茹芭咕噜
是什么?
大黄中发现的新物质,它是一种对血管内皮细胞损伤的修复,有帮助的药,在澳洲市场属于商业运营的药品。
大精酸抗炎作用机理
治疗痛点: 糖尿病治疗痛点是糖尿病并发症,迄今仍未解决。医生说: 糖尿病不可怕,可怕的是并发症,因为并发症导致患者失明,脑梗、心梗、尿毒症,截肢等,致残率达90%。
填补空白: 并发症治疗至今尚未见同类产品上市,一旦上市,市场潜力巨大。
经济负担: 糖尿病并发症患者与政府医保都将背负沉重的经济包袱。
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已发布的研究报告
- (1)Hu C, Cong XD, Dai DZ, Zhang Y, Zhang GL, Dai Y. Argirein alleviates diabetic nephropathy through attenuating NADPH oxidase, Cx43, and PERK in renal tissue. Naunyn Schmiedebergs Arch Pharmacol. 2011 Mar;383(3):309-19.
大精酸治疗糖尿病肾病:大精酸治疗糖尿病肾病的药效很好。 药效由抑制NOX,内质网应激和解除异常Cx43所介导。
  - (2)Cong XD, Wu Y, Dai DZ, Ding MJ, Zhang Y, Dai Y. Activation of AQP4, p66Shc and endoplasmic reticulum stress is involved in inflammation by carrageenan and is suppressed by argirein, a derivative of rhein. J Pharm Pharmacol. 2012 Aug;64(8):1138-45.
抗炎症的作用:抑制角叉菜胶性关节炎,由于内质网应激, p66Shc, 和AQP4 水通道的异常 等机制,从而使炎症平息。
  - (3)Shi FH, Wu Y, Dai DZ, Cong XD, Zhang YM, Dai Y. Hepatosteatosis and hepatic insulin resistance are blunted by argirein, an anti-inflammatory agent, through normalizing endoplasmic reticulum stress and apoptosis in diabetic liver. J Pharm Pharmacol. 2013 Jun;65(6):916-27.
大精酸治疗糖尿病肝病:2型糖尿病性肝病, 脂肪肝和肝内脂肪堆积,肝内胰岛素抵抗,内质网应激和出现凋亡。大精酸使恢复到正常。J Pharm Pharmacol. 2013
  - (4)Cong XD, Ding MJ, Dai DZ, Wu Y, Zhang Y, Dai Y. ER stress, p66shc, and p-Akt/Akt mediate adjuvant-induced inflammation, which is blunted by argirein, a supermolecule and rhein in rats. Inflammation. 2012 Jun;35(3):1031-40.
大精酸的对抗炎症的作用:抑制佐剂关节炎,由于抑制炎症因子, 内质网应激, p66Shc, p-Akt/Akt 等机制,从而使炎症平息。
  - (5)Cheng YS, Cong XD, Dai DZ, Zhang Y, Dai Y. Argirein alleviates corpus cavernosum dysfunction by suppressing pro-inflammatory factors p66Shc and ER stress chaperone Bip in diabetic rats. J Pharm Pharmacol. 2013 Jan;65(1):94-101.
改善糖尿病性勃起障害:大精酸抑制内质网应激和p66Shc 的激活,改善阴茎海绵体的舒张功能。
  - (6) Liu GL, Zhang YM, Dai DZ, Ding MJ, Cong XD, Dai Y. Male hypogonadism induced by high fat diet and low dose streptozotocin is mediated by activated endoplasmic reticulum stress and IκBβ and attenuated by argirein and valsartan. Eur J Pharmacol. 2013 Aug 5;713(1-3):78-88.
高脂饮食与低剂量链脲佐菌素(STZ)引起的男性性腺功能低下被激活内质网应激、IκBβ可被大精酸及缬沙坦缓解。
  - (7)Cong XD, Fu PR, Dai DZ, Zhang Y, Dai Y. Pharmacokinetic behavior of argirein, derived from rhein, is characterized as slow release and prolonged T₁/₂ of rhein in rats. Eur J Pharm Sci. 2012 Aug 15;46(5):468-74.
药代动力学特征:与大黄酸相比,大精酸优良的抗炎作用和L-精氨酸可补充NO前体,改善血管内皮细胞。 药动学具有长效缓释功能;t1/2 为12 h,明显长于大黄酸的4 h。有效血浓明显降低,药效增强。活性广泛,抗炎作用强于大黄酸, 改善血管损害的作用,强于L-精氨酸。
  - (8) Shi FH, Cheng YS, Dai DZ, Peng HJ, Cong XD, Dai Y. Depressed calcium-handling proteins due to endoplasmic reticulum stress and apoptosis in the diabetic heart are attenuated by argirein. Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):521-31.
大精酸改善损害心功能和相应的靶点:糖尿病心肌病的发病, 由于内质网应激,凋亡,和炎症因子。 大精酸的治疗作用很显著。
  - (9) Zhang GL, Dai DZ, Xi T, Cong XD, Zhang Y, Dai Y. Isoproterenol-induced FKBP12.6/12 downregulation is modulated by ETA and ETB receptors and reversed by argirhein, a derivative of rhein. Acta Pharmacol Sin. 2011 Feb;32(2):223-9.
改善应激性心肌损害,和钙调蛋白的下调。
  - (10)Zhang YM, Yu F, Dai DZ, Gao J, Cong XD, Dai Y. Hypoxia alters pharmacokinetics of argirein because of mitochondrial dysfunction that is alleviated by apocynin. J Pharm Pharmacol. 2013 Sep;65(9):1360-72.
大精酸的代谢受到线粒体控制:在缺氧损害的大鼠,线粒体损害,使大精酸代谢异常。在改善线粒体功能后, 大精酸的代谢回到正常。
 
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