fluids, nutraceuticals as polyphenolic compounds, able in the prevention and in the treatment of a series of chronic-degenerative diseases, from plant matrices like the cactus pear. Supercritical fluid technology is an innovative method to extract nutraceuticals from natural matrices. This method offers numerous advantages that include the use of moderate temperatures, solvents with good transport properties (high diffusivity and low viscosity), and cheap and nontoxic fluids. Fresh cladodes from two different wild ecotypes of Opuntia ficus-indica (L.) Mill. were extracted both with methanol and with SFE-CO2 using different samples preparations, to maximize the % yields and the selectivity of extraction of polyphenols. The biggest contents of phenolics, evaluated by Folin-Ciocalteu assay, has been observed with the sample dehydrated of O. ficus-indica cultivar that shows, as well, the best yield % (m/m) of extraction with both methanol and SFE-CO2. Better results were obtained with the samples of O. ficus-indica cult. (OFI cult.), in spite of the O. ficus-indica s.l. (OFI s.l.); the two different ecotypes of OFI showed dissimilar phytochemicals profile. We noticed that the reduction of both quantity and quality of polyphenols was drastic with the increase of pressure at 250 bar; this shows that high pressures result in a loss of bioactive principles, like polyphenols. By changing the variables of extraction processes with SFE-CO2 and by varying the preventive treatments of the natural matrices, it was possible to increase the selectivity and the purity of the products. Thus, the optimization of this useful and green technique allowed us to increase the value of the Opuntia cladodes, a by-product very diffused in Calabria, which is an extraordinary source of nutraceuticals. These extracts could be used directly as functional foods or as starting material in the pharmaceutical, nutraceutical or cosmetic companies; they are safe and without any solvents traces and it is possible to obtain it in a few hours respect to the conventional extraction that requires longer extraction time. Full article
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12 pages, 1686 KiB  
Article
Synthesis of Novel Potent Biologically Active N-Benzylisatin-Aryl Hydrazones in Comparison with Lung Cancer Drug ‘Gefitinib’
by Huda S. Al-Salem, Hatem A. Abuelizz, Iman S. Issa, Amany Z. Mahmoud, Ali AlHoshani, Md Arifuzzaman and A. F. M. Motiur Rahman
Appl. Sci. 2020, 10(11), 3669; https://doi.org/10.3390/app10113669 - 26 May 2020
Cited by 6 | Viewed by 2821
Abstract
Developing anticancer therapeutics with no/few side effects is a challenge for medicinal chemists. The absence of antibacterial activity of an anticancer drug removes its detrimental effect toward intestinal flora and therefore leads to reduced side effects. Here, a series of novel N-benzylisatin-aryl-hydrazones [...] Read more.
Developing anticancer therapeutics with no/few side effects is a challenge for medicinal chemists. The absence of antibacterial activity of an anticancer drug removes its detrimental effect toward intestinal flora and therefore leads to reduced side effects. Here, a series of novel N-benzylisatin-aryl-hydrazones was designed, synthesized and evaluated for their antimicrobial and antiproliferative activities with SAR and ADME studies, aiming to develop anticancer drugs with no antimicrobial, yet high antiproliferative activities. The results were then compared with the effects of first-line treatments for lung cancer drug Gefitinib. Novel N-benzylisatin-aryl-hydrazones were synthesized from isatin and benzyl bromide in three steps with good to moderate yields. Antimicrobial activity was tested with six Gram-positive/negative bacterial strains, antifungal activity with a fungal strain and antiproliferative activity against ‘A549’ and ‘HeLa cell lines’, respectively. As expected, synthesized hydrazones reveled no effects on any of the strains of bacteria and fungi up to 100-µg/disc concentration. However, four compounds showed two-to-four fold antiproliferative activity over Gefitinib. For instance, IC50 of a compound (6c) shows concentration of 4.35 µM, whereas gefitinib shows 15.23 µM against ‘A549.’ ADME predicted studies reveled that our synthesized hydrazones exhibited higher ADME values than the Gefitinib. Therefore, our synthesized hydrazones can be an excellent scaffold for the development of anticancer therapeutics after considering further investigations. Full article
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13 pages, 5916 KiB  
Article
Enamine Barbiturates and Thiobarbiturates as a New Class of Bacterial Urease Inhibitors
by M. Ali, Assem Barakat, Ayman El-Faham, Abdullah Mohammed Al-Majid, Sammer Yousuf, Sajda Ashraf, Zaheer Ul-Haq, M. Iqbal Choudhary, Beatriz G. de la Torre and Fernando Albericio
Appl. Sci. 2020, 10(10), 3523; https://doi.org/10.3390/app10103523 - 20 May 2020
Cited by 7 | Viewed by 3020
Abstract
Urease is a therapeutic target associated with several important diseases and health problems. Based on our previous work on the inhibition of glucosidase and other enzymes and exploiting the privileged structure assigned to the (thio)barbiturate (pyrimidine) scaffold, here we tested the capacity of [...] Read more.
