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Separations
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Separation, Analysis and Biological Evaluation of Bioactive Compounds
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Separation, Analysis and Biological Evaluation of Bioactive Compounds

A special issue of Separations (ISSN 2297-8739). This special issue belongs to the section "Analysis of Natural Products and Pharmaceuticals".

Deadline for manuscript submissions: closed (30 June 2023) | Viewed by 10747

Special Issue Editors

Prof. Dr. Fatma M. Abdel Bar

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Guest Editor
1. Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
2. Department of Pharmacognosy, Faculty of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj 11942, Saudi Arabia
Interests: natural products; chromatographic separation; structural elucidation; antioxidant activity; biological activities of natural products
Dr. Ahmed Awad Zaki

E-Mail Website
Guest Editor
1. Pharmacognosy Department, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
2. Department of Medicinal Chemistry College of Pharmacy, University of Florida, Gainesville, FL 32610, USA
Interests: isolation, structure elucidation and bioassays of the secondary metabolites from medicinal plants, endophytes and marine life; biotransformation of secondary metabolites by different microorganisms and total synthesis of natural products
Dr. Ahmed Adel Ashour

E-Mail Website
Guest Editor
1. Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
2. Department of Pharmacognosy, Faculty of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj 11942, Saudi Arabia
Interests: natural product chemistry; phytochemical isolation of natural compounds from different sources including plant, fungi and marine life and their structural elucidation using different techniques

Special Issue Information

Dear Colleagues,

The development of new procedures for the separation, extraction, characterization, and analysis of bioactive compounds, with either synthetic or natural origins, is of critical concern. For natural bioactive compounds, their general features, including structural diversity and complexity, and the existence of chiral centers and stereochemistry usually affect pharmacological actions, whereas synthetic chemicals represent the basis of pharmaceutical industrial production. Moreover, screening the biological activities of compounds by in vitro, in vivo, ex vivo, and in silico models introduces new opportunities for pharmaceutical and therapeutic applications. Additionally, many bioactive molecules can be reintroduced now, especially after revolutions in molecular biology, high-throughput screening, and in silico technologies. Several methods are engaged in the separation, extraction, identification, and analysis of bioactive compounds, including Nuclear Magnetic Resonance (NMR), Fourier Transform Infrared Spectroscopy (FTIR), X-ray diffraction (XRD), UV-VIS spectrophotometry, hyphenated HPLC, GC analytical methods, etc. Thus, separation and structure identification are two stages in the drug discovery and development (DD and D) process.

Prof. Dr. Fatma M. Abdel Bar
Dr. Ahmed Awad Zaki
Dr. Ahmed Adel Ashour
Guest Editors

Manuscript Submission Information

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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. Separations 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 2600 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

  • separation of bioactive compounds
  • identification of bioactive compounds
  • extraction of bioactive compounds
  • analysis of bioactive compounds
  • biological evaluation of bioactive compounds

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Published Papers (5 papers)

