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Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges

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A special issue of Biology (ISSN 2079-7737).

Deadline for manuscript submissions: closed (10 April 2021) | Viewed by 61388

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Dr. Marcus Krüger

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Environmental Cell Biology Group, Department of Microgravity and Translational Regenerative Medicine, Otto von Guericke University, 39106 Magdeburg, Germany
Interests: cell biology; cancer biology; environmental influences; microgravity; cellular communication; photodynamic therapy; cancer treatment; antimicrobial resistance; tumor microbiome
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Dr. Peter Richter

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Gravitational Biology Group, Department of Biology, Cell Biology Division, Friedrich-Alexander-Universität Erlangen-Nürnberg, 91058 Erlangen, Germany
Interests: cell biology; plant physiology; photodynamic therapy
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Dr. Sebastian M. Strauch

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Postgraduate Program in Health and Environment, University of the Region of Joinville - Univille, Rua Paulo Malschitzki 10, Joinville 89219–710, Brazil
Interests: chlorophyll; gravitational biology; phytoplankton; photodynamic therapy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The use and exploitation of natural products (NPs) is anchored throughout the history of mankind. Today, the modern tools of biology (bioinformatics, proteomics, genomics, metagenomics, structural biology, and analytical technologies) allow scientists to understand the biological effects of natural compounds on cells, organisms, and the human body. NPs have evolved their function over millions of years making them often more efficient than synthetic substances if a specific biological activity is needed. The discovery of penicillin by Alexander Fleming or the discovery of streptomycin by Selman A. Waksman, were not only history-changing milestones that greatly affect human life, but also heralded a ‘Golden Age’ of NP-based drug discovery. During the last years, antimicrobial photodynamic therapy using NPs has become an effective way in the control of pathogenic bacteria, and curcumin holds much promise for the development of new therapies against cancer and other diseases.

Taken together, the complex NPs represent an eminent source of novel lead compounds, in particular for antibiotics and antiproliferative agents, and maybe only a very small part of this ‘gold mine’ had just been discovered. With continuing insights into the molecular basis of various diseases (in different organisms), more approaches for NP-based therapies will be created. Innovative strategies in drug discovery are of great importance to meet today’s global health challenges such as the rise of drug-resistant pathogens, increasing cancer incidence or the growing prevalence of other diseases.

This Special Issue welcomes the submission of original research, short communications, and review manuscripts focusing on the biological effects of natural products, especially in therapy approaches (not restricted to humans), but also on the specific technologies employed in their identification and targeting, helping us to provide a realistic overview of this very exciting and interdisciplinary field of biological research.

Dr. Marcus Krüger
Dr. Peter Richter
Dr. Sebastian M. Strauch
Guest Editors

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Keywords

Antimicrobials
Cancer Treatment
Immunomodulators
Antimutagens
Neuroprotective Agents
Photodynamic Therapy
Bioactive Substances
Pharmaceutical Biology
Pharmacognosy
Plant Protection

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Published Papers (9 papers)

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Editorial

Jump to: Research, Review

3 pages, 210 KiB

Open AccessEditorial

Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges

by Marcus Krüger, Peter Richter and Sebastian M. Strauch

Biology 2021, 10(5), 369; https://doi.org/10.3390/biology10050369 - 25 Apr 2021

Cited by 2 | Viewed by 2292

Abstract

Nature provides a unique diversity of primary and secondary metabolites [...] Full article

(This article belongs to the Special Issue Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges)

Research

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13 pages, 6260 KiB

Open AccessArticle

Flaxseed Lignans and Polyphenols Enhanced Activity in Streptozotocin-Induced Diabetic Rats

by Dan Draganescu, Calin Andritoiu, Doina Hritcu, Gianina Dodi and Marcel Ionel Popa

