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Highly selective alkylcoumarates and diterpenoids isolated from leaves of Baccharis quitensis : a search for new hit compounds against Trypanosoma cruzi
In the present work, the hexane extract of aerial parts of Kunth. was subjected to chromatographic fractionation to afford two alkyl phenylpropanoids: -docosyl ( -coumarate ( ) and -tetracosyl -coumarate ( ) as well as five diterpenes: kaurenoic acid ( ), grandifloric acid ( ), 15β-senecioyl-oxy- -k...
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Published in: | Natural product research 2024-03, p.1-7 |
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creator | Peres, Nathalia Silva, Matheus L Ueno, Anderson K Antar, Guilherme M Levatti, Erica V C Tempone, Andre G Lago, João Henrique G |
description | In the present work, the hexane extract of aerial parts of
Kunth. was subjected to chromatographic fractionation to afford two alkyl phenylpropanoids:
-docosyl (
-coumarate (
) and
-tetracosyl
-coumarate (
) as well as five diterpenes:
kaurenoic acid (
), grandifloric acid (
), 15β-senecioyl-oxy-
-kaur-16-en-19-oic acid (
), and 15-oxo-
-kaurenoic acid (
). Using an
assay with macrophages infected with
, compounds
and
demonstrated high potency against intracellular amastigotes, with EC
values of 7.5 and 6.9 µM, respectively. Compound
revealed a moderate potency against
, with an EC
of 25.6 µM, and compounds
showed no effectiveness. Additionally, compounds
compounds presented no toxicity for mammalian cells to the highest tested concentration of 200 µM. Based on potency and the selectivity indexes of
,
and
, these compounds could be future candidates for optimisation studies for the design of prototypes against Chagas disease. |
doi_str_mv | 10.1080/14786419.2024.2335362 |
format | article |
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Kunth. was subjected to chromatographic fractionation to afford two alkyl phenylpropanoids:
-docosyl (
-coumarate (
) and
-tetracosyl
-coumarate (
) as well as five diterpenes:
kaurenoic acid (
), grandifloric acid (
), 15β-senecioyl-oxy-
-kaur-16-en-19-oic acid (
), and 15-oxo-
-kaurenoic acid (
). Using an
assay with macrophages infected with
, compounds
and
demonstrated high potency against intracellular amastigotes, with EC
values of 7.5 and 6.9 µM, respectively. Compound
revealed a moderate potency against
, with an EC
of 25.6 µM, and compounds
showed no effectiveness. Additionally, compounds
compounds presented no toxicity for mammalian cells to the highest tested concentration of 200 µM. Based on potency and the selectivity indexes of
,
and
, these compounds could be future candidates for optimisation studies for the design of prototypes against Chagas disease.</description><identifier>ISSN: 1478-6419</identifier><identifier>EISSN: 1478-6427</identifier><identifier>DOI: 10.1080/14786419.2024.2335362</identifier><identifier>PMID: 38538549</identifier><language>eng</language><publisher>England</publisher><ispartof>Natural product research, 2024-03, p.1-7</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c257t-5ce69deb4466bbd74a699cdc3926d377e3abfc7c7bebb3d95b7537bc7bb009323</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27923,27924</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/38538549$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Peres, Nathalia</creatorcontrib><creatorcontrib>Silva, Matheus L</creatorcontrib><creatorcontrib>Ueno, Anderson K</creatorcontrib><creatorcontrib>Antar, Guilherme M</creatorcontrib><creatorcontrib>Levatti, Erica V C</creatorcontrib><creatorcontrib>Tempone, Andre G</creatorcontrib><creatorcontrib>Lago, João Henrique G</creatorcontrib><title>Highly selective alkylcoumarates and diterpenoids isolated from leaves of Baccharis quitensis : a search for new hit compounds against Trypanosoma cruzi</title><title>Natural product research</title><addtitle>Nat Prod Res</addtitle><description>In the present work, the hexane extract of aerial parts of
Kunth. was subjected to chromatographic fractionation to afford two alkyl phenylpropanoids:
-docosyl (
-coumarate (
) and
-tetracosyl
-coumarate (
) as well as five diterpenes:
kaurenoic acid (
), grandifloric acid (
), 15β-senecioyl-oxy-
-kaur-16-en-19-oic acid (
), and 15-oxo-
-kaurenoic acid (
). Using an
assay with macrophages infected with
, compounds
and
demonstrated high potency against intracellular amastigotes, with EC
