scholarly journals An Overview of Bioactive 1,3-Oxazole-Containing Alkaloids from Marine Organisms

2021 ◽  
Vol 14 (12) ◽  
pp. 1274
Author(s):  
Jinyun Chen ◽  
Sunyan Lv ◽  
Jia Liu ◽  
Yanlei Yu ◽  
Hong Wang ◽  
...  
Keyword(s):  
Nitrogen Atom ◽  
Chemical Synthesis ◽  
Biological Activities ◽  
Structural Features ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Marine Organisms ◽  
Chemical Structures ◽  
First Time ◽  
Oxazole Derivatives

1,3-Oxazole chemicals are a unique class of five-membered monocyclic heteroarenes, containing a nitrogen atom and an oxygen. These alkaloids have attracted extensive attention from medicinal chemists and pharmacologists owing to their diverse arrays of chemical structures and biological activities, and a series of 1,3-oxazole derivatives has been developed into therapeutic agents (e.g., almoxatone, befloxatone, cabotegravir, delpazolid, fenpipalone, haloxazolam, inavolisib). A growing amount of evidence indicates that marine organisms are one of important sources of 1,3-oxazole-containing alkaloids. To improve our knowledge regarding these marine-derived substances, as many as 285 compounds are summarized in this review, which, for the first time, highlights their sources, structural features and biological properties, as well as their biosynthesis and chemical synthesis. Perspective for the future discovery of new 1,3-oxazole compounds from marine organisms is also provided.

scholarly journals Sphingolipids of Asteroidea and Holothuroidea: Structures and Biological Activities

Marine Drugs ◽  
2021 ◽  
Vol 19 (6) ◽  
pp. 330
Author(s):  
Timofey V. Malyarenko ◽  
Alla A. Kicha ◽  
Valentin A. Stonik ◽  
Natalia V. Ivanchina
Keyword(s):  
Marine Invertebrates ◽  
Biological Activities ◽  
Complete Information ◽  
Structural Features ◽  
Marine Organisms ◽  
Structural Components ◽  
Chemical Structures ◽  
The Past ◽  
Complex Lipids ◽  
Complex Sphingolipids

Sphingolipids are complex lipids widespread in nature as structural components of biomembranes. Commonly, the sphingolipids of marine organisms differ from those of terrestrial animals and plants. The gangliosides are the most complex sphingolipids characteristic of vertebrates that have been found in only the Echinodermata (echinoderms) phylum of invertebrates. Sphingolipids of the representatives of the Asteroidea and Holothuroidea classes are the most studied among all echinoderms. In this review, we have summarized the data on sphingolipids of these two classes of marine invertebrates over the past two decades. Recently established structures, properties, and peculiarities of biogenesis of ceramides, cerebrosides, and gangliosides from starfishes and holothurians are discussed. The purpose of this review is to provide the most complete information on the chemical structures, structural features, and biological activities of sphingolipids of the Asteroidea and Holothuroidea classes.

scholarly journals A Review of the Traditional Uses, Phytochemistry and Biological Activities of the Genus Santolina

Planta Medica ◽  
2018 ◽  
Vol 84 (09/10) ◽  
pp. 627-637 ◽  
Author(s):  
Rosa Tundis ◽  
Monica Loizzo
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Future Research ◽  
Chemical Profile ◽  
Bioactive Constituents ◽  
Mediterranean Flora ◽  
Traditional Uses ◽  
Ancient Times ◽  
Analgesic Activities ◽  
First Time

AbstractThe genus Santolina is a taxonomically complex group of plant species widely distributed in the Mediterranean flora and used in traditional medicine since ancient times for their biological properties, including antimicrobial, anti-inflammatory, antispasmodic, digestive, and analgesic activities. Phytochemical investigations of Santolina species have revealed the presence of terpenoids as the main bioactive constituents of the genus. Coumarins and flavonoids were also identified. This review deals, for the first time, with information on the traditional uses, chemical profile, and biological properties of plants of the genus Santolina in order to provide input for future research prospects.

scholarly journals Effect of the Modifications on the Physicochemical and Biological Properties of β-Glucan—A Critical Review

