scholarly journals Discovery of Antimalarial Drugs from Streptomycetes Metabolites Using a Metabolomic Approach

2017 ◽  
Vol 2017 ◽  
pp. 1-7
Author(s):  
Siti Junaidah Ahmad ◽  
Mohd Badrin Hanizam Abdul Rahim ◽  
Syarul Nataqain Baharum ◽  
Mohd Shukri Baba ◽  
Noraziah Mohamad Zin
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Bioactive Compounds ◽  
Antimalarial Activity ◽  
Classical Method ◽  
Biologically Active ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Wide Range ◽  
Bioassay Guided Fractionation

Natural products continue to play an important role as a source of biologically active substances for the development of new drug.Streptomyces, Gram-positive bacteria which are widely distributed in nature, are one of the most popular sources of natural antibiotics. Recently, by using a bioassay-guided fractionation, an antimalarial compound, Gancidin-W, has been discovered from these bacteria. However, this classical method in identifying potentially novel bioactive compounds from the natural products requires considerable effort and is a time-consuming process. Metabolomics is an emerging “omics” technology in systems biology study which integrated in process of discovering drug from natural products. Metabolomics approach in finding novel therapeutics agent for malaria offers dereplication step in screening phase to shorten the process. The highly sensitive instruments, such as Liquid Chromatography-Mass Spectrophotometry (LC-MS), Gas Chromatography-Mass Spectrophotometry (GC-MS), and Nuclear Magnetic Resonance (1H-NMR) spectroscopy, provide a wide range of information in the identification of potentially bioactive compounds. The current paper reviews concepts of metabolomics and its application in drug discovery of malaria treatment as well as assessing the antimalarial activity from natural products. Metabolomics approach in malaria drug discovery is still new and needs to be initiated, especially for drug research in Malaysia.

The Potential of Biologically Active Brazilian Plant Species as a Strategy to Search for Molecular Models for Mosquito Control

Planta Medica ◽  
2020 ◽  
Author(s):  
Marilia Valli ◽  
Letícia Cristina Vieira Atanázio ◽  
Gustavo Claro Monteiro ◽  
Roberta Ramos Coelho ◽  
Daniel Pecoraro Demarque ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Vector Control ◽  
Plant Species ◽  
Mosquito Control ◽  
Biologically Active ◽  
Molecular Models ◽  
Public Health Importance ◽  
Active Compounds ◽  
Brazilian Biodiversity

AbstractNatural products are a valuable source of biologically active compounds and continue to play an important role in modern drug discovery due to their great structural diversity and unique biological properties. Brazilian biodiversity is one of the most extensive in the world and could be an effective source of new chemical entities for drug discovery. Mosquitoes are vectors for the transmission of dengue, Zika, chikungunya, yellow fever, and many other diseases of public health importance. These diseases have a major impact on tropical and subtropical countries, and their incidence has increased dramatically in recent decades, reaching billions of people at risk worldwide. The prevention of these diseases is mainly through vector control, which is becoming more difficult because of the emergence of resistant mosquito populations to the chemical insecticides. Strategies to provide efficient and safe vector control are needed, and secondary metabolites from plant species from the Brazilian biodiversity, especially Cerrado, that are biologically active for mosquito control are herein highlighted. Also, this is a literature revision of targets as insights to promote advances in the task of developing active compounds for vector control. In view of the expansion and occurrence of arboviruses diseases worldwide, scientific reviews on bioactive natural products are important to provide molecular models for vector control and contribute with effective measures to reduce their incidence.

