Kukoamine A is a spermine alkaloid originally isolated from L. chinense that has diverse biological activities, including anticancer, neuroprotective, and anti-inflammatory properties. Kukoamine A (5-20 μg/ml) inhibits colony formation of U251 and WJ1 glioblastoma cells in a concentration-dependent manner. It halts the cell cycle at the G0/G1 phase and induces apoptosis when used at concentrations of 60 and 80 μg/ml. Kukoamine A (20 and 40 μM) induces autophagy and increases cell viability in an SH-SY5Y cell model of MPP-induced injury. It increases the number of dopamine neurons in the substantia nigra and striatum, decreases α-synuclein expression, and improves motor function in an MPTP mouse model of Parkinson’s disease when administered at a dose of 20 mg/kg per day. Kukoamine A (10 and 20 mg/kg) decreases IL-1β, TNF-α, and COX-2 protein levels in the hippocampus and increases hippocampal neurogenesis in a rat model of radiation injury. It also selectively inhibits trypanothione reductase (Ki = 1.8 μM), an enzyme that protects certain parasites from oxidative stress, over human glutathione reductase (Ki = >10 mM).
White crystalline powder, soluble in organic solvents such as methanol, ethanol, DMSO, etc., derived from the bark of Lycium bark.
(1) take the ground bone skin crushed 20-80 mesh, placed in the CO2 supercritical extraction tank extraction, through the liquid CO2, flow rate of 1-4 ml/min/g raw materials, while through the methanol to do the entrainment agent, flow rate of 1-4 ml/min/g, raw material extraction temperature of 40-50 , the pressure of 15-30Mpa, the extraction time of 1-3h, analysis of the extract;
(2) The above extract is dissolved in methanol solution over alumina short column, collect the liquid concentration, then separated by high-speed counter-current chromatography, UV detector on-line monitoring, collect the flow fraction decompression drying that is obtained.
Example:
Take the ground bone skin 5kg, crushed 60 mesh, placed in the CO2 supercritical extraction tank, through the liquid CO2, flow rate of 2ml/min / g raw materials, while through the 90% methanol to do the entrainment agent, flow rate of 2ml/min / g, raw material extraction temperature of 40 , the pressure of 23Mpa, the extraction time of 2h, resolution of the extract with 99% methanol solution dissolved in short columns of alumina (250g of neutral) Alumina short column (250g neutral alumina, particle size 120-200 mesh) to collect the liquid concentration, get extract. Take chloroform, methanol, water, according to 3:2:3 mixing, take the upper phase to do stationary phase, the lower phase for the mobile phase, the host speed of 850rpm, the flow rate of 2ml/min, UV detector on-line monitoring, collection of flow fraction decompression and drying, to get the Ground Bone Skin Methylene, detected by HPLC, the content of 98.3%.
[1] SHINJI FUNAYAMA. Structure of kukoamine A, a hypotensive principle of Lycium chinense root barks1[J]. Tetrahedron Letters, 1980, 21 14: Pages 1355-1356. DOI:
10.1016/s0040-4039(00)74574-6[2] QIAOPING WANG. Kukoamine A inhibits human glioblastoma cell growth and migration through apoptosis induction and epithelial-mesenchymal transition attenuation[J]. Scientific Reports, 2016, 6 1. DOI:
10.1038/srep36543[3] XIAOLONG HU . Neuroprotective effects of Kukoamine A on neurotoxin-induced Parkinson’s model through apoptosis inhibition and autophagy enhancement[J]. Neuropharmacology, 2017, 117: Pages 352-363. DOI:
10.1016/j.neuropharm.2017.02.022[4] YAQIONG ZHANG. Kukoamine A Prevents Radiation-Induced Neuroinflammation and Preserves Hippocampal Neurogenesis in Rats by Inhibiting Activation of NF-κB and AP-1[J]. Neurotoxicity Research, 2016, 31 1: 259-268. DOI:
10.1007/s12640-016-9679-4[5] J A PONASIK. Kukoamine A and other hydrophobic acylpolyamines: potent and selective inhibitors of Crithidia fasciculata trypanothione reductase.[J]. Biochemical Journal, 1995, 311 ( Pt 2): 371-375. DOI:
10.1042/bj3110371
