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Bioactive Compounds from Natural Sources II

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (10 January 2023) | Viewed by 35452

Special Issue Editors


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Guest Editor
Plant Production and Processing, University of Applied Sciences Weihenstephan-Triesdorf, Markgrafenstr 16, 91746 Weidenbach, Germany
Interests: food biotechnology; innovative food; bio-active compounds; antioxidants
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Plant Biology, Institute Biology and Medicine, Taras Shevchenko National University of Kyiv, 01033 Kyiv, Ukraine
Interests: secondary metabolites; phenolics; novel compounds; applied research
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In recent decades, there has been a huge interest in bio-active compounds from natural sources. Plant biodiversity proposes a big quantity of bio-active compounds. Bio-active compounds are mostly some specific secondary metabolites with antioxidant, inflammatory, immunomodulative potential, antimicrobial property, etc. The bioactive compounds of classes of terpenes, flavonoids, alkaloids, coumarins, stilbenes, etc. alongside the description of some of their mechanisms of action are important to study. It is important to admit that the use of plant extracts complicates the identification of effects of antiviral, antimicrobial or other capacities of separate biologically active compounds, the effects of activities of solute compounds in extracts can be additive (the synergistic effect) or an antagonistic effect can come into play. In that context, the current issue is open for scientific research on the description of novel isolated bio-active compounds, as well as some of their unknown effects, which are a priority for the applied needs of humans in different areas of life. Due to strong interest in the current topic in the previous Special Issue, we continue to collect unique and interesting research works connected with plant natural compounds and their biological effects.

Prof. Dr. Iryna Smetanska
Dr. Oksana Sytar
Guest Editors

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Keywords

  • secondary metabolites
  • bio-active compounds
  • plant biotechnology
  • innovative food
  • plant natural resources

Published Papers (16 papers)

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Editorial

Jump to: Research, Review

4 pages, 193 KiB  
Editorial
Special Issue—“Bioactive Compounds from Natural Sources II”
by Oksana Sytar and Iryna Smetanska
Molecules 2023, 28(11), 4450; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28114450 - 31 May 2023
Viewed by 840
Abstract
In recent decades, there has been a great interest in bioactive compounds from natural sources [...] Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)

