scholarly journals Double the Chemistry, Double the Fun: Structural Diversity and Biological Activity of Marine-Derived Diketopiperazine Dimers

Marine Drugs ◽  
2019 ◽  
Vol 17 (10) ◽  
pp. 551 ◽  
Author(s):  
Nelson G. M. Gomes ◽  
Renato B. Pereira ◽  
Paula B. Andrade ◽  
Patrícia Valentão

While several marine natural products bearing the 2,5-diketopiperazine ring have been reported to date, the unique chemistry of dimeric frameworks appears to remain neglected. Frequently reported from marine-derived strains of fungi, many naturally occurring diketopiperazine dimers have been shown to display a wide spectrum of pharmacological properties, particularly within the field of cancer and antimicrobial therapy. While their structures illustrate the unmatched power of marine biosynthetic machinery, often exhibiting unsymmetrical connections with rare linkage frameworks, enhanced binding ability to a variety of pharmacologically relevant receptors has been also witnessed. The existence of a bifunctional linker to anchor two substrates, resulting in a higher concentration of pharmacophores in proximity to recognition sites of several receptors involved in human diseases, portrays this group of metabolites as privileged lead structures for advanced pre-clinical and clinical studies. Despite the structural novelty of various marine diketopiperazine dimers and their relevant bioactive properties in several models of disease, to our knowledge, this attractive subclass of compounds is reviewed here for the first time.

2020 ◽  
Vol 17 (7) ◽  
pp. 872-883
Author(s):  
Guang-Yao Su ◽  
Ming-Long Chen ◽  
Kui-Wu Wang

Rubiaceae family belongs to the Gentianales, it contains 650 genera and 13,000 species and its worldwide distribution makes it the fourth largest angiosperms. Rubiaceae contains a large amount of anthraquinone compounds, especially in the roots. Anthraquinones are very important natural products with various bioactivities, including antibacterial, antiviral, cytotoxic and antitumor, which make it play an important role in recent research. In the previous study, many researchers have reported anthraquinones from Rubiaceae in different aspects. The present paper provides an overview of the bioactive properties of new naturally occurring anthraquinones and its structural diversity that have been isolated from the Rubiaceae family in recent years. The article covers the literature from 2007 to 2018, overall 95 new anthraquinones.


2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.


Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 620
Author(s):  
Anne Ardaillou ◽  
Jérôme Alsarraf ◽  
Jean Legault ◽  
François Simard ◽  
André Pichette

Several families of naturally occurring C-alkylated dihydrochalcones display a broad range of biological activities, including antimicrobial and cytotoxic properties, depending on their alkylation sidechain. The catalytic Friedel–Crafts alkylation of the readily available aglycon moiety of neohesperidin dihydrochalcone was performed using cinnamyl, benzyl, and isoprenyl alcohols. This procedure provided a straightforward access to a series of derivatives that were structurally related to natural balsacones, uvaretin, and erioschalcones, respectively. The antibacterial and cytotoxic potential of these novel analogs was evaluated in vitro and highlighted some relations between the structure and the pharmacological properties of alkylated dihydrochalcones.


Polymers ◽  
2021 ◽  
Vol 13 (13) ◽  
pp. 2125
Author(s):  
José María Rosales ◽  
Cristina Cejudo ◽  
Lidia Verano ◽  
Lourdes Casas ◽  
Casimiro Mantell ◽  
...  

Polylactic Acid (PLA) filaments impregnated with ethanolic mango leaves extract (MLE) with pharmacological properties were obtained by supercritical impregnation. The effects of pressure, temperature and amount of extract on the response variables, i.e., swelling, extract loading and bioactivity of the PLA filaments, were determined. The analysis of the filaments biocapacities revealed that impregnated PLA filaments showed 11.07% antidenaturant capacity and 88.13% antioxidant activity, which after a 9-day incubation shifted to 30.10% and 9.90%, respectively. Subsequently, the same tests were conducted on printed samples. Before their incubation, the printed samples showed 79.09% antioxidant activity and no antidenaturant capacity was detected. However, after their incubation, the antioxidant activity went down to only 2.50%, while the antidenaturant capacity raised up to 23.50%. The persistence of the bioactive properties after printing opens the possibility of using the functionalized PLA filaments as the feed for a three-dimensional (3D) printer.


2010 ◽  
Vol 3 (2) ◽  
pp. 86-100 ◽  
Author(s):  
Peter Kovacic ◽  
Ratnasamy Somanathan

Resveratrol (RVT) is a naturally occurring trihydroxy stilbene that displays a wide spectrum of physiological activity. Its ability to behave therapeutically as a component of red wine has attracted wide attention. The phenol acts as a protective agent involving various body constituents. Most attention has been given to beneficial effects in insults involving cancer, aging, cardiovascular system, inflammation and the central nervous system. One of the principal modes of action appears to be as antioxidant. Other mechanistic pathways entail cell signaling, apoptosis and gene expression. There is an intriguing dichotomy in relation to pro-oxidant property. Also discussed are metabolism, receptor binding, rationale for safety and suggestions for future work. This is the first comprehensive review of RVT based on a broad, unifying mechanism.


2004 ◽  
Vol 443-444 ◽  
pp. 259-262 ◽  
Author(s):  
Yuriy Perlovich ◽  
Margarita Isaenkova

The substructure inhomogeneity of real textured metal materials was studied by use of the X-ray method of Generalized Pole Figures and the computer data treatment. Main regularities of substructure inhomogeneity were revealed for the first time. Substructure conditions of grains in rolled material form an extremely wide spectrum and vary by passing from texture maxima to texture minima, where residual deformation effects are most significant. The distribution of residual elastic microstrains in the orientational space of rolled material shows the distinct system.


