| ecteinascidia turbinata extracts inhibit dna synthesis in lymphocytes after mitogenic stimulation by lectins. | aqueous ethanol extract of a tunicate which was previously found to exert antitumor and immunosuppressive activities in vivo was tested for its effect on normal human lymphocytes in vitro. the extract suppressed the uptake of tritiated thymidine by lymphocytes stimulated with mitogen. this suppressive effect did not require continuous presence of the extract. treatment of lymphocytes prior to mitogenic stimulation resulted in suppressive effect. the fact that suppression by the extract could als ... | 1975 | 1208565 |
| additional antitumor ecteinascidins from a caribbean tunicate: crystal structures and activities in vivo. | ecteinascidins (ets), isolated from the caribbean tunicate ecteinascidia turbinata, protect mice in vivo against p388 lymphoma, b16 melanoma, m5076 ovarian sarcoma, lewis lung carcinoma, and the lx-1 human lung and mx-1 human mammary carcinoma xenografts. crystal structures of two tris(tetrahydroisoquinoline) ets were investigated with single crystals of the 21-o-methyl-n12-formyl derivative of et 729 and the natural n12-oxide of et 743. representatives of an additional class of ets, et 722 and ... | 1992 | 1454834 |
| immunosuppressive effect of ecteinascidia turbinata in mice. | | 1973 | 4618657 |
| effects of an extract from the sea squirt ecteinascidia turbinata on dna synthesis and excision repair in human fibroblasts. | an aqueous ethanol extract from the marine tunicate species ecteinascidia turbinata was studied to determine its effect on semiconservative dna synthesis in human skin fibroblast cultures as measured by [3h] thymidine uptake in acid-insoluble cell fractions. in addition, the effect of this extract on dna excision repair in ultraviolet light (254 nm) irradiated fibroblasts was measured by the bromodeoxyuridine photolysis assay, thymine dimer chromatography, and dna single-strand break analysis on ... | 1982 | 7135413 |
| dna sequence- and structure-selective alkylation of guanine n2 in the dna minor groove by ecteinascidin 743, a potent antitumor compound from the caribbean tunicate ecteinascidia turbinata. | ecteinascidin 743 is one of several related marine alkaloids isolated from the caribbean tunicate ecteinascidia turbinata. it is remarkably active and potent in a variety of in vitro and in vivo systems and has been selected for development as an anticancer agent. the present study investigates the interactions of ecteinascidin 743 with dna. ecteinascidin 743 retarded the electrophoretic migration of both supercoiled and relaxed simian virus 40 dna even in the presence of sodium dodecyl sulfate ... | 1996 | 8873596 |
| in vitro antitumor activity of the novel marine agent, ecteinascidin-743 (et-743, nsc-648766) against human tumors explanted from patients. | ecteinascidin-743 (et-743), a member of the ecteinascidin family selected for clinical development, is a tetrahydroisoquinolone alkaloid isolated from the marine ascidian, ecteinascidia turbinata. this novel compound is a minor groove binding, guanine-specific alkylating agent which also interacts with the microtubule network and blocks cell cycle progression at late s/g2. | 1998 | 9818072 |
| poisoning of human dna topoisomerase i by ecteinascidin 743, an anticancer drug that selectively alkylates dna in the minor groove. | ecteinascidin 743 (et743, national service center 648766) is a potent antitumor agent from the caribbean tunicate ecteinascidia turbinata. although et743 is presently in clinical trials for human cancers, the mechanisms of antitumor activity of et743 have not been elucidated. et743 can alkylate selectively guanine n2 from the dna minor groove, and this alkylation is reversed by dna denaturation. thus, et743 differs from other dna alkylating agents presently in the clinic (by both its biochemical ... | 1999 | 10377391 |
| high antitumour activity of et743 against human tumour xenografts from melanoma, non-small-cell lung and ovarian cancer. | ecteinascidin-743 (et743) is a novel antitumour agent originating from the caribbean tunicate ecteinascidia turbinata. it has potent cytotoxic and antitumour activity and a potential new mechanism of action. the aim of the present study was to further explore the antitumour activity of et743 in human tumour xenografts from melanoma, non-small-cell lung and ovarian cancer. | 1999 | 10586342 |
| oxepinamides a-c and fumiquinazolines h--i: bioactive metabolites from a marine isolate of a fungus of the genus acremonium. | three new oxepin-containing natural products (1-3) and two new fumiquinazoline metabolites (4-5) have been isolated from organic extracts of the culture broth and mycelia of an acremonium sp., a fungus obtained from the surface of the caribbean tunicate ecteinascidia turbinata. the structures of the five compounds were determined through extensive analysis of 1d- and 2d-nmr data, and mass spectrometry. compound 1 exhibited good anti-inflammatory activity in a topical rtx-induced mouse ear edema ... | 2000 | 10840958 |
| interference of transcriptional activation by the antineoplastic drug ecteinascidin-743. | ecteinascidin-743 (et-743) is a tetrahydroisoquinoline alkaloid isolated from the tunicate ecteinascidia turbinata currently under phase ii clinical trials for its potent anticancer activity. et-743 binds dna in the minor groove and forms covalent adducts with some sequence specificity. it selectively inhibits in vitro binding of the ccaat box factor nf-y. in this study, we assayed et-743 function in vivo on the hsp70 promoter. on heat induction, the drug blocks transcription rapidly at pharmaco ... | 2000 | 10841573 |