Research

Jump to: Editorial, Review

22 pages, 3815 KiB  
Article
Unravelling Novel Phytochemicals and Anticholinesterase Activity in Irish Cladonia portentosa
by Shipra Nagar, Maria Pigott, Wirginia Kukula-Koch and Helen Sheridan
Molecules 2023, 28(10), 4145; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28104145 - 17 May 2023
Cited by 3 | Viewed by 1337
Abstract
Acetylcholinesterase inhibitors remain the mainstay of symptomatic treatment for Alzheimer’s disease. The natural world is rich in acetylcholinesterase inhibitory molecules, and research efforts to identify novel leads is ongoing. Cladonia portentosa, commonly known as reindeer lichen, is an abundant lichen species found [...] Read more.
Acetylcholinesterase inhibitors remain the mainstay of symptomatic treatment for Alzheimer’s disease. The natural world is rich in acetylcholinesterase inhibitory molecules, and research efforts to identify novel leads is ongoing. Cladonia portentosa, commonly known as reindeer lichen, is an abundant lichen species found in Irish Boglands. The methanol extract of Irish C. portentosa was identified as an acetylcholinesterase inhibitory lead using qualitative TLC-bioautography in a screening program. To identify the active components, the extract was deconvoluted using a successive extraction process with hexane, ethyl acetate and methanol to isolate the active fraction. The hexane extract demonstrated the highest inhibitory activity and was selected for further phytochemical investigations. Olivetolic acid, 4-O-methylolivetolcarboxylic acid, perlatolic acid and usnic acid were isolated and characterized using ESI-MS and two-dimensional NMR techniques. LC-MS analysis also determined the presence of the additional usnic acid derivatives, placodiolic and pseudoplacodiolic acids. Assays of the isolated components confirmed that the observed anticholinesterase activity of C. portentosa can be attributed to usnic acid (25% inhibition at 125 µM) and perlatolic acid (20% inhibition at 250 µM), which were both reported inhibitors. This is the first report of isolation of olivetolic and 4-O-methylolivetolcarboxylic acids and the identification of placodiolic and pseudoplacodiolic acids from C. portentosa. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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9 pages, 1021 KiB  
Communication
Geobarrettin D, a Rare Herbipoline-Containing 6-Bromoindole Alkaloid from Geodia barretti
by Xiaxia Di, Ingibjorg Hardardottir, Jona Freysdottir, Dongdong Wang, Kirk R. Gustafson, Sesselja Omarsdottir and Tadeusz F. Molinski
Molecules 2023, 28(7), 2937; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28072937 - 24 Mar 2023
Cited by 2 | Viewed by 1586
Abstract
Geobarrettin D (1), a new bromoindole alkaloid, was isolated from the marine sponge Geodia barretti collected from Icelandic waters. Its structure was elucidated by 1D, and 2D NMR (including 1H-15N HSQC, 1H-15N HMBC spectra), as [...] Read more.
Geobarrettin D (1), a new bromoindole alkaloid, was isolated from the marine sponge Geodia barretti collected from Icelandic waters. Its structure was elucidated by 1D, and 2D NMR (including 1H-15N HSQC, 1H-15N HMBC spectra), as well as HRESIMS data. Geobarrettin D (1) is a new 6-bromoindole featuring an unusual purinium herbipoline moiety. Geobarrettin D (1) decreased secretion of the pro-inflammatory cytokine IL-12p40 by human monocyte derived dendritic cells, without affecting secretion of the anti-inflammatory cytokine IL-10. Thus, compound 1 shows anti-inflammatory activity. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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10 pages, 1080 KiB  
Article
Novel Indane Derivatives with Antioxidant Activity from the Roots of Anisodus tanguticus
by Chun-Wang Meng, Hao-Yu Zhao, Huan Zhu, Cheng Peng, Qin-Mei Zhou and Liang Xiong
Molecules 2023, 28(3), 1493; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28031493 - 03 Feb 2023
Cited by 5 | Viewed by 1419
Abstract
Four novel indane derivatives, anisotindans A–D (14), were isolated from the roots of Anisodus tanguticus. Their structures were established using comprehensive spectroscopic analyses, and their absolute configurations were determined by electronic circular dichroism (ECD) calculations and single-crystal X-ray [...] Read more.
Four novel indane derivatives, anisotindans A–D (14), were isolated from the roots of Anisodus tanguticus. Their structures were established using comprehensive spectroscopic analyses, and their absolute configurations were determined by electronic circular dichroism (ECD) calculations and single-crystal X-ray diffraction analyses. Anisotindans C and D (3 and 4) are two unusual indenofuran analogs. ABTS•+ and DPPH•+ assays of radical scavenging activity reveal that all compounds (14) are active. Specifically, the ABTS•+ assay results show that anisotindan A (1) exhibits the best antioxidant activity with an IC50 value of 15.62 ± 1.85 μM (vitamin C, IC50 = 22.54 ± 5.18 μM). Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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19 pages, 3843 KiB  