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Research

12 pages, 1806 KiB  
Article
Isolation of Alkaloids from Sinomenium acutum by Centrifugal Partition Chromatography and Their Ameliorating Effects on Dexamethasone-Induced Atrophy in C2C12 Myotubes
by Eun Ju Jung, Ji Hoon Kim, Hye Mi Kim, Shuo Guo, Do Hyun Lee, Gyu Min Lim, Ahmed Shah Syed, Wondong Kim and Chul Young Kim
Separations 2023, 10(9), 470; https://doi.org/10.3390/separations10090470 - 25 Aug 2023
Viewed by 1576
Abstract
Bioactivity-guided isolation was conducted using centrifugal partition chromatography (CPC) from an extract of Sinomenium acutum rhizome, which has shown promising preventive effects in a dexamethasone-induced C2C12 myotube atrophy model. CPC was operated with a solvent system of n-butanol–acetonitrile–water (10:2:8, v/v [...] Read more.
Bioactivity-guided isolation was conducted using centrifugal partition chromatography (CPC) from an extract of Sinomenium acutum rhizome, which has shown promising preventive effects in a dexamethasone-induced C2C12 myotube atrophy model. CPC was operated with a solvent system of n-butanol–acetonitrile–water (10:2:8, v/v/v, containing 0.5% triethylamine) in dual mode (ascending to descending), which provided a high recovery rate (>99%) with a high resolution. Then, the preventive effects of the obtained CPC fractions were examined against dexamethasone-induced atrophy in C2C12 myotubes according to the weight ratios of the obtained fractions. The active fractions were further purified by semi-preparative HPLC that led to obtaining five alkaloids, one lignan glycoside, and one phenylpropanoid glycoside. Among these, at a concentration of 1 nM, sinomenine, magnoflorine, and acutumine could ameliorate dexamethasone-induced myotube atrophy in C2C12 myotubes by 9.3%, 13.8%, and 11.3%, respectively. Full article
(This article belongs to the Special Issue Separation, Analysis and Biological Evaluation of Bioactive Compounds)
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13 pages, 3014 KiB  
Article
Isolation of Osteoblastic Differentiation-Inducing Constituents from Peanut Sprouts and Development of Optimal Extraction Method
by Eun-Sang Cho, Chung Hyeon Lee, Min Sung Ko, Jee Yeon Choi, Kwang Woo Hwang and So-Young Park
Separations 2023, 10(8), 435; https://doi.org/10.3390/separations10080435 - 1 Aug 2023
Viewed by 1234
Abstract
Osteoporosis, one of the most common bone diseases, results from an imbalance between bone formation and resorption. Osteoblasts are primarily involved in bone formation, whereas osteoclasts are involved in bone resorption. Therefore, any substances that can increase osteoblastic differentiation would be beneficial for [...] Read more.
Osteoporosis, one of the most common bone diseases, results from an imbalance between bone formation and resorption. Osteoblasts are primarily involved in bone formation, whereas osteoclasts are involved in bone resorption. Therefore, any substances that can increase osteoblastic differentiation would be beneficial for the prevention or treatment of osteoporosis. In this study, peanut sprouts, a germinated product of peanuts, significantly enhanced osteoblastic differentiation of pre-osteoblastic MC3T3-E1 cells, as determined by the alkaline phosphatase (ALP) assay. The ethyl acetate fraction of peanut sprout extract was subjected to diverse column chromatographies using silica gel, ODS, and Sephadex LH-20 as stationary phases, and three nucleobases, namely, adenine, uracil, and thymine, and three phenolic acids, including caffeic acid, coumaric acid, and ferulic acid, were isolated as active constituents. In particular, adenine at 4 μg/mL and caffeic acid at 1 μg/mL increased ALP activity by 40 and 30%, respectively, compared with the osteoblastic differentiation medium-treated group, and these two compounds were set as marker compounds. Furthermore, extraction of peanut sprouts grown for 14–17 days with 60% ethanol was the best condition to obtain a high quantity of extract for peanut sprouts by analyzing the contents of marker compounds through HPLC. Together, these results suggest that peanut sprouts and their isolated compounds significantly enhance osteoblastic differentiation. Therefore, peanut sprouts have the potential to be developed as functional foods against osteoporosis. Full article
