P-glycoprotein-mediated transport of berberine across Caco-2 cell monolayers
Abstract
The objective of this study was to investigate the mechanisms by which berberine is transported in the secretory and absorptive directions across Caco-2 cell monolayers. The basolateral-to-apical (B-A) flux was 30-fold greater than the apical-to-basolateral flux and temperature dependent (i.e., drastic decrease at 4 degrees C compared with 37 degrees C). The above results suggest the involvement of a carrier-mediated active transport mechanism for the B-A transport of berberine. However, no significant concentration dependency for the permeability (P(app)) of berberine was observed for B-A transport over a concentration range of 5-300 microM, indicating that the K(m) value of berberine for the carrier system is greater than 300 microM. Well-documented P-glycoprotein (P-gp) substrates such as verapamil, daunomycin, and rhodamine123 inhibited the B-A flux of berberine, whereas tetraethylammonium and taurocholate did not, suggesting that P-gp is involved in the transport. For the case of daunomycin, the B-A flux, but not the apical-to-basolateral flux, was significantly increased after pretreatment of the cell monolayers with berberine. In addition, the uptake of 1 microM daunomycin into Caco-2 cells was decreased as a result of this pretreatment. These results suggest that the repeated administration of berberine may up-regulate P-gp functions in Caco-2 cells. If this occurs in the gastrointestinal epithelial cells, the repeated administration of berberine may reduce the gastrointestinal absorption of P-gp substrates including chemotherapeutic agents such as daunomycin.
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Local inhibition of CYP3A4 and P-glycoprotein in the intestinal wall can markedly increase the absorbed fraction of the victim drug, independently of berberine's modest plasma concentrations.
“Local inhibition of CYP3A4 and P-glycoprotein in the intestinal wall can markedly increase the absorbed fraction of the victim drug, independently of berberine’s modest plasma concentrations [36,58].”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [58]
Berberine is both a substrate and an inhibitor of P-glycoprotein and can increase the intestinal absorption of its substrates.
“Berberine is both a substrate and an inhibitor of P-glycoprotein (P-gp/MDR1), and can increase the intestinal absorption of its substrates [58,77,78]”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [58]
Because P-glycoprotein and CYP3A4 are frequently colocalized in the enterocyte and share substrates, simultaneous inhibition of both can have a multiplicative effect on bioavailability.
“Because P-gp and CYP3A4 are frequently colocalized in the enterocyte and share substrates, simultaneous inhibition of both can have a multiplicative effect on bioavailability [58,64].”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [58]
Cites
BIOCHEMISTRY OF MULTIDRUG RESISTANCE MEDIATED BY THE MULTIDRUG TRANSPORTER
Gottesman, M. M., & PASTAN, I. (1993) · Annual Review of Biochemistry · doi:10.1146/annurev.bi.62.070193.002125 · Cited by 3,515 · see citing works
Thiebaut, F., TSURUO, T., Hamada, H., Gottesman, M. M., PASTAN, I., & Willingham, M. C. (1987) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.84.21.7735 · Cited by 2,777 · see citing works
A pharmacokinetic analysis program (multi) for microcomputer.
Yamaoka, K., Tanigawara, Y., Nakagawa, T., & Uno, T. (1981) · Journal of Pharmacobio-Dynamics · doi:10.1248/bpb1978.4.879 · Cited by 2,451 · see citing works
Expression of a multidrug-resistance gene in human tumors and tissues.
Fojo, A. T., Ueda, K., Slamon, D. J., Poplack, D. G., Gottesman, M. M., & Pastan, I. H. (1987) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.84.1.265 · Cited by 1,545 · see citing works
Tang, W., & Eisenbrand, G. (1992) · Springer eBooks · doi:10.1007/978-3-642-73739-8 · Cited by 1,311 · see citing works
Yee, S. (1997) · Pharmaceutical Research · doi:10.1023/a:1012102522787 · Cited by 1,035 · see citing works
Sparreboom, A., van Asperen, J., Mayer, U., Schinkel, A. H., Smit, J. W., Meijer, D. K. F., Borst, P., Nooijen, W. J., Beijnen, J. H., & van Tellingen, O. (1997) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.94.5.2031 · Cited by 884 · see citing works
Wacher, V. J., Wu, C., & Benet, L. Z. (1995) · Molecular Carcinogenesis · doi:10.1002/mc.2940130302 · Cited by 862 · see citing works
Stermitz, F. R., Lorenz, P., Tawara, J. N., Zenewicz, L. A., & Lewis, K. (2000) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.030540597 · Cited by 763 · see citing works
Human P-glycoprotein transports cortisol, aldosterone, and dexamethasone, but not progesterone.