Biology 2021, 10(1), 43; https://doi.org/10.3390/biology10010043 - 11 Jan 2021

Cited by 31 | Viewed by 3521

Abstract

Flaxseeds play an important role in human health due to their chemical composition and recognized beneficial outcomes. This study investigated the antidiabetic effects of present lignans and polyphenols found in the flaxseed extract on streptozotocin (STZ)-induced diabetic rats. The flaxseed administration produced favorable changes in body weight, food and water intake, and glycosylated hemoglobin and blood glucose quantities in the treated diabetic rats. Additionally, significant positive results were observed in the biochemical parameters, namely reduced plasma cholesterol, LDL cholesterol and triglycerides, plasma creatinine, and urea and uric acid levels, highlighting the seeds’ use in traditional medicine. The results were sustained by histopathological observations that showed better tissue preservation following the flaxseed diet. Overall, the consumption of flaxseeds produced moderate reduction in glucose levels and hyperlipidemia, together with improvement in the impaired organs’ function in diabetic rats. The daily administration of polyphenols and lignans compounds could impact therapeutic potential in diabetes management. Full article

(This article belongs to the Special Issue Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges)

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14 pages, 2604 KiB

Open AccessArticle

Modification and Targeted Design of N-Terminal Truncates Derived from Brevinin with Improved Therapeutic Efficacy

by Haoyang He, Yuqing Chen, Zhuming Ye, Xiaoling Chen, Chengbang Ma, Mei Zhou, Xinping Xi, James F. Burrows, Tianbao Chen and Lei Wang

Biology 2020, 9(8), 209; https://doi.org/10.3390/biology9080209 - 6 Aug 2020

Cited by 14 | Viewed by 3014

Abstract

Antimicrobial peptides (AMPs) are a class of molecules that play an essential role in innate immune regulation. The Brevinin-1 family are AMPs that show strong pharmacological and antimicrobial potential. A novel peptide, B1A, was designed based on the primary structure of brevinin-1PLb and brevinin-1PLc. Subsequently, a synthesised replicate was subjected to a series of bioassays and was found to display antimicrobial activity. However, it also displayed high levels of haemolysis in a horse red blood cell haemolytic assay, suggesting potential toxicity. Therefore, we rationally designed a number of B1A analogues with aim of retaining antimicrobial activity, lowering toxicity, and to explore the structure–activity relationship of its N-terminus. B1A and its analogues still retained the “Rana Box” and the FLP-motif, which is a feature of this subfamily. However, the introduction of Lys and Trp residues into the peptide sequences revealed that antimicrobial activity of these analogues remained unchanged once the hydrophobicity and the charge reached the threshold. Hence, the idea that the hydrophobicity saturation in different situations is related to antimicrobial activity can be understood via the structure–activity relationship. Meanwhile, it could also be the starting point for the generation of peptides with specific antimicrobial activity. Full article

(This article belongs to the Special Issue Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges)

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13 pages, 2026 KiB

Open AccessArticle

Isolation of Antidiabetic Withanolides from Withania coagulans Dunal and Their In Vitro and In Silico Validation

by Saima Maher, M. Iqbal Choudhary, Farooq Saleem, Saima Rasheed, Imran Waheed, Sobia Ahsan Halim, Muhammad Azeem, Iskandar Bin Abdullah, Matheus Froeyen, Muhammad Usman Mirza and Sarfraz Ahmad