Article
Identifying the Anti-MERS-CoV and Anti-HcoV-229E Potential Drugs from the Ginkgo biloba Leaves Extract and Its Eco-Friendly Synthesis of Silver Nanoparticles
by Ezzat H. Elshazly, Alyaa Nasr, Mohamed E. Elnosary, Gamal A. Gouda, Hassan Mohamed and Yuanda Song
Molecules 2023, 28(3), 1375; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28031375 - 01 Feb 2023
Cited by 8 | Viewed by 2371
Abstract
The present study aimed to estimate the antiviral activities of Ginkgo biloba (GB) leaves extract and eco-friendly free silver nanoparticles (Ag NPs) against the MERS-CoV (Middle East respiratory syndrome-coronavirus) and HCoV-229E (human coronavirus 229E), as well as isolation and identification of phytochemicals from [...] Read more.
The present study aimed to estimate the antiviral activities of Ginkgo biloba (GB) leaves extract and eco-friendly free silver nanoparticles (Ag NPs) against the MERS-CoV (Middle East respiratory syndrome-coronavirus) and HCoV-229E (human coronavirus 229E), as well as isolation and identification of phytochemicals from GB. Different solvents and high-performance liquid chromatography (HPLC) were used to extract and identify flavonoids and phenolic compounds from GB leaves. The green, silver nanoparticle synthesis was synthesized from GB leaves aqueous extract and investigated for their possible effects as anti-coronaviruses MERS-CoV and HCoV-229E using MTT assay protocol. To verify the synthesis of Ag NPs, several techniques were employed, including X-ray diffraction (XRD), scan, transmission electron microscopy, FT-IR, and UV–visible spectroscopy. The highest contents of flavonoids and phenolic compounds were recorded for acetone, methanol, and ethanol as mixtures with water, in addition to pure water. HPLC flavonoids were detected as apegenin, luteolin, myricetin, and catechin, while HPLC phenolic compounds were pyrogallol, caffeic acid, gallic acid, and ellagic acid. In addition, our results revealed that Ag NPs were produced through the shift from yellow to dark brown. TEM examination of Ag NPs revealed spherical nanoparticles with mean sizes ranging from 5.46 to 19.40 nm and an average particle diameter of 11.81 nm. A UV–visible spectrophotometric investigation revealed an absorption peak at λ max of 441.56 nm. MTT protocol signified the use of GB leaves extract as an anti-coronavirus to be best from Ag NPs because GB extract had moderate anti-MERS-CoV with SI = 8.94, while had promising anti-HCov-229E, with an SI of 21.71. On the other hand, Ag NPs had a mild anti-MERS-CoV with SI = 4.23, and a moderate anti-HCoV-229E, with an SI of 7.51. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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12 pages, 326 KiB  
Article
Effects of Sonication and Thermal Pasteurization on the Nutritional, Antioxidant, and Microbial Properties of Noni Juice
by Yi Xuan Choo, Lai Kuan Teh and Chin Xuan Tan
Molecules 2023, 28(1), 313; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28010313 - 30 Dec 2022
Cited by 6 | Viewed by 2089
Abstract
Sonication is recognized as a potential food processing method to improve the functional properties of fruit juice. This study evaluated the effects of different sonication durations (20, 40, and 60 min) and thermal pasteurization on the nutritional, antioxidant, and microbial properties of noni [...] Read more.
Sonication is recognized as a potential food processing method to improve the functional properties of fruit juice. This study evaluated the effects of different sonication durations (20, 40, and 60 min) and thermal pasteurization on the nutritional, antioxidant, and microbial properties of noni juice. Fresh noni juice served as the control. The main organic acids detected were malic (57.54–89.31 mg/100 mL) and ascorbic (17.15–31.55 mg/100 mL) acids. Compared with the fresh sample, the concentrations of these compounds were significantly improved (p < 0.05) in the 60 min sonicated sample but reduced (p < 0.05) in the pasteurized sample. Moreover, sonication for 60 min resulted in increments of scopoletin, rutin, and vanillic acid compared to the fresh sample. The antioxidant activity of the juice sample was improved in the sample sonicated for 60 min. Irrespective of juice processing method, the level of microbial counts in noni juice was within the satisfactory level over the 8 weeks of refrigerated (4 °C) storage. This study highlights the feasibility of using ultrasound processing to enhance the quality of noni juice on the industrial scale. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
11 pages, 1316 KiB  
Article
