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Raymond J. Andersen - One of the best experts on this subject based on the ideXlab platform.
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nigricanosides a and b Antimitotic glycolipids isolated from the green alga avrainvillea nigricans collected in dominica
Journal of the American Chemical Society, 2007Co-Authors: David E Williams, Christopher M Sturgeon, Michel Roberge, Raymond J. AndersenAbstract:The methyl esters 3 and 4 of the Antimitotic glycolipids nigricanosides A (1) and B (2) have been isolated from extracts of the green alga Avrainvillea nigrans collected in Dominica. The structures of 3 and 4 were elucidated by detailed analysis of MS and NMR data. Nigricanoside A dimethyl ester 3 arrests human breast cancer MCF-7 cells in mitosis with an IC50 of 3 nM. Arrested cells have highly disorganized microtubule spindles, compared with the bipolar spindles of untreated metaphase cells. Ester 3 at 20 μM stimulates the polymerization of pure tubulin in vitro and it inhibits the proliferation of both MCF-7 and human colon cancer HCT-116 cells with an IC50 ≈ 3 nM. The nigricanosides are the first examples of a new class of ether-linked glycoglycerolipids. The potent Antimitotic activity of the nigricanosides and their ability to promote tubulin polymerization is without precedent among previously known glycoglycerolipids.
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Nigricanosides A and B, Antimitotic glycolipids isolated from the green alga Avrainvillea nigricans collected in Dominica.
Journal of the American Chemical Society, 2007Co-Authors: David E Williams, Christopher M Sturgeon, Michel Roberge, Raymond J. AndersenAbstract:The methyl esters 3 and 4 of the Antimitotic glycolipids nigricanosides A (1) and B (2) have been isolated from extracts of the green alga Avrainvillea nigrans collected in Dominica. The structures of 3 and 4 were elucidated by detailed analysis of MS and NMR data. Nigricanoside A dimethyl ester 3 arrests human breast cancer MCF-7 cells in mitosis with an IC50 of 3 nM. Arrested cells have highly disorganized microtubule spindles, compared with the bipolar spindles of untreated metaphase cells. Ester 3 at 20 μM stimulates the polymerization of pure tubulin in vitro and it inhibits the proliferation of both MCF-7 and human colon cancer HCT-116 cells with an IC50 ≈ 3 nM. The nigricanosides are the first examples of a new class of ether-linked glycoglycerolipids. The potent Antimitotic activity of the nigricanosides and their ability to promote tubulin polymerization is without precedent among previously known glycoglycerolipids.
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ceratamines a and b Antimitotic heterocyclic alkaloids isolated from the marine sponge pseudoceratina sp collected in papua new guinea
Organic Letters, 2003Co-Authors: Emiliano Manzo, Michel Roberge, Rob Van Soest, Lohi Matainaho, Raymond J. AndersenAbstract:Two novel Antimitotic heterocyclic alkaloids, ceratamines A (1) and B (2), have been isolated from the marine sponge Pseudoceratina sp., collected in Papua New Guinea. The structures of 1 and 2 were elucidated by analysis of spectroscopic data.
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synthesis and Antimitotic cytotoxic activity of hemiasterlin analogues
Journal of Natural Products, 2003Co-Authors: James A Nieman, Michel Roberge, John Coleman, Debra Wallace, Edward Piers, Lynette Lim, Raymond J. AndersenAbstract:The Antimitotic sponge tripeptide hemiasterlin (1) and a number of structural analogues have been synthesized and evaluated in cell-based assays for both cytotoxic and Antimitotic activity in order to explore the SAR for this promising anticancer drug lead. One synthetic analogue, SPA110 (8), showed more potent in vitro cytotoxicty and Antimitotic activity than the natural product hemiasterlin (1), and consequently it has been subjected to thorough preclinical evaluation and targeted for clinical evaluation. The details of the synthesis of hemiasterlin (1) and the analogues and a discussion of how their biological activities vary with their structures are presented in this paper.
