scholarly journals Natural Cyclic Peptides as an Attractive Modality for Therapeutics: A Mini Review

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2080 ◽  
Author(s):  
Muna Abdalla ◽  
Lyndy McGaw
Keyword(s):  
Drug Discovery ◽  
Cyclic Peptides ◽  
Cyclic Peptide ◽  
Pharmacological Properties ◽  
Biological Processes ◽  
Peptide Antibiotics ◽  
Natural Sources ◽  
Biological Targets ◽  
Naturally Occurring ◽  
Wide Range

Peptides are important biomolecules which facilitate the understanding of complex biological processes, which in turn could be serendipitous biological targets for future drugs. They are classified as a unique therapeutic niche and will play an important role as fascinating agents in the pharmaceutical landscape. Until now, more than 40 cyclic peptide drugs are currently in the market, and approximately one new cyclopeptide drug enters the market annually on average. Interestingly, the majority of clinically approved cyclic peptides are derived from natural sources, such as peptide antibiotics and human peptide hormones. In this report, the importance of cyclic peptides is discussed, and their role in drug discovery as interesting therapeutic biomolecules will be highlighted. Recently isolated naturally occurring cyclic peptides from microorganisms, sponges, and other sources with a wide range of pharmacological properties are reviewed herein.

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.

Natural Bioactive Cyclopeptides from Microbes as Promising Anticancer Drug Leads: A Mini-review

2021 ◽  
pp. 291-303
Author(s):  
Linda Sukmarini
Keyword(s):  
Natural Products ◽  
Cyclic Peptides ◽  
Recent Decade ◽  
Bioactive Molecules ◽  
Marine Cyanobacteria ◽  
Anticancer Activities ◽  
Natural Sources ◽  
Naturally Occurring ◽  
Lead Candidate ◽  
Drug Leads

Natural products from microbes are a rich source of bioactive molecules to serve as drug leads, predominantly in cancer therapy. Peptides are among the essential nature-derived biomolecules. Owing to their great diversity and favorable characteristics, cyclic peptides (cyclopeptides) from natural sources have become a propitious lead candidate for the development of therapeutics, including anticancer drugs. This present mini-review highlights cyclopeptides from microbial-derived natural products that have demonstrated significant cytotoxicity or anticancer activities. Moreover, this mini-review also provides a look into the mode of action of anticancer cyclopeptides. Selected examples are given for the potent anticancer cyclopeptides isolated in the recent decade from fungi and bacteria from both terrestrial and marine origins. Naturally occurring cyclopeptides with canonical and non-canonical amino acids isolated from fungi, myxobacteria, actinomycetes, marine cyanobacteria, and microbes associated with marine organisms and their anticancer activity are featured herein.

scholarly journals A Review of the Ethnomedicinal Uses, Biological Activities, and Triterpenoids of Euphorbia Species

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 4019
Author(s):  
Douglas Kemboi ◽  
Xolani Peter ◽  
Moses Langat ◽  
Jacqueline Tembu
Keyword(s):  
Drug Discovery ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Structural Diversity ◽  
Pharmacological Properties ◽  
Anticancer Activities ◽  
Sensory Disorders ◽  
Wide Range ◽  
Ethnomedicinal Uses

The genus Euphorbia is one of the largest genera in the spurge family, with diversity in range, distribution, and morphology. The plant species in this genus are widely used in traditional medicine for the treatment of diseases, ranging from respirational infections, body and skin irritations, digestion complaints, inflammatory infections, body pain, microbial illness, snake or scorpion bites, pregnancy, as well as sensory disorders. Their successes have been attributed to the presence of diverse phytochemicals like polycyclic and macrocyclic diterpenes with various pharmacological properties. As a result, Euphorbia diterpenes are of interest to chemists and biochemists with regard to drug discovery from natural products due to their diverse therapeutic applications as well as their great structural diversity. Other chemical constituents such as triterpenoids have also been reported to possess various pharmacological properties, thus supporting the traditional uses of the Euphorbia species. These triterpenoids can provide potential leads that can be developed into pharmaceutical compounds for a wide range of medicinal applications. However, there are scattered scientific reports about the anticancer activities of these constituents. Harnessing such information could provide a database of bioactive pharmacopeia or targeted scaffolds for drug discovery. Therefore, this review presents an updated and comprehensive summary of the ethnomedicinal uses, phytochemistry, and the anticancer activities of the triterpenoids of Euphorbia species. Most of the reported triterpenoids in this review belong to tirucallane, cycloartanes, lupane, oleanane, ursane, and taraxane subclass. Their anticancer activities varied distinctly with the majority of them exhibiting significant cytotoxic and anticancer activities in vitro. It is, therefore, envisaged that the report on Euphorbia triterpenoids with interesting anticancer activities will form a database of potential leads or scaffolds that could be advanced into the clinical trials with regard to drug discovery.

