Abstract：OBJECTIVE To study the effects of three aconitine transporters in Caco-2 cells and tannin (tannic acid) in Terminalia on the transport of three di-ester aconitine (aconitine, meoaconitine and hypaconitine) in Aconitum chinensis. METHODS The components were detected by UPLC/Q exactive MS in terms of the cumulative transshipment volume of three aconitine and the apparent permeability coefficient Papp as indicators to investigate the two-way transport behaviors of three aconitine in the Caco-2 cell model, as well as the proportion of tannic acid, and the changes of the transport behaviors of three aconitine. RESULTS There was a positive correlation between the cumulative transshipment volume of aconitine and the incubation time. There was no statistical difference in Papp values of the three aconitine, and the efflux effect was significantly stronger than the absorption, with an external ratio close to 1.5.When the compatibility ratio of three aconitine with tannic acid was 1∶1 and 1∶0.5, the absorption of aconitine was significantly inhibited (P was 0.05), but the transport behavior with effluent was not significantly affected. CONCLUSION Aconitine, meoaconitine, and hypaconitine in P. aeruginosa are mainly passive transporters, and may involve in efferent proteins, which are a kind of drug with good absorption.When mixed with tannic acid, the absorption and transshipment of three kinds of alkali were significantly reduced, which proves that Terminalia chebula could detoxify aconitum by inhibiting its absorption.
张晓菲, 苗鑫, 邢海燕, 李刚. 单宁酸对双酯型乌头碱在Caco-2细胞模型上转运行为的影响[J]. 中国药学杂志, 2019, 54(14): 1142-1147.
ZHANG Xiao-fei, MIAO Xin, XING Hai-yan, LI Gang. Effect of Tannic Acid on Transport of Diaco-Aconitine in Caco-2 Cell Model. Chinese Pharmaceutical Journal, 2019, 54(14): 1142-1147.
KANG Y, ZENG D, MAN Y B, et al. Comparison of sorption kinetics of PAHs by sorptive sinks and caco-2 cell and the correlation between bioaccessibility and bioavailability of PAHs in indoor dust[J] . Sci Total Environ, 2018, 645(15):170-178.
[2]
CAI J, ZHANG L, PENG J G, et al. Study on the transport mechanism of treponemate A in Caco-2 cell monolayer model [J] . Chin Pharm J(中国药学杂志), 2018, 53 (10):793-798.
[3]
WANG B, LI B. Effect of molecular weight on the transepithelial transport and peptidase degradation of casein-derived peptides by using Caco-2 cell model[J] . Food Chem, 2017, 218:1-8.
[4]
ZHANG X F, CUI T T, MIAO X, et al. Protective effects of Mongolian medicine Terminalin chebula on cardiotoxicity induced by Radix Aconiti Kusenezoffii in rats[J] . Chin Herb Med(中药材),2017,40(11):210-213.
ZHANG X W, JIN Y N, ZHANG B, et al. Benefit-risk assessment of Radix Aconiti Kusnezoffii in the treatment of Rheumatoid Arthritis [J] . Chin J Tradit Chin Med(中国中药杂志), 2018,43(2):234-241.
[7]
THONGON N, CHAMNIANSAWAT S. The inhibitory role of purinergic P2Y receptor on Mg2+ transport across intestinal epithelium-like Caco-2 monolayer[J] . J Physiol Sci, 2019,69(1):129-141.
[8]
QIU K, WU H, WANG H Y. Simultaneous determination of aconitine and hypaconitine in human plasma and urine by LC-MS/MS [J] . Chin Pharm J(中国药学杂志), 2010, 45 (8):633-636.
2019, Vol. 54 
