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Bioactive Natural Compounds for Pharmaceutical and Nutraceutical Applications
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Bioactive Natural Compounds for Pharmaceutical and Nutraceutical Applications

A special issue of Life (ISSN 2075-1729). This special issue belongs to the section "Plant Science".

Deadline for manuscript submissions: closed (30 August 2021) | Viewed by 22385

Special Issue Editor

Dr. Stefania Lamponi

E-Mail Website
Guest Editor
Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100 Siena, Italy
Interests: drug discovery; natural products; bioactive molecules; functional foods; nutraceuticals; in vitro biological tests; carriers for bioactive molecules; bioactivity
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

For a long time, plants have been widely used all over the world for their numerous properties, however, today, there is growing interest in the study of not only the classes of compounds obtained from plant species, but also from algae, fungi, and all biomass processing by-products, because of their specific activity, which allow their application for many selected therapeutic purposes, and they are able to respond to the demand for healthy ingredients and represent a natural way of preventing diseases.

The role of bioactive principles obtained from natural resources is closely related to their chemical structure, and the type and amount of different classes of molecules in natural extracts influence their bioactivity and consequently their use. The selection of appropriate extraction methods, and the phytochemical and biological activity characterization of novel classes of natural compounds have to be directed in order to select new compounds able to respond to the new therapeutics and nutraceuticals needs.

This Special Issue titled “Bioactive Natural Compounds for Pharmaceutical and Nutraceutical Applications” aims to collect original research papers and reviews in this field concerning the extraction, and phytochemical and biological characterization of new natural bioactive compounds obtained from natural resources for their potential applications as therapeutic and nutraceutical agents.

Dr. Stefania Lamponi
Guest Editor

Manuscript Submission Information

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Keywords

  • natural extracts
  • natural biomolecules
  • bioactivity
  • phytochemical analysis
  • nutraceuticals
  • biomass
  • functional matrices

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Published Papers (6 papers)