scholarly journals Cyclic Peptides that Govern Signal Transduction Pathways: From Prokaryotes to Multi-Cellular Organisms

2018 ◽  
Vol 18 (7) ◽  
pp. 625-644 ◽  
Author(s):  
Ryan W. Mull ◽  
Anthony Harrington ◽  
Lucia A. Sanchez ◽  
Yftah Tal-Gan
Keyword(s):  
Signal Transduction ◽  
Quorum Sensing ◽  
Cyclic Peptides ◽  
Cyclic Peptide ◽  
Endocrine System ◽  
Peptide Hormones ◽  
Signal Transduction Pathways ◽  
Wide Range ◽  
Eukaryotic Organisms ◽  
Multicellular Organisms

Cyclic peptide scaffolds are key components of signal transduction pathways in both prokaryotic and eukaryotic organisms since they act as chemical messengers that activate or inhibit specific cognate receptors. In prokaryotic organisms these peptides are utilized in non-essential pathways, such as quorum sensing, that are responsible for virulence and pathogenicity. In the more evolved eukaryotic systems, cyclic peptide hormones play a key role in the regulation of the overall function of multicellular organisms, mainly through the endocrine system. This review will highlight several prokaryote and eukaryote systems that use cyclic peptides as their primary signals and the potential associated with utilizing these scaffolds for the discovery of novel therapeutics for a wide range of diseases and illnesses.

scholarly journals Review of Chemical, Pharmacological, Biological Activities of Isatin and its Derivatives – Part-1 (1877 to 2002)

2020 ◽  
Keyword(s):  
Enzyme Activity ◽  
Biological Activities ◽  
Biological Effects ◽  
Coal Tar ◽  
Review Article ◽  
Pharmacological Properties ◽  
Naturally Occurring ◽  
Wide Range ◽  
Cns Activity

:Isatin is a naturally occurring substance present in humans, animals, plants and coal tar. Isatin itself exhibits a variety of biological effects (invivo and invitro) and substituted isatins are reported to possess a wide range of pharmacological properties such as antimicrobial, antineoplastic, analgesic, antiinflammatory, antipyretic, enzyme activity, CNS activity, antiprotozoal, antihelminthic and association with biomolecules. In this review article, we have attempted to compile the most signigicant reports (1877 to 2002) of biological and pharmacological activites of isatin and its derivatives.

scholarly journals Rapid Biosynthesis of Gold Nanoparticles by the Extracellular Secretion ofBacillus niabensis45: Characterization and Antibiofilm Activity

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Yumei Li ◽  
Yamei Li ◽  
Qiang Li ◽  
Xiangyu Fan ◽  
Juan Gao ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Gold Nanoparticles ◽  
Cyclic Peptides ◽  
Cyclic Peptide ◽  
Xrd Analysis ◽  
Antibiofilm Activity ◽  
Extracellular Biosynthesis ◽  
Extracellular Secretion ◽  
Wide Range ◽  
Imagej Software

The present study demonstrated that the extracellular biosynthesis of gold nanoparticles (GNPs) usingB. niabensis45 may be mediated by a cyclic peptide (P2). The molecular weight of P2 was determined to be about 1122 Da by MALDI-TOF-MS and ESI-MS. A novel protocol for rapid biosynthesis of GNPs using P2 was developed. The results showed that GNP synthesis could be completed in a wide range of temperatures (40–100°C) and pH (6.0–10.0) within few minutes when 9 mL of P2 (2 mg/mL) and 1 mL of HAuCl4solution (2 mM) were mixed together. The synthesized GNPs were further characterized. Energy dispersive spectroscopy (EDS) and X-ray diffraction (XRD) analysis confirmed the presence of elemental gold and crystalline structure of the GNPs, respectively. Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) revealed the formation of spherical metallic GNPs. The size distribution of GNPs calculated using ImageJ software was found to be 10–20 nm. And these GNPs showed excellent antibiofilm activity againstPseudomonas aeruginosaPAO1 andStaphylococcus aureusATCC25923. The results revealed microbial cyclic peptides could be used as synthesis of GNPs which had potent antibiofilm potential.

