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Bioactive Formulations in Agri-Food-Pharma: Source and Applications

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A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Synthetic Biology and Bioengineering".

Deadline for manuscript submissions: closed (31 January 2021) | Viewed by 54373

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Special Issue Editors

Prof. Dr. Vijai Kumar Gupta

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Guest Editor

AgroBioSciences (AgBS) and Chemical & Biochemical Sciences (CBS) Department, University Mohammed VI Polytechnic (UM6P), Hay Moulay Rachid, Ben Guerir 43150, Morocco
Interests: bioactive natural products; microbial biotechnology; applied mycology; enzyme and bioprocess technology; biomass to bioproducts development
Special Issues, Collections and Topics in MDPI journals

Prof. David Julian McClements

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Guest Editor

Department of Food Science, University of Massachusetts Amherst, Amherst, MA 01003, USA
Interests: food biopolymers and colloids; oral delivery systems; gastrointestinal fate of nutrients and nutraceuticals; food nanotechnology

Dr. Minaxi Sharma

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Guest Editor

Haute Ecole Provinciale de Hainaut-Condorcet, Rue Paul Pastur, 7800 Ath, Belgium
Interests: nanoemulsions; bioactive natural extracts; controlled drug delivery; nanoencapsulation; food ingredients; functional and nutraceutical foods; bioavailability
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Pratyoosh Shukla

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Guest Editor

School of Biotechnology, Banaras Hindu University, Varanasi, India
Interests: enzyme technology; microbial biotechnology; proteins; bioinformatics; bioprocessing technologies

Special Issue Information

Dear Colleagues,

Bioactive compounds comprise both essential and nonessential compounds and have been shown to have a beneficial effect on agri-food pharma-health. Biologically active compounds, also known as secondary metabolites (including flavonoids, phytosterols, polyphenols, and saponins), possess several biological activities (including nutraceuticals, biopharma, biosurfactant, biostimulants, cosmeceuticals, etc.) and are produced alongside primary biosynthetic and metabolic routes for compounds associated with growth and development. The advancement of the agri-food pharma-health industry depends on the development of new and novel bioactive compounds and their formulations from natural sources. Thus, progress in the identification and production of novel natural bioactives may be a critical functional source of therapeutic, commercial, and industrial importance. Observations from nature and diversity of natural bioactive complexes have encouraged researchers to engineer novel compounds from microbes as well as plant sources.

Due to their high potential, several efforts should be directed to the study and enhanced production of new bioactives as antioxidant, antimicrobial, antiviral, and anticancer compounds, among others. Additionally, bioactive components present as natural ingredients in food provide wellbeing benefits beyond the essential nutritive value of the product. Different classes of bio-phytochemicals have been identified as having a preventive effect against specific wellbeing and health-promoting activities in the agri-food pharma sector.

Extraction and purification of valuable natural products from native biological sources is very important. Further, their bioprospecting for a variety of applications in agri-food pharma is very much dependent on their efficient formulations. This Special Issue aims to compile the recent developments in the production of natural compounds from various bioresources, and their formulations as bioactives. In addition, this SI will also cover the in-depth engineered approaches for enhanced biological properties and potential industrial applications of new bioactive formulations through novel strategies aiming at the identification of novel compounds and bioprocess tools to improve the quantity and quality of such products. Increasing knowledge on the bioactive formulations on regulation at the genomic and molecular levels will lead to a re-consideration of health goals.

This SI will publish the articles on recent trends, applications, advancements, and engineering approaches for the biosynthesis of natural products, with a particular emphasis on bioactive formulations for applications in agri-food pharma.

