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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 (10 February 2022) | Viewed by 30264

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Dr. Anca Pop

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Department of Toxicology, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 6 L. Pasteur Street, 400349 Cluj-Napoca, Romania
Interests: bioactive compounds; oxidative stress; antioxidants; inflammation; endocrine disruptors
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Prof. Dr. Felicia Loghin

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Department of Toxicology, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 6 L. Pasteur Street, 400349 Cluj-Napoca, Romania
Interests: safety evaluation; nanotoxicity; oxidative stress biomarkers; toxicokinetics; analysis of toxicants
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Dr. Catalina Bogdan

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Department of Dermopharmacy and Cosmetics, Faculty of Pharmacy, “Iuliu Haţieganu” University of Medicine and Pharmacy, 12 I. Creanga Street, 400010 Cluj-Napoca, Romania
Interests: development and characterization of solid and semisolid dosage forms; texture analysis; development and optimization of cosmetic products based on nanocarriers or herbal extracts
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Dr. Ionel Fizesan

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Department of Toxicology, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 6 L. Pasteur Street, 400349 Cluj-Napoca, Romania
Interests: antioxidants; inflammation; cancer; anti-aging; phytochemical and drug analysis; functional foods; in vitro testing
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Special Issue Information

Dear Colleague,

We are pleased to announce the Special Issue on “Advances in Natural Bioactive Compounds and Biological Effects” in Applied Sciences (ISSN 2076-3417, IF-2.474, https://www.mdpi.com/journal/applsci).

Natural bioactive compounds include substances of vegetal or animal origin that can preserve the health status and prevent different diseases by modulation of cellular processes involved in pathological conditions. Although bioactive compounds have gained attention as beneficial health elements due to their tissue-protective effects (antibacterial, antioxidant, anti-inflammatory, etc.), more scientific data is needed to make science-based recommendations.

Moreover, the use of by-products as alternative sources for the isolation of bioactive compounds is in line with the reduced waste strategy that various institutions and industries are focused on.

In this context, we encourage the submission of research papers and reviews on natural bioactive compounds regarding their isolation methods and biological functions that would recommend their use in various fields, such as food, pharmaceutical, and cosmetic industries.

Dr. Anca Pop
Prof. Dr. Felicia Loghin
Dr. Catalina Bogdan
Dr. Ionel Fizesan
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Applied Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

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

extraction
bioactive compounds
polyphenolic compounds
phytochemicals
disease prevention
oxidative stress
inflammation
anti-aging

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Published Papers (10 papers)

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Research

14 pages, 2117 KiB

Open AccessArticle

Orientin Alleviates Liver Inflammation via Downregulation of ZEB-2/PTEN Markers—Hepatic Stellate Cells Approach

by Hany Ezzat Khalil, Hairul-Islam Mohamed Ibrahim, Kareem Ahmed El-Fass, Sabah H. Akrawi and Mohamed A. Morsy

Appl. Sci. 2022, 12(5), 2725; https://doi.org/10.3390/app12052725 - 6 Mar 2022

Cited by 7 | Viewed by 2356

Abstract

Liver inflammation is associated with an increased risk of liver fibrosis that substantially progresses to cirrhosis. Recently, usage of the herbal supplement has been increased because of its emerging role to dominate oxidative stress in hepatic injury. Orientin is one of the bioactive flavonoids that possesses a diversity of curative activities. Therefore, the present study was conducted to evaluate the anti-inflammatory role of orientin (1 mg/kg) in vitro in lipopolysaccharide (LPS)-induced inflammation in hepatic stellate cells (HSCs) and in vivo in carbon tetrachloride (CCl₄)-induced liver fibrosis in mice. Moreover, the current study was supported by in silico investigation. Orientin demonstrated protection against LPS-induced HSC inflammation as evidenced by a decrease in iNOS, NO, and TNF-α and inhibition of the fibrotic markers ZEB-2 and PTEN. In addition, orientin afforded protection against CCl₄-induced liver fibrosis in mice as shown from decreased AST/ALT ratio, inhibition of the pro-inflammatory mediators TNF-α, IL-6, IL-8, and IFN-γ, reduction of fibrotic markers ZEB-2 and PTEN, and improvement of the histopathological changes. Furthermore, the docking study demonstrated virtual interactions of orientin with ZEB-2 and PTEN. Taken together, the current study suggested that the protective effects of orientin against LPS- and CCl₄-induced liver inflammation are via inhibition of fibrotic markers and reduction of pro-inflammatory mediators. Full article