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Antimitotic diterpenes from erythropodium caribaeorum test pharmacophore models for microtubule stabilization
Organic Letters, 2000Co-Authors: Bruno Cinel, Michel Roberge, Hans W Behrisch, Leen Van Ofwegen, And Clovis B Castro, Raymond J. AndersenAbstract:Six new Antimitotic diterpenes, 2−7, have been isolated from the Caribbean octocoral Erythropodium caribaeorum. Structural variations encountered in this group of natural products test recently proposed pharmacophore models for microtubule stabilizing compounds.
Magdalena Litaay - One of the best experts on this subject based on the ideXlab platform.
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The Potency of ??-Sitosterol Isolated From Hydroid Aglaophenia cupressina Lamoureoux as Antimitotic Agent towards Seatowards Sea Urchin Tripneustes gratilla Linn.
2017Co-Authors: Eva Johannes, Magdalena LitaayAbstract:The potency of ??-Sitosterol isolated from hydroid Aglaophenia cupressina Lamoureoux as\ud Antimitotic agent towards early cleavage of Sea Urchin Tripneustes gratilla Linn had been\ud conducted. The study aimed to determine ??-Sitosterol activity isolated compound from hydroid A. cupressina Lamoureoux as Antimitotic compound towards early cleavage of zygote of Sea Urchin T. gratilla Linn. Antimitotic treatments were ??-Sitosterol (concentration 1 ??g/ml, 10 ??g/ml and100??g/ml), positive control vincristine (concentration 0.01 ??g/ml, 0.1 ??g/ml, and 1 ??g/ml) and negative control. A protozoa-free seawater was used in this assay. The results revealed that ??-Sitosterol compound had the highest inhibition activity at concentration of 100 ??g/ml was 69.22 % with IC-50 on 0.95 ??g/ml which could develop as cancer chemotherapy compound. Keywords: Antimitotic, ??-Sitosterol, Hydroid Aglaophenia cupressina Lamoureoux, Tripneustes gratilla\ud Linn
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the potency of β sitosterol isolated from hydroid aglaophenia cupressina lamoureoux as Antimitotic agent towards sea urchin tripneustes gratilla linn
International Journal of Engineering, 2017Co-Authors: Afriansyah Afriansyah, Eva Johannes, Sjafaraenan Sjafaraenan, Magdalena LitaayAbstract:The potency of β-Sitosterol isolated from hydroid Aglaophenia cupressina Lamoureoux as Antimitotic agent towards early cleavage of Sea Urchin Tripneustes gratilla Linn had been conducted. The study aimed to determine β-Sitosterol activity isolated compound from hydroid A. cupressina Lamoureoux as Antimitotic compound towards early cleavage of zygote of Sea Urchin T. gratilla Linn. Antimitotic treatments were β-Sitosterol (concentration 1 µg/ml, 10 µg/ml and100 µg/ml), positive control vincristine (concentration 0.01 µg/ml, 0.1 µg/ml, and 1 µg/ml) and negative control. A protozoa-free seawater was used in this assay. The results revealed that β-Sitosterol compound had the highest inhibition activity at concentration of 100 μg/ml was 69.22 % with IC-50 on 0.95 µg/ml which could develop as cancer chemotherapy compound.
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UJI ANTIMITOTIK SENYAWA ??-SITOSTEROL HASIL ISOLASI DARI HYDROID Aglaophenia cupressina Lamoureoux TERHADAP PEMBELAHAN AWAL SEL ZIGOT BULU BABI Tripneustes gratilla Linn
2016Co-Authors: Eva Johannes, Magdalena LitaayAbstract:Telah dilakukan penelitian uji antimitotik senyawa ??-Sitosterol hasil isolasi dari Hydroid Aglaophenia cupressina Lamoureoux terhadap pembelahan awal sel zigot bulu babi Tripneustes gratilla Linn. Penelitian ini bertujuan untuk mengetahui aktivitas senyawa ??-sitosterol hasil isolasi dari hydroid A. cupressina Lamoureoux sebagai bahan antimitotik pembelahan awal (cleavage pertama) sel zigot bulu babi T. gratilla Linn. Uji antimitotik dilakukan terhadap pembelahan awal (cleavage pertama) sel zigot bulu babi T. gratilla Linn dengan senyawa uji ??-Sitosterol (konsentrasi 1 ??g/ml, 10 ??g/ml dan 100 ??g/ml), kontrol positif vinkristin (konsentrasi 0.01 ??g/ml, 0.1 ??g/ml, dan 1 ??g/ml) dan kontrol negatif dengan air laut bebas protozoa (ALBP). Hasil yang diperoleh menunjukkan bahwa senyawa ??-Sitosterol memiliki nilai penghambatan tertinggi pada konsentrasi 100 ??g/ml yaitu 69,22 % dengan nilai IC-50 sebesar 0,95 ??g/ml yang dapat dikembangkan sebagai bahan dasar kemoterapi kanker.\ud \ud Kata Kunci: Antimitotik, ??-Sitosterol, Hydroid Aglaophenia cupressina Lamoureoux, Tripneustes gratilla Linn
L D Konyushkin - One of the best experts on this subject based on the ideXlab platform.