Medicinal applications of coumarins bearing azetidinone and thiazolidinone moieties

2021 ◽  
Author(s):  
Siddappa A Patil ◽  
Shivaputra A Patil ◽  
Temilade Fariyike ◽  
Kostiantyn O Marichev ◽  
Hector Mario Heras Martinez ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Pharmacological Properties ◽  
Structure Activity Relationships ◽  
Naturally Occurring ◽  
Structure Activity ◽  
Wide Range ◽  
Synthetic Routes ◽  
Synthetic Methodologies

Coumarins (2 H-chromen-2-ones), also known as benzopyran-2-ones, are a family of naturally occurring heterocyclic ring systems that contain a lactone moiety. Coumarins exhibit a wide range of well-studied pharmacological properties. Over the last few decades, as a result of advances in diverse oriented synthetic routes, physicochemical properties and numerous biological activities, coumarins have become globally studied molecules from various synthetic and medicinal chemists. Recently, several bioactive coumarins bearing azetidinone and thiazolidinone moieties have been found to display a range of therapeutic characteristics, including antimicrobial, anticancer, antidiabetic and anti-inflammatory properties. This review offers a brief description of the synthetic methodologies, known bioactivity and structure–activity relationships of coumarins bearing azetidinones and thiazolidinones.

scholarly journals Contemplating 1,2,4-Thiadiazole-Inspired Cyclic Peptide Mimics: A Computational Investigation

2019 ◽  
Vol 72 (11) ◽  
pp. 894 ◽  
Author(s):  
Sida Xie ◽  
Paul V. Bernhardt ◽  
Lawrence R. Gahan ◽  
Craig M. Williams
Keyword(s):  
Metal Binding ◽  
Metal Ion ◽  
Cyclic Peptides ◽  
Cyclic Peptide ◽  
Computational Study ◽  
Ion Binding ◽  
Metal Ion Binding ◽  
Binding Studies ◽  
Naturally Occurring ◽  
The Stability

Marine derived cyclic peptides have inspired chemists for decades as the cavitand architecture can be compared with macrocyclic ligands, and hence easily conceived as mediators of metal-ion transport. Lissoclinamide 5 and ascidiacyclamide are two such cyclic peptides that have received much attention both for their metal ion complexation properties and biological activity; the metal ion binding properties of mimics of these two systems have been reported. Reported herein is a computational study aimed at evaluating the stability, and potential for copper(ii) ion binding by lissoclinamide 5 mimics that substitute the naturally occurring 4-carboxy-1,3-thiazole units for novel valine- and phenylalanine-derived 1,2,4-thiadiazole units. Our results suggest that one lissoclinamide 5 mimic, 1,2,4-thiadiazole (TDA)-lissoclinamide 9, may be capable of forming a complex with one CuII ion, [Cu(9-H)(H2O)]+. A complex with two CuII ions, [Cu2(9-H)(μ-OH)]2+, was also considered. These results set the stage for synthetic and experimental metal binding studies.

One-Pot Glycosylation Strategy for Rapid Access of Oligosaccharides with Wide Range of Molecular Diversity

2021 ◽  
Vol 25 ◽  
Author(s):  
Rekha Sangwan ◽  
Pintu Kumar Mandala
Keyword(s):  
Drug Discovery ◽  
Molecular Diversity ◽  
Vaccine Development ◽  
Carbohydrate Chemistry ◽  
One Pot ◽  
Natural Sources ◽  
Biologically Relevant ◽  
Rapid Access ◽  
Wide Range ◽  
Complex Glycans

: In carbohydrate chemistry, the synthesis of complex saccharides with well-defined structures is the most formidable process as it is quite strenuous to isolate carbohydrates in acceptable purity and amounts from natural sources. Therefore, complex saccharides with well-defined structures are often most conveniently accessed through chemical syntheses. This review mainly focuses on the methodologies for one-pot glycosylation into the complex glycans from the non-reducing end to reducing end and vice versa, orthogonal, preactivation based, photochemical as well as hybrid one-pot glycosylation. The main goal of this review is to be able to rapidly synthesize biologically relevant glycans in carbohydrates that can be implemented to research in carbohydrate-based vaccine development, diagnostics, as well as drug discovery.

Discovery and applications of naturally occurring cyclic peptides

Planta Medica ◽  
2011 ◽  
Vol 77 (12) ◽  
Author(s):  
D Craik ◽  
A Poth ◽  
M Colgrave ◽  
M Akcan ◽  
B Oku ◽  
...  
Keyword(s):  
Cyclic Peptides ◽  
Naturally Occurring
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