(This article belongs to the Special Issue Advances in Natural Bioactive Compounds and Biological Effects)

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15 pages, 2501 KiB

Open AccessArticle

A Potential “Vitaminic Strategy” against Caries and Halitosis

by Laura Pietrangelo, Irene Magnifico, Giulio Petronio Petronio, Marco Alfio Cutuli, Noemi Venditti, Daria Nicolosi, Angelica Perna, Germano Guerra and Roberto Di Marco

Appl. Sci. 2022, 12(5), 2457; https://doi.org/10.3390/app12052457 - 26 Feb 2022

Cited by 5 | Viewed by 2598

Abstract

Streptococcus mutans and Fusobacterium nucleatum are two key bacteria of the oral microbiota. Due to their ability to form biofilms on oral tissues, they are both involved in the onset of the most common oral diseases. F. nucleatum is also the principal producer of hydrogen sulfide (H₂S), causative of the awkward bad breath of halitosis. In this study, the oral product Vea^® Oris, made by vitamin E and capric/caprylic acid only, was evaluated as a potential treatment for the most common oral diseases. Different concentrations of the product were tested against both S. mutans and F. nucleatum. The effect on planktonic and biofilm growth was investigated for both strains, and for F. nucleatum, the influence on H₂S production was evaluated. From our data, the product did not relevantly reduce the planktonic growth of both strains, whereas it validly counteracted biofilm assemblage. Moreover, an interesting trend of H₂S reduction was highlighted. Overall, these results suggested, on the one hand, a synergistic antimicrobial–antibiofilm action of two Vea^® Oris components and, together, potential modulation activity on H₂S production. However, the study should be implemented to confirm these only preliminary findings, certainly extending the panel of tested bacteria and using alternative methods of detection. Full article

(This article belongs to the Special Issue Advances in Natural Bioactive Compounds and Biological Effects)

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9 pages, 1890 KiB

Open AccessArticle

Beneficial Effects of Caffeic Acid Phenethyl Ester on Wound Healing in a Diabetic Mouse: Role of VEGF and NO

by Sin-Hee Park, Soo-Young Song, Eun-Hye Park, Eunmin Kim, Gyu Chul Oh, Eun Ho Choo, Byung-Hee Hwang, Kiyuk Chang and Min-Ho Oak

Appl. Sci. 2022, 12(5), 2320; https://doi.org/10.3390/app12052320 - 23 Feb 2022

Cited by 4 | Viewed by 2462

Abstract

Cutaneous wound healing is delayed in patients with diabetes. Caffeic acid phenethyl ester (CAPE) has been identified as an effective constituent of propolis with improved wound healing abilities via an oxidative stress decrease. However, its impact on wound healing in diabetic models and its underlying mechanisms remain unclear. Determining the vascular endothelial growth factor (VEGF) contents in a human vascular smooth muscle cell (VSMC)-conditioned medium was assessed using human VEGF immunoassay and vascular reactivity using porcine coronary artery rings. Later, C57BL/6 or db/db mice were anesthetized, after which a 6-mm biopsy punch was manipulated for perforation via the back skin. Subsequently, CAPE was applied to the wound and changed daily. Furthermore, the injury in each mouse was digitally photographed, and the wound area was quantified. We observed that CAPE increased VEGF levels in human VSMC-conditioned medium, improved endothelium-dependent nitric oxide (NO)-mediated vasorelaxation, inhibited U46619-induced vasoconstriction porcine coronary artery, and enhanced cutaneous wound healing in the diabetic mouse model. Hence, we propose that CAPE improves wound healing in diabetic mice, which is aided by increased VEGF and NO expression. Full article

(This article belongs to the Special Issue Advances in Natural Bioactive Compounds and Biological Effects)

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26 pages, 4850 KiB

Open AccessArticle

Dracocephalum palmatum S. and Dracocephalum ruyschiana L. Originating from Yakutia: A High-Resolution Mass Spectrometric Approach for the Comprehensive Characterization of Phenolic Compounds

by Zhanna M. Okhlopkova, Mayya P. Razgonova, Konstantin S. Pikula, Alexander M. Zakharenko, Wojciech Piekoszewski, Yuri A. Manakov, Sezai Ercisli and Kirill S. Golokhvast

