Role of Intestinal Microbiota in Metabolism of Gastrodin In Vitro and In Vivo
Alteration in the number and composition of intestinal microbiota affects the metabolism of several xenobiotics. Gastrodin, isolated from <i>Gastrodia elata,</i> is prone to be hydrolyzed by intestinal microbiota. In the present study, the role of intestinal microbiota in gastrodin metab...
| Main Authors: | , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2019-04-01
|
| Series: | Metabolites |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2218-1989/9/4/69 |
| _version_ | 1818765651286687744 |
|---|---|
| author | Mahesh Raj Nepal Ki Sun Jeong Geon Ho Kim Dong Ho Cha Mi Jeong Kang Jin Sung Kim Ju-Hyun Kim Tae Cheon Jeong |
| author_facet | Mahesh Raj Nepal Ki Sun Jeong Geon Ho Kim Dong Ho Cha Mi Jeong Kang Jin Sung Kim Ju-Hyun Kim Tae Cheon Jeong |
| author_sort | Mahesh Raj Nepal |
| collection | DOAJ |
| description | Alteration in the number and composition of intestinal microbiota affects the metabolism of several xenobiotics. Gastrodin, isolated from <i>Gastrodia elata,</i> is prone to be hydrolyzed by intestinal microbiota. In the present study, the role of intestinal microbiota in gastrodin metabolism was investigated in vitro and in vivo. Gastrodin was incubated in an anaerobic condition with intestinal contents prepared from vehicle- and antibiotics-treated rats and the disappearance of gastrodin and formation of 4-hydroxybenzyl alcohol (4-HBA) was measured by liquid chromatography coupled to mass spectroscopy (LC-MS/MS). The results showed that almost all gastrodin incubated with control intestinal contents was metabolized to its aglycone in time- and concentration-dependent manners. In contrast, much less formation of 4-HBA was detected in intestinal contents from antibiotics-treated rats. Subsequently, in vivo pharmacokinetic study revealed that the antibiotic pretreatment of rats significantly affected the metabolism of gastrodin to 4-HBA. When administered orally, gastrodin was rapidly absorbed rapidly into plasma, metabolized to 4-HBA, and disappeared from the body within six hours. Interestingly, the pharmacokinetic parameters of 4-HBA were changed remarkably in antibiotics-treated rats, compared to control rats. The results clearly indicated that the antibiotics treatment of rats suppressed the ability of intestinal microbiota to metabolize gastrodin to 4-HBA and that, thereby, the pharmacodynamic action was significantly modulated. |
| first_indexed | 2024-12-18T08:21:29Z |
| format | Article |
| id | doaj.art-c52506e21fdd40ddbe9774a05f98f037 |
| institution | Directory Open Access Journal |
| issn | 2218-1989 |
| language | English |
| last_indexed | 2024-12-18T08:21:29Z |
| publishDate | 2019-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Metabolites |
| spelling | doaj.art-c52506e21fdd40ddbe9774a05f98f0372022-12-21T21:14:44ZengMDPI AGMetabolites2218-19892019-04-01946910.3390/metabo9040069metabo9040069Role of Intestinal Microbiota in Metabolism of Gastrodin In Vitro and In VivoMahesh Raj Nepal0Ki Sun Jeong1Geon Ho Kim2Dong Ho Cha3Mi Jeong Kang4Jin Sung Kim5Ju-Hyun Kim6Tae Cheon Jeong7College of Pharmacy, Yeungnam University, 280 Daehak-Ro, Gyeongsan 38541, KoreaCollege of Pharmacy, Yeungnam University, 280 Daehak-Ro, Gyeongsan 38541, KoreaCollege of Pharmacy, Yeungnam University, 280 Daehak-Ro, Gyeongsan 38541, KoreaCollege of Pharmacy, Yeungnam University, 280 Daehak-Ro, Gyeongsan 38541, KoreaCollege of Pharmacy, Yeungnam University, 280 Daehak-Ro, Gyeongsan 38541, KoreaCollege of Pharmacy, Yeungnam