| ecteinascidin-743 (et-743), a natural marine compound, with a unique mechanism of action. | the mode of action of ecteinascidin-743 (et-743), a marine tetrahydroisoquinoline alkaloid isolated from ecteinascidia turbinata, which has shown very potent antitumour activity in preclinical systems and encouraging results in phase i clinical trials was investigated at a cellular level. both sw620 and lovo human intestinal carcinoma cell lines exposed for 1 h to et-743 progress through s phase more slowly than control cells and then accumulate in the g2m phase. the sensitivity to et-743 of g1 ... | 2001 | 11165136 |
| unique pattern of et-743 activity in different cellular systems with defined deficiencies in dna-repair pathways. | the cytotoxic activity of ecteinascidin 743 (et-743), a natural product derived from the marine tunicate ecteinascidia turbinata that exhibits potent anti-tumor activity in pre-clinical systems and promising activity in phase i and ii clinical trials, was investigated in a number of cell systems with well-defined deficiencies in dna-repair mechanisms. et-743 binds to n2 of guanine in the minor groove, but its activity does not appear to be related to dna-topoisomerase i poisoning as the drug is ... | 2001 | 11304695 |
| unique features of the mode of action of et-743. | this paper describes the current knowledge of the primary mode of action of a natural product, ecteinascidin 743 (et-743), derived from the marine tunicate ecteinascidia turbinata. et-743 was initially selected for preclinical development because of its potent antitumor activity observed against several human solid tumor types. in vitro, the drug is cytotoxic in the nanomolar range, and in the case of some very sensitive cell lines, in the picomolar range. the large potency differences observed ... | 2002 | 12065793 |
| sequence-dependent synergistic cytotoxicity of ecteinascidin-743 and paclitaxel in human breast cancer cell lines in vitro and in vivo. | ecteinascidin 743 (et-743) is a potent antitumor agent from the caribbean tunicate ecteinascidia turbinata and is presently in clinical trials for human cancers. the aim of this study was to assess the nature of the interaction between et-743 and other antineoplastic agents using the combination index method of chou and talalay to better understand how et-743 might be used clinically. we examined the cytotoxic effect of et-743 combined with six other antineoplastic agents on human breast cancer ... | 2002 | 12460906 |
| effectiveness of ecteinascidin-743 against drug-sensitive and -resistant bone tumor cells. | the identification of new drugs is strongly needed for bone tumors.ecteinascidin-743 (et-743), a highly promising antitumor agent isolated from the marine tunicate ecteinascidia turbinata, is currently under phase ii clinical investigation in europe and the united states for treatment of soft tissue sarcoma. in this study, we analyzed the preclinical effectiveness of this drug in osteosarcoma and ewing's sarcoma. | 2002 | 12473605 |
| preclinical and clinical results with the natural marine product et-743. | et-743 (yondelis, trabectedin) is a natural marine product with antitumour properties derived from the tunicate ecteinascidia turbinata. et-743 binds to the n2 position of guanine in the minor groove of dna with some degree of sequence specificity, altering the transcription regulation of induced genes. cells that are deficient in nucleotide excision repair, hypersensitive to uv rays, cisplatin and conventional alkylating agents, are resistant to et-743. this is a unique property of et-743 and i ... | 2003 | 14585059 |
| molecular characterisation of two human cancer cell lines selected in vitro for their chemotherapeutic drug resistance to et-743. | et-743 (yondelis(tm), trabectedin) isolated from the tunicate ecteinascidia turbinata, is being tested in phase ii clinical trials in europe and the united states of america (usa). studies with different solid tumours have shown antitumour activity in advanced, pre-treated sarcomas as well as in drug-resistant breast and ovarian cancer. the primary mechanism of action for et-743 has not been fully elucidated and different models have been suggested to explain its molecular mechanism of action. e ... | 2005 | 15661559 |
| anti-inflammatory properties of the novel antitumor agent yondelis (trabectedin): inhibition of macrophage differentiation and cytokine production. | yondelis (trabectedin) is a novel antitumor agent of marine origin extracted from the tunicate ecteinascidia turbinata. this original compound is active against several human tumors including sarcoma and ovarian and breast adenocarcinoma, as evidenced in phase ii clinical trials in advanced multitreated patients. yondelis is a dna minor groove binder that blocks cell cycle and interferes with inducible gene transcription in a selective manner. in this study, we investigated the immunomodulatory ... | 2005 | 15805300 |
| antibiotic bisanthraquinones produced by a streptomycete isolated from a cyanobacterium associated with ecteinascidia turbinata. | chemical studies of a streptomycete isolated from a cyanobacterium associated with the tropical tunicate ecteinascidia turbinata led to the bioassay-guided purification of two antibacterial bisanthraquinone metabolites and a cytotoxic artifact. the structures, including relative configurations of these octacyclic compounds, were established by spectroscopic analyses. their potent antibacterial properties (ic(50) = 0.15-130 microm) versus methicillin-resistant staphylococcus aureus and vancomycin ... | 2006 | 16872146 |