Appl. Sci. 2022, 12(3), 1766; https://doi.org/10.3390/app12031766 - 8 Feb 2022

Cited by 10 | Viewed by 3209

Abstract

Dracocephalum palmatum S. and Dracocephalum ruyschiana L. contain a large number of target analytes, which are biologically active compounds. High performance liquid chromatography (HPLC) in combination with an ion trap (tandem mass spectrometry) was used to identify target analytes in extracts of D. palmatum S. and D. ruyschiana L. originating from Yakutia. The results of initial studies revealed the presence of 114 compounds, of which 92 were identified for the first time in the genus Dracocephalum. New identified metabolites belonged to 17 classes, including 16 phenolic acids and their conjugates, 18 flavones, 5 flavonols, 2 flavan-3-ols, 1 flavanone, 2 stilbenes, 10 anthocyanins, 1 condensed tannin, 2 lignans, 6 carotenoids, 3 oxylipins, 2 amino acids, 3 sceletium alkaloids, 3 carboxylic acids, 8 fatty acids, 1 sterol, and 3 terpenes, along with 6 miscellaneous compounds. It was shown that extracts of D. palmatum are richer in the spectrum of polyphenolic compounds compared with extracts of D. ruyschiana, according to a study of the presence of these compounds in extracts, based on the results of mass spectrometric studies. Full article

(This article belongs to the Special Issue Advances in Natural Bioactive Compounds and Biological Effects)

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16 pages, 758 KiB

Open AccessArticle

Microwave- and Ultrasound-Assisted Extraction of Cucurbita pepo Seeds: A Comparison Study of Antioxidant Activity, Phenolic Profile, and In-Vitro Cells Effects

by Catarina Macedo, Ana Margarida Silva, Ana Sofia Ferreira, Manuela M. Moreira, Cristina Delerue-Matos and Francisca Rodrigues

Appl. Sci. 2022, 12(3), 1763; https://doi.org/10.3390/app12031763 - 8 Feb 2022

Cited by 3 | Viewed by 3173

Abstract

Nowadays there is a growing demand for nutraceuticals to prevent diseases related to redox imbalances, such as atherosclerosis and diabetes, being crucial to search for new matrixes rich in bioactive compounds. This work aims to characterize the value-added compounds extracted from Curcubita pepo seeds using green methodologies, namely microwave-assisted extraction (MAE) and ultrasound-assisted extraction (UAE), employing water as an extracting solvent for two ratios (condition 1: 1 mg/20 mL; condition 2: 2.5 mg/20 mL). The extract with the best antioxidant/antiradical activity in FRAP (71.09 μmol FSE/g DW) and DPPH (5.08 mg TE/g DW) assays was MAE condition 1, while MAE condition 2 exhibited the highest activity in the ABTS assay (13.29 mg AAE/g DW) and TPC (16.89 mg GAE/g DW). A remarkable scavenging capacity was observed, particularly for HOCl, with IC50 values ranging from 1.88–13.50 μg/mL. A total of 21 phenolic compounds were identified, being catechin (4.567–7.354 mg/g DW), caffeine (1.147–2.401 mg/g DW) and gallic acid (0.945–1.337 mg/g DW) predominant. No adverse effects were observed on Caco-2 viability after exposure to MAE extracts, while the other conditions led to a slight viability decrease in NSC-34. These results highlighted that the extract from MAE condition 2 is the most promising as a potential nutraceutical ingredient. Full article

(This article belongs to the Special Issue Advances in Natural Bioactive Compounds and Biological Effects)

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14 pages, 2899 KiB

Open AccessArticle

Thermosonication Process Design for Recovering Bioactive Compounds from Fennel: A Comparative Study with Conventional Extraction Techniques

by Adela Cristina Martinez Urango, Monique Martins Strieder, Eric Keven Silva and Maria Angela A. Meireles

Appl. Sci. 2021, 11(24), 12104; https://doi.org/10.3390/app112412104 - 19 Dec 2021