Ueda, K., Okamura, N., Hirai, M., Tanigawara, Y., Saeki, T., Kioka, N., Komano, T., & Hori, R. (1992) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)35757-0 · Cited by 672 · see citing works
Tanigawara, Y., Okamura, N., Hirai, M., Yasuhara, M., Ueda, K., Kioka, N., Komano, T., & Hori, R. (1992) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)10423-0 · Cited by 338 · see citing works
P-Glycoproteins and Multidrug Resistance
Bellamy, W. T. (1996) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pa.36.040196.001113 · Cited by 332 · see citing works
Terao, T., Hisanaga, E., Sai, Y., Tamai, I., & Tsuji, A. (1996) · Journal of Pharmacy and Pharmacology · doi:10.1111/j.2042-7158.1996.tb05904.x · Cited by 234 · see citing works
Augustijns, P., Bradshaw, T., Gan, L., Hendren, R. W., & Thakker, D. R. (1993) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.1993.2487 · Cited by 172 · see citing works
Sack, R. B., & Froehlich, J. L. (1982) · Infection and Immunity · doi:10.1128/iai.35.2.471-475.1982 · Cited by 158 · see citing works
Hsing, S., Gatmaitan, Z., & Arias, I. M. (1992) · Gastroenterology · doi:10.1016/0016-5085(92)90173-v · Cited by 146 · see citing works
Wils, P., Phung-Ba, V., Warnery, A., Lechardeur, D., Raeissi, S. D., Hidalgo, I. J., & Scherman, D. (1994) · Biochemical Pharmacology · doi:10.1016/0006-2952(94)90580-0 · Cited by 131 · see citing works
Lin, H.-L., Liu, T.-Y., Wu, C.-W., & Chi, C.-W. (1999) · British Journal of Cancer · doi:10.1038/sj.bjc.6690710 · Cited by 100 · see citing works
Determination of berberine in plasma, urine and bile by high-performance liquid chromatography
Chen, C., & Chang, H.-C. (1995) · Journal of Chromatography B Biomedical Sciences and Applications · doi:10.1016/0378-4347(94)00517-9 · Cited by 92 · see citing works
YAMAMOTO, K., TAKASE, H., Ken-ichi, A. B. E., Saito, Y., & SUZUKI, A. (1993) · Folia Pharmacologica Japonica · doi:10.1254/fpj.101.3_169 · Cited by 71 · see citing works
Zhang, R. X., Dougherty, D. V., & Rosenblum, M. L. (1990) · PubMed · Cited by 63 · see citing works
Lin, H.-L., Liu, T., Lui, W., & Chi, C. (1999) · Cancer · doi:10.1002/(sici)1097-0142(19990501)85:9 · Cited by 57 · see citing works
Antisecretory effects of berberine in rat ileum
Tai, Y. H., Feser, J. F., Marnane, W. G., & Desjeux, J. F. (1981) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.1981.241.3.g253 · Cited by 49 · see citing works
Berberine inhibition of electrogenic ion transport in rat colon
Taylor, C. T., & Baird, A. W. (1995) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.1995.tb17224.x · Cited by 43 · see citing works
Antitumor activity of 13-methyl-berberrubine derivatives.
Ikekawa, T., & Ikeda, Y. (1982) · Journal of Pharmacobio-Dynamics · doi:10.1248/bpb1978.5.469 · Cited by 33 · see citing works
Berberine in toxin‐induced experimental cholera
Dutta, N. K., MARKER, P. H., & RAO, N. R. (1972) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.1972.tb07247.x · Cited by 28 · see citing works
Tanaka, K., Hirai, M., Tanigawara, Y., Ueda, K., Takano, M., Hori, R., & Inui, K.-I. (1997) · Biochemical Pharmacology · doi:10.1016/s0006-2952(96)00810-6 · Cited by 27 · see citing works
Antagonism of cholera toxin by berberine in the gastrointestinal tract of adult rats.
Sabir, M., Akhter, M. H., & Bhide, N. K. (1977) · PubMed · Cited by 21 · see citing works
Hunter, J., Hirst, B. H., & Simmons, N. L. (1993) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/0167-4889(93)90069-2 · Cited by 20 · see citing works
Effects of Berberine on Basal and Secretagogue-Modified Ion Transport in the Rabbit Ileum in Vitro
Guandalini, S., Fasano, A., Migliavacca, M., Marchesano, G., Ferola, A., & Rubino, A. (1987) · Journal of Pediatric Gastroenterology and Nutrition · doi:10.1097/00005176-198711000-00023 · Cited by 19 · see citing works
Flagged first, then by citations
2 of the 32 references couldn’t be matched to a known paper.
