Therapeutic Potential of Orally Administered Rubiscolin-6.

Yusuke Karasawa, Kanako Miyano, Masahiro Yamaguchi, Miki Nonaka, Keisuke Yamaguchi, Masako Iseki, Izumi Kawagoe, Yasuhito Uezono

Journal: International journal of molecular sciences 2023;24(12):9959

PMID: 37373107

Abstract

["Rubiscolins are naturally occurring opioid peptides derived from the enzymatic digestion of the ribulose bisphosphate carboxylase\/oxygenase protein in spinach leaves. They are classified into two subtypes based on amino acid sequence, namely rubiscolin-5 and rubiscolin-6. In vitro studies have determined rubiscolins as G protein-biased delta-opioid receptor agonists, and in vivo studies have demonstrated that they exert several beneficial effects via the central nervous system. The most unique and attractive advantage of rubiscolin-6 over other oligopeptides is its oral availability. Therefore, it can be considered a promising candidate for the development of a novel and safe drug. In this review, we show the therapeutic potential of rubiscolin-6, mainly focusing on its effects when orally administered based on available evidence. Additionally, we present a hypothesis for the pharmacokinetics of rubiscolin-6, focusing on its absorption in the intestinal tract and ability to cross the blood-brain barrier."]
Address: Department of Pain Medicine, Juntendo University Graduate School of Medicine, Tokyo 113-8421, Japan.; Department of Pain Control Research, The Jikei University School of Medicine, Tokyo 105-8461, Japan.; Medical Affairs, Viatris Pharmaceuticals Japan Inc., Tokyo 105-0001, Japan.; Division of Cancer Pathophysiology, National Cancer Center Research Institute, Tokyo 104-0045, Japan.; Medical Affairs, Pfizer Japan Inc., Tokyo 151-8589, Japan.; Department of Anesthesiology and Pain Medicine, Faculty of Medicine, Juntendo University, Tokyo 113-8421, Japan.; Supportive and Palliative Care Research Support Office, National Cancer Center Hospital East, Chiba 277-8577, Japan.
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