生物活性

• 描述Tanshinone IIA Sulfonate Sodium (STS) is a derivative of tanshinone IIA, which acts as an inhibitor of store-operated Ca2+ entry (SOCE), and is used to treat cardiovascular disorders. Morris water maze results showed that oral administration of STS (10 mg/kg and 20 mg/kg) and Donepezil shortened escape latency, increased crossing times of the original position of the platform, and increased the time spent in the target quadrant. STS decreased the activity of acetylcholinesterase (AChE) and increased the activity of choline acetyltransferase (ChAT) in the hippocampus and cortex of SCOP-treated mice^[3]. Sodium Tanshinone IIA sulfonate (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats^[4]. 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^[5]. STS significantly ameliorated pulmonary inflammatory responses, mucus hypersecretion and lung function decline in CS-exposed mice challenged with LPS. STS treatment also significantly attenuated increased IL-6 and IL-8 releases from cigarette smoke extract (CSE)-treated human bronchial epithelial cells (16HBE) challenged with LPS^[6]. Intermittent hypoxia treatment resulted in high oxidative stress and low apoptosis in Lewis lung carcinoma-implanted mice, which could be attenuated by sodium tanshinone IIA sulfonate administration possibly through a mechanism mediated by the nuclear factor erythroid 2-related factor 2/nuclear factor kappa B signaling pathway^[7].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02524964	Left Ventricular Remodeling ... more >> Acute Myocardial Infarction Collapse <<	Phase 4	Unknown	July 2017	China, Guangdong ... more >> Guangdong Provincial Hospital of Chinese Medicine Recruiting Guangzhou, Guangdong, China, 510120 Contact: Minzhou Zhang, Dr.    86-20-81887233 ext 32801    minzhouzhang@yeah.net    Contact: Liheng Guo, Dr.    86-8187236 ext 32907    lihengguo1@yeah.net Collapse <<
  NCT01637675	Pulmonary Hypertension ... more >> Pulmonary Arterial Hypertension Cardiovascular Diseases Lung Diseases Tanshinone IIA Sulfonate Collapse <<	Phase 2 Phase 3	Unknown	December 2014	China, Guangdong ... more >> The First Affiliated Hospital of Guangzhou Medical University Recruiting Guangzhou, Guangdong, China, 510120 Contact: Jian Wang, MD    +8615013388183    jwang31@jhmi.edu Collapse <<

• 参考文献

• [1] Xu QQ, Xu YJ, et al. Sodium Tanshinone IIA Sulfonate Attenuates Scopolamine-Induced Cognitive Dysfunctions via Improving Cholinergic System. Biomed Res Int. 2016;2016:9852536.

  [2] Jiang Q, Lu W, et al. Sodium tanshinone IIA sulfonate inhibits hypoxia-induced enhancement of SOCE in pulmonary arterial smooth muscle cells viathe PKG-PPAR-γ signaling axis. Am J Physiol Cell Physiol. 2016 Jul 1;311(1):C136-49.

  [3] Xu QQ, Xu YJ, Yang C, Tang Y, Li L, Cai HB, Hou BN, Chen HF, Wang Q, Shi XG, Zhang SJ. Sodium Tanshinone IIA Sulfonate Attenuates Scopolamine-Induced Cognitive Dysfunctions via Improving Cholinergic System. Biomed Res Int. 2016;2016:9852536

  [4] Jiang Q, Lu W, Yang K, Hadadi C, Fu X, Chen Y, Yun X, Zhang J, Li M, Xu L, Tang H, Yuan JX, Wang J, Sun D. 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

  [5] Ouyang DS, Huang WH, Chen D, Zhang W, Tan ZR, Peng JB, Wang YC, Guo Y, Hu DL, Xiao J, Chen Y. Kinetics of cytochrome P450 enzymes for metabolism of sodium tanshinone IIA sulfonate in vitro. Chin Med. 2016 Mar 22;11:11

  [6] Li D, Sun D, Yuan L, Liu C, Chen L, Xu G, Shu J, Guan R, Xu J, Li Y, Yi G, Yao H, Zhong N, Wang J, Lu W. Sodium tanshinone IIA sulfonate protects against acute exacerbation of cigarette smoke-induced chronic obstructive pulmonary disease in mice. Int Immunopharmacol. 2020 Apr;81:106261

  [7] Zhang XB, Chen XY, Sun P, Su XM, Zeng HQ, Zeng YM, Wang M, Luo X. Sodium Tanshinone IIA Sulfonate Attenuates Tumor Oxidative Stress and Promotes Apoptosis in an Intermittent Hypoxia Mouse Model. Technol Cancer Res Treat. 2020 Jan-Dec;19:1533033820928073

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