Urease is a therapeutic target associated with several important diseases and health problems. Based on our previous work on the inhibition of glucosidase and other enzymes and exploiting the privileged structure assigned to the (thio)barbiturate (pyrimidine) scaffold, here we tested the capacity of two (thio)barbiturate-based compound collections to inhibit urease. Several compounds showed more activity than acetohydroxamic acid as a standard tested compound. In addition, by means of a conformational study and using the Density Functional Theory (DFT) method, we identified energetically low-lying conformers. Finally, we undertook a docking study to explore the binding mechanism of these new pyrimidine derivatives as urease inhibitors. Full article
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20 pages, 2316 KiB  
Article
In Vitro and In Silico Screening of 2,4,5-Trisubstituted Imidazole Derivatives as Potential Xanthine Oxidase and Acetylcholinesterase Inhibitors, Antioxidant, and Antiproliferative Agents
by Eduardo Noriega-Iribe, Laura Díaz-Rubio, Arturo Estolano-Cobián, Victor Wagner Barajas-Carrillo, José M. Padrón, Ricardo Salazar-Aranda, Raúl Díaz-Molina, Victor García-González, Rocio Alejandra Chávez-Santoscoy, Daniel Chávez and Iván Córdova-Guerrero
Appl. Sci. 2020, 10(8), 2889; https://doi.org/10.3390/app10082889 - 22 Apr 2020
Cited by 12 | Viewed by 3960
Abstract
The employment of privileged scaffolds in medicinal chemistry supplies scientists with a solid start in the search for new and improved therapeutic molecules. One of these scaffolds is the imidazole ring, from which several derivatives have shown a wide array of biological activities. [...] Read more.
The employment of privileged scaffolds in medicinal chemistry supplies scientists with a solid start in the search for new and improved therapeutic molecules. One of these scaffolds is the imidazole ring, from which several derivatives have shown a wide array of biological activities. A series of 2,4,5-triphenyl imidazole derivatives were synthesized, characterized, and evaluated in vitro as antioxidant molecules using 1,1-diphenyl-2-picrylhydrazyl (DPPH.) and 2-2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonate) (ABTS.+) assays, acetylcholinesterase (AChE) and xanthine oxidase (XO) inhibitors as well as antiproliferative agents. Additional in silico studies such as docking and determination of their absorption, distribution, metabolism, and excretion (ADME) properties were calculated. Compounds 3 and 10 were the most active antioxidants in both the DPPH and ABTS assays (EC50 of 0.141 and 0.174 mg/mL, and 0.168 and 0.162 mg/mL, respectively). In the enzymatic inhibition, compound 1 showed the best activity, inhibiting 25.8% of AChE at a concentration of 150 μg/mL, and compound 3 was the most active XO inhibitor with an IC50 of 85.8 μg/mL. Overall, against the six different evaluated cancerous cell lines, molecules 2, 10, and 11 were the most antiproliferative compounds. In silico predictions through docking point out 11, and ADME analysis to 11 and 12, as good candidates for being lead compounds for further derivations. Full article
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13 pages, 10922 KiB  
Article
Sol–Gel Treatment of Textiles for the Entrapping of an Antioxidant/Anti-Inflammatory Molecule: Functional Coating Morphological Characterization and Drug Release Evaluation
by Francesco Puoci, Carmela Saturnino, Valentina Trovato, Domenico Iacopetta, Elpida Piperopoulos, Claudia Triolo, Maria Grazia Bonomo, Dario Drommi, Ortensia Ilaria Parisi, Candida Milone, Maria Stefania Sinicropi, Giuseppe Rosace and Maria Rosaria Plutino
Appl. Sci. 2020, 10(7), 2287; https://doi.org/10.3390/app10072287 - 27 Mar 2020
Cited by 23 | Viewed by 3182
Abstract
The growing interest towards textile-based drug delivery systems is due to their potential innovative medical and well-being applications. In recent years, the technique of encapsulation or inclusion of the medicine/active principle into a polymer functional matrix has been employed in order to obtain [...] Read more.
