The Experts below are selected from a list of 1428 Experts worldwide ranked by ideXlab platform
Nunziatina De Tommasi - One of the best experts on this subject based on the ideXlab platform.
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A fast and efficient LC-MS/MS method for detection, identification and quantitative analysis of bioactive Sesterterpenes in Salvia dominica crude extracts.
Journal of pharmaceutical and biomedical analysis, 2009Co-Authors: Fabrizio Dal Piaz, Laura Lepore, Ammar Bader, Salvatore Imparato, Nunziatina De TommasiAbstract:Sesterterpenes are a small group of terpenoids showing a number of interesting pharmacological properties, including cytotoxicity, anti-inflammatory, anti-microbial and anti-angiogenic activities and platelet aggregation inhibition. Recently, some Sesterterpene lactones isolated from Salvia dominica have been shown to modulate enzymatic activity of tubulin tyrosine ligase (TTL), a promising target for new anticancer therapeutic strategies. However, to allow a direct use of S. dominica extracts as a source of TTL inhibitors, analytical method aimed to their fast qualitative and quantitative characterization is required. Despite the structural features and diverse biological activities of sesterterpenoids, actually no analytical method for their quantization into complex mixtures has been published. Here we describe an LC–MS/MS method aimed to qualitative and quantitative analysis of Sesterterpenes lactones in the crude extracts obtained from different parts of S. dominica. This approach allowed us to characterize all the Sesterterpenes by a single step analysis and also to identify two unknown compounds. Moreover, a quantitative comparison of the composition in Sesterterpenes of extracts obtained from S. dominica leaves, roots and leaf galls was performed, leading to the definition of both leaves and leaf galls as suitable sources of TTL inhibitors.
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Sesterterpenes as Tubulin Tyrosine Ligase Inhibitors. First Insight of Structure−Activity Relationships and Discovery of New Lead
Journal of medicinal chemistry, 2009Co-Authors: Fabrizio Dal Piaz, Antonio Vassallo, Laura Lepore, Alessandra Tosco, Ammar Bader, Nunziatina De TommasiAbstract:Twenty-four new Sesterterpenes, compounds 1−24, were isolated from the aerial parts of Salvia dominica. Their structures were elucidated by 1D and 2D NMR experiments as well as ESIMS analysis and chemical methods. The evaluation of the biological activity of Salvia dominica Sesterterpenes by means of a panel of chemical and biological approaches, including chemical proteomics, surface plasmon resonance (SPR) measurements, and biochemical assays were realized. Obtained results showed that 18 out of the 24 Sesterterpene lactones isolated from Salvia dominica interact with tubulin−tyrosine ligase (TTL) an enzyme involved in the tyrosination cycle of the C-terminal of tubulin, and inhibit TTL activity in cancer cells. Besides, results of our studies provided an activity/structure relationship that can be used to design effective TTL inhibitors.
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Sesterterpenes as Tubulin Tyrosine Ligase Inhibitors. First Insight of Structure-Activity Relationships and Discovery of New Lead
2009Co-Authors: Fabrizio Dal Piaz, Antonio Vassallo, Laura Lepore, Alessandra Tosco, Ammar Bader, Nunziatina De TommasiAbstract:Twenty-four new Sesterterpenes, compounds 1-24, were isolated from the aerial parts of SalVia dominica. Their structures were elucidated by 1D and 2D NMR experiments as well as ESIMS analysis and chemical methods. The evaluation of the biological activity of SalVia dominica Sesterterpenes by means of a panel of chemical and biological approaches, including chemical proteomics, surface plasmon resonance (SPR) measurements, and biochemical assays were realized. Obtained results showed that 18 out of the 24 Sesterterpene lactones isolated from SalVia dominica interact with tubulin-tyrosine ligase (TTL) an enzyme involved in the tyrosination cycle of the C-terminal of tubulin, and inhibit TTL activity in cancer cells. Besides, results of our studies provided an activity/structure relationship that can be used to design effective TTL inhibitors
Bill J. Baker - One of the best experts on this subject based on the ideXlab platform.
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new cytotoxic Sesterterpenes from the marine sponge spongia sp
Tetrahedron Letters, 1994Co-Authors: Haiyin He, Bill J. Baker, Palaniappan KulanthaivelAbstract:Abstract Six new cytotoxic Sesterterpene lactones, spongianolides A-F ( 1–6 ) were isolated from the extracts of the marine sponge Spongia sp. The structures were determined by the interpretation of spectral data.
Fabrizio Dal Piaz - One of the best experts on this subject based on the ideXlab platform.
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A fast and efficient LC-MS/MS method for detection, identification and quantitative analysis of bioactive Sesterterpenes in Salvia dominica crude extracts.
