Sargachromanols as inhibitors of Na +/K + ATPase and isocitrate lyase
Sargachromanol D ( 4) and H ( 8) were found to be strong Na +/K + ATPase inhibitors, with IC 50 values of 3.6 and 4.6 μM, respectively. Sargachromanols A–P ( 1– 16), 16 meroterpenoids of the chromene class isolated from the brown alga Sargassum siliquastrum, were evaluated for their inhibitory activ...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2011-04, Vol.21 (7), p.1958-1961 |
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| container_issue | 7 |
| container_start_page | 1958 |
| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Chung, Soon-Chun Jang, Kyoung Hwa Park, Jiyoung Ahn, Chan-Hong Shin, Jongheon Oh, Ki-Bong |
| description | Sargachromanol D (
4) and H (
8) were found to be strong Na
+/K
+ ATPase inhibitors, with IC
50 values of 3.6 and 4.6
μM, respectively.
Sargachromanols A–P (
1–
16), 16 meroterpenoids of the chromene class isolated from the brown alga
Sargassum siliquastrum, were evaluated for their inhibitory activities toward Na
+/K
+ ATPase from porcine cerebral cortex and isocitrate lyase (ICL) from
Candida albicans. These studies led to the identification of compounds
4,
6,
8, and
12 as potent Na
+/K
+ ATPase inhibitors. Compounds
12,
13, and
16 exhibited moderate ICL inhibitory activity. Compound
12 also showed weak antibacterial activity. The preliminary structure–activity relationship of these compounds is described to elucidate the essential structural requirements. |
| doi_str_mv | 10.1016/j.bmcl.2011.02.035 |
| format | Article |
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4) and H (
8) were found to be strong Na
+/K
+ ATPase inhibitors, with IC
50 values of 3.6 and 4.6
μM, respectively.
Sargachromanols A–P (
1–
16), 16 meroterpenoids of the chromene class isolated from the brown alga
Sargassum siliquastrum, were evaluated for their inhibitory activities toward Na
+/K
+ ATPase from porcine cerebral cortex and isocitrate lyase (ICL) from
Candida albicans. These studies led to the identification of compounds
4,
6,
8, and
12 as potent Na
+/K
+ ATPase inhibitors. Compounds
12,
13, and
16 exhibited moderate ICL inhibitory activity. Compound
12 also showed weak antibacterial activity. The preliminary structure–activity relationship of these compounds is described to elucidate the essential structural requirements.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2011.02.035</identifier><identifier>PMID: 21377877</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Animals ; Antibacterial activity ; Antibacterial agents ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Benzopyrans - pharmacology ; Biological and medical sciences ; Candida albicans ; Candida albicans - enzymology ; Cerebral Cortex - enzymology ; Chromenes ; Enzyme Inhibitors - pharmacology ; General pharmacology ; Isocitrate lyase ; Isocitrate Lyase - antagonists & inhibitors ; Medical sciences ; Na +/K + ATPase ; Pharmacognosy. Homeopathy. Health food ; Pharmacology. Drug treatments ; Sargachromanols ; Sargassum siliquastrum ; Sodium-Potassium-Exchanging ATPase - antagonists & inhibitors ; Swine</subject><ispartof>Bioorganic & medicinal chemistry letters, 2011-04, Vol.21 (7), p.1958-1961</ispartof><rights>2011 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2011 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c417t-a69acc49e8d2c6ddd762aaa963333dfc490a0aa5c38a84d84b9149c0b892cf5a3</citedby><cites>FETCH-LOGICAL-c417t-a69acc49e8d2c6ddd762aaa963333dfc490a0aa5c38a84d84b9149c0b892cf5a3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2011.02.035$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,45974</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=23982114$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21377877$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chung, Soon-Chun</creatorcontrib><creatorcontrib>Jang, Kyoung Hwa</creatorcontrib><creatorcontrib>Park, Jiyoung</creatorcontrib><creatorcontrib>Ahn, Chan-Hong</creatorcontrib><creatorcontrib>Shin, Jongheon</creatorcontrib><creatorcontrib>Oh, Ki-Bong</creatorcontrib><title>Sargachromanols as inhibitors of Na +/K + ATPase and isocitrate lyase</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Sargachromanol D (
4) and H (
8) were found to be strong Na
+/K
+ ATPase inhibitors, with IC
50 values of 3.6 and 4.6
μM, respectively.
