{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,10]],"date-time":"2025-10-10T01:39:40Z","timestamp":1760060380598,"version":"build-2065373602"},"reference-count":66,"publisher":"MDPI AG","issue":"17","license":[{"start":{"date-parts":[[2025,8,29]],"date-time":"2025-08-29T00:00:00Z","timestamp":1756425600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"University of the Free State"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>This study aimed to investigate the glycaemic control potential and modulation of GABA-induced chloride currents (IGABA) of H. revolutum and the possible bioactive xanthones. Fractions from the leaf and stem extracts (dichloromethane and methanol) were assessed for in vitro \u03b1-glucosidase-inhibitory potential and their ability to modulate IGABA (GABAergic effect) through GABAA receptors heterologously expressed in Xenopus oocytes. Xanthones 4-hydroxy-2,3-dimethoxy-9H-xanthen-9-one (1), 3-hydroxy-2,4-dimethoxy-9H-xanthen-9-one (2) and trans-3-(4-hydroxy-3-methoxyphenyl)-2-(hydroxymethyl)-5-methoxy-2,3-dihydro-7H-[1,4]dioxino[2,3-c]xanthen-7-one (3) were isolated from the stem and tested in the GABAA receptors assay, but only 3 was assessed for \u03b1-glucosidase-inhibitory action. Compared to acarbose (IC50 = 6.16 \u00b5M), 3 showed a mild to moderate \u03b1-glucosidase-inhibitory activity (IC50 = 45.1 \u00b5M), which may be attributed to the absence of a hydroxyl group at its xanthone core. Isomeric compounds 1 and 2 significantly enhanced IGABA with similar efficacy, while 3 was inactive, which may be attributed to its notable structural difference (cyclic ether substitution) compared to compounds 1 and 2. H. revolutum stem contains xanthones with \u03b1-glucosidase-inhibitory potential, which also enhance IGABA and could be further studied as a medicinal plant for managing GABAA receptor-mediated mental disorders and\/or diabetes.<\/jats:p>","DOI":"10.3390\/molecules30173530","type":"journal-article","created":{"date-parts":[[2025,8,29]],"date-time":"2025-08-29T12:25:57Z","timestamp":1756470357000},"page":"3530","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["GABAergic and \u03b1-Glucosidase-Inhibitory Potentials of Fractions and Isolated Xanthones from Hypericum\u00a0revolutum Vahl subsp. revolutum"],"prefix":"10.3390","volume":"30","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0014-4130","authenticated-orcid":false,"given":"Maria S.","family":"Chukwuma","sequence":"first","affiliation":[{"name":"Department of Chemistry, Faculty of Natural and Agricultural Sciences, University of the Free State, Bloemfontein 9301, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Lorenza","family":"Bertaina","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Sciences, Faculty of Life Sciences, University of Vienna, 1090 Vienna, Austria"},{"name":"Vienna Doctoral School of Pharmaceutical, Nutritional and Sport Sciences (PhaNuSpo), University of Vienna, 1090 Vienna, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sophia","family":"Khom","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Sciences, Faculty of Life Sciences, University of Vienna, 1090 Vienna, Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Chika I.","family":"Chukwuma","sequence":"additional","affiliation":[{"name":"Center for Quality of Health and Living (CQHL), Faculty of Health and Environmental Sciences, Central University of Technology, Bloemfontein 9301, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Pieter C.","family":"Zietsman","sequence":"additional","affiliation":[{"name":"Bloemfontein National Museum, Bloemfontein 9301, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4561-5589","authenticated-orcid":false,"given":"Anke","family":"Wilhelm","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Faculty of Natural and Agricultural Sciences, University of the Free State, Bloemfontein 9301, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Susanna L.","family":"Bonnet","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Faculty of Natural and Agricultural Sciences, University of the Free State, Bloemfontein 9301, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2025,8,29]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"491","DOI":"10.1007\/s11892-014-0491-3","article-title":"Diabetes and Depression","volume":"14","author":"Holt","year":"2014","journal-title":"Curr. 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