Dr. Vijai Kumar Gupta
Prof. David Julian McClements
Dr. Minaxi Sharma
Prof. Pratyoosh Shukla
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. Biomolecules is an international peer-reviewed open access monthly 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 2700 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

Agri-food pharma-health
Anticancer
Antioxidant
Antimicrobial
Biopharmaceuticals
Biostimulants
Bioactivity and chemical profiling
Drug delivery
Encapsulation
Nanoemulsions
Nanoparticles
Nutraceuticals
Value-added bioactives

Published Papers (14 papers)

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Editorial

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6 pages, 390 KiB

Open AccessEditorial

Bio-Based Formulations for Sustainable Applications in Agri-Food-Pharma

by Minaxi Sharma, Rajeev Bhat, Zeba Usmani, David Julian McClements, Pratyoosh Shukla, Vinay B. Raghavendra and Vijai Kumar Gupta

Biomolecules 2021, 11(5), 768; https://doi.org/10.3390/biom11050768 - 20 May 2021

Cited by 3 | Viewed by 2778

Abstract

Currently, there is a strong enduring interest towards obtaining high-value, sustainable bio-based bioactive compounds from natural resources, as there is great demand for these compounds in various market sectors such as agriculture, food, pharma, cosmeceuticals, and others [...] Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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Research

Jump to: Editorial

17 pages, 7037 KiB

Open AccessArticle

Comparison of Anticancer Activity of Dorycnium pentaphyllum Extract on MCF-7 and MCF-12A Cell Line: Correlation with Invasion and Adhesion

by Gözde Koygun, Emine Arslan, Gökhan Zengin, Giustino Orlando and Claudio Ferrante

Biomolecules 2021, 11(5), 671; https://doi.org/10.3390/biom11050671 - 30 Apr 2021

Cited by 6 | Viewed by 2717

Abstract

Dorycnium pentaphyllum subsp. haussknechtii is an important medicinal plant in several countries, including Turkey. This study aimed to evaluate the cytotoxicity of a crude extract of D. pentaphyllum subsp. haussknechtii against different breast cell lines to determine invasion, adhesion, and lipid peroxidation. The cytotoxic effects on MCF-7 breast cancer and MCF-12A as the immortalized cell line were examined by the XTT assay. Invasion and adhesion studies were performed according to the manufacturer’s kit procedure to IC₅₀ values for 48 h. Lipid peroxidation was measured in the MCF-7 cell. A bioinformatics analysis was conducted to unravel the mechanism of action underlying antiproliferative effects, as well. According to XTT results, the tested extract showed a time- and a concentration-dependent cytotoxic effect. The most effective concentration was 100.5 µg/mL (48 h), which was selected for biological activities, such as apoptotic activity, invasion, adhesion, and lipid peroxidation assays. The extract caused tumoral cell death, and it did not have a cytotoxic effect on healthy human breast cells. Duplication times and measurement of CI analyses of cells were performed using the real-time cell analysis system xCELLigence. Finally, the bioinformatics analysis indicated the prominent role of quercetin as an extract component exerting a key role in the observed antiproliferative effects. This was supported by the micromolar/submicromolar affinity of quercetin towards proto-oncogene serine/threonine–protein kinase (PIM-1) and hematopoietic cell kinase (HCK), both involved in breast cancer. Altogether, our findings proposed that the extraction of the plant can be an effective strategy to isolate biomolecules with promising cytotoxic effects against breast cancer cells. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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10 pages, 1092 KiB

Open AccessArticle

Evaluation of In Vitro Capsaicin Release and Antimicrobial Properties of Topical Pharmaceutical Formulation

by Enkelejda Goci, Entela Haloci, Antonio Di Stefano, Annalisa Chiavaroli, Paola Angelini, Ajkuna Miha, Ivana Cacciatore and Lisa Marinelli

Biomolecules 2021, 11(3), 432; https://doi.org/10.3390/biom11030432 - 15 Mar 2021

