scholarly journals Antitumor Profile of Carbon-Bridged Steroids (CBS) and Triterpenoids

Marine Drugs ◽  
2021 ◽  
Vol 19 (6) ◽  
pp. 324
Author(s):  
Valery M. Dembitsky ◽  
Tatyana A. Gloriozova ◽  
Vladimir V. Poroikov
Keyword(s):  
Confidence Level ◽  
Marine Invertebrates ◽  
Biological Activities ◽  
Cyclopropane Ring ◽  
Fungal Endophytes ◽  
Marine Sponges ◽  
Lymphocytic Leukemia ◽  
Moderate Activity ◽  
Activity Levels ◽  
Wide Range

This review focuses on the rare group of carbon-bridged steroids (CBS) and triterpenoids found in various natural sources such as green, yellow-green, and red algae, marine sponges, soft corals, ascidians, starfish, and other marine invertebrates. In addition, this group of rare lipids is found in amoebas, fungi, fungal endophytes, and plants. For convenience, the presented CBS and triterpenoids are divided into four groups, which include: (a) CBS and triterpenoids containing a cyclopropane group; (b) CBS and triterpenoids with cyclopropane ring in the side chain; (c) CBS and triterpenoids containing a cyclobutane group; (d) CBS and triterpenoids containing cyclopentane, cyclohexane or cycloheptane moieties. For the comparative characterization of the antitumor profile, we have added several semi- and synthetic CBS and triterpenoids, with various additional rings, to identify possible promising sources for pharmacologists and the pharmaceutical industry. About 300 CBS and triterpenoids are presented in this review, which demonstrate a wide range of biological activities, but the most pronounced antitumor profile. The review summarizes biological activities both determined experimentally and estimated using the well-known PASS software. According to the data obtained, two-thirds of CBS and triterpenoids show moderate activity levels with a confidence level of 70 to 90%; however, one third of these lipids demonstrate strong antitumor activity with a confidence level exceeding 90%. Several CBS and triterpenoids, from different lipid groups, demonstrate selective action on different types of tumor cells such as renal cancer, sarcoma, pancreatic cancer, prostate cancer, lymphocytic leukemia, myeloid leukemia, liver cancer, and genitourinary cancer with varying degrees of confidence. In addition, the review presents graphical images of the antitumor profile of both individual CBS and triterpenoids groups and individual compounds.

scholarly journals Sulfated and Sulfur-Containing Steroids and Their Pharmacological Profile

Marine Drugs ◽  
2021 ◽  
Vol 19 (5) ◽  
pp. 240
Author(s):  
Tatyana A. Pounina ◽  
Tatyana A. Gloriozova ◽  
Nick Savidov ◽  
Valery M. Dembitsky
Keyword(s):  
Antitumor Activity ◽  
Confidence Level ◽  
Biological Activities ◽  
Marine Sponges ◽  
Bioactive Lipids ◽  
Pharmacological Profile ◽  
Wide Range ◽  
Sulfated Steroids ◽  
Strong Antitumor Activity ◽  
Sulfur Containing

The review focuses on sulfated steroids that have been isolated from seaweeds, marine sponges, soft corals, ascidians, starfish, and other marine invertebrates. Sulfur-containing steroids and triterpenoids are sourced from sedentary marine coelenterates, plants, marine sediments, crude oil, and other geological deposits. The review presents the pharmacological profile of sulfated steroids, sulfur-containing steroids, and triterpenoids, which is based on data obtained using the PASS program. In addition, several semi-synthetic and synthetic epithio steroids, which represent a rare group of bioactive lipids that have not yet been found in nature, but possess a high level of antitumor activity, were included in this review for the comparative pharmacological characterization of this class of compounds. About 140 steroids and triterpenoids are presented in this review, which demonstrate a wide range of biological activities. Therefore, out of 71 sulfated steroids, thirteen show strong antitumor activity with a confidence level of more than 90%, out of 50 sulfur-containing steroids, only four show strong antitumor activity with a confidence level of more than 93%, and out of eighteen epithio steroids, thirteen steroids show strong antitumor activity with a confidence level of 91% to 97.4%.

scholarly journals In Silico Prediction of Steroids and Triterpenoids as Potential Regulators of Lipid Metabolism

Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 650
Author(s):  
Valery M. Dembitsky
Keyword(s):  
Lipid Metabolism ◽  
Marine Invertebrates ◽  
Cholesterol Metabolism ◽  
Biological Activities ◽  
Fungal Endophytes ◽  
Marine Sponges ◽  
Parkinson’S Diseases ◽  
Degree Of Certainty ◽  
High Degree ◽  
Rare Group

This review focuses on a rare group of steroids and triterpenoids that share common properties as regulators of lipid metabolism. This group of compounds is divided by the type of chemical structure, and they represent: aromatic steroids, steroid phosphate esters, highly oxygenated steroids such as steroid endoperoxides and hydroperoxides, α,β-epoxy steroids, and secosteroids. In addition, subgroups of carbon-bridged steroids, neo steroids, miscellaneous steroids, as well as synthetic steroids containing heteroatoms S (epithio steroids), Se (selena steroids), Te (tellura steroids), and At (astatosteroids) were presented. Natural steroids and triterpenoids have been found and identified from various sources such as marine sponges, soft corals, starfish, and other marine invertebrates. In addition, this group of rare lipids is found in fungi, fungal endophytes, and plants. The pharmacological profile of the presented steroids and triterpenoids was determined using the well-known computer program PASS, which is currently available online for all interested scientists and pharmacologists and is currently used by research teams from more than 130 countries of the world. Our attention has been focused on the biological activities of steroids and triterpenoids associated with the regulation of cholesterol metabolism and related processes such as anti-hyperlipoproteinemic activity, as well as the treatment of atherosclerosis, lipoprotein disorders, or inhibitors of cholesterol synthesis. In addition, individual steroids and triterpenoids were identified that demonstrated rare or unique biological activities such as treating neurodegenerative diseases, Alzheimer’s, and Parkinson’s diseases with a high degree of certainty over 95 percent. For individual steroids or triterpenoids or a group of compounds, 3D drawings of their predicted biological activities are presented.

scholarly journals Natural Product Repertoire of the Genus Amphimedon

Marine Drugs ◽  
2018 ◽  
Vol 17 (1) ◽  
pp. 19 ◽  
Author(s):  
Nourhan Shady ◽  
Mostafa Fouad ◽  
Mohamed Salah Kamel ◽  
Tanja Schirmeister ◽  
Usama Abdelmohsen
Keyword(s):  
Secondary Metabolites ◽  
Natural Product ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Marine Sponges ◽  
Rich Source ◽  
Undescribed Species ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Complete Survey

Marine sponges are a very attractive and rich source in the production of novel bioactive compounds. The sponges exhibit a wide range of pharmacological activities. The genus Amphimedon consists of various species, such as viridis, compressa, complanata, and terpenensis, along with a handful of undescribed species. The Amphimedon genus is a rich source of secondary metabolites containing diverse chemical classes, including alkaloids, ceramides, cerebrososides, and terpenes, with various valuable biological activities. This review covers the literature from January 1983 until January 2018 and provides a complete survey of all the compounds isolated from the genus Amphimedon and the associated microbiota, along with their corresponding biological activities, whenever applicable.

scholarly journals The Extracts of Some Marine Invertebrates and Algae Collected off the Coast Waters of Vietnam Induce the Inhibitory Effects on the Activator Protein-1 Transcriptional Activity in JB6 Cl41 Cells

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
S. N. Fedorov ◽  
V. B. Krasokhin ◽  
L. K. Shubina ◽  
S. A. Dyshlovoy ◽  
N. H. Nam ◽  
...  
Keyword(s):  
Transcriptional Activity ◽  
Marine Invertebrates ◽  
Biological Activities ◽  
Marine Sponges ◽  
Marine Organisms ◽  
Biologically Active ◽  
Luciferase Reporter ◽  
Nuclear Factor ◽  
Inhibitory Effects ◽  
Luciferase Reporter Gene

