In vitro hepatic biotransformation of the algal toxin pectenotoxin-2

We have investigated the in vitro metabolism of pectenotoxin-2 (PTX-2) using primary hepatocytes from Wistar rats in suspension. Purified PTX-2 was rapidly metabolized. Two major and several minor oxidized PTX-2 metabolites were formed, none of which had retention times corresponding to PTX-1, -11,...

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Chi tiết về thư mục
Những tác giả chính: Morten Sandvik, Christopher O. Miles, Alistair L. Wilkins, Christiane Fæste
Định dạng: Bài viết
Ngôn ngữ:English
Được phát hành: Elsevier 2020-06-01
Loạt:Toxicon: X
Truy cập trực tuyến:http://www.sciencedirect.com/science/article/pii/S2590171020300096
Miêu tả
Tóm tắt:We have investigated the in vitro metabolism of pectenotoxin-2 (PTX-2) using primary hepatocytes from Wistar rats in suspension. Purified PTX-2 was rapidly metabolized. Two major and several minor oxidized PTX-2 metabolites were formed, none of which had retention times corresponding to PTX-1, -11, or −13. Hydrolysis products, such as PTX-2 seco acid, were not observed. Preliminary multi-stage LC-MS analyses indicated that the major hepatic PTX-2 metabolites resulted from the insertion of an oxygen atom at the positions C-19 to C-24, or at C-44. The rapid oxidative metabolism may explain the low oral toxicity of PTXs observed in vivo studies.
số ISSN:2590-1710