Puerarin

Puerarin is a phytoestrogen extracted from Pueraria lobata with protective functions on the cardiovascular system^[1]. Puerarin exerts vasodilator effects on rat thoracic aorta by activating large conductance voltage-activated and calcium-activated potassium channels (BKCa)^[2]. Puerarin has been widely used to delay the progression of hepatitis, liver fibrosis, and non-alcoholic fatty liver disease in animal models of liver disease^[3].

In vitro, Puerarin treatment for 24 hours significantly inhibited the activity of SH-SY5Y cells with an IC₅₀ value of 174.4μM^[4]. Treatment of U251 and U87 cells with 200μM Puerarin for 48 hours significantly inhibited cell proliferation, induced cell apoptosis, and promoted the expression of Bax and cleaved caspase-3^[5]. Puerarin treatment (20μM) for 48 hours promoted the proliferation of MC3T3-E1 cells, increased alkaline phosphatase (ALP) activity, and up-regulated the expression of osteogenesis-related proteins^[6].

In vivo, Puerarin treatment (80mg/kg/day; i.p.) for three months improved myocardial structure and function, alleviated cardiac morphological disorder and collagen fiber proliferation in spontaneously hypertensive rats^[7]. Oral administration of Puerarin (100mg/kg/day) for 28 days ameliorated Aβ(1-42) -induced cognitive impairment and reversed hippocampal cell apoptosis in rats^[8]. Daily intraperitoneal injection of Puerarin (100mg/kg/day) for 13 weeks prevented high-fat diet (HFD)-induced obesity and steatosis in mice, significantly altered the composition of gut microbiota, and greatly increased the abundance of Akkermansia muciniphil ^[9].

References:
[1] Shu-Yong W E I, Yi C, Xiao-Yu X U. Progress on the pharmacological research of puerarin: a review[J]. Chinese Journal of Natural Medicines, 2014, 12(6): 407-414.
[2] Zhou Y X, Zhang H, Peng C. Puerarin: a review of pharmacological effects[J]. Phytotherapy Research, 2014, 28(7): 961-975.
[3] Wang D, Bu T, Li Y, et al. Pharmacological activity, pharmacokinetics, and clinical research progress of puerarin[J]. Antioxidants, 2022, 11(11): 2121.
[4] Sui X, Liu T, Zou Z, et al. Effects and mechanisms of puerarin against neuroblastoma: insights from bioinformatics and in vitro experiments[J]. BMC Complementary Medicine and Therapies, 2024, 24(1): 257.
[5] Yang J A, Li J Q, Shao L M, et al. Puerarin inhibits proliferation and induces apoptosis in human glioblastoma cell lines[J]. International journal of clinical and experimental medicine, 2015, 8(6): 10132.
[6] Wang N, Wang X, Cheng W, et al. Puerarin promotes osteogenesis and inhibits adipogenesis in vitro[J]. Chinese Medicine, 2013, 8(1): 17.
[7] Yan J, Honglei Y, Yun W, et al. Puerarin ameliorates myocardial remodeling of spontaneously hypertensive rats through inhibiting TRPC6-CaN-NFATc3 pathway[J]. European Journal of Pharmacology, 2022, 933: 175254.
[8] Li J, Wang G, Liu J, et al. Puerarin attenuates amyloid-beta-induced cognitive impairment through suppression of apoptosis in rat hippocampus in vivo[J]. European Journal of Pharmacology, 2010, 649(1-3): 195-201.
[9] Wang L, Wu Y, Zhuang L, et al. Puerarin prevents high-fat diet-induced obesity by enriching Akkermansia muciniphila in the gut microbiota of mice[J]. PLoS One, 2019, 14(6): e0218490.

Puerarin是一种从葛根中提取的植物雌激素，对心血管系统具有保护功能^[1]。Puerarin通过激活高电导电压和钙激活钾通道（BKCa）对大鼠胸主动脉产生血管舒张作用^[2]。Puerarin广泛应用于肝病动物模型中延缓肝炎、肝纤维化和非酒精性脂肪肝的进展^[3]。

在体外，Puerarin处理24小时可显著抑制SH-SY5Y细胞活性，IC₅₀值为174.4μM^[4]。200μM的Puerarin处理U251和U87细胞48小时能抑制细胞增殖、诱导凋亡，并促进Bax和cleaved caspase-3表达^[5]。20μM的Puerarin处理MC3T3-E1细胞48小时可促进细胞增殖，提高碱性磷酸酶（ALP）活性，并上调成骨相关蛋白表达^[6]。

在体内，自发性高血压大鼠每日腹腔注射Puerarin（80mg/kg/day；持续三个月）可改善心肌结构和功能，减轻心脏形态紊乱和胶原纤维增生^[7]。大鼠每日口服100mg/kg/day剂量的Puerarin（持续28天）能改善Aβ(1-42)诱导的认知障碍并逆转海马细胞凋亡^[8]。小鼠每日腹腔注射100mg/kg/day剂量的Puerarin（持续13周）可预防高脂饮食（HFD）诱导的肥胖和脂肪变性，显著改变肠道菌群组成并大幅提高Akkermansia muciniphila丰度^[9]。