| bacterial diversity associated with the caribbean tunicate ecteinascidia turbinata. | the caribbean tunicate, ecteinascidia turbinata produces the anti-cancer agent et-743 that could well be a metabolite of an associated bacterial strain. this current study aims at the analysis of bacteria that are persistently and specifically associated with this invertebrate. utilizing techniques such as denaturing gradient gel electrophoresis, dna sequencing and phylogenetic analysis of bacteria from e. turbinata collected from different locations in the caribbean sea, we report here the iden ... | 2007 | 17265101 |
| cytotoxic and apoptogenic activity of a methanolic extract from the marine invertebrate ciona intestinalis on malignant cell lines. | marine invertebrates provide a series of natural products with different biological activities. several of these compounds and their derivatives showed a potent anticancer effect. tunicates represent an important source of bioactive agents, leading to the isolation of ecteinascidin-743 (et-743), a compound isolated from the caribbean sea squirt ecteinascidia turbinata with a potent cytotoxic activity against a variety of tumours in vitro and in vivo. current phase ii clinical trials against soft ... | 2008 | 18336328 |
| total synthesis and biological evaluation of (+)- and (-)-bisanthraquinone antibiotic be-43472b and related compounds. | the bisanthraquinone antibiotic be-43472b [(+)-1] was isolated by rowley and co-workers from a streptomycete strain found in a blue-green algae associated with the ascidian ecteinascidia turbinata and has shown promising antibacterial activity against clinically derived isolates of methicillin-susceptible, methicillin-resistant, and tetracyclin-resistant staphylococcus aureus (mssa, mrsa, and trsa, respectively) and vancomycin-resistant enterococcus faecalis (vre). described herein is the first ... | 2009 | 19778008 |
| Meta-omic characterization of the marine invertebrate microbial consortium that produces the chemotherapeutic natural product ET-743. | In many macroorganisms, the ultimate source of potent biologically active natural products has remained elusive due to an inability to identify and culture the producing symbiotic microorganisms. As a model system for developing a meta-omic approach to identify and characterize natural product pathways from invertebrate-derived microbial consortia, we chose to investigate the ET-743 (Yondelis) biosynthetic pathway. This molecule is an approved anticancer agent obtained in low abundance (10(-4)-1 ... | 2011 | 21875091 |
| suppressor activity of splenocytes from mice treated with ecteinascidia turbinata extract. | extracts of a marine tunicate, ecteinascidia turbinata (ete) were previously shown to be capable of suppressing humoral and cellular immune responses in vivo and in vitro. in the present work we have examined the mechanisms of suppression in ete-treated dba/2 and balb/c mice. treatment with ete resulted in a significant splenomegaly accompanied by a diminished response to mitogenic stimulation, reaching coincident maxima of effect at days 4 to 6. spleen size and blastogenic reaction returned to ... | 1999 | 310837 |
| identification and analysis of the bacterial endosymbiont specialized for production of the chemotherapeutic natural product et-743. | ecteinascidin 743 (et-743, yondelis) is a clinically approved chemotherapeutic natural product isolated from the caribbean mangrove tunicate ecteinascidia turbinata. researchers have long suspected that a microorganism may be the true producer of the anticancer drug, but its genome has remained elusive due to our inability to culture the bacterium in the laboratory using standard techniques. here, we sequenced and assembled the complete genome of the et-743 producer, candidatus endoecteinascidia ... | 2015 | 26013440 |
| biosynthesis of tetrahydroisoquinoline antibiotics. | the tetrahydroisoquinoline (thiq) alkaloids are naturally occurring antibiotics isolated from a variety of microorganisms and marine invertebrates. this family of natural products exhibit broad spectrum antimicrobial and strong antitumor activities, and the potency of clinical application has been validated by the marketing of ecteinascidin 743 (et-743) as anticancer drug. in the past 20 years, the biosynthetic gene cluster of six thiq antibiotics has been characterized including saframycin mx1 ... | 2016 | 26456466 |
| trabectedin as a chemotherapy option for patients with brca deficiency. | trabectedin is a marine-derived product that was originally isolated from the caribbean sea squirt ecteinascidia turbinata and the first anticancer marine drug to be approved by the european union. it is currently used as a single agent for the treatment of patients with soft tissue sarcoma after failure of anthracyclines and ifosfamide, or for those patients who are unsuited to receive these agents, and in patients with relapsed, platinum-sensitive ovarian cancer in combination with pegylated l ... | 2016 | 27710871 |
| trabectedin for soft tissue sarcoma: current status and future perspectives. | trabectedin (et743, yondelis(®), manufactured by baxter oncology gmbh, halle/westfalen, germany, for janssen products, lp, horsham, pa), derived from the marine ascidian, ecteinascidia turbinata, is a natural alkaloid with multiple complex mechanisms of action. on 23 october 2015, 15 years after the results of the first phase 1 clinical trial using trabectedin for chemotherapy-resistant solid malignancies was reported, and 8 years after its approval in europe, the united states food and drug adm ... | 2016 | 27234989 |