values of 7.5 and 6.9 µM, respectively. Compound
revealed a moderate potency against
, with an EC
of 25.6 µM, and compounds
showed no effectiveness. Additionally, compounds
compounds presented no toxicity for mammalian cells to the highest tested concentration of 200 µM. Based on potency and the selectivity indexes of
,
and
, these compounds could be future candidates for optimisation studies for the design of prototypes against Chagas disease.</description><issn>1478-6419</issn><issn>1478-6427</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><recordid>eNo9kU1uFDEQhS0EIiFwBJCXbGZw-3fMDiIgSJHYhHWrbFdnDO52x-4OGk7CcfEok0glucr13rPkj5C3Hdt2bMc-dNLstOzsljMut1wIJTR_Rs6P9xstuXn-1Hf2jLyq9RdjvFNKvSRnYqdaSXtO_l3F23060IoJ_RLvkUL6fUg-ryMUWLBSmAINccEy45RjqDTWnNom0KHkkSaE-6bKA_0M3u-hxErv1qafaus-UmjRUPyeDrnQCf_QfVyoz-Oc16mFwS3EqS70phxmmHLNI1Bf1r_xNXkxQKr45nRekJ9fv9xcXm2uf3z7fvnpeuO5MstGedQ2oJNSa-eCkaCt9cELy3UQxqAAN3jjjUPnRLDKGSWMa7NjzAouLsj7h9y55LsV69KPsXpMCSbMa-0F6yRjUlrdpOpB6kuuteDQzyW2bzr0HeuPUPpHKP0RSn-C0nzvTk-sbsTw5HqkIP4D3-WMGA</recordid><startdate>20240327</startdate><enddate>20240327</enddate><creator>Peres, Nathalia</creator><creator>Silva, Matheus L</creator><creator>Ueno, Anderson K</creator><creator>Antar, Guilherme M</creator><creator>Levatti, Erica V C</creator><creator>Tempone, Andre G</creator><creator>Lago, João Henrique G</creator><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20240327</creationdate><title>Highly selective alkylcoumarates and diterpenoids isolated from leaves of Baccharis quitensis : a search for new hit compounds against Trypanosoma cruzi</title><author>Peres, Nathalia ; Silva, Matheus L ; Ueno, Anderson K ; Antar, Guilherme M ; Levatti, Erica V C ; Tempone, Andre G ; Lago, João Henrique G</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c257t-5ce69deb4466bbd74a699cdc3926d377e3abfc7c7bebb3d95b7537bc7bb009323</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Peres, Nathalia</creatorcontrib><creatorcontrib>Silva, Matheus L</creatorcontrib><creatorcontrib>Ueno, Anderson K</creatorcontrib><creatorcontrib>Antar, Guilherme M</creatorcontrib><creatorcontrib>Levatti, Erica V C</creatorcontrib><creatorcontrib>Tempone, Andre G</creatorcontrib><creatorcontrib>Lago, João Henrique G</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Natural product research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Peres, Nathalia</au><au>Silva, Matheus L</au><au>Ueno, Anderson K</au><au>Antar, Guilherme M</au><au>Levatti, Erica V C</au><au>Tempone, Andre G</au><au>Lago, João Henrique G</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Highly selective alkylcoumarates and diterpenoids isolated from leaves of Baccharis quitensis : a search for new hit compounds against Trypanosoma cruzi</atitle><jtitle>Natural product research</jtitle><addtitle>Nat Prod Res</addtitle><date>2024-03-27</date><risdate>2024</risdate><spage>1</spage><epage>7</epage><pages>1-7</pages><issn>1478-6419</issn><eissn>1478-6427</eissn><abstract>In the present work, the hexane extract of aerial parts of
Kunth. was subjected to chromatographic fractionation to afford two alkyl phenylpropanoids:
-docosyl (
-coumarate (
) and
-tetracosyl
-coumarate (
) as well as five diterpenes:
kaurenoic acid (
), grandifloric acid (
), 15β-senecioyl-oxy-
-kaur-16-en-19-oic acid (
), and 15-oxo-
-kaurenoic acid (
). Using an
assay with macrophages infected with
, compounds
and
demonstrated high potency against intracellular amastigotes, with EC
values of 7.5 and 6.9 µM, respectively. Compound
revealed a moderate potency against
, with an EC
of 25.6 µM, and compounds
showed no effectiveness. Additionally, compounds
compounds presented no toxicity for mammalian cells to the highest tested concentration of 200 µM. Based on potency and the selectivity indexes of
,
and
, these compounds could be future candidates for optimisation studies for the design of prototypes against Chagas disease.</abstract><cop>England</cop><pmid>38538549</pmid><doi>10.1080/14786419.2024.2335362</doi><tpages>7</tpages></addata></record> |
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source | Taylor and Francis Science and Technology Collection |
title | Highly selective alkylcoumarates and diterpenoids isolated from leaves of Baccharis quitensis : a search for new hit compounds against Trypanosoma cruzi |
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