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 57 ◽  
Author(s):  
Hongjie Yuan ◽  
Ping Lan ◽  
Yan He ◽  
Chengliang Li ◽  
Xia Ma
Keyword(s):  
Food Processing ◽  
Triple Helix ◽  
Functional Foods ◽  
Physiological Function ◽  
Biological Activities ◽  
Structural Features ◽  
Biological Properties ◽  
Enzymatic Modification ◽  
Anti Oxidant

β-Glucan exhibits many biological activities and functions such as stimulation of the immune system and anti-inflammatory, anti-microbial, anti-infective, anti-viral, anti-tumor, anti-oxidant, anti-coagulant, cholesterol-lowering, radio protective, and wound healing effects. It has a wide variety of uses in pharmaceutical, cosmetic, and chemical industries as well as in food processing units. However, due to its dense triple helix structure, formed by the interaction of polyhydroxy groups in the β-d-glucan molecule, it features poor solubility, which not only constrains its applications, but also inhibits its physiological function in vivo. One aim is to expand the applications for modified β-glucan with potential to prevent disease, various therapeutic purposes and as health-improving ingredients in functional foods and cosmetics. This review introduces the major modification methods required to understand the bioactivity of β-glucan and critically provides a literature survey on the structural features of this molecule and reported biological activity. We also discuss a new method to create novel opportunities to exploit maximally various properties of β-glucan, namely ultrasound-assisted enzymatic modification.

scholarly journals Cornus mas L. Stones: A Valuable by-Product as an Ellagitannin Source with High Antioxidant Potential

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4646
Author(s):  
Dominika Przybylska ◽  
Alicja Z. Kucharska ◽  
Iwona Cybulska ◽  
Tomasz Sozański ◽  
Narcyz Piórecki ◽  
...  
Keyword(s):  
Biological Activities ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
Raw Material ◽  
Hydrolyzable Tannins ◽  
Cornus Mas ◽  
Fruit Processing ◽  
High Antioxidant Activity ◽  
Total Polyphenolic Content ◽  
First Time

The stone of Cornus mas L. remains the least known morphological part of this plant, whereas the fruit is appreciated for both consumption purposes and biological activity. The stone is considered to be a byproduct of fruit processing and very little is known about its phytochemical composition and biological properties. In this study, the complete qualitative determination of hydrolyzable tannins, their quantitative analysis, total polyphenolic content, and antioxidant properties of the stone of C. mas are presented for the first time. The 37 identified compounds included the following: various gallotannins (11), monomeric ellagitannins (7), dimeric ellagitannins (10), and trimeric ellagitannins (7). The presence of free gallic acid and ellagic acid was also reported. Our results demonstrate that C. mas stone is a source of various bioactive hydrolyzable tannins and shows high antioxidant activity which could allow potential utilization of this raw material for recovery of valuable pharmaceutical or nutraceutical substances. The principal novelty of our findings is that hydrolyzable tannins, unlike other polyphenols, have been earlier omitted in the evaluation of the biological activities of C. mas. Additionally, the potential recovery of these bioactive chemicals from the byproduct is in line with the ideas of green chemistry and sustainable production.

scholarly journals Synthesis of Imidazole-Based Medicinal Molecules Utilizing the van Leusen Imidazole Synthesis

2020 ◽  
Vol 13 (3) ◽  
pp. 37 ◽  
Author(s):  
Xunan Zheng ◽  
Zhengning Ma ◽  
Dawei Zhang
Keyword(s):  
Drug Discovery ◽  
Chemical Synthesis ◽  
Small Molecules ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Structural Features ◽  
Pharmaceutical Companies ◽  
Recent Developments ◽  
Van Leusen Reaction

Imidazole and its derivatives are one of the most vital and universal heterocycles in medicinal chemistry. Owing to their special structural features, these compounds exhibit a widespread spectrum of significant pharmacological or biological activities, and are widely researched and applied by pharmaceutical companies for drug discovery. The van Leusen reaction based on tosylmethylisocyanides (TosMICs) is one of the most appropriate strategies to synthetize imidazole-based medicinal molecules, which has been increasingly developed on account of its advantages. In this review, we summarize the recent developments of the chemical synthesis and bioactivity of imidazole-containing medicinal small molecules, utilizing the van Leusen imidazole synthesis from 1977.