The growing interest towards textile-based drug delivery systems is due to their potential innovative medical and well-being applications. In recent years, the technique of encapsulation or inclusion of the medicine/active principle into a polymer functional matrix has been employed in order to obtain textile materials with controlled drug release. In this study, a sol–gel-based coating was developed and used as an entrapping polymeric cross-linked network for a N-Palmitoyl-ethanolamine (PEA) derivative, 2-methyl-pentadecanoic acid (4-nitro-phenyl)-amide or N-Palmitoyl-(4-nitro-phenyl)-amine (PNPA), whose anti-inflammatory and antioxidant properties have already been shown. A wide series of chemical-physical methods have been used to characterize the silica-based functional sol and to ascertain the efficient and temporary deposit of PNPA on the sol–gel coated cotton fabrics. The medicine release system achieved was shown to ensure biocompatibility, PNPA reservoir and its subsequent releasing under the action of cutaneous stimuli, thus providing useful insights in the design of medical textiles. Full article
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11 pages, 4799 KiB  
Article
Synthesis, Anticancer Activity, and Molecular Modeling of New Halogenated Spiro[pyrrolidine-thiazolo-oxindoles] Derivatives
by Mohammad Shahidul Islam, Abdullah Mohammed Al-Majid, Fardous F. El-Senduny, Farid A. Badria, A. F. M. Motiur Rahman, Assem Barakat and Yaseen A. M. M. Elshaier
Appl. Sci. 2020, 10(6), 2170; https://doi.org/10.3390/app10062170 - 23 Mar 2020
Cited by 27 | Viewed by 3594
Abstract
A one-pot, single-step, and an atom-economical process towards the synthesis of highly functionalized spirooxindoles analogues was efficiently conducted to produce a satisfactory chemical yields (70–93%) with excellent relative diastereo-, and regio-selectivity. An in vitro antiproliferative assay was carried out on different cancer cell [...] Read more.
A one-pot, single-step, and an atom-economical process towards the synthesis of highly functionalized spirooxindoles analogues was efficiently conducted to produce a satisfactory chemical yields (70–93%) with excellent relative diastereo-, and regio-selectivity. An in vitro antiproliferative assay was carried out on different cancer cell lines to evaluate the biological activity of the synthesized tetrahydro-1’H-spiro[indoline-3,5’-pyrrolo[1,2-c]thiazol]-2-one 5a–n. The prepared hybrids were then tested in vitro for their antiproliferative effects against three cancer cell lines, namely, HepG2 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer). The spirooxindole analogue 5g exhibited a broad activity against HepG2, MCF-7, and HCT-116 cell lines of liver, breast, and colorectal cancers when compared to cisplatin. Modeling studies including shape similarity, lipophilicity scores, and physicochemical parameters were calculated. The results of this study indicated that spirooxindole analogue 5g retained a good physiochemical parameters with acceptable lipophilicity scores. Full article
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16 pages, 5736 KiB  
Article
Directed Silica Co-Deposition by Highly Oxidized Silver: Enhanced Stability and Versatility of Silver Oxynitrate
by Carla J. Spina, Roohee Ladhani, Carlie Goodall, Michelle Hay and Rod Precht
Appl. Sci. 2019, 9(23), 5236; https://doi.org/10.3390/app9235236 - 2 Dec 2019
Cited by 5 | Viewed by 3199
Abstract
Novel silver compounds in higher oxidation states, Ag (II) and Ag (III), have emerged as desirable alternatives to existing forms of antimicrobial silver compounds. Offering enhanced efficacy without sacrificing biocompatibility. Unique physiochemical characteristics associated with higher oxidation state silver confer desirable therapeutic traits. [...] Read more.