Biology 2020, 9(8), 197; https://doi.org/10.3390/biology9080197 - 30 Jul 2020

Cited by 25 | Viewed by 6187

Abstract

Withania coagulans (W. coagulans) is well-known in herbal medicinal systems for its high biological potential. Different parts of the plant are used against insomnia, liver complications, asthma, and biliousness, as well as it is reported to be sedative, emetic, diuretic, antidiabetic antimicrobial, anti-inflammatory, antitumor, hepatoprotective, antihyperglycemic, cardiovascular, immuno-suppressive and central nervous system depressant. Withanolides present in W. coagulans have attracted an immense interest in the scientific field due to their diverse therapeutic applications. The current study deals with chemical and biological evaluation of chloroform, and n-butanol fractions of W. coagulans. The activity-guided fractionation of both extracts via multiple chromatographic steps and structure elucidation of pure isolates using spectroscopies (NMR, mass spectrometry, FTIR and UV-Vis) led to the identification of a new withanolide glycoside, withacogulanoside-B (1) from n-butanol extract and five known withanolides from chloroform extract [withanolid J (2), coagulin E (3), withaperuvin C (4), 27-hydroxywithanolide I (5), and ajugin E (6)]. Among the tested compounds, compound 5 was the most potent α-glucosidase inhibitor with IC₅₀ = 66.7 ± 3.6 µM, followed by compound 4 (IC₅₀: 407 ± 4.5 µM) and compound 2 (IC₅₀: 683 ± 0.94 µM), while no antiglycation activity was observed with the six isolated compounds. Molecular docking was used to predict the binding potential and binding site interactions of these compounds as α-glucosidase inhibitors. Consequently, this study provides basis to discover specific antidiabetic compounds from W. coagulans. Full article

(This article belongs to the Special Issue Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges)

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21 pages, 5659 KiB

Open AccessArticle

Protective Mechanism of Acacia saligna Butanol Extract and Its Nano-Formulations against Ulcerative Colitis in Rats as Revealed via Biochemical and Metabolomic Assays

by Heba M.I. Abdallah, Naglaa M. Ammar, Mohamed F. Abdelhameed, Abd El-Nasser G. El Gendy, Tamer I. M. Ragab, Ahmed M. Abd-ElGawad, Mohamed A. Farag, Mona S. Alwahibi and Abdelsamed I. Elshamy

Biology 2020, 9(8), 195; https://doi.org/10.3390/biology9080195 - 30 Jul 2020

Cited by 30 | Viewed by 5387

Abstract

Ulcerative colitis (UC) is a relapsing inflammatory disease of unknown etiology. The increased risk of cancer in UC patients warrants for the development of novel drug treatments. Herein, this work concerns with the investigation of the protective effects of Acacia saligna butanol extract (ASBE) and its nanoformulations on UC in a rat model and its underlying mechanism. Colitis was induced by slow intrarectal infusion of 2 mL of 4% (v/v in 0.9% saline) acetic acid. Colon samples were evaluated macroscopically, microscopically, and assayed for pro-inflammatory cytokine levels. To monitor associated metabolic changes in acetic acid-induced UC model, serum samples were analyzed for primary metabolites using GC–MS followed by multivariate data analyses. Treatment with ASBE attenuated acetic acid-induced UC as revealed by reduction of colon weight, ulcer area, and ulcer index. ASBE treatment also reduced Cyclooxygenase-2 (COX-2), Prostaglandin E2 (PGE2) & Interleukin-1β (IL-1β) levels in the inflamed colon. The nano-formulation of ASBE showed better protection than the crude extract against ulcer indices, increased PGE2 production, and histopathological alterations such as intestinal mucosal lesions and inflammatory infiltration. Distinct metabolite changes were recorded in colitis rats including a decrease in oleamide and arachidonic acid along with increased levels of lactic acid, fructose, and pyroglutamic acid. Treatment with nano extract restored metabolite levels to normal and suggests that cytokine levels were regulated by nano extract in UC. Conclusion: ASBE nano extract mitigated against acetic acid-induced colitis in rats, and the underlying mechanism could be attributed to the modulatory effects of ASBE on the inflammatory cascades. The applicability of metabolomics developed in this rat model seems to be crucial for evaluating the anti-inflammatory mechanisms of new therapeutics for acute colitis. Full article

(This article belongs to the Special Issue Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges)

