Abstract:
:This work describes the synthesis and biological evaluation of a new heterocyclic hybrid derived from the ellipticine and the marine alkaloid makaluvamine A. Pyridoquinoxalinedione 12 was obtained in seven steps with 6.5% overall yield. 12 and its intermediates 1-11 were evaluated for their in vitro cytotoxic activity against different cancer cell lines and tested for their inhibitory activity against the human DNA topoisomerase II. The analysis by electrophoresis shows that the pentacycle 12 inhibits the topoisomerase II like doxorubicine at 100 µM. Compound 9 was found to have an interesting profile, having a cytotoxicity of 15, 15, 15 and 10 μM against Caco-2, HCT-116, Pc-3 and NCI cell lines respectively, without any noticeable toxicity against human fibroblast.
journal_name
Mar Drugsjournal_title
Marine drugsauthors
Boucle S,Melin C,Clastre M,Guillard Jdoi
10.3390/md13010655subject
Has Abstractpub_date
2015-01-19 00:00:00pages
655-65issue
1issn
1660-3397pii
md13010655journal_volume
13pub_type
杂志文章相关文献
Marine Drugs文献大全abstract::The dinoflagellate Prorocentrum belizeanum is responsible for the production of several toxins involved in the red tide phenomenon known as Diarrhetic Shellfish Poisoning (DSP). In this paper we report on the biosynthetic origin of an okadaic acid water-soluble ester derivative, DTX5c, on the basis of the spectroscopi...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md10102234
更新日期:2012-10-01 00:00:00
abstract::Genome mining has become an increasingly powerful, scalable, and economically accessible tool for the study of natural product biosynthesis and drug discovery. However, there remain important biological and practical problems that can complicate or obscure biosynthetic analysis in genomic and metagenomic sequencing pr...
journal_title:Marine drugs
pub_type: 杂志文章,评审
doi:10.3390/md15060165
更新日期:2017-06-06 00:00:00
abstract::In our continuous chemical investigation on the marine-derived fungus Dichotomomyces cejpii F31-1, two new polyketides dichocetides B-C (1, 2), two new alkaloids dichotomocejs E-F (3, 4), and three known fumiquinozalines: scequinadoline A (5), quinadoline A (6), and scequinadoline E (7) were discovered from the cultur...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md16070229
更新日期:2018-07-06 00:00:00
abstract::Marine organisms produce secondary metabolites that may be valuable for the development of novel drug leads as such and can also provide structural scaffolds for the design and synthesis of novel bioactive compounds. The marine alkaloids, clathrodin and oroidin, which were originally isolated from sponges of the genus...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md12020940
更新日期:2014-02-14 00:00:00
abstract::Cone snails produce a distinctive repertoire of venom peptides that are used both as a defense mechanism and also to facilitate the immobilization and digestion of prey. These peptides target a wide variety of voltage- and ligand-gated ion channels, which make them an invaluable resource for studying the properties of...
journal_title:Marine drugs
pub_type: 杂志文章,评审
doi:10.3390/md10061244
更新日期:2012-06-01 00:00:00
abstract::Lung cancer is the leading cause of cancer mortality worldwide and non-small-cell lung cancer (NSCLC) is the most common type. Marine plants provide rich resources for anticancer drug discovery. Fucoxanthin (FX), a Laminaria japonica extract, has attracted great research interest for its antitumor activities. Accumula...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md15020039
更新日期:2017-02-15 00:00:00
abstract::Mere15 is a novel polypeptide from Meretrix meretrix Linnaeus with cytotoxicity in solid cancer cells. In this study, we investigated its activity on human K562 chronic myelogenous leukemia cells. Mere15 inhibited the growth of K562 cells with IC₅₀ values of 38.2 μg/mL. Mere15 also caused concentration dependent induc...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md10112596
更新日期:2012-11-21 00:00:00
abstract::Four new sesquiterpene lactones (3, 4, 6 and 7) and three known compounds, purpuride (1), berkedrimane B (2) and purpuride B (5), were isolated from the marine fungus, Talaromyces minioluteus (Penicillium minioluteum). New compounds were drimane sesquiterpenes conjugated with N-acetyl-l-valine, and their structures we...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md13063567
更新日期:2015-06-05 00:00:00
abstract::Three major forms of the nicotinic agonist toxin anabaseine (cyclic iminium, cyclic imine and the monocationic open-chain ammonium-ketone) co-exist in almost equal concentrations at physiological pH. We asked the question: Which of these forms is pharmacologically active? First, we investigated the pH dependence of an...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md17110614
更新日期:2019-10-29 00:00:00
abstract::Three new benzofuranoids, asperfuranoids A-C (1-3), two new phenylpropanoid derivatives (6 and 7), and nine known analogues (4, 5, and 8-14) were isolated from the liquid substrate fermentation cultures of the mangrove endopytic fungus Aspergillus sp. ZJ-68. The structures of the new compounds were determined by exten...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md17080478
更新日期:2019-08-18 00:00:00
abstract::Spirotetronates are actinomyces-derived polyketides that possess complex structures and exhibit potent and unexplored bioactivities. Due to their anticancer and antimicrobial properties, they have potential as drug hits and deserve further study. In particular, abyssomicin C and tetrocarcin A have shown significant pr...