| new distributional data on ascidian fauna (tunicata: ascidiacea) from mandapam coast, gulf of mannar, india. | ascidians play a key role in the ecology and biodiversity of marine ecosystem. ascidians can be transported in ship ballast water and while attached to ship and boat hulls. heavy traffic by domestic and international ships as well as cargo vessels between the major and minor ports warrants continuous monitoring for new introductions of ascidians. the mandapam coast is situated in the gulf of mannar, india, a marine hot spot area in the indian ocean which provides an environment suitable for the ... | 2016 | 27099557 |
| the value of trabectedin in the treatment of soft tissue sarcoma. | soft tissue sarcomas (stss) are a group of rare tumors accounting for less than 1% of all adult malignant tumors, a heterogeneous group of more than 50 histological subtypes. five percent to 30% of sts patients experience local recurrence and 10%-38% present with clinically detectable metastases. doxorubicin either alone or in combination with ifosfamide has been used as first-line chemotherapy for advanced disease. after failure of first-line chemotherapy, high-dose ifosfamide, gemcitabine + do ... | 2016 | 26834480 |
| unique features of trabectedin mechanism of action. | trabectedin (yondelis®, et-743) is a marine-derived natural product that was initially isolated from the marine ascidian ecteinascidia turbinata and is currently prepared synthetically. trabectedin is used as a single agent for the treatment of patients with soft tissue sarcoma after failure of doxorubicin or ifosfamide or who are unsuited to receive these agents, and in patients with relapsed, platinum-sensitive ovarian cancer in combination with pegylated liposomal doxorubicin. trabectedin pre ... | 2016 | 26666647 |
| enhanced g2/m arrest, caspase related apoptosis and reduced e-cadherin dependent intercellular adhesion by trabectedin in prostate cancer stem cells. | trabectedin (yondelis, et-743) is a marine-derived tetrahydroisoquinoline alkaloid. it is originally derived from the caribbean marine tunicate ecteinascidia turbinata and currently produced synthetically. trabectedin is active against a variety of tumor cell lines growing in culture. the present study focused on the effect of trabectedin in cell proliferation, cell cycle progression, apoptosis and spheroid formation in prostate cancer stem cells (cscs). cluster of differentiation (cd) 133+high/ ... | 2015 | 26485709 |
| trabectedin in soft tissue sarcomas. | soft tissue sarcomas are a group of rare tumors derived from mesenchymal tissue, accounting for about 1% of adult cancers. there are over 60 different histological subtypes, each with their own unique biological behavior and response to systemic therapy. the outcome for patients with metastatic soft tissue sarcoma is poor with few available systemic treatment options. for decades, the mainstay of management has consisted of doxorubicin with or without ifosfamide. trabectedin is a synthetic agent ... | 2015 | 25686274 |
| trabectedin as a single agent and in combination with pegylated liposomal doxorubicin - activity against ovarian cancer cells. | over 225 000 new cases of ovarian cancer are diagnosed each year. symptoms are often vague, so most cases are detected when the disease is at an advanced stage. there is a need to find new drugs which will be able to treat ovarian cancer effectively. one of the most promising antineoplastic agents is trabectedin (yondelis), derived from the marine tunicate ecteinascidia turbinata, approved by the european union in july 2007 for the treatment of soft-tissue sarcomas. this drug shows a mechanism o ... | 2014 | 25520572 |
| trabectedin in soft tissue sarcomas. | trabectedin (yondelis®; pharmamar, madrid, spain), a synthetic anticancer agent originally isolated from the caribbean tunicate, ecteinascidia turbinata, is currently approved in more than 70 countries worldwide for the treatment of soft tissue sarcoma (sts). trabectedin is an isoquinoline alkylating agent that, unlike other alkylating agents, binds in the dna minor groove to initiate cytotoxic activity. other multitarget mechanisms of action of trabectedin include important effects within the t ... | 2014 | 25048043 |
| anti-angiogenic effects of trabectedin (yondelis; et-743) on human breast cancer cells. | trabectedin, a tetrahydroisoquinoline alkaloid derived from a caribbean tunicate ecteinascidia turbinata, has been shown to have antitumor effects. in this study, we assessed the possible anti-angiogenic effects of trabectedin on human umbilical vein endothelial cells (huvecs) and breast cancer cell lines. an xtt cell viability assay was used to determine cytotoxicity. a scratch assay was used to detect the migration of cells after trabectedin treatment. angiogenic cytokine profiles of breast ca ... | 2014 | 24941346 |
| activation of the nuclear factor e2-related factor 2 pathway by novel natural products halomadurones a-d and a synthetic analogue. | two novel chlorinated pyrones, halomadurones a and b, and two novel brominated analogues, halomadurones c and d, were isolated from a marine actinomadura sp. cultivated from the ascidian ecteinascidia turbinata. additionally, a non-halogenated analogue, 2-methyl-6-((e)-3-methyl-1,3-hexadiene)-γ-pyrone, was synthesized to understand the role of the halogens for activity. halomadurones c and d demonstrated potent nuclear factor e2-related factor antioxidant response element (nrf2-are) activation, ... | 2013 | 24351907 |
