Molecular Mechanisms of Action of Emodin: As an Anti-Cardiovascular Disease Drug

Abstract

Emodin is a natural occurring anthraquinone derivative isolated from roots and barks of numerous plants, molds, and lichens. It is found to be an active ingredient in different Chinese herbs including Rheum palmatum and Polygonam multiflorum, and it is a pleiotropic molecule with diuretic, vasorelaxant, anti-bacterial, anti-viral, antiulcerogenic, anti-inflammatory, and anti-cancer effects. Moreover, emodin has also been shown to have a wide activity of anti-cardiovascular diseases. It is mainly involved in multiple molecular targets such as inflammatory, anti-apoptosis, anti-hypertrophy, antifibrosis, anti-oxidative damage, abnormal, and excessive proliferation of smooth muscle cells in cardiovascular diseases. As a new type of cardiovascular disease treatment drug, emodin has broad application prospects. However, a large amount of evidences detailing the effect of emodin on many signaling pathways and cellular functions in cardiovascular disease, the overall understanding of its mechanisms of action remains elusive. In addition, by describing the evidence of the effects of emodin in detail, the toxicity and poor oral bioavailability of mice have been continuously discovered. This review aims to describe a timely overview of emodin related to the treatment of cardiovascular disease. The emphasis is to summarize the pharmacological effects of emodin as an anticardiovascular drug, as well as the targets and its potential mechanisms. Furthermore, the treatment of emodin compared with conventional cardiovascular drugs or target inhibitors, the toxicity, pharmacokinetics and derivatives of emodin were discussed.

Phylobioactive hotspots in plant resources used to treat Chagas disease

“…Moreover, benznidazole emodin combinations may be tested for potential synergistic antichagasic effects in vivo. However, as reviewed recently, emodin shows relatively low oral bioavailability in rodents (5-10%) (Li et al, 2020). As some anthraquinones did not inhibit T. cruzi epimastigote proliferation in our study (Table 5), their antichagasic effects in the infection/parasite release assays may be due to host cell ROS generation induced by these compounds.…”

Advances in Research on Chemical Constituents and Their Biological Activities of the Genus Actinidia

“…Lipoxygenases (LOXs) are potential treatment targets in a variety of inflammatory conditions, enzyme kinetics showed that aloe emodin inhibited lipoxygenase competitively with an IC 50 of 29.49 μM [126]. Compound 215 was reported to possess wide biological activities including anti-inflammatory, neuroprotection, anti-cardiovascular and α-glucosidase inhibitory activity [129][130][131][132]. It exhibited potent inhibition of α-glucosidase with an IC 50 value of 19 ± 1 μM and lower cytotoxicity to the Caco-2 cell line [132].…”

Natural Products and Their Derivatives against Human Herpesvirus Infection

“…Anthraquinones are a class of aromatic compounds demonstrating a broad spectrum of bioactivities. Emodin (32) and aloe-emodin (33) are active ingredients in different Chinese herbs including Aloe vera, Cassia occidentalis, Rheum palmatum, and Polygonam multiflorumto and possesses broad pharmacological effects, such as antibacterial, antiviral, antiinflammatory, anticancer, neuroprotective, hepatoprotective, and anticardiovascular effects [134][135][136][137][138][139]176,177]. At a concentration of 50 µg/mL, 32 inhibited HSV-1 and 2 in Hep-2 cells with antiviral indices of 2.07 and 3.53, respectively, and the compound with equivalent antiviral efficacy to acyclovir also increased the survival rate and time of HSVinfected mice with higher efficacy in eliminating HSV-infected brain, heart, liver, and ganglion compared to the viral control [135].…”