Biosynthesis of bioactive natural products from Basidiomycota

2019 ◽  
Vol 17 (5) ◽  
pp. 1027-1036 ◽  
Author(s):  
Hsiao-Ching Lin ◽  
Ranuka T. Hewage ◽  
Yuan-Chun Lu ◽  
Yit-Heng Chooi
Keyword(s):  
Natural Products ◽  
Bioactive Compounds ◽  
Biosynthetic Pathways ◽  
Bioactive Natural Products ◽  
Wide Range

The club fungi, Basidioycota, produce a wide range of bioactive compounds. Here, we describe recent studies on the biosynthetic pathways and enzymes of bioactive natural products from these fungi.

scholarly journals Enduracididine, a rare amino acid component of peptide antibiotics: Natural products and synthesis

2016 ◽  
Vol 12 ◽  
pp. 2325-2342 ◽  
Author(s):  
Darcy J Atkinson ◽  
Briar J Naysmith ◽  
Daniel P Furkert ◽  
Margaret A Brimble
Keyword(s):  
Natural Products ◽  
Amino Acid ◽  
Drug Discovery ◽  
Peptide Antibiotic ◽  
Peptide Antibiotics ◽  
Global Public Health ◽  
Development Of Resistance ◽  
Wide Range ◽  
Imminent Threat ◽  
Synthetic Approaches

Rising resistance to current clinical antibacterial agents is an imminent threat to global public health and highlights the demand for new lead compounds for drug discovery. One such potential lead compound, the peptide antibiotic teixobactin, was recently isolated from an uncultured bacterial source, and demonstrates remarkably high potency against a wide range of resistant pathogens without apparent development of resistance. A rare amino acid residue component of teixobactin, enduracididine, is only known to occur in a small number of natural products that also possess promising antibiotic activity. This review highlights the presence of enduracididine in natural products, its biosynthesis together with a review of analogues of enduracididine. Reported synthetic approaches to the cyclic guanidine structure of enduracididine are discussed, illustrating the challenges encountered to date in the development of efficient synthetic routes to facilitate drug discovery efforts inspired by the discovery of teixobactin.

scholarly journals Discovery of Novel Caeridins from the Skin Secretion of the Australian White’s Tree Frog, Litoria caerulea

2018 ◽  
Vol 2018 ◽  
pp. 1-18
Author(s):  
Lei Li ◽  
Qing Wu ◽  
Xi Wang ◽  
Huimin Lu ◽  
Xinping Xi ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Drug Discovery ◽  
Frog Skin ◽  
Smooth Muscles ◽  
Biologically Active ◽  
Tree Frog ◽  
Skin Secretion ◽  
Bladder Smooth Muscle ◽  
Gram Positive Bacteria ◽  
Litoria Caerulea

Abundant biologically active peptides have been discovered from frog skin secretions, a rich natural source of bioactive compounds with great potential in drug discovery. In this study, three Caeridin peptides, namely, Caeridin-1, S5-Caeridin-1, and Caeridin-a1, were discovered from the skin secretion of the Australian White’s tree frog, Litoria caerulea, for the first time, by means of combining transcriptomic and peptidomic analyses. It also represents the first report on bioactive Caeridins since this family of peptides was initially studied 20 years ago. Chemically synthetic versions of each natural Caeridin demonstrated promising bioactivities either on rat smooth muscles or against microbial growth. Specifically, Caeridin-1 produced contraction of rat bladder smooth muscle, while S5-Caeridin-1 induced relaxation of rat ileum smooth muscle, both at nanomolar concentrations. Moreover, Caeridin-a1 was shown to potently inhibit the growth of the planktonic Gram-positive bacteria Staphylococcus aureus (S. aureus), methicillin-resistant S. aureus (MRSA), and Enterococcus faecalis (E. faecalis), the Gram-negative bacterium, Escherichia coli (E. coli), and the yeast, Candida albicans (C. albicans). The discovery of these Caeridins may induce further intensive and systematic studies of frog skin peptides to promote the discovery of natural templates as lead compounds for drug discovery and therapeutic application.

scholarly journals Ecopharmacognosy: Exploring The Chemical And Biological Potential Of Nature For Human Health

2014 ◽  
Vol 3 (1) ◽  
pp. 1 ◽  
Author(s):  
Geoffrey A. Cordell
Keyword(s):  
Health Care ◽  
Natural Products ◽  
Drug Discovery ◽  
Natural Product ◽  
Developed Countries ◽  
Biologically Active ◽  
Minor Role ◽  
Natural Product Research ◽  
Biological Potential ◽  
The World