Cited by
Sorted by citations
Current knowledge and pharmacological profile of berberine: An update
Kumar, A., Ekavali, Chopra, K., Mukherjee, M., Pottabathini, R., & Dhull, D. K. (2015) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2015.05.068 · Cited by 533 · see citing works
Berberine in Cardiovascular and Metabolic Diseases: From Mechanisms to Therapeutics
Feng, X., Sureda, A., Jafari, S., Memariani, Z., Tewari, D., Annunziata, G., Barrea, L., Hassan, S. T. S., Šmejkal, K., Malaník, M., et al. (2019) · Theranostics · doi:10.7150/thno.30787 · Cited by 465 · see citing works
Cancer prevention and therapy through the modulation of the tumor microenvironment
Casey, S. C., Amedei, A., Aquilano, K., Azmi, A. S., Benencia, F., Bhakta-Guha, D., Bilsland, A. E., Boosani, C. S., Chen, S., Ciriolo, M. R., et al. (2015) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2015.02.007 · Cited by 373 · see citing works
Pirillo, A., & Catapano, A. L. (2015) · Atherosclerosis · doi:10.1016/j.atherosclerosis.2015.09.032 · Cited by 308 · see citing works
Classification Analysis of P-Glycoprotein Substrate Specificity
Didžiapetris, R., Japertas, P., Avdeef, A., & Petrauskas, A. A. (2003) · Journal of drug targeting · doi:10.1080/10611860310001648248 · Cited by 254 · see citing works
Nguyen, T., Duong, V., & Maeng, H. (2021) · Pharmaceutics · doi:10.3390/pharmaceutics13071103 · Cited by 262 · see citing works
Self-citationNatural alkaloids as P-gp inhibitors for multidrug resistance reversal in cancer
Joshi, P., Vishwakarma, R. A., & Bharate, S. B. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.06.047 · Cited by 179 · see citing works
β-Phenylethylamines and the isoquinoline alkaloids
Bentley, K. W. (2004) · Natural Product Reports · doi:10.1039/b212259f · Cited by 126 · see citing works
Nies, A. T., Herrmann, E., Brom, M., & KEPPLER, D. O. R. (2007) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-007-0219-x · Cited by 124 · see citing works
Zhang, S., & Morris, M. E. (2003) · Pharmaceutical Research · doi:10.1023/a:1025044913766 · Cited by 120 · see citing works
Zhang, X., Qiu, F., Jiang, J. C., Gao, C., & Tan, Y. (2011) · Xenobiotica · doi:10.3109/00498254.2010.529180 · Cited by 109 · see citing works
Wu, J., Guo, Z., Zhu, Y., Huang, Z., Gong, X., Li, Y., Son, W.-J., Li, X., Lou, Y.-M., Zhu, L., et al. (2018) · Phytomedicine · doi:10.1016/j.phymed.2018.03.001 · Cited by 108 · see citing works
Naturally Occurring PCSK9 Inhibitors
Adorni, M. P., Zimetti, F., Lupo, M. G., Ruscica, M., & Ferri, N. (2020) · Nutrients · doi:10.3390/nu12051440 · Cited by 93 · see citing works
Wu, X., Li, Q., Xin, H., Yu, A., & Zhong, M. (2005) · European Journal of Clinical Pharmacology · doi:10.1007/s00228-005-0952-3 · Cited by 90 · see citing works
Meng, Z., Zhang, M., Shengnan, W., Xiaojia, B., Hatch, G. M., Gu, J., & Li, C. (2014) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2014.03.017 · Cited by 86 · see citing works
Zhang, M., Lv, X., Li, J., Meng, Z., Wang, Q., Chang, W., Li, W., Chen, L., & Liu, Y. (2012) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2012.08.006 · Cited by 84 · see citing works
Zhang, Y., Cui, Y., Gao, L., & Jiang, H.-L. (2013) · International Journal of Biological Macromolecules · doi:10.1016/j.ijbiomac.2013.04.074 · Cited by 83 · see citing works
Ye, L., Yang, X., Yang, Z., Gao, S., Yin, T., Liu, W., Wang, F., Hu, M., & Liu, Z. (2012) · Toxicology Letters · doi:10.1016/j.toxlet.2012.11.011 · Cited by 77 · see citing works
Kwon, M., Lim, D. Y., Lee, C. H., Jeon, J.-H., Choi, M.-K., & Song, I.-S. (2020) · Pharmaceutics · doi:10.3390/pharmaceutics12090882 · Cited by 76 · see citing works
“The treatment of known P-gp inhibitors, such as cyclosporine A, verapamil, and C219 antibodies, increased the berberine uptake in Caco-2 cells [13,14].”