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sea urchin embryo model as a reliable in vivo phenotypic screen to characterize selective Antimitotic molecules comparative evaluation of combretapyrazoles isoxazoles 1 2 3 triazoles and pyrroles as tubulin binding agents
ACS Combinatorial Science, 2018Co-Authors: Marina N Semenova, Dmitry V Tsyganov, Dmitry V Demchuk, N B Chernysheva, Alexander V Samet, Eugenia A Silyanova, V P Kislyi, Anna S Maksimenko, Alexander E Varakutin, L D KonyushkinAbstract:A series of both novel and reported combretastatin analogues, including diarylpyrazoles, -isoxazoles, -1,2,3-triazoles, and -pyrroles, were synthesized via improved protocols to evaluate their Antimitotic antitubulin activity using in vivo sea urchin embryo assay and a panel of human cancer cells. A systematic comparative structure–activity relationship studies of these compounds were conducted. Pyrazoles 1i and 1p, isoxazole 3a, and triazole 7b were found to be the most potent Antimitotics across all tested compounds causing cleavage alteration of the sea urchin embryo at 1, 0.25, 1, and 0.5 nM, respectively. These agents exhibited comparable cytotoxicity against human cancer cells. Structure–activity relationship studies revealed that compounds substituted with 3,4,5-trimethoxyphenyl ring A and 4-methoxyphenyl ring B displayed the highest activity. 3-Hydroxy group in the ring B was essential for the antiproliferative activity in the diarylisoxazole series, whereas it was not required for potency of diar...
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Sea Urchin Embryo Model As a Reliable in Vivo Phenotypic Screen to Characterize Selective Antimitotic Molecules. Comparative evaluation of Combretapyrazoles, -isoxazoles, -1,2,3-triazoles, and -pyrroles as Tubulin-Binding Agents
2018Co-Authors: Marina N. Semenova, Dmitry V Tsyganov, Dmitry V Demchuk, N B Chernysheva, Alexander V Samet, Eugenia A Silyanova, V P Kislyi, Anna S Maksimenko, Alexander E Varakutin, L D KonyushkinAbstract:A series of both novel and reported combretastatin analogues, including diarylpyrazoles, -isoxazoles, -1,2,3-triazoles, and -pyrroles, were synthesized via improved protocols to evaluate their Antimitotic antitubulin activity using in vivo sea urchin embryo assay and a panel of human cancer cells. A systematic comparative structure–activity relationship studies of these compounds were conducted. Pyrazoles 1i and 1p, isoxazole 3a, and triazole 7b were found to be the most potent Antimitotics across all tested compounds causing cleavage alteration of the sea urchin embryo at 1, 0.25, 1, and 0.5 nM, respectively. These agents exhibited comparable cytotoxicity against human cancer cells. Structure–activity relationship studies revealed that compounds substituted with 3,4,5-trimethoxyphenyl ring A and 4-methoxyphenyl ring B displayed the highest activity. 3-Hydroxy group in the ring B was essential for the antiproliferative activity in the diarylisoxazole series, whereas it was not required for potency of diarylpyrazoles. Isoxazoles 3 with 3,4,5-trimethoxy-substituted ring A and 3-hydroxy-4-methoxy-substituted ring B were more active than the respective pyrazoles 1. Of the azoles substituted with the same set of other aryl pharmacophores, diarylpyrazoles 1, 4,5-diarylisoxazoles 3, and 4,5-diaryl-1,2,3-triazoles 7 displayed similar strongest Antimitotic antitubulin effect followed by 3,4-diarylisoxazoles 5, 1,5-diaryl-1,2,3-triazoles 8, and pyrroles 10 that showed the lowest activity. Introduction of the amino group into the heterocyclic core decreased the Antimitotic antitubulin effect of pyrazoles, triazoles, and to a lesser degree of 4,5-diarylisoxazoles, whereas potency of the respective 3,4-diarylisoxazoles was increased
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synthesis of polyalkoxy 3 4 methoxyphenyl coumarins with Antimitotic activity from plant allylpolyalkoxybenzenes
ChemInform, 2013Co-Authors: Dmitry V Tsyganov, Marina N Semenova, L D Konyushkin, N B Chernysheva, Lev K Salamandra, Olga P Atamanenko, Victor V SemenovAbstract:Coumarins, analogues of natural Antimitotic compounds, are synthesized and tested in vivo in the phenotypic sea urchin embryo assay for antiproliferative antitubulin activity.