Cited by 13 | Viewed by 2940

Abstract

This study aimed to examine the impact of the combination of acoustic energy at the nominal powers of 100, 200, 300, and 400 W with moderate heat processing at 40, 50, and 60 °C on the extraction of phytochemical compounds from Foeniculum vulgare. Thermosonication processing, based on high-intensity ultrasound combined with an external heat source, can potentialize the extraction of soluble solids from plant material. However, the excessive temperature increase generated by the two energy sources during thermosonication treatment may degrade the thermolabile bioactive compounds. Regardless of the temperature condition, fennel extracts obtained at 400 W presented lower total phenolic content (TPC) than those obtained at 300 W. The cavitation heat and mechanical stress provided at 400 W may have degraded the phenolic compounds. Thereby, the best extraction condition was 300 W and 60 °C. The fennel extract presented the highest content of TPC (3670 ± 67 µg GAE/g) and antioxidant activity determined by DPPH and ABTS methods (1195 ± 16 µg TE/g and 2543.12 ± 0.00 µg TE/g, respectively) using this treatment. Thermosonication can be an innovative technique for extracting phytochemicals because it provides good results in shorter processing times, with 73% and 88% less energy consumption than Percolation and Soxhlet techniques, respectively. Full article

(This article belongs to the Special Issue Advances in Natural Bioactive Compounds and Biological Effects)

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21 pages, 3422 KiB

Open AccessArticle

Anti-Psoriatic Effects and IL-22 Targeting Mechanism of Indirubin by Suppressing Keratinocyte Inflammation and Proliferation

by Ly Thi Huong Nguyen, Tae-Woo Oh, Min-Jin Choi, In-Jun Yang and Heung-Mook Shin

Appl. Sci. 2021, 11(24), 11599; https://doi.org/10.3390/app112411599 - 7 Dec 2021

Cited by 4 | Viewed by 3036

Abstract

Indigo naturalis, which is extracted from the leaves and branches of Baphicacanthus cusia (Nees) Bremek, has traditionally been used to treat psoriasis. The current study aimed to examine a new mechanism of the components of indigo naturalis, including indirubin, indigo, and tryptanthrin. The anti-psoriatic effects were assessed by the proliferation biomarkers (Ki67, K16), cell cycle progression, ROS production, and interleukin profiling (ICAM-1, TNF-α, IL-6, and IL-8) in IL-22-treated HaCaT cells. Among the components, indirubin significantly decreased intracellular ROS production and lowered the production of ICAM-1, TNF-α, and IL-6 in IL-22-treated HaCaT cells. Indirubin, indigo, and tryptanthrin could decrease the proportion of Ki67-positive cells, but only indirubin decreased the proportion of cells entering the S phase and suppressed the expression of cyclin D1 and cyclin E1 in IL-22-treated HaCaT cells. Indirubin significantly suppressed the phosphorylation of STAT3 and ERK. In vivo, IL-22 was intradermally injected into mouse ears for six days and topically treated with 0.1% or 1% indirubin. In the IL-22-injected mice, treatment with indirubin inhibited epidermal hyperplasia. Immunohistochemistry and western blot analysis demonstrated the downregulation of K16 expression in psoriatic lesions. These results suggest that indirubin, which is a major component of indigo naturalis, may have therapeutic potential in an IL-22-induced psoriasis model. Full article

(This article belongs to the Special Issue Advances in Natural Bioactive Compounds and Biological Effects)

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10 pages, 1165 KiB

Open AccessArticle

Evaluation of Anti-Photoaging Effects of a Novel Cosmeceutical Containing a Retinoids Mixture Using In Vitro Cell Models

by Nicola Zerbinati, Sabrina Sommatis, Cristina Maccario, Maria Chiara Capillo, Serena Di Francesco, Elsa Liga, Raffaele Rauso, Edoardo D’Este, Daniela Dalla Gasperina, Stefania Guida and Roberto Mocchi

