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 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 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.

Synthesis, Antioxidant and Antitumor Activity of Some Substituted 9-Anilinoacridine and 4-Anilinoquinolines Derivatives

2018 ◽  
Vol 15 (6) ◽  
pp. 846-852 ◽  
Author(s):  
Fatimah A. Agili
Keyword(s):  
Antioxidant Activity ◽  
Antitumor Activity ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Breast Adenocarcinoma ◽  
Liver Carcinoma ◽  
Quinoline Derivatives ◽  
Wide Range ◽  
Anti Cancer ◽  
Radical Scavenging Ability

Background: Acridine and quinoline derivatives have a wide range of biological activities such as antioxidant and antitumor where quinoline derivatives intercalate between base pairs of double-stranded DNA through π-π interactions. Therefore, the development of new compounds with antitumor activity could be an important therapeutic strategy against this metabolic syndrome. Objective: This study was undertaken to synthesize different series of new anilinoacridines and anlinoquinoline with different substituents having biological activity. Materials and Methods: A series of new anilinoacridines and anlinoquinoline with different substituents was prepared by condensation of methyl 3-amino-4-methoxybenzoate hydrochloride with 9- chloroacridine and 4- chloroquinoline to give the target derivatives. Results: New anilinoacridines and anlinoquinoline with different substituents have been synthesized as antioxidant and anti-cancer agents. The structure of the synthesized compounds was confirmed by using spectral methods (FT-IR, 1H-NMR). The antioxidant activity of the synthesized compounds was evaluated by using DPPH radical scavenging ability. Also, the anti-cancer activity was evaluated using lung carcinoma, breast adenocarcinoma and liver carcinoma. The developed compounds 4a, b, 5a,b, 7a,b and 8a,b have shown a potent antioxidant activity. On the other hand, 4a, b, 5a and 7a exhibited the best antitumor activity against both A-549 and MCF7 cancer cells. Conclusion: For the active developed compounds, the most active antioxidant and antitumor one was 4a which registered the highest radical scavenging as well as antitumor activity.

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.

scholarly journals SYNTHESIS OF N-ALKYL AMINO LACTAM DERIVATIVES

2018 ◽  
Vol 54 (2C) ◽  
pp. 291
Author(s):  
Phi Thi Dao
Keyword(s):  
Natural Products ◽  
Antitumor Activity ◽  
Alkyl Group ◽  
Structural Variation ◽  
Biological Activities ◽  
Biological Studies ◽  
Wide Range

Bengamides are sponge-derived natural products of mixed biosynthesis (polyketides andamino acids), the first two members, isolated from Jaspidae sponges in coral surrounding Fijiislands, were reported in 1986. The main structural variation is located on the 3-aminocaprolactam moiety, and displays a wide range of biological activities, includingantitumor, antibiotic, and anthelmintic properties. These interesting biological activities havemade bengamides popular targets for synthesis and biological studies. There have been somereports on diverse modifications of the caprolactame unit, and indication that N-substitution oncaprolactam greatly influences the antitumor activity. In this paper, we reported the method forsynthesis of 6 amino lactams containing an additional N-alkyl group (4a-4c) and (8a-8c) forfurther synthesis of new bengamide analogues. Their structures were established by MS andNMR spectroscopies.

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.

Heterocycle Compounds with Antimicrobial Activity

2020 ◽  
Vol 26 (8) ◽  
pp. 867-904 ◽  
Author(s):  
Maria Fesatidou ◽  
Anthi Petrou ◽  
Geronikaki Athina
Keyword(s):  
Heterocyclic Compounds ◽  
Bacterial Infections ◽  
Scientific Community ◽  
Antimicrobial Agents ◽  
Fungal Infections ◽  
Biological Activities ◽  
Literature Survey ◽  
New Findings ◽  
Wide Range ◽  
Number Of Microorganisms

Background: Bacterial infections are a growing problem worldwide causing morbidity and mortality mainly in developing countries. Moreover, the increased number of microorganisms, developing multiple resistances to known drugs, due to abuse of antibiotics, is another serious problem. This problem becomes more serious for immunocompromised patients and those who are often disposed to opportunistic fungal infections. Objective: The objective of this manuscript is to give an overview of new findings in the field of antimicrobial agents among five-membered heterocyclic compounds. These heterocyclic compounds especially five-membered attracted the interest of the scientific community not only for their occurrence in nature but also due to their wide range of biological activities. Method: To reach our goal, a literature survey that covers the last decade was performed. Results: As a result, recent data on the biological activity of thiazole, thiazolidinone, benzothiazole and thiadiazole derivatives are mentioned. Conclusion: It should be mentioned that despite the progress in the development of new antimicrobial agents, there is still room for new findings. Thus, research still continues.

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