Novel silver compounds in higher oxidation states, Ag (II) and Ag (III), have emerged as desirable alternatives to existing forms of antimicrobial silver compounds. Offering enhanced efficacy without sacrificing biocompatibility. Unique physiochemical characteristics associated with higher oxidation state silver confer desirable therapeutic traits. However, these same characteristics create challenges in terms of long-term stability and chemical compatibility with conventional biomedical materials. Core-shell methodologies, utilizing silica as a mesoporous or amorphous shell, have been adopted to enhance the stability of reactive active ingredients or cores. These methodologies commonly utilize controlled condensation of silicic acids in non-aqueous media by way of hydrolyzing alkyl silicates: the Stöber process or modified processes thereof. However, these strategies are not conducive to cores of higher oxidation state silver wherein hydroxyl organic precursors and by-products are incompatible with strong oxidizing agents. Addressing these challenges, we present a strategy herein for the preparation of a self-directed silver oxynitrate-silica, Ag7NO11:SiO2, framework. The method described utilizes pH gradients generated from the oxidation reaction of soluble silver, Ag (I), with a strong oxidizing agent/alkaline silicate media to facilitate spatial control over the protonation and subsequent condensation of silicic acid from aqueous solution. The resulting Ag7NO11:SiO2 framework confers enhanced long term and thermal stability to silver oxynitrate without impairing aqueous degradation profiles or subsequent antimicrobial and antibiofilm activities. Full article
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11 pages, 1642 KiB  
Article
Synthesis, Tyrosinase Inhibiting Activity and Molecular Docking of Fluorinated Pyrazole Aldehydes as Phosphodiesterase Inhibitors
by Vesna Rastija, Harshad Brahmbhatt, Maja Molnar, Melita Lončarić, Ivica Strelec, Mario Komar and Valentina Pavić
Appl. Sci. 2019, 9(8), 1704; https://doi.org/10.3390/app9081704 - 25 Apr 2019
Cited by 4 | Viewed by 3833
Abstract
A series of fluorinated 4,5-dihydro-1H-pyrazole derivatives were synthesized in the reaction of corresponding acetophenone and different aldehydes followed by the second step synthesis of desired compounds from synthesized chalcone, hydrazine hydrate, and formic acid. Structures of all compounds were confirmed by [...] Read more.