Assessing the Quality of Burkina Faso Soybeans Based on Fatty Acid Composition and Pesticide Residue Contamination
by Elisabeth Rakiswendé Ouédraogo, Kiessoun Konaté, Abdoudramane Sanou, Hemayoro Sama, Ella Wendinpuikondo Rakèta Compaoré, Oksana Sytar, Adama Hilou, Marian Brestic and Mamoudou Hama Dicko
Molecules 2022, 27(19), 6260; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27196260 - 23 Sep 2022
Cited by 2 | Viewed by 1609
Abstract
Soybean is widely used in the food industry because of its high fatty acid and protein content. However, the increased use of pesticides to control pests during cultivation, in addition to being a public health concern, may influence the nutritional quality of soybeans. [...] Read more.
Soybean is widely used in the food industry because of its high fatty acid and protein content. However, the increased use of pesticides to control pests during cultivation, in addition to being a public health concern, may influence the nutritional quality of soybeans. This study aimed to assess the nutritional quality of soybeans with respect to fatty acid profile and pesticide residue contamination. The levels of fatty acids and pesticides in soybean varieties G196 and G197 were determined by gas chromatography and by the QuEChERS method, respectively. The results showed a significant variation in the quantitative and qualitative fatty acid composition of the two varieties, with 18.03 g/100 g and 4 fatty acids detected for the G196 variety and 21.35 g/100 g and 7 fatty acids for the G197 variety, respectively. In addition, 12 active pesticide compounds were found, and among them, imazalil, quintozene, cyfluthrin and lindane exceeded their maximum limits. The G197 variety had a better nutritional profile compared to G196. The profile of fatty acids and the content of pesticide residues were used as important determinants for soybean utilization in human nutrition. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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12 pages, 2239 KiB  
Article
Identification of Novel Natural Inhibitors to Human 3-Phosphoglycerate Dehydrogenase (PHGDH) for Cancer Treatment
by Ayesha Sadiqa, Azhar Rasul, Mudassir Hassan, Salma Sultana and Farhat Jabeen
Molecules 2022, 27(18), 6108; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27186108 - 19 Sep 2022
Cited by 3 | Viewed by 1978
Abstract
Targeting the serine biosynthesis pathway enzymes has turned up as a novel strategy for anti-cancer therapeutics. 3- Phosphoglycerate dehydrogenase (PHGDH) is the rate-limiting enzyme that catalyzes the conversion of 3-Phosphoglyceric acid (3-PG) into 3-Phosphohydroxy pyruvate (3-PPyr) in the first step of serine synthesis [...] Read more.
Targeting the serine biosynthesis pathway enzymes has turned up as a novel strategy for anti-cancer therapeutics. 3- Phosphoglycerate dehydrogenase (PHGDH) is the rate-limiting enzyme that catalyzes the conversion of 3-Phosphoglyceric acid (3-PG) into 3-Phosphohydroxy pyruvate (3-PPyr) in the first step of serine synthesis pathway and perform a critical role in cancer progression. PHGDH has been reported to be overexpressed in different types of cancers and emerged as a novel target for cancer therapeutics. During this study, virtual screening tools were used for the identification of inhibitors of PHGDH. A library of phenolic compounds was docked against two binding sites of PHGDH using Molegro Virtual Docker (MVD) software. Out of 169 virtually tested compounds, Salvianolic acid C and Schizotenuin F possess good binding potential to co-factor binding site of PHGDH while Salvianolic acid I and Chicoric acid were identified as the best binding compounds toward the substrate binding site of PHGDH. The top selected compounds were evaluated for different physiochemical and ADMET properties, the obtained results showed that none of these hit compounds violated the Pfizer Rule and they possess acceptable ADMET profiles. Further, a commercially available hit compound, Chicoric acid, was evaluated for its anti-cancer potential against PHGDH-expressing gastric cancer cell lines (MGC-803 and SGC-7901) as well as cell lines with low expression of PHGDH (MCF-7 and MDA-MB2-31), which demonstrated that Chicoric acid possesses selective cytotoxicity toward PHGDH expressing cancer cell lines. Thus, this study has unveiled the potential of phenolic compounds, which could serve as novel candidates for the development of PHGDH inhibitors as anti-cancer agents. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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15 pages, 3869 KiB  
Article
Coumarinolignans with Reactive Oxygen Species (ROS) and NF-κB Inhibitory Activities from the Roots of Waltheria indica
by Feifei Liu, Sudipta Mallick, Timothy J. O’Donnell, Ruxianguli Rouzimaimaiti, Yuheng Luo, Rui Sun, Marisa Wall, Supakit Wongwiwatthananukit, Abhijit Date, Dane Kaohelani Silva, Philip G. Williams and Leng Chee Chang