Cited by 22 | Viewed by 4414

Abstract

(1) Background: Capsaicin is the main capsaicinoid of the Capsicum genus and it is responsible for the pungent taste. Medical uses of the fruits of chili peppers date from the ancient time until nowadays. Most of all, they are used topically as analgesic in anti-inflammatory diseases as rheumatism, arthritis and in diabetic neuropathy. Reports state that the Capsicum genus, among other plant genera, is a good source of antimicrobial and antifungal compounds. The aim of this study was the preparation of a pharmaceutical Carbopol-based formulation containing capsaicin and the evaluation of its in vitro release and antimicrobial and antifungal properties. (2) Methods: It was first stabilized with an extraction method from the Capsicum annuum fruits with 98% ethanol and then the identification and determination of Capsaicin in this extract was realized by HPLC. (3) Results and Conclusions: Rheological analyses revealed that the selected formulation exhibited a pseudo-plastic behavior. In vitro release studies of capsaicin from a Carbopol-based formulation reported that approximately 50% of capsaicin was release within 52 h. Additionally, the Carbopol-based formulation significantly increased the antimicrobial effects of capsaicin towards all tested bacteria and fungi strains. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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17 pages, 4798 KiB

Open AccessArticle

Chemical and Bioinformatics Analyses of the Anti-Leishmanial and Anti-Oxidant Activities of Hemp Essential Oil

by Luigi Menghini, Claudio Ferrante, Simone Carradori, Marianna D’Antonio, Giustino Orlando, Francesco Cairone, Stefania Cesa, Antonello Filippi, Caterina Fraschetti, Gokhan Zengin, Gunes Ak, Massimo Tacchini and Kashif Iqbal

Biomolecules 2021, 11(2), 272; https://doi.org/10.3390/biom11020272 - 12 Feb 2021

Cited by 25 | Viewed by 3988

Abstract

Industrial hemp is a multiuse crop that has been widely cultivated to produce fibers and nutrients. The capability of the essential oil (EO) from inflorescences as antimicrobial agent has been reported. However, literature data are still lacking about the hemp EO antiprotozoal efficacy in vivo. The present study aims to unravel this concern through the evaluation of the efficacy of hemp EOs (2.5 mL/kg, intraperitoneally) of three different cultivars, namely Futura 75, Carmagnola selezionata and Eletta campana, in mice intraperitoneally infected with Leishmania tropica. A detailed description of EO composition and targets-components analysis is reported. Myrcene, α-pinene and E-caryophyllene were the main components of the EOs, as indicated by the gas-chromatographic analysis. However, a prominent position in the scenario of the theoretical interactions underlying the bio-pharmacological activity was also occupied by selina-3,7(11)-diene, which displayed affinities in the micromolar range (5.4–28.9) towards proliferator-activated receptor α, cannabinoid CB2 receptor and acetylcholinesterase. The content of this compound was higher in Futura 75 and Eletta campana, in accordance with their higher scavenging/reducing properties and efficacy against the tissue wound, induced by L. tropica. Overall, the present study recommends hemp female inflorescences, as sources of biomolecules with potential pharmacological applications, especially towards infective diseases. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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16 pages, 4796 KiB

Open AccessArticle

Green Synthesis of Silver Nanoparticles by Cytobacillus firmus Isolated from the Stem Bark of Terminalia arjuna and Their Antimicrobial Activity

by Sujesh Sudarsan, Madan Kumar Shankar, Anil Kumar Belagal Motatis, Sushmitha Shankar, Darshan Krishnappa, Chakrabhavi Dhananjaya Mohan, Kanchugarakoppal S. Rangappa, Vijai Kumar Gupta and Chandra Nayaka Siddaiah

Biomolecules 2021, 11(2), 259; https://doi.org/10.3390/biom11020259 - 10 Feb 2021