Molecules ◽  
2022 ◽  
Vol 27 (1) ◽  
pp. 305
Author(s):  
Willy Cely-Veloza ◽  
Diego Quiroga ◽  
Ericsson Coy-Barrera

Fusarium oxysporum is an aggressive phytopathogen that affects various plant species, resulting in extensive local and global economic losses. Therefore, the search for competent alternatives is a constant pursuit. Quinolizidine alkaloids (QA) are naturally occurring compounds with diverse biological activities. The structural diversity of quinolizidines is mainly contributed by species of the family Fabaceae, particularly the genus Lupinus. This quinolizidine-based chemo diversity can be explored to find antifungals and even mixtures to address concomitant effects on F. oxysporum. Thus, the antifungal activity of quinolizidine-rich extracts (QREs) from the leaves of eight greenhouse-propagated Lupinus species was evaluated to outline promising QA mixtures against F. oxysporum. Thirteen main compounds were identified and quantified using an external standard. Quantitative analysis revealed different contents per quinolizidine depending on the Lupinus plant, ranging from 0.003 to 32.8 mg/g fresh leaves. Bioautography showed that all extracts were active at the maximum concentration (5 µg/µL). They also exhibited >50% mycelium growth inhibition. All QREs were fungistatic except for the fungicidal QRE of L. polyphyllus Lindl. Angustifoline, matrine, 13α-hydroxylupanine, and 17-oxolupanine were ranked to act jointly against the phytopathogen. Our findings constitute reference information to better understand the antifungal activity of naturally afforded QA mixtures from these globally important plants.


2014 ◽  
Vol 63 (2) ◽  
pp. 117-137 ◽  
Author(s):  
Beata Zagórska-Marek

Impermanent initials and thus the shift of the axis in the stochastic meristems are postulated to be responsible for ontogenetic phyllotactic diversity in plants. In the gynoecium of <i>Magnolia acuminata</i> the main Fibonacci pattern develops in much less than 50% of individual generative shoots. There is also an extremely wide spectrum of other patterns, among them even the rarest I, 3, 8, 11 ... pattern is present. Regarded sometimes as "impossible", the pattern has been documented in SEM for the first time. Beside the presence of various patterns, frequent ontogenetic transformations of phyllotaxis have been found in <i>Magnolia</i>. These are indicated by dislocations in the periodic distribution of carpel primordia. In other magnolias, exemplified by <i>M. soulangeana</i>, the Fibonacci pattern prevails, but not as much as in coniferous vegetative shoots, where, as demonstrated earlier, it reaches 95%. Other pattern numbers are also different. This suggests the involvement of the genetic factor and may be attributed to the higher frequency of discontinuous phyllotactic transformations in some species. The stochastic character of the meristem is perhaps more pronounced in some plants, which leads in turn to more frequent transitions and greater pattern diversity.


2019 ◽  
Vol 67 (1) ◽  
Author(s):  
Hugo R. Fernández ◽  
Ana Lucia Gonzalez Achem ◽  
Marcela Correa ◽  
Virginia H. Albarracín

The solubility equilibrium of calcite is influenced by physicochemical, climatic and biological factors. Annual cycles of exceptionally prolonged drought, in conjunction with naturally occurring diffuse organic pollution, generate the unique conditions for the precipitation of lithified carbonate structures (microbialites). The aim of this article is to analyze the possible implications of calcite precipitation produced in mats of Cladophora sp. in an Andean subtropical basin, considering it is the first time this phenomenon is described for the region. We collected samples from selected sites at the Lules River Basin, in four sampling dates between the years 2003 and 2004, within a monitoring work of 15 years. Samples were analyzed using an electron microscope and X-ray diffraction analysis. We found that Gomphonema sp. attached to Cladophora sp. contributes to precipitation of calcite and formation of microbialite like structures, in the studied area. This work presents an initial discussion of the discovery of microbialites-like structures attached to Cladophora sp. mats in a subtropical Andean stream and the environmental conditions that lead to their production, as well as the possible ecological implications of these microbialites.


Química Nova ◽  
2021 ◽  
Author(s):  
Dartagnan Ferreira ◽  
Valter Murie ◽  
Thiago Santos ◽  
Paulo Vieira ◽  
Giuliano Clososki

RECENT ADVANCES IN SELECTIVE FUNCTIONALIZATION OF QUINOLINES. Heterocyclic compounds form an important and extensive group of organic substances. Among nitrogenous heterocyclic molecules, quinolines stand out for exhibiting attractive chemical and biological properties. These substances can be used as ligands, sensors, luminescent and agrochemical materials. In addition, quinoline-containing compounds can exhibit a wide spectrum of pharmacological properties, allowing their use in several approved drugs nowadays. Due to its importance, the synthesis of molecules containing this nucleus becomes a point of interest for synthetic chemists. In this way, several methodologies have been recently developed to prepare quinoline derivatives with high structural diversity. Such chemical transformations allow the chemical modification of these rings with high selectivity and tolerance to diverse functional groups and these properties have been conveniently used in the preparation of biologically active molecules containing this unit. Herein, we present a review of the main methodologies employed in the selective functionalization of quinolines in the last twenty years. In this context, a brief introduction addressing general synthetic and medicinal aspects related to the functionalization positions of the quinoline ring is presented. Several methodologies used in the functionalization of this moiety are discussed, as well relevant synthetic applications, both in the preparation and functionalization of substances of biological interest.


Sign in / Sign up

Export Citation Format

Share Document