A series of fluorinated 4,5-dihydro-1H-pyrazole derivatives were synthesized in the reaction of corresponding acetophenone and different aldehydes followed by the second step synthesis of desired compounds from synthesized chalcone, hydrazine hydrate, and formic acid. Structures of all compounds were confirmed by both 1H and 13C NMR and mass spectrometry. Antibacterial properties of compounds were tested on four bacterial strains, Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus. Among synthesized compounds, the strongest inhibitor of monophenolase activity of mushroom tyrosinase (32.07 ± 3.39%) was found to be 5-(2-chlorophenyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbaldehyde. The PASS program has predicted the highest probable activity for the phosphodiesterase inhibition. To shed light on molecular interactions between the synthesized compounds and phosphodiesterase, all compounds were docked into the active binding site. The obtained results showed that the compound with the dimethoxyphenyl ring could be potent as an inhibitor of phosphodiesterase, which interacts in PDE5 catalytic domain of the enzyme. Key interactions are bidentate hydrogen bond (H-bond) with the side-chain of Gln817 and van der Waals interactions of the dimethoxyphenyl ring and pyrazole ring with hydrophobic clamp, which contains residuals, Val782, Phe820, and Tyr612. Interactions are similar to the binding mode of the inhibitor sildenafil, the first oral medicine for the treatment of male erectile dysfunction. Full article
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Review

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34 pages, 6330 KiB  
Review
Pomegranate: Nutraceutical with Promising Benefits on Human Health
by Anna Caruso, Alexia Barbarossa, Antonio Tassone, Jessica Ceramella, Alessia Carocci, Alessia Catalano, Giovanna Basile, Alessia Fazio, Domenico Iacopetta, Carlo Franchini and Maria Stefania Sinicropi
Appl. Sci. 2020, 10(19), 6915; https://doi.org/10.3390/app10196915 - 2 Oct 2020
Cited by 36 | Viewed by 7312
Abstract
Pomegranate is an old plant made up by flowers, roots, fruits and leaves, native to Central Asia and principally cultivated in the Mediterranean and California (although now widespread almost all over the globe). The current use of this precious plant regards not only [...] Read more.
Pomegranate is an old plant made up by flowers, roots, fruits and leaves, native to Central Asia and principally cultivated in the Mediterranean and California (although now widespread almost all over the globe). The current use of this precious plant regards not only the exteriority of the fruit (employed also for ornamental purpose) but especially the nutritional and, still potential, health benefits that come out from the various parts composing this one (carpellary membranes, arils, seeds and bark). Indeed, the phytochemical composition of the fruit abounds in compounds (flavonoids, ellagitannins, proanthocyanidins, mineral salts, vitamins, lipids, organic acids) presenting a significant biological and nutraceutical value. For these reasons, pomegranate interest is increased over the years as the object of study for many research groups, particularly in the pharmaceutical sector. Specifically, in-depth studies of its biological and functional properties and the research of new formulations could be applied to a wide spectrum of diseases including neoplastic, cardiovascular, viral, inflammatory, metabolic, microbial, intestinal, reproductive and skin diseases. In this review, considering the increasing scientific and commercial interest of nutraceuticals, we reported an update of the investigations concerning the health-promoting properties of pomegranate and its bioactive compounds against principal human pathologies. Full article
15 pages, 1155 KiB  
Review
The Clinical and Economic Value of Triclosan-Coated Surgical Sutures in Abdominal Surgery
by Marco Ceresoli, Francesca Carissimi, Alessandra Piemontese, Vito Paragò, Thibaut Galvain, Giovanni A. Tommaselli and Luca Gianotti
Appl. Sci. 2020, 10(3), 1090; https://doi.org/10.3390/app10031090 - 6 Feb 2020
Cited by 3 | Viewed by 3242
Abstract
Surgical site infection (SSI) is a frequent complication of surgical procedures. The aim of this study was to analyze the clinical evidence for SSI prevention with triclosan-coated sutures (TCS) in abdominal surgery and to investigate the economic impact of TCS in this type [...] Read more.
