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Investigation on the intestinal absorption characters of harmine derivative H-2-168 using Caco-2 cells and single-pass intestinal perfusion
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Qin-wei XU1, Liang TENG2, Bei CHEN2, Qin MA3, Jin-xin LI1, Yu-jie HUANG1, Hui-jing GAO2, *
Chinese Journal of New Drugs | 2025, 34(17) : 1845 - 1851
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Chinese Journal of New Drugs | 2025, 34(17): 1845-1851
Investigation on the intestinal absorption characters of harmine derivative H-2-168 using Caco-2 cells and single-pass intestinal perfusion
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Qin-wei XU1, Liang TENG2, Bei CHEN2, Qin MA3, Jin-xin LI1, Yu-jie HUANG1, Hui-jing GAO2, *
Affiliations
  • 1College of Pharmacy, Xinjiang Medical University, Urumqi 830011, China
  • 2State Key Laboratory of Pathogenesis, Prevention and Treatment of High Incidence Diseases in Central Asia Fund, Department of Pharmacy, The First Affiliated Hospital of Xinjiang Medical University, Urumqi 830054, China
  • 3Xinjiang Huashidan Pharmaceutical Co., Ltd., Urumqi 830011, China
Published: 2025-09-15 doi: 10.20251/j.cnki.1003-3734.2025.17.009
Outline
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Objective:

To investigate the intestinal absorption characteristics of harmine derivative H-2-168 using Caco-2 cells model and in situ single-pass intestinal perfusion method.

Methods:

The Caco-2 cell monolayer model and in situ single pass intestinal perfusion model of rat were established. The concentrations of H-2-168 in cell permeation fluid and intestinal perfusion fluid were determined by HPLC. The changes of apparent permeability coefficient (Papp) of H-2-168 in Caco-2 cell model and those of absorption rate constant (Ka) and Papp in in situ single pass intestinal perfusion model of rat under different influence factors (intestinal segment, concentration, pH and P-glycoprotein inhibitor) were investigated.

Results:

In Caco-2 cell model, Papp values at medium and high concentrations of H-2-168 were significantly higher than that at low concentration (P<0.05), but Papp at high concentration was slightly lower than that at medium concentration, showing a high concentration saturation phenomenon. H-2-168 was absorbed in the whole intestine of rats, with Ka and Papp decreased significantly with the increase of drug concentration (P<0.05). Ka and Papp at pH 7.4 were significantly higher than those at pH 5.4. There were no significant changes in the absorption parameters before and after the addition of P-glycoprotein inhibitor (P>0.05).

Conclusion:

H-2-168 is a well-absorbed drug, and its absorption mechanism may involve active transport or facilitated diffusion, and it is not a substrate of P-glycoprotein.

harmine derivative  /  Caco-2 cell model  /  in situ single-pass intestinal perfusion  /  intestinal absorption
Qin-wei XU, Liang TENG, Bei CHEN, Qin MA, Jin-xin LI, Yu-jie HUANG, Hui-jing GAO. Investigation on the intestinal absorption characters of harmine derivative H-2-168 using Caco-2 cells and single-pass intestinal perfusion[J]. Chinese Journal of New Drugs, 2025 , 34 (17) : 1845 -1851 . DOI: 10.20251/j.cnki.1003-3734.2025.17.009
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Year 2025 volume 34 Issue 17
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Article Info
doi: 10.20251/j.cnki.1003-3734.2025.17.009
  • Online Date：2026-03-06
  • Published：2025-09-15
Article Data
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History
  • Accepted：2025-01-06
Funding
Affiliations
    1College of Pharmacy, Xinjiang Medical University, Urumqi 830011, China
    2State Key Laboratory of Pathogenesis, Prevention and Treatment of High Incidence Diseases in Central Asia Fund, Department of Pharmacy, The First Affiliated Hospital of Xinjiang Medical University, Urumqi 830054, China
    3Xinjiang Huashidan Pharmaceutical Co., Ltd., Urumqi 830011, China
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https://castjournals.cast.org.cn/joweb/zgxyzz/EN/10.20251/j.cnki.1003-3734.2025.17.009
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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
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