“Why didn’t they develop natural product drugs in a sustainable manner at the beginning of this century?”  In 2035, when about 10.0 billion will inhabit Earth, will this be our legacy as the world contemplates the costs and availability of synthetic and gene-based products for primary health care?  Acknowledging the recent history of the relationship between humankind and the Earth, it is essential that the health care issues being left for our descendants be considered in terms of resources. For most people in the world, there are two vast health care “gaps”, access to quality drugs and the development of drugs for major global and local diseases.  Consequently for all of these people, plants, in their various forms, remain a primary source of health care.  In the developed countries, natural products derived from plants assume a relatively minor role in health care, as prescription and over-the-counter products, even with the widespread use of phytotherapeutical preparations.  Significantly, pharmaceutical companies have retrenched substantially in their disease areas of focus.  These research areas do not include the prevalent diseases of the middle- and lower-income countries, and important diseases of the developed world, such as drug resistance. What then is the vision for natural product research to maintain the choices of drug discovery and pharmaceutical development for future generations?  In this discussion some facets of how natural products must be involved globally, in a sustainable manner, for improving health care will be examined within the framework of the new term “ecopharmacognosy”, which invokes sustainability as the basis for research on biologically active natural products.  Access to the biome, the acquisition, analysis and dissemination of plant knowledge, natural product structure diversification, biotechnology development, strategies for natural product drug discovery, and aspects of multitarget therapy and synergy research will be discussed.  Options for the future will be presented which may be significant as countries decide how to develop approaches to relieve their own disease burden, and the needs of their population for improved access to medicinal agents.

scholarly journals Drug Discovery on Natural Products: From Ion Channels to nAChRs, from Nature to Libraries, from Analytics to Assays

2019 ◽  
Vol 24 (3) ◽  
pp. 362-385 ◽  
Author(s):  
Reka A. Otvos ◽  
Kristina B. M. Still ◽  
Govert W. Somsen ◽  
August B. Smit ◽  
Jeroen Kool
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Ion Channels ◽  
Ion Channel ◽  
Bioactive Compounds ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Drug Targets ◽  
Α7 Nachr ◽  
Analytical Approaches

Natural extracts are complex mixtures that may be rich in useful bioactive compounds and therefore are attractive sources for new leads in drug discovery. This review describes drug discovery from natural products and in explaining this process puts the focus on ion-channel drug discovery. In particular, the identification of bioactives from natural products targeting nicotinic acetylcholine receptors (nAChRs) and serotonin type 3 receptors (5-HT3Rs) is discussed. The review is divided into three parts: “Targets,” “Sources,” and “Approaches.” The “Targets” part will discuss the importance of ion-channel drug targets in general, and the α7-nAChR and 5-HT3Rs in particular. The “Sources” part will discuss the relevance for drug discovery of finding bioactive compounds from various natural sources such as venoms and plant extracts. The “Approaches” part will give an overview of classical and new analytical approaches that are used for the identification of new bioactive compounds with the focus on targeting ion channels. In addition, a selected overview is given of traditional venom-based drug discovery approaches and of diverse hyphenated analytical systems used for screening complex bioactive mixtures including venoms.

Natural Products from Deep-Sea-Derived Fungi ̶ A New Source of Novel Bioactive Compounds?

2018 ◽  
Vol 25 (2) ◽  
pp. 186-207 ◽  
Author(s):  
Georgios Daletos ◽  
Weaam Ebrahim ◽  
Elena Ancheeva ◽  
Mona El-Neketi ◽  
Weiguo Song ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Secondary Metabolites ◽  
Bioactive Compounds ◽  
Deep Sea ◽  
Underlying Assumption ◽  
Pharmacologically Active ◽  
Promising Source ◽  
New Metabolites

Background: Over the last two decades, deep-sea-derived fungi are considered to be a new source of pharmacologically active secondary metabolites for drug discovery mainly based on the underlying assumption that the uniqueness of the deep sea will give rise to equally unprecedented natural products. Indeed, up to now over 200 new metabolites have been identified from deep-sea fungi, which is in support of the statement made above. Results: This review summarizes the new and/or bioactive compounds reported from deepsea- derived fungi in the last six years (2010 – October 2016) and critically evaluates whether the data published so far really support the notion that these fungi are a promising source of new bioactive chemical entities.