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Research

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14 pages, 5575 KiB  
Article
Insecticidal and Antifungal Activities of Chemically-Characterized Essential Oils from the Leaves of Withania frutescens L.
by El Moussaoui Abdelfattah, Allali Aimad, Mohammed Bourhia, Khalid Chebbac, Ahmad Mohammad Salamatullah, Walid Soufan, Hiba-Allah Nafidi, Mourad A. M. Aboul-Soud, Lahcen Ouahmane and Amina Bari
Life 2022, 12(1), 88; https://doi.org/10.3390/life12010088 - 8 Jan 2022
Cited by 19 | Viewed by 2243
Abstract
The current study was conducted to investigate antifungal and insecticidal activities of essential oil extracted from the Moroccan Withania frutescens L. (EOW), and their chemical composition was profiled. To achieve this goal, EOW was extracted by the hydro-distillation method and their phytochemical constituents [...] Read more.
The current study was conducted to investigate antifungal and insecticidal activities of essential oil extracted from the Moroccan Withania frutescens L. (EOW), and their chemical composition was profiled. To achieve this goal, EOW was extracted by the hydro-distillation method and their phytochemical constituents were characterized by gas chromatography-mass spectrometry analyses (GC-MS). Insecticidal activity was evaluated by use of four tests: contact toxicity, inhalation toxicity, and repellent tests. Antifungal activity was evaluated on Fusarium oxysporum f. sp. Ciceris (F. oxysporum) using different concentrations of EOW. GC/MS analysis revealed that EOW was rich in carvacrol (31.87%), thymol (30.08%), and camphor (9.13%). At a 1-µL/L dose, EOW exhibited mortality rates of 23.13 ± 1.07% and 24.41 ± 1.21% against Callosobruchus maculatus (C.maculatus) by inhalation and contact, respectively. Notably, EOW dose of 20 μL/L caused significant mortality rates of 95.1 ± 3.5% and 76.69 ± 1.71% by inhalation and contact, respectively. EOW exhibited an inhibitory effect on mycelial growth against the tested fungi F. oxysporum of 100% and 93.5 ± 1.1% for the 9 and 4.5 mg/mL doses, respectively. The reduced mycelial growth rate for F. oxysporum was recorded to be 0.3 ± 0.1 and 0.6 ± 0.1 mm/h for the EOW doses of 2.25 and 4.5 mg/mL, respectively. The outcome of the present work showed that EOW has a promising antifungal and insecticidal activity, and it can therefore be employed as a natural alternative insecticidal and mycocidal agent to replace the chemically-synthesized ones. Full article
(This article belongs to the Special Issue Bioactive Natural Compounds for Pharmaceutical and Nutraceutical Applications)
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18 pages, 2879 KiB  
Article
Inhibition of Non-Small Cell Lung Cancer Proliferation and Survival by Rosemary Extract Is Associated with Activation of ERK and AMPK
by Eric J. O’Neill, Jessy Moore, Joon Song and Evangelia Litsa Tsiani
Life 2022, 12(1), 52; https://doi.org/10.3390/life12010052 - 31 Dec 2021
Cited by 13 | Viewed by 3187
Abstract
Non-small cell lung cancer (NSCLC) represents an aggressive form of lung cancer which often develops resistance to chemo- and radiotherapy emphasizing a need to identify novel treatment agents to combat it. Many plants contain compounds with anti-inflammatory, antimicrobial, antidiabetic, and anticancer properties and [...] Read more.
Non-small cell lung cancer (NSCLC) represents an aggressive form of lung cancer which often develops resistance to chemo- and radiotherapy emphasizing a need to identify novel treatment agents to combat it. Many plants contain compounds with anti-inflammatory, antimicrobial, antidiabetic, and anticancer properties and some plant-derived chemicals are used in the treatment of cancer. A limited number of in vitro and in vivo animal studies provide evidence of anticancer effects of rosemary (Rosmarinus officinalis) extract (RE); however, no studies have explored its role in H1299 NSCLC cells, and its underlying mechanism(s) of action are not understood. The current study examined the effects of RE on H1299 cell proliferation, survival, and migration using specific assays. Additionally, immunoblotting was used to investigate the effects of RE treatment on signalling molecules implicated in cell growth and survival. Treatment with RE dose-dependently inhibited H1299 proliferation with an IC50 value of 19 µg/mL. Similarly, RE dose-dependently reduced cell survival, and this reduction correlated with increased levels of cleaved poly (ADP-ribose) polymerase (PARP), a marker of apoptosis. RE was also able to inhibit cell migration as assessed with a wound healing assay. These cellular effects of RE were associated with an increase in phosphorylated levels of extracellular signal-regulated kinase (ERK), AMP-activated protein kinase (AMPK), and its downstream targets ACC, the mTORC1 protein raptor, and decreased p70S6K phosphorylation. More studies are required to fully examine the effects of RE against NSCLC. Full article
(This article belongs to the Special Issue Bioactive Natural Compounds for Pharmaceutical and Nutraceutical Applications)
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12 pages, 2672 KiB  
Article
Gomisin L1, a Lignan Isolated from Schisandra Berries, Induces Apoptosis by Regulating NADPH Oxidase in Human Ovarian Cancer Cells
by Young Hyun Ko, Miran Jeong, Dae Sik Jang and Jung-Hye Choi
Life 2021, 11(8), 858; https://doi.org/10.3390/life11080858 - 21 Aug 2021
Cited by 8 | Viewed by 2590
Abstract
The fruits of Schisandra chinensis (Schisandra berries) are used as health food supplements and popular food ingredients in East Asia. Lignans, major and characteristic polyphenol compounds of Schisandra berries, possess various biological activities, including hepatoprotective and anticancer effects. However, the biological activities of [...] Read more.