Molecules 2022, 27(10), 3270; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27103270 - 19 May 2022
Cited by 3 | Viewed by 1567
Abstract
Seven new coumarinolignans, walthindicins A–F (1a, 1b, 25, 7), along with five known analogs (6, 811), were isolated from the roots of Waltheria indica. The structures of the new compounds [...] Read more.
Seven new coumarinolignans, walthindicins A–F (1a, 1b, 25, 7), along with five known analogs (6, 811), were isolated from the roots of Waltheria indica. The structures of the new compounds are determined by detailed nuclear magnetic resonance (NMR), circular dichroism (CD) with extensive computational support, and mass spectroscopic data interpretation. Compounds were tested for their antioxidant activity in Human Cervical Cancer cells (HeLa cells). Compounds 1a and 6 showed higher reactive oxygen species (ROS) inhibitory activity at 20 μg/mL when compared with other natural compound-based antioxidants such as ascorbic acid. Considering the role of ROS in nuclear-factor kappa B (NF-κB) activation, compounds 1a and 6 were evaluated for NF-κB inhibitory activity and showed a concentration-dependent inhibition in Human Embryonic Kidney 293 cells (Luc-HEK-293). Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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18 pages, 5067 KiB  
Article
Anticancer, Anticoagulant, Antioxidant and Antimicrobial Activities of Thevetia peruviana Latex with Molecular Docking of Antimicrobial and Anticancer Activities
by Aisha M. H. Al-Rajhi, Reham Yahya, Tarek M. Abdelghany, Mohamed A. Fareid, Alawlaqi M. Mohamed, Basma H. Amin and Abdurrahman S. Masrahi
Molecules 2022, 27(10), 3165; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27103165 - 16 May 2022
Cited by 25 | Viewed by 3336
Abstract
Natural origin molecules represent reliable and excellent sources to overcome some medicinal problems. The study of anticancer, anticoagulant, and antimicrobial activities of Thevetia peruviana latex were the aim of the current research. An investigation using high-performance liquid chromatography (HPLC) revealed that the major [...] Read more.
Natural origin molecules represent reliable and excellent sources to overcome some medicinal problems. The study of anticancer, anticoagulant, and antimicrobial activities of Thevetia peruviana latex were the aim of the current research. An investigation using high-performance liquid chromatography (HPLC) revealed that the major content of the flavonoids are rutin (11.45 µg/mL), quersestin (7.15 µg/mL), naringin (5.25 µg/mL), and hisperdin (6.07 µg/mL), while phenolic had chlorogenic (12.39 µg/mL), syringenic (7.45 µg/mL), and ferulic (5.07 µg/mL) acids in latex of T. peruviana. Via 1,1-diphenyl-2- picrylhydrazyl (DPPH) radical scavenging, the experiment demonstrated that latex had a potent antioxidant activity with the IC50 43.9 µg/mL for scavenging DPPH. Hemolysis inhibition was 58.5% at 1000 µg/mL of latex compared with 91.0% at 200 µg/mL of indomethacin as positive control. Negligible anticoagulant properties of latex were reported where the recorded time was 11.9 s of prothrombin time (PT) and 29.2 s of the activated partial thromboplastin time (APTT) at 25 µg/mL, compared with the same concentration of heparin (PT 94.6 s and APPT 117.7 s). The anticancer potential of latex was recorded against PC-3 (97.11% toxicity) and MCF-7 (96.23% toxicity) at 1000 μg/mL with IC50 48.26 μg/mL and 40.31 µg/mL, respectively. Disc diffusion assessment for antimicrobial activity recorded that the most sensitive tested microorganisms to latex were Bacillus subtilis followed by Escherichia coli, with an inhibition zone (IZ) of 31 mm with minimum inhibitory concentration (MIC) (10.2 μg/mL) and 30 mm (MIC, 12.51 μg/mL), respectively. Moreover, Candida albicans was sensitive (IZ, 28 mm) to latex, unlike black fungus (Mucor circinelloides). TEM examination exhibited ultrastructure changes in cell walls and cell membranes of Staphylococcus aureus and Pseudomonas aeruginosa treated with latex. Energy scores of the molecular docking of chlorogenic acid with E. coli DNA (7C7N), and Rutin with human prostate-specific antigen (3QUM) and breast cancer-associated protein (1JNX), result in excellent harmony with the experimental results. The outcome of research recommended that the latex is rich in constituents and considered a promising source that contributes to fighting cancer and pathogenic microorganisms. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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15 pages, 7923 KiB  
Article
Rutin Promotes Pancreatic Cancer Cell Apoptosis by Upregulating miRNA-877-3p Expression
by Mingxing Huo, Aowen Xia, Wenwen Cheng, Mengjie Zhou, Jiankang Wang, Tiantian Shi, Cifeng Cai, Wenqi Jin, Meiliang Zhou, Yueling Liao and Zhiyong Liao
