Abstract
This review aimed to provide a general view of catalpol in protection against diabetes and diabetic complications, as well as its pharmacokinetics and safety concerns. The following databases were consulted with the retrieval of more than 100 publications through June 2019: PubMed, Chinese National Knowledge Infrastructure, WanFang Data, and web of science. Catalpol exerts an anti-diabetic effect in different animal models with an oral dosage ranging from 2.5 to 200 mg/kg in rats and 10 to 200 mg/kg in mice. Besides, catalpol may prevent the development of diabetic complications in kidney, heart, central nervous system, and bone. The underlying mechanism may be associated with an inhibition of inflammation, oxidative stress, and apoptosis through modulation of various cellular signaling, such as AMPK/PI3K/Akt, PPAR/ACC, JNK/NF-κB, and AGE/RAGE/NOX4 signaling pathways, as well as PKCγ and Cav-1 expression. The pharmacokinetic profile reveals that catalpol could pass the blood-brain barrier and has a potential to be orally administrated. Taken together, catalpol is a well-tolerated natural compound with promising pharmacological actions in protection against diabetes and diabetic complications via multi-targets, offering a novel scaffold for the development of anti-diabetic drug candidate. Further prospective and well-designed clinical trials will shed light on the potential of clinical usage of catalpol.
Highlights
Catalpol is an iridoid glucoside widely found in plants belonging to several families of the order Lamiales, such as Plantaginaceae [1], Lamiaceae, and Bignoniaceae [2]
The results showed that the bioavailability of intramuscular injection was 71.63%, and that of oral administration was 49.38%, suggesting that catalpol is unstable in the gastrointestinal tract
The results showed that only mild non-fatal adverse events were found, indicate that catalpol is well-tolerated with no-toxicity in rodent animals and patients with colon such as nausea, vomiting, gastrointestinal ulcers, and constipation
Summary
Catalpol is an iridoid glucoside widely found in plants belonging to several families of the order Lamiales, such as Plantaginaceae [1], Lamiaceae, and Bignoniaceae [2]. Catalpol may assume the anti-diabetic action of Rehmannia glutinosa and has gained increasing attention for its potential contribution in controlling glycolipid metabolism and diabetic complications, making it a very promising scaffold for seeking new anti-diabetic drug candidate [7,8]. The current countermeasures for DM may run into bottlenecks for the potential persisting search for new drug candidates [12,13] For this purpose, we reviewed the current advances side effects,inwhich needs persisting searchand for diabetic new drug candidates [12,13]. We reviewed the current advances side effects,inwhich needs persisting searchand for diabetic new drug candidates [12,13] For this purpose, we of catalpol the management of diabetes complications, its pharmacokinetic profiles, reviewed the current advances of catalpol in the management of diabetes and diabetic complications, and safety concerns.
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