Tanshinone IIA (Tan IIA) is one of the main compositions in the root of red-rooted salvia. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.
IC50 & Target
VEGF/VEGFR2[1]
体外研究 (In Vitro)
The anti-tumor effect of Tanshinone IIA includes inhibiting tumor cell proliferation, disturbing tumor cell cycle, promoting tumor cell apoptosis, and inhibiting tumor cell invasion and transfer. Tanshinone IIA has anti-proliferative effects on A549 cells: the IC50 of Tanshinone IIA after 24, 48 and 72 h are 145.3, 30.95 and 11.49 μM, respectively. The CCK-8 assay is used to evaluate the proliferative activity of A549 cells treated with Tanshinone IIA (2.5-80 μM) for 24, 48 and 72 h, respectively. The CCK-8 results show that Tanshinone IIA can significantly inhibit A549 cell proliferation in a dose- and time-dependent manner. Obvious apoptosis and cell growth inhibition of A549 cells are observed after drug treatment for 48 h (concentrations used are approximately IC50 values: Tanshinone IIA 31 μM on A549). Western blotting finds that 48 h exposures to Tanshinone IIA (31 μM) in A549 cells, downregulates expression of VEGF and VEGFR2 protein in both drug treatment groups vs. vehicle[1]. Tanshinone IIA, one of the most abundant constituents of the root of Salvia miltiorrhiza, protects rat myocardium-derived H9C2 cells against apoptosis. Treatment of H9C2 cells with Tanshinone IIA inhibits angiotensin II-induced apoptosis by downregulating the expression of PTEN (phosphatase and tensin homolog), a tumor suppressor that plays a critical role in apoptosis. Tanshinone IIA inhibits angiotensin II (AngII)-induced apoptosis by downregulating the expression of phosphatase and tensin homolog (PTEN)[2]. Tanshinone IIA decreases the protein expression of EGFR, and IGFR blocking the PI3K/Akt/mTOR pathway in gastric carcinoma AGS cells[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Tanshinone IIA (10 or 20 mg/kg; p.o) significantly reverses scopolamine-induced cognitive impairments[4]. Tanshinone IIA (2, 4, 8 mg/kg; i.p.) mediated protective effects on the STZ-induced diabetic nephropathy may be associates with the reduced endoplasmic reticulum stress via attenuating PERK signaling activities[5]. Tanshinone IIA (3 and 12 mg/kg; i.p.) significantly inhibits the growth of ectopic endometrium[6].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Decreased the expression levels of transforming growth factor-beta1, TSP-1, Grp78 and CHOP and attenuated the increase in the protein levels of p-PERK, p-elf2α and ATF-4 from the renal tissues of diabetic rats.
Animal Model:
Female Sprague-Dawley rats (180 -200g)[6]
Dosage:
3 and 12 mg/kg
Administration:
I.p.
Result:
Significantly inhibited the growth of ectopic endometrium.
分子量
294.34
Formula
C19H18O3
CAS 号
568-72-9
中文名称
丹参酮 IIA
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
[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.
Tanshinone IIA sulfonate sodium Chemical Structure
CAS No. : 69659-80-9
规格
价格
是否有货
数量
10 mg
¥500
In-stock
25 mg
¥1100
In-stock
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
Tanshinone IIA sulfonate sodium 相关产品
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生物活性
Tanshinone IIA sulfonate (sodium) is a derivative of tanshinone IIA, which acts as an inhibitor of store-operated Ca2+ entry (SOCE), and is used to treat cardiovascular disorders.
