Haemolytic activity of formyl- and acetyl-derivatives of bile acids and their gramine salts.

作者: Weronika Kozanecka-Okupnik , Beata Jasiewicz , Tomasz Pospieszny , Monika Matuszak , Lucyna Mrówczyńska

DOI: 10.1016/J.STEROIDS.2017.07.003

关键词:

摘要: Bile acids (lithocholic: LCA, deoxycholic: DCA and cholic: CA) their formyl- acetyl-derivatives can be used as starting material in chemical synthesis of compounds with different biological activity strongly depended on structures. Our previous studies showed that bile salts gramine toward human erythrocytes was significantly from the alone. Moreover, effectively modified membrane perturbing other steroids. As a continuation our work, haemolytic acetyl-substituet well studied vitro. The structures new were confirmed by spectral (NMR, FT-IR) analysis, mass spectrometry (ESI-MS) PM5 semiempirical methods. results shown acetyl-LCA higher comparison native forms at whole concentration range. At high concentration, formyl derivative CA effective LCA derivatives whereas lower its level original acid. acetyl-CA not active agents. Furthermore, decreased membrane-perturbing hydrophobic derivatives. obtained cellular system are line physicochemical calculation.

参考文章(30)
Uday Maitra, Samrat Mukhopadhyay, Chemistry and biology of bile acids Current Science. ,vol. 87, pp. 1666- 1683 ,(2004)
A F Hofmann, Bile acids as drugs: principles, mechanisms of action and formulations The Italian journal of gastroenterology. ,vol. 27, pp. 106- 113 ,(1995)
Patrícia GG Do Nascimento, Telma LG Lemos, Macia CS Almeida, Juliana MO De Souza, Ayla MC Bizerra, Gilvandete MP Santiago, José GM Da Costa, Henrique DM Coutinho, None, Lithocholic acid and derivatives: Antibacterial activity Steroids. ,vol. 104, pp. 8- 15 ,(2015) , 10.1016/J.STEROIDS.2015.07.007
Thomas Pusl, Ursodeoxycholic acid treatment of vanishing bile duct syndromes World Journal of Gastroenterology. ,vol. 12, pp. 3487- 3495 ,(2006) , 10.3748/WJG.V12.I22.3487
Laura K. Chico, Linda J. Van Eldik, D. Martin Watterson, Targeting protein kinases in central nervous system disorders Nature Reviews Drug Discovery. ,vol. 8, pp. 892- 909 ,(2009) , 10.1038/NRD2999
L Mrówczyńska, J Bielawski, The mechanism of bile salt-induced hemolysis. Cellular & Molecular Biology Letters. ,vol. 6, pp. 881- 895 ,(2001)
Akiyoshi Horie, Miho Akimoto, Hiroto Tsumura, Makoto Makishima, Takeshi Taketani, Seiji Yamaguchi, Yoshio Honma, Induction of differentiation of myeloid leukemia cells in primary culture in response to lithocholic acid acetate, a bile acid derivative, and cooperative effects with another differentiation inducer, cotylenin A Leukemia Research. ,vol. 32, pp. 1112- 1123 ,(2008) , 10.1016/J.LEUKRES.2007.12.004
Ryutaro Adachi, Yoshio Honma, Hiroyuki Masuno, Katsuyoshi Kawana, Iichiro Shimomura, Sachiko Yamada, Makoto Makishima, Selective activation of vitamin D receptor by lithocholic acid acetate, a bile acid derivative Journal of Lipid Research. ,vol. 46, pp. 46- 57 ,(2005) , 10.1194/JLR.M400294-JLR200