Sargachromanols A–P (
1–
16), 16 meroterpenoids of the chromene class isolated from the brown alga
Sargassum siliquastrum, were evaluated for their inhibitory activities toward Na
+/K
+ ATPase from porcine cerebral cortex and isocitrate lyase (ICL) from
Candida albicans. These studies led to the identification of compounds
4,
6,
8, and
12 as potent Na
+/K
+ ATPase inhibitors. Compounds
12,
13, and
16 exhibited moderate ICL inhibitory activity. Compound
12 also showed weak antibacterial activity. The preliminary structure–activity relationship of these compounds is described to elucidate the essential structural requirements.</description><subject>Animals</subject><subject>Antibacterial activity</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Benzopyrans - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Candida albicans</subject><subject>Candida albicans - enzymology</subject><subject>Cerebral Cortex - enzymology</subject><subject>Chromenes</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>General pharmacology</subject><subject>Isocitrate lyase</subject><subject>Isocitrate Lyase - antagonists & inhibitors</subject><subject>Medical sciences</subject><subject>Na +/K + ATPase</subject><subject>Pharmacognosy. Homeopathy. Health food</subject><subject>Pharmacology. Drug treatments</subject><subject>Sargachromanols</subject><subject>Sargassum siliquastrum</subject><subject>Sodium-Potassium-Exchanging ATPase - antagonists & inhibitors</subject><subject>Swine</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1r3DAQhkVISbZp_0AORZfQQ7Az-rAtQS8hpB80tIWm0JsYS3KixbZSyVvIv6-W3aS3di4DM887DA8hpwxqBqy9WNf9ZMeaA2M18BpEc0BWTLayEhKaQ7IC3UKltPx5TF7mvAZgEqQ8Isecia5TXbci198x3aG9T3HCOY6ZYqZhvg99WGLKNA70C9Lzi8_0nF7efsPsKc6OhhxtWBIuno6PZfiKvBhwzP71vp-QH--vb68-VjdfP3y6uryprGTdUmGr0VqpvXLcts65ruWIqFtRyg1lAwiIjRUKlXRK9ppJbaFXmtuhQXFC3u7uPqT4a-PzYqaQrR9HnH3cZKNa3ikhdfN_sumYAKZ5IfmOtCnmnPxgHlKYMD0aBmbr2azN1rPZejbATfFcQm_25zf95N1z5ElsAc72AGaL45BwtiH_5YRWnDFZuHc7zhdtv4NPJtvgZ-tdSN4uxsXwrz_-ANZ_meY</recordid><startdate>20110401</startdate><enddate>20110401</enddate><creator>Chung, Soon-Chun</creator><creator>Jang, Kyoung Hwa</creator><creator>Park, Jiyoung</creator><creator>Ahn, Chan-Hong</creator><creator>Shin, Jongheon</creator><creator>Oh, Ki-Bong</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20110401</creationdate><title>Sargachromanols as inhibitors of Na +/K + ATPase and isocitrate lyase</title><author>Chung, Soon-Chun ; Jang, Kyoung Hwa ; Park, Jiyoung ; Ahn, Chan-Hong ; Shin, Jongheon ; Oh, Ki-Bong</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c417t-a69acc49e8d2c6ddd762aaa963333dfc490a0aa5c38a84d84b9149c0b892cf5a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Animals</topic><topic>Antibacterial activity</topic><topic>Antibacterial agents</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Benzopyrans - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Candida albicans</topic><topic>Candida albicans - enzymology</topic><topic>Cerebral Cortex - enzymology</topic><topic>Chromenes</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>General pharmacology</topic><topic>Isocitrate lyase</topic><topic>Isocitrate Lyase - antagonists & inhibitors</topic><topic>Medical sciences</topic><topic>Na +/K + ATPase</topic><topic>Pharmacognosy. Homeopathy. Health food</topic><topic>Pharmacology. Drug treatments</topic><topic>Sargachromanols</topic><topic>Sargassum siliquastrum</topic><topic>Sodium-Potassium-Exchanging ATPase - antagonists & inhibitors</topic><topic>Swine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chung, Soon-Chun</creatorcontrib><creatorcontrib>Jang, Kyoung Hwa</creatorcontrib><creatorcontrib>Park, Jiyoung</creatorcontrib><creatorcontrib>Ahn, Chan-Hong</creatorcontrib><creatorcontrib>Shin, Jongheon</creatorcontrib><creatorcontrib>Oh, Ki-Bong</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chung, Soon-Chun</au><au>Jang, Kyoung Hwa</au><au>Park, Jiyoung</au><au>Ahn, Chan-Hong</au><au>Shin, Jongheon</au><au>Oh, Ki-Bong</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Sargachromanols as inhibitors of Na +/K + ATPase and isocitrate lyase</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2011-04-01</date><risdate>2011</risdate><volume>21</volume><issue>7</issue><spage>1958</spage><epage>1961</epage><pages>1958-1961</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Sargachromanol D (
4) and H (
8) were found to be strong Na
+/K
+ ATPase inhibitors, with IC
50 values of 3.6 and 4.6
μM, respectively.
Sargachromanols A–P (
1–
16), 16 meroterpenoids of the chromene class isolated from the brown alga
Sargassum siliquastrum, were evaluated for their inhibitory activities toward Na
+/K
+ ATPase from porcine cerebral cortex and isocitrate lyase (ICL) from
Candida albicans. These studies led to the identification of compounds
4,
6,
8, and
12 as potent Na
+/K
+ ATPase inhibitors. Compounds
12,
13, and
16 exhibited moderate ICL inhibitory activity. Compound
12 also showed weak antibacterial activity. The preliminary structure–activity relationship of these compounds is described to elucidate the essential structural requirements.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>21377877</pmid><doi>10.1016/j.bmcl.2011.02.035</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2011-04, Vol.21 (7), p.1958-1961 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Antibacterial activity Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Benzopyrans - pharmacology Biological and medical sciences Candida albicans Candida albicans - enzymology Cerebral Cortex - enzymology Chromenes Enzyme Inhibitors - pharmacology General pharmacology Isocitrate lyase Isocitrate Lyase - antagonists & inhibitors Medical sciences Na +/K + ATPase Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments Sargachromanols Sargassum siliquastrum Sodium-Potassium-Exchanging ATPase - antagonists & inhibitors Swine |
| title | Sargachromanols as inhibitors of Na +/K + ATPase and isocitrate lyase |
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