Molecules 2022, 27(7), 2293; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27072293 - 31 Mar 2022
Cited by 9 | Viewed by 2343
Abstract
(1) Background: pancreatic cancer is one of the most serious cancers due to its rapid and inevitable fatality, which has been proved very difficult to treat, compared with many other common cancers. Thus, developing an effective therapeutic strategy, especially searching for potential drugs, [...] Read more.
(1) Background: pancreatic cancer is one of the most serious cancers due to its rapid and inevitable fatality, which has been proved very difficult to treat, compared with many other common cancers. Thus, developing an effective therapeutic strategy, especially searching for potential drugs, is the focus of current research. The exact mechanism of rutin in pancreatic cancer remains unknown. (2) Method: three pancreatic cancer cell lines were used to study the anti-pancreatic cancer effect of rutin. The potent anti-proliferative, anti-migration and pro-apoptotic properties of rutin were uncovered by cell viability, a wound-healing migration assay, and a cell apoptosis assay. High-throughput sequencing technology was used to detect the change of miRNAs expression. Immunoblotting analysis was used to detect the expression of apoptotic proteins. (3) Results: CCK-8 and EDU assays revealed that rutin significantly inhibited pancreatic cancer cells’ proliferation (p < 0.05). A wound-healing assay showed that rutin significantly suppressed pancreatic cancer cells’ migration (p < 0.05). A flow cytometric assay showed that rutin could promote pancreatic cancer cells’ apoptosis. Intriguingly, rutin significantly upregulated miR-877-3p expression to repress the transcription of Bcl-2 and to induce pancreatic cancer cell apoptosis. Accordingly, rutin and miR-877-3p mimics could promote apoptotic protein expression. (4) Conclusions: our findings indicate that rutin plays an important role in anti-pancreatic cancer effects through a rutin-miR-877-3p-Bcl-2 axis and suggests a potential therapeutic strategy for pancreatic cancer. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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20 pages, 5974 KiB  
Article
Anatomical and Phytochemical Characteristics of Different Parts of Hypericum scabrum L. Extracts, Essential Oils, and Their Antimicrobial Potential
by Kubra Nalkiran Ergin, Songul Karakaya, Gamze Göger, Oksana Sytar, Betul Demirci and Hayri Duman
Molecules 2022, 27(4), 1228; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27041228 - 11 Feb 2022
Cited by 11 | Viewed by 2493
Abstract
Hypericum (Hypericaceae) is a genus that comprises a high number of species around the world. In this study, the roots, aerial parts, flowers, fruits, and aerial parts with flowers from Hypericum scabrum were macerated separately by methanol and water and then fractionated by [...] Read more.
Hypericum (Hypericaceae) is a genus that comprises a high number of species around the world. In this study, the roots, aerial parts, flowers, fruits, and aerial parts with flowers from Hypericum scabrum were macerated separately by methanol and water and then fractionated by different solvents of, such as ethyl acetate, n-hexane, butanol, dichloromethane, aqueous residue sub-extracts, and ethnobotanical use. All the extracts, sub-extracts and essential oils of H. scabrum were investigated for the first time in detail for their antimicrobial, total phenolics, and antioxidant activities. Anatomical structures of the root, stem, leaf, upper and lower leaf surface, stamen, sepal, and petal of H. scabrum were examined. The biochemical layout of essential oils was determined by GC and GC/MS. The antioxidant activity was determined by free radical scavenging activity (by DPPH). Antimicrobial activity was applied against Candida albicans ATCC 10231, Escherichia coli ATCC 8739, Staphylococcus aureus ATCC 6538, Bacillus subtilis ATCC 19659, and C. tropicalis ATCC 750 using microdilution methods. The essentials of the aerial parts, flower, and fruit are characterized by the presence of monoterpene hydrocarbons, whereas roots oil include alkanes. The GC-FID and GC-MS analysis showed that major components of roots, aerial parts, flowers, and fruits oils were undecane (66.1%); α-pinene (17.5%), γ-terpinene (17.4%), and α-thujene (16.9%); α-pinene (55.6%), α-thujene (10.9%), and γ-terpinene (7.7%); α-pinene (85.2%), respectively. The aerial part sub-extracts indicated a greater level of total phenolics and antioxidant potential. The n-hexane sub-extracts (from aerial part, flower, and aerial part with flower) showed the best activity against B. subtilis, with 39.06 µg/mL MIC value. The presented research work indicates that H. scabrum can be a novel promising resource of natural antioxidant and antimicrobial compounds. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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Review

