Pharmacological Effects Of Musk Ketone
Musk Ketone has the functions of aroma, opening the orifices, dredging the meridians, activating the collaterals, reducing swelling and relieving pain. Small doses have excitatory effects on the central nervous system, while large doses have inhibitory effects. It has excitatory effect on isolated frog heart, androgen-like effect and anti-inflammatory effect. It is clinically used for coronary heart disease, angina pectoris, vascular headache, sciatica, vitiligo, etc. This product has been synthesized and produced in China. The pharmacological action of the synthetic product is similar to that of natural muskone. Repeated oral administration (5mg/kg) can significantly shorten the sleep time caused by pentobarbital sodium in rats. The principle is that muskone has the effect of stimulating liver microsomal drug invertase, which causes the rapid destruction and inactivation of pentobarbital sodium in the liver. Its pharmacological effects are as follows:
Anti-dementia
Studies have shown that muskone can significantly promote the uptake of calcium ions in the thoracic aorta of scopolamine-induced dementia model rats, and improve learning and memory by promoting calcium influx to increase intracellular available calcium. It has significant curative effect on senile dementia caused by intracellular available calcium lower than physiological level; It can increase the activity of superoxide dismutase (SOD) in serum and decrease the activity of malondialdehyde (MAO) in brain tissue of aging model mice; At the same time, it can improve the learning and memory function of dementia mice, and play its anti-dementia role by clearing excess free radicals; It can inhibit the decomposition of monoamine neurotransmitters in the brain, delay the disturbance of brain neurotransmitters caused by dementia, and improve the function of central nervous system, thus having the function of promoting intelligence.
Anti-cerebral ischemia
Muscone has a significant protective effect on neuroblastoma cells from hypoxia, glucose deficiency and reoxygenation injury, suggesting that Muscone may be used for the treatment of acute stroke; It can significantly reduce the volume of cerebral infarction in rats with cerebral ischemia-reperfusion injury, and alleviate the nerve cell damage involved in cerebral ischemia-reperfusion injury
antiinflammatory
Musk Ketone inhibits interleukin-1 β （IL-1 β） And tumor necrosis factor- α （TNF- α）、 The production of cyclooxygenase-2 (COX-2), inhibitive nitric oxide synthase (iNOS), nitric oxide (NO), matrix metalloproteinase 13, and extracellular signal-regulated kinase (ERK1/2) and c-Jun N-terminal kinase chemicalbook (JNK) signal pathways were significantly inhibited.
Antimyocardial ischemia
Musk Ketone can significantly prolong the survival time of myocardial ischemia model rats induced by coronary artery ligation, increase the coronary flow, reduce the peak value of T wave and the content of creatine kinase (CK) and LDH, and have a significant effect on myocardial ischemia and angina pectoris; It can improve myocardial ischemia by reducing the release of plasma endothelin (ET), increasing the content of calcitonin gene-related peptide (CGRP) and increasing the expression of myocardial vascular endothelial growth factor (VEGF).
Antitumor
The respiratory inhibition rate of muskone on Ehrlich ascites tumor and leukocyte in mice was higher than that in normal mice; It has destructive effect on isolated animal cancer cells, and has obvious inhibitory effect on cell respiration of animal tumor tissue; Through the function of aromatics to promote qi, promote blood circulation and remove blood stasis, improve blood hypercoagulability, reduce platelet adhesion and aggregation, improve fibrin content, increase fibrinolysis and blood flow, improve the hypoxia state of tumor cell microenvironment, make HIF-1 low expression, and then reduce the expression of vascular endothelial growth factor (VEGF) and fibroblast growth factor (bFGF), thus play a role in inhibiting tumor angiogenesis.
Effect on central nervous system
Musk Ketone has a certain effect on the conditioned reflex of animals, and changes with the dose. Musk Ketone 5mg/kg orally administered to rats can significantly shorten the sleep time caused by pentobarbital sodium, but a large dose (100-500mg/kg) can prolong the sleep time, so it is believed that a small dose of Muscone has an excitatory effect on the central nervous system, and a large amount can also be inhibited.
Anti-early pregnancy and anti-implantation
Natural musk has obvious excitatory effect on the isolated uterus of pregnant rats, rabbits or guinea pigs after abortion. It can promote the gradual increase of uterine contractility and rhythm, and has a more obvious effect on the uterus of rabbits in late pregnancy. Therefore, musk has always been regarded as a contraindication of pregnancy in traditional Chinese medicine. Synthetic muskone has a similar effect. The daily subcutaneous injection of muskone 20mg in mice can induce anti-implantation and anti-early pregnancy effects, and the longer the pregnancy, the stronger the anti-pregnancy effect.
In addition, Musk Ketone also has anticoagulant, anti-inflammatory, antibacterial and anti-ulcer effects.