Journal of pharmaceutical and biomedical analysis, 2009Co-Authors: Fabrizio Dal Piaz, Laura Lepore, Ammar Bader, Salvatore Imparato, Nunziatina De TommasiAbstract:Sesterterpenes are a small group of terpenoids showing a number of interesting pharmacological properties, including cytotoxicity, anti-inflammatory, anti-microbial and anti-angiogenic activities and platelet aggregation inhibition. Recently, some Sesterterpene lactones isolated from Salvia dominica have been shown to modulate enzymatic activity of tubulin tyrosine ligase (TTL), a promising target for new anticancer therapeutic strategies. However, to allow a direct use of S. dominica extracts as a source of TTL inhibitors, analytical method aimed to their fast qualitative and quantitative characterization is required. Despite the structural features and diverse biological activities of sesterterpenoids, actually no analytical method for their quantization into complex mixtures has been published. Here we describe an LC–MS/MS method aimed to qualitative and quantitative analysis of Sesterterpenes lactones in the crude extracts obtained from different parts of S. dominica. This approach allowed us to characterize all the Sesterterpenes by a single step analysis and also to identify two unknown compounds. Moreover, a quantitative comparison of the composition in Sesterterpenes of extracts obtained from S. dominica leaves, roots and leaf galls was performed, leading to the definition of both leaves and leaf galls as suitable sources of TTL inhibitors.
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Sesterterpenes as Tubulin Tyrosine Ligase Inhibitors. First Insight of Structure−Activity Relationships and Discovery of New Lead
Journal of medicinal chemistry, 2009Co-Authors: Fabrizio Dal Piaz, Antonio Vassallo, Laura Lepore, Alessandra Tosco, Ammar Bader, Nunziatina De TommasiAbstract:Twenty-four new Sesterterpenes, compounds 1−24, were isolated from the aerial parts of Salvia dominica. Their structures were elucidated by 1D and 2D NMR experiments as well as ESIMS analysis and chemical methods. The evaluation of the biological activity of Salvia dominica Sesterterpenes by means of a panel of chemical and biological approaches, including chemical proteomics, surface plasmon resonance (SPR) measurements, and biochemical assays were realized. Obtained results showed that 18 out of the 24 Sesterterpene lactones isolated from Salvia dominica interact with tubulin−tyrosine ligase (TTL) an enzyme involved in the tyrosination cycle of the C-terminal of tubulin, and inhibit TTL activity in cancer cells. Besides, results of our studies provided an activity/structure relationship that can be used to design effective TTL inhibitors.
Jongheon Shin - One of the best experts on this subject based on the ideXlab platform.
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Cytotoxic Scalarane Sesterterpenes from the Sponge Hyrtios erectus
Marine drugs, 2020Co-Authors: Oh-seok Kwon, Chung J. Sim, Chang-kwon Kim, Donghwa Kim, Jeongyoon Sun, Sang Kook Lee, Jongheon ShinAbstract:Twelve new Sesterterpenes along with eight known Sesterterpenes were isolated from the marine sponge Hyrtios erectus collected off the coast of Chuuk Island, the Federated State of Micronesia. Based upon a combination of spectroscopic and computational analyses, these compounds were determined to be eight glycine-bearing scalaranes (1–8), a 3-keto scalarane (9), two oxidized-furan-bearing scalaranes (10 and 11), and a salmahyrtisane (12). Several of these compounds exhibited weak antiproliferation against diverse cancer cell lines as well as moderate anti-angiogenesis activities. The antiproliferative activity of new compound 4 was found to be associated with G0/G1 arrest in the cell cycle.
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Gombaspiroketals A-C, Sesterterpenes from the sponge Clathria gombawuiensis.
Organic letters, 2014Co-Authors: Jung-kyun Woo, Chang-kwon Kim, Seong-hwan Kim, Heegyu Kim, Jongheon ShinAbstract:Gombaspiroketals A–C (1–3), tetracyclic Sesterterpenes of a novel skeletal class, were isolated from the Korean marine sponge Clathria gombawuiensis. On the basis of the combined spectroscopic analyses, the structures of these compounds were determined to be highly rearranged Sesterterpene spiroketal methoxyacetals (1 and 2) and a corresponding hemiacetal (3). The relative and absolute configurations were assigned by NOESY analysis and ECD calculations, respectively. These compounds exhibited moderate cytotoxicities and antibacterial activities.
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Gombaspiroketals A–C, Sesterterpenes from the Sponge Clathria gombawuiensis
2014Co-Authors: Jung-kyun Woo, Chang-kwon Kim, Seong-hwan Kim, Heegyu Kim, Jongheon ShinAbstract:Gombaspiroketals A–C (1–3), tetracyclic Sesterterpenes of a novel skeletal class, were isolated from the Korean marine sponge Clathria gombawuiensis. On the basis of the combined spectroscopic analyses, the structures of these compounds were determined to be highly rearranged Sesterterpene spiroketal methoxyacetals (1 and 2) and a corresponding hemiacetal (3). The relative and absolute configurations were assigned by NOESY analysis and ECD calculations, respectively. These compounds exhibited moderate cytotoxicities and antibacterial activities
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Scalarane Sesterterpenes from the sponge Hyatella sp.
