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In Vivo Screening of Xanthones from Garcinia oligantha Identified Oliganthin H as a Novel Natural Inhibitor of Convulsions
Gong,Guiyi1,2; Chen,Hanbin1; Kam,Hiotong1; Chan,Ging1; Tang,Yue Xun4; Wu,Man4; Tan,Hongsheng5; Tse,Yu Chung6; Xu,Hong Xi3,4; Lee,Simon Ming Yuen1
Source PublicationJournal of Natural Products

Epilepsy is a chronic neurological disorder, characterized by recurrent, spontaneous, and transient seizures, and affects more than 70 million people worldwide. Although two dozen antiepileptic drugs (AEDs) are approved and available in the market, seizures remain poorly controlled in one-third of epileptic patients who are suffering from drug resistance or various adverse effects. Recently, the xanthone skeleton has been regarded as an attractive scaffold for the discovery and development of emerging anticonvulsants. We had isolated several dihydroxanthone derivatives previously, including oliganthin H, oliganthin I, and oliganthin N, whose structures were similar and delicately elucidated by spectrum analysis or X-ray crystallographic data, from extracts of leaves of Garcinia oligantha. These xanthone analogues were evaluated for anticonvulsant activity, and a novel xanthone, oliganthin H, has been identified as a sound and effective natural inhibitor of convulsions in zebrafish in vivo. A preliminary structure-activity relationship analysis on the relationship between structures of the xanthone analogues and their activities was also conducted. Oliganthin H significantly suppressed convulsant behavior and reduced to about 25% and 50% of PTZ-induced activity, in 12.5 and 25 μM treatment groups (P < 0.01 and 0.001), respectively. Meanwhile, it reduced seizure activity, velocity, seizure duration, and number of bursts in zebrafish larvae (P < 0.05). Pretreatment of oliganthin H significantly restored aberrant induction of gene expressions including npas4a, c-fos, pyya, and bdnf, as well as gabra1, gad1, glsa, and glula, upon PTZ treatment. In addition, in silico analysis revealed the stability of the oliganthin H-GABAA receptor complex and their detailed binding pattern. Therefore, direct interactions with the GABAA receptor and involvement of downstream GABA-glutamate pathways were possible mechanisms of the anticonvulsant action of oliganthin H. Our findings present the anticonvulsant activity of oliganthin H, provide a novel scaffold for further modifications, and highlight the xanthone skeleton as an attractive and reliable resource for the development of emerging AEDs.

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Indexed BySCIE
WOS Research AreaPlant Sciences ; Pharmacology & Pharmacy
WOS SubjectPlant Sciences ; Pharmacology & Pharmacy ; Chemistry, Medicinal
WOS IDWOS:000603402900025
Scopus ID2-s2.0-85097843687
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Cited Times [WOS]:5   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorXu,Hong Xi; Lee,Simon Ming Yuen
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macau,Macau,Macao
2.Second Affiliated Hospital,Southern University of Science and Technology (SUSTech),Shenzhen,518055,China
3.Shuguang Hospital,Shanghai University of Traditional Chinese Medicine,Shanghai,201203,China
4.School of Pharmacy,Shanghai University of Traditional Chinese Medicine,Shanghai,201203,China
5.Clinical Research Center,Shanghai Jiao Tong University,School of Medicine,Shanghai,200240,China
6.Guangdong Provincial Key Laboratory of Cell Microenvironment and Disease Research,Department of Biology,Southern University of Science and Technology (SUSTech),Shenzhen,518055,China
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Gong,Guiyi,Chen,Hanbin,Kam,Hiotong,et al. In Vivo Screening of Xanthones from Garcinia oligantha Identified Oliganthin H as a Novel Natural Inhibitor of Convulsions[J]. Journal of Natural Products,2020,83(12):3706-3716.
APA Gong,Guiyi,Chen,Hanbin,Kam,Hiotong,Chan,Ging,Tang,Yue Xun,Wu,Man,Tan,Hongsheng,Tse,Yu Chung,Xu,Hong Xi,&Lee,Simon Ming Yuen.(2020).In Vivo Screening of Xanthones from Garcinia oligantha Identified Oliganthin H as a Novel Natural Inhibitor of Convulsions.Journal of Natural Products,83(12),3706-3716.
MLA Gong,Guiyi,et al."In Vivo Screening of Xanthones from Garcinia oligantha Identified Oliganthin H as a Novel Natural Inhibitor of Convulsions".Journal of Natural Products 83.12(2020):3706-3716.
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