journal_title:Marine drugs
pub_type: 杂志文章,评审
doi:10.3390/md17040232
更新日期:2019-04-19 00:00:00
abstract::Marine derived cyclo(Gly-l-Ser-l-Pro-l-Glu) was selected as a lead to evaluate antitumor-antibiotic activity. Histidine was chosen to replace the serine residue to form cyclo(Gly-l-His-l-Pro-l-Glu). Cyclic tetrapeptides (CtetPs) were then synthesized using a solution phase method, and subjected to antitumor and antibi...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md13053029
更新日期:2015-05-15 00:00:00
abstract::Cyclic imine toxins are neurotoxic, macrocyclic compounds produced by marine dinoflagellates. Mass spectrometric screenings of extracts from natural plankton assemblages revealed a high chemical diversity among this toxin class, yet only few toxins are structurally known. Here we report the structural characterization...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md16110446
更新日期:2018-11-14 00:00:00
abstract::Fish consumption is a potential route of human exposure to the hepatotoxic microcystins, especially in lakes and reservoirs that routinely experience significant toxic Microcystis blooms. Understanding the rates of uptake and elimination for microcystins as well as the transfer efficiency into tissues of consumers are...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md9122553
更新日期:2011-12-01 00:00:00
abstract::Over the past decades, a number of novel compounds, which are produced in the marine environment, have been found to exhibit the anticancer effects. This review focuses on molecular targets of marine-derived anticancer candidates in clinical and preclinical studies. They are kinases, transcription factors, histone dea...
journal_title:Marine drugs
pub_type: 杂志文章,评审
doi:10.3390/md16050175
更新日期:2018-05-22 00:00:00
abstract::Anemonia viridis is a widespread and extensively studied Mediterranean species of sea anemone from which a large number of polypeptide toxins, such as blood depressing substances (BDS) peptides, have been isolated. The first members of this class, BDS-1 and BDS-2, are polypeptides belonging to the β-defensin fold fami...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md11114213
更新日期:2013-10-30 00:00:00
abstract::A new alkaloid, 2-(furan-2-yl)-6-(2S,3S,4-trihydroxybutyl)pyrazine (1), along with 12 known compounds, 2-(furan-2-yl)-5-(2S,3S,4-trihydroxybutyl)pyrazine (2), (S)-4-isobutyl-3-oxo-3,4-dihydro-1H-pyrrolo[2,1-c][1,4]oxazine-6-carbaldehyde (3), (S)-4-isopropyl-3-oxo-3,4-dihydro-1H-pyrrolo[2,1-c][1,4]oxazine-6-carbaldehyd...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md12010477
更新日期:2014-01-21 00:00:00
abstract::Species in the genus Gambierdiscus produce ciguatoxins (CTXs) and/or maitotoxins (MTXs), which may cause ciguatera fish poisoning (CFP) in humans if contaminated fish are consumed. Species of Gambierdiscus have previously been isolated from macroalgae at Rangitahua (Raoul Island and North Meyer Islands, northern Kerma...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md15070219
更新日期:2017-07-11 00:00:00
abstract::In the last decades, research has focused on the capabilities of microbes to secrete exopolysaccharides (EPS), because these polymers differ from the commercial ones derived essentially from plants or algae in their numerous valuable qualities. These biopolymers have emerged as new polymeric materials with novel and u...