The fruits of Schisandra chinensis (Schisandra berries) are used as health food supplements and popular food ingredients in East Asia. Lignans, major and characteristic polyphenol compounds of Schisandra berries, possess various biological activities, including hepatoprotective and anticancer effects. However, the biological activities of gomisin L1, a lignan isolated from Schisandra berries, are less to be investigated. In this study, the antitumor activity of gomisin L1 and its underlying molecular mechanism in human ovarian cancer cells were investigated. Gomisin L1 exhibited potent cytotoxic activity against A2780 and SKOV3 ovarian cancer cells. Flow cytometry analysis revealed that the growth inhibitory effects of gomisin L1 were mediated by the induction of apoptosis. Furthermore, gomisin L1 induced an increase in intracellular reactive oxygen species (ROS) levels, and the antioxidant N-acetyl cysteine significantly negated gomisin L1-induced cell death. Moreover, inhibition of NADPH oxidase (NOX) using an inhibitor and siRNA attenuated gomisin L1-induced death of, and ROS production in, human ovarian cancer cells. Taken together, these data indicate that the lignan gomisin L1 from Schisandra berries induces apoptotic cell death by regulating intracellular ROS production via NOX. Full article
(This article belongs to the Special Issue Bioactive Natural Compounds for Pharmaceutical and Nutraceutical Applications)
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12 pages, 702 KiB  
Article
Phytochemical and Biological Screening of Leaf, Bark and Fruit Extracts from Ilex dipyrena Wall.
by Amjad Ali, Atif Ali Khan Khalil, Fazli Khuda, Nausheen Nazir, Riaz Ullah, Ahmed Bari, Adnan Haider, Syed Babar Jamal, Sareer Ahmad, Zahid Khan, Syed Muhammad Mukarram Shah, Syed Wadood Ali Shah, Abdul Nasir, Abid Ali, Muhammad Zahoor and Samin Jan
Life 2021, 11(8), 837; https://doi.org/10.3390/life11080837 - 16 Aug 2021
Cited by 5 | Viewed by 2923
Abstract
The Aquifoliaceae is an important family and has been used traditionally for some time. One of the members of this family is the Ilex dipyrena wall, which itself possesses a potential medicinal importance. This plant is traditionally used for the treatment of various [...] Read more.
The Aquifoliaceae is an important family and has been used traditionally for some time. One of the members of this family is the Ilex dipyrena wall, which itself possesses a potential medicinal importance. This plant is traditionally used for the treatment of various ailments including pain, swelling, burns, and fever. The current study was designed to screen out the antioxidant and analgesic potential of this plant and to verify its traditional uses, along with its phytochemical profile. Extracts were subjected to antioxidant, analgesic, and phytochemical analysis using DPPH, chemical-induced (acetic acid and formalin) nociception models and GC-MS analysis, respectively. The leaf, bark, and fruit extracts showed significant antioxidant activity compared to that of standard. Likewise, all the extracts demonstrated significant (p < 0.01) analgesic activity in a mice model. In acetic acid induced analgesia, the leaf, bark, and fruit extracts caused 51.64, 56.13 and 59.52% inhibition, respectively at a dose of 100 mg/kg while at 200 mg/kg it showed 83.01, 71.69 and 75.47% inhibition, respectively. In Formalin-induced paw-licking assay, fruit extract showed 59.42 and 64.19% inhibition at 200 mg/kg dose in the first and second phase, respectively. The GC-MS analysis revealed the presence of cathinone, phenylpropanolamine, dl-phenylephrine, amphetamine, myristic acid, and palmitic acid. Results of the study suggest that crude extracts from different parts of this plant may be a useful source for the development of novel analgesics. However, further investigation in terms of isolation of bioactive compounds and their toxicological evaluations are needed to validate the observed results. Full article
(This article belongs to the Special Issue Bioactive Natural Compounds for Pharmaceutical and Nutraceutical Applications)
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16 pages, 3994 KiB  
Communication
Extensive Metabolite Profiling in the Unexploited Organs of Black Tiger for Their Potential Valorization in the Pharmaceutical Industry
by Jianfei Gao, Kangning Xiong, Wei Zhou and Weijie Li
Life 2021, 11(6), 544; https://doi.org/10.3390/life11060544 - 10 Jun 2021
Cited by 2 | Viewed by 2267
Abstract
Black tiger (Kadsura coccinea (Lem.)) has been reported to hold enormous pharmaceutical potential. The fruit and rhizome of black tiger are highly exploited in the pharmaceutical and other industries. However, the most important organs from the plant such as the leaf and [...] Read more.
Black tiger (Kadsura coccinea (Lem.)) has been reported to hold enormous pharmaceutical potential. The fruit and rhizome of black tiger are highly exploited in the pharmaceutical and other industries. However, the most important organs from the plant such as the leaf and stem are considered biowastes mainly because a comprehensive metabolite profile has not been reported in these organs. Knowledge of the metabolic landscape of the unexploited black tiger organs could help identify and isolate important compounds with pharmaceutical and nutritional values for a better valorization of the species. In this study, we used a widely targeted metabolomics approach to profile the metabolomes of the K. coccinea leaf (KL) and stem (KS) and compared them with the root (KR). We identified 642, 650 and 619 diverse metabolites in KL, KS and KR, respectively. A total of 555 metabolites were mutually detected among the three organs, indicating that the leaf and stem organs may also hold potential for medicinal, nutritional and industrial applications. Most of the differentially accumulated metabolites between organs were enriched in flavone and flavonol biosynthesis, phenylpropanoid biosynthesis, arginine and proline metabolism, arginine biosynthesis, tyrosine metabolism and 2-oxocarboxylic acid metabolism pathways. In addition, several important organ-specific metabolites were detected in K. coccinea. In conclusion, we provide extensive metabolic information to stimulate black tiger leaf and stem valorization in human healthcare and food. Full article
(This article belongs to the Special Issue Bioactive Natural Compounds for Pharmaceutical and Nutraceutical Applications)
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Review

