Abstract
Cardiovascular disorders (CVDs) are the leading risk factor for death worldwide, and research into the processes and treatment regimens has received a lot of attention. Tilianin is a flavonoid glycoside that can be found in a wide range of medicinal plants and is most commonly obtained from Dracocephalum moldavica. Due to its extensive range of biological actions, it has become a well-known molecule in recent years. In particular, numerous studies have shown that tilianin has cardioprotective properties against CVDs. Hence, this review summarises tilianin’s preclinical research in CVDs, as well as its mechanism of action and opportunities in future drug development. The physicochemical and drug-likeness properties, as well as the toxicity profile, were also highlighted. Tilianin can be a natural lead molecule in the therapy of CVDs such as coronary heart disease, angina pectoris, hypertension, and myocardial ischemia, according to scientific evidence. Free radical scavenging, inflammation control, mitochondrial function regulation, and related signalling pathways are all thought to play a role in tilianin’s cardioprotective actions. Finally, we discuss tilianin-derived compounds, as well as the limitations and opportunities of using tilianin as a lead molecule in drug development for CVDs. Overall, the scientific evidence presented in this review supports that tilianin and its derivatives could be used as a lead molecule in CVD drug development initiatives.
Highlights
The circulatory system, known as the cardiovascular system, is the organ system that distributes blood to and from all regions of the body through vessels
Shen et al [29] investigated the anti-atherosclerotic mechanism of tilianin by developing in vitro models with macrophages, vascular smooth muscle cells (VSMC) and human umbilical vein endothelial cells, all of which contribute to atherosclerosis progression
Nanoparticles in drug delivery such as polylactic-co-glycolic acid (PLGA), polyethylene glycol (PEG), liposomal delivery methods, and RNA-based delivery have various advantages, including: (1) enhanced adsorption; (2) selective targeting; (3) simple encapsulation (4) an increase in bioavailability; (5) decrease in adverse effects and (6) enhanced stability for Cardiovascular disorders (CVDs) [59,60,61]. These new delivery systems provide a number of approaches for achieving tissue selectivity and reducing system exposure, which are both necessary for deploying new pharmacological compounds derived from tilianin for improved CVD treatment (Figure 9)
Summary
The circulatory system, known as the cardiovascular system, is the organ system that distributes blood to and from all regions of the body through vessels. Researchers are intrigued by the prospect of finding novel biologically active compounds in natural products, in herbs, for the treatment of diseases, especially CVD. Tilianin (acacetin-7-glucoside) is an active flavonoid glycoside (Figure 1) obtained from numerous medicinal plants and especially from Dracocephalum moldavica It is found in various common medicinal herbal plants including Agastache Mexicana, Agastache rugosa, Dracocephalum moldavia, Dracocephalum tanguticum, Dracocephalum moldavica, Lygodium japonicum and Discocleidion rufescens [10,11]. Scientific evidence clearly indicated that tilianin is a potential natural compound against CVDs such as atherosclerosis, coronary heart disease, angina pectoris, hypertension and myocardial ischemia (Figure 2). We discuss tilianin-derived molecules, as well as the limitations and possible opportunities of using tilianin as a lead molecule in the drug development for CVDs
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