The Pharmacological Effects and Application Prospects of Puerarin

Puerarin, also known as Puerarin, is a natural isoflavone C-glycoside and the key component responsible for the medicinal effects of kudzu. Puerarin possesses various pharmacological effects such as lowering blood sugar, regulating blood lipids, protecting blood vessels, combating oxidative stress, fighting infections, and enhancing insulin sensitivity index. With relatively few adverse reactions, it is hailed as the "plant estrogen" and is clinically used to treat cardiovascular and cerebrovascular diseases, cancer, Parkinson's disease, Alzheimer's disease, diabetes, and diabetic complications.

1. Treatment of Diabetes

Puerarin can treat diabetes by lowering blood glucose concentrations. It upregulates the expression of insulin receptor substrate IRS-1 and insulin-like growth factor IGF-1 proteins, while promoting the expression of insulin receptor InsR and peroxisome proliferator-activated receptor PPARα, thereby achieving the goal of reducing blood glucose and treating diabetes. Additionally, puerarin inhibits the activity of α-glucosidase, further lowering blood glucose concentrations and treating diabetes. Studies have found that administering puerarin to patients with type 2 diabetes can improve their sensitivity to insulin, weakening insulin resistance and treating diabetes. Puerarin also inhibits the production of TNF-α in the plasma, enhancing sensitivity to insulin levels and reducing blood glucose content. Furthermore, applying puerarin in diabetic retinopathy can help reduce blood flow resistance in the ophthalmic artery, accelerate blood flow velocity, promote muscular artery dilation, and reduce local thrombosis, thus having a preventive effect on diabetic retinopathy. Puerarin also exhibits therapeutic effects on gestational diabetes.

2.Antitumor Effects

Puerarin exhibits significant inhibitory effects on the proliferation of tumor cells, demonstrating therapeutic potential by promoting tumor cell apoptosis. Researchers have established a prostate cancer PC3 cell model and treated PC3 cells with puerarin. Results showed that compared to the control group, the expression level of the proliferation protein Akt in the puerarin-treated group was significantly reduced, while the expression levels of apoptosis proteins Bax, Fas, caspase-3, and caspase-8 were all elevated. This indicates that puerarin can inhibit the proliferation of prostate cancer cells by regulating the activity of the proliferation protein Akt, while increasing the expression of apoptosis proteins Bax and Fas, thereby activating the caspase-3 apoptosis signaling pathway and ultimately leading to cancer cell apoptosis.

Furthermore, puerarin can also induce tumor cell apoptosis through a mitochondrial-dependent pathway. In liver cancer cells, cytochrome c released from mitochondria interacts with ATP and apoptotic proteases to activate caspase-9 and caspase-3, leading to apoptosis dependent on liver cancer cells. Puerarin can promote tumor cell apoptosis by activating the TLR4/NF-κB pathway, thereby inhibiting tumor growth. In colon cancer cell lines, puerarin promotes the activation of TLR4 expression factors, activates the PI3K/Akt pathway, leading to the expression of the downstream target protein NF-κB transcription factor, increases the expression level of caspase-3 protein, and induces apoptosis in colon tumor cells.

3.Protective Effects on the Liver

Puerarin possesses protective effects against liver damage caused by alcohol intoxication. In liver damage induced by various factors, the levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), and total cholesterol (CHOL) often increase abnormally. Researchers divided mice into a control group, a model group, and a puerarin-treated group to observe the expression levels of ALT, AST, and CHOL proteins, which represent the degree of liver damage. The results showed that the expression levels of ALT, AST, and CHOL proteins in the model group were significantly higher compared to the control group, while the levels in the puerarin-treated group were lower compared to the model group.

Furthermore, studies on models of liver damage caused by chronic alcohol consumption have found that compared to the control group, the expression of ALT, AST, ALP, and pro-inflammatory cytokines IL-1β, IL-6, and TNF-α were significantly reduced in the puerarin-treated group. This indicates that puerarin can alleviate liver damage caused by chronic alcohol consumption by modulating the inflammatory process.

