5th International Conference on Heart and Cardiovascular Diseases

Ulyana V Rozhkova graduated from Belarusian State University in 2011 with a degree in Chemistry, specializing in pharmacy. Since 2024, she has been working at the Research Institute of Atherosclerosis as a Clinical Trial Manager, particularly focusing on the dietary supplement Tertinat. From 2018 to 2023, she served as a Clinical Research Specialist at X7 Research, IQVIA, and Medpace, coordinating investigator teams in cardiology, endocrinology, oncology, conducting monitoring, and managing data for drug products like Kinezia®, Ferrum Lek®, Repatha®, and Vectibix®. Earlier roles include translator/editor (2012–2019) for companies such as Roche, GlaxoSmithKline, Novartis, and others, and Research Scientist at LOTIOS (2011–2018), where she developed and validated analytical methods (GC, HPLC, UV-spectrometry) and assisted in clinical trials for Gamastat® and Gamaferron®.

Background: Lipid accumulation, especially of cholesteryl esters, in the arterial intima is an early indicator of atherogenesis. Bloodstream LDL is the main lipid source, yet native LDL does not promote lipid accumulation in cultured cells, whereas modified LDL is markedly atherogenic. Oxidation is commonly held responsible, but recent findings indicate that desialylated rather than oxidized LDL is the crucial atherogenic variant in human plasma — vital for identifying correct pharmacological targets.

Objectives: Our aim was to develop a pharmacological strategy preventing LDL desialylation and slowing atherogenesis. Specific objectives were to identify potent sialidase inhibitors, to characterize the best candidate as a standardized formulation, to assess its effect on LDL sialic acid content clinically, and to evaluate sialyltransferase stimulation as a complementary mechanism.

Methodology: More than 60 compounds were screened in vitro for sialidase inhibition, measured as hydrolysis of 4MU-NANA with release of fluorescent 4MU. Epigallocatechin, available as the supplement Tertinat, was assessed in pilot studies. Patients were recruited from the cardiac surgery outpatient flow of the Moscow Regional Research and Clinical Institute. LDL was isolated by two-stage ultracentrifugation; sialic acid was determined colorimetrically; epigallocatechin in green tea extracts was quantified by HPLC; LDL atherogenicity was assessed as its ability to induce cholesterol accumulation in cultured THP-1 cells.

Key Results/Findings: Screening identified several potent inhibitors, epigallocatechin showing the highest efficacy and safety. Green tea extract contains up to 70% epigallocatechin and served as the basis for Tertinat. In pilot studies Tertinat significantly increased LDL sialic acid content, maintained over 12 months. Avicularin from Polygonum aviculare stimulates sialyltransferase, raising LDL sialic acid, and acts synergistically with epigallocatechin.

Conclusion: Sialidase inhibition and/or sialyltransferase stimulation is a promising therapeutic strategy for atherosclerotic cardiovascular disease. A multicenter, randomized, double-blind, placebo-controlled trial — Sialidase Inhibition as Antiatherosclerotic Therapy (SIAT) — has been initiated to evaluate Tertinat in preventing LDL modification and slowing atherogenesis.