Cryptotanshinone

As a representative component of the fat-soluble components of Danshen, a blood-activating and stasis-removing drug, cryptotanshinone has gradually become the focus of attention due to its unique chemical structure and pharmacokinetic properties. Recent studies have confirmed that it shows good prospects in cardiovascular diseases, anti-tumor, antibacterial and anti-inflammatory, metabolic disorders and neurodegenerative diseases.
1. Antibacterial effect: The chemical components separated from total tanshinone have been shown by in vitro antibacterial tests to have the strongest antibacterial activity and a high content, so it is the main component with antibacterial activity in total tanshinone. Cryptotanshinone has a significant inhibitory effect on Staphylococcus aureus, methicillin-resistant Staphylococcus aureus and β-lactamase-positive Staphylococcus aureus. Cryptotanshinone destroys the structure of bacterial cell walls and cell membranes, resulting in increased cell membrane permeability, which in turn causes the leakage of cell contents; at the same time, cryptotanshinone has a certain effect on the synthesis of bacterial proteins, reducing the amount of protein in the bacteria, affecting and hindering the expression of intracellular proteins, and ultimately leading to the loss of normal physiological functions of bacteria.
2. Cardiovascular protection: It has the effect of preventing and treating coagulation and restoring blood circulation.
3. Anti-allergic effect: Guided by the anti-allergic activity tracking, tanshinone I, tanshinone II A, cryptotanshinone and dihydrotanshinone I were isolated from Danshen, and it was found that they have the effect of interfering with IgE receptor-mediated PLCγ2 and MAPK tyrosine phosphorylation. Among them, dihydrotanshinone I and cryptotanshinone have significant activity, with IC50 of 16 and 36μM, respectively. This result shows that the dihydrofuran ring may play an important role in its activity.

1) Anti-inflammatory and antioxidant
In lipopolysaccharide (LPS)-induced mouse macrophages RAW 264.7, cryptotanshinone can inhibit the production of inflammatory mediators and significantly increase the survival rate of D-galactosamine-sensitized mice. In addition, it can also have a protective effect on the inflammatory response by reducing the expression of CD14 and TLR4 and inhibiting LPS-induced TAK1 phosphorylation. In the study of the effect of cryptotanshinone on lymphocyte proliferation response, it was found that when used in vitro, it has a concentration- and function-dependent two-way regulatory effect on the immune function of normal rats, and has a certain effect on the abnormal immune function of rats with collagen arthritis. improvement effect. IJi et al. reported that the antioxidant activity of the four components of tanshinone, from weak to strong, is tanshinone I, dihydrotanshinone, tanshinone IIA and CT.

2) Protect liver and lung damage
Cryptotanshinone in D-galactose/lipopolysaccharide-induced fulminant liver failure. The results showed that it can inhibit the activation of aspartate proteolytic enzyme, reduce cell apoptosis and the release of cytochrome C from mitochondria, thereby reducing liver failure mortality and TNF levels, and can also significantly inhibit JNK and ERK in cells. , p38 and TAK1 phosphorylation. It is speculated that the hepatoprotective effect of cryptotanshinone may be related to its anti-apoptotic activity, downregulation of MAPKs and NF-KB, and partial inhibition of TAK1 phosphorylation.

3) Antibacterial
Cryptotanshinone has significant inhibitory effects on Staphylococcus aureus, methicillin-resistant Staphylococcus aureus and B-lactamase-positive Staphylococcus aureus. It can destroy the bacterial cell wall and cell membrane structure, causing increased cell membrane permeability, leading to the leakage of cell contents. Moreover, it also has a certain impact on bacterial protein synthesis, which can reduce proteins in bacteria and hinder their expression, ultimately leading to the loss of normal physiological functions of proteins.

4. Other pharmacological effects
Gene chips were used to study the effect of cryptotanshinone on the gene expression of insulin-resistant ovarian granulosa cells, and found that it can improve the status of the cells by regulating multiple genes and signaling pathways. When studying the effect of cryptotanshinone on rats with dexamethasone-induced ovarian insulin resistance, it was found that in vivo, it can significantly reduce ovulation rate; in vitro, it can reduce testosterone and estrogen production. It is speculated that cryptotanshinone can weaken the inhibitory effect of dexamethasone on AKT2, thereby inhibiting the expression levels of CYP11 and CYP17.