PMID- 35333534 OWN - NLM STAT- MEDLINE DCOM- 20220503 LR - 20220509 IS - 1543-8392 (Electronic) IS - 1543-8384 (Linking) VI - 19 IP - 5 DP - 2022 May 2 TI - Bile Acid Sequestrants for Hypercholesterolemia Treatment Using Sustainable Biopolymers: Recent Advances and Future Perspectives. PG - 1248-1272 LID - 10.1021/acs.molpharmaceut.2c00007 [doi] AB - 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-alpha-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. FAU - Islam, Muhammad Shahidul AU - Islam MS AD - Department of Chemical Engineering, Waterloo Institute for Nanotechnology, University of Waterloo, 200 University Avenue West, Waterloo, Ontario N2L 3G1, Canada. FAU - Sharif, Anjiya AU - Sharif A AD - Department of Chemical Engineering, Waterloo Institute for Nanotechnology, University of Waterloo, 200 University Avenue West, Waterloo, Ontario N2L 3G1, Canada. FAU - Kwan, Nathania AU - Kwan N AD - Department of Chemical Engineering, Waterloo Institute for Nanotechnology, University of Waterloo, 200 University Avenue West, Waterloo, Ontario N2L 3G1, Canada. FAU - Tam, Kam C AU - Tam KC AUID- ORCID: 0000-0002-7603-5635 AD - Department of Chemical Engineering, Waterloo Institute for Nanotechnology, University of Waterloo, 200 University Avenue West, Waterloo, Ontario N2L 3G1, Canada. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Review DEP - 20220325 PL - United States TA - Mol Pharm JT - Molecular pharmaceutics JID - 101197791 RN - 0 (Anticholesteremic Agents) RN - 0 (Bile Acids and Salts) RN - 0 (Biopolymers) RN - 0 (Cholesterol, LDL) RN - 0 (Hypolipidemic Agents) RN - 97C5T2UQ7J (Cholesterol) RN - IY9XDZ35W2 (Glucose) SB - IM MH - *Anticholesteremic Agents/therapeutic use MH - Bile Acids and Salts/therapeutic use MH - Biopolymers MH - Cholesterol MH - Cholesterol, LDL/therapeutic use MH - *Diabetes Mellitus, Type 2/drug therapy/metabolism MH - Glucose/therapeutic use MH - Humans MH - *Hypercholesterolemia/drug therapy MH - Hypolipidemic Agents/therapeutic use OTO - NOTNLM OT - LDL-C OT - amphiphilic OT - bile acid sequestrants OT - bile metabolism OT - biopolymer OT - dextran OT - dyslipidemia OT - glucose regulation OT - lipid-lowering EDAT- 2022/03/26 06:00 MHDA- 2022/05/04 06:00 CRDT- 2022/03/25 17:17 PHST- 2022/03/26 06:00 [pubmed] PHST- 2022/05/04 06:00 [medline] PHST- 2022/03/25 17:17 [entrez] AID - 10.1021/acs.molpharmaceut.2c00007 [doi] PST - ppublish SO - Mol Pharm. 2022 May 2;19(5):1248-1272. doi: 10.1021/acs.molpharmaceut.2c00007. Epub 2022 Mar 25.