Jump to: Editorial, Research

18 pages, 2941 KiB  
Review
Comprehensive Review of Recent Advances in Chiral A-Ring Flavonoid Containing Compounds: Structure, Bioactivities, and Synthesis
by Changyue Zhang, Yanzhi Liu, Xiaojing Liu, Xiaochuan Chen and Ruijiao Chen
Molecules 2023, 28(1), 365; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28010365 - 02 Jan 2023
Cited by 4 | Viewed by 1869
Abstract
Flavonoids are a group of natural polyphenolic substances that are abundant in vegetables, fruits, grains, and tea. Chiral A-ring-containing flavonoids are an important group of natural flavonoid derivatives applicable in a wide range of biological activities such as, cytotoxic, anti-inflammatory, anti-microbial, antioxidant, and [...] Read more.
Flavonoids are a group of natural polyphenolic substances that are abundant in vegetables, fruits, grains, and tea. Chiral A-ring-containing flavonoids are an important group of natural flavonoid derivatives applicable in a wide range of biological activities such as, cytotoxic, anti-inflammatory, anti-microbial, antioxidant, and enzyme inhibition. The desirable development of chiral A-ring-containing flavonoids by isolation, semi-synthesis or total synthesis in a short duration proves their great value in medicinal chemistry research. In this review, the research progress of chiral A-ring-containing flavonoids, including isolation and extraction, structural identification, pharmacological activities, and synthetic methods, is comprehensively and systematically summarized. Furthermore, we provide suggestions for future research on the synthesis and biomedical applications of flavonoids. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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11 pages, 752 KiB  
Review
Molecular Shield for Protection of Buckwheat Plants from UV-B Radiation
by Ivan Kreft, Alena Vollmannová, Judita Lidiková, Janette Musilová, Mateja Germ, Aleksandra Golob, Blanka Vombergar, Darja Kocjan Ačko and Zlata Luthar
Molecules 2022, 27(17), 5577; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27175577 - 30 Aug 2022
Cited by 9 | Viewed by 2129
Abstract
Tartary buckwheat (Fagopyrum tataricum (L.) Gaertn.) and common buckwheat (Fagopyrum esculentum Moench) are adapted to growing in harsh conditions of high altitudes. Ultraviolet radiation at high altitudes strongly impacts plant growth and development. Under the influence of ultraviolet radiation, protecting substances [...] Read more.
Tartary buckwheat (Fagopyrum tataricum (L.) Gaertn.) and common buckwheat (Fagopyrum esculentum Moench) are adapted to growing in harsh conditions of high altitudes. Ultraviolet radiation at high altitudes strongly impacts plant growth and development. Under the influence of ultraviolet radiation, protecting substances are synthesized in plants. The synthesis of UV-B defense metabolites is genetically conditioned, and their quantity depends on the intensity of the ultraviolet radiation to which the plants and plant parts are exposed. These substances include flavonoids, and especially rutin. Other substances with aromatic rings of six carbon atoms have a similar function, including fagopyrin, the metabolite specific for buckwheat. Defensive substances are formed in the leaves and flowers of common and Tartary buckwheat, up to about the same concentration in both species. In comparison, the concentration of rutin in the grain of Tartary buckwheat is much higher than in common buckwheat. Flavonoids also have other functions in plants so that they can protect them from pests and diseases. After crushing the grains, rutin is exposed to contact with the molecules of rutin-degrading enzymes. In an environment with the necessary humidity, rutin is turned into bitter quercetin under the action of rutin-degrading enzymes. This bitterness has a deterrent effect against pests. Moreover, flavonoids have important functions in human nutrition to prevent several chronic diseases, including obesity, cardiovascular diseases, gallstone formation, and hypertension. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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25 pages, 3908 KiB  
