{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,24]],"date-time":"2026-09-24T04:16:03Z","timestamp":1790223363021,"version":"4.1.0"},"reference-count":41,"publisher":"PeerJ","license":[{"start":{"date-parts":[[2024,7,17]],"date-time":"2024-07-17T00:00:00Z","timestamp":1721174400000},"content-version":"unspecified","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Suranaree University of Technology Research and Development Fund","award":["IRD1-107-67-12-24"],"award-info":[{"award-number":["IRD1-107-67-12-24"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"abstract":"<jats:sec>\n               <jats:title>Background<\/jats:title>\n               <jats:p>Allicin, a bioactive compound derived from garlic (<jats:italic>Allium sativum<\/jats:italic>), demonstrates antibacterial activity against a broad spectrum of bacteria including the most common meningitis pathogens. In order to advocate for allicin as a potential therapeutic candidate for bacterial meningitis, the present study aimed to assess the ability of allicin to cross the blood-brain barrier (BBB) using an <jats:italic>in vitro<\/jats:italic> model.<\/jats:p>\n            <\/jats:sec>\n            <jats:sec>\n               <jats:title>Methods<\/jats:title>\n               <jats:p>The cell viability of the human brain endothelial cell line hCMEC\/D3 after incubation with various concentrations of allicin was investigated using an MTT assay at 3 and 24 h. Additionally, reactive oxygen species (ROS) production of allicin-treated hCMEC\/D3 cells was examined at 3 h. The concentrations of allicin that were not toxic to the cells, as determined by the MTT assay, and did not significantly increase ROS generation, were then used to investigate allicin\u2019s ability to traverse the <jats:italic>in vitro<\/jats:italic> BBB model for 3 h. High-performance liquid chromatography (HPLC) analysis was utilized to examine the allicin concentration capable of passing the <jats:italic>in vitro<\/jats:italic> BBB model. The cellular uptake experiments were subsequently performed to observe the uptake of allicin into hCMEC\/D3 cells. The pkCSM online tool was used to predict the absorption, distribution, metabolism, excretion, and pharmacokinetic properties of allicin and S-allylmercaptoglutathione (GSSA).<\/jats:p>\n            <\/jats:sec>\n            <jats:sec>\n               <jats:title>Results<\/jats:title>\n               <jats:p>The results from MTT assay indicated that the highest non-toxicity concentration of allicin on hCMEC\/D3 cells was 5 \u00b5g\/ml at 3 h and 2 \u00b5g\/ml at 24 h. Allicin significantly enhanced ROS production of hCMEC\/D3 cells at 10 \u00b5g\/ml at 3 h. After applying the non-toxicity concentrations of allicin (0.5\u20135 \u00b5g\/ml) to the <jats:italic>in vitro<\/jats:italic> BBB model for 3 h, allicin was not detectable in both apical and basolateral chambers in the presence of hCMEC\/D3 cells. On the contrary, allicin was detected in both chambers in the absence of the cells. The results from cellular uptake experiments at 3 h revealed that hCMEC\/D3 cells at 1\u00a0\u00d7\u00a010<jats:sup>4<\/jats:sup> cells could uptake allicin at concentrations of 0.5, 1, and 2 \u00b5g\/ml. Moreover, allicin uptake of hCMEC\/D3 cells was proportional to the cell number, and the cells at 5\u00a0\u00d7\u00a010<jats:sup>4<\/jats:sup> could completely uptake allicin at a concentration of 5 \u00b5g\/ml within 0.5 h. The topological polar surface area (TPSA) predicting for allicin was determined to be 62.082 \u00c5<jats:sup>2<\/jats:sup>, indicating its potential ability to cross the BBB. Additionally, the calculated logBB value surpassing 0.3 suggests that the compound may exhibit ease of penetration through the BBB.<\/jats:p>\n            <\/jats:sec>\n            <jats:sec>\n               <jats:title>Conclusion<\/jats:title>\n               <jats:p>The present results suggested that allicin was rapidly taken up by hCMEC\/D3 cells <jats:italic>in vitro<\/jats:italic> BBB model. The prediction results of allicin\u2019s distribution patterns suggested that the compound possesses the capability to enter the brain.<\/jats:p>\n            <\/jats:sec>","DOI":"10.7717\/peerj.17742","type":"journal-article","created":{"date-parts":[[2024,7,17]],"date-time":"2024-07-17T08:53:59Z","timestamp":1721206439000},"page":"e17742","source":"Crossref","is-referenced-by-count":7,"title":["Cellular uptake of allicin in the hCMEC\/D3 human brain endothelial cells: exploring blood-brain barrier penetration in an <i>in vitro<\/i> model"],"prefix":"10.7717","volume":"12","author":[{"given":"Kankawi","family":"Satsantitham","sequence":"first","affiliation":[{"name":"School of Preclinical Sciences, Institute of Science, Suranaree University of Technology,  Nakhon Ratchasima, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Pishyaporn","family":"Sritangos","sequence":"additional","affiliation":[{"name":"School of Preclinical Sciences, Institute of Science, Suranaree University of Technology,  Nakhon Ratchasima, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sirawit","family":"Wet-osot","sequence":"additional","affiliation":[{"name":"Department of Medical Sciences, Ministry of Public Health, Nonthaburi, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Nuannoi","family":"Chudapongse","sequence":"additional","affiliation":[{"name":"Department of Basic Medical Sciences, Siam University, Bangkok, Thailand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Oratai","family":"Weeranantanapan","sequence":"additional","affiliation":[{"name":"School of Preclinical Sciences, Institute of Science, Suranaree University of Technology,  Nakhon Ratchasima, 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