scholarly journals Uncovering Novel Peptide Chemistry from Bacterial Natural Products

2021 ◽  
Vol 75 (6) ◽  
pp. 543-547
Author(s):  
Florian Hubrich ◽  
Alessandro Lotti ◽  
Thomas A. Scott ◽  
Jörn Piel
Keyword(s):  
Natural Products ◽  
Bioactive Peptides ◽  
Biological Activities ◽  
Biological Properties ◽  
Post Translational Modifications ◽  
Peptide Chemistry ◽  
Chemical Structures ◽  
Therapeutic Value ◽  
Modified Peptides ◽  
Unique Chemical

Nature has evolved a remarkable array of biosynthetic enzymes that install diverse chemistries into natural products (NPs), bestowing them with a range of important biological properties that are of considerable therapeutic value. This is epitomized by the ribosomally synthesized and post-translationally modified peptides (RiPPs), a class of peptide natural products that undergo extensive post-translational modifications to produce structurally diverse bioactive peptides. In this review, we provide an overview of our research into the proteusin RiPP family, describing characterized members and the maturation enzymes responsible for their unique chemical structures and biological activities. The diverse enzymology identified in the first two proteusin pathways highlights the enormous potential of the RiPP class for new lead structures and novel pharmacophore-installing maturases as biocatalytic tools for drug discovery efforts.

scholarly journals Phytochemical Profile and Biological Properties of Colchicum triphyllum (Meadow Saffron)

Foods ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 457 ◽  
Author(s):  
Biancamaria Senizza ◽  
Gabriele Rocchetti ◽  
Murat Ali Okur ◽  
Gokhan Zengin ◽  
Evren Yıldıztugay ◽  
...  
Keyword(s):  
High Performance ◽  
Biological Activities ◽  
Reducing Power ◽  
Extraction Methods ◽  
Biological Properties ◽  
Leaf Extracts ◽  
Antioxidant Power ◽  
Phytochemical Profile ◽  
First Time

In this work, the phytochemical profile and the biological properties of Colchicum triphyllum (an unexplored Turkish cultivar belonging to Colchicaceae) have been comprehensively investigated for the first time. Herein, we focused on the evaluation of the in vitro antioxidant and enzyme inhibitory effects of flower, tuber, and leaf extracts, obtained using different extraction methods, namely maceration (both aqueous and methanolic), infusion, and Soxhlet. Besides, the complete phenolic and alkaloid untargeted metabolomic profiling of the different extracts was investigated. In this regard, ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) allowed us to putatively annotate 285 compounds when considering the different matrix extracts, including mainly alkaloids, flavonoids, lignans, phenolic acids, and tyrosol equivalents. The most abundant polyphenols were flavonoids (119 compounds), while colchicine, demecolcine, and lumicolchicine isomers were some of the most widespread alkaloids in each extract analyzed. In addition, our findings showed that C. triphyllum tuber extracts were a superior source of both total alkaloids and total polyphenols, being on average 2.89 and 10.41 mg/g, respectively. Multivariate statistics following metabolomics allowed for the detection of those compounds most affected by the different extraction methods. Overall, C. triphyllum leaf extracts showed a strong in vitro antioxidant capacity, in terms of cupric reducing antioxidant power (CUPRAC; on average 96.45 mg Trolox Equivalents (TE)/g) and ferric reducing antioxidant power (FRAP) reducing power (on average 66.86 mg TE/g). Interestingly, each C. triphyllum methanolic extract analyzed (i.e., from tuber, leaf, and flower) was active against the tyrosinase in terms of inhibition, recording the higher values for methanolic macerated leaves (i.e., 125.78 mg kojic acid equivalent (KAE)/g). On the other hand, moderate inhibitory activities were observed against AChE and α-amylase. Strong correlations (p < 0.01) were also observed between the phytochemical profiles and the biological activities determined. Therefore, our findings highlighted, for the first time, the potential of C. triphhyllum extracts in food and pharmaceutical applications.