Review
Bio-Active Compounds from Teucrium Plants Used in the Traditional Medicine of Kurdistan Region, Iraq
by Fuad O. Abdullah, Faiq H. S. Hussain, Abdullah Sh. Sardar, Gianluca Gilardoni, Zaw Min Thu and Giovanni Vidari
Molecules 2022, 27(10), 3116; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27103116 - 12 May 2022
Cited by 7 | Viewed by 2386
Abstract
Herbal medicine is still widely practiced in the Kurdistan Region, Iraq, especially by people living in villages in mountainous regions. Seven taxa belonging to the genus Teucrium (family Lamiaceae) are commonly employed in the Kurdish traditional medicine, especially to treat jaundice, stomachache and [...] Read more.
Herbal medicine is still widely practiced in the Kurdistan Region, Iraq, especially by people living in villages in mountainous regions. Seven taxa belonging to the genus Teucrium (family Lamiaceae) are commonly employed in the Kurdish traditional medicine, especially to treat jaundice, stomachache and abdominal problems. We report, in this paper, a comprehensive account about the chemical structures and bioactivities of most representative specialized metabolites isolated from these plants. These findings indicate that Teucrium plants used in the folk medicine of Iraqi Kurdistan are natural sources of specialized metabolites that are potentially beneficial to human health. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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31 pages, 5554 KiB  
Review
A Review on Mechanistic Insight of Plant Derived Anticancer Bioactive Phytocompounds and Their Structure Activity Relationship
by Kishor Mazumder, Asma Aktar, Priyanka Roy, Biswajit Biswas, Md. Emran Hossain, Kishore Kumar Sarkar, Sitesh Chandra Bachar, Firoj Ahmed, A. S. M. Monjur-Al-Hossain and Koichi Fukase
Molecules 2022, 27(9), 3036; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27093036 - 09 May 2022
Cited by 26 | Viewed by 4311
Abstract
Cancer is a disorder that rigorously affects the human population worldwide. There is a steady demand for new remedies to both treat and prevent this life-threatening sickness due to toxicities, drug resistance and therapeutic failures in current conventional therapies. Researchers around the world [...] Read more.
Cancer is a disorder that rigorously affects the human population worldwide. There is a steady demand for new remedies to both treat and prevent this life-threatening sickness due to toxicities, drug resistance and therapeutic failures in current conventional therapies. Researchers around the world are drawing their attention towards compounds of natural origin. For decades, human beings have been using the flora of the world as a source of cancer chemotherapeutic agents. Currently, clinically approved anticancer compounds are vincristine, vinblastine, taxanes, and podophyllotoxin, all of which come from natural sources. With the triumph of these compounds that have been developed into staple drug products for most cancer therapies, new technologies are now appearing to search for novel biomolecules with anticancer activities. Ellipticine, camptothecin, combretastatin, curcumin, homoharringtonine and others are plant derived bioactive phytocompounds with potential anticancer properties. Researchers have improved the field further through the use of advanced analytical chemistry and computational tools of analysis. The investigation of new strategies for administration such as nanotechnology may enable the development of the phytocompounds as drug products. These technologies have enhanced the anticancer potential of plant-derived drugs with the aim of site-directed drug delivery, enhanced bioavailability, and reduced toxicity. This review discusses mechanistic insights into anticancer compounds of natural origins and their structural activity relationships that make them targets for anticancer treatments. Full article
(This article belongs to the Special Issue Bioactive Compounds from Natural Sources II)
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