Design, synthesis and evaluation of new marine alkaloid-derived pentacyclic structures with anti-tumoral potency.


: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.


Mar Drugs


Marine drugs


Boucle S,Melin C,Clastre M,Guillard J




Has Abstract


2015-01-19 00:00:00












  • Synthesis of glycyrrhetinic acid-modified chitosan 5-fluorouracil nanoparticles and its inhibition of liver cancer characteristics in vitro and in vivo.

    abstract::Nanoparticle drug delivery (NDDS) is a novel system in which the drugs are delivered to the site of action by small particles in the nanometer range. Natural or synthetic polymers are used as vectors in NDDS, as they provide targeted, sustained release and biodegradability. Here, we used the chitosan and hepatoma cell...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Cheng M,Gao X,Wang Y,Chen H,He B,Xu H,Li Y,Han J,Zhang Z

    更新日期:2013-09-17 00:00:00

  • Sphaeroane and neodolabellane diterpenes from the red alga Sphaerococcus coronopifolius.

    abstract::Investigation of minor metabolites in the extracts of the red alga Sphaerococcus coronopifolius collected from the rocky coasts of Corfu Island in the Ionian Sea yielded two new diterpene alcohols, sphaerollanes I, and II (1, 2) featuring neodolabellane skeletons, and the new sphaeroane diterpene alcohol 16-hydroxy-9S...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Smyrniotopoulos V,Vagias C,Roussis V

    更新日期:2009-05-19 00:00:00

  • Nocapyrones: α- and γ-pyrones from a marine-derived Nocardiopsis sp.

    abstract::One new α-pyrone (nocapyrone R (1)), and three known γ-pyrones (nocapyrones B, H and L (2-4)) were isolated from the culture extract of a Nocardiopsis strain collected from marine sediment. Structures of these compounds were determined on the basis of spectroscopic data including NMR and MS. γ-Pyrones 2-4 were found t...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Kim Y,Ogura H,Akasaka K,Oikawa T,Matsuura N,Imada C,Yasuda H,Igarashi Y

    更新日期:2014-07-08 00:00:00

  • Marine and semi-synthetic hydroxysteroids as new scaffolds for pregnane X receptor modulation.

    abstract::In recent years many sterols with unusual structures and promising biological profiles have been identified from marine sources. Here we report the isolation of a series of 24-alkylated-hydroxysteroids from the soft coral Sinularia kavarattiensis, acting as pregnane X receptor (PXR) modulators. Starting from this scaf...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Sepe V,Di Leva FS,D'Amore C,Festa C,De Marino S,Renga B,D'Auria MV,Novellino E,Limongelli V,D'Souza L,Majik M,Zampella A,Fiorucci S

    更新日期:2014-05-27 00:00:00

  • Natural product research in the Australian marine invertebrate Dicathais orbita.

    abstract::The predatory marine gastropod Dicathais orbita has been the subject of a significant amount of biological and chemical research over the past five decades. Natural products research on D. orbita includes the isolation and identification of brominated indoles and choline esters as precursors of Tyrian purple, as well ...

    journal_title:Marine drugs

    pub_type: 杂志文章,评审


    authors: Benkendorff K

    更新日期:2013-04-23 00:00:00

  • Separacenes A-D, novel polyene polyols from the marine actinomycete, Streptomyces sp.

    abstract::Separacenes A-D (1-4), novel polyene polyols, were isolated from Streptomyces sp. collected from the southern area of Jeju Island, Korea. The chemical structures of 1-4 were established by NMR, mass, UV, and IR spectroscopy as well as the modified Mosher's method. Separacenes A-B (1-2), which share an identical planar...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Bae M,Kim H,Shin Y,Kim BY,Lee SK,Oh KB,Shin J,Oh DC

    更新日期:2013-08-13 00:00:00

  • Production of bioactive secondary metabolites by marine vibrionaceae.

    abstract::Bacteria belonging to the Vibrionaceae family are widespread in the marine environment. Today, 128 species of vibrios are known. Several of them are infamous for their pathogenicity or symbiotic relationships. Despite their ability to interact with eukaryotes, the vibrios are greatly underexplored for their ability to...

    journal_title:Marine drugs

    pub_type: 杂志文章,评审


    authors: Mansson M,Gram L,Larsen TO

    更新日期:2011-01-01 00:00:00

  • Anti-Inflammatory Polyoxygenated Steroids from the Soft Coral Lobophytum michaelae.

