Taspine

About: Taspine is a research topic. Over the lifetime, 73 publications have been published within this topic receiving 1377 citations.

A novel taspine derivative suppresses human liver tumor growth and invasion in vitro and in vivo.

Abstract: Taspine is an attractive target of research due to the anticancer and anti-angiogenic effects shown by in vitro and in vivo experiments. The present study investigated the role of tas1611, which is a derivative of taspine that has increased activity and solubility, in the regulation of the invasive properties of the SMMC-7721 liver cell line in vitro and in tumor inhibition in vivo. The proliferation of the SMMC-7721 cells was examined using the tetrazole blue colorimetric method. Matrigel® invasion chamber assays and zymogram analyses were performed to assess the inhibitory effect of tas1611 on cell invasion. Finally, a solid tumor athymic mouse model was employed to further investigate the anti-tumor effect of this compound. The results revealed that tas1611 had a marked inhibitory effect on the invasion of the SMMC-7721 cells and that this effect was associated with the activity and expression levels of matrix metalloproteinase (MMP)-2 and MMP-9. Furthermore, tas1611 was able to inhibit tumor growth effectively in a solid tumor SMMC-7721 athymic mouse model. In conclusion, tas1611 may serve as a promising novel therapeutic candidate for the treatment of metastatic liver cancer.

Cosmetic composition containing croton lechleri resin extract

Abstract: PURPOSE: A cosmetic composition containing a Croton Lechleri resin extract is provided to improve skin moisturization, elasticity, anti-aging, and skin whitening, and to ensure antibacterial and anti-inflammatory effects. CONSTITUTION: A cosmetic composition contains 0.0001-20 wt% of a Croton Lechleri resin extract as an active ingredient. The extract contains proanthocyanidin and taspine as active ingredients. The extract is prepared by leaching Croton Lechleri resin in water or an organic solvent, purifying, and extracting. [Reference numerals] (AA) Example 1; (BB) Comparative example 1; (CC) 0 week; (DD) 2 weeks; (EE) 4 weeks

Effect of Taspine Derivatives on Human Liver Cancer SMMC7721

Abstract: OBJECTIVE To analyse the inhibition effect of taspine derivatives on human Liver cancer SMMC7721 cell and its mechanism. METHODS The effects of five taspine derivatives on SMMC7721 cell growth were determined by MTT. The flow cytometry was used to determine the cell cycle. The effects of Tas-D1 on the EGF and VEGF in SMMC7721 cell were determined by ELISA. The mRNA level of EGF and VEGF in SMMC7721 cell was determined by RT-PCR. RESULTS The MTT assay demonstrated that the taspine derivative Tas-D1 significantly inhibited the growth of SMMC7721 cell in a dose-dependent manner. Cell was stopped at S phase by Tas-D1. Tas-D1 inhibited the expression of EGF and VEGF and their mRNA in a dose-dependent manner (P<0.05). CONCLUSIONS The taspine derivative Tas-D1 can inhibit the growth of human Liver cancer SMMC7721 cell and change cell cycle, which may be related to the inhibition of EGF and VEGF expression.

Taspine is a natural product that suppresses P2X4 receptor activity via phosphoinositide 3-kinase inhibition.

Abstract: Background & purpose P2X4 is a ligand-gated cation channel activated by extracellular ATP, involved in neuropathic pain, inflammation and arterial tone. Experimental approach Natural products were screened against human or mouse P2X4 activity using fura-2 loaded 1321N1 cells for measurement of intracellular Ca2+ responses; whole-cell currents were measured by patch clamp electrophysiological. Human primary macrophage chemokine release was used to assess effect of taspine on inflammatory cell function. An enzymatic assay was performed to assess the effect of taspine on recombinant PI3-kinase. Key results A natural product screen identified taspine as an inhibitor of human P2X4 activity. Taspine inhibits human and mouse P2X4-mediated Ca2+ influx in 1321N1 cells expressing receptors (IC50 1.6±0.4 μM and 1.6±0.3 μM, respectively), but lacked activity at human P2X2, P2X3, P2X2/3 and P2X7 receptors. Taspine inhibited the maximal response at human and mouse P2X4 but had no effect on ATP potency. Taspine has a slow onset rate (~15 mins for half-maximal inhibition), irreversible over 30 minutes of washout. Taspine inhibits P2X4-mediated Ca2+ signalling in mouse BV-2 microglia cells and human primary macrophage. Taspine inhibited P2X4-mediated CXCL5 secretion in human primary macrophage. Taspine reversed ivermectin-induced potentiation of P2X4 currents in 1321N1 stably expressing cells. The known PI3-kinase inhibitor LY294002 mimicked the properties of taspine on P2X4-mediated Ca2+ influx and whole-cell currents. Taspine directly inhibited the enzymatic activity of recombinant PI3-kinase in a competitive manner. Conclusions and implications Taspine is a novel natural product P2X4 inhibitor, mediating its effect through PI3-kinase inhibitor rather than receptor antagonism. Taspine can inhibit the pro-inflammatory signalling by P2X4 in human primary macrophage.