| a diverse induction of apoptosis by trabectedin in mcf-7 (her2-/er+) and mda-mb-453 (her2+/er-) breast cancer cells. | trabectedin (yondelis, et-743), a semi synthetic tetrahydroisoquinoline alkaloid that was originally derived from the marine tunicate ecteinascidia turbinata. the objective of this study was to investigate whether trabectedin mediated apoptosis shows any diversity in human breast cancer cell lines with different genotypes. trabectedin induced cytotoxicity and apoptosis in both breast cancer cells in a time and concentration-dependent manner. the expression levels of the death receptor pathway mo ... | 2013 | 23792433 |
| trabectedin as a new chemotherapy option in the treatment of relapsed platinum sensitive ovarian cancer. | trabectedin (et-743, yondelis®) is a novel marine antineoplastic alkaloid with a unique mechanism of action. the active substance trabectedin, a tetrahydroisoquinoline alkaloid, is a natural product originally isolated from the caribbean sea squirt, ecteinascidia turbinata and is currently manufactured by total synthesis. trabectedin is licensed by the spanish pharmaceutical drug company, pharmamar and co-developed by johnson & johnson pharmaceutical research and development, l.l.c., pursuant to ... | 2012 | 22591421 |
| yondelis® (et-743, trabectedin) sensitizes cancer cell lines to cd95-mediated cell death: new molecular insight into the mechanism of action. | trabectedin, a naturally occurring substance isolated from the caribbean marine invertebrate ecteinascidia turbinata, is the active compound of the antitumor drug yondelis®. the mechanism of action of trabectedin has been attributed to interactions with the minor groove of the dna double helix, thereby affecting transcription of different genes involved in dna repair and thus facilitating lethal dna strand breaks. nevertheless, the existence of other clinically important molecular mechanisms has ... | 2011 | 21371453 |
| trabectedin for metastatic soft tissue sarcoma: a retrospective single center analysis. | soft tissue sarcoma (sts) comprises a large variety of rare malignant tumors. development of distant metastasis is frequent, even in patients undergoing initial curative surgery. trabectedin, a tetrahydroisoquinoline alkaloid isolated from the caribbean marine tunicate ecteinascidia turbinata, was approved in 2007 for patients with advanced sts after failure of anthracyclines and ifosfamide, or for patients unsuited to receive these agents. in this study, we retrospectively analyzed 25 patients ... | 2010 | 21116412 |
| a review of trabectedin (et-743): a unique mechanism of action. | trabectedin (et-743) is a marine alkaloid isolated from the caribbean tunicate ecteinascidia turbinata, with a chemical structure characterized by three fused tetrahydroisoquinoline rings. two of these rings (subunits a and b) provide the framework for covalent interaction with the minor groove of the dna double helix, whereas the third ring (subunit c) protrudes from the dna duplex, apparently allowing interactions with adjacent nuclear proteins. the compound's chemical interactions trigger a c ... | 2010 | 20647340 |
| wide-spectrum characterization of trabectedin: biology, clinical activity and future perspectives. | ecteinascidin-743 (trabectedin, yondelis((r)); pharmamar, madrid, spain), a 25-year-old antineoplastic alkylating agent, has recently shown unexpected and interesting mechanisms of action. trabectedin causes perturbation in the transcription of inducible genes (e.g., the multidrug resistance gene mdr1) and interaction with dna repair mechanisms (e.g., the nucleotide excision repair pathway) owing to drug-related dna double strand breaks and adduct formation. trabectedin was the first antineoplas ... | 2010 | 20504257 |
| trabectedin: an anticancer drug from the sea. | trabectedin (et-743) is an anticancer agent originally isolated from ecteinascidia turbinata, a marine organism. | 2009 | 19743937 |
| development of yondelis (trabectedin, et-743). a semisynthetic process solves the supply problem. | ecteinascidins are marine natural products consisting of two or three linked tetrahydroisoquinoline subunits and an active carbinolamine functional group. their potent antiproliferative activity against a variety of tumor cells makes them attractive candidates for development as anticancer agents. the lead compound, yondelis (trabectedin, et-743) is the first marine anticancer agent approved in the european union for patients with soft tissue sarcoma (sts). positive results of a large randomized ... | 2009 | 19240944 |
| role of trabectedin in the treatment of soft tissue sarcoma. | interest in marine natural products has allowed the discovery of new drugs and trabectedin (et-743, yondelis), derived from the marine tunicate ecteinascidia turbinata, was approved for clinical use in 2007. it binds to the dna minor groove leading to interferences with the intracellular transcription pathways and dna-repair proteins. in vitro antitumor activity was demonstrated against various cancer cell lines and soft tissue sarcoma cell lines. in phase i studies tumor responses were observed ... | 2009 | 20616899 |