    abstract::Three new polyoxygenated steroids, michosterols A-C (1-3), and four known compounds (4-7) were isolated from the ethyl acetate (EtOAc) extract of the soft coral Lobophytum michaelae, collected off the coast of Taitung. The structures of the new compounds were elucidated on the basis of spectroscopic analyses and compa...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Huang CY,Tseng WR,Ahmed AF,Chiang PL,Tai CJ,Hwang TL,Dai CF,Sheu JH

    更新日期:2018-03-13 00:00:00

  • Rumphellaoic acid A, a novel sesquiterpenoid from the formosan gorgonian coral Rumphella antipathies.

    abstract::A novel sesquiterpenoid, rumphellaoic acid A (1), was isolated from the gorgonian coral Rumphella antipathies, and was found to possess a carbon skeleton that was obtained for the first time from a natural sources. The structure of 1 was elucidated by spectroscopic methods and this compound and was found to exert a mo...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Chung HM,Wang WH,Hwang TL,Fang LS,Wen ZH,Chen JJ,Wu YC,Sung PJ

    更新日期:2014-12-04 00:00:00

  • Effect of Methionine Oxidation and Substitution of α-Conotoxin TxID on α3β4 Nicotinic Acetylcholine Receptor.

    abstract::α-Conotoxin TxID was discovered from Conus textile by gene cloning, which has 4/6 inter-cysteine loop spacing and selectively inhibits α3β4 nicotinic acetylcholine receptor (nAChR) subtype. However, TxID is susceptible to modification due to it containing a methionine (Met) residue that easily forms m...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Ren J,Li R,Ning J,Zhu X,Zhangsun D,Wu Y,Luo S

    更新日期:2018-06-20 00:00:00

  • The Inhibitory Effect of Protamine on Platelets is Attenuated by Heparin without Inducing Thrombocytopenia in Rodents.

    abstract::Protamine sulfate (PS) is a polycationic protein drug obtained from the sperm of fish, and is used to reverse the anticoagulant effect of unfractionated heparin (UFH). However, the interactions between PS, UFH, and platelets are still not clear. We measured the platelet numbers and collagen-induced aggregation, P-sele...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Miklosz J,Kalaska B,Kaminski K,Rusak M,Szczubialka K,Nowakowska M,Pawlak D,Mogielnicki A

    更新日期:2019-09-17 00:00:00

  • Smenospongine, a sesquiterpene aminoquinone from a marine sponge, induces G1 arrest or apoptosis in different leukemia cells.

    abstract::Smenospongine, a sesquiterpene aminoquinone isolated from the marine sponge Dactylospongia elegans, was previously reported by us to induce erythroid differentiation and G1 phase arrest of K562 chronic myelogenous leukemia cells. In this study, we investigated the effect of smenospongine on the cell cycles of other le...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Kong D,Aoki S,Sowa Y,Sakai T,Kobayashi M

    更新日期:2008-01-01 00:00:00

  • Physicochemical and Functional Properties of Type I Collagens in Red Stingray (Dasyatis akajei) Skin.

    abstract::Collagen is widely used in the pharmaceutical, tissue engineering, nutraceutical, and cosmetic industries. In this study, acid-soluble collagen (ASC) and pepsin-soluble collagen (PSC) were extracted from the skin of red stingray, and its physicochemical and functional properties were investigated. The yields of ASC an...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Chen J,Li J,Li Z,Yi R,Shi S,Wu K,Li Y,Wu S

    更新日期:2019-09-28 00:00:00

  • Astaxanthin from Shrimp Cephalothorax Stimulates the Immune Response by Enhancing IFN-γ, IL-10, and IL-2 Secretion in Splenocytes of Helicobacter Pylori-Infected Mice.

    abstract::Infection with Helicobacter pylori is a critical cause of gastrointestinal diseases. A crucial host response associated with H. pylori infection includes gastric inflammation, which is characterized by a sustained recruitment of T-helper (Th) cells to the site of infection and distinct patterns of cytokine production....

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Davinelli S,Melvang HM,Andersen LP,Scapagnini G,Nielsen ME

    更新日期:2019-06-26 00:00:00

  • Water-Soluble Fish Protein Intake Led to Lower Serum and Liver Cholesterol Concentrations in Obese Zucker fa/fa Rats.

    abstract::Proteins from different fish species and different raw materials such as fish fillets and by-products have shown promising cardioprotective effects in rodents and humans, including effects on cholesterol metabolism. Blue whiting is used mainly to produce fish meal for the feed industry and during this production, a wa...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Drotningsvik A,Vikøren LA,Mjøs SA,Oterhals Å,Pampanin D,Flesland O,Gudbrandsen OA