Medicinal Potential of Heterocyclic Compounds from Diverse Natural Sources for the Management of Cancer

2020 ◽  
Vol 20 (11) ◽  
pp. 942-957
Author(s):  
Manjinder Singh ◽  
Pratibha Sharma ◽  
Pankaj Kumar Singh ◽  
Thakur Gurjeet Singh ◽  
Balraj Saini
Keyword(s):  
Natural Products ◽  
Biological Properties ◽  
Chemotherapeutic Agents ◽  
Marine Organisms ◽  
New Era ◽  
Complex Disorders ◽  
Chemical Structures ◽  
Action Mechanisms ◽  
Anti Cancer ◽  
Micro Organisms

Natural products form a significant portion of medicinal agents that are currently used for the management of cancer. All these natural products have unique structures along with diverse action mechanisms with the capacity to interact with different therapeutic targets of several complex disorders. Although plants contribute as a major source of natural products with anti-cancer potential, the marine environment and microbes have also bestowed some substantial chemotherapeutic agents. A few examples of anti-cancer agents of natural origin include vincristine, vinblastine, paclitaxel, camptothecin and topotecan obtained from plants, bryostatins, sarcodictyin and cytarabine from marine organisms and bleomycin and doxorubicin from micro-organisms (dactinomycin, bleomycin and doxorubicin). The incredible diversity in the chemical structures and biological properties of compounds obtained from million species of plants, marine organisms and microorganisms present in nature has commenced a new era of potential therapeutic anti-cancer agents.

scholarly journals Chemistry and Biology of Bioactive Glycolipids of Marine Origin

Marine Drugs ◽  
2018 ◽  
Vol 16 (9) ◽  
pp. 294 ◽  
Author(s):  
Iván Cheng-Sánchez ◽  
Francisco Sarabia
Keyword(s):  
Natural Products ◽  
Chemical Synthesis ◽  
Broad Class ◽  
Structural Features ◽  
Biological Properties ◽  
Present Review ◽  
Marine Origin ◽  
Structural Variety

Glycolipids represent a broad class of natural products structurally featured by a glycosidic fragment linked to a lipidic molecule. Despite the large structural variety of these glycoconjugates, they can be classified into three main groups, i.e., glycosphingolipids, glycoglycerolipids, and atypical glycolipids. In the particular case of glycolipids derived from marine sources, an impressive variety in their structural features and biological properties is observed, thus making them prime targets for chemical synthesis. In the present review, we explore the chemistry and biology of this class of compounds.

scholarly journals Coumarin sulfonamide derivatives: An emerging class of therapeutic agents

2020 ◽  
Vol 26 (1) ◽  
pp. 46-59 ◽  
Author(s):  
Ali Irfan ◽  
Laila Rubab ◽  
Mishbah Ur Rehman ◽  
Rukhsana Anjum ◽  
Sami Ullah ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Structural Features ◽  
Therapeutic Agents ◽  
Review Article ◽  
Structural Motif ◽  
Structure Activity ◽  
Anti Cancer ◽  
Novel Therapeutic

AbstractCoumarin sulfonamide is a heterocyclic pharmacophore and an important structural motif which is a core and integral part of different therapeutic scaffolds and analogues. Coumarin sulfonamides are privileged and pivotal templates which have a broad spectrum of applications in the fields of medicine, pharmacology and pharmaceutics. Coumarin sulfonamide exhibited versatile and myriad biomedical activities such as anti-bacterial, antiviral, antifungal, anti-inflammatory and anti-cancer. This review article focuses on the structural features of coumarin sulfonamide derivatives in the treatment of different lethal diseases on the basis of structure-activity relationships (SAR). The plethora of research cited in this review article summarizes and discusses the various substitutions around the coumarin sulfonamide nucleus which have provided a wide spectrum of biological activities and therapeutic potential that has proved attractive to many researchers looking to exploit the coumarin sulfonamide skeleton for drug discovery and the development of novel therapeutic agents.

Sign in / Sign up

Export Citation Format

Share Document