Appl. Sci. 2021, 11(21), 9992; https://doi.org/10.3390/app11219992 - 26 Oct 2021

Cited by 6 | Viewed by 2936

Abstract

Physiological ageing due to the passing of time and prolonged exposure to harmful sun rays generate wrinkles and reduce skin elasticity. These visible and clinical signs can be prevented or reversed by known strategies, such as the daily use of cosmetic products with antioxidant combinations or retinoids. A new dermocosmetic formulation enriched with a complex of retinoids, called RETINOIDS SERUM, was investigated through in vitro assays using human skin cells. The experiments were carried out to assess the anti-ageing activity in normal human dermal fibroblasts (NHDF) and epidermal keratinocytes (HaCaT). After the preliminary MTT assay, the proliferation together with the synthesis of collagen and elastin fibers was performed on NHDF cells after 24 h treatment with the two non-cytotoxic concentrations. Using UVB-irradiated HaCaT cells, the measurement of matrix metalloproteinase-1 (MMP-1) levels was also investigated. In vitro studies show that the dermocosmetic product improves collagen and elastin synthesis and the renewal of dermal fibroblasts. Moreover, a reduction in the MMP-1 secretion was also highlighted in UVB-irradiated HaCaT cells. These results suggest that the cosmetic formulation containing functional compounds such as retinoids can be useful to prevent the natural sign of ageing. Full article

(This article belongs to the Special Issue Advances in Natural Bioactive Compounds and Biological Effects)

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16 pages, 34616 KiB

Open AccessArticle

Development of a Mouthwash Using Freeze-Drying Technique: An Optimization Study

by Sonia M. Iurian, Diana-Roxana Adespei, Anca Pop, Ionel Fizeșan, Rahela Carpa, Mirela L. Moldovan, Felicia Loghin, Marcela Achim and Cătălina Bogdan

Appl. Sci. 2021, 11(20), 9609; https://doi.org/10.3390/app11209609 - 15 Oct 2021

Cited by 3 | Viewed by 2613

Abstract

In recent years, the development of solid cosmetics, as part of sustainable cosmetics strategy, is generating increasing interest. In addition, novel approaches such as Quality by Design concept allowed the development of high-quality products together with a decrease in waste generation. The present study aimed the development of freeze-dried mouthwashes containing Cetraria islandica extract using the Quality by Design approach. Based on the results of preliminary experiments, a factorial design with three factors that varied on two levels was developed. As factors, the filler type (sorbitol or mannitol) was chosen as the qualitative factor and the two quantitative factors were: the filler ratio set from 3 to 5% and polymer (methylcellulose) ratio from 0 to 0.5%. After the preparation and the complete characterization of the formulations generated through the experimental design, the effect of the formulation variables on the lyophilized mouthwashes and the interactions between formulation factors were investigated. Finally, an optimal formulation with appropriate mechanical properties that ensure easy manipulation and no material loss when extracted from the package and fast reconstitution was generated. Full article

(This article belongs to the Special Issue Advances in Natural Bioactive Compounds and Biological Effects)

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15 pages, 2852 KiB

Open AccessArticle

Puerarin Improves Dexamethasone-Impaired Wound Healing In Vitro and In Vivo by Enhancing Keratinocyte Proliferation and Migration

by Ly Thi Huong Nguyen, Sang-Hyun Ahn, Min-Jin Choi, In-Jun Yang and Heung-Mook Shin

Appl. Sci. 2021, 11(19), 9343; https://doi.org/10.3390/app11199343 - 8 Oct 2021

Cited by 6 | Viewed by 3011

Abstract

The delayed and impaired wound healing caused by dexamethasone (DEX) is commonly reported. Puerarin, the major isoflavone found in Pueraria montana var. lobata (Willd.) Sanjappa & Pradeep promoted the wound healing process in diabetic rats. However, the effects and underlying mechanisms of puerarin on DEX-impaired wound healing have not been investigated. This study examined the potential uses of puerarin in upregulating keratinocyte proliferation and migration in dexamethasone (DEX)-suppressed wound healing model. The effects of puerarin on wound healing in vivo were investigated by taking full-thickness 5 mm punch biopsies from the dorsal skin of BALB/c mice and then treating them topically with 0.1% DEX. For the in vitro study, DEX-treated HaCaT cells were used to examine the effects of puerarin on DEX-induced keratinocyte proliferation and migration and the mechanisms of its action. Puerarin, when applied topically, accelerated the wound closure rate, increased the density of the capillaries, and upregulated the level of collagen fibers and TGF-β in the wound sites compared to the DEX-treated mice. Puerarin promoted the proliferation and migration of keratinocytes by activating the ERK and Akt signaling pathways in DEX-treated HaCaT cells. In conclusion, puerarin could be effective in reversing delayed and disrupted wound healing associated with DEX treatments. Full article

(This article belongs to the Special Issue Advances in Natural Bioactive Compounds and Biological Effects)

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