Iridóides

Sesamoside is a main chemical ingredient iridoid glycoside from Lamiophlomic rotata , has analgesic and anti-inflammatory effects in animal studies.

Aucubin is an iridoid glycoside with a wide range of biological activities, including pancreas-protective, chondroprotective, antispasmodic, liver-protective, anti-inflammatory, anti-microbial, antioxidant, anti-algesic as well as anti-tumor activities. Aucubin prevents neuronal death in the hippocampal CA1 region in rats with diabetic encephalopathy, it also has protective effects on H2O2-induced apoptosis in PC12 cells. Aucubin may improve obesity-induced atherosclerosis by attenuating TNF-α-induced inflammatory responses. Aucubin suppresses hepatitis B viral DNA replication in vitro.

Picroside II has antioxidant, anti-inflammatory, immune regulatory, anti-virus and other pharmacological activities. It has potent anti-apoptotic activity against renal I/R injury by suppressing the TLR4/NF-κB signaling pathway, it can protect the ischemic kidney against renal fibrosis and improve the neurological function of rats upon cerebral ischemia reperfusion injury. Picroside II enhances nerve growth factor (NGF)-induced neurite outgrowth from PC12D cells by amplifying a down-stream step of MAP kinase in the NGF receptor-mediated intracellular MAP kinase-dependent signaling pathway.

Loganic acid( 0.7% solution) has a strong intraocular pressure (IOP)-hypotensive effect, it exhibits both sides effect on superoxide generation. Loganic acid also has protective effects on atherosclerosis risk factors in hypercholesterolemic rabbits, it shows significant anti-inflammatory effects decreasing TNF-α and IL-6 activity in serum.

Loganin is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively. Loganin has neuroprotective, anti-amnesic, anti-inflammatory and anti-shock effects, it also exhibits protective effects against hepatic injury and other diabetic complications associated with abnormal metabolic states and inflammation caused by oxidative stress and advanced glycation endproduct formation. Loganin can attenuate neuroinflammatory responses through the inactivation of NF-κB by NF-κB dependent inflammatory pathways and phosphorylation of MAPK in Aβ25-35-induced PC12 cells, and can protect against hydrogen peroxide-induced apoptosis by inhibiting phosphorylation of JNK, p38, and ERK 1/2 MAPKs in SH-SY5Y cells.

Shanzhiside methylester, the principle effective iridoid glycoside from the analgesic herb Lamiophlomis rotata , reduces neuropathic pain by activating spinal GLP-1 receptors and subsequently stimulating microglial β-endorphin expression via the p38 MAPK signaling; stimulation of the endogenous β-endorphin expression may be a novel and effective strategy for the discovery and development of analgesics for the long-term treatment of chronic pain.