    更新日期:2018-05-01 00:00:00

  • Bacterial Long-Chain Polyunsaturated Fatty Acids: Their Biosynthetic Genes, Functions, and Practical Use.

    abstract::The nutritional and pharmaceutical values of long-chain polyunsaturated fatty acids (LC-PUFAs) such as arachidonic, eicosapentaenoic and docosahexaenoic acids have been well recognized. These LC-PUFAs are physiologically important compounds in bacteria and eukaryotes. Although little is known about the biosynthetic me...

    journal_title:Marine drugs

    pub_type: 杂志文章,评审


    authors: Yoshida K,Hashimoto M,Hori R,Adachi T,Okuyama H,Orikasa Y,Nagamine T,Shimizu S,Ueno A,Morita N

    更新日期:2016-05-12 00:00:00

  • The Oxepane Motif in Marine Drugs.

    abstract::Oceans have shown to be a remarkable source of natural products. The biological properties of many of these compounds have helped to produce great advances in medicinal chemistry. Within them, marine natural products containing an oxepanyl ring are present in a great variety of algae, sponges, fungus and corals and sh...

    journal_title:Marine drugs

    pub_type: 杂志文章,评审


    authors: Barbero H,Díez-Poza C,Barbero A

    更新日期:2017-11-15 00:00:00

  • Astaxanthin Counteracts Excitotoxicity and Reduces the Ensuing Increases in Calcium Levels and Mitochondrial Reactive Oxygen Species Generation.

    abstract::Astaxanthin (ASX) is a carotenoid pigment with strong antioxidant properties. We have reported previously that ASX protects neurons from the noxious effects of amyloid-β peptide oligomers, which promote excessive mitochondrial reactive oxygen species (mROS) production and induce a sustained increase in cytoplasmic Ca2...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: García F,Lobos P,Ponce A,Cataldo K,Meza D,Farías P,Estay C,Oyarzun-Ampuero F,Herrera-Molina R,Paula-Lima A,Ardiles ÁO,Hidalgo C,Adasme T,Muñoz P

    更新日期:2020-06-26 00:00:00

  • Haliotis discus discus Sialic Acid-Binding Lectin Reduces the Oncolytic Vaccinia Virus Induced Toxicity in a Glioblastoma Mouse Model.

    abstract::Although oncolytic viruses provide attractive vehicles for cancer treatment, their adverse effects are largely ignored. In this work, rat C6 glioblastoma cells were subcutaneously xenografted into mice, and a thymidine kinase-deficient oncolytic vaccinia virus (oncoVV) induced severe toxicity in this model. However, o...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Li G,Mei S,Cheng J,Wu T,Luo J

    更新日期:2018-04-26 00:00:00

  • Inhibition of bacterial quorum sensing by extracts from aquatic fungi: first report from marine endophytes.

    abstract::In our search for quorum-sensing (QS) disrupting molecules, 75 fungal isolates were recovered from reef organisms (endophytes), saline lakes and mangrove rhizosphere. Their QS inhibitory activity was evaluated in Chromobacterium violaceum CVO26. Four strains of endophytic fungi stood out for their potent activity at c...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Martín-Rodríguez AJ,Reyes F,Martín J,Pérez-Yépez J,León-Barrios M,Couttolenc A,Espinoza C,Trigos A,Martín VS,Norte M,Fernández JJ

    更新日期:2014-11-19 00:00:00

  • Polyhydroxylated steroids from the South China Sea soft coral Sarcophyton sp. and their cytotoxic and antiviral activities.

    abstract::Chemical investigation on the soft coral Sarcophyton sp. collected from the South China Sea yielded three new polyhydroxylated steroids, compounds (1-3), together with seven known ones (4-10). Their structures were established by extensive spectroscopic methods and comparison of their data with those of the related kn...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Gong KK,Tang XL,Zhang G,Cheng CL,Zhang XW,Li PL,Li GQ

    更新日期:2013-12-02 00:00:00

  • Marine Drugs Regulating Apoptosis Induced by Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand (TRAIL).

    abstract::Marine biomass diversity is a tremendous source of potential anticancer compounds. Several natural marine products have been described to restore tumor cell sensitivity to TNF-related apoptosis inducing ligand (TRAIL)-induced cell death. TRAIL is involved during tumor immune surveillance. Its selectivity for cancer ce...

    journal_title:Marine drugs

    pub_type: 杂志文章,评审


    authors: Elmallah MI,Micheau O

    更新日期:2015-11-13 00:00:00

  • Preparation of calibration standards of N1-H paralytic shellfish toxin analogues by large-scale culture of cyanobacterium Anabaena circinalis (TA04).

