TY - JOUR
T1 - Assessment of hypolipidaemic activity of three thiazolidin-4-ones in mice given high-fat diet and fructose
AU - Nampurath, Gopalan Kutty
AU - Mathew, Suma P.
AU - Khanna, Vivek
AU - Zachariah, Robby T.
AU - Kanji, Suman
AU - Chamallamudi, Mallikarjuna Rao
PY - 2008/2/15
Y1 - 2008/2/15
N2 - Three 4-thiazolidinones, two with nicotinamide (NAT1 and NAT2) and one with 4-chlorophenoxyacetamide (PAT1) side chains were evaluated for their hypolipidaemic, hypoglycaemic activity in Swiss albino mice fed a high-fat diet along with fructose administered in drinking water. NAT1 and PAT caused reduction of elevated triglycerides, cholesterol and glucose; NAT2 was effective only against triglycerides. Nicotinamide side chain might have contributed to the lipid lowering effect of both NAT1 and NAT2, but the bulky group of the latter could have affected proper binding to the receptor sites, making it ineffective against elevated cholesterol. On the other hand, the 4-chlorophenoxyacetamide side chain of PAT might have exerted powerful hypolipidaemic activity, despite the bulky substitution at C2. As antioxidants, NAT2 and PAT1 showed superior activity, compared to NAT1. The thiazolidinone ring might be responsible for the lipid lowering effect, which is however, modified by the type of substitutions at C2 and N of the ring. Detailed study is warranted to explain the mechanism of action of these compounds as also to make more potent ones.
AB - Three 4-thiazolidinones, two with nicotinamide (NAT1 and NAT2) and one with 4-chlorophenoxyacetamide (PAT1) side chains were evaluated for their hypolipidaemic, hypoglycaemic activity in Swiss albino mice fed a high-fat diet along with fructose administered in drinking water. NAT1 and PAT caused reduction of elevated triglycerides, cholesterol and glucose; NAT2 was effective only against triglycerides. Nicotinamide side chain might have contributed to the lipid lowering effect of both NAT1 and NAT2, but the bulky group of the latter could have affected proper binding to the receptor sites, making it ineffective against elevated cholesterol. On the other hand, the 4-chlorophenoxyacetamide side chain of PAT might have exerted powerful hypolipidaemic activity, despite the bulky substitution at C2. As antioxidants, NAT2 and PAT1 showed superior activity, compared to NAT1. The thiazolidinone ring might be responsible for the lipid lowering effect, which is however, modified by the type of substitutions at C2 and N of the ring. Detailed study is warranted to explain the mechanism of action of these compounds as also to make more potent ones.
UR - http://www.scopus.com/inward/record.url?scp=38549086049&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=38549086049&partnerID=8YFLogxK
U2 - 10.1016/j.cbi.2007.10.006
DO - 10.1016/j.cbi.2007.10.006
M3 - Article
C2 - 18053977
AN - SCOPUS:38549086049
SN - 0009-2797
VL - 171
SP - 363
EP - 368
JO - Chemico-Biological Interactions
JF - Chemico-Biological Interactions
IS - 3
ER -