茹芭咕嚕
是什么?
大黃中發現的新物質,它是一種對血管內皮細胞損傷的修復,有幫助的藥,在澳洲市場屬于商業運營的藥品。
大精酸抗炎作用機理
治療痛點: 糖尿病治療痛點是糖尿病并發癥,迄今仍未解決。醫生說: 糖尿病不可怕,可怕的是并發癥,因為并發癥導致患者失明,腦梗、心梗、尿毒癥,截肢等,致殘率達90%。
填補空白: 并發癥治療至今尚未見同類產品上市,一旦上市,市場潛力巨大。
經濟負擔: 糖尿病并發癥患者與政府醫保都將背負沉重的經濟包袱。
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已發布的研究報告
- (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.
大精酸治療糖尿病腎?。捍缶嶂委熖悄虿∧I病的藥效很好。 藥效由抑制NOX,內質網應激和解除異常Cx43所介導。
  - (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.
抗炎癥的作用:抑制角叉菜膠性關節炎,由于內質網應激, p66Shc, 和AQP4 水通道的異常 等機制,從而使炎癥平息。
  - (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.
大精酸治療糖尿病肝?。?型糖尿病性肝病, 脂肪肝和肝內脂肪堆積,肝內胰島素抵抗,內質網應激和出現凋亡。大精酸使恢復到正常。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.
大精酸的對抗炎癥的作用:抑制佐劑關節炎,由于抑制炎癥因子, 內質網應激, p66Shc, p-Akt/Akt 等機制,從而使炎癥平息。
  - (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:大精酸抑制內質網應激和p66Shc 的激活,改善陰莖海綿體的舒張功能。
  - (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.
高脂飲食與低劑量鏈脲佐菌素(STZ)引起的男性性腺功能低下被激活內質網應激、IκBβ可被大精酸及纈沙坦緩解。
  - (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 T?/? of rhein in rats. Eur J Pharm Sci. 2012 Aug 15;46(5):468-74.
藥代動力學特征:與大黃酸相比,大精酸優良的抗炎作用和L-精氨酸可補充NO前體,改善血管內皮細胞。 藥動學具有長效緩釋功能;t1/2 為12 h,明顯長于大黃酸的4 h。有效血濃明顯降低,藥效增強?;钚詮V泛,抗炎作用強于大黃酸, 改善血管損害的作用,強于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.
大精酸改善損害心功能和相應的靶點:糖尿病心肌病的發病, 由于內質網應激,凋亡,和炎癥因子。 大精酸的治療作用很顯著。
  - (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.
改善應激性心肌損害,和鈣調蛋白的下調。
  - (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.
大精酸的代謝受到線粒體控制:在缺氧損害的大鼠,線粒體損害,使大精酸代謝異常。在改善線粒體功能后, 大精酸的代謝回到正常。
 
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