Narrow Results

Puerarin is an isoflavonoid isolated from the Chinese herb, Kudzu roots (also known as Gegen), which has been widely used for the treatment of hypertensive diseases and diabetic mellitus in traditional Chinese medicine. Dahl salt-sensitive (DS) rat is a genetic model of salt-sensitive hypertension with cardiovascular injury and vascular insulin resistance. Here, we investigated whether puerarin improved vascular insulin resistance and attenuated cardiac and aortic remodeling in salt-sensitive hypertension. DS rats were given a normal (NS) or high salt diet (HS) for five weeks. An additional group of DS rats was pretreated with puerarin and NS for 10 days, then switched to HS plus puerarin for five weeks. HS for five weeks increased systolic blood pressure (SBP), cardiac hypertrophy and fibrosis, and aortic hypertrophy with increased the expression of phosphor-ERK1/2 in the aorta and heart; puerarin attenuated cardiac and aortic hypertrophy, cardiac fibrosis and phosphor-ERK1/2 with a mild reduction in SBP. Hypertensive rats also manifested impairment of acetylcholine- and insulin-mediated vasorelaxation and insulin-mediated Akt and eNOS phosphorylation associated with the activation of NF$\kappa$B/TNF$\alpha$/JNK pathway. Puerarin improved acetylcholine- and insulin-mediated vasorelaxation and insulin-stimulated Akt/NO signaling with the inhibition of the NF$\kappa$B inflammatory pathway. Our results demonstrated that in salt-sensitive hypertension, puerarin improved vascular insulin action with cardiovascular beneficial effects. Our results found that the underlying mechanisms may involve its inhibition of NF$\kappa$B/JNK and ERK1/2 pathway. These results suggest that puerarin could be used as a new antihypertensive agent to expand our armamentarium for the prevention and treatment of end-organ damage in individuals with hypertension and metabolic diseases.

Diabetes mellitus (DM) has become one of the most challenging public health problems globally. The increasing prevalence and mortality rates call for more effective therapeutic agents, especially for DM complications. Traditional herbs have a long clinical application history for DM treatment. Puerarin is a natural isoflavone from Pueraria lobata (Wild.) Ohwi which has been consumed both as a functional food and herb in Eastern Asia countries. Documented data has shown that puerarin has cardio-protective, neuroprotective, anti-oxidative, anti-inflammatory and many other effects. In this review, we will summarize the beneficial effects and underlying mechanisms of puerarin on DM and complications. Puerarin may directly benefit DM by decreasing blood glucose levels, improving insulin resistance, protecting islets, inhibiting inflammation, decreasing oxidative stress and inhibiting Maillard reaction and advanced glycation end products (AGEs) formation. Furthermore, puerarin may also benefit DM indirectly by retarding and improving a series of DM complications, such as cardiovascular complications, diabetic nephropathy, diabetic retinopathy, diabetic neuropathy, etc. However, comprehensive studies of its effect and mechanisms are needed. In addition, its efficacy is relatively low, which is partially due to its pharmacokinetics profiles. Though puerarin shows low toxicity to experimental animals, its safety on human remains to be clarified. Collectively, we suggest that puerarin might be a potential adjuvant agent for the treatment of DM and DM complications in future.

Gegen (Radix Puerariae Lobatae), the root of Pueraria lobata, is an edible and medicinal herb which has been used in treating diabetic symptoms in the orient for thousands of years. We present an evidence map of the efficacy and safety of Gegen and Gegen formulas (GGFs) that use Gegen as an essential herb for diabetes, and also its mechanism of actions. We comprehensively searched the ancient medical records to identify empirical evidence; conducted a systematic review (SR) based on moderate- to high-quality randomized controlled trials (RCTs) to synthesize the clinical evidence; and reviewed the possible mechanisms of its antidiabetic effects. Empirical application of Gegen in treating diabetic symptoms dated back to more than 2000 years ago. Common herbs used in RCTs that accompany with Gegen included Radix et Rhizoma Glycyrrhizae, Radix et Rhizoma Ginseng, Rhizoma Dioscoreae, Poria, and Radix Ophiopogonis. The combinations used today are consistent with their usage in ancient times. Results of the SR showed that GGFs could benefit patients with type 2 diabetes for blood glucose control. When in combination with hypoglycemic agents or insulin, GGFs enhanced the glucose-lowering effect as well as the lipid-lowering effects. Also, the incidence and the risk of adverse events (AE), especially the hypoglycemic episodes, were lower in the combination group. No serious or life-threatening AE was reported. The experimental evidence presented that Gegen and GGFs might exert and enhance the anti-diabetic effects through activation of multiple mechanisms, such as reducing insulin resistance, increasing insulin release, inhibiting glucose absorption and reabsorption, and improving insulin sensitivity, glucose uptake, and metabolism.