体外研究 (In Vitro)
Sodium Tanshinone IIA sulfonate (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats. The suppressive effects of Sodium Tanshinone IIA sulfonate on TRPC1 and TRPC6 expression in hypoxic PASMCs can be prevented by specific knockdown PKG or PPAR-γ. The suppressive effects of Sodium Tanshinone IIA sulfonate on basal calcium concentration and SOCE in hypoxic PASMCs can be reversed by specific knockdown of PKG or PPAR-γ. PKG-PPAR-γ signaling axis participates in the suppressive effects of Sodium Tanshinone IIA sulfonate on proliferation in hypoxic PASMCs. PPAR-γ agonist promotes the protective role of Sodium Tanshinone IIA sulfonate on basal [Ca2+]i and SOCE in hypoxic PASMCs[2]. Sodium tanshinone IIA sulfonate inhibits the activity of CYP3A4 in a dose-dependent manner by the HLMs and CYP3A4 isoform. The KM and Vmax values of STS are 54.8±14.6 µM and 0.9±0.1 nmol/mg protein/min, respectively, for the HLMs and 7.5±1.4 µM and 6.8±0.3 nmol/nmol P450/min, respectively, for CYP3A4. CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, and CYP2C19 show minimal or no effects on the metabolism of STS[3]. Sodium Tanshinone IIA sulfonate inhibits the activity of CYP3A4 in a dose-dependent manner in the HLMs and CYP3A4 isoform. Sodium Tanshinone IIA sulfonate primarily inhibits the activities of CYP3A4 in vitro, and Sodium Tanshinone IIA sulfonate has the potential to perpetrate drug-drug interactions with other CYP3A4 substrates[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Sodium Tanshinone IIA sulfonate (10 mg/kg, 20 mg/kg) and Donepezil shorten escape latency, increase crossing times of the original position of the platform, and increase the time spent in the target quadrant. Sodium Tanshinone IIA sulfonate decreases the activity of acetylcholinesterase (AChE) and increases the activity of choline acetyltransferase (ChAT) in the hippocampus and cortex of SCOP-treated mice. Sodium Tanshinone IIA sulfonate increases the activity of superoxide dismutase (SOD) and decreases the levels of malondialdehyde (MDA) and reactive oxygen species (ROS) in hippocampus and cortex[1]. Sodium Tanshinone IIA sulfonate prevention (30 mg/kg/day) alleviates hypoxia-induced characteristic changes in chronic hypoxia PH rat model[2]. Sodium Tanshinone IIA sulfonate (20, 10, and 5 mg/kg, i.p.) effectively prevents peritoneal adhesion without affecting anastomotic healing in the rats. Compared with the adhesion model group, the Sodium Tanshinone IIA sulfonate-treated groups show increased peritoneal lavage fluid tPA activity and tPA/PAI-1 ratio in the ischemic tissues with loared TGF-β1 and collagen I expressions in the ischemic tissues[5].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
396.39
Formula
C19H17NaO6S
CAS 号
69659-80-9
中文名称
丹参酮IIA磺酸盐
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Xu QQ, et al. Sodium Tanshinone IIA Sulfonate Attenuates Scopolamine-Induced Cognitive Dysfunctions via Improving Cholinergic System. Biomed Res Int. 2016;2016:9852536
[2]. Jiang Q, et al. Sodium tanshinone IIA sulfonate inhibits hypoxia-induced enhancement of SOCE in pulmonary arterial smooth muscle cells via the PKG-PPAR-γ signaling axis. Am J Physiol Cell Physiol. 2016 Jul 1;311(1):C136-49.
[3]. Ouyang DS, et al. Kinetics of cytochrome P450 enzymes for metabolism of sodium tanshinone IIA sulfonate in vitro. Chin Med. 2016 Mar 22;11:11.
[4]. Chen D, et al. Sodium tanshinone IIA sulfonate and its interactions with human CYP450s. Xenobiotica. 2016 Dec;46(12):1085-1092. Epub 2016 Mar 2.
[5]. Lin S, et al. [Sodium tanshinone IIA sulfonate prevents postoperative peritoneal adhesions in rats by enhancing the activity of the peritoneal fibrinolytic system]. Nan Fang Yi Ke Da Xue Xue Bao. 2016 Feb;36(2):260-4.