BackgroundSelf-citationBranton, A. (2017) · American Journal of Clinical and Experimental Medicine · doi:10.11648/j.ajcem.20170504.16 · Cited by 76 · see citing works
Liver-target nanotechnology facilitates berberine to ameliorate cardio-metabolic diseases
Guo, H., Feng, C., Zhang, W., Luo, Z., Zhang, H., Zhang, T., Ma, C., Zhan, Y., Li, R. P., Wu, S., et al. (2019) · Nature Communications · doi:10.1038/s41467-019-09852-0 · Cited by 75 · see citing works
Xu, H., Liu, C., Huang, C., Chen, L., Zheng, Y.-R., Si-hang, H., & Long, X. (2019) · Colloids and Surfaces B Biointerfaces · doi:10.1016/j.colsurfb.2019.06.006 · Cited by 73 · see citing works
Zhu, Y. Z., Xie, N., Chai, Y., Nie, Y., Liu, K., Liu, Y., Yang, Y., Su, J., & Zhang, C. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.803717 · Cited by 75 · see citing works
Videmann, B., Tep, J., Cavret, S., & Lecoeur, S. (2007) · Food and Chemical Toxicology · doi:10.1016/j.fct.2007.04.011 · Cited by 71 · see citing works
Gurley, B. J., Swain, A., Barone, G. W., Williams, D. K., Breen, P. J., Yates, C. R., Stuart, L. B., Hubbard, M. A., Tong, Y., & Cheboyina, S. (2006) · Drug Metabolism and Disposition · doi:10.1124/dmd.106.012708 · Cited by 69 · see citing works
Ma, B., & Ma, Y. (2016) · Drug Metabolism Reviews · doi:10.3109/03602532.2015.1124888 · Cited by 68 · see citing works
Cao, S., Zhou, Y., Xu, P., Wang, Y., Yan, J., Bin, W., Qiu, F., & Kang, N. (2013) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2013.07.025 · Cited by 67 · see citing works
Research progress on pharmacological effects and bioavailability of berberine
Cui, Y., Zhou, Q., Jin, M., Jiang, S., Shang, P., Dong, X., & Li, L. (2024) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-024-03199-0 · Cited by 70 · see citing works
Roytrakul, S., & Verpoorte, R. (2007) · Phytochemistry Reviews · doi:10.1007/s11101-006-9022-4 · Cited by 60 · see citing works
Zhang, B., Wang, L., Ji, X., Zhang, S., Attila Gabor, S. I. K., Liu, K., & Jin, M. (2020) · Journal of Neuroimmune Pharmacology · doi:10.1007/s11481-019-09902-w · Cited by 57 · see citing works
Cao, S., Xu, P., Yan, J., Liu, H., Liu, L., Cheng, L., Qiu, F., & Kang, N. (2018) · Journal of Cellular Biochemistry · doi:10.1002/jcb.27102 · Cited by 56 · see citing works
Effect of organophosphate pesticide diazinon on expression and activity of intestinal P-glycoprotein
Lecoeur, S., Videmann, B., & Mazallon, M. (2005) · Toxicology Letters · doi:10.1016/j.toxlet.2005.09.003 · Cited by 53 · see citing works
Enhancement of Sodium Caprate on Intestine Absorption and Antidiabetic Action of Berberine
Lv, X., Li, J., Zhang, M., Wang, C., Fan, Z., Wang, C., & Chen, L. (2010) · AAPS PharmSciTech · doi:10.1208/s12249-010-9386-z · Cited by 53 · see citing works
Shan, Y., Ren, G., Wang, Y., Pang, J., Zhao, Z., Yao, J., You, X., Si, S., Song, D., Kong, W., et al. (2012) · Metabolism · doi:10.1016/j.metabol.2012.09.009 · Cited by 53 · see citing works
Djebbi, M. A., Elabed, A., Bouaziz, Z., Sadiki, M., Elabed, S., Namour, P., Jaffrezic-Renault, N. J., & Amara, A. B. H. (2016) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2016.09.089 · Cited by 52 · see citing works
Tetrandrine Potentiates the Hypoglycemic Efficacy of Berberine by Inhibiting P-Glycoprotein Function
Shan, Y., Zhu, Y., Pang, J., Wang, Y., Song, D., Kong, W., & Jiang, J. (2013) · Biological and Pharmaceutical Bulletin · doi:10.1248/bpb.b13-00272 · Cited by 52 · see citing works
Zhang, Y., Yang, Y., & Yang, X. (2017) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2017.12.017 · Cited by 48 · see citing works
Fan, D., Wu, X., Dong, W., Sun, W., Li, J., & Tang, X. (2012) · Drug Development and Industrial Pharmacy · doi:10.3109/03639045.2012.723219 · Cited by 46 · see citing works
Berberine in type 2 diabetes therapy: a new perspective for an old antidiarrheal drug?