Journal of natural products, 2011Co-Authors: Ju-eun Jeon, Jaemin Bae, Kyung Jin Lee, Jongheon ShinAbstract:Five new Sesterterpenes (7−11) along with six known compounds (1−6) were isolated from the sponge Hyatella sp., collected off the coast of Soheuksan-do, Korea. Spectroscopic analyses revealed these compounds as scalarane Sesterterpenes with oxidized furan moieties (7−10) and a corresponding lactam (11). The compounds exhibited moderate cytotoxicity, antibacterial activity, and weak inhibitory activity against isocitrate lyase.
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Scalarane Sesterterpenes from the sponge Smenospongia sp.
Journal of natural products, 2008Co-Authors: Jueun Song, Wooyeol Jeong, Nan Wang, Hyi-seung Lee, Chung J. Sim, Jongheon ShinAbstract:Ten new Sesterterpene compounds (4−13) and seven known metabolites (1−3, 14−17) were isolated from the sponge Smenospongia sp. collected from Korean coastal waters. On the basis of combined spectroscopic analyses, the new compounds exhibited diverse functionalities on a common scalarane Sesterterpene structure. The presence of a 23-aldehyde on compound 6 and a 20-carboxylic acid on 11 is unprecedented among sponge-derived scalarane Sesterterpenes. Several of the new compounds showed significant cytotoxicity and antimicrobial activity, as well as moderate inhibitory activity against isocitrate lyase.
Laura Lepore - One of the best experts on this subject based on the ideXlab platform.
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A fast and efficient LC-MS/MS method for detection, identification and quantitative analysis of bioactive Sesterterpenes in Salvia dominica crude extracts.
Journal of pharmaceutical and biomedical analysis, 2009Co-Authors: Fabrizio Dal Piaz, Laura Lepore, Ammar Bader, Salvatore Imparato, Nunziatina De TommasiAbstract:Sesterterpenes are a small group of terpenoids showing a number of interesting pharmacological properties, including cytotoxicity, anti-inflammatory, anti-microbial and anti-angiogenic activities and platelet aggregation inhibition. Recently, some Sesterterpene lactones isolated from Salvia dominica have been shown to modulate enzymatic activity of tubulin tyrosine ligase (TTL), a promising target for new anticancer therapeutic strategies. However, to allow a direct use of S. dominica extracts as a source of TTL inhibitors, analytical method aimed to their fast qualitative and quantitative characterization is required. Despite the structural features and diverse biological activities of sesterterpenoids, actually no analytical method for their quantization into complex mixtures has been published. Here we describe an LC–MS/MS method aimed to qualitative and quantitative analysis of Sesterterpenes lactones in the crude extracts obtained from different parts of S. dominica. This approach allowed us to characterize all the Sesterterpenes by a single step analysis and also to identify two unknown compounds. Moreover, a quantitative comparison of the composition in Sesterterpenes of extracts obtained from S. dominica leaves, roots and leaf galls was performed, leading to the definition of both leaves and leaf galls as suitable sources of TTL inhibitors.
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Sesterterpenes as Tubulin Tyrosine Ligase Inhibitors. First Insight of Structure−Activity Relationships and Discovery of New Lead
Journal of medicinal chemistry, 2009Co-Authors: Fabrizio Dal Piaz, Antonio Vassallo, Laura Lepore, Alessandra Tosco, Ammar Bader, Nunziatina De TommasiAbstract:Twenty-four new Sesterterpenes, compounds 1−24, were isolated from the aerial parts of Salvia dominica. Their structures were elucidated by 1D and 2D NMR experiments as well as ESIMS analysis and chemical methods. The evaluation of the biological activity of Salvia dominica Sesterterpenes by means of a panel of chemical and biological approaches, including chemical proteomics, surface plasmon resonance (SPR) measurements, and biochemical assays were realized. Obtained results showed that 18 out of the 24 Sesterterpene lactones isolated from Salvia dominica interact with tubulin−tyrosine ligase (TTL) an enzyme involved in the tyrosination cycle of the C-terminal of tubulin, and inhibit TTL activity in cancer cells. Besides, results of our studies provided an activity/structure relationship that can be used to design effective TTL inhibitors.
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Sesterterpenes as Tubulin Tyrosine Ligase Inhibitors. First Insight of Structure-Activity Relationships and Discovery of New Lead
2009Co-Authors: Fabrizio Dal Piaz, Antonio Vassallo, Laura Lepore, Alessandra Tosco, Ammar Bader, Nunziatina De TommasiAbstract:Twenty-four new Sesterterpenes, compounds 1-24, were isolated from the aerial parts of SalVia dominica. Their structures were elucidated by 1D and 2D NMR experiments as well as ESIMS analysis and chemical methods. The evaluation of the biological activity of SalVia dominica Sesterterpenes by means of a panel of chemical and biological approaches, including chemical proteomics, surface plasmon resonance (SPR) measurements, and biochemical assays were realized. Obtained results showed that 18 out of the 24 Sesterterpene lactones isolated from SalVia dominica interact with tubulin-tyrosine ligase (TTL) an enzyme involved in the tyrosination cycle of the C-terminal of tubulin, and inhibit TTL activity in cancer cells. Besides, results of our studies provided an activity/structure relationship that can be used to design effective TTL inhibitors
