Scutellaria baicalensis was first recorded in "Shen Nong's Materia Medica", also known as Camellia Root and Tujin Tea Root.
Dampness, purging fire and detoxification, hemostasis, and tocolytic effects have a long history of medication, and are now commonly used clinically for damp-temperature, summer heat, chest tightness and nausea, lung-heat cough and other syndromes.
It is one of the most commonly used traditional Chinese medicines in clinical Chinese medicine and Chinese patent medicine.
According to statistics, there are 477 patent medicines containing Scutellaria baicalensis in the "Ministry of Traditional Chinese Medicine Standards", including 153 kinds of main diseases.
Therefore, the research on Scutellaria baicalensis has been widely concerned, and scholars at home and abroad have carried out extensive and in-depth research reports on the cultivation and identification, processing, material basis, pharmacological effects, and clinical application of Scutellaria baicalensis.
Scutellaria baicalensis extract includes baicalin, wogonin, baicalein and wogonin.
Studies have shown that Scutellaria baicalensis and its active components have a wide range of pharmacological effects, such as anti-inflammatory, antioxidant, anti-tumor and immune regulation, etc., especially the anti-bacterial/fungal effect is the most significant.
Scutellaria baicalensis is a commonly used medicine in traditional Chinese medicine, with a wide range of pharmacological effects and important clinical application value.
In recent years, researches on antibacterial, antiviral and antitumor researches on Scutellaria baicalensis extracts such as baicalin and baicalein have been increasing day by day.
In the face of the prevalence of bacterial multidrug resistance, basic and clinical research on anti-infection of traditional Chinese medicines represented by Scutellaria baicalensis and its active ingredients is particularly important, and the prospect of developing new antibacterial drugs is very broad.
In the Scutellaria baicalensis extract, baicalein shows significant antibacterial efficacy whether used alone or in combination, so it is necessary to conduct in-depth research on its antibacterial effect and mechanism, and it is expected to develop new antibacterial drugs based on active ingredients such as baicalein or baicalein.
In addition, the active ingredients of Scutellaria baicalensis with no obvious antibacterial activity or low antibacterial activity can also be explored, as a synergist of commonly used clinical antibacterial drugs to broaden the antibacterial means.
In a word, in-depth research on antibacterial effects of Scutellaria baicalensis and its extracts, and comprehensive and in-depth research on pharmacodynamic material basis and mechanism of action can open up new ways for the development of new antibacterial drugs.
【Element】
Scutellaria baicalensis extract mainly includes the following:
1. Flavonoids and their glycosides: Flavonoids and their glycosides are the main medicinal material basis of Scutellaria baicalensis.
At present, more than 40 kinds of flavonoids have been discovered from the medicinal materials of Scutellaria baicalensis. Among them, flavonoids and flavonols include baicalin and baicalein. , wogonin, wogonin, etc.;
Dihydroflavonoids and dihydroflavonols mostly have hydroxyl substitutions at C5 and C7, and the common ones are dihydrobaicalin, 7,2',6'-trihydroxy-5-methoxydihydroflavonoids, 5,7, 6'-Tetrahydroxyflavonol, etc.;
It also contains 4', 5, 7-trihydroxy-6-methylflavanone, 2', 6', 5, 7-tetrahydroxyflavanone and other flavanone components and chalcone components 2, 6 -2', 4'-tetrahydroxy-6'-methoxychalcone, etc.
Processing is the characteristic of the clinical application of traditional Chinese medicine. The ingredients contained in Chinese herbal medicines may change before and after processing, resulting in the effect of reducing toxicity and enhancing efficacy.
The processed products of Scutellaria baicalensis mainly include wine Scutellaria baicalensis, fried Scutellaria baicalensis, and Scutellaria baicalensis charcoal.
In the processed products, the content of flavonoid glycosides decreased and the content of flavonoid aglycones increased.
The change of material basis had a certain impact on various pharmacological effects of Scutellaria baicalensis and its processed products.
2. Terpenoids: Scutellariae contains a variety of sesquiterpene lignan glycosides and diterpenoids. Three new sesqui-lignan glycosides have been isolated from Scutellaria baicalensis in Nepal;
Except for Scuterpenin H, most of the diterpenoids isolated from Scutellaria are neocroane-type bicyclic diterpenoids; Shim isolated a new type of diterpenoid Barbatellarine F from Scutellaria and identified it. its structure.
It can be seen from the literature reports that in addition to flavonoids, Scutellaria baicalensis and its congeners still contain a variety of terpenoids, but there are few literature reports on the pharmacological effects of terpenoids in Scutellaria baicalensis, which deserves further in-depth study.