It has previously been shown that inhibition of the transcriptional activity of the oncogenic nuclear factor AP-1 can result in cancer prevention. Marine invertebrates and alga are a rich source of natural compounds that possess various biological activities. The inhibitory effects of the extracts of Vietnamese marine organisms in relation to the AP-1 transcriptional activity were examined by the luciferase method using JB6 Cl41 cells stably expressing a luciferase reporter gene controlled by AP-1 DNA binding sequence. As was found, 71 species of marine sponges out of 148 species studied contain inhibitors of the AP-1 transcriptional activity. Therefore, marine organisms as a source of biologically active compounds have a great potential for isolation of the new cancer preventive compounds that inhibit the oncogenic AP-1 nuclear factor.

scholarly journals In Vitro and In Vivo Assessment of the Efficacy of Bromoageliferin, an Alkaloid Isolated from the Sponge Agelas dilatata, against Pseudomonas aeruginosa

Marine Drugs ◽  
2020 ◽  
Vol 18 (6) ◽  
pp. 326
Author(s):  
Dawrin Pech-Puch ◽  
Mar Pérez-Povedano ◽  
Marta Martinez-Guitian ◽  
Cristina Lasarte-Monterrubio ◽  
Juan Carlos Vázquez-Ucha ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Carboxylic Acid ◽  
Galleria Mellonella ◽  
Biological Activities ◽  
Marine Sponges ◽  
In Vitro Assays ◽  
Significant Activity ◽  
Wide Range

The pyrrole-imidazoles, a group of alkaloids commonly found in marine sponges belonging to the genus Agelas, display a wide range of biological activities. Herein, we report the first chemical study of the secondary metabolites of the sponge A. dilatata from the coastal area of the Yucatan Peninsula (Mexico). In this study, we isolated eight known alkaloids from an organic extract of the sponge. We used NMR and MS analysis and comparison with existing databases to characterize the alkaloids: ageliferin (1), bromoageliferin (2), dibromoageliferin (3), sceptrin (4), nakamuric acid (5), 4-bromo-1H-pyrrole-2-carboxylic acid (6), 4,5-dibromopyrrole-2-carboxylic acid (7) and 3,7-dimethylisoguanine (8). We also evaluated, for the first time, the activity of these alkaloids against the most problematic multidrug-resistant (MDR) pathogens, i.e., the Gram-negative bacteria Pseudomonas aeruginosa, Klebsiella pneumoniae and Acinetobacter baumannii. Bromoageliferin (2) displayed significant activity against P. aeruginosa. Comparison of the antibacterial activity of ageliferins 1–3 (of similar structure) against P. aeruginosa revealed some relationship between structure and activity. Furthermore, in in vitro assays, 2 inhibited growth and biofilm production in clinical strains of P. aeruginosa. Moreover, 2 increased the survival time in an in vivo Galleria mellonella model of infection. The findings confirm bromoageliferin (2) as a potential lead for designing new antibacterial drugs.

Improvement of cytoprotective and antioxidant activity of Rosa canina L. and Salix alba L. by controlled differential sieving process against H2O2-induced oxidative stress in mouse primary splenocytes

2017 ◽  
Vol 87 (3-4) ◽  
pp. 191-200 ◽  
Author(s):  
Nidhal Soualeh ◽  
Aliçia Stiévenard ◽  
Elie Baudelaire ◽  
Rachid Soulimani ◽  
Jaouad Bouayed
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Good Alternative ◽  
Activity Levels ◽  
Salix Alba ◽  
Rosa Canina ◽  
Free Process ◽  
Plant Powders ◽  
Sieving Process

Abstract. In this study, cytoprotective and antioxidant activities of Rosa canina (RC) and Salix alba (SA), medicinal plants, were studied on mouse primary splenocytes by comparing Controlled Differential Sieving process (CDSp), which is a novel green solvent-free process, versus a conventional technique, employing hydroethanolic extraction (HEE). Thus, preventive antioxidant activity of three plant powders of homogeneous particle sizes, 50–100 µm, 100–180 µm and 180–315 µm, dissolved directly in the cellular buffer, were compared to those of hydroethanolic (HE) extract, at 2 concentrations (250 and 500 µg/mL) in H2O2-treated spleen cells. Overall, compared to HE extract, the superfine powders, i. e., fractions < 180 µm, at the lowest concentration, resulted in greater reactive oxygen species (ROS) elimination, increased glutathione peroxidase (GPx) activity and lower malondialdehyde (MDA) production. Better antioxidant and preventive effects in pre-treated cells were found with the superfine powders for SA (i. e., 50–100 µm and 100–180 µm, both p < 0.001), and with the intermediate powder for RC (i. e., 100–180 µm, p < 0.05) versus HE extract. The activity levels of catalase (CAT) and superoxide dismutase (SOD) in pretreated splenocytes exposed to H2O2, albeit reduced, were near to those in unexposed cells, suggesting that pretreatment with the fine powders has relatively restored the normal levels of antioxidant-related enzymes. These findings supported that CDSp improved the biological activities of plants, avoiding the use of organic solvents and thus it could be a good alternative to conventional extraction techniques.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