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synthesis of polyalkoxy 3 4 methoxyphenyl coumarins with Antimitotic activity from plant allylpolyalkoxybenzenes
Mendeleev Communications, 2013Co-Authors: Dmitry V Tsyganov, Marina N Semenova, L D Konyushkin, N B Chernysheva, Lev K Salamandra, Olga P Atamanenko, Victor V SemenovAbstract:Novel polyalkoxy-3-(4-methoxyphenyl)coumarins – analogues of natural Antimitotic compounds – were synthesized from plant allylpolyalkoxybenzenes and tested in vivo in the phenotypic sea urchin embryo assay for antiproliferative antitubulin activity.
Eva Johannes - One of the best experts on this subject based on the ideXlab platform.
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The Potency of ??-Sitosterol Isolated From Hydroid Aglaophenia cupressina Lamoureoux as Antimitotic Agent towards Seatowards Sea Urchin Tripneustes gratilla Linn.
2017Co-Authors: Eva Johannes, Magdalena LitaayAbstract:The potency of ??-Sitosterol isolated from hydroid Aglaophenia cupressina Lamoureoux as\ud Antimitotic agent towards early cleavage of Sea Urchin Tripneustes gratilla Linn had been\ud conducted. The study aimed to determine ??-Sitosterol activity isolated compound from hydroid A. cupressina Lamoureoux as Antimitotic compound towards early cleavage of zygote of Sea Urchin T. gratilla Linn. Antimitotic treatments were ??-Sitosterol (concentration 1 ??g/ml, 10 ??g/ml and100??g/ml), positive control vincristine (concentration 0.01 ??g/ml, 0.1 ??g/ml, and 1 ??g/ml) and negative control. A protozoa-free seawater was used in this assay. The results revealed that ??-Sitosterol compound had the highest inhibition activity at concentration of 100 ??g/ml was 69.22 % with IC-50 on 0.95 ??g/ml which could develop as cancer chemotherapy compound. Keywords: Antimitotic, ??-Sitosterol, Hydroid Aglaophenia cupressina Lamoureoux, Tripneustes gratilla\ud Linn
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the potency of β sitosterol isolated from hydroid aglaophenia cupressina lamoureoux as Antimitotic agent towards sea urchin tripneustes gratilla linn
International Journal of Engineering, 2017Co-Authors: Afriansyah Afriansyah, Eva Johannes, Sjafaraenan Sjafaraenan, Magdalena LitaayAbstract:The potency of β-Sitosterol isolated from hydroid Aglaophenia cupressina Lamoureoux as Antimitotic agent towards early cleavage of Sea Urchin Tripneustes gratilla Linn had been conducted. The study aimed to determine β-Sitosterol activity isolated compound from hydroid A. cupressina Lamoureoux as Antimitotic compound towards early cleavage of zygote of Sea Urchin T. gratilla Linn. Antimitotic treatments were β-Sitosterol (concentration 1 µg/ml, 10 µg/ml and100 µg/ml), positive control vincristine (concentration 0.01 µg/ml, 0.1 µg/ml, and 1 µg/ml) and negative control. A protozoa-free seawater was used in this assay. The results revealed that β-Sitosterol compound had the highest inhibition activity at concentration of 100 μg/ml was 69.22 % with IC-50 on 0.95 µg/ml which could develop as cancer chemotherapy compound.
