1.The main source of betulinic acid?
First, it is extracted and separated from natural plants. This method consumes a large amount of solvent, has low yield and is difficult to separate impurities, so it is rarely used;
Secondly, betulinic acid was synthesized from betulin by organic synthesis. This method has been applied to industrial production, and betulinic acid of industrial scale can be obtained, which is the main source of betulinic acid in the market;
Thirdly, betulin was used as precursor to produce betulinic acid by microbial transformation.
2.Application and efficacy of betulinic acid
(1). Anti tumor effect
Betulinic acid was first found to have extremely strong selective cytotoxicity to melanoma cells, and in recent years, it has also been found to have strong broad-spectrum activity against other tumor cells, such as glioblastoma, neuroblastoma, neuroblastoma, Ewing tumor and other malignant tumors, colon cancer, breast cancer, lung cancer, liver cancer, prostate cancer, kidney cell Ovarian or cervical cancer and leukemia have strong inhibitory effects
(2). Anti inflammatory effect
Most pentacyclic triterpenoids have anti-inflammatory activities. Betulin and betulinic acid both have mild anti-inflammatory properties at higher concentrations, and their anti-inflammatory properties may depend on the inhibition of protein kinase C without involving any neurogenic inflammatory mechanism.
(3). Bacteriostatic effect
At present, betulinic acid has been found to have a certain antibacterial effect, which can inhibit a variety of bacteria including Escherichia coli, Bacillus subtilis, Staphylococcus aureus and Staphylococcus epidermidis. However, it has been proved that its antibacterial activity is weak, which may be related to the fact that it belongs to lupane pentacyclic triterpenes and that there are substances on the bacterial membrane that can biosynthesis hopane pentacyclic triterpenes. Based on the research on the antibacterial ability of betulinic acid, it has little potential as an antibacterial drug.
(4). Antiviral effect
Betulinic acid has outstanding antiviral activity, especially anti HIV activity. It also has effective effects on anti HCV, anti herpes simplex virus, anti Aiko virus, anti influenza virus and so on.
(5). Anti hyperlipidemia effect
Some studies have found that betulinic acid and its derivatives can play an anti hyperlipidemic role by regulating adipokines, reducing lipid production, reducing triacylglycerol and total cholesterol levels.
(6). Anti diabetes effect
Betulinic acid has shown good efficacy in the treatment of diabetes, mainly by inhibiting α- Amylase and α- Glucosidase can reduce the hydrolysis of polysaccharides and promote the synthesis of glycogen.
(7). Antioxidant stress activation
BA has a protective effect on normal cells and the body, which is related to antioxidant stress. For example, betulinic acid can protect the brain, kidney and heart from ischemia-reperfusion injury. BA has a protective effect on cerebral ischemia-reperfusion injury in mice through anti oxidative stress, anti nitriding stress and increasing blood flow.
(8). Other diseases
Now, some studies have found that betulinic acid has a certain improvement effect on Alzheimer's disease. Its protective effect is mainly through weakening neurobehavioral and cognitive dysfunction, reducing proinflammatory cytokines in the hippocampus, and reducing oxidation and nitrosation reactions.
Betulinic acid has certain anti anxiety effects, and betulinic acid components have been applied in some anti anxiety drugs. This may be related to the high fat solubility of betulinic acid, which can penetrate the brain barrier.
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