Pharmacokinetics and Pharmacological Activities of Berberine in Diabetes Mellitus Treatment

Abstract

Traditional Chinese medicine (TCM) has good clinical application prospects in diabetes treatment. In addition, TCM is less toxic and/or has fewer side effects and provides various therapeutic effects. Berberine (BBR) is isolated as the main component in many TCM kinds (e.g., Rhizoma Coptidis and Berberidis Cortex). Furthermore, BBR can reduce blood sugar and blood fat, alleviate inflammation, and improve the state of patients. Based on the recent study results of BBR in diabetes treatment, the BBR pharmacokinetics and mechanism on diabetes are mainly studied, and the specific molecular mechanism of related experimental BBR is systematically summarized and analyzed. Clinical studies have proved that BBR has a good therapeutic effect on diabetes, suggesting that BBR may be a promising drug candidate for diabetes. More detailed BBR mechanisms and pathways of BBR need to be studied further in depth, which will help understand the BBR pharmacology in diabetes treatment.

Research Progress in the Pharmacological Activities, Toxicities, and Pharmacokinetics of Sophoridine and Its Derivatives

“…Berberine is widely used to treat diabetes mellitus, and its mechanism probably consists of inhibiting hepatic gluconeogenesis and inducing hyperglycolysis and insulin sensitivity. 124 On the other hand, sophoridine is the focus of anti-tumor research, particularly malignant trophoblastic tumors. Many experimental studies have confirmed that berberine is metabolized rapidly in vivo, primarily by the liver and intestinal flora, and its content and structure change after metabolism.…”

“…Many experimental studies have confirmed that berberine is metabolized rapidly in vivo, primarily by the liver and intestinal flora, and its content and structure change after metabolism. 124 In contrast, research shows that sophoridine is metabolized primarily through urine excretion as a prototype of the human kidney. 8 , 98 Still, the difference in LD 50 between sophoridine and berberine (65.19 vs 57.6 mg/kg) by intraperitoneal injection is miniscule.…”

Berberine: A Review of its Pharmacokinetics Properties and Therapeutic Potentials in Diverse Vascular Diseases

“…Berberine exerts superior therapeutical effects on the vascular diseases, such as atherosclerosis; however, its effects are limited in clinic due to poor oral absorption and low bioavailability ( Han et al, 2021b ). Previous research has reported that the absolute bioavailability of berberine is 0.37% when administered in a single oral administration (48.2, 120, or 240 mg/kg body weight) in rats ( Feng et al, 2021 ).…”

“…However, due to its low in vivo bioavailability, exploring methods that increase the concentration of berberine in blood is key to improving its usefulness in this context. Although intravenous administration provides a direct approach that may improve the bioavailability of berberine, this can lead to serious side effects including respiratory arrest ( Han et al, 2021b ). Therefore, berberine is often administered orally in clinic.…”

“…The main cause of DM and associated complications is a low level or lack of pancreatic islet function, including insulin resistance, resulting in disordered glucose metabolism in the body ( Pearson, 2019 ; Han et al, 2021b ). Sustained hyperglycemia progresses to various diabetic microangiopathies, including diabetic cardiovascular disease, nephropathy, neuropathy and retinopathy ( Reddy et al, 2015 ; Montero et al, 2019 ; Tang and Yiu, 2020 ).…”