Oridonin: A Review of Its Pharmacology, Pharmacokinetics and Toxicity

Abstract

Oridonin, as a natural terpenoids found in traditional Chinese herbal medicine Isodon rubescens (Hemsl.) H.Hara, is widely present in numerous Chinese medicine preparations. The purpose of this review focuses on providing the latest and comprehensive information on the pharmacology, pharmacokinetics and toxicity of oridonin, to excavate the therapeutic potential and explore promising ways to balance toxicity and efficacy of this natural compound. Information concerning oridonin was systematically collected from the authoritative internet database of PubMed, Elsevier, Web of Science, Wiley Online Library and Europe PMC applying a combination of keywords involving “pharmacology,” “pharmacokinetics,” and “toxicology”. New evidence shows that oridonin possesses a wide range of pharmacological properties, including anticancer, anti-inflammatory, hepatorenal activities as well as cardioprotective protective activities and so on. Although significant advancement has been witnessed in this field, some basic and intricate issues still exist such as the specific mechanism of oridonin against related diseases not being clear. Moreover, several lines of evidence indicated that oridonin may exhibit adverse effects, even toxicity under specific circumstances, which sparked intense debate and concern about security of oridonin. Based on the current progress, future research directions should emphasize on 1) investigating the interrelationship between concentration and pharmacological effects as well as toxicity, 2) reducing pharmacological toxicity, and 3) modifying the structure of oridonin—one of the pivotal approaches to strengthen pharmacological activity and bioavailability. We hope that this review can provide some inspiration for the research of oridonin in the future.

Oridonin Attenuates Cisplatin-Induced Acute Kidney Injury via Inhibiting Oxidative Stress, Apoptosis, and Inflammation in Mice

“…Importantly, various natural compounds have antioxidative activity [ 31 , 32 ]. Antioxidative effect of oridonin has also been reported in several studies [ 8 , 9 ]. Oridonin suppressed reactive oxygen species generation in lipopolysaccharide- (LPS-) treated human renal tubular epithelial cells [ 33 ].…”

“…Indeed, oridonin has been shown to exert anticancer activity on many types of cancers [ 21 – 23 ]. However, subsequent studies suggest that in addition to its anticancer effect, oridonin has several other favorable effects including antioxidative and anti-inflammatory effects [ 8 , 9 ]. Therefore, we hypothesized that oridonin may have a beneficial effect on cisplatin nephrotoxicity.…”

“…Oridonin has broad potential for drug development due to its wide range of pharmacological activities [ 8 , 52 ]. However, oridonin has low solubility and poor bioavailability, which limits its clinical application.…”

Jatrorrhizine: A Review of Sources, Pharmacology, Pharmacokinetics and Toxicity

“…Toxicity and safety are critical for the assessment of clinical applications of natural products ( Li et al, 2021 ). Jatrorrhizine is a bioactive metabolite in some commonly used medicinal plants and has been used for centuries in traditional medicine.…”

A Review of Twenty Years of Research on the Regulation of Signaling Pathways by Natural Products in Breast Cancer

“…Cimigenoside, a novel natural compound isolated from C. dahurica , also inhibited the release of gamma–secretase from the transmembrane region by inhibiting their catalytic core PSEN-1, ultimately inhibiting the binding of NICD to CSL, and thus marinating the regulation of the Notch pathway. Cimigenoside showed its usefulness by inducing apoptosis and inhibiting Bcl-2, which ultimately then inhibited the Notch pathway [ 23 , 88 , 89 ].…”