| structure elucidation and 1h/13c nmr spectral assignments of four trabectedin related compounds. | this article presents the structure elucidation of four new compounds, formed during the hemisynthetic preparation of trabectedin, an anti-tumor natural product from ecteinascidia turbinata. we report herein on the use of uv, ms and nmr spectroscopic data along with (1)h and (13)c spectral assignments obtained by means of 1d and 2d homo- and heteronuclear nmr techniques. | 2008 | 18821578 |
| clinical impact of trabectedin (ecteinascidin-743) in advanced/metastatic soft tissue sarcoma. | patients with advanced or metastatic non-gastrointestinal stromal tumour soft tissue sarcoma (sts) whose disease progresses during or after chemotherapy with doxorubicin or ifosfamide have few options and very limited life expectancy. in this setting, the dna and transcription interacting agent trabectedin (ecteinascidin-743), isolated originally from the tunicate ecteinascidia turbinata, has encouraging activity and is now approved in the european union. | 2008 | 18518789 |
| [distribution and abundance of the ascidian ecteinascidia turbinata (ascidiacea: perophoridae) in cuba]. | permanently submerged mangrove roots (rhizophora mangle) are the main habitat of the ascidian ecteinascidia turbinata in cuba. it was occasionally found on black coral (antiphates caribeana) between 22 and 38 meters deep. this species exhibits a wide distribution in all the mangrove keys surrounding the island of cuba but does not occur in riparian or fringing mangroves. populations of this species are abundant in cuba: in 75% of the 58 localities sampled the species was present and in 57% more ... | 2007 | 18457133 |
| trabectedin : a review of its use in the management of soft tissue sarcoma and ovarian cancer. | trabectedin (yondelis); et-743) is an antineoplastic agent that was originally derived from the caribbean marine tunicate ecteinascidia turbinata and is now produced synthetically. it binds to the minor groove of dna, disrupting the cell cycle and inhibiting cell proliferation. intravenous trabectedin administered once every 3 weeks is approved as monotherapy in europe for use in patients with advanced soft tissue sarcoma (sts) after failure of standard therapy with anthracyclines or ifosfamide, ... | 2007 | 17927287 |
| trabectedin (et-743): evaluation of its use in advanced soft-tissue sarcoma. | trabectedin (et-743; yondelis) is a novel dna-binding agent, originally derived from the marine tunicate, ecteinascidia turbinata, and now produced synthetically. the efficacy of trabectedin in patients with advanced soft-tissue sarcoma has been demonstrated in three phase ii studies involving 189 previously treated patients. a pooled analysis of data from these studies showed that trabectedin induced tumor control (objective responses plus disease stabilization) in approximately 50% of patients ... | 2007 | 17661712 |
| lack of genetic variation in mtdna sequences over the amphiatlantic distribution range of the ascidian ecteinascidia turbinata. | | 2007 | 17629714 |
| [diet of the ascidian ecteinascidia turbinata (ascidiacea: perophoridae) in two mangrove areas of cuba]. | diet of the ascidian ecteinascidia turbinata (ascidiacea: perophoridae) in two mangrove areas of cuba. stomach contents of 88 zooids ofecteinascidia turbinata herdman 1880 and the qualitative and quantitative composition of phytoplankton in the water column were studied in santa fe (north coast of havana) and punta del este (sw of cuba). we identified 59 microalgal species and four tintinnids in the stomachs. cell size was 75-165 microm in length and 2-105 microm in width. there were not signifi ... | 2007 | 19069762 |
| trabectedin: ecteinascidin 743, ecteinascidin-743, et 743, et-743, nsc 684766. | trabectedin [ecteinascidin 743, yondelis, et 743, nsc 684766] is a tetrahydroisoquinoline alkaloid derived from the caribbean marine tunicate, ecteinascidia turbinata. the drug is being developed by pharmamar (zeltia) in partnership with johnson & johnson pharmaceutical research & development llc. it was synthetically isolated and developed by the university of illinois and licensed to pharmamar; the company has completed the hemisynthesis of agent. trabectedin interacts with the minor groove of ... | 2006 | 16922593 |
| a phase ii study of yondelis (trabectedin, et-743) as a 24-h continuous intravenous infusion in pretreated advanced breast cancer. | yondelis (trabectedin, et-743) is a novel marine-derived anticancer compound found in the ascidian ecteinascidia turbinata. it is currently under phase ii/iii development in breast cancer, hormone refractory prostate cancer, sarcomas and ovarian cancer. activity in breast cancer experimental models has been reported, and preliminary evidence of activity in this setting during the phase i programme has also been observed. the present study assessed the activity and feasibility of trabectedin in w ... | 2006 | 16736024 |
| et743: chemical analysis of the sea squirt ecteinascidia turbinata ecosystem. | the sea squirt ecteinascidia turbinata produces the powerful drug et743. in this study inductively coupled plasma-atomic emission spectroscopy (icp-aes) and matrix assisted laser desorption ionization-mass spectrometry (maldi-ms) are systematically used to measure elemental and molecular species in a florida keys mangrove ecosystem that contains the sea squirt. icp-aes is used to measure the concentration of 27 elements down to the parts per billion level in 16 organisms and 3 sediment samples t ... | 2006 | 16644544 |