Cited by 32 | Viewed by 3643

Abstract

This work reports an eco-friendly synthesis of silver nanoparticles (AgNPs) using endophytic bacteria, Cytobacillus firmus isolated from the stem bark of Terminalia arjuna. The synthesis of AgNPs was confirmed by visual observation as a change in color of the bacterial solution impregnated with silver. Further, the morphology of the AgNPs, average size, and presence of elemental silver were characterized by UV–Visible spectroscopy, scanning electron microscopy, and dynamic light scattering spectroscopy. The roles of endophytic secondary metabolites in the metal reduction, stabilization, and capping of silver nanoparticles were studied by qualitative FTIR spectral peaks. The antimicrobial ability of AgNPs was evaluated against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria and pearl millet blast disease-causing fungi (Magnoporthe grisea). The biosynthesized AgNPs showed good antibacterial and antifungal activities. AgNPs effectively inhibited the bacterial growth in a dose-dependent manner and presented as good antifungal agents towards the growth of Magnoporthe grisea. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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17 pages, 2029 KiB

Open AccessArticle

Deeper Insights on Alchornea cordifolia (Schumach. & Thonn.) Müll.Arg Extracts: Chemical Profiles, Biological Abilities, Network Analysis and Molecular Docking

by Kouadio Ibrahime Sinan, Gunes Ak, Ouattara Katinan Etienne, József Jekő, Zoltán Cziáky, Katalin Gupcsó, Maria João Rodrigues, Luisa Custodio, Mohamad Fawzi Mahomoodally, Jugreet B. Sharmeen, Luigi Brunetti, Sheila Leone, Lucia Recinella, Annalisa Chiavaroli, Giustino Orlando, Luigi Menghini, Massimo Tacchini, Claudio Ferrante and Gokhan Zengin

Biomolecules 2021, 11(2), 219; https://doi.org/10.3390/biom11020219 - 4 Feb 2021

Cited by 8 | Viewed by 3405

Abstract

Alchornea cordifolia (Schumach. & Thonn.) Müll. Arg. is a well-known African medicinal plant traditionally used for various healing purposes. In the present study, methanolic, ethyl acetate and infusion extracts of A. cordifolia leaves were studied for their total phenolic and flavonoid contents and screened for their chemical composition. Moreover, the enzyme (acetyl- and butyryl-cholinesterases, α-amylase, α-glucosidase, and tyrosinase) inhibitory and cytotoxicity activities on HepG2: human hepatocellular carcinoma cells, B16 4A5: murine melanoma cells, and S17: murine bone marrow (normal) cells of extracts were evaluated. Finally, components-targets and docking analyzes were conducted with the aim to unravel the putative mechanisms underlying the observed bio-pharmacological effects. Interestingly, the infusion and methanolic extracts showed significantly higher total phenolic and flavonoid contents compared with the ethyl acetate extract (TPC: 120.38–213.12 mg GAE/g and TFC: 9.66–57.18 mg RE/g). Besides, the methanolic extracts followed by the infusion extracts were revealed to contain a higher number of compounds (84 and 74 compounds, respectively), while only 64 compounds were observed for the ethyl acetate extract. Gallic acid, ellagic acid, shikimic acid, rutin, quercetin, myricetin, vitexin, quercitrin, kaempferol, and naringenin were among the compounds that were commonly identified in all the studied extracts. Additionally, the methanolic and infusion extracts displayed higher antioxidant capacity than ethyl acetate extract in all assays performed. In ABTS and DPPH radical scavenging assays, the methanol extract (500.38 mg TE/g for DPPH and 900.64 mg TE/g for ABTS) exhibited the best ability, followed by the water and ethyl acetate extracts. Furthermore, the extracts exhibited differential enzyme inhibitory profiles. In particular, the methanolic and infusion extracts showed better cytotoxic selectivity activity against human hepatocellular carcinoma cells. Overall, this study demonstrated A cordifolia to be a species worthy of further investigations, given its richness in bioactive phytochemicals and wide potentialities for antioxidants and pharmacological agents. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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13 pages, 1062 KiB

Open AccessArticle

Tailoring the Health-Promoting Potential of Protein Hydrolysate Derived from Fish Wastes and Flavonoids from Yellow Onion Skins: From Binding Mechanisms to Microencapsulated Functional Ingredients

by Leontina Grigore-Gurgu, Oana Crăciunescu, Iuliana Aprodu, Carmen Alina Bolea, Andreea Iosăgeanu, Brîndușa Alina Petre, Gabriela Elena Bahrim, Anca Oancea and Nicoleta Stănciuc