Animal Administration [1][2]
Mice[1] Male Kunming mice (KM, weighing 35-40 g) are maintained on standard laboratory conditions with free access to water and food. Mice are randomly divided into five groups: vehicle control group (CON, 0.9% saline, n=10), scopolamine group (SCOP, n=10), low dose Sodium Tanshinone IIA sulfonate group (Sodium Tanshinone IIA sulfonate L, SCOP 3 mg/kg + Sodium Tanshinone IIA sulfonate 10 mg/kg, n=10), high dose Sodium Tanshinone IIA sulfonate group (Sodium Tanshinone IIA sulfonate H, SCOP 3 mg/kg + Sodium Tanshinone IIA sulfonate 20 mg/kg, n=10), and Donepezil group (DON, SCOP 3 mg/kg + ARI 3 mg/kg, n=10). Mice are treated with saline, Sodium Tanshinone IIA sulfonate, and Donepezil, respectively, by gavage, once per day for two weeks. SCOP is injected from the eighth day for one week (intraperitoneally, IP). The SCOP is injected 0.5 h before the Morris water maze test. Rats[2] Male Sprague-Dawley rats (200-250 g) are randomly divided into four groups by the random number table: 1) normoxia control group, 2) normoxia + Sodium Tanshinone IIA sulfonate group, 3) hypoxia control group, and 4) hypoxia + Sodium Tanshinone IIA sulfonate group. Groups 1 and 2 are placed in normoxic condition and groups 3 and 4 in a hypoxic cabin with normal pressure, as previously reported, where the oxygen concentration is maintained at 10±1%, in a sustained hypoxic condition for 21 days. Groups 2 and 4, starting from the first day of hypoxia, are, respectively, intraperitoneally injected with 30 mg/kg tanshinone IIA sulfonate; meanwhile, groups 1 and 3 receive the same dose of saline.
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Xu QQ, et al. Sodium Tanshinone IIA Sulfonate Attenuates Scopolamine-Induced Cognitive Dysfunctions via Improving Cholinergic System. Biomed Res Int. 2016;2016:9852536
[2]. Jiang Q, et al. Sodium tanshinone IIA sulfonate inhibits hypoxia-induced enhancement of SOCE in pulmonary arterial smooth muscle cells via the PKG-PPAR-γ signaling axis. Am J Physiol Cell Physiol. 2016 Jul 1;311(1):C136-49.
[3]. Ouyang DS, et al. Kinetics of cytochrome P450 enzymes for metabolism of sodium tanshinone IIA sulfonate in vitro. Chin Med. 2016 Mar 22;11:11.
[4]. Chen D, et al. Sodium tanshinone IIA sulfonate and its interactions with human CYP450s. Xenobiotica. 2016 Dec;46(12):1085-1092. Epub 2016 Mar 2.
[5]. Lin S, et al. [Sodium tanshinone IIA sulfonate prevents postoperative peritoneal adhesions in rats by enhancing the activity of the peritoneal fibrinolytic system]. Nan Fang Yi Ke Da Xue Xue Bao. 2016 Feb;36(2):260-4.
Mogroside IIA1 is a triterpenoid glycoside and a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities[1].
分子量
801.01
Formula
C42H72O14
CAS 号
88901-44-4
中文名称
罗汉果苷 IIA1;罗汉果甜苷 IIA1;罗汉果甙 IIA1;罗汉果甜甙 IIA1
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Itkin M, et al. The biosynthetic pathway of the nonsugar, high-intensity sweetener mogroside V from Siraitia grosvenorii.Proc Natl Acad Sci U S A. 2016 Nov 22;113(47):E7619-E7628.
11-Oxomogroside IIa (11-oxomogroside II A1) is a cucurbitane glycoside extracted from the fruits of Siraitia grosVenorii. 11-Oxomogroside IIa has inhibitory effects against the Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), shows weak inhibitory effects on activation of (+/-)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexemide (NOR 1), a nitric oxide (NO) donor[1].
分子量
799.00
Formula
C42H70O14
中文名称
11-氧代葡萄糖苷IIa
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4deg;C, sealed storage, away from moisture and light
*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Akihisa T, et al. Cucurbitane glycosides from the fruits of Siraitia gros venorii and their inhibitory effects on Epstein-Barr virus activation. J Nat Prod. 2007 May;70(5):783-8. Epub 2007 May 4.
Cucurbitacin IIa is a triterpene isolated from Hemsleya amalils Diels, induces apoptosis of cancer cells, reduces expression of survivin, reduces phospho-Histone H3 and increases cleaved PARP in cancer cells[1].
分子量
562.73
Formula
C32H50O8
CAS 号
58546-34-2
中文名称
葫芦素 IIa;雪胆素甲
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Boykin C, et al. Cucurbitacin IIa: a novel class of anti-cancer drug inducing non-reversible actin aggregation and inhibiting survivin independent of JAK2/STAT3 phosphorylation. Br J Cancer. 2011 Mar 1;104(5):781-9.