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21 pages, 7336 KiB  
Review
Bioactive Natural Compounds with Antiplatelet and Anticoagulant Activity and Their Potential Role in the Treatment of Thrombotic Disorders
by Stefania Lamponi
Life 2021, 11(10), 1095; https://doi.org/10.3390/life11101095 - 15 Oct 2021
Cited by 18 | Viewed by 7754
Abstract
Natural anticoagulant drugs can be obtained from plants, rich in secondary bioactive metabolites which, in addition to being effective antioxidants, also possess anticoagulant and antiplatelet properties and, for this reason, can be excellent candidates for the treatment of thrombotic diseases. This review reports [...] Read more.
Natural anticoagulant drugs can be obtained from plants, rich in secondary bioactive metabolites which, in addition to being effective antioxidants, also possess anticoagulant and antiplatelet properties and, for this reason, can be excellent candidates for the treatment of thrombotic diseases. This review reports an overview of the hemostatic process and thrombotic disorders together with data on plants, more and less common from around the world, containing bioactive compounds characterized by antiplatelet and anticoagulant activity. The reported literature was obtained from Medline, PubMed, Elsevier, Web of Science, Google Scholar considering only articles in the English language, published in peer-reviewed journals. The number of citations of the articles and the impact factor of the journals were other parameters used to select the scientific papers to be included in the review. The analysis of the literature data selected demonstrates that many plants’ bioactive compounds show antiplatelet and anticoagulant activity that make them potential candidates to be used as new natural compounds able to interfere with both primary and secondary hemostasis. Moreover, they could be used together with anticoagulants currently administered in clinical practice to increase their efficacy and to reduce complications in the treatment of thrombotic disorders. Full article
(This article belongs to the Special Issue Bioactive Natural Compounds for Pharmaceutical and Nutraceutical Applications)
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