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Research progress on chemical constituents and pharmacological effects of Chuanxiong

Research progress on chemical constituents and pharmacological effects of Chuanxiong

  • Time of issue:2023-11-28
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Research progress on chemical constituents and pharmacological effects of Chuanxiong

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  • Time of issue:2023-11-28
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Ligusticum chuanxiong Hort is a plant in the umbelliaceae family ligusticum chuanxiong Hort. It is usually used to treat chest numbness and pain, thorax and hypochondriac tingling pain, tumorous swelling pain, irregular menstruation, amenorrhea, abdominal pain, headache and rheumatism numbness pain. It can play a role in promoting blood circulation and qi, expelling wind and relieving pain. Its main components include ligustrazine, ferulic acid, etc., which can obviously remove oxygen free radicals; At the same time, it has the effects of blocking calcium channels, dilating blood vessels and anti-platelet aggregation, so it has been widely used in clinical practice. In this paper, the active components and pharmacological effects of ligusticum chuanxiong were reviewed.

 

 

Chemical composition

Ligustrum chuanxiong contains phthalides, terpenes, organic acids and their esters, alkaloids, polysaccharides and other chemical components. The volatile oils and alkaloids in ligusticum chuanxiong are the focus of research.

 

1.1 Volatile oils

The content of volatile oil in ligusticum chuanxiong is about 1%. The volatile oil is extracted by supercritical CO2 extraction and steam distillation. Then it was detected by column chromatography, GC-MS, LC-MS and other methods. More than 60 components have been identified from the volatile oil of ligusticum chuanxiong. Phthalein compounds are the main components of volatile oils.

 

1.2 Alkaloids

The main alkaloid components of ligustrazine, rye base, trimethylamine, adenine, adenosine, choline, uracil and so on. These alkaloids are small molecule compounds, and the content is low. Tetramethylpyrazine is the most reported in modern research, including extraction, separation, synthesis and content determination.

 

1.3 Polysaccharides

The content of polysaccharide in ligusticum chuanxiong was about 5.71%. Sun Xiaochun et al. used water extraction and alcohol precipitation method to extract polysaccharide from Ligusticum chuanxiong and purified it by DEAE-cellulose column chromatography to obtain LCXP-1,LCXP-2 and LCXP-3 polysaccharides. Among them, LCXP-1 and LCXP-2 are composed of mannose, glucose, galactose and arabinose, while LCXP-3 is composed of mannose, glucose, galactose, arabinose, rhamnose-galacturonic acid, which lays a foundation for pharmacologic research and processing of Chinese patent medicine.

 

 

Pharmacological action 

Chuanxiong not only can promote blood circulation and remove blood stasis, but also can act as a qi medicine in blood. It is widely used in chest, hypochondriac and abdominal pain caused by blood stasis and qi stagnation. The main diseases of Chuanxiong are closely related to cardiovascular and cerebrovascular diseases, thrombosis and pain, such as coronary heart disease, thromboangiitis obliterans, ischemic encephalopathy, hyperviscoemia and so on. Pharmacological studies on the chemical components of ligustrum Chuanxiong, such as water extract, phthalein components, ligustrolide, ligustrolide A, total alkaloids, ligustrazine and its injection have been extensively reported, mainly involving cardiovascular and cerebrovascular system, nervous system, respiratory system, liver and kidney function.

 

1 Effect on the cardiovascular system

(1)Effect on cardiomyocytes. The chemical components of ligustrazine, vanillin, chrysophanol and ferulic acid can directly act on myocardial cell membrane receptors. Among them, ligustrazine can act on α receptor, vanillin can act on β receptor. The results showed that lipopolysaccharide could significantly promote the expression of early response gene epoxidase 2(COX-2) and produce a series of inflammatory mediators, while ligustrazine could inhibit the expression of protein in COX-2 mRNA, and did not affect the activity of COX-2, indicating that tetramethylpyrazine antagonized myocardial cell apoptosis induced by lipopolysaccharide mainly by blocking lipopolysaccharide signal transduction.

 

(2)Improved myocardial ischemia. Ligustrazine has the effect of protecting myocardium injured by ischemia. Myocardial ischemia and hypoxia can lead to metabolic disorders of high-energy phosphorus compounds, further reduce ATP content, and then lead to the decrease of mitochondrial Ca2* -ATPase activity, resulting in the increase of Ca2+ content in myocardial mitochondria. Ligustrazine can stabilize the content of Ca²* in mitochondria, and increase the activity of mitochondrial Ca2+ -ATPase to protect the structure and function of mitochondria.

