Flavonoids: Potent inhibitors of arachidonate 5-lipoxygenase
Various flavonoids were found to be relatively selective inhibitors of arachidonate 5-lipoxygenase which initiates the biosynthesis of leukotrienes with the activity of slow reacting substance of anaphylaxis. Cirsiliol (3′,4′,5-trihydroxy-6,7-dimethoxyflavone) was most potent, and the enzyme partial...
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| Veröffentlicht in: | Biochemical and biophysical research communications 1983-10, Vol.116 (2), p.612-618 |
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| container_title | Biochemical and biophysical research communications |
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| creator | Yoshimoto, Tanihiro Furukawa, Masayuki Yamamoto, Shozo Horie, Tokunaru Watanabe-Kohno, Shigekatsu |
| description | Various flavonoids were found to be relatively selective inhibitors of arachidonate 5-lipoxygenase which initiates the biosynthesis of leukotrienes with the activity of slow reacting substance of anaphylaxis. Cirsiliol (3′,4′,5-trihydroxy-6,7-dimethoxyflavone) was most potent, and the enzyme partially purified from rat basophilic leukemia cells was inhibited by 97% at a concentration of 10 μM (IC
50, about 0.1 μM). 12-Lipoxygenases from bovine platelets and porcine leukocytes were also inhibited but at higher concentrations (IC
50, about 1 μM), and fatty acid cyclooxygenase purified from bovine vesicular gland was scarcely affected. The compound at 10 μM suppressed by 99% the immunological release of slow reacting substance of anaphylaxis from passively sensitized guinea pig lung (IC
50, about 0.4 μM). |
| doi_str_mv | 10.1016/0006-291X(83)90568-5 |
| format | Article |
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50, about 0.1 μM). 12-Lipoxygenases from bovine platelets and porcine leukocytes were also inhibited but at higher concentrations (IC
50, about 1 μM), and fatty acid cyclooxygenase purified from bovine vesicular gland was scarcely affected. The compound at 10 μM suppressed by 99% the immunological release of slow reacting substance of anaphylaxis from passively sensitized guinea pig lung (IC
50, about 0.4 μM).</description><identifier>ISSN: 0006-291X</identifier><identifier>EISSN: 1090-2104</identifier><identifier>DOI: 10.1016/0006-291X(83)90568-5</identifier><identifier>PMID: 6418162</identifier><language>eng</language><publisher>United States: Elsevier Inc</publisher><subject>Animals ; arachidonate 5-lipoxygenase ; Arachidonate Lipoxygenases ; Blood Platelets - enzymology ; Cattle ; Dose-Response Relationship, Drug ; Flavones ; flavonoids ; Flavonoids - pharmacology ; Guinea Pigs ; leukemia ; leukocytes ; Leukocytes - enzymology ; Lipoxygenase Inhibitors ; Lung - drug effects ; Male ; Muscle Contraction - drug effects ; pigs ; platelets ; rats ; SRS-A - metabolism ; Swine</subject><ispartof>Biochemical and biophysical research communications, 1983-10, Vol.116 (2), p.612-618</ispartof><rights>1983</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c388t-eadfba25e27e823aac19905f556fc28ca6d9f494a6233d6490189eef6623c1a3</citedby><cites>FETCH-LOGICAL-c388t-eadfba25e27e823aac19905f556fc28ca6d9f494a6233d6490189eef6623c1a3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0006-291X(83)90568-5$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6418162$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Yoshimoto, Tanihiro</creatorcontrib><creatorcontrib>Furukawa, Masayuki</creatorcontrib><creatorcontrib>Yamamoto, Shozo</creatorcontrib><creatorcontrib>Horie, Tokunaru</creatorcontrib><creatorcontrib>Watanabe-Kohno, Shigekatsu</creatorcontrib><title>Flavonoids: Potent inhibitors of arachidonate 5-lipoxygenase</title><title>Biochemical and biophysical research communications</title><addtitle>Biochem Biophys Res Commun</addtitle><description>Various flavonoids were found to be relatively selective inhibitors of arachidonate 5-lipoxygenase which initiates the biosynthesis of leukotrienes with the activity of slow reacting substance of anaphylaxis. Cirsiliol (3′,4′,5-trihydroxy-6,7-dimethoxyflavone) was most potent, and the enzyme partially purified from rat basophilic leukemia cells was inhibited by 97% at a concentration of 10 μM (IC
50, about 0.1 μM). 12-Lipoxygenases from bovine platelets and porcine leukocytes were also inhibited but at higher concentrations (IC
50, about 1 μM), and fatty acid cyclooxygenase purified from bovine vesicular gland was scarcely affected. The compound at 10 μM suppressed by 99% the immunological release of slow reacting substance of anaphylaxis from passively sensitized guinea pig lung (IC