University, 280 Daehak-Ro, Gyeongsan 38541, KoreaCollege of Pharmacy, Yeungnam University, 280 Daehak-Ro, Gyeongsan 38541, KoreaCollege of Pharmacy, Yeungnam University, 280 Daehak-Ro, Gyeongsan 38541, KoreaAlteration in the number and composition of intestinal microbiota affects the metabolism of several xenobiotics. Gastrodin, isolated from <i>Gastrodia elata,</i> is prone to be hydrolyzed by intestinal microbiota. In the present study, the role of intestinal microbiota in gastrodin metabolism was investigated in vitro and in vivo. Gastrodin was incubated in an anaerobic condition with intestinal contents prepared from vehicle- and antibiotics-treated rats and the disappearance of gastrodin and formation of 4-hydroxybenzyl alcohol (4-HBA) was measured by liquid chromatography coupled to mass spectroscopy (LC-MS/MS). The results showed that almost all gastrodin incubated with control intestinal contents was metabolized to its aglycone in time- and concentration-dependent manners. In contrast, much less formation of 4-HBA was detected in intestinal contents from antibiotics-treated rats. Subsequently, in vivo pharmacokinetic study revealed that the antibiotic pretreatment of rats significantly affected the metabolism of gastrodin to 4-HBA. When administered orally, gastrodin was rapidly absorbed rapidly into plasma, metabolized to 4-HBA, and disappeared from the body within six hours. Interestingly, the pharmacokinetic parameters of 4-HBA were changed remarkably in antibiotics-treated rats, compared to control rats. The results clearly indicated that the antibiotics treatment of rats suppressed the ability of intestinal microbiota to metabolize gastrodin to 4-HBA and that, thereby, the pharmacodynamic action was significantly modulated.https://www.mdpi.com/2218-1989/9/4/69gastrodin4-hydroxybenzyl alcoholantibioticsintestinal microbiotametabolismLC-MS/MS |
| spellingShingle | Mahesh Raj Nepal Ki Sun Jeong Geon Ho Kim Dong Ho Cha Mi Jeong Kang Jin Sung Kim Ju-Hyun Kim Tae Cheon Jeong Role of Intestinal Microbiota in Metabolism of Gastrodin In Vitro and In Vivo Metabolites gastrodin 4-hydroxybenzyl alcohol antibiotics intestinal microbiota metabolism LC-MS/MS |
| title | Role of Intestinal Microbiota in Metabolism of Gastrodin In Vitro and In Vivo |
| title_full | Role of Intestinal Microbiota in Metabolism of Gastrodin In Vitro and In Vivo |
| title_fullStr | Role of Intestinal Microbiota in Metabolism of Gastrodin In Vitro and In Vivo |
| title_full_unstemmed | Role of Intestinal Microbiota in Metabolism of Gastrodin In Vitro and In Vivo |
| title_short | Role of Intestinal Microbiota in Metabolism of Gastrodin In Vitro and In Vivo |
| title_sort | role of intestinal microbiota in metabolism of gastrodin in vitro and in vivo |
| topic | gastrodin 4-hydroxybenzyl alcohol antibiotics intestinal microbiota metabolism LC-MS/MS |
| url | https://www.mdpi.com/2218-1989/9/4/69 |
| work_keys_str_mv | AT maheshrajnepal roleofintestinalmicrobiotainmetabolismofgastrodininvitroandinvivo AT kisunjeong roleofintestinalmicrobiotainmetabolismofgastrodininvitroandinvivo AT geonhokim roleofintestinalmicrobiotainmetabolismofgastrodininvitroandinvivo AT donghocha roleofintestinalmicrobiotainmetabolismofgastrodininvitroandinvivo AT mijeongkang roleofintestinalmicrobiotainmetabolismofgastrodininvitroandinvivo AT jinsungkim roleofintestinalmicrobiotainmetabolismofgastrodininvitroandinvivo AT juhyunkim roleofintestinalmicrobiotainmetabolismofgastrodininvitroandinvivo AT taecheonjeong roleofintestinalmicrobiotainmetabolismofgastrodininvitroandinvivo |