 

(3)The effect on blood vessels. Ligustrazine can significantly inhibit vasoconstriction, prevent CI outflow, reduce cell excitability, and facilitate the relaxation of vascular smooth muscle. Especially for the damaged vascular endothelial cells, it can inhibit the release of lactate dehydrogenase to some extent. In addition, it can inhibit the production of malondialdehyde, reduce the fluidity of cell membrane, play a role in stabilizing cell membrane, help prevent the formation of microthrombus, and reduce the damage degree of vascular endothelial cells; It can also prevent atherosclerotic lesions through other ways, play a certain anti-effect on lipid peroxidation, and help delay the progression of early atherosclerotic lesions.

 

(4)Improve cerebral ischemia. The results show that ischemic cerebrovascular disease can lead to the gradual apoptosis of neurons. Only by regulating the blood state and protecting the vascular endothelial cells and nerve cells, can we achieve the purpose of improving nerve function. Ligustrazine can improve microcirculation, increase cerebral cortex blood flow, and promote the recovery of nerve function. It can protect ischemic hypoxic brain tissue by regulating the expression of apoptotic gene and pro-apoptotic gene. In addition, ligustrylphthalein and ligustrin can also improve ischemic brain injury, and the latter mainly reduces the size of cerebral infarction by enhancing extracellular signal-regulating kinases in the cerebral cortex, which is conducive to improving the degree of neurological impairment.

 

(5)Influence on hemorheology. Ligustrazine can significantly inhibit platelet aggregation in vivo and in vitro, reduce whole blood high tangential viscosity and blood cell aggregation index, increase red blood cell deformation index, and play a role in improving hemorheology. Ligustrindole also has the above effect, but it is weaker than ligustrazine.

 

 

2 Effects on the respiratory system   

(1)The effect on asthma. Ligustrazine had no significant effect on peripheral blood lymphocytes and cell membrane protein kinase C in normal body, and only inhibited peripheral blood lymphocytes and cell membrane protein kinase C induced by asthma mediators. It can also inhibit the synthesis of type III collagen in the airway wall of asthma, reduce the thickening of the network basement membrane, and further inhibit the fibrosis in the early stage of airway reconstruction. In addition, it is beneficial to reduce the level of interleukin 4 and inhibit the dominant response of helper T cell subgroup 2.

(2) Improved hypoxic-respiratory depression. The results showed that ligustrazine could increase the expression of nitric oxide synthase in many parts of the brain stem after hypoxia, inhibit the expression of FOS protein in the brain stem nerve nuclei after hypoxia, and play an anti-effect on respiratory depression, which is conducive to the effect of protecting brain stem neurons, thus delaying the occurrence of respiratory depression and extending the survival time.

 

3 Anti-malignant tumor effect

(1)Self-anti-malignant tumor effect. Ligustrazine can directly act on human hepatocellular carcinoma cells Bel-7402, play a certain inhibitory effect on cell proliferation, reduce the secretion of alpha-fetoprotein, reduce the activity of aldolase, and increase the activity of ornithine carbamyltransferase. It can also induce the differentiation of Bel-7402 cells.

(2)Sensitization. The combination of Chuanxiongxiong and chemotherapeutic drugs can increase the concentration of intracellular chemotherapeutic drugs, so as to enhance the effect of killing tumor cells.

 

4 Effect on bone marrow hematopoietic system

Ligustrazine can significantly enhance the expression of bone marrow hematopoietic cells, which is conducive to promoting hematopoietic cell regeneration and repairing microvessels in the hematopoietic microenvironment, and further accelerate hematopoietic reconstruction.

 

5 Effects on urinary and digestive systems

(1) Ligustrazine has a certain protective effect on the ischemic injury of kidney, liver and intestinal tissue, which is conducive to the expansion of arterioles, improvement of microcirculation, and significantly reducing the content of active substances in ischemic tissue.

(2) Effect on the kidney. Ligustrazine has protective effect on accelerated glomerular basement membrane antibody nephritis in rats, which may be related to its antioxidative mechanism. In addition, it can promote the synthesis of autoantibodies and significantly improve the level of interleukin-12.

(3) Effect on digestive system. Ligustrazine can promote the continuous relaxation of the precapillary sphincter and make the true capillary have continuous blood perfusion. The distal colonic epithelium was stimulated to secrete CL and HCO, which was conducive to generating short-circuit currents in the basement membrane.

 

 

Outlook summary

In summary, the active components of ligustrazine and ferulic acid are mainly ligustrazine and ferulic acid, which can play a role in scavenging oxygen free radicals, alleviating Ca2* overload and dilating blood vessels, as well as protecting vascular endothelial cells, regulating immune function and inhibiting cell hypertrophy and apoptosis. Therefore, Chuanxiong is of great significance in the clinical treatment of multi-systems, multi-organs and a variety of diseases, and is affordable, extensive, and safe, worthy of in-depth clinical research and application.

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