Biomolecules 2020, 10(10), 1416; https://doi.org/10.3390/biom10101416 - 7 Oct 2020

Cited by 8 | Viewed by 2676

Abstract

This study focuses on combining different bioprocessing tools in order to develop an in-depth engineering approach for enhancing the biological properties of two valuable food by-products, namely fish waste and yellow onion skins, in a single new bioactive formulation. Bone tissue from phytophagous carp (Hypophthalmichthys molitrix) was used to obtain bioactive peptides through papain-assisted hydrolysis. The peptides with molecular weight lower than 3 kDa were characterized through MALDI-ToF/ToF mass spectrometry and bioinformatics tools. As a prerequisite for microencapsulation, the ability of these peptides to bind the flavonoids extracted from yellow onion skins was further tested through fluorescence quenching measurements. The results obtained demonstrate a considerable binding potency with a binding value of 10⁶ and also the presence of one single or one class of binding site during the interaction process of flavonoids with peptides, in which the main forces involved are hydrogen bonds and van der Waals interactions. In the freeze-drying microencapsulation process, an efficiency for total flavonoids of 88.68 ± 2.37% was obtained, considering the total flavonoids and total polyphenols from the powder of 75.72 ± 2.58 quercetin equivalents/g dry weight (DW) and 97.32 ± 2.80 gallic acid equivalents/g DW, respectively. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) test on the L929 cell line cultivated in the presence of different concentrations of microencapsulated samples (0.05–1.5 mg/mL) proved no sign of cytotoxicity, the cell viability being over 80% for all the samples. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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18 pages, 2139 KiB

Open AccessArticle

Detection and Characterization of Antibacterial Siderophores Secreted by Endophytic Fungi from Cymbidium aloifolium

by Srinivas Chowdappa, Shubha Jagannath, Narasimhamurthy Konappa, Arakere C. Udayashankar and Sudisha Jogaiah

Biomolecules 2020, 10(10), 1412; https://doi.org/10.3390/biom10101412 - 6 Oct 2020

Cited by 61 | Viewed by 5041

Abstract

Endophytic fungi from orchid plants are reported to secrete secondary metabolites which include bioactive antimicrobial siderophores. In this study endophytic fungi capable of secreting siderophores were isolated from Cymbidium aloifolium, a medicinal orchid plant. The isolated extracellular siderophores from orchidaceous fungi act as chelating agents forming soluble complexes with Fe³⁺. The 60% endophytic fungi of Cymbidium aloifolium produced hydroxamate siderophore on CAS agar. The highest siderophore percentage was 57% in Penicillium chrysogenum (CAL1), 49% in Aspergillus sydowii (CAR12), 46% in Aspergillus terreus (CAR14) by CAS liquid assay. The optimum culture parameters for siderophore production were 30 °C, pH 6.5, maltose and ammonium nitrate and the highest resulting siderophore content was 73% in P. chrysogenum. The total protein content of solvent-purified siderophore increased four-fold compared with crude filtrate. The percent Fe³⁺ scavenged was detected by atomic absorption spectra analysis and the highest scavenging value was 83% by P. chrysogenum. Thin layer chromatography of purified P. chrysogenum siderophore showed a wine-colored spot with R_f value of 0.54. HPLC peaks with R_ts of 10.5 and 12.5 min were obtained for iron-free and iron-bound P. chrysogenum siderophore, respectively. The iron-free P. chrysogenum siderophore revealed an exact mass-to-charge ratio (m/z) of 400.46 and iron-bound P. chrysogenum siderophore revealed a m/z of 453.35. The solvent-extracted siderophores inhibited the virulent plant pathogens Ralstonia solanacearum, that causes bacterial wilt in groundnut and Xanthomonas oryzae pv. oryzae which causes bacterial blight disease in rice. Thus, bioactive siderophore-producing endophytic P. chrysogenum can be exploited in the form of formulations for development of resistance against other phytopathogens in crop plants. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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17 pages, 4779 KiB

