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Volume 11
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10.3390/pharmaceutics11070355
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Article

Identification of Catalposide Metabolites in Human Liver and Intestinal Preparations and Characterization of the Relevant Sulfotransferase, UDP-glucuronosyltransferase, and Carboxylesterase Enzymes

by
Deok-Kyu Hwang
1,†,
Ju-Hyun Kim
2,†,
Yongho Shin
1,
Won-Gu Choi
1,
Sunjoo Kim
1,
Yong-Yeon Cho
1,
Joo Young Lee
1,
Han Chang Kang
1 and
Hye Suk Lee
1,*
1
BK21 PLUS Team for Creative Leader Program for Pharmacomics-based Future Pharmacy, College of Pharmacy, The Catholic University of Korea, Bucheon 14662, Korea
2
College of Pharmacy, Yeungnam University, Gyeongsan 38541, Korea
*
Author to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Pharmaceutics 2019, 11(7), 355; https://doi.org/10.3390/pharmaceutics11070355
Submission received: 24 June 2019 / Revised: 18 July 2019 / Accepted: 19 July 2019 / Published: 22 July 2019
(This article belongs to the Special Issue Drug Metabolism/Transport and Pharmacokinetics)
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Abstract

Catalposide, an active component of Veronica species such as Catalpa ovata and Pseudolysimachion lingifolium, exhibits anti-inflammatory, antinociceptic, anti-oxidant, hepatoprotective, and cytostatic activities. We characterized the in vitro metabolic pathways of catalposide to predict its pharmacokinetics. Catalposide was metabolized to catalposide sulfate (M1), 4-hydroxybenzoic acid (M2), 4-hydroxybenzoic acid glucuronide (M3), and catalposide glucuronide (M4) by human hepatocytes, liver S9 fractions, and intestinal microsomes. M1 formation from catalposide was catalyzed by sulfotransferases (SULTs) 1C4, SULT1A1*1, SULT1A1*2, and SULT1E1. Catalposide glucuronidation to M4 was catalyzed by gastrointestine-specific UDP-glucuronosyltransferases (UGTs) 1A8 and UGT1A10; M4 was not detected after incubation of catalposide with human liver preparations. Hydrolysis of catalposide to M2 was catalyzed by carboxylesterases (CESs) 1 and 2, and M2 was further metabolized to M3 by UGT1A6 and UGT1A9 enzymes. Catalposide was also metabolized in extrahepatic tissues; genetic polymorphisms of the carboxylesterase (CES), UDP-glucuronosyltransferase (UGT), and sulfotransferase (SULT) enzymes responsible for catalposide metabolism may cause inter-individual variability in terms of catalposide pharmacokinetics.
Keywords: catalposide; in vitro human metabolism; UDP-glucuronosyltransferase; sulfotransferase; carboxylesterase catalposide; in vitro human metabolism; UDP-glucuronosyltransferase; sulfotransferase; carboxylesterase
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MDPI and ACS Style

Hwang, D.-K.; Kim, J.-H.; Shin, Y.; Choi, W.-G.; Kim, S.; Cho, Y.-Y.; Lee, J.Y.; Kang, H.C.; Lee, H.S. Identification of Catalposide Metabolites in Human Liver and Intestinal Preparations and Characterization of the Relevant Sulfotransferase, UDP-glucuronosyltransferase, and Carboxylesterase Enzymes. Pharmaceutics 2019, 11, 355. https://doi.org/10.3390/pharmaceutics11070355

AMA Style

Hwang D-K, Kim J-H, Shin Y, Choi W-G, Kim S, Cho Y-Y, Lee JY, Kang HC, Lee HS. Identification of Catalposide Metabolites in Human Liver and Intestinal Preparations and Characterization of the Relevant Sulfotransferase, UDP-glucuronosyltransferase, and Carboxylesterase Enzymes. Pharmaceutics. 2019; 11(7):355. https://doi.org/10.3390/pharmaceutics11070355

Chicago/Turabian Style

Hwang, Deok-Kyu, Ju-Hyun Kim, Yongho Shin, Won-Gu Choi, Sunjoo Kim, Yong-Yeon Cho, Joo Young Lee, Han Chang Kang, and Hye Suk Lee. 2019. "Identification of Catalposide Metabolites in Human Liver and Intestinal Preparations and Characterization of the Relevant Sulfotransferase, UDP-glucuronosyltransferase, and Carboxylesterase Enzymes" Pharmaceutics 11, no. 7: 355. https://doi.org/10.3390/pharmaceutics11070355

APA Style

Hwang, D.-K., Kim, J.-H., Shin, Y., Choi, W.-G., Kim, S., Cho, Y.-Y., Lee, J. Y., Kang, H. C., & Lee, H. S. (2019). Identification of Catalposide Metabolites in Human Liver and Intestinal Preparations and Characterization of the Relevant Sulfotransferase, UDP-glucuronosyltransferase, and Carboxylesterase Enzymes. Pharmaceutics, 11(7), 355. https://doi.org/10.3390/pharmaceutics11070355

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