Surgical site infection (SSI) is a frequent complication of surgical procedures. The aim of this study was to analyze the clinical evidence for SSI prevention with triclosan-coated sutures (TCS) in abdominal surgery and to investigate the economic impact of TCS in this type of procedure compared with conventional absorbable sutures (CS). A literature review was carried out to identify meta-analyses that were published between 1990 and 2019 that assessed the use of TCS in abdominal surgery. A budget impact analysis was performed from an Italian hospital perspective based on the most recently published evidence to simulate the financial impact of TCS in a general surgery unit. Uncertainty was explored through scenario analysis, as well as deterministic and probabilistic sensitivity analyses. Nine meta-analyses and two additional randomized clinical trials were retrieved. All meta-analyses described a reduction (range 19%–44%) in the risk of SSI when TCS were used. The use of TCS was associated with an overall annual net saving for the general surgery unit of €14,785 and a reduction of 3.2 SSIs compared with CS. Sensitivity analyses resulted in a positive annual saving associated with TCS in 98% of scenarios. TCS are a valuable, cost-saving SSI prevention strategy. TCS additional costs would be offset by the reduction in SSIs. Full article
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19 pages, 1222 KiB  
Review
β-Caryophyllene: A Sesquiterpene with Countless Biological Properties
by Fabrizio Francomano, Anna Caruso, Alexia Barbarossa, Alessia Fazio, Chiara La Torre, Jessica Ceramella, Rosanna Mallamaci, Carmela Saturnino, Domenico Iacopetta and Maria Stefania Sinicropi
Appl. Sci. 2019, 9(24), 5420; https://doi.org/10.3390/app9245420 - 11 Dec 2019
Cited by 153 | Viewed by 29037
Abstract
β-Caryophyllene (BCP), a natural bicyclic sesquiterpene, is a selective phytocannabinoid agonist of type 2 receptors (CB2-R). It isn’t psychogenic due to the absence of an affinity to cannabinoid receptor type 1 (CB1). Among the various biological activities, BCP exerts anti-inflammatory action via [...] Read more.
β-Caryophyllene (BCP), a natural bicyclic sesquiterpene, is a selective phytocannabinoid agonist of type 2 receptors (CB2-R). It isn’t psychogenic due to the absence of an affinity to cannabinoid receptor type 1 (CB1). Among the various biological activities, BCP exerts anti-inflammatory action via inhibiting the main inflammatory mediators, such as inducible nitric oxide synthase (iNOS), Interleukin 1 beta (IL-1β), Interleukin-6 (IL-6), tumor necrosis factor-alfa (TNF-α), nuclear factor kapp a-light-chain-enhancer of activated B cells (NF-κB), cyclooxygenase 1 (COX-1), cyclooxygenase 2 (COX-2). Peroxisome proliferator-activated receptors alpha (PPAR-α) effects are also mediated by the activation of PPAR-α and PPAR-γ receptors. In detail, many studies, in vitro and in vivo, suggest that the treatment with β-caryophyllene improves the phenotype of animals used to model various inflammatory pathologies, such as nervous system diseases (Parkinson’s disease, Alzheimer’s disease, multiple sclerosis, amyotrophic lateral sclerosis, stroke), atherosclerosis, and tumours (colon, breast, pancreas, lymphoma, melanoma and glioma cancer). Furthermore, pre-clinical data have highlighted that BCP is potentially useful in Streptococcus infections, osteoporosis, steatohepatitis, and exerts anticonvulsant, analgesic, myorelaxing, sedative, and antidepressive effects. BCP is non-toxic in rodents, with a Lethal dose, 50% (LD50) greater than 5000 mg/kg. Nevertheless, it inhibits various cytochrome P450 isoforms (above all, CYP3A4), which metabolise xenobiotics, leading to adverse effects, due to drug levels over therapeutic window. All the reported data have highlighted that both pharmacological and toxicological aspects need to be further investigated with clinical trials. Full article
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10 pages, 569 KiB  
Review
Effect of Tinospora cordifolia-Derived Phytocomponents on Cancer: A Systematic Review
by Babji Deepa, Harsha V. Babaji, Jagadish V. Hosmani, Abdul Wahab H. Alamir, Shazia Mushtaq, A. Thirumal Raj and Shankargouda Patil
Appl. Sci. 2019, 9(23), 5147; https://doi.org/10.3390/app9235147 - 28 Nov 2019
Cited by 5 | Viewed by 5648
Abstract
The major cancer therapeutic modalities include surgery, chemotherapy and radiotherapy. Although these treatment regimens have played a significant role in effectively inhibiting cancer, their associated morbidity reduces the overall quality of life. Thus, researchers are striving to identify any alternate therapeutic approach capable [...] Read more.