Open AccessArticle

Anti-Survival and Pro-Apoptotic Effects of 6-Shogaol on SW872 Human Liposarcoma Cells via Control of the Intrinsic Caspase Pathway, STAT-3, AMPK, and ER Stress

by Anil Kumar Yadav and Byeong-Churl Jang

Biomolecules 2020, 10(10), 1380; https://doi.org/10.3390/biom10101380 - 28 Sep 2020

Cited by 10 | Viewed by 2615

Abstract

Notably, 6-Shogaol, a bioactive natural substance, has anticancer effects on many types of tumors. Up to date, the anticancer effect and mode of action of 6-Shogaol on liposarcoma are not known. In this study, we investigated whether 6-Shogaol inhibits the growth of SW872 and 93T449 cells, two different human liposarcoma cell lines. Of note, 6-Shogaol inhibited the growth of SW872 and 93T449 cells without affecting that of normal 3T3-L1 preadipocytes. Specifically, 6-Shogaol further induced the apoptosis of SW872 cells, as evidenced by nuclear DNA fragmentation, increased sub G1 population, activation of the intrinsic caspase pathway, and PARP cleavage. However, pretreatment with either z-VAD-fmk, a pan-caspase inhibitor, or N-acetylcysteine, an antioxidant, attenuated the 6-Shogaol’s growth-suppressive and apoptosis-inducing effects on SW872 cells. Moreover, 6-Shogaol activated AMPK while inhibited STAT-3 in SW872 cells, and siRNA-based genetic silencing of AMPK or STAT-3 considerably blocked the growth-suppressive and apoptotic response of 6-Shogaol to SW872 cells. Moreover, 6-Shogaol also upregulated the expression and phosphorylation of GRP-78, eIF-2α, ATF4, and CHOP, known ER stress markers, in SW872 cells, illustrating the induction of ER stress. These findings collectively demonstrate that 6-Shogaol has strong antigrowth and proapoptotic effects on SW872 cells through regulation of the intrinsic caspase pathway, oxidative stress, STAT-3, AMPK, and ER stress. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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14 pages, 1731 KiB

Open AccessArticle

The Interaction of Bovine β-Lactoglobulin with Caffeic Acid: From Binding Mechanisms to Functional Complexes

by Nicoleta Stănciuc, Gabriela Râpeanu, Gabriela Elena Bahrim and Iuliana Aprodu

Biomolecules 2020, 10(8), 1096; https://doi.org/10.3390/biom10081096 - 23 Jul 2020

Cited by 10 | Viewed by 2586

Abstract

In this study, the interaction of native and transglutaminase (Tgase) cross-linked β-lactoglobulin (β-LG) with caffeic acid (CA) was examined, aiming to obtain functional composites. Knowledge on the binding affinity and interaction mechanism was provided by performing fluorescence spectroscopy measurements, after heating the native and cross-linked protein at temperatures ranging from 25 to 95 °C. Regardless of the protein aggregation state, a static quenching mechanism of intrinsic fluorescence of β-LG by CA was established. The decrease of the Stern–Volmer constants with the temperature increase indicating the facile dissociation of the weakly bound complexes. The thermodynamic analysis suggested the existence of multiple contact types, such as Van der Waals’ force and hydrogen bonds, between β-LG and CA. Further molecular docking tests indicated the existence of various CA binding sites on the β-LG surface heat-treated at different temperatures. Anyway, regardless of the simulated temperature, the CA-β-LG assemblies appeared to be unstable. Compared to native protein, the CA-β-LG and CA-β-LG_Tgase complexes (ratio 1:1) exhibited significantly higher antioxidant activity and inhibitory effects on α-glucosidase, α-amylase, and pancreatic lipase, enzymes associated with metabolic syndrome. These findings might help the knowledge-based development of novel food ingredients with valuable biological properties. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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0 pages, 4429 KiB

