In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes
Context: Bergenin, isolated from the herb of Bergenia purpurascens (Hook. f. et Thoms.) Engl., has anti-inflammatory, antitussive, and wound healing activities. However, whether bergenin affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear. Materials and methods: In this...
| Main Authors: | , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2018-01-01
|
| Series: | Pharmaceutical Biology |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/13880209.2018.1525413 |
| _version_ | 1818511451952775168 |
|---|---|
| author | Gang Dong Yun Zhou Xiaoli Song |
| author_facet | Gang Dong Yun Zhou Xiaoli Song |
| author_sort | Gang Dong |
| collection | DOAJ |
| description | Context: Bergenin, isolated from the herb of Bergenia purpurascens (Hook. f. et Thoms.) Engl., has anti-inflammatory, antitussive, and wound healing activities. However, whether bergenin affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear. Materials and methods: In this study, the inhibitory effects of bergenin (100 μM) on the eight human liver CYP isoforms (i.e., 1A2, 3A4, 2A6, 2E1, 2D6, 2C9, 2C19 and 2C8) were investigated, enzyme kinetics and time-dependent inhibition studies were also performed in vitro using human liver microsomes (HLMs). Results: The results showed that bergenin inhibited the activity of CYP3A4, 2E1 and 2C9, with IC50 values of 14.39, 22.83 and 15.11 μM, respectively, but other CYP isoforms were not affected. Enzyme kinetic studies showed that bergenin was not only a non-competitive inhibitor of CYP3A4, but also a competitive inhibitor of CYP2E1 and 2C9, with Ki values of 7.71, 11.39 and 8.89 μM, respectively. In addition, bergenin is a time-dependent inhibitor for CYP3A4 with Kinact/KI value of 0.025/3.50 μM−1 min−1. Discussion and conclusions: The in vitro studies of bergenin with CYP isoforms indicate that bergenin has the potential to cause pharmacokinetic drug interactions with other co-administered drugs metabolized by CYP3A4, 2E1 and 2C9. Further clinical studies are needed to evaluate the significance of this interaction. |
| first_indexed | 2024-12-10T23:33:32Z |
| format | Article |
| id | doaj.art-408d627dd8f14776aa696d9578f51d2c |
| institution | Directory Open Access Journal |
| issn | 1388-0209 1744-5116 |
| language | English |
| last_indexed | 2024-12-10T23:33:32Z |
| publishDate | 2018-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Pharmaceutical Biology |
| spelling | doaj.art-408d627dd8f14776aa696d9578f51d2c2022-12-22T01:29:17ZengTaylor & Francis GroupPharmaceutical Biology1388-02091744-51162018-01-0156162062510.1080/13880209.2018.15254131525413In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymesGang Dong0Yun Zhou1Xiaoli Song2Yidu Central Hospital of WeifangYidu Central Hospital of WeifangYidu Central Hospital of WeifangContext: Bergenin, isolated from the herb of Bergenia purpurascens (Hook. f. et Thoms.) Engl., has anti-inflammatory, antitussive, and wound healing activities. However, whether bergenin affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear. Materials and methods: In this study, the inhibitory effects of bergenin (100 μM) on the eight human liver CYP isoforms (i.e., 1A2, 3A4, 2A6, 2E1, 2D6, 2C9, 2C19 and 2C8) were investigated, enzyme kinetics and time-dependent inhibition studies were also performed in vitro using human liver microsomes (HLMs). Results: The results showed that bergenin inhibited the activity of CYP3A4, 2E1 and 2C9, with IC50 values of 14.39, 22.83 and 15.11 μM, respectively, but other CYP isoforms were not affected. Enzyme kinetic studies showed that bergenin was not only a non-competitive inhibitor of CYP3A4, but also a competitive inhibitor of CYP2E1 and 2C9, with Ki values of 7.71, 11.39 and 8.89 μM, respectively. In addition, bergenin is a time-dependent inhibitor for CYP3A4 with Kinact/KI value of 0.025/3.50 μM−1 min−1. Discussion and conclusions: The in vitro studies of bergenin with CYP isoforms indicate that bergenin has the potential to cause pharmacokinetic drug interactions with other co-administered drugs metabolized by CYP3A4, 2E1 and 2C9. Further clinical studies are needed to evaluate the significance of this interaction.http://dx.doi.org/10.1080/13880209.2018.1525413cyp3a4cyp2e1cyp2c9herb–drug interaction |
| spellingShingle | Gang Dong Yun Zhou Xiaoli Song In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes Pharmaceutical Biology cyp3a4 cyp2e1 cyp2c9 herb–drug interaction |
| title | In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes |
| title_full | In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes |
| title_fullStr | In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes |
| title_full_unstemmed | In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes |
| title_short | In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes |
| title_sort | in vitro inhibitory effects of bergenin on human liver cytochrome p450 enzymes |
| topic | cyp3a4 cyp2e1 cyp2c9 herb–drug interaction |
| url | http://dx.doi.org/10.1080/13880209.2018.1525413 |
| work_keys_str_mv | AT gangdong invitroinhibitoryeffectsofbergeninonhumanlivercytochromep450enzymes AT yunzhou invitroinhibitoryeffectsofbergeninonhumanlivercytochromep450enzymes AT xiaolisong invitroinhibitoryeffectsofbergeninonhumanlivercytochromep450enzymes |