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Planta Med 2021; 87(06): 498-506
DOI: 10.1055/a-1351-0618
Biological and Pharmacological Activity
Original Papers

Sulfation of Quercitrin, Epicatechin and Rutin by Human Cytosolic Sulfotransferases (SULTs): Differential Effects of SULT Genetic Polymorphisms

Xue Mei
1   Department of Pharmacology, College of Pharmacy and Pharmaceutical Sciences, University of Toledo Health Science Campus, Toledo, OH, USA
2   School of Pharmacy, Institute of Material Medica, North Sichuan Medical College, Nanchong, Sichuan, China
,
Saud A. Gohal
1   Department of Pharmacology, College of Pharmacy and Pharmaceutical Sciences, University of Toledo Health Science Campus, Toledo, OH, USA
,
Eid S. Alatwi
1   Department of Pharmacology, College of Pharmacy and Pharmaceutical Sciences, University of Toledo Health Science Campus, Toledo, OH, USA
,
Ying Hui
1   Department of Pharmacology, College of Pharmacy and Pharmaceutical Sciences, University of Toledo Health Science Campus, Toledo, OH, USA
3   Department of Obstetrics and Gynecology, Beijing Hospital, Beijing, China
,
Chunyan Yang
2   School of Pharmacy, Institute of Material Medica, North Sichuan Medical College, Nanchong, Sichuan, China
,
Yongyan Song
4   School of Basic Medical Science, North Sichuan Medical College, Nanchong, Sichuan, China
,
Chunyang Zhou
2   School of Pharmacy, Institute of Material Medica, North Sichuan Medical College, Nanchong, Sichuan, China
,
Ming-Cheh Liu
1   Department of Pharmacology, College of Pharmacy and Pharmaceutical Sciences, University of Toledo Health Science Campus, Toledo, OH, USA
› Author AffiliationsSupported by: China Scholarship Council 18SXHZ0250
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Abstract

Radix Bupleuri is one of the most widely used herbal medicines in China for the treatment of fever, pain, and/or chronic inflammation. Quercitrin, epicatechin, and rutin, the flavonoids present in Radix Bupleuri, have been reported to display anti-inflammatory, antitumor, and antioxidant biological activities among others. Sulfation has been reported to play an important role in the metabolism of flavonoids. In this study, we aimed to systematically identify the human cytosolic sulfotransferase enzymes that are capable of catalyzing the sulfation of quercitrin, epicatechin, and rutin. Of the thirteen known human cytosolic sulfotransferases, three (cytosolic sulfotransferase 1A1, cytosolic sulfotransferase 1C2, and cytosolic sulfotransferase 1C4) displayed sulfating activity toward quercitrin, three (cytosolic sulfotransferase 1A1, cytosolic sulfotransferase 1A3, and cytosolic sulfotransferase 1C4) displayed sulfating activity toward epicatechin, and six (cytosolic sulfotransferase 1A1, cytosolic sulfotransferase 1A2, cytosolic sulfotransferase 1A3, cytosolic sulfotransferase 1B1, cytosolic sulfotransferase 1C4, and cytosolic sulfotransferase 1E1) displayed sulfating activity toward rutin. The kinetic parameters of the cytosolic sulfotransferases that showed the strongest sulfating activities were determined. To investigate the effects of genetic polymorphisms on the sulfation of quercitrin, epicatechin, and rutin, individual panels of cytosolic sulfotransferase allozymes previously prepared were analyzed and shown to display differential sulfating activities toward each of the three flavonoids. Taken together, these results provided a biochemical basis underlying the metabolism of quercitrin, epicatechin, and rutin through sulfation in humans.

Key words

Bupleurum scorzonerifolium - Apiaceae - quercitrin - epicatechin - rutin - sulfation - cytosolic sulfotransferase - SULT - single nucleotide polymorphism - SNP


Publication History

Received: 08 July 2020

Accepted after revision: 01 January 2021

Article published online:
11 February 2021

© 2021. Thieme. All rights reserved.

Georg Thieme Verlag KG
Rüdigerstraße 14, 70469 Stuttgart, Germany

 

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