Baicalin

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.