3. Volatile oil: In recent years, the volatile oil components in Scutellaria baicalensis have received attention, and many studies have analyzed the volatile oil components contained in Scutellaria baicalensis through different extraction and analysis methods.
The volatile oil components of the aerial parts of Scutellaria baicalensis were extracted by steam distillation, and 37 chemical components were identified by gas analysis method, mainly including allyl alcohol, caryophyllene, etc.
The volatile oil components of Scutellaria baicalensis were extracted by supercritical extraction technology GC-MS analysis identified 64 of these components, such as palmitic acid, menthone, methyl linoleate, etc.
Comparing the differences of volatile oil components and contents in the flowers, stems, leaves, roots and seeds of Scutellaria baicalensis showed that there are a lot of active components of volatile oil in various parts of Scutellaria baicalensis, which has a high development and application prospect.
4. Trace elements: The types and contents of trace elements in medicinal materials have gradually become important indicators for measuring the quality of medicinal materials and judging the authenticity of medicinal materials.
Scutellaria baicalensis contains a variety of trace elements, which not only have physiological activities themselves, but also form complexes with organic molecules contained in medicinal materials to exert their medicinal effects.
The contents of Ca, Mg, Cu, Zn, Fe, and Mn in 10 batches of Scutellaria baicalensis were determined by inductively coupled plasma atomic emission spectrometry, and the results showed that there were significant differences in their contents. The system provides a scientific basis.
5. Others: In addition, Scutellaria baicalensis extract also includes polysaccharides, β-sitosterol, benzoic acid and baicalenase.
【Pharmacological action and application】
1. Antipyretic and anti-inflammatory: Traditional Chinese medicine uses prescriptions and medicines, and treats based on syndrome differentiation.
Excessive heat syndrome is mostly guided by the treatment principle of cold in those with heat. Scutellaria baicalensis is cold in nature, so it has a certain clinical effect on the treatment of excess heat syndrome.
In recent years, the antipyretic and anti-inflammatory mechanisms of Scutellaria baicalensis and its components have been studied in depth.
Baicalin and baicalein can produce antipyretic and anti-inflammatory effects by interfering with the metabolic pathway of arachidonic acid and inhibiting the activity of cytokines.
2. Antimicrobial: Scutellaria baicalensis has a strong inhibitory effect on microorganisms, and its decoction has a broad-spectrum antibacterial effect. In addition, it can still resist a variety of fungi, viruses, mycoplasma, chlamydia and other microorganisms.
Scutellaria baicalensis and its active ingredients inhibit the growth of bacteria, fungi and chlamydia, which may be related to the inhibition of ATP synthase, the formation of microbial membranes and the inhibition of the expression of certain proteins.
Modern research has shown that baicalein has a strong effect on bacteria such as Escherichia coli, Micrococcus sessilei, Staphylococcus hominis, Staphylococcus epidermidis, fungi such as Candida albicans and other microorganisms.
Very good inhibitory effect; baicalin has a certain inhibitory effect on Helicobacter pylori, Staphylococcus aureus, yeast-type fungi, Chlamydia pneumoniae, etc.
The latest research found that baicalin can increase the cell apoptosis of yeast-type fungus Candida albicans.
The mechanism may be related to baicalin inhibiting the activities of succinate dehydrogenase and Ca2+-Mg2+ ATPase, increasing the amount of Ca2+ in the cytoplasm and destroying the ultrastructure of Candida albicans.
The combination of baicalein and baicalin with gentamicin, fluconazole, β-lactam antibiotics, etc., will produce synergistic effect and enhance the antibacterial effect.
3. Free radical scavenging and anti-oxidation: Free radicals have strong oxidative properties, which can damage the cells and tissues of the body, thereby causing chronic diseases and aging.
The molecular structure of flavonoids in Scutellaria baicalensis mostly contains phenolic hydroxyl groups, so it has certain free radical scavenging and antioxidant effects. Baicalein and baicalin are effective antioxidants in Scutellaria baicalensis, and have a strong scavenging effect on various free radicals, such as superoxide anion, hydroperoxidase, alkane peroxy radical, hydroxyl radical, etc.
In addition, baicalein and baicalin can effectively inhibit the metabolism of xanthine oxidase to generate oxygen free radicals, which can be used to treat diseases related to free radicals and oxidative stress.
4. Anti-tumor: With the in-depth research on Scutellaria baicalensis, it has been found that Scutellaria baicalensis has a certain inhibitory effect on various tumor cells.
Baicalin, baicalein, wogonin and wogonin are the material basis for the anti-tumor effect of baicalin, but their mechanisms are different.