| ascidian neural crest-like cells: phylogenetic distribution, relationship to larval complexity, and pigment cell fate. | migratory neural crest-like cells, which express the cell surface antigen hnk-1 and develop into pigment cells, have recently been identified in the ascidian ecteinascidia turbinata. here we use hnk-1 expression as a marker to determine whether neural crest-like cells are responsible for pigment development in diverse ascidian species. we surveyed hnk-1 expression and tyrosinase activity in 12 ascidian species, including those with different adult organizations, developmental modes, and larval s ... | 2006 | 16619245 |
| selective effects of the anticancer drug yondelis (et-743) on cell-cycle promoters. | yondelis is a potent dna-binding anticancer drug isolated from the tunicate ecteinascidia turbinata currently undergoing phase iii clinical trials. we and others have shown selective inhibition to the transcriptional induction of several genes. we tested the hypothesis that yondelis specifically targets cell-cycle genes. our analysis on endogenous and transfected reporter systems revealed complex patterns of transcriptional inhibition and, surprisingly, activation. other inducible systems-the me ... | 2005 | 15961672 |
| migratory neural crest-like cells form body pigmentation in a urochordate embryo. | the neural crest, a source of many different cell types in vertebrate embryos, has not been identified in other chordates. current opinion therefore holds that neural crest cells were a vertebrate innovation. here we describe a migratory cell population resembling neural crest cells in the ascidian urochordate ecteinascidia turbinata. labelling of embryos and larvae with the vital lipophilic dye dii enabled us to detect cells that emerge from the neural tube, migrate into the body wall and sipho ... | 2004 | 15470430 |
| [progress in the studies on antitumor natural product ecteinascidin-743]. | the alkaloid ecteinascidin-743, isolated from the marine tunicate ecteinascidia turbinata, binds to dna and induces cytotoxic effects in several tumors. the drug is being codeveloped by pharma mar and ortho biotech. in may 2001 and october 2003, it was granted orphan drug status by the european commission for soft tissue sarcoma and ovarian cancer, respectively. this paper reviews its research progress, including chemical synthesis, in vitro studies and mechanism of action, antitumor activity in ... | 2004 | 15379280 |
| yondelis (trabectedin, et-743): the development of an anticancer agent of marine origin. | yondelis (trabectedin, et-743) is a novel antitumor agent derived from a marine source, the caribbean tunicate ecteinascidia turbinata. preclinical studies demonstrated activity at low concentrations against a variety of tumors. the mechanism by which et-743 exerts its antitumor activity has not been completely elucidated yet. binding to the minor groove of dna which causes a bend towards the major groove has been demonstrated. furthermore, et-743 interferes with dna binding proteins and transcr ... | 2003 | 12960733 |
| phase i and pharmacokinetic study of yondelis (ecteinascidin-743; et-743) administered as an infusion over 1 h or 3 h every 21 days in patients with solid tumours. | yondelis (et-743) is a novel anticancer agent isolated from the marine ascidian ecteinascidia turbinata. et-743 possesses potent antitumour activity and a novel mechanism of action at the level of gene transcription. we conducted two sequential phase i dose escalation and pharmacokinetic studies of et-743 given as a 1- or a 3-h intravenous (i.v.) infusion. seventy-two adults with metastatic or advanced solid tumours received et-743 in escalating doses between 50 and 1100 microg/m(2), initially a ... | 2003 | 12932661 |
| advances in the chemistry and pharmacology of ecteinascidins, a promising new class of anti-cancer agents. | ecteinascidins are marine natural products consisting of two or three linked tetrahydroisoquinoline subunits and an active carbinolamine functional group. their potent antiproliferative activity against a variety of tumor cells has made them attractive candidates for development as anticancer agents. the lead compound, ecteinascidin 743 (et 743), is currently in phase ii clinical trials but the low amounts present in its natural source, the tunicate ecteinascidia turbinata, made it necessary to ... | 2001 | 12678757 |
| et-743: more than an innovative mechanism of action. | ecteinascidin-743 (et-743), an anti-tumor agent derived from the marine tunicate, ecteinascidia turbinata, is active against various solid tumor cell lines, including soft tissue sarcoma, breast, ovarian, non-small-cell lung and prostate cancers and melanoma, and has a broad spectrum of anti-cancer activity in vivo. for reasons as yet unclear, sarcoma cell lines are exquisitely sensitive to et-743. the drug has a unique mechanism of action that makes it a novel anti-tumor agent. et-743 is a dna- ... | 2002 | 12173491 |
| a clinical armamentarium of marine-derived anti-cancer compounds. | the sea, covering 70% of the earth's surface, offers a considerably broader spectrum of biological diversity than terra firma. containing approximately 75% of all living organisms, the marine environment offers a rich source of natural products with potential therapeutic application. marine organisms have evolved the enzymatic capability to produce potent chemical entities that make them promising sources of innovative cytotoxic compounds. prominent in the identification and development of novel ... | 2002 | 12173490 |
