What is the role of berberine hydrochloride

1. Antibacterial effect


Berberine hydrochloride has a long history of antibacterial medicinal use, and is mainly used for the treatment of gastrointestinal inflammation, intestinal parasite infection, bacterial diarrhea and trachoma. 



Berberine hydrochloride has a synergistic effect in combination with various antibacterial drugs including aztreonam, ceftazidime, and piperacillin-tazobactam. The antibacterial mechanism of berberine hydrochloride is as follows:


(1) Inhibit bacterial DNA replication and transcription. The antibacterial mechanism of berberine is similar to that of rifampicin and norfloxacin, and its target sites are RNA polymerase, gyrase and topoisomerase IV, which are all related to nucleic acids. 


Therefore, berberine exerts its antibacterial effect by affecting the replication and transcription of bacterial DNA.


(2) Inhibit protein synthesis. Berberine also exerts its antibacterial effects by altering the bacteria's ribosomes and cell walls to interfere with their protein biosynthesis.


(3) Inhibit the activity of important enzymes in bacteria. The molecular target of berberine's antibacterial effect may be the inhibition of stortase activity.


(4) Antagonize the activity of bacterial enterotoxins and the adhesion of bacteria. 

The results showed that berberine has a strong inhibitory effect on intestinal secretion disorders caused by Escherichia coli (E.coli) heat-resistant enterotoxin and Vibrio cholerae (V.cholera) toxin.


(5) Other mechanisms. Other studies have found that berberine can interfere with the oxidative decarboxylation of bacterial pyruvate and inhibit bacterial growth; berberine can cause the efflux of intracellular calcium ions, which may change the permeability of calcium ion channels on the cell membrane to allow calcium efflux;


2. Antifungal effect

Due to the overuse of drugs, the phenomenon of drug resistance in the treatment of fungal infections is becoming more and more serious. 


The combined application of traditional Chinese medicine ingredients is a new method for the treatment of fungal drug resistance. 


The combined use of berberine hydrochloride and fungal therapeutic drugs shows a synergistic effect. For example, the combined use of fluconazole can well treat Candida albicans infection.


3. Anti-inflammatory effect


Berberine hydrochloride has shown a good effect in the treatment of acute, chronic, ulcerative inflammation and other diseases. 


Berberine hydrochloride achieves anti-inflammatory effect by inhibiting the secretion of pro-inflammatory factors stimulated by lipopolysaccharide. 


Berberine hydrochloride can be anti-inflammatory by inhibiting the expression of inflammatory factors, and animal experiments have shown that it has a curative effect on mouse endometritis. 

More studies have shown that the anti-inflammatory effect of berberine hydrochloride can be used to prevent intestinal adhesions after abdominal surgery.


4. Regulating blood sugar


Diabetes has a large prevalence in the world. Several studies have shown that berberine hydrochloride has antioxidant capacity, which can significantly control the development of diabetes. 


On the basis of anti-inflammatory effect, it can improve insulin resistance by inhibiting inflammation. By affecting glucose metabolism and then treating type 2 diabetes mellitus, it can improve the patient's tolerance to glucose, and also achieve the effect of improving insulin resistance.


5. Anti-tumor effect

Preliminary experiments by a number of researchers have proved that berberine hydrochloride has anti-tumor effects. 


Berberine hydrochloride has also shown anti-cancer activity in various models including gastric cancer and nasopharyngeal cancer, which can inhibit tumor proliferation, block Cell division affects the normal function of mitochondria and induces tumor cell apoptosis. 


A review of various studies shows that berberine hydrochloride can inhibit tumors from the following aspects: regulating cell cycle CyclinD1 inhibits tumor growth; inhibiting new tumor angiogenesis; promoting ROS generation and inducing apoptosis; destroying tumor growth environment; inhibiting cancer cells Metastasis and proliferation.


6. Anti-atherosclerosis effect Berberine hydrochloride can inhibit atherosclerosis through multiple channels and has relatively low side effects, and the natural ingredients are suitable for long-term use by patients. 


Some studies have also shown that berberine hydrochloride plays an anti-atherosclerotic effect by reducing the levels of TC and LDL, preventing the expression of cell adhesion molecules, thereby reducing the chemotaxis of TMAs.


7. The effect of lowering blood uric acid

Oral administration of berberine hydrochloride tablets can reduce blood uric acid. Berberine hydrochloride tablets (0.5g/time, 3 times/d) can not only reduce blood TC, TG, LDL-C, FBG in hyperuricemia patients with hyperlipidemia, hypertension, diabetes and other diseases , SBP, DBP, body weight level, but also has the effect of reducing its fasting blood uric acid level.


