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Tanshinone IIA (Tan IIA) is one of the main fat soluble compositions in the roots of red root Salvia miltiorrhiza. Tanshinone IIA can inhibit angiogenesis by targeting the protein kinase domain of VEGF / VEGFR2.

Name of Tanshinone IIA

English Name: tanshinone IIA
Chinese Alias: tanshinone | tanshinone IIA | tanshinone 2A | tanshinone IIA | tanshinone IIA biological activity

Description:
Tanshinone IIA (Tan IIA) is one of the main fat soluble compositions in the roots of red root Salvia miltiorrhiza. Tanshinone IIA can inhibit angiogenesis by targeting the protein kinase domain of VEGF / VEGFR2.

Relevant categories:
Research field > > cardiovascular disease
Natural Products > > Quinones

Target:
VEGF/VEGFR2[1]

In Vitro Study: The antitumor effects of tanshinone IIA include inhibiting tumor cell proliferation, disturbing tumor cell cycle, promoting tumor cell apoptosis and inhibiting tumor cell invasion and metastasis. Tanshinone IIA had anti proliferative effect on A549 cells: the IC50 of tanshinone IIA after 24, 48 and 72 hours were 145.3, 30.95 and 11.49, respectively μ M。 CCK-8 assay was used to evaluate tanshinone IIA (2.5-80 μ M) The proliferative activity of treated A549 cells at 24, 48 and 72 hours, respectively. CCK-8 results showed that tanshinone IIA could significantly inhibit the proliferation of A549 cells in a dose-dependent and time-dependent manner. Significant apoptosis and cell growth inhibition of A549 cells were observed 48 hours after drug treatment (the concentration used was about IC50 value: tanshinone iia31 on A549) μ M）。 Western blotting revealed exposure to tanshinone IIA (31) in A549 cells for 48 hours μ M) , down regulate the expression of VEGF and VEGFR2 protein in drug treatment group and vector [1]. Tanshinone IIA is one of the most abundant components of Salvia miltiorrhiza root, which can protect H9c2 cells from apoptosis. H9c2 cells treated with tanshinone IIA inhibited angiotensin II induced apoptosis by down regulating the expression of PTEN (phosphatase and tensin homologue). PTEN is a tumor suppressor that plays a key role in apoptosis. Tanshinone IIA inhibits angiotensin II (AngII) – induced apoptosis by down regulating the expression of phosphatase and tensin homologue (PTEN) [2]. Tanshinone IIA reduces the protein expression of EGFR, and IGFR blocks the PI3K / Akt / mTOR pathway in gastric cancer AGS cells [3].

Cell Experiment: A549 cells were counted in logarithmic phase and 6000 cells (90 μ L volume) in 96 well plate. Will 10 μ L different concentrations of tanshinone IIA (final concentrations 80,60,40,30,20,15,10,5 and 2.5 μ M) And ADM (final concentrations 8,4,2,1,0.5 and 0.25 μ M) It was added to the drug group, while the negative control group (carrier group) was added only 10 μ Ldmso or normal saline without tanshinone IIA or Adm. Mix the cells with CCK-8 reagent (100 μ L / ml medium) for another 2 hours, and the absorbance was read at 450 nm using a microplate reader. The cell proliferation inhibition rate is calculated according to the following formula: proliferation inhibition rate (%) = 1 – [(A1-A4) / (A2-A3)] × 100, where A1 is the OD value of the drug experimental group, A2 is the OD value of the blank control group, A3 is the OD value of RPMI1640 medium without cells, and A4 is the OD value of the drug with the same concentration as A1 but without cells. The IC50 value was calculated by nonlinear regression analysis using graphpad prism software [1], which represents the drug concentration showing 50% cell growth inhibition.

Reference:[1].  Xie J, et al. The antitumor effect of tanshinone IIA on anti-proliferation and decreasing VEGF/VEGFR2 expression on the human non-small cell lung cancer A549 cell line. Acta Pharm Sin B. 2015 Nov; 5(6):554-63.
[2].  Zhang Z, et al. Tanshinone IIA inhibits apoptosis in the myocardium by inducing microRNA-152-3p expression and thereby downregulating PTEN. Am J Transl Res. 2016 Jul 15; 8(7):3124-32.
[3].  Su CC, et al. Tanshinone IIA decreases the protein expression of EGFR, and IGFR blocking the PI3K/Akt/mTOR pathway in gastric carcinoma AGS cells both in vitro and in vivo. Oncol Rep. 2016 Aug; 36(2):1173-9.

Physicochemical properties of tanshinone IIA

Density: 1.2 ± 0.1 g / cm³

Boiling Point: 480.7 ± 44.0 ° C at 760 mmHg

Melting point: 205-207 º C

Molecular Formula: c19h18o3

Molecular Weight: 294.344

Flash Point: 236.4 ± 21.1 ° C

Exact Mass: 294.125580

PSA:47.28000

LogP:5.47

Appearance: Crystal

Steam Pressure: 0.0 ± 1.2 mmHg at 25 ° C

Refractive Index: 1.588

Storage Conditions: 2-8 ° C

Tanshinone IIA Safety Information

Personal Protective Equipment: eyeshields; Gloves; type N95 (US); type P1 (EN143) respirator filter

Transport Code Of Dangerous Goods: nonh for all modes of transport

Tanshinone IIA Literature

Customs Code: 2942000000

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Tanshinone IIA English Alias

Phenanthro[1,2-b]furan-10,11-dione, 6,7,8,9-tetrahydro-1,6,6-trimethyl-

Tanshinone IIA

tanshinone II-A

Dan Shen Ketone

Tanshionesiia

Tanshine II

TANSHION P.E

1,6,6-Trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]furan-10,11-dione

SweetOrange

MFCD00238692

QS-D-77-4-2

TANSHINONE A

Tanshiones

Tanshinone II