Open AccessArticle

RETRACTED: Optimized Ellagic Acid–Ca Pectinate Floating Beads for Gastroprotection against Indomethacin-Induced Gastric Injury in Rats

by Nabil A. Alhakamy, Shaimaa M. Badr-Eldin, Osama A. A. Ahmed, Abdulrahman A. Halwani, Hibah M. Aldawsari, Mohamed A. El-Moselhy, Aliaa Anter, Sara S. Sharkawi, Muhammad H. Sultan, Osama A. A. Madkhali, Muhammed A. Bakhrebah, Mohammad N. Alomary, Wesam H. Abdulaal and Usama A. Fahmy

Biomolecules 2020, 10(7), 1006; https://doi.org/10.3390/biom10071006 - 6 Jul 2020

Cited by 7 | Viewed by 3850 | Retraction

Abstract

A peptic ulcer is an alimentary tract injury that leads to a mucosal defect reaching the submucosa. This work aimed to optimize and maximize ellagic acid (EA) loading in Ca pectinate floating beads to maximize the release for 24 h. Three factors were selected: Ca pectinate concentration (X1, 1–3 w/v %), EA concentration (X2, 1–3 w/v %) and the dropping time (X3, 10–30 min). The factorial design proposed eight formulations. The optimized EA–Ca pectinate formulation was evaluated for the gastric ulcer index and the oxidative stress parameter determination of gastric mucosa. The results indicated that the optimum EA–Ca pectinate formula significantly improved the gastric ulcer index in comparison with raw EA. The protective effect of the optimized EA–Ca pectinate formula was further indicated by the histopathological features of the stomach. The results of the study indicate that an EA formulation in the form of Ca pectinate beads would be effective for protection against gastric ulcers because of Nonsteroidal anti-inflammatory drugs (NSAID) administration. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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19 pages, 4063 KiB

Open AccessArticle

Co-Delivery of Imiquimod and Curcumin by Nanoemugel for Improved Topical Delivery and Reduced Psoriasis-Like Skin Lesions

by Mohammed S. Algahtani, Mohammad Zaki Ahmad, Ihab Hamed Nourein and Javed Ahmad

Biomolecules 2020, 10(7), 968; https://doi.org/10.3390/biom10070968 - 27 Jun 2020

Cited by 56 | Viewed by 5215

Abstract

The current investigation aimed to improve the topical efficacy of imiquimod in combination with curcumin using the nanoemulsion-based delivery system through a combinatorial approach. Co-delivery of curcumin acts as an adjuvant therapeutic and to minimize the adverse skin reactions that are frequently associated with the topical therapy of imiquimod for the treatment of cutaneous infections and basal cell carcinomas. The low-energy emulsification method was used for the nano-encapsulation of imiquimod and curcumin in the nanodroplet oil phase, which was stabilized using Tween 20 in an aqueous dispersion system. The weak base property of imiquimod helped to increase its solubility in oleic acid compared with ethyl oleate, which indicates that fatty acids should be preferred as the oil phase for the design of imiquimod-loaded topical nanoemulsion compared with fatty acid esters. The phase diagram method was used to optimize the percentage composition of the nanoemulsion formulation. The mean droplet size of the optimized nanoemulsion was 76.93 nm, with a polydispersity index (PdI) value of 0.121 and zeta potential value of −20.5 mV. The optimized imiquimod-loaded nanoemulsion was uniformly dispersed in carbopol 934 hydrogel to develop into a nanoemulgel delivery system. The imiquimod nanoemulgel exhibited significant improvement (p < 0.05) in skin permeability and deposition profile after topical application. The in vivo effectiveness of the combination of imiquimod and curcumin nanoemulgel was compared to the imiquimod nanoemulgel and imiquimod gel formulation through topical application for ten days in BALB/c mice. The combination of curcumin with imiquimod in the nanoemulgel system prevented the appearance of psoriasis-like symptoms compared with the imiquimod nanoemulgel and imiquimod gel formulation entirely. Further, the imiquimod nanoemulgel as a mono-preparation slowed and reduced the psoriasis-like skin reaction when compared with the conventional imiquimod gel, and that was contributed to by the control release property of the nano-encapsulation approach. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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15 pages, 6815 KiB