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14 pages, 3164 KiB

Open AccessArticle

A Novel Antimicrobial Peptide (Kassinatuerin-3) Isolated from the Skin Secretion of the African Frog, Kassina senegalensis

by Hui Wang, Haoyang He, Xiaoling Chen, Mei Zhou, Minjie Wei, Xinping Xi, Chengbang Ma, Qiang Du, Tianbao Chen, Chris Shaw and Lei Wang

Biology 2020, 9(7), 148; https://doi.org/10.3390/biology9070148 - 2 Jul 2020

Cited by 13 | Viewed by 3327

Abstract

Amphibian skin secretions are remarkable sources of novel bioactive peptides. Among these, antimicrobial peptides have demonstrated an outstanding efficacy in killing microorganisms via a general membranolytic mechanism, which may offer the prospect of solving specific target-driven antibiotic resistance. Here, the discovery of a novel defensive peptide is described from the skin secretion of the African frog, Kassina senegalensis. Named kassinatuerin-3, it was identified through a combination of “shot-gun” cloning and MS/MS fragmentation sequencing. Subsequently, a synthetic replicate was subjected to biofunctional evaluation. The results indicated that kassinatuerin-3 possessed antimicrobial activity against Gram-positive bacteria but no effect against Gram-negative bacteria. Additionally, it was active in biofilm eradication on S. aureus and MRSA and in the antiproliferation of selected cancer cell lines. Moreover, it had a very mild hemolytic effect, which demonstrated a high therapeutic index for kassinatuerin-3. Collectively, although kassinatuerin-3 did not demonstrate remarkable bioactivities compared with other natural or synthetic antimicrobial peptides (AMPs), it offered a new insight into the design of antimicrobial derivatives. Full article

(This article belongs to the Special Issue Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges)

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25 pages, 2519 KiB

Open AccessArticle

Anti-Inflammatory and Physicochemical Characterization of the Croton rhamnifolioides Essential Oil Inclusion Complex in β-Cyclodextrin

by Anita Oliveira Brito Pereira Bezerra Martins, Almir Gonçalves Wanderley, Isabel Sousa Alcântara, Lindaiane Bezerra Rodrigues, Francisco Rafael Alves Santana Cesário, Maria Rayane Correia de Oliveira, Fyama Ferreira e Castro, Thaís Rodrigues de Albuquerque, Maria Sanadia Alexandre da Silva, Jaime Ribeiro-Filho, Henrique Douglas Melo Coutinho, Paula Passos Menezes, Lucindo José Quintans-Júnior, Adriano Antunes de Souza Araújo, Marcello Iriti, Jackson Roberto Guedes da Silva Almeida and Irwin Rose Alencar de Menezes

Biology 2020, 9(6), 114; https://doi.org/10.3390/biology9060114 - 30 May 2020

Cited by 15 | Viewed by 3995

Abstract

Croton rhamnifolioides is used in popular medicine for the treatment of inflammatory diseases. The objective of this study was to characterize and evaluate the anti-inflammatory effect of C. rhamnifolioides essential oil complexed in β-cyclodextrin (COEFC). The physicochemical characterization of the complexes was performed using different physical methods. The anti-inflammatory activity was evaluated in vivo by ear edema, paw edema, cotton pellet-induced granuloma, and vascular permeability by Evans blue extravasation. The mechanism of action was validated by molecular docking of the major constituent into the cyclooxygenase-2 (COX-2 enzyme). All doses of the COEFC reduced acute paw edema induced by carrageenan and dextran, as well as vascular permeability. Our results suggest the lowest effective dose of all samples inhibited the response induced by histamine or arachidonic acid as well as the granuloma formation. The complexation process showed that the pharmacological effects were maintained, however, showing similar results using much lower doses. The results demonstrated an involvement of the inhibition of pathways dependent on eicosanoids and histamine. Complexation of β-cyclodextrin/Essential oil (β-CD/EO) may present an important tool in the study of new compounds for the development of anti-inflammatory drugs. Full article