50, about 0.4 μM).</description><subject>Animals</subject><subject>arachidonate 5-lipoxygenase</subject><subject>Arachidonate Lipoxygenases</subject><subject>Blood Platelets - enzymology</subject><subject>Cattle</subject><subject>Dose-Response Relationship, Drug</subject><subject>Flavones</subject><subject>flavonoids</subject><subject>Flavonoids - pharmacology</subject><subject>Guinea Pigs</subject><subject>leukemia</subject><subject>leukocytes</subject><subject>Leukocytes - enzymology</subject><subject>Lipoxygenase Inhibitors</subject><subject>Lung - drug effects</subject><subject>Male</subject><subject>Muscle Contraction - drug effects</subject><subject>pigs</subject><subject>platelets</subject><subject>rats</subject><subject>SRS-A - metabolism</subject><subject>Swine</subject><issn>0006-291X</issn><issn>1090-2104</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1983</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkEtLAzEQx4MotT6-gcKeRA-reWzSREQQ8QUFPfTgLaTJxEa2m5psi_32bm3pUU_D8H_M8EPohOBLgom4whiLkiryfi7ZhcJcyJLvoD7BCpeU4GoX9beWfXSQ8yfGhFRC9VBPVEQSQfvo5rE2i9jE4PJ18RZbaNoiNJMwDm1MuYi-MMnYSXCxMS0UvKzDLH4vP6AxGY7Qnjd1huPNPESjx4fR_XM5fH16ub8blpZJ2ZZgnB8byoEOQFJmjCWq-9dzLryl0hrhlK9UZQRlzIlKYSIVgBfdbolhh-hsXTtL8WsOudXTkC3UtWkgzrOWWGIuqfzXSNiAKslxZ6zWRptizgm8nqUwNWmpCdYruHpFTq_Iacn0L1zNu9jppn8-noLbhjY0O_12rUMHYxEg6WwDNBZcSGBb7WL4-8APZmOItQ</recordid><startdate>19831031</startdate><enddate>19831031</enddate><creator>Yoshimoto, Tanihiro</creator><creator>Furukawa, Masayuki</creator><creator>Yamamoto, Shozo</creator><creator>Horie, Tokunaru</creator><creator>Watanabe-Kohno, Shigekatsu</creator><general>Elsevier Inc</general><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>7QL</scope><scope>7T5</scope><scope>C1K</scope><scope>H94</scope><scope>7X8</scope></search><sort><creationdate>19831031</creationdate><title>Flavonoids: Potent inhibitors of arachidonate 5-lipoxygenase</title><author>Yoshimoto, Tanihiro ; Furukawa, Masayuki ; Yamamoto, Shozo ; Horie, Tokunaru ; Watanabe-Kohno, Shigekatsu</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c388t-eadfba25e27e823aac19905f556fc28ca6d9f494a6233d6490189eef6623c1a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1983</creationdate><topic>Animals</topic><topic>arachidonate 5-lipoxygenase</topic><topic>Arachidonate Lipoxygenases</topic><topic>Blood Platelets - enzymology</topic><topic>Cattle</topic><topic>Dose-Response Relationship, Drug</topic><topic>Flavones</topic><topic>flavonoids</topic><topic>Flavonoids - pharmacology</topic><topic>Guinea Pigs</topic><topic>leukemia</topic><topic>leukocytes</topic><topic>Leukocytes - enzymology</topic><topic>Lipoxygenase Inhibitors</topic><topic>Lung - drug effects</topic><topic>Male</topic><topic>Muscle Contraction - drug effects</topic><topic>pigs</topic><topic>platelets</topic><topic>rats</topic><topic>SRS-A - metabolism</topic><topic>Swine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yoshimoto, Tanihiro</creatorcontrib><creatorcontrib>Furukawa, Masayuki</creatorcontrib><creatorcontrib>Yamamoto, Shozo</creatorcontrib><creatorcontrib>Horie, Tokunaru</creatorcontrib><creatorcontrib>Watanabe-Kohno, Shigekatsu</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Bacteriology Abstracts (Microbiology B)</collection><collection>Immunology Abstracts</collection><collection>Environmental Sciences and Pollution Management</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Biochemical and biophysical research communications</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Yoshimoto, Tanihiro</au><au>Furukawa, Masayuki</au><au>Yamamoto, Shozo</au><au>Horie, Tokunaru</au><au>Watanabe-Kohno, Shigekatsu</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Flavonoids: Potent inhibitors of arachidonate 5-lipoxygenase</atitle><jtitle>Biochemical and biophysical research communications</jtitle><addtitle>Biochem Biophys Res Commun</addtitle><date>1983-10-31</date><risdate>1983</risdate><volume>116</volume><issue>2</issue><spage>612</spage><epage>618</epage><pages>612-618</pages><issn>0006-291X</issn><eissn>1090-2104</eissn><abstract>Various flavonoids were found to be relatively selective inhibitors of arachidonate 5-lipoxygenase which initiates the biosynthesis of leukotrienes with the activity of slow reacting substance of anaphylaxis. Cirsiliol (3′,4′,5-trihydroxy-6,7-dimethoxyflavone) was most potent, and the enzyme partially purified from rat basophilic leukemia cells was inhibited by 97% at a concentration of 10 μM (IC
50, about 0.1 μM). 12-Lipoxygenases from bovine platelets and porcine leukocytes were also inhibited but at higher concentrations (IC
50, about 1 μM), and fatty acid cyclooxygenase purified from bovine vesicular gland was scarcely affected. The compound at 10 μM suppressed by 99% the immunological release of slow reacting substance of anaphylaxis from passively sensitized guinea pig lung (IC
50, about 0.4 μM).</abstract><cop>United States</cop><pub>Elsevier Inc</pub><pmid>6418162</pmid><doi>10.1016/0006-291X(83)90568-5</doi><tpages>7</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | Biochemical and biophysical research communications, 1983-10, Vol.116 (2), p.612-618 |
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| language | eng |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Animals arachidonate 5-lipoxygenase Arachidonate Lipoxygenases Blood Platelets - enzymology Cattle Dose-Response Relationship, Drug Flavones flavonoids Flavonoids - pharmacology Guinea Pigs leukemia leukocytes Leukocytes - enzymology Lipoxygenase Inhibitors Lung - drug effects Male Muscle Contraction - drug effects pigs platelets rats SRS-A - metabolism Swine |
| title | Flavonoids: Potent inhibitors of arachidonate 5-lipoxygenase |
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