| et-743. | et-743 is a novel antineoplastic dna-binding agent derived from the marine tunicate ecteinascidia turbinata. it has significant cytotoxic activity against soft tissue sarcomas (sts). it also has in vitro activity against melanoma, breast, ovarian, colon, renal, non-small cell lung and prostate carcinomas. the drug has unique mechanism of action which includes in vitro inhibition of transcription-dependent nucleotide excision repair pathways and inhibition of cell cycle progression leading to p53 ... | 2002 | 12010079 |
| clinical pharmacology of the novel marine-derived anticancer agent ecteinascidin 743 administered as a 1- and 3-h infusion in a phase i study. | ecteinascidin 743 (et-743) is an anticancer agent derived from the caribbean tunicate ecteinascidia turbinata. in the present article, the pharmacokinetics and pharmacodynamics of et-743 are described within a phase i study. forty patients with solid tumors initially received et-743 as a 1-h i.v. infusion every 21 days at nine dose levels (50-1100 microg/m(2)). the maximal tolerated dose (mtd) was 1100 microg/m(2), with thrombocytopenia and fatigue as dose-limiting toxicities (dlts). as this mtd ... | 2002 | 11984084 |
| et-743 (pharmamar/nci/ortho biotech). | ecteinascidin-743 (et-743), a tetrahydroisoquinoline alkaloid isolated from the caribbean tunicate, ecteinascidia turbinata, is under development by pharmamar (the pharmaceutical subsidiary of zeltia), the national cancer institute (nci) and ortho biotech, as a potential treatment for several tumor types including breast cancer, lung cancer, ovarian cancer and melanoma. it appears to function by dna minor groove alkylation, which induces topoisomerase i-mediated protein-linked dna strand breakag ... | 2001 | 11763168 |
| [distribution of ecteinascidia turbinata (ascidiacea: perophoridae) in mangroves of the yucatán peninsula, mexico]. | the ascidian ecteinascidia turbinata synthesizes some of the most promising substances against solid-type tumors, but the only available source are the natural populations of this tunicate, which is reared or collected in different parts of the world. a total of 33 locations were sampled in the gulf of mexico and the yucatan peninsula. the tunicate was not found in veracruz, tabasco and campeche, but it was well established on mangrove roots in the yucatan peninsula where we estimated densities ... | 2006 | 11354944 |
| pharmacokinetics and pharmacodynamics of the novel marine-derived anticancer agent ecteinascidin 743 in a phase i dose-finding study. | ecteinascidin (et) 743 is an anticancer agent derived from the caribbean tunicate ecteinascidia turbinata. preclinical studies revealed activity of et-743 against different tumor types. a phase i clinical trial was designed with et-743 to identify the maximum tolerated dose and dose-limiting toxicities (dlts). furthermore, the pharmacokinetics of et-743 and relationships with pharmacodynamics were evaluated. adult patients with solid, resistant tumors received et-743 as a 24-h i.v. infusion ever ... | 2000 | 11156226 |
| antitumor compounds from tunicates. | of the six marine-derived compounds that have reached clinical trials as antitumor agents three-didemnin b, aplidine, and ecteinascidin 743-are derived from tunicates. di-demnin b (db), a cyclic depsipeptide from the compound tunicate trididemnum solidum, was the first marine-derived compound to enter phases i and ii clinical trials. the phase ii studies, sponsored by the u. s. national cancer institute, indicated complete or partial remissions with non-hodgkins lymphoma, but cardiotoxicity caus ... | 2000 | 10608919 |
| effect of ecteinascidin-743 on the interaction between dna binding proteins and dna. | ecteinascidin-743 (et-743) is a tetrahydroisoquinoline alkaloid isolated from ecteinascidia turbinata, a tunicate growing in mangrove roots in caribbean. it has been shown to bind in the minor groove of dna forming covalent adducts by reaction of the n2 of guanine with the carbinolamine moiety. we investigated et-743 ability to inhibit the binding of different transcription factors to their consensus sequences by using gel shift assays. we have selected three types of factors: (i) oncogene produ ... | 1999 | 10500494 |
| molecular and crystal structures of ecteinascidins: potent antitumor compounds from the caribbean tunicate ecteinascidia turbinata. | some members of marine alkaloid ecteinascidins (et's), isolated from the caribbean tunicate ecteinascidia turbinata, exhibit potent anticancer activity. the three dimensional structures of the n12-formyl derivative of et729 1a and the natural n12-oxide of et743 2 have been determined by x-ray crystallography at 0.9 a resolution. compounds 1a and 2 crystallize in the space groups p2(1)2(1)2(1) (a = 23.214(9) a, b = 28.541(10) a and c = 13.303(9) a) and p2(1) (a = 11.720(5) a, b = 13.230(4) a, c = ... | 1993 | 8318161 |
| antitumor activity of aqueous extracts of marine animals. | aqueous extracts (macromolecule fractions in particular) of 25 species of well-known marine animals were tested for their antitumor activity against transplanted sarcoma 180 solid form in icr mice. all of the macromolecule fractions from the extracts of animals in the shellfish category except that of mytilus edulis inhibited the growth of sarcoma 180. the use of aqueous extracts from strongylocentrotus nudus, halocynthia hilgendorfi f. ritteri, styela plicata, ecteinascidia turbinata, and megab ... | 1985 | 4093851 |
| immunostimulatory activity of ecteinascidia turbinata (ete) extract on a variety of animal species. | | 1984 | 6435132 |