(This article belongs to the Special Issue Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges)

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Review

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24 pages, 8760 KiB

Open AccessReview

Histone Deacetylase Inhibitors from Marine Invertebrates

by Claudio Luparello, Manuela Mauro, Vincenzo Arizza and Mirella Vazzana

Biology 2020, 9(12), 429; https://doi.org/10.3390/biology9120429 - 28 Nov 2020

Cited by 19 | Viewed by 3381

Abstract

Histone deacetylases (HDACs) are key components of the epigenetic machinery controlling gene expression. They are involved in chromatin remodeling events via post-translational histone modifications but may also act on nonhistone proteins, influencing many fundamental cellular processes. Due to the key involvement of HDACs in serious human pathologies, including cancer, HDAC inhibitors (HDACis) have received increased attention in recent years. It is known that marine invertebrates produce significant amounts of secondary metabolites showing active pharmacological properties and an extensive spectrum of biomedical applications. The aim of this review is to gather selected studies that report the extraction and identification of marine invertebrate-derived compounds that possess HDACi properties, grouping the producing species according to their taxonomic hierarchy. The molecular, biochemical, and/or physiological aspects, where available, and modes of action of these naturally occurring HDACis will be recapitulated, taking into consideration their possible utilization for the future design of analogs with increased bioavailability and efficacy, less toxicity, and, also, higher isoform selectivity. Full article

(This article belongs to the Special Issue Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges)

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31 pages, 12793 KiB

Open AccessReview

Bioactive Compounds in Anti-Diabetic Plants: From Herbal Medicine to Modern Drug Discovery

by Ngan Tran, Bao Pham and Ly Le

Biology 2020, 9(9), 252; https://doi.org/10.3390/biology9090252 - 28 Aug 2020

Cited by 262 | Viewed by 29076

Abstract

Natural products, including organisms (plants, animals, or microorganisms) have been shown to possess health benefits for animals and humans. According to the estimation of the World Health Organization, in developing countries, 80% of the population has still depended on traditional medicines or folk medicines which are mostly prepared from the plant for prevention or treatment diseases. Traditional medicine from plant extracts has proved to be more affordable, clinically effective and relatively less adverse effects than modern drugs. Literature shows that the attention on the application of phytochemical constituents of medicinal plants in the pharmaceutical industry has increased significantly. Plant-derived secondary metabolites are small molecules or macromolecules biosynthesized in plants including steroids, alkaloids, phenolic, lignans, carbohydrates and glycosides, etc. that possess a diversity of biological properties beneficial to humans, such as their antiallergic, anticancer, antimicrobial, anti-inflammatory, antidiabetic and antioxidant activities Diabetes mellitus is a chronic disease result of metabolic disorders in pancreas β-cells that have hyperglycemia. Hyperglycemia can be caused by a deficiency of insulin production by pancreatic (Type 1 diabetes mellitus) or insufficiency of insulin production in the face of insulin resistance (Type 2 diabetes mellitus). The current medications of diabetes mellitus focus on controlling and lowering blood glucose levels in the vessel to a normal level. However, most modern drugs have many side effects causing some serious medical problems during a period of treating. Therefore, traditional medicines have been used for a long time and play an important role as alternative medicines. Moreover, during the past few years, some of the new bioactive drugs isolated from plants showed antidiabetic activity with more efficacy than oral hypoglycemic agents used in clinical therapy. Traditional medicine performed a good clinical practice and is showing a bright future in the therapy of diabetes mellitus. World Health Organization has pointed out this prevention of diabetes and its complications is not only a major challenge for the future, but essential if health for all is to be attained. Therefore, this paper briefly reviews active compounds, and pharmacological effects of some popular plants which have been widely used in diabetic treatment. Morphological data from V-herb database of each species was also included for plant identification. Full article

(This article belongs to the Special Issue Natural Products in Modern Biology: Ancient Wisdom for Today’s Challenges)

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