(This article belongs to the Special Issue Separation, Analysis and Biological Evaluation of Bioactive Compounds)
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19 pages, 1119 KiB  
Article
Phytochemical Profile, Antioxidant Activity and Cholinesterase Inhibition Potential of Essential Oil and Extracts of Teucrium montanum from Bosnia and Herzegovina
by Mejra Bektasevic, Mladenka Jurin, Marin Roje and Olivera Politeo
Separations 2023, 10(8), 421; https://doi.org/10.3390/separations10080421 - 26 Jul 2023
Cited by 9 | Viewed by 2387
Abstract
Bioactive compounds from plants play an important role in slowing many neurodegenerative diseases, such as Alzheimer’s disease, by inhibiting cholinesterase enzymes. Studies have shown that oxidative stress is associated with the development of Alzheimer’s disease. In traditional medicine of Bosnia and Herzegovina, Teucrium [...] Read more.
Bioactive compounds from plants play an important role in slowing many neurodegenerative diseases, such as Alzheimer’s disease, by inhibiting cholinesterase enzymes. Studies have shown that oxidative stress is associated with the development of Alzheimer’s disease. In traditional medicine of Bosnia and Herzegovina, Teucrium montanum is used to treat numerous diseases. The chemical composition and biological activity of the essential oil (EO) and aqueous (AE) and methanol extract (ME) of this plant were studied. The chemical composition of EO was studied using GC-MS, while the composition of the extracts was studied using HPLC-DAD. Antioxidant activity was tested using the DPPH and FRAP methods. The protection of lipids and proteins from oxidation was tested using the ammonium thiocyanate and BSA oxidation methods. The ability to inhibit cholinesterases was tested by the Ellman method. The main identified EO compounds were α-cadinol, ß-selinene, δ-cadinene, epi-α-cadinol, germacrene D-4-ol, and α-pinene. The main phenolic compounds of the extracts were p-coumaric acid, ellagic acid and caffeic acid. The tested extracts showed good antioxidant radical scavenging and reducing potential and a very good ability to protect lipids and proteins from oxidation. The EO showed moderate AChE and BChE inhibition potential, while the extracts showed weak or no ability. Full article
(This article belongs to the Special Issue Separation, Analysis and Biological Evaluation of Bioactive Compounds)
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17 pages, 3709 KiB  
Article
Bacterial Endophytes from Moringa oleifera Leaves as a Promising Source for Bioactive Compounds
by Amr H. Hashem, Abdulaziz A. Al-Askar, Hamada Abd Elgawad and Amer M. Abdelaziz
Separations 2023, 10(7), 395; https://doi.org/10.3390/separations10070395 - 6 Jul 2023
Cited by 9 | Viewed by 2636
Abstract
Bacterial endophytes reside within the tissues of living plant species without causing any harm or disease to their hosts. Bacterial endophytes have produced a variety of bioactive compounds that can be used for different biomedical applications. In the current study, two bacterial endophytes [...] Read more.
Bacterial endophytes reside within the tissues of living plant species without causing any harm or disease to their hosts. Bacterial endophytes have produced a variety of bioactive compounds that can be used for different biomedical applications. In the current study, two bacterial endophytes were isolated from healthy Moringa oleifera leaves, and identified genetically as Stenotrophomonas maltophilia and Alcaligenes faecalis. Phytochemical results illustrated that A. faecalis produced phenolics at 547.2 mg/g, tannins at 156.7 µg/g, flavonoids at 32.8 µg/g, and alkaloids at 111.2 µg/g compared to S. maltophilia, which produced phenolics at 299.5 mg/g, tannins at 78.2 µg/g, flavonoids at 12.4 µg/g, and alkaloids at 29.4 µg/g. GC-MS analysis indicated that A. faecalis extract has 24 bioactive compounds, including 9 major compounds, namely octadecanoic acid, hexadecanoic acid, linoleic acid ethyl ester, octadecenoic acid, methyl ester, methyl stearate, nonacosane, indolizine, palmitoleic acid, and heptacosane. On the other hand, S. maltophilia extract has 11 bioactive compounds, including 8 major compounds, namely oleic acid, octadecanoic acid, hexadecanoic acid, cis-2-phenyl-1, 3-dioxolane-4-methyl, ergotamine, diisooctyl phthalate, diethyl phthalate, and pentadecanoic acid. To check the safety of these extracts, the cytotoxicity of Ethyl acetate (EA) extracts of S. maltophilia and A. faecalis were evaluated against the Vero normal cell line, and the results confirmed that these extracts are safe to use. Moreover, results revealed that EA extracts of S. maltophilia and A. faecalis exhibited anticancer activity against the cancerous MCF7 cell line, where IC50 was 202.4 and 119.7 µg/mL, respectively. Furthermore, EA extracts of S. maltophilia had antibacterial and antifungal activity against Gram-positive and Gram-negative bacteria, and unicellular fungi. Likewise, the EA extract of A. faecalis exhibited antibacterial and antifungal activity against Gram-positive bacteria, as well as unicellular fungi, but did not show any activity against Gram-negative bacteria. Also, EA extracts of S. maltophilia and A. faecalis exhibited moderate antioxidant activity where IC50 were 146.2 and 147.6 µg/mL, respectively. In conclusion, the two isolated endophytic bacteria S. maltophilia and A. faecalis have promising bioactive compounds that have antibacterial, antioxidant, and anticancer activities. Full article
(This article belongs to the Special Issue Separation, Analysis and Biological Evaluation of Bioactive Compounds)
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21 pages, 10936 KiB  
Article
Biosynthesized ZnO-NPs Using Sea Cucumber (Holothuria impatiens): Antimicrobial Potential, Insecticidal Activity and In Vivo Toxicity in Nile Tilapia Fish, Oreochromis niloticus
by Mostafa A. Elbahnasawy, Hussein A. El-Naggar, Ibrahim E. Abd-El Rahman, Mohamed H. Kalaba, Saad A. Moghannem, Fatimah Al-Otibi, Reham M. Alahmadi, Othman F. Abdelzaher, Mohamed M. Mabrouk, Ahmed G. A. Gewida, Marwa F. AbdEl-Kader and Ahmed I. Hasaballah
Separations 2023, 10(3), 173; https://doi.org/10.3390/separations10030173 - 3 Mar 2023
Cited by 6 | Viewed by 2162
Abstract
In this study, a sustainable and eco-friendly method was used to prepare zinc oxide nanoparticles (ZnO-NPs) using a sea cucumber aqueous extract. Then, ZnO-NPs were characterized by instrumental analysis (UV-vis, HR-TEM, XRD, FT-IR, and DLS) and evaluated for their possible antibacterial, antifungal, and [...] Read more.
In this study, a sustainable and eco-friendly method was used to prepare zinc oxide nanoparticles (ZnO-NPs) using a sea cucumber aqueous extract. Then, ZnO-NPs were characterized by instrumental analysis (UV-vis, HR-TEM, XRD, FT-IR, and DLS) and evaluated for their possible antibacterial, antifungal, and insecticidal activities. Additionally, the toxicity of ZnO-NPs was evaluated in vivo against Nile Tilapia (Oreochromis niloticus). The sea cucumber was collected from the Gulf of Suez (Red Sea) at Al-Ain Al-Sokhna coast in Egypt and identified as Holothuria impatiens. The prepared Hi-ZnO-NPs peaked at 350 nm in UV–Vis spectral analysis. They showed quasi-spherical shaped particles with sizes ranging from 13 nm to 47 nm and a predominate size of 26 nm as indicated by HR-TEM. The XRD pattern of Hi-ZnO-NPs revealed a crystalline phase with an average size of 17.2 nm as calculated by Debye–Scherrer equation. FTIR analysis revealed the possible role of H. impatiens biological molecules in the biosynthesis process of ZnO-NPs. Hi-ZnO-NPs showed a negative zeta potential of −19.6 mV, demonstrating moderate stability. Biosynthesized Hi-ZnO-NPs revealed broad antimicrobial activity against Gram-positive bacteria (S. aureus ATCC 25923 and E. feacalis), Gram-negative bacteria (S. typhi, K. pneumonia and E. coli), and filamentous fungi (Aspergillus niger). Hi-ZnO-NPs demonstrated larvicidal activity against the mosquito, Culex pipiens (LC50 = 2.756 ppm and LC90 = 9.294 ppm), and adulticidal action against the housefly, Musca domestica (LD50 = 4.285 ppm and LD90 = 22.847 ppm). Interestingly, Hi-ZnO-NPs did not show mortality effects against Nile tilapia fish (Oreochromis niloticus), highlighting the potential safety of Hi-ZnO-NPs to highly exposed, non-target organisms. However, histopathological and hematological investigations provided dose-dependent impacts of Hi-ZnO-NPs to Nile tilapia. Overall, data provide an eco-friendly approach for synthesizing novel Hi-ZnO-NPs with multiple biomedical properties and potentially low toxicity to Nile tilapia fish. Full article
(This article belongs to the Special Issue Separation, Analysis and Biological Evaluation of Bioactive Compounds)
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