Ming, Z., & Chen, L. (2012) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2012.06.004 · Cited by 46 · see citing works
Ma, B., & Ma, Y. (2012) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1517/17425255.2012.722995 · Cited by 45 · see citing works
Qian, P., Zhang, Y.-B., Yang, Y., Xu, W., & Yang, X. (2017) · Molecules · doi:10.3390/molecules22020214 · Cited by 46 · see citing works
He, W., Liu, G., Cai, H., Sun, X., Hou, W., Zhang, P., Xie, Z., & Liao, Q. (2014) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2014.04.040 · Cited by 44 · see citing works
Kumar, A., Ekavali, Mishra, J., Chopra, K., & Dhull, D. K. (2015) · Psychopharmacology · doi:10.1007/s00213-015-4095-7 · Cited by 43 · see citing works
Han, L., Sheng, W., Li, X., Attila Gabor, S. I. K., Lin, H., Liu, K., & Wang, L. (2019) · MedChemComm · doi:10.1039/c9md00036d · Cited by 42 · see citing works
Habtemariam, S. (2020) · Biomedicines · doi:10.3390/biomedicines8040090 · Cited by 42 · see citing works
Murakami, T., Bodor, E., & Bodor, N. (2023) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1080/17425255.2023.2203857 · Cited by 41 · see citing works
Wang, L., Kong, H., Jin, M., Li, X., Stoika, R. S., Lin, H., & Liu, K. (2020) · Organic & Biomolecular Chemistry · doi:10.1039/d0ob00327a · Cited by 39 · see citing works
Nguyen, J. T., Tian, D., Tanna, R. S., Hadi, D. L., Bansal, S., Calamia, J. C., Arian, C. M., Shireman, L. M., Molnár, B., Horváth, M., et al. (2021) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.2107 · Cited by 40 · see citing works
Poor permeability and absorption affect the activity of four alkaloids from Coptis
Cui, H., Zhang, Q., Wang, J., Chen, J., Zhang, Y., & Tong, X. (2015) · Molecular Medicine Reports · doi:10.3892/mmr.2015.4288 · Cited by 40 · see citing works
Qiao, X., Wang, Q., Wang, S., Kuang, Y., Li, K., Song, W., & Ye, M. (2018) · Frontiers in Pharmacology · doi:10.3389/fphar.2018.00622 · Cited by 40 · see citing works
Mujtaba, M. A., Akhter, M. H., Alam, M. S., Ali, M. D., & Hussain, A. (2021) · Current Pharmaceutical Biotechnology · doi:10.2174/1389201022666210208152113 · Cited by 41 · see citing works
Wu, J., Li, J., Li, W., Sun, B., Xie, J., Cheng, W., & Zhang, Q. (2018) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2018.04.025 · Cited by 39 · see citing works
Zha, W., Wang, G., Xu, W., Liu, X., Wang, Y., Zha, B. S., Shi, J., Zhao, Q., Gerk, P. M., Studer, E. J., et al. (2013) · PLoS ONE · doi:10.1371/journal.pone.0054349 · Cited by 39 · see citing works
Luo, S., Pal, D., Shah, S. J., Kwatra, D., Paturi, K. D., & Mitra, A. K. (2010) · Molecular Pharmaceutics · doi:10.1021/mp900193e · Cited by 38 · see citing works
Zhao, W., Uehera, S., Tanaka, K., Tadokoro, S., Kusamori, K., Katsumi, H., Sakane, T., & Yamamoto, A. (2016) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2016.01.020 · Cited by 37 · see citing works
Transporter-mediated natural product–drug interactions for the treatment of cardiovascular diseases
Zha, W. (2017) · Journal of Food and Drug Analysis · doi:10.1016/j.jfda.2017.11.008 · Cited by 35 · see citing works
Xiao, L. J., Poudel, A. J., Huang, L., Wang, Y., Abdalla, A. M. E., & Yang, G. (2020) · International Journal of Biological Macromolecules · doi:10.1016/j.ijbiomac.2020.03.030 · Cited by 34 · see citing works
Nutraceutical approaches to metabolic syndrome