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aktivitas uji antimitotik senyawa asam heksadekanoat isolat dari hydroid aglaophenia cupressina lamoureoux pada cleavage bulu babi tripneustes gratilla linn
BIOMA : JURNAL BIOLOGI MAKASSAR, 2017Co-Authors: Sjafaraenan Sjafaraenan, Eva JohannesAbstract:Abstrak Studi tentang aktivitas antimitotik senyawa asam heksadekanoat isolat dari hydroid Aglaopehenia cupressina Lamoureoux pada cleavage bulu babi Tripneustes gratilla Linn. Penelitian ini bertujuan untuk mengetahui pengaruh senyawa bioaktif asam heksadekanoat dari hydroid Aglaopehenia cupressina Lamoureoux pada cleavage bulu babi Tripneustes gratilla Linn. Metode yang digunakan adalah metode uji aktivitas antimitotik senyawa asam heksadekanoat pada cleavage bulu babi Tripneustes gratilla Linn. pada konsentrasi 1, 10, dan 100 µg/ml dengan kontrol positif vinkristin pada konsentrasi 0.01, 0.1, dan 1 µg/ml setelah fertilisasi penghambatan tertinggi terjadi pada konsentrasi 100 µg/ml yaitu 66,66 %. Kemudian setelah dihitung dengan analisis probit, asam heksadekanoat memiliki IC50 sebesar 22,076 µg/ml yang memiliki kesamaan sifat antimitotik dengan vinkristin yang memiliki IC 50 sebesar 0,219 µg/ml. Sehingga asam heksadekanoat isolat dari hydroid Aglaopehenia cupressina Lamoureoux berpotensi untuk dijadikan bahan dasar anti kanker
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UJI ANTIMITOTIK SENYAWA ??-SITOSTEROL HASIL ISOLASI DARI HYDROID Aglaophenia cupressina Lamoureoux TERHADAP PEMBELAHAN AWAL SEL ZIGOT BULU BABI Tripneustes gratilla Linn
2016Co-Authors: Eva Johannes, Magdalena LitaayAbstract:Telah dilakukan penelitian uji antimitotik senyawa ??-Sitosterol hasil isolasi dari Hydroid Aglaophenia cupressina Lamoureoux terhadap pembelahan awal sel zigot bulu babi Tripneustes gratilla Linn. Penelitian ini bertujuan untuk mengetahui aktivitas senyawa ??-sitosterol hasil isolasi dari hydroid A. cupressina Lamoureoux sebagai bahan antimitotik pembelahan awal (cleavage pertama) sel zigot bulu babi T. gratilla Linn. Uji antimitotik dilakukan terhadap pembelahan awal (cleavage pertama) sel zigot bulu babi T. gratilla Linn dengan senyawa uji ??-Sitosterol (konsentrasi 1 ??g/ml, 10 ??g/ml dan 100 ??g/ml), kontrol positif vinkristin (konsentrasi 0.01 ??g/ml, 0.1 ??g/ml, dan 1 ??g/ml) dan kontrol negatif dengan air laut bebas protozoa (ALBP). Hasil yang diperoleh menunjukkan bahwa senyawa ??-Sitosterol memiliki nilai penghambatan tertinggi pada konsentrasi 100 ??g/ml yaitu 69,22 % dengan nilai IC-50 sebesar 0,95 ??g/ml yang dapat dikembangkan sebagai bahan dasar kemoterapi kanker.\ud \ud Kata Kunci: Antimitotik, ??-Sitosterol, Hydroid Aglaophenia cupressina Lamoureoux, Tripneustes gratilla Linn
Michel Roberge - One of the best experts on this subject based on the ideXlab platform.