The major cancer therapeutic modalities include surgery, chemotherapy and radiotherapy. Although these treatment regimens have played a significant role in effectively inhibiting cancer, their associated morbidity reduces the overall quality of life. Thus, researchers are striving to identify any alternate therapeutic approach capable of inhibiting cancer without eliciting the added morbidity. Among the alternate cancer therapeutics being researched, much importance is being given to the use of plants due to the presence of a wide variety of anti-carcinogenic compounds. Tinospora cordifolia (Tc) is one such plant and has shown to exhibit anti-carcinogenic properties. The present review aimed to systematically analyze published data on the effect of Tinospora cordifolia-derived phytocomponents on cancer. PubMed, Scopus, Web of Science, Embase and Cochrane library were searched using the keywords Tinospora cordifolia; anticancer; phytocomponents until March 20, 2019. In vivo and in vitro original studies in the English language were included. Of the 342 articles identified, only 25 articles met the selection criteria and were included in the review. Significant anti-carcinogenic properties were exhibited by Tinospora cordifolia-derived phytocompounds including palmative, berberine, new clerodane furanoditerene glycoside, arabinogalactan, phenolic compounds and epoxy cleodane diterpene. No significant side effects have been elicited with its use. Based on the data from the included studies, Tinospora cordifolia could be a natural therapeutic agent for cancer, provided its anti-carcinogenic properties can be elicited consistently at a large scale in clinical trials. Full article
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8 pages, 219 KiB  
Project Report
New Local Drug Delivery with Antibiotic in the Nonsurgical Treatment of Periodontitis—Pilot Study
by Aleksandra Sender-Janeczek, Jacek Zborowski, Małgorzata Szulc and Tomasz Konopka
Appl. Sci. 2019, 9(23), 5077; https://doi.org/10.3390/app9235077 - 25 Nov 2019
Cited by 6 | Viewed by 3654
Abstract
Combination of the classical subgingival instrumentation (scaling and root planing procedure, SRP) with an antibiotic administered to periodontal pockets in a suitable medium is a promising alternative protocol of nonsurgical periodontal treatment. It enables obtaining the long-term minimum drug concentration inhibiting the development [...] Read more.
Combination of the classical subgingival instrumentation (scaling and root planing procedure, SRP) with an antibiotic administered to periodontal pockets in a suitable medium is a promising alternative protocol of nonsurgical periodontal treatment. It enables obtaining the long-term minimum drug concentration inhibiting the development of periopathogens. Objectives: Clinical and microbiological evaluation of periodontal pockets two months after single application of a gel containing piperacillin and tazobactam (Gelcide)® in relation to the nonsurgical treatment procedure (SRP). Materials and methods: Ten patients aged 24–56 years (mean 39.5) with chronic periodontitis, nonsmokers with acceptable oral hygiene and no classical exclusion criteria were qualified for treatment. In the maxilla area, SRP was performed and the assessed gel was inserted to two randomly selected adjacent periodontal pockets. Clinical evaluation included the assessment of bleeding on probing (BoP), pocket depth (PD), and clinical attachment loss (CAL) at six measurement points. A microbiological examination with the use of PET deluxe diagnostic kit in the drug-administered pockets and symmetrically in two pockets on the other side of the dental arch was performed. The examination was conducted before the treatment and two months later. Results: Two months after the treatment, a significant improvement in all analyzed clinical parameters was observed. However, the extent of this improvement did not differ significantly between the compared treatment methods. No statistically significant differences were found in the number of bacteria before and after the treatment, except for a significant decrease in the number of Micromonas micros (2957 vs. 589, p = 0.028) and a higher number of the green complex bacteria Capnocytophaga gingivalis (5439 vs. 2050, p = 0.041) after antibiotic had been used. Conclusion: No significant clinical and microbiological differences were found after additional administration of gel with piperacillin and tazobactam in relation to SRP in the preliminary study. Full article
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