Effects of Gukang Capsules on activity and protein expression of hepatic cytochrome P450 enzymes in rats.
10.19540/j.cnki.cjcmm.20220620.201
- Author:
Chang YANG
1
;
Jing LI
1
;
Jia SUN
1
;
Ding-Yan LU
2
;
Shuai-Shuai CHEN
2
;
Yong-Jun LI
3
;
Yong-Lin WANG
1
;
Ting LIU
1
Author Information
1. State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University Guiyang 550004, China.
2. State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University Guiyang 550004, China Engineering Research Center for the Development and Application of Ethnic Medicine and Traditional Chinese Medicine (Ministry of Education), Guizhou Medical University Guiyang 550004, China.
3. Engineering Research Center for the Development and Application of Ethnic Medicine and Traditional Chinese Medicine (Ministry of Education), Guizhou Medical University Guiyang 550004, China.
- Publication Type:Journal Article
- Keywords:
Cocktail probes;
Gukang Capsules;
Western blot;
cytochrome P450;
liver microsomes
- MeSH:
Rats;
Animals;
Cytochrome P-450 CYP1A2/metabolism*;
Cytochrome P-450 CYP2C19;
Cytochrome P-450 CYP2E1/pharmacology*;
Rats, Sprague-Dawley;
Cytochrome P-450 Enzyme System/metabolism*;
Microsomes, Liver;
Liver;
Cytochrome P-450 CYP3A/metabolism*
- From:
China Journal of Chinese Materia Medica
2022;47(21):5936-5943
- CountryChina
- Language:Chinese
-
Abstract:
Gukang Capsules are often used in combination with drugs to treat fractures, osteoarthritis, and osteoporosis. Cytochrome P450(CYP450) mainly exists in the liver and participates in the oxidative metabolism of a variety of endogenous and exogenous substances and serves as an important cause of drug-metabolic interactions and adverse reactions. Therefore, it is of great significance to study the effect of Gukang Capsules on the activity and expression of CYP450 for increasing its clinical rational medication and improving the safety of drug combination. In this study, the Cocktail probe method was used to detect the changes in the activities of CYP1A2, CYP3A2, CYP2C11, CYP2C19, CYP2D4, and CYP2E1 in rat liver after treatment with high-, medium-and low-dose Gukang Capsules. The rat liver microsomes were extracted by the calcium chloride method, and protein expression of the above six CYP isoform enzymes was detected by Western blot. The results showed that the low-dose Gukang Capsules could induce CYP3A2 and CYP2D4 in rats, medium-dose Gukang Capsules had no effect on them, and high-dose Gukang Capsules could inhibit them in rats. The high-dose Gukang Capsules did not affect CYP2C11 in rats, but low-and medium-dose Gukang Capsules could induce CYP2C11 in rats. Gukang Capsules could inhibit CYP2C19 in rats and induce CYP1A2 in a dose-independent manner, but did not affect CYP2E1. If Gukang Capsules were co-administered with CYP1A2, CYP2C19, CYP3A2, CYP2C11, and CYP2D4 substrates, the dose should be adjusted to avoid drug interactions.
