![]() ![]() The results showed that the chelerythrine was mostly excreted in feces and a small proportion of alkaloid was absorbed. Kosina and their research group investigated the levels of chelerythrine in plasma, tissues and feces of pigs ( 6). Previous pharmacokinetic studies have indicated that the bioavailability of chelerythrine was apparently low after oral administration. Thus, the pharmacokinetic study of chelerythrine in animals is very important due to its biological effects and commercial use. ![]() cordata have significant pharmacological activities, but they are also toxic. In 1982, the pharmaceutical industry began to produce the drug ( 5). Sanguiritrin was reportedly authorized by the Ministry of Health of the Union of Soviet Socialist Republics for industrial production and a wide range of medical uses for pharmaceutical formulations. The efficacy and safety of sanguiritrinin oral care has been tested in many long-term and short-term clinical trials, e.g., using products presented by Paraskevas ( 4). cordata is made up of QBAs in part containing sanguinarine and chelerythrine, which has been used as an antiplaque agent for mouthwash and toothpaste, and in veterinary preparation for the treatment of mastoiditis in cows. Quaternary benzophenanthrine alkaloids (QBAs) can improve the performance of an animal by eliminating the demand for antibiotics in the feed ( 3). cordataare are Sanguinarine and chelerythrine ( 3). The powdered mixture of seeds, capsules, and leaves are the main components of the feed additive Sangrovit ( 2). (Papaveraceae), a perennial plant, is listed as feed additive for animal production by the European Food Safety Authorityin 2004 ( 1). In addition, it provided a reference basis for the metabolic mechanism of chelerythrinein rats. Chelerythrine had a weak impact on NQO1 activity, but sanguinarine inhibited NQO1 activityĬonclusion: Through studying the effects of cytosolic reductase inhibitors on chelerythrine reduction and the impact of chelerythrine and sanguinarine on the activity of NQO1 in vitro and in vivo, we clarified the potential drug interaction of Macleaya cordata extract in clinical application, so as to provide theoretical guidance for clinically safe medication. Macleaya cordata extracts treated female and male rats, respectively, showed different responses, inhibiting NQO1 activity in males, but inducing NQO1 activity in females. The results also indicated that XO, NQO1, NQO2, and carbonyl reductase are involved in chelerythrine reduction. After the rats were given intragastric administration, the low concentration residues of sanguinarine and chelerythrine in different rat tissues were found at 48 h after the last dose, suggesting that both compounds could be widely distributed in tissues. The reduction of the iminium bond of chelerythrine and subsequent O-demethylation was the main metabolic pathway of chelerythrine in rat liver S9 while the reduction of the iminium bond of chelerythrine was the main metabolic pathway of chelerythrine in rats in vivo. Results: A total of twelve metabolites of chelerythrine were characterized by this approach in rat liver S9 and in vivo. The tissue distribution of chelerythrine and the effects on NQO1 following intragastric administration with M. The metabolic enzymes that were involved in chelerythrine reduction were investigated using an inhibition method. The structures of CHE metabolites were elucidated by comparing their changes in accurate molecular masses and fragment ions with those of parent ion or metabolite. Methods: The metabolites of chelerythrine in rats were measured in vitro and in vivo by rapid and accurate high-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry (HPLC/QqTOF-MS). 4Yiyang Vocational and Technical College, Yiyang, Chinaīackground: Macleaya cordata (Willd.) (Papaveraceae) is listed as a feed additive in animal production by the European Food Authority.3Hunan Prima Drug Research Center Co., Ltd., Changsha, China.2Hunan Engineering Technology Research Center of Veterinary Drugs, Hunan Agricultural University, Changsha, China.1College of Veterinary Medicine, Hunan Agricultural University, Changsha, China.Chong-Yin Huang 1,2 †, Ya-Jun Huang 1,3 †, Zhuo-Yi Zhang 1,4, Yi-Song Liu 1 and Zhao-Ying Liu 1,2 * ![]()
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