Bile acids, the endogenous steroid
nucleus containing signaling
molecules, are responsible for the regulation of multiple metabolic
processes, including lipoprotein and glucose metabolism to maintain
homeostasis. Within our body, they are directly produced from their
immediate precursors, cholesterol C (low-density lipoprotein C, LDL-C),
through the enzymatic catabolic process mediated by 7-α-hydroxylase
(CYP7A1). Bile acid sequestrants (BASs) or amphiphilic resins that
are nonabsorbable to the human body (being complex high molecular
weight polymers/electrolytes) are one of the classes of drugs used
to treat hypercholesterolemia (a high plasma cholesterol level) or
dyslipidemia (lipid abnormalities in the body); thus, they have been
used clinically for more than 50 years with strong safety profiles
as demonstrated by the Lipid Research Council–Cardiovascular
Primary Prevention Trial (LRC–CPPT). They reduce plasma LDL-C
and can slightly increase high-density lipoprotein C (HDL-C) levels,
whereas many of the recent clinical studies have demonstrated that
they can reduce glucose levels in patients with type 2 diabetes mellitus
(T2DM). However, due to higher daily dosage requirements, lower efficacy
in LDL-C reduction, and concomitant drug malabsorption, research to
develop an “ideal” BAS from sustainable or natural sources
with better LDL-C lowering efficacy and glucose regulations and lower
side effects is being pursued. This Review discusses some recent developments
and their corresponding efficacies as bile removal or LDL-C reduction
of natural biopolymer (polysaccharide)-based compounds.