The Fungal Metabolites with Potential Antiplasmodial Activity

2018 ◽  
Vol 25 (31) ◽  
pp. 3796-3825 ◽  
Author(s):  
Bin Yang ◽  
Jingxia Huang ◽  
Xuefeng Zhou ◽  
Xiuping Lin ◽  
Juan Liu ◽  
...  
Keyword(s):  
Natural Products ◽  
Antimicrobial Agents ◽  
Antimalarial Activity ◽  
Management Strategies ◽  
Marine Fungus ◽  
Chemical Diversity ◽  
Biologically Active ◽  
Antiplasmodial Activity ◽  
Marine Environments ◽  
Tropical Regions

Malaria caused by Plasmodium parasites is amongst many prevalent public health concerns in several tropical regions of the world. Nowadays, the parasite resistance patterns to most currently used drugs in therapy and insecticides have created an urgent need for new chemical entities exhibiting new modes of action and management strategies. Fungus has been proven to be an excellent source of biologically active compounds, which have been screened for antiplasmodial activity as potential sources of new antimalarial drugs. This review summarizes the current 255 natural products from fungus, which may possess antimalarial activity and can be classified as sesquiterpenes, diterpenes, sesterterpenes, alkaloids, peptides depsipeptides, xanthones, anthraquinones, anthrones, bioxanthracenes, bixanthones, preussomerins, depsidones, phenols, trichothecenes, azaphliones, macrolides, and steroids. However, the treatments available for malaria are limited. Thus, the identification of novel antimicrobial agents should be continued, and all possible strategies should be explored. Carrying forward the antimalarial screening in exited terrestrial and marine natural products library, and finding the new natural products in new resources, particularly those living in marine environments, are still important approaches to find new antimalarial agents. Unusual marine environments are associated with chemical diversity, leading to a resource of novel active substances for the development of bioactive products. Finding new antimalarial natural products in marine fungus, particularly those living in deep-sea and special marine environments, is an important approach to identify novel active agents.

3,4-Dihydroisocoumarins, Interesting Natural Products: Isolation, Organic Syntheses and Biological Activities

2019 ◽  
Vol 16 (1) ◽  
pp. 112-129 ◽  
Author(s):  
Aurelio Ortiz ◽  
Miriam Castro ◽  
Estibaliz Sansinenea
Keyword(s):  
Natural Products ◽  
Biological Activities ◽  
Natural Compounds ◽  
Biologically Active ◽  
Bacterial Strains ◽  
Drug Candidates ◽  
Heterocyclic Molecules ◽  
Naturally Occurring ◽  
Wide Range ◽  
Different Sources

Background:3,4-dihydroisocoumarins are an important small group belonging to the class of naturally occurring lactones isolated from different bacterial strains, molds, lichens, and plants. The structures of these natural compounds show various types of substitution in their basic skeleton and this variability influences deeply their biological activities. These lactones are structural subunits of several natural products and serve as useful intermediates in the synthesis of different heterocyclic molecules, which exhibit a wide range of biological activities, such as anti-inflammatory, antiplasmodial, antifungal, antimicrobial, antiangiogenic and antitumoral activities, among others. Their syntheses have attracted attention of many researchers reporting many synthetic strategies to achieve 3,4-dihydroisocoumarins and other related structures. </P><P> Objective: In this context, the isolation of these natural compounds from different sources, their syntheses and biological activities are reviewed, adding the most recent advances and related developments.Conclusion:This review aims to encourage further work on the isolation and synthesis of this class of natural products. It would be beneficial for synthetic as well as the medicinal chemists to design selective, optimized dihydroisocoumarin derivatives as potential drug candidates, since dihydroisocoumarin scaffolds have significant utility in the development of therapeutically relevant and biologically active compounds.

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