journal_title:Marine drugs
pub_type: 杂志文章,评审
doi:10.3390/md12053005
更新日期:2014-05-22 00:00:00
abstract::Nine new sulfated triterpene glycosides, magnumosides A₁ (1), A₂ (2), A₃ (3), A₄ (4), B₁ (5), B₂ (6), C₁ (7), C₂ (8) and C₄ (9) as well as a known colochiroside B₂ (10) have been isolated from the tropical Indo-West Pacific sea cucumber Neothynidium (=Massinium) magnum (Phyllophoridae, Dendrochirotida) collected in th...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md15080256
更新日期:2017-08-16 00:00:00
abstract::Chitosan has been the subject of interest for its use as a polymeric drug carrier material in dosage form design due to its appealing properties such as biocompatibility, biodegradability, low toxicity and relatively low production cost from abundant natural sources. However, one drawback of using this natural polysac...
journal_title:Marine drugs
pub_type: 杂志文章,评审
doi:10.3390/md8041305
更新日期:2010-04-19 00:00:00
abstract::Global incidence of type 2 diabetes has escalated over the past few decades, necessitating a continued search for natural sources of enzyme inhibitors to offset postprandial hyperglycemia. The objective of this study was to evaluate coastal Alaskan seaweed inhibition of α-glucosidase and α-amylase, two carbolytic enzy...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md12105277
更新日期:2014-10-22 00:00:00
abstract::In this review, we focus on processes, organs and systems targeted by the marine toxins yessotoxin (YTX), okadaic acid (OA) and palytoxin (PTX). The effects of YTX and their basis are analyzed from data collected in the mollusc Mytilus galloprovincialis, the annelid Enchytraeus crypticus, Swiss CD1 mice and invertebra...
journal_title:Marine drugs
pub_type: 杂志文章,评审
doi:10.3390/md8030658
更新日期:2010-03-16 00:00:00
abstract::The cultivation of macroalgae to supply the biofuel, pharmaceutical or food industries generates a considerable amount of organic residue, which represents a potential substrate for biomethanation. Its use optimizes the total resource exploitation by the simultaneous disposal of waste biomaterials. In this study, we e...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md13095947
更新日期:2015-09-18 00:00:00
abstract::Ecklonia cava (E. cava) can alleviate vascular dysfunction in diseases associated with poor circulation. E. cava contains various polyphenols with different functions, but few studies have compared the effects of these polyphenols. Here, we comparatively investigated four major compounds present in an ethanoic extract...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md16110441
更新日期:2018-11-09 00:00:00
abstract::Thirteen nitrogen-containing molecules (1a/1b and 2-12) were isolated from the Indonesian sponge Acanthostrongylophora ingens, highlighting the richness of this organism as a source of alkaloids. Their structures were elucidated using one- and two-dimensional NMR spectroscopy and HR-ESI-MS, while the stereochemistry o...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md17080472
更新日期:2019-08-15 00:00:00
abstract::Collagen has become a key-molecule in cell culture studies and in the tissue engineering field. Industrially, the principal sources of collagen are calf skin and bones which, however, could be associated to risks of serious disease transmission. In fact, collagen derived from alternative and riskless sources is requir...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md12094912
更新日期:2014-09-24 00:00:00
abstract::AIDS is a pandemic responsible for more than 35 million deaths. The emergence of resistant mutations due to drug use is the biggest cause of treatment failure. Marine organisms are sources of different molecules, some of which offer promising HIV-1 reverse transcriptase (RT) inhibitory activity, such as the diterpenes...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md11114127
更新日期:2013-10-29 00:00:00
abstract::The genus Streptomyces produces secondary metabolic compounds that are rich in biological activity. Many of these compounds are genetically encoded by large secondary metabolism biosynthetic gene clusters (smBGCs) such as polyketide synthases (PKS) and non-ribosomal peptide synthetases (NRPS) which are modular and can...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md16020067
更新日期:2018-02-20 00:00:00
abstract::Hepatocellular carcinoma (HCC) is a malignant tumor that can cause systemic invasion; however, the exact etiology and molecular mechanism are unknown. Astaxanthin (ASX), a powerful antioxidant, has efficient anti-oxidant, anti-inflammatory, and other activities, and has great research prospects in cancer therapy. We s...
journal_title:Marine drugs
pub_type: 杂志文章
doi:10.3390/md13106064
更新日期:2015-09-24 00:00:00