    abstract::Mouse bioassay is the official testing method to quantify paralytic shellfish toxins (PSTs) in bivalves. A number of alternative analytical methods have been reported. Some methods have been evaluated by a single laboratory validation. Among the different types of methods, chemical analyses are capable of identifying ...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Watanabe R,Suzuki T,Oshima Y

    更新日期:2011-03-22 00:00:00

  • Seaweed hydrocolloid production: an update on enzyme assisted extraction and modification technologies.

    abstract::Agar, alginate, and carrageenans are high-value seaweed hydrocolloids, which are used as gelation and thickening agents in different food, pharmaceutical, and biotechnological applications. The annual global production of these hydrocolloids has recently reached 100,000 tons with a gross market value just above US$ 1....

    journal_title:Marine drugs

    pub_type: 杂志文章,评审


    authors: Rhein-Knudsen N,Ale MT,Meyer AS

    更新日期:2015-05-27 00:00:00

  • Mannose-Specific Lectins from Marine Algae: Diverse Structural Scaffolds Associated to Common Virucidal and Anti-Cancer Properties.

    abstract::To date, a number of mannose-specific lectins have been isolated and characterized from seaweeds, especially from red algae. In fact, man-specific seaweed lectins consist of different structural scaffolds harboring a single or a few carbohydrate-binding sites which specifically recognize mannose-containing glycans. De...

    journal_title:Marine drugs

    pub_type: 杂志文章,评审


    authors: Barre A,Simplicien M,Benoist H,Van Damme EJM,Rougé P

    更新日期:2019-07-26 00:00:00

  • Total Synthesis of Mycalisine B.

    abstract::The first total synthesis of the marine nucleoside Mycalisine B-a naturally occurring and structurally distinct 4,5-unsaturated 7-deazapurine nucleoside-has been accomplished in 10 linear steps with 27.5% overall yield from commercially available 1,2,3,5-tetra-O-acetyl-ribose and tetracyanoethylene. Key steps of the a...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Ding H,Ruan Z,Kou P,Dong X,Bai J,Xiao Q

    更新日期:2019-04-14 00:00:00

  • Angiotensin-I Converting Enzyme (ACE) Inhibitory and Anti-Hypertensive Effect of Protein Hydrolysate from Actinopyga lecanora (Sea Cucumber) in Rats.

    abstract::Food protein hydrolysates are known to exhibit angiotensin converting enzyme (ACE) inhibitory properties and can be used as a novel functional food for prevention of hypertension. This study evaluated the ACE inhibitory potentials of Actinopyga lecanora proteolysate (ALP) in vivo. The pre-fed rats with ALP at various ...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Sadegh Vishkaei M,Ebrahimpour A,Abdul-Hamid A,Ismail A,Saari N

    更新日期:2016-09-30 00:00:00

  • New Mammalian Target of Rapamycin (mTOR) Modulators Derived from Natural Product Databases and Marine Extracts by Using Molecular Docking Techniques.

    abstract::Mammalian target of rapamycin (mTOR) is a PI3K-related serine/threonine protein kinase that functions as a master regulator of cellular growth and metabolism, in response to nutrient and hormonal stimuli. mTOR functions in two distinct complexes-mTORC1 is sensitive to rapamycin, while, mTORC2 is insensitive to this dr...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Ruiz-Torres V,Losada-Echeberría M,Herranz-López M,Barrajón-Catalán E,Galiano V,Micol V,Encinar JA

    更新日期:2018-10-15 00:00:00

  • The Mediterranean red alga Asparagopsis: a source of compounds against Leishmania.

    abstract::Crude extracts and column fractions from the red algae Asparagopsis taxiformis and A. armata from the Strait of Messina (Italy) were screened for the production of antimicrobial compounds. Extracts from both species revealed remarkable antiprotozoal activity against Leishmania, revealing such algae as a great source o...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Genovese G,Tedone L,Hamann MT,Morabito M

    更新日期:2009-08-11 00:00:00

  • Anticancer Activity of Fascaplysin against Lung Cancer Cell and Small Cell Lung Cancer Circulating Tumor Cell Lines.

    abstract::Lung cancer is a leading cause of tumor-associated mortality. Fascaplysin, a bis-indole of a marine sponge, exhibit broad anticancer activity as specific CDK4 inhibitor among several other mechanisms, and is investigated as a drug to overcome chemoresistance after the failure of targeted agents or immunotherapy. The c...

    journal_title:Marine drugs

    pub_type: 杂志文章


    authors: Rath B,Hochmair M,Plangger A,Hamilton G

    更新日期:2018-10-14 00:00:00