丹参酮IIA磺酸钠

中文名	丹参酮IIA磺酸钠
英文名	sodium 1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-2-sulfonate
别名	丹参酮IIA磺酸钠丹参酮IIA磺酸盐丹参酮IIA-磺酸钠丹参酮IIA-磺酸钠(标准品) TANSHINONE IIA-SULFONIC SODIUM 丹参酮IIA-磺酸钠
英文别名	DS 201 TanshinoneIIA Sodium TanshinonⅡA SilateA Sulfotanshinone sodiuM II-A Tanshinone ⅡASulfonate SodiuM SodiuM tanshinone IIA sulfonate Tanshinone IIA sodium sulfonate Sulfotanshinone SodiuM Injection sodium 1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-2-sulfonate SodiuM 1,6,6-triMethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-2-sulfonate
CAS	69659-80-9
化学式	C19H19NaO6S
分子量	398.4
InChI	InChI=1/C19H18O6S.Na/c1-9-13-15(20)16(21)14-10-5-4-8-19(2,3)12(10)7-6-11(14)17(13)25-18(9)26(22,23)24;/h6-7H,4-5,8H2,1-3H3,(H,22,23,24);/q;+1/p-1
熔点	To dark to Visualize
溶解度	DMSO (微溶) 、甲醇 (微溶)
存储条件	under inert gas (nitrogen or Argon) at 2-8°C
外观	固体
颜色	Red
物化性质	红色结晶粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于丹参根茎。
MDL号	MFCD09028094
体外研究	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 [Ca 2+ ]i and SOCE in hypoxic PASMCs. Sodium tanshinone IIA sulfonate inhibits the activity of CYP3A4 in a dose-dependent manner by the HLMs and CYP3A4 isoform. The K M 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. 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.
体内研究	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. Sodium Tanshinone IIA sulfonate prevention (30 mg/kg/day) alleviates hypoxia-induced characteristic changes in chronic hypoxia PH rat model. 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.
参考资料展开查看	1. [IF=4.545] Ningning Yang et al."Tanshinone IIA exerts therapeutic effects by acting on endogenous stem cells in rats with liver cirrhosis."Biomed Pharmacother. 2020 Dec;132:110815 2. [IF=4.432] Jiao Lan et al."Tanshinone IIA sodium sulfonate attenuates inflammation by upregulating circ-Sirt1 and inhibiting the entry of NF-κB into the nucleus."Eur J Pharmacol. 2022 Jan;914:174693

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