Oleandrin: A Systematic Review of its Natural Sources, Structural Properties, Detection Methods, Pharmacokinetics and Toxicology

Abstract

Oleandrin is a highly lipid-soluble cardiac glycoside isolated from the plant Nerium oleander (Apocynaceae) and is used as a traditional herbal medicine due to its excellent pharmacological properties. It is widely applied for various disease treatments, such as congestive heart failure. Recently, oleandrin has attracted widespread attention due to its extensive anti-cancer and novel anti-viral effects. However, oleandrin has a narrow therapeutic window and exhibits various toxicities, especially typical cardiotoxicity, which is often fatal. This severe toxicity and low polarity have significantly hindered its application in the clinic. This review describes natural sources, structural properties, and detection methods of oleandrin. Based on reported poisoning cases and sporadic animal experiments, the pharmacokinetic characteristics of oleandrin are summarized, so as to infer some possible phenomena, such as enterohepatic circulation. Moreover, the relevant factors affecting the pharmacokinetics of oleandrin are analyzed, and some research approaches that may ameliorate the pharmacokinetic behavior of oleandrin are proposed. With the toxicology of oleandrin being thoroughly reviewed, the development of safe clinical applications of oleandrin may be possible given potential research strategies to decrease toxicity.

Discovery of senolytics using machine learning

“…Further validation on animal models may strengthen the evidence for oleandrin as a promising new senolytic. A caveat, however, is that cardiac glycosides that have been employed in heart conditions have severe limitations due to toxicity 76 , and our results suggest that oleandrin is not an exception because of its narrow therapeutic range and cardiotoxicity, and hence its use as systemic senolytic should be considered cautiously. The high potency of oleandrin could potentially benefit senolytic therapies administered locally on the site of damage; clinical trials are currently assessing such local administration of senolytics for osteoarthritis 10 , 77 .…”

“…From a translational point of view, we highlight that the three senolytics identified in this study are natural products found in traditional herbal medicines: Ginkgo biloba (ginkgetin) 79 Nerium oleander (oleandrin) 76 and Periploca sepium (periplocin) 80 . Oleandrin and periplocin belong to the group of cardenolide glycosides, which are highly potent cardioactive agents, while ginkgetin is a biflavone with a broad pharmacological spectrum.…”

Streptomyces sp. Strain PBR11, a Forest-Derived Soil Actinomycetia with Antimicrobial Potential

“…Campestanol ( 83 ), SM(d18:0/0:0) ( 84 ), ethoxyquin ( 85 , 86 ), phendimetrazine ( 87 ), 10-deoxymethymycin ( 88 ), anandamide (20:2, n -6) ( 89 ), and miltefosine ( 90 ) have hypocholesterolemic, cell signaling, antioxidant, anticarcinogenic, anorexigenic, antibacterial, fatty acid neurotransmitter, and antileishmanial effects, while no bioactivity has been reported for 11-amino-undecanoic acid, d -pantetheine 4′-phosphate, and 3-hydroxytetradecanedioic acid. The biologically active compounds diethylcarbamazine, acetylsalicylic acid (aspirin), 2-propyl-9 Z -octadecenoic acid, and oleandrin ( 72 , 91 – 95 ) detected in the bioactive fraction of PBR11Fr-2 exhibited anti-inflammatory effects, nonsteroidal anti-inflammatory action, antiplasmodial activity, anticancer effects, novel antiviral activity, and anorexigenic effects. However, there is no bioactivity reported for 12,14-pentacosadiynoic.…”

Detection of Highly Poisonous Nerium oleander Using Quantitative Real-Time PCR with Specific Primers

“…Previous studies have verified that oleander can be quickly absorbed in the gastrointestinal tract and results in immediately toxic effects after oral administration [3]. The stomach contents from patients or the dead could be suitable for determining oleander poisoning [22].…”

“…Nerium oleander, also known as oleander, is a highly toxic shrub with beautiful flowers. The presence of various cardiac glycosides in all the parts of the oleander plant are the main toxins that cause acute cardiotoxicity [2,3]. Trace consumption of oleander is enough to trigger dizziness, emesis, diarrhea, arrhythmia, and even death.…”