PDF
Full
Outline
HPLC was used to establish the methods for the determination of harmaline (HM) and the derivative 9-butyl-1-methyl-N-(2-hydroxy) ethyl-β- carboline-3-formamide (No.: H-2-104) in rat blood samples in order to evaluate repeated dosing toxicokinetics (TK).
The Wistar rats were randomly divided into HM low, medium, and high-dose groups and H-2-104 low, medium, and high-dose groups (35, 70, 140 mg·kg-1) with eight rats in each group. Repeated dosing toxicity experiments were conducted to investigate the toxicokinetic profile of HM and H-2-104 in rats 28 days after the first dose to the end of administration and the kinetic parameters were calculated.
Both HM and derivative H-2-104 could be detected with good linearity in the range of 66.67~500 ng·mL-1. The specialized properties, accuracy, precision, extraction recovery, and stability of the proposed method were in accordance with the requirements for the determination of biological samples. After the administration of HM, the Cmax and AUC0-t in rats were (301.78±67.24) ng·mL-1, (234.18±98.35) ng·mL-1 (low concentration); (478.65±99.74) ng·mL-1, (710.03±208.93) ng·mL-1 (medium concentration); (721.51±107.52) ng·mL-1, (819.61±310.54) ng·mL-1 (high concentration). After the administration of H-2-104, the Cmax and AUC0-t in rats were (234.84±102.03) ng·mL-1, (198.67±38.88) ng·mL-1 (low concentration); (298.73±87.52), (676.55±210.83) ng·mL-1 (medium concentration); (411.81±123.71), (1 004.86±426.05) ng·mL-1 (high concentration). After administration, Tmax of the two compounds was shorter and both drugs were eliminated within 4 hours.
The first and last Cmax and AUC0-t of HM and derivative H-2-104 at each dose increased disproportionately with dose and were positively correlated with dose, exhibiting nonlinear kinetics. This study provides preliminary elucidation of the in vivo toxicokinetic behavior of HM and derivative H-2-104 in rats, and the experimental results provide support and reference for their subsequent studies.
PDF
33
13
| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
关闭全屏
No. 86 Xueyuan South Road, Haidian District, Beijing
010-62199257
qkjq@cast.org.cn
Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House
