Dantron

The roots of Rheum palmatum

Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.

In Vitro:Danthron (0.1, 1, and 10 μM) dose-dependently promotes the phosphorylation of AMPK and acetyl-CoA carboxylase (ACC) in both HepG2 and C2C12 cells. Meanwhile, Danthron treatment significantly reduces the lipid synthesis related sterol regulatory element-binding protein 1c (SREBP1c) and fatty acid synthetase (FAS) gene expressions, and the total cholesterol (TC) and triglyceride (TG) levels. In addition, Danthron treatment efficiently increases glucose consumption. Danthron effectively reduces intracellular lipid contents and enhances glucose consumption in vitro via activation of AMPK signaling pathway. 10 μM Danthron/24 h is safe for HepG2 cells. With 80% confluence, HepG2 cells are incubated with Danthron (0.1-10 μM) in FBS-Free media for 8 h. Subsequently, cells are harvested for Western blot assay. Danthron increases the p-AMPK protein in a dose-dependent manner, and no changes in t-AMPK protein are observed[1]. Danthron inhibits 9-cis retinoic acid (9cRA)-induced retinoic X receptor α (RXRα) transactivation by IC50 at 0.11 μM. To further clarify the stoichimetric ratio of Danthron binding to RXRα-ligand-binding domain (LBD), isothermal titration calorimetry (ITC) experiment is performed. The KD value of Danthron binds to RXRα-LBD by ITC experiment is determined at 7.5 μM[2].

In Vivo:Danthron functions as an insulin sensitizer in vivo. Danthron improves insulin sensitivity in diet-induced obese (DIO) mice. The insulin tolerance test result shows that Danthron (5 mg/kg) treated diet-induced obesity mice exhibit lower glucose levels after insulin challenge, compared with the control vehicle-treated group[2].

References:
[1]. Zhou R, et al. Danthron activates AMP-activated protein kinase and regulates lipid and glucose metabolism in vitro. Acta Pharmacol Sin. 2013 Aug;34(8):1061-9. [2]. Zhang H, et al. Danthron functions as a retinoic X receptor antagonist by stabilizing tetramers of the receptor. J Biol Chem. 2011 Jan 21;286(3):1868-75.

Factors influencing constipation in advanced cancer patients: a prospective study of opioid dose, dantron dose and physical functioning.[Pubmed:12882260]

Palliat Med. 2003 Jul;17(5):418-22.

The relationship between opioid dose, Dantron dose, bowel function and physical functioning (measured with the modified Barthel Index) was determined in a sample of 50 inpatients with advanced cancer. Data were collected prospectively from chart review and patient interviews one week after admission to allow for protocol-driven management of constipation to be established. Bowel scores were significantly reduced in 35 patients treated with opioids compared with 15 patients not treated with opioids. Within the opioid group, however