{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,3]],"date-time":"2026-04-03T17:08:08Z","timestamp":1775236088934,"version":"3.50.1"},"reference-count":49,"publisher":"Oxford University Press (OUP)","issue":"9","license":[{"start":{"date-parts":[[2020,9,1]],"date-time":"2020-09-01T00:00:00Z","timestamp":1598918400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/academic.oup.com\/journals\/pages\/open_access\/funder_policies\/chorus\/standard_publication_model"}],"funder":[{"name":"IPICYT\/CIIDZA"},{"DOI":"10.13039\/501100003141","name":"CONACyT","doi-asserted-by":"publisher","award":["APN-2001"],"award-info":[{"award-number":["APN-2001"]}],"id":[{"id":"10.13039\/501100003141","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100003141","name":"CONACyT","doi-asserted-by":"publisher","award":["CB-2015"],"award-info":[{"award-number":["CB-2015"]}],"id":[{"id":"10.13039\/501100003141","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2020,9,1]]},"abstract":"<jats:title>Abstract<\/jats:title>\n               <jats:sec>\n                  <jats:title>Objective<\/jats:title>\n                  <jats:p>This work describes the vasorelaxant and antihypertensive effects and the mechanism of action on vascular smooth muscle cells of Nibethione, a synthetic thiazolidinedione derivative. Additionally, evidence of its cytotoxicity is assessed.<\/jats:p>\n               <\/jats:sec>\n               <jats:sec>\n                  <jats:title>Methods<\/jats:title>\n                  <jats:p>Nibethione (NB) was synthesized, and its vasorelaxant effect and mechanism of action were assessed through ex vivo experiments. Molecular docking studies were used to predict the mode of interaction with L-type Ca2+ channel, and in vivo antihypertensive activity was assayed on spontaneously hypertensive rats (SHR). The cytotoxicity potential was evaluated in porcine aortic endothelial cells (PAECs) from primary explants.<\/jats:p>\n               <\/jats:sec>\n               <jats:sec>\n                  <jats:title>Key findings<\/jats:title>\n                  <jats:p>Nibethione vasorelaxant effect was efficient on KCl (80 mm) and NE-contraction. This effect was deleteriously modified in the presence of potassium channel block drugs, while the maximal contraction induced with NE was significantly decreased by NB; the CaCl2-induced contraction was abolished entirely. In vivo experiments showed that NB decreased diastolic blood pressure in 20.3 % after its administration on SHR. The molecular docking showed that NB blocks L-type Ca2+ channel, and in vitro tests showed that NB did not produce cytotoxic activity on PAECs (IC50 &amp;gt;1000 \u00b5m).<\/jats:p>\n               <\/jats:sec>\n               <jats:sec>\n                  <jats:title>Conclusions<\/jats:title>\n                  <jats:p>Nibethione showed in vivo antihypertensive and ex vivo vasorelaxant effects with implication of voltage-dependent L-type Ca2+ channel blocking, and this may contribute to the research of novel antihypertensive drugs.<\/jats:p>\n               <\/jats:sec>","DOI":"10.1111\/jphp.13295","type":"journal-article","created":{"date-parts":[[2020,6,5]],"date-time":"2020-06-05T00:15:45Z","timestamp":1591316145000},"page":"1186-1198","source":"Crossref","is-referenced-by-count":3,"title":["Pharmacological characterization of the cardiovascular effect of Nibethione: <i>ex vivo<\/i>, <i>in vivo<\/i> and <i>in silico<\/i> studies"],"prefix":"10.1093","volume":"72","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-1429-8085","authenticated-orcid":false,"given":"Amanda","family":"S\u00e1nchez-Recillas","sequence":"first","affiliation":[{"name":"Laboratorio de Farmacolog\u00eda, Facultad de Qu\u00edmica, Universidad Aut\u00f3noma de Yucat\u00e1n , M\u00e9rida,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5344-4762","authenticated-orcid":false,"given":"Gabriel","family":"Navarrete-V\u00e1zquez","sequence":"additional","affiliation":[{"name":"Laboratorio de Qu\u00edmica Farmac\u00e9utica, Facultad de Farmacia, Universidad Aut\u00f3noma del Estado de Morelos , Cuernavaca,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4344-642X","authenticated-orcid":false,"given":"Sergio","family":"Hidalgo-Figueroa","sequence":"additional","affiliation":[{"name":"CONACyT, IPICYT\/Consorcio de Investigaci\u00f3n, Innovaci\u00f3n y Desarrollo para las Zonas \u00c1ridas , San Luis Potos\u00ed,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6909-2044","authenticated-orcid":false,"given":"Marcos","family":"Bonilla-Hern\u00e1ndez","sequence":"additional","affiliation":[{"name":"Unidad de Materiales, Centro de Investigaci\u00f3n Cient\u00edfica de Yucat\u00e1n , M\u00e9rida,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8822-7389","authenticated-orcid":false,"given":"Rolffy","family":"Ortiz-Andrade","sequence":"additional","affiliation":[{"name":"Laboratorio de Farmacolog\u00eda, Facultad de Qu\u00edmica, Universidad Aut\u00f3noma de Yucat\u00e1n , M\u00e9rida,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2874-8291","authenticated-orcid":false,"given":"Maximiliano","family":"Ibarra-Barajas","sequence":"additional","affiliation":[{"name":"Unidad de Investigaci\u00f3n en Biomedicina, Facultad de Estudios Superiores Iztacala, Universidad Aut\u00f3noma de M\u00e9xico , Tlalnepantla de Baz,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6168-7350","authenticated-orcid":false,"given":"V\u00edctor","family":"Y\u00e1\u00f1ez-P\u00e9rez","sequence":"additional","affiliation":[{"name":"Laboratorio de Farmacolog\u00eda, Facultad de Qu\u00edmica, Universidad Aut\u00f3noma de Yucat\u00e1n , M\u00e9rida,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2796-2440","authenticated-orcid":false,"given":"Juan 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