Open AccessArticle

Anti-Bacterial and Anti-Candidal Activity of Silver Nanoparticles Biosynthesized Using Citrobacter spp. MS5 Culture Supernatant

by Aftab Hossain Mondal, Dhananjay Yadav, Asghar Ali, Neelofar Khan, Jun O Jin and Qazi Mohd Rizwanul Haq

Biomolecules 2020, 10(6), 944; https://doi.org/10.3390/biom10060944 - 22 Jun 2020

Cited by 21 | Viewed by 3267

Abstract

The present study described the extracellular synthesis of silver nanoparticles (AgNPs) using environmental bacterial isolate Citrobacter spp. MS5 culture supernatant. To our best knowledge, no previous study reported the biosynthesis of AgNPs using this bacterial isolate. The biosynthesized AgNPs were characterized using different techniques like UV-Vis spectroscopy, fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), transmission electron microscopy (TEM), scanning electron microscopy (SEM) equipped with energy dispersive X-ray (EDX). The analysis of UV-Vis spectra revealed absorption maxima at 415 nm due to surface plasmon resonance (SPR) indicated the formation of AgNPs and FTIR spectrum confirmed the participation of proteins molecule in AgNPs synthesis. XRD and EDX spectrum confirmed the metallic and crystalline nature of AgNPs. TEM and SEM showed spherical nanoparticles with a size range of 5–15 nm. The biosynthesized AgNPs showed effective independent as well as enhanced combined antibacterial activity against extended spectrum β-lactamase (ESBL) producing multidrug resistant Gram-negative bacteria. Further, effective antifungal activity of AgNPs was observed towards pathogenic Candida spp. The present study provides evidence for eco-friendly biosynthesis of well-characterized AgNPs and their potential antibacterial as well as antifungal activity. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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13 pages, 7572 KiB

Open AccessArticle

Development of Biodegradable Agar-Agar/Gelatin-Based Superabsorbent Hydrogel as an Efficient Moisture-Retaining Agent

by Jyoti Chaudhary, Sourbh Thakur, Minaxi Sharma, Vijai Kumar Gupta and Vijay Kumar Thakur

Biomolecules 2020, 10(6), 939; https://doi.org/10.3390/biom10060939 - 22 Jun 2020

Cited by 37 | Viewed by 6374

Abstract

Downgrading in the yield of crop is due to the inadequate availability of water. The way out for this trouble is to construct synthetic resources dependent on natural polymers with great water absorption and preservation limits. The present study investigated the design of agar-agar (Agr) and gelatin (GE) copolymerized methyl acrylate (MA) and acrylic acid (AA) hydrogel (Agr/GE-co-MA/AA) as a soil conditioner for moisture maintenance in agriculture. Agr/GE-co-MA/AA hydrogel was prepared by utilizing microwave-assisted green synthesis following the most suitable reaction conditions to obtain a remarkable water swelling percentage. The fabricated Agr/GE-co-MA/AA hydrogel was investigated through field emission scanning electron microscopy (FESEM), fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). The water holding capacity of the soil and sand was examined by mixing Agr/GE-co-MA/AA hydrogel with soil and sand. The result demonstrates that the water holding time extended from 10 to 30 days for soil and 6 to 10 days for sand by using Agr/GE-co-MA/AA hydrogel. This synthesized biodegradable, low-cost and non-toxic Agr/GE-co-MA/AA hydrogel shows novelty as soil water maintaining material for irrigation in agriculture. Full article

(This article belongs to the Special Issue Bioactive Formulations in Agri-Food-Pharma: Source and Applications)

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