Baicalin can inhibit the proliferation of rat islet cell tumor cells by inducing tumor cell apoptosis. Baicalein can make human umbilical vein endothelial cells arrest in G1/S phase, inhibit the formation of new blood vessels and have anti-tumor effect;
Baicalein can also inhibit the migration and invasion of skin cancer A431 cells to achieve anti-tumor purposes.
The latest research found that wogonin can inhibit the growth of malignant glioma by inducing tumor cell apoptosis, while wogonin can up-regulate the expression of natural killer cells (NK cells) GraB, etc., and enhance the effect of NK cells on gastric cancer MKN45 cells.
Ccan inhibit the growth of human ovarian cancer cell line SKOV3 xenograft tumor in nude mice by inhibiting the expression of telomerase hTERT in the tumor.
The role of total flavonoids from leaves and stems of Scutellaria baicalensis on tumor cell metastasis and invasion of Walker-256 tumor line.
To sum up, Scutellaria baicalensis has a certain anti-tumor activity and a broad anti-tumor spectrum, which can act in multiple links of tumor cell growth and play an anti-tumor effect.
5. Hepatoprotection and anti-ulcer: Activity studies have shown that baicalin can protect liver damage, treat chronic hepatitis, and resist liver fibrosis.
Baicalin may improve the effect of carbon tetrachloride by reducing the amount of transforming growth factor-β1 (TGF-β1), TNF-α, IL-6 and inhibiting the expression of platelet-derived factor-β (PDGF-β) receptors. induced hepatic fibrosis in rats.
Baicalin may play a protective effect on the liver injury of mice caused by carbon tetrachloride by inhibiting the production of cytokine NO.
For example, baicalin capsules, which are capsule preparations prepared from baicalin extracted from scutellaria baicalensis, have significant inhibitory effects on hepatitis B surface antigen, e antigen, and core antigen, and can inhibit hepatitis B virus DNA to a certain extent. copy;
After taking the medicine, the content of alanine aminotransferase can be obviously reduced, and it has a good protective effect on the liver. It is clinically used for the adjuvant treatment of acute, chronic hepatitis and persistent hepatitis.
6. Anti-ischemia-reperfusion injury: The cardiovascular and cerebrovascular protective activity of Scutellaria baicalensis is mainly manifested in the protection of myocardial ischemia-reperfusion injury and cerebral ischemia-reperfusion injury, improving the progression of atherosclerotic lesions, lowering blood pressure, and resisting thrombosis. aspect.
Recent studies have shown that baicalein can restore the contractile ability of myocardial cells and play a protective role during ischemia and reperfusion of myocardial cells;
Intravenous injection of baicalein may also improve myocardial contractility in endotoxic shock rats by reducing oxidative stress and myocardial inflammatory responses.
7. Protect neurons: Modern research shows that baicalin and baicalein have protective effects on a variety of neurons, and may become potential drugs for the treatment of Parkinson's and other neurological diseases.
Baicalin can reduce the expression of Fas protein and FasL protein, and play a protective effect on the neurons of neonatal hypoxic-ischemic brain damage (HIBD) mice.
8. Regulation of immunity: The active ingredients in Scutellaria baicalensis have two-way regulation of immune suppression and immune enhancement, and are expected to be used in the treatment of various allergic diseases.
Baicalin can significantly inhibit the proliferation of mouse CD3 + T cells induced by concanavalin (ConA) or phorbol ester polyclonal stimulator (PDB) and ionomycin (Lon) with obvious cycle specificity , suggesting that baicalin has the potential to develop into an immunosuppressant;
At the same time, baicalin also has the effect of enhancing the body's immunity. Baicalin can significantly reduce the immune liver injury caused by Bacille Calmette-Guérin (BCG) and lipopolysaccharide (LPS) in mice with alanine aminotransferase (ALT), aspartate aminotransferase ( AST) increase, reduce hepatocyte necrosis and promote hepatocyte proliferation.
9. Other Scutellaria baicalensis extracts also have the effects of treating and preventing diabetes and its complications, protecting human periodontal ligament fibroblasts, anti-parasitic, tocolytic, inhibiting lipid accumulation, and anti-photoaging. Baicalin can reduce blood glucose concentration in streptozotocin-induced diabetic rats.
【Baicalin Extraction】
Taking the content of baicalin and the extraction rate of ointment as comprehensive indicators, the extraction process of scutellaria baicalensis was optimized by orthogonal experimental design.
The results show that the optimal process for Scutellaria baicalensis extraction is to add 8 times the amount of water, extract 3 times, 1 hour each time, when the extract is concentrated to 1:2 (grams of crude drug/volume of drug solution), add 60% ethanol for alcohol precipitation.
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