4.Anti-arrhythmic and Anti-anginal Effects

Research indicates that puerarin can reduce the incidence of cardiac fibrillation induced by chloroform in Kunming mice and significantly elevate the threshold dose of aconitine-induced cardiac arrest, ventricular premature contractions, ventricular fibrillation, and ventricular tachycardia in SD rats, suggesting that puerarin is suitable for the treatment of arrhythmias. Puerarin injection has shown remarkable efficacy in treating coronary heart disease with angina pectoris. Its mechanisms include, firstly, reducing heart rate and blood pressure levels, improving vital signs, decreasing myocardial oxygen consumption, dilating coronary arteries, improving myocardial hypoxia and ischemia, and enhancing hemorheological indicators. Secondly, it reduces blood viscosity, softens blood vessels, improves atherosclerosis, repairs vascular endothelial cells, and prevents disease progression. Studies have confirmed that the application of puerarin injection in elderly patients with coronary heart disease and angina pectoris not only improves the incidence rate but also expands blood vessels, relieves hypoxia and ischemia, and further enhances various indicators such as hemorheology and myocardial oxygen consumption index, achieving ideal results.

5.Effects on the Cardiovascular System

Puerarin exerts effective antihypertensive effects in hypertensive animals. Injecting puerarin into experimental mice can cause a transient but significant reduction in blood pressure and a slowing of heart rate. Puerarin promotes local microvascular blood flow and increases the amplitude of movement, resulting in accelerated circulation and enhancement of normal cerebral microcirculation in the body, thereby reducing microcirculatory disorders. Additionally, puerarin can significantly improve the nailfold microcirculation in patients with sudden deafness. By clearing blood stasis in the vessels and accelerating blood flow, puerarin ultimately helps restore hearing in these patients.

Puerarin also plays a role in treating arrhythmias due to its content of β-adrenoceptor blockers, which can antagonize premature ventricular contractions and ventricular tachycardia, thereby reducing the occurrence of arrhythmias. Clinically, puerarin can decrease tachycardia and effectively treat arrhythmias. Furthermore, puerarin protects ischemic myocardium by increasing blood flow to ischemic regions and enhancing collateral blood flow, thereby treating ischemic myocardial conditions.

The clinical application of puerarin is also extensive. It not only demonstrates clinical value in treating cardiovascular diseases such as angina pectoris, coronary heart disease, myocardial infarction, and hypertension, but also activates blood vessels, improves cardiovascular conditions, and reduces the incidence of cardiovascular diseases. Additionally, the application of puerarin can also achieve certain clinical therapeutic effects in diseases such as retinal arteriovenous occlusion, optic atrophy, and sudden deafness.

The extensive pharmacological activities, clear efficacy, and low toxic and side effects of puerarin have been recognized by most people. However, its disadvantages such as poor lipid solubility, poor water solubility, and low bioavailability have limited its application. Nevertheless, in recent years, thanks to the application of high-molecular-weight materials with high biocompatibility, various puerarin nano-formulations have been developed, including liposomes, nanocrystals/nanoparticles, polymeric micelles, microemulsions, dendrimers, etc. These formulations enable puerarin to be uniformly dispersed and more easily penetrate biological membranes, increasing its solubility, stability, and bioavailability compared to traditional sustained-release and controlled-release formulations such as rapid-release tablets, matrix tablets, and solid dispersions. With the continuous development of pharmacological theories and modern medical technologies, research on puerarin has also deepened, and puerarin is poised to have a broader prospect in the future.

References:

[1] Ren Zhengxiao, Che Ping, Li Ziwei, Zhang Yingying. Research Progress on the Pharmacological Effects of Puerarin [J]. Shandong Chemical Industry, 2019, 48(19): 74-75.

[2] Li Zhiying, Fan Hongyan. Research Progress on the Pharmacological Effects of Puerarin [J]. Journal of Jilin Medical College, 2020, 41(05): 375-377.

[3] Lv Shuai. Research Progress on the Pharmacology and Clinical Application of Puerarin [J]. Health for All, 2020(10): 294-295.

About the Author

Xiaonisha, a food technology professional holding a Master's degree in Food Science, is currently employed at a prominent domestic pharmaceutical research and development company. Her primary focus lies in the development and research of nutritional foods, where she contributes her expertise and passion to create innovative products.