{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,12]],"date-time":"2025-10-12T20:06:33Z","timestamp":1760299593227},"reference-count":0,"publisher":"Georg Thieme Verlag KG","issue":"14\/15","content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Planta Med"],"published-print":{"date-parts":[[2017,10]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>A dichloromethane extract from leaves of Searsia pyroides potentiated gamma aminobutyric acid-induced chloride currents by 171.8\u2009\u00b1\u200954% when tested at 100\u2009\u00b5g\/mL in Xenopus oocytes transiently expressing gamma aminobutyric acid type A receptors composed of \u03b1\n          1\n          \u03b2\n          2\n          \u03b3\n          2s subunits. In zebrafish larvae, the extract significantly lowered pentylenetetrazol-provoked locomotion when tested at 4\u2009\u00b5g\/mL. Active compounds of the extract were tracked with the aid of HPLC-based activity profiling utilizing a previously validated zebrafish larval locomotor activity assay. From two active HPLC fractions, compounds 1\u200a\u2013\u200a3 were isolated. Structurally related compounds 4\u200a\u2013\u200a6 were purified from a later eluting inactive HPLC fraction. With the aid of 1H and 13C NMR and high-resolution mass spectrometry, compounds 1\u200a\u2013\u200a6 were identified as analogues of anacardic acid. Compounds 1\u200a\u2013\u200a3 led to a concentration-dependent decrease of pentylenetetrazol-provoked locomotion in the zebrafish larvae model, while 4\u200a\u2013\u200a6 were inactive. Compounds 1\u200a\u2013\u200a3 enhanced gamma aminobutyric acid-induced chloride currents in Xenopus oocytes in a concentration-dependent manner, while 4\u200a\u2013\u200a6 only showed marginal enhancements of gamma aminobutyric acid-induced chloride currents. Compounds 2, 3, and 5 have not been reported previously.<\/jats:p>","DOI":"10.1055\/s-0043-110768","type":"journal-article","created":{"date-parts":[[2017,5,16]],"date-time":"2017-05-16T22:48:11Z","timestamp":1494974891000},"page":"1169-1175","source":"Crossref","is-referenced-by-count":4,"title":["HPLC-Based Activity Profiling for GABAA Receptor Modulators in Searsia pyroides Using a Larval Zebrafish Locomotor Assay"],"prefix":"10.1055","volume":"83","author":[{"given":"Fahimeh","family":"Moradi-Afrapoli","sequence":"additional","affiliation":[{"name":"Pharmaceutical Biology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hannes","family":"van der Merwe","sequence":"additional","affiliation":[{"name":"Faculty of Natural and Agricultural Sciences, University of the Free State, Bloemfontein, Republic of South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Maria","family":"De Mieri","sequence":"additional","affiliation":[{"name":"Pharmaceutical Biology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Anke","family":"Wilhelm","sequence":"additional","affiliation":[{"name":"Faculty of Natural and Agricultural Sciences, University of the Free State, Bloemfontein, Republic of South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Marco","family":"Stadler","sequence":"additional","affiliation":[{"name":"Institute of Pharmacology and Toxicology, Pharmaziezentrum, University of Vienna, Vienna, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Pieter","family":"Zietsman","sequence":"additional","affiliation":[{"name":"National Museum, Bloemfontein, Republic of South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Steffen","family":"Hering","sequence":"additional","affiliation":[{"name":"Institute of Pharmacology and Toxicology, Pharmaziezentrum, University of Vienna, Vienna, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kenneth","family":"Swart","sequence":"additional","affiliation":[{"name":"Faculty of Natural and Agricultural Sciences, University of the Free State, Bloemfontein, Republic of South Africa"},{"name":"FARMOVS-PAREXEL, University of the Free State, Bloemfontein, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Matthias","family":"Hamburger","sequence":"additional","affiliation":[{"name":"Pharmaceutical Biology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"194","published-online":{"date-parts":[[2017,5,16]]},"container-title":["Planta Medica"],"original-title":[],"language":"en","link":[{"URL":"http:\/\/www.thieme-connect.de\/products\/ejournals\/pdf\/10.1055\/s-0043-110768.pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2019,5,6]],"date-time":"2019-05-06T19:29:21Z","timestamp":1557170961000},"score":1,"resource":{"primary":{"URL":"http:\/\/www.thieme-connect.de\/DOI\/DOI?10.1055\/s-0043-110768"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2017,5,16]]},"references-count":0,"journal-issue":{"issue":"14\/15","published-online":{"date-parts":[[2017,9,27]]},"published-print":{"date-parts":[[2017,10]]}},"URL":"https:\/\/doi.org\/10.1055\/s-0043-110768","relation":{},"ISSN":["0032-0943","1439-0221"],"issn-type":[{"value":"0032-0943","type":"print"},{"value":"1439-0221","type":"electronic"}],"subject":[],"published":{"date-parts":[[2017,5,16]]}}}