Baicalin is a flavonoid glycoside and an allosteric carnitine palmitoyltransferase 1 (CPT1) activator[1]. Baicalin can inhibit the replication of human immunodeficiency virus type 1 (HIV-1)[2]. Baicalin can reduce NF-κB expression and mediate the regulation of key cancer signaling pathways[3].
In vitro, Baicalin (0.005-0.5nM) treatment of RAW264.7 cells inhibited LPS-induced cell proliferation and reduced the expression of intercellular adhesion molecule-1 (ICAM-1), monocyte chemoattractant protein-1 (MCP-1), and cyclooxygenase-2 (Cox-2) proteins[4]. Baicalin (100μM) pretreatment of HK-2 cells for 1h can improve cell viability after H2O2 stimulation, reduce oxidative stress, and inhibit caspase-3 activation and cell apoptosis[5].
In vivo, Baicalin (10, 100 mg/kg) was intraperitoneally injected into rats with renal ischemia-reperfusion injury (IRI), which reduced oxidative stress and histological damage, improved renal function, inhibited proinflammatory response and tubular apoptosis, and reduced the expression of TLR2, TLR4, MyD88, p-NF-κB and p-IκB proteins and caspase-3 activity, and increased the Bcl-2/Bax ratio[6]. Baicalin (400 mg/kg) was intraperitoneally injected into diabetic nephropathy (DN) mice, which effectively improved diabetic conditions, proteinuria, renal histopathological changes and cell apoptosis, and inhibited the activation of the classic proinflammatory signaling pathway MAPK family, such as Erk1/2, JNK and P38MAPK signaling pathways [7].
References:
[1] Dai J, Liang K, Zhao S, et al. Chemoproteomics reveals baicalin activates hepatic CPT1 to ameliorate diet-induced obesity and hepatic steatosis[J]. Proceedings of the National Academy of Sciences, 2018, 115(26): E5896-E5905.
[2] Kitamura K, Honda M, Yoshizaki H, et al. Baicalin, an inhibitor of HIV-1 production in vitro[J]. Antiviral research, 1998, 37(2): 131-140.
[3] Yu X, Liu Y, Wang Y, et al. Baicalein induces cervical cancer apoptosis through the NF-κB signaling pathway[J]. Molecular Medicine Reports, 2018, 17(4): 5088-5094.
[4] Cui L, Feng L, Zhang Z H, et al. The anti-inflammation effect of baicalin on experimental colitis through inhibiting TLR4/NF-κB pathway activation[J]. International Immunopharmacology, 2014, 23(1): 294-303.
[5] Lin M, Li L, Zhang Y, et al. Baicalin ameliorates H2O2 induced cytotoxicity in HK-2 cells through the inhibition of ER stress and the activation of Nrf2 signaling[J]. International journal of molecular sciences, 2014, 15(7): 12507-12522.
[6] Lin M, Li L, Li L, et al. The protective effect of baicalin against renal ischemia-reperfusion injury through inhibition of inflammation and apoptosis[J]. BMC complementary and alternative medicine, 2014, 14: 1-9.
[7] Ma L, Wu F, Shao Q, et al. Baicalin alleviates oxidative stress and inflammation in diabetic nephropathy via Nrf2 and MAPK signaling pathway[J]. Drug design, development and therapy, 2021: 3207-3221.
黄岑苷（Baicalin）是一种类黄酮糖苷，是一种别构肉毒碱棕榈酰转移酶1（CPT1）激活剂[1]。Baicalin可抑制1型人类免疫缺陷病毒（HIV-1）的复制[2]。Baicalin可降低 NF-κB表达，介导癌症关键信号通路的调节[3]。
在体外，Baicalin（0.005-0.5nM）处理RAW264.7细胞，抑制了LPS诱导的细胞增殖，降低了细胞间粘附分子-1（ICAM-1）、单核细胞趋化蛋白-1 （MCP-1）、环氧合酶-2（Cox-2）蛋白的表达[4]。Baicalin（100μM）预处理HK-2细胞1h，可提高H2O2刺激后的细胞活力，降低氧化应激，抑制caspase-3的激活和细胞凋亡[5]。
在体内，Baicalin（10, 100 mg/kg）通过腹腔注射治疗肾缺血再灌注损伤（IRI）大鼠，减轻了氧化应激和组织学损伤，改善肾功能，抑制促炎反应和肾小管凋亡，还降低了TLR2、TLR4、MyD88、p-NF-κB 和 p-IκB 蛋白的表达及caspase-3活性，并增加Bcl-2/Bax比率[6]。Baicalin（400 mg/kg）通过腹腔注射治疗糖尿病肾病（DN）小鼠，有效改善糖尿病状况、蛋白尿、肾脏组织病理学变化和细胞凋亡，抑制了经典促炎信号通路MAPK家族的激活，例如Erk1/2、JNK和P38MAPK信号通路[7]。