Activities Models Biological activities Action mechanism Ref. Anti-breast cancer MCF-7 Inhibit proliferation, reversing multidrug resistance - [4 , 5 ] MCF -7/TAM Inhibit proliferation (at 48 h IC50 =191.16 g/mL; at 72 h, IC50 =138.10 g/mL), induce apoptosis Decrease expression of Bcl-2 [6 ] 4T1 Inhibit proliferation (at 48h, IC50=14.7 μ mol/L) (1) Down-regulate TGF-β , VEGF and MCP-1 secretion, decrease TGF-β and VEGF mRNA expression, regulating its tumor inflammatory microenvironment. (2) Regulate blood viscosity, improve blood flow state, reduce the expression of u-PA, VEGF, PAI-1 protein and the secretion of IL-8, reduce the infiltration of neutrophils, improve TFPI-2 protein expression [7 , 8 ] Anti-human leukemia HL60, HL-60/ADR, K562 K562/A02 Inhibit proliferation (IC50 =288.27±34.23, 256.52±26.15, 320.80±36.52, 300.06±33.18, μ g/mL), reverse multidrug resistance Increase intracellular drug concentration and inhibit P-gp protein expression [5 , 9 ] K562 /A02 Inhibit the cell viability and induce apoptosis, different concentrations of verticine (100, 200, 400 mol/L); the cell viabilities were 0.392±0.040, 0.314±0.022, 0.161±0.033 Induce the ROS outbreak and increase the GSH content, redox imbalance [10 , 11 ] K562 Inhibit proliferation ( Anti-lung cancer A549/DDP Inhibit proliferation, induce apoptosis, reversing multidrug resistance Down-regulate expression of LRP and ERCC1 mRNA [12 , 13 ] Anti-gastric cancer SGC-7901 and SGC-7901/VCR Inhibit proliferation - [14 ] Anti-inflammatory effect 4T1 Regulate inflammatory microenvironment Control release of inflammatory factors, such as TGF-β , VEGF, MMP-9, and MCP-1, decreasing the expression of TGF-β and VEGF mRNA [6 ] Confluent NCI-H292 cells Remedy for inflammatory pulmonary diseases Inhibit gene and protein expression of MUC5AC mucin induced by EGF, PMA or TNF-α by directly acting on airway epithelial cells [15 ] LPS-induced RAW264.7 macrophages Inhibit production of inflammatory cytokines induced by LPS Block MAPKs and NF-kB signaling pathways [16 ] HMC-1 Cells Inhibit production of inflammatory cytokines Regulate the Phosphorylation of NF-κ B and MAPKs [17 ] HEK 293 anti-inflammatory Inhibit Kv1.3 channels [18 ] Protection against acute lung injury Mice Protective effect on acute lung injury Inhibit expression of TNF-α , IL-2, IL-6 and IL-8 and COX-2, promote the synthesis and release of SP-A, decrease the levels of PGE2 and NO. And, in addition, down-regulate phosphorylation level of MAPKs in the inflammatory response signaling pathway, and reduce NF-κ B gene transcriptional intensity [19 –23 ] Tracheobronchial Relaxation Isolated tracheal strips of guinea pigs Inhibit contraction M receptor [24 ] rat isolated tracheal and bronchial Inhibit carbachol-induced contraction Inhibit influx of calcium ions [25 ] Antitussive effect Mice Antitussive effect for ammonium hydroxide induced cough (4 mg/kg) - [26 ] Guinea pig trachea Antitussive effect for mechanical stimulation induced cough(4 mg/kg) - [26 ] Cat superior laryngeal nerve Antitussive effect electrical stimulation induced cough (4 mg/kg) - [26 ] Mice Inhibit cough frequency and increase latent period of cough induced by ammonia - [27 ] Expectorant effect Mice’s tracheal Enhance mice’s tracheal phenol red output in expectorant evaluation Increase tracheobronchial mucus secretion and decrease the viscosity of mucus [27 , 28 ] Sedative effect Mice Reduce spontaneous activity, prolong pentobarbital sleep time and increase sleep rate - [29 ] Analgesic effect Mice Inhibit writhing reaction induced by acetic acid Block Nav1.7 ion channel (μ M) [17 , 26 ] Inhibit proliferation of cultured Orbital fibroblast Thyroid-associated ophthalmopathy (TAO)-patients Different concentrations (5, 25,50, 75, 100 mg/L) inhibit the proliferation of orbital fibroblasts in vitro in a dose-dependent manner. - [30 ] Inhibit angiotensin converting enzyme (ACE) activity Rat plasma Inhibit ACE I activity in a dose-dependent manner (μ M) - [31 ] Inhibit acetylcholine (AChE) inhibitory activity At 100 μ g/mL, inhibition rate was only 25% - [32 ] Inhibit hERG potassium channels HEK293 cell line Inhibit hERG peak tail currents with channel inactivation, Mutation of Y652 to Alanine reduced sensitivity [33 ]