Sirtori, C. R., Pavanello, C., Calabresi, L., & Ruscica, M. (2017) · Annals of Medicine · doi:10.1080/07853890.2017.1366042 · Cited by 33 · see citing works
Effect of ion-pair formation with bile salts on the in vitro cellular transport of berberine
Chae, H.-W., Kim, I., Jin, H., Kim, D., Chung, S., & Shim, C. (2008) · Archives of Pharmacal Research · doi:10.1007/s12272-008-1127-4 · Cited by 31 · see citing works
Self-citationBiodistribution and pharmacokinetic profile of berberine and its metabolites in hepatocytes
Liu, X., Li, W., Zhang, H., Wang, X., Huang, Y., Li, Y., & Pan, G. (2022) · Phytomedicine · doi:10.1016/j.phymed.2022.154288 · Cited by 27 · see citing works
Ai, Y., Wu, Y., Wang, F., Ma, W., Bian, Q., Lee, D. Y. W., & Dai, R. (2015) · Journal of Mass Spectrometry · doi:10.1002/jms.3563 · Cited by 26 · see citing works
Li, Q., Li, K., Sun, H. L., Jin, W., Shi, J.-W., & Shi, Y. (2014) · Molecules · doi:10.3390/molecules191016312 · Cited by 25 · see citing works
Formisano, E., Pasta, A., Cremonini, A. L., Favari, E., Ronca, A., Carbone, F., Semino, T., Pierro, F. D., Sukkar, S. G., & Pisciotta, L. (2019) · Journal of Medicinal Food · doi:10.1089/jmf.2019.0168 · Cited by 25 · see citing works
Response of Escherichia coli to Prolonged Berberine Exposure
Gökgöz, N. B., Avcı, F. G., Yoneten, K. K., Alaybeyoglu, B., Özkırımlı, E., Sayar, N. A., Kazan, D., & Akbulut, B. S. (2016) · Microbial Drug Resistance · doi:10.1089/mdr.2016.0063 · Cited by 24 · see citing works
Liu, Y., Zhu, K., Cao, L., Xie, Z., Gu, M., Lu, W. P., Li, J., & Nan, F. (2020) · Acta Pharmacologica Sinica · doi:10.1038/s41401-019-0346-1 · Cited by 24 · see citing works
Murakami, T., Bodor, E. T., & Bodor, N. S. (2023) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1080/17425255.2023.2203858 · Cited by 23 · see citing works
Xu, Y., Quan, H., Wang, Y., Zhong, H., Sun, J., Xu, J., Jia, N., & Jiang, Y. (2017) · Frontiers in Cellular and Infection Microbiology · doi:10.3389/fcimb.2017.00491 · Cited by 23 · see citing works
Lyu, Y., Zhang, Y., Yang, M., Lin, L., Yang, X., Cheung, S. C. K., Shaw, P. C., Chan, P. K. S., Kong, A. P. S., & Zuo, Z. (2019) · Life Sciences · doi:10.1016/j.lfs.2019.116818 · Cited by 23 · see citing works
Berberine in fish nutrition: Impact on hepatoenteric health, antioxidative and immune status
Wang, L., Sagada, G., Wang, C., Gao, C. Y., Wang, B., Shao, Q., & Yan, Y. (2022) · Frontiers in Marine Science · doi:10.3389/fmars.2022.967748 · Cited by 22 · see citing works
Wang, X., Xing, D., Wang, W., Fan, L., Su, H. C., & Du, L. (2005) · Neuroscience Letters · doi:10.1016/j.neulet.2004.12.050 · Cited by 22 · see citing works
Saha, L., Kumari, P., Rawat, K., Gautam, V., Sandhu, A., Singh, N., Bhatia, A., Bhattacharya, S., Sinha, V. R., & Chakrabarti, A. (2023) · Neurochemical Research · doi:10.1007/s11064-023-03967-z · Cited by 20 · see citing works
Sun, Y.-H., He, X., Xiao-Lin, Y. A. N. G., Dong, C.-L., Zhang, C.-F., Song, Z., Lu, M., Yang, Z., & Li, P. (2014) · Chinese Journal of Natural Medicines · doi:10.1016/s1875-5364(14)60085-6 · Cited by 20 · see citing works
Sun, J.-M., Bao, H., Peng, Y., Zhang, H., Sun, Y. N., Qi, J., Zhang, H., & Gao, Y. (2018) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2018.04.014 · Cited by 20 · see citing works
Clinical Drug Interactions with Medicinal Herbs
