MONO, DI AND TRIKETO DERIVATIVES OF CHOLIC ACID AND THEIR HYPOGLYCEMIC EFFECTS
Journal Title: World Journal of Pharmaceutical and life sciences - Year 2018, Vol 4, Issue 4
Abstract
Bile acids are amphiphilic molecules, which consist of a hydrophobic and a rigid steroid nucleus to which they are attached a hydrophilic hydroxyl groups, as well as flexible aliphatic acid side chain. The number, position and orientation of hydroxyl groups in the bile acid molecules may vary. The steroidal core of bile acids constitutes a saturated cyclopentanoperhydrophenanthrene hydrocarbon skeleton, consisting of three six-member (A, B, C) and one five-membered ring (D). Natural bile acids are derivatives of 5β-cholanic acid, wherein A and B rings are cislinked. The planar structure of amphiphilic bile acid, or the existence of a hydrophilic and hydrophobic surface molecule affects its physico-chemical characteristics and the ability to self-aggregation conditions. Monoketo derivatives of bile acids facilitate the permeability of the membrane. It has been shown that the 3α,7α−dihydroxy−12−keto−5β−cholanic acid exhibits hypoglycemic effect in diabetes type 1. Better effects are noted if mentioned 3α,7α−dihydroxy−12−keto−5β−cholanic acid is used in combination with hypoglycemic gliclazide or preparate of stevioside. The best effect in glycemic control was achieved when rats with type 1 diabetes were pretreated with probiotics, and then simultaneously with the use of a derivative of 3α,7α−dihydroxy−12−keto−5β−cholanic acid and gliclazide. The latest studies of diabetes in rodents in experimental models have shown that synthetic derivatives such as sodium 3α,7 −dihydroxy−12−keto−5β−cholanate results in the reduction of blood glucose concentration, which is the concentration reached 54% of that obtained following subcutaneous administration of the same dose of insulin. The aim of this paper is to explain the synthesis of various mono, di and tri keto derivatives of cholic acid, as well as to analyze the discovery of the association between bile acids (the most of 3α,7α−dihydroxy−12−keto−5β−cholanic acid) and glucose regulation, which gives us a new perspective in the design of hypoglycemic drugs in the treatment of diabetes.
Authors and Affiliations
Tanja Šarenac
Keywords
Related Articles
- EP ID EP655408
- DOI -
- Views 130
- Downloads 0
SINGLE VISIT ENDODONTIC THERAPY: A REVIEW
Successful endodontic treatment depends upon localization, proper chemo-mechanical preparation of the root canal system, debridement, shaping, disinfection, and three dimensional obturation of canal system. Thus multiple...
RICE BRAN - A WONDERFUL SOURCE OF MEDICINAL PROPERTIES
Rice bran is the cuticle existing between the rice and the husk of the paddy. It is obtained as a by-product of the rice milling process. Since the milling process has been known to remove much of the vitamins and minera...
A CONCEPTUAL STUDY OF PANDU ROGA AND ROLE OF DARVYADI LAUHA AND VASADI KASHAYA IN ITS MANAGEMENT- A REVIEW ARTICLE
Ayurveda is the science of life which focuses on maintenance of positive health in healthy and eradication of ailments in diseased through its holistic approach, lifestyle practices, dietary habits and safer medications....
ANTI-INFLAMMATORY ACTIVITY OF ETHANOLIC EXTRACT OF LEAVES BRYOPHYLLUM PINNATUM LINN
The present study is carried out to investigate the anti-inflammatory potential of Ethanolic extract of Bryophyllum pinnatum. Anti-inflammatory activity was evaluated by using Egg Albumin, Turpentine Oil & Formaldehyde a...
RUSSIAN GMP INSPECTION. USER’S MANUAL
Development of pharmaceutical industry in Russia requires for a common approach to the qualification and standardization of manufacturing process for drug products. To achieve this goal the package of relevant legal Acts...