|Source:||The roots of Salvia miltiorrhiza|
|Biological Activity or Inhibitors:||1. Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a concentration-dependent manner; TSB also suppresses the elevated Bax protein and decreased bcl-2 and caspase-3 proteins induced by staurosporine in rat cortical neurons; TSB is effective in reducing stroke-induced brain damage and may represent a novel drug candidate for further development.
2. TSB significantly inhibits the uptake of digoxin and vinblastine in membrane vesicles containing PgP or MRP1, moderately stimulates PgP ATPase activity, suggesting TSB is a substrate for PgP and MRP1 and that drug resistance to TSB therapy and drug interactions may occur through PgP and MRP1 modulation.
|Solvent:||Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.|
|Storage:||Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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|After receiving:||The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.|
|1 mg||5 mg||10 mg||20 mg||25 mg|
|1 mM||3.2216 mL||16.1082 mL||32.2165 mL||64.433 mL||80.5412 mL|
|5 mM||0.6443 mL||3.2216 mL||6.4433 mL||12.8866 mL||16.1082 mL|
|10 mM||0.3222 mL||1.6108 mL||3.2216 mL||6.4433 mL||8.0541 mL|
|50 mM||0.0644 mL||0.3222 mL||0.6443 mL||1.2887 mL||1.6108 mL|
|100 mM||0.0322 mL||0.1611 mL||0.3222 mL||0.6443 mL||0.8054 mL|
Drug Metab Lett. 2007 Aug;1(3):205-17.
|Involvement of P-glycoprotein and multidrug resistance associated protein 1 in the transport of tanshinone IIB, a primary active diterpenoid quinone from the roots of Salvia miltiorrhiza, across the blood-brain barrier.[Pubmed: 19356045]|
|Tanshinone IIB (TSB) is a major constituent of Salvia miltiorrhiza, which is widely used in treatment of cardiovascular and central nervous system (CNS) diseases such as coronary heart disease and stroke. This study aimed to investigate the role of various drug transporters in the brain penetration of Tanshinone IIB using several in vitro and in vivo mouse and rat models. The uptake and efflux of Tanshinone IIB in rat primary microvascular endothelial cells (RBMVECs) were ATP-dependent and significantly altered in the presence of a P-glycoprotein (P-gp) or multidrug resistance associated protein (Mrp1/2) inhibitor. A polarized transport of Tanshinone IIB was found in RBMVEC monolayers with facilitated efflux from the abluminal to luminal side. Addition of a P-gp inhibitor (e.g. verapamil) in both abluminal and luminal sides attenuated the polarized transport. In an in situ rat brain perfusion model, Tanshinone IIB crossed the blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier at a greater rate than that for sucrose, and the brain penetration was increased in the presence of a P-gp or Mrp1/2 inhibitor. The brain levels of Tanshinone IIB were only about 30% of that in the plasma and it could be increased to up to 72% of plasma levels when verapamil, quinidine, or probenecid was co-administered in rats. The entry of Tanshinone IIB to CNS increased by 67-97% in rats subjected to middle cerebral artery occlusion or treatment with the neurotoxin, quinolinic acid, compared to normal rats. Furthermore, The brain levels of Tanshinone IIB in mdr1a(-/-) and mrp1(-/-) mice were 28- to 2.6-fold higher than those in the wild-type mice. Tanshinone IIB has limited brain penetration through the BBB due to the contribution of P-gp and to a lesser extent of Mrp1 in rodents. Further studies are needed to confirm whether these corresponding transporters in humans are involved in limiting the penetration of Tanshinone IIB across the BBB and the clinical relevance.|