Johne, A., & Roots, I. (2005) · Evidence-Based Integrative Medicine · doi:10.2165/01197065-200502040-00004 · Cited by 19 · see citing works
Hwang, Y.-H., Cho, W.-K., Jang, D., Ha, J.-H., Jung, K., Yun, H.-I., & Ma, J. Y. (2012) · Evidence-Based Complementary and Alternative Medicine · doi:10.1155/2012/673132 · Cited by 18 · see citing works
Metformin inhibits mitochondrial complex I in intestinal epithelium to promote glycaemic control
Sebo, Z. L., Chakrabarty, R. P., Grant, R. A., D’Alessandro, K. B., Koss, A. R., Blum, J. L. E., Davidson, S. M., Reczek, C. R., & Chandel, N. S. (2026) · Nature Metabolism · doi:10.1038/s42255-026-01530-y · Cited by 21 · see citing works
Wang, L., Yang, X., Li, X., Stoika, R. S., Wang, X., Lin, H., Ma, Y., Wang, R., & Liu, K. (2020) · New Journal of Chemistry · doi:10.1039/d0nj01645d · Cited by 16 · see citing works
Therapeutic Effects of Berberine in Metabolic Diseases and Diabetes Mellitus
Aram, K., Bahari, Z., Elliyeh, M., & Ghasemi, M. (2021) · Revista Brasileira de Farmacognosia · doi:10.1007/s43450-021-00159-0 · Cited by 16 · see citing works
Improving the oral bioavailability of berberine: A crystal engineering approach
Surampudi, A. V. S. D., Prasad, S. R., Ramanujam, P., Swain, D., Wadje, B. N., Bharate, S. B., Kamalakannan, U., Kathirvel, M., & Sridhar, B. (2025) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2025.126177 · Cited by 15 · see citing works
Fratter, A., & Servi, B. (2015) · International Journal of Drug Delivery Technology · doi:10.25258/ijddt.v5i1.8866 · Cited by 15 · see citing works
A Comprehensive Review Highlighting the Prospects of Phytonutrient Berberine as an Anticancer Agent
Haque, S., Mathkor, D. M., Bhat, S. A., Musayev, A., Khituova, L., Ramniwas, S., Phillips, E., Swamy, N., Kumar, S., Yerer, M. B., et al. (2024) · Journal of Biochemical and Molecular Toxicology · doi:10.1002/jbt.70073 · Cited by 14 · see citing works
Pharmacological/Biological Effects of Berberine
Gálvez, E. M., Perez, M., Domingo, P., Núñez-Jurado, D., Cebolla, V. L., Matt, M., & Pardo, J. (2013) · Springer eBooks · doi:10.1007/978-3-642-22144-6_182 · Cited by 14 · see citing works
Zhang, Y., & Liu, H. (2016) · International Journal of Polymer Science · doi:10.1155/2016/4235832 · Cited by 13 · see citing works
Konsoula, Z., & Jung, M. (2009) · Biological and Pharmaceutical Bulletin · doi:10.1248/bpb.32.74 · Cited by 13 · see citing works
Doo, M.-H., Li, H., Jang, H.-I., Song, I., Chung, S., & Shim, C. (2005) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2005.06.014 · Cited by 13 · see citing works
Self-citationGong, Z., Yang, Q., Wang, Y., Weng, X., Li, Y., Dong, Y. J., Zhu, X., & Chen, Y. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.948678 · Cited by 12 · see citing works
Enhancement of Berberine Hypoglycemic Activity by Oligomeric Proanthocyanidins
Zhang, H., Wang, X., Wang, T., Chen, K., Wang, H., Jia, Q., & Li, Y. (2018) · Molecules · doi:10.3390/molecules23123318 · Cited by 12 · see citing works
Mazza, A., Nicoletti, M., Lenti, S., Torin, G., Rigatelli, G., Pellizzato, M., & Fratter, A. (2020) · Journal of Medicinal Food · doi:10.1089/jmf.2020.0019 · Cited by 12 · see citing works
Mishra, R., & Dhole, S. N. (2019) · Journal of Applied Pharmaceutical Science · doi:10.7324/japs.2019.91105 · Cited by 12 · see citing works