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nigricanosides a and b Antimitotic glycolipids isolated from the green alga avrainvillea nigricans collected in dominica
Journal of the American Chemical Society, 2007Co-Authors: David E Williams, Christopher M Sturgeon, Michel Roberge, Raymond J. AndersenAbstract:The methyl esters 3 and 4 of the Antimitotic glycolipids nigricanosides A (1) and B (2) have been isolated from extracts of the green alga Avrainvillea nigrans collected in Dominica. The structures of 3 and 4 were elucidated by detailed analysis of MS and NMR data. Nigricanoside A dimethyl ester 3 arrests human breast cancer MCF-7 cells in mitosis with an IC50 of 3 nM. Arrested cells have highly disorganized microtubule spindles, compared with the bipolar spindles of untreated metaphase cells. Ester 3 at 20 μM stimulates the polymerization of pure tubulin in vitro and it inhibits the proliferation of both MCF-7 and human colon cancer HCT-116 cells with an IC50 ≈ 3 nM. The nigricanosides are the first examples of a new class of ether-linked glycoglycerolipids. The potent Antimitotic activity of the nigricanosides and their ability to promote tubulin polymerization is without precedent among previously known glycoglycerolipids.
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Nigricanosides A and B, Antimitotic glycolipids isolated from the green alga Avrainvillea nigricans collected in Dominica.
Journal of the American Chemical Society, 2007Co-Authors: David E Williams, Christopher M Sturgeon, Michel Roberge, Raymond J. AndersenAbstract:The methyl esters 3 and 4 of the Antimitotic glycolipids nigricanosides A (1) and B (2) have been isolated from extracts of the green alga Avrainvillea nigrans collected in Dominica. The structures of 3 and 4 were elucidated by detailed analysis of MS and NMR data. Nigricanoside A dimethyl ester 3 arrests human breast cancer MCF-7 cells in mitosis with an IC50 of 3 nM. Arrested cells have highly disorganized microtubule spindles, compared with the bipolar spindles of untreated metaphase cells. Ester 3 at 20 μM stimulates the polymerization of pure tubulin in vitro and it inhibits the proliferation of both MCF-7 and human colon cancer HCT-116 cells with an IC50 ≈ 3 nM. The nigricanosides are the first examples of a new class of ether-linked glycoglycerolipids. The potent Antimitotic activity of the nigricanosides and their ability to promote tubulin polymerization is without precedent among previously known glycoglycerolipids.
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ceratamines a and b Antimitotic heterocyclic alkaloids isolated from the marine sponge pseudoceratina sp collected in papua new guinea
Organic Letters, 2003Co-Authors: Emiliano Manzo, Michel Roberge, Rob Van Soest, Lohi Matainaho, Raymond J. AndersenAbstract:Two novel Antimitotic heterocyclic alkaloids, ceratamines A (1) and B (2), have been isolated from the marine sponge Pseudoceratina sp., collected in Papua New Guinea. The structures of 1 and 2 were elucidated by analysis of spectroscopic data.
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synthesis and Antimitotic cytotoxic activity of hemiasterlin analogues
Journal of Natural Products, 2003Co-Authors: James A Nieman, Michel Roberge, John Coleman, Debra Wallace, Edward Piers, Lynette Lim, Raymond J. AndersenAbstract:The Antimitotic sponge tripeptide hemiasterlin (1) and a number of structural analogues have been synthesized and evaluated in cell-based assays for both cytotoxic and Antimitotic activity in order to explore the SAR for this promising anticancer drug lead. One synthetic analogue, SPA110 (8), showed more potent in vitro cytotoxicty and Antimitotic activity than the natural product hemiasterlin (1), and consequently it has been subjected to thorough preclinical evaluation and targeted for clinical evaluation. The details of the synthesis of hemiasterlin (1) and the analogues and a discussion of how their biological activities vary with their structures are presented in this paper.
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Antimitotic diterpenes from erythropodium caribaeorum test pharmacophore models for microtubule stabilization
Organic Letters, 2000Co-Authors: Bruno Cinel, Michel Roberge, Hans W Behrisch, Leen Van Ofwegen, And Clovis B Castro, Raymond J. AndersenAbstract:Six new Antimitotic diterpenes, 2−7, have been isolated from the Caribbean octocoral Erythropodium caribaeorum. Structural variations encountered in this group of natural products test recently proposed pharmacophore models for microtubule stabilizing compounds.