Synthesis, Characterization and Antiproliferative Activity Assessment of a Novel 1H-5-mercapto-1,2,4 Triazole Derivative

2017 ◽  
Vol 68 (4) ◽  
pp. 745-747 ◽  
Author(s):  
Marius Mioc ◽  
Sorin Avram ◽  
Vasile Bercean ◽  
Mihaela Balan Porcarasu ◽  
Codruta Soica ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Vascular Endothelial ◽  
Triazole Derivative ◽  
Activity Assessment ◽  
Wide Range ◽  
Specific Receptors ◽  
Endothelial Growth Factor ◽  
Selection Of

Angiogenesis plays an important function in tumor proliferation, one of the main angiogenic promoters being the vascular endothelial growth factor (VEGF) which activates specific receptors, particularly VEGFR-2. Thus, VEGFR-2 has become an essential therapeutic target in the development of new antitumor drugs. 1,2,4-triazoles show a wide range of biological activities, including antitumor effect, which was documented by numerous reports. In the current study the selection of 5-mercapto-1,2,4-triazole structure (1H-3-styryl-5-benzylidenehydrazino-carbonyl-methylsulfanil-1,2,4-triazole, Tz3a.7) was conducted based on molecular docking that emphasized it as suitable ligand for VEGFR-2 and EGFR1 receptors. Compound Tz3a.7 was synthesized and physicochemically and biologically evaluated thus revealing a moderate antiproliferative activity against breast cancer cell line MDA-MB-231.

Potential Triazole-based Molecules for the Treatment of Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4403-4434 ◽  
Author(s):  
Susimaire Pedersoli Mantoani ◽  
Peterson de Andrade ◽  
Talita Perez Cantuaria Chierrito ◽  
Andreza Silva Figueredo ◽  
Ivone Carvalho
Keyword(s):  
Effective Treatment ◽  
Chagas Disease ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Neglected Diseases ◽  
Triazole Derivatives ◽  
Wide Range ◽  
The World ◽  
Great Relevance ◽  
The Moment

Neglected Diseases (NDs) affect million of people, especially the poorest population around the world. Several efforts to an effective treatment have proved insufficient at the moment. In this context, triazole derivatives have shown great relevance in medicinal chemistry due to a wide range of biological activities. This review aims to describe some of the most relevant and recent research focused on 1,2,3- and 1,2,4-triazolebased molecules targeting four expressive NDs: Chagas disease, Malaria, Tuberculosis and Leishmaniasis.

Structural and Bioactive Studies of Halogenated Constituents from Sponges

2020 ◽  
Vol 27 (14) ◽  
pp. 2335-2360 ◽  
Author(s):  
Chao Li ◽  
Dayong Shi
Keyword(s):  
Microbial Communities ◽  
Organic Compounds ◽  
Biological Activities ◽  
Marine Sponges ◽  
Nitrogen Compounds ◽  
Halogenated Organic Compounds ◽  
Bioactive Natural Products ◽  
The Past ◽  
Tyrosine Derivatives ◽  
Polyunsaturated Lipids

: Marine organisms are abundant sources of bioactive natural products. Among metabolites produced by sponges and their associated microbial communities, halogenated natural compounds accounted for an important part due to their potent biological activities. The present review updates and compiles a total of 258 halogenated organic compounds isolated in the past three decades, especially brominated derivatives derived from 31 genera of marine sponges. These compounds can be classified as the following classes: brominated polyunsaturated lipids, nitrogen compounds, brominated tyrosine derivatives and other halogenated compounds. These substances were listed together with their source organisms, structures and bioactivities. For this purpose, 84 references were consulted.

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