Detoxification mechanisms of ginseng to aconite: A review
Bao, Y., Zhang, R., Jiang, X., Liu, F., He, Y., Hu, H., Hou, X., Li, H., & Pei, X. (2022) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2022.116009 · Cited by 11 · see citing works
Cao, S., Yu, S., Cheng, L., Yan, J., Zhu, Y., Deng, Y., Qiu, F., & Kang, N. (2018) · Environmental Toxicology and Pharmacology · doi:10.1016/j.etap.2018.09.007 · Cited by 11 · see citing works
Berberine: A Bitter Phytochemical With Diversely Sweet Therapeutic Properties
Sikora, B., Bahadori, M. B., Magg, A. D., Moghadasian, N., & Moghadasian, M. H. (2025) · Nutrition Reviews · doi:10.1093/nutrit/nuaf172 · Cited by 10 · see citing works
Teodori, E., Braconi, L., Manetti, D., Romanelli, M. N., & Dei, S. (2022) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026623666221025111528 · Cited by 9 · see citing works
Lu, F., Li, E., & Yang, X. (2023) · Heliyon · doi:10.1016/j.heliyon.2023.e19371 · Cited by 8 · see citing works
Shaikh, A. S., Chilvery, S., Patil, S., Mourya, A., Kumar, A., Sharma, A., Ikhe, A. S., Makhal, P. N., Madan, J., Godugu, C., et al. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.108791 · Cited by 8 · see citing works
Lee, S., Joo, S.-A., Kim, H., Lee, Y., Chung, S., Chae, Y., & Maeng, H. (2023) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2023.106396 · Cited by 8 · see citing works
Self-citationAssessment and modulation of phillyrin absorption by P-gp using Caco-2 cells and MDR1-MDCKII cells
Li, Y., Ye, L.-H., Jiang, X., & Peng, C. Y. (2011) · European Journal of Drug Metabolism and Pharmacokinetics · doi:10.1007/s13318-011-0026-0 · Cited by 8 · see citing works
Xiao, L., Xue, Y., Zhang, C., Wang, L., Lin, Y., & Pan, G. (2017) · Xenobiotica · doi:10.1080/00498254.2017.1300707 · Cited by 8 · see citing works
Feng, H., Hong, Y.-J., Zheng, Q.-Q., Ge, J.-M., Cheng, H., Liu, Y., Deng, J., Li, Q., & Qu, S. (2025) · Journal of Colloid and Interface Science · doi:10.1016/j.jcis.2025.138500 · Cited by 6 · see citing works
The Effect of Streptozotocin and Alloxan on the mRNA Expression of Rat Hepatic Transporters In Vivo
Zhai, T., Wang, J., Sun, L., & Chen, Y. (2014) · AAPS PharmSciTech · doi:10.1208/s12249-014-0262-0 · Cited by 6 · see citing works
- Authors
- Maeng, H.-J., Yoo, H.-J., Kim, I.-W., Song, I.-S., Chung, S.-J., & Shim, C.-K.
- Affiliations
- Seoul National University (KR)
- Corresponding author
- Shim, Chang-Koo
- Venue
- Journal of Pharmaceutical Sciences
- Publisher
- Elsevier BV
- Published
- 2002-12
- Volume
- 91
- Issue
- 12
- Pages
- 2614-2621
- ISSN
- 0022-3549 (ISSN-L)
- OpenAlex
- W2091571409
- Cited by
- 128
- References
- 32
- Citations by year
- 2026: 9 · 2025: 8 · 2024: 7 · 2023: 7 · 2022: 7 · 2021: 3 · 2020: 10 · 2019: 7 · 2018: 8 · 2017: 9 · 2016: 6 · 2015: 7 · 2014: 6 · 2013: 5 · 2012: 7
- FWCI
- 1.18
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Pharmaceutical Sciences (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- berberine, P-glycoprotein, Caco-2 cell monolayers, intestinal drug transport, active transport, daunorubicin, gastrointestinal absorption, drug-drug interactions, verapamil, rhodamine 123
- MeSH terms
- Berberine, Biological Transport, Daunorubicin, Humans, Caco-2 Cells, ATP Binding Cassette Transporter, Subfamily B, Member 1
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