8. Anti-rheumatoid arthritis effect

Berberine hydrochloride can significantly inhibit cell proliferation in immune serum-deficient people in a dose-dependent manner. 


Cell cycle analysis showed that the arrest of berberine occurred in the GO/G1 phase. 


Berberine increases the apoptosis of raflss by increasing the expression of apoptotic protein genes, reducing the anti-apoptotic proteins Bcl-2 and Bcl-xl, disrupting mitochondrial membrane potential, activating caspase-3,9 and poly(ADP-ribose) polymerase Death, berberine has potential therapeutic significance for the treatment of rheumatoid arthritis.


9. The effect of anti-heart failure and improving cardiac function


10. Inhibition of platelet aggregation


The anti-platelet aggregation effect of berberine hydrochloride mainly includes the following aspects:


(1) It has an inhibitory effect on platelet aggregation caused by platelet inducers;


(2) It can inhibit the contraction of platelet blood clots;


(3) It can also accelerate the depolymerization of platelet aggregates. 

Its mechanism of action may be related to the binding of berberine hydrochloride to a2 receptors, increasing the level of cyclic adenosine monophosphate (cAMP) in platelets, and inhibiting the synthesis of thromboxane (TX) A2 and prostacyclin (PGI2).


 11. Lowering blood lipids


 12. Lowering blood pressure


The hypotensive mechanism of berberine hydrochloride may be by inhibiting the activity of cholinesterase, increasing the concentration of acetylcholine, and stimulating M receptors, thereby inhibiting the release of norepinephrine, resulting in vasodilation and lowering blood pressure. 


Berberine hydrochloride can also competitively block α receptors on vascular smooth muscle, reduce peripheral vascular resistance, and play a role in lowering blood pressure.


 13. Antiarrhythmic effect


 Berberine hydrochloride can significantly prolong the action potential time course and effective refractory period of cardiomyocytes, so that the one-way conduction block becomes a two-way conduction block or the time course required to destroy the reentrant loop, thereby eliminating the reentrant arrhythmia.


14. Inhibits the effect of cardiac hypertrophy


Berberine hydrochloride has a protective effect on the myocardium in hypertensive patients and in animal models of cardiac hypertrophy.


15. The effect of treating hyperthyroidism


16. The role of treating urinary tract infections during pregnancy


 17. Anticancer effect


In clinical treatment, berberine hydrochloride has therapeutic effects on esophageal cancer, gastric cancer, colon cancer, etc. Its mechanism of action includes:


(1) Inhibition of mitochondrial energy production affects cell proliferation. In vitro experiments found that berberine hydrochloride can inhibit the proliferation of mouse colon cancer cells, accompanied by a decrease in intracellular and mitochondrial adenosine triphosphate (ATP) levels.


(2) Induce apoptosis of cancerous cells through various ways. Berberine hydrochloride induces apoptosis by up-regulating the expression of apoptosis gene Bax and inhibiting the expression of Bd-2 in gastric cancer cells. 

It can also induce tumor cell apoptosis by promoting the increase of inflammatory factors, and can also be induced by DNA strand breaks. apoptosis and exert its therapeutic effect.


(3) Affect the metastasis of tumor cells. Intratumoral neovascularization can promote tumor cell proliferation and metastasis. 


These two factors play an important role in angiogenesis. Berberine hydrochloride can reduce the expression of vascular endothelial growth factor and hypoxia-inducible factor in tumor cells, inhibit the formation of new blood vessels and reduce the invasive ability of cancer cells.


【Extraction Method】


1. Acid water extraction method, 


2. Enzymatic extraction method


3. Ultrasonic extraction method


4. Microwave extraction method


5. Ethanol extraction of berberine


6. The specific method of lime milk method is to add lime milk and stir evenly, soak in water for 24 hours, collect the leachate, adjust the pH to about 1.5 with hydrochloric acid, add salt overnight, and then precipitate berberine hydrochloride. up to 1.17%. 


7. Liquid membrane method 


8. Supercritical carbon dioxide extraction method


【Application】

Clinically, berberine hydrochloride is mainly used to clear away heat and detoxify, and to treat intestinal infections. 


Cells, esophageal cancer cell lines, nasopharyngeal cancer cells, bladder cancer cells, malignant teratoma cells, etc. all have certain inhibitory and killing effects.

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