Relative inhibitory activity of bile acids against 12-O-tetradecanoylphorbol-13-acetate-induced inflammation, and chenodeoxycholic acid inhibition of tumour promotion in mouse skin two-stage carcinogenesis

Abstract

This is the first report on the anti-inflammatory activity of bile acids on TPA-induced inflammatory ear oedema in mice. Chenodeoxycholic acid, methyl 3alpha,7alpha,15alpha-trihydroxy-5beta-cholan-24-oate and methyl 3alpha,7alpha,15beta-trihydroxy-5beta-cholan-24-oate showed the most potent activity, at a level corresponding to that of hydrocortisone. Furthermore, chenodeoxycholic acid markedly inhibited tumour promotion in a two-stage carcinogenesis model in mouse skin.

Structure-dependent inhibitory effects of synthetic cannabinoids against 12-O-tetradecanoylphorbol-13-acetate-induced inflammation and skin tumour promotion in mice

“…Table summarizes the inhibitory effects of the synthetic cannabinoids on TPA‐induced inflammation in mice. Most of the naphthoylindoles (compounds 1 – 3 , 5 – 8 , 10 , 11 , 13 and 14 ) inhibited the TPA‐induced inflammation, with an ID50 value of 168–675 n m /ear, more effective than indometacin (ID50 = 908 n m ) . Naphthoylindoles 9 and 12 were inactive.…”

“…The assay was conducted according to methods reported by Yasukawa et al . TPA (1 μg) was dissolved in acetone (20 μl) and applied (10 μl each) to the inner and outer surfaces of the right ear of ICR mice (7 weeks old, four mice per group) using a micropipette.…”

“…The test was conducted according to methods by Yasukawa et al . Skin carcinogenesis was initiated by topically applying 50 μg of DMBA to the back of each mouse (7 weeks old, 15 mice per group) and promoted by topically applying 1 μg TPA twice per week, from 1 week after the initiation up to the end of week 20.…”

Solvent-Free Synthesis of 2-Alkylbenzothiazoles and Bile Acid Derivatives Containing Benzothiazole Ring by Using Active Carbon/Silica Gel and Microwave

“…In a comparison with standard drugs, all compounds were more effective than indomethacin ID 50 908.2 nmol/ear , and 6b with a chenodeoxycholyl bile acid moiety was similar in activity to hydrocortisone ID 50 69.5 nmol/ear . Some authors have previously described the anti-inflammatory activity of cholic acid derivatives 35 . Almost all cholic acid derivatives containing a benzothiazole ring exhibited higher activity than their comparative free cholic acids.…”

The role of the bile acid chenodeoxycholic acid in the targeted oral delivery of the anti-diabetic drug gliclazide, and its applications in type 1 diabetes

“…CDCA has shown permeation-enhancing eff ects (Tsutsumi et al 2008) similar to many other BAs (Yang et al 2012). CDCA has also shown anti-infl ammatory eff ects (Yasukawa et al 2009, Chen et al 2000, Goyal et al 2015. ACM can be used to encapsulate G with CDCA to produce a targeted oral delivery system using a biodegradable and biocompatible polymer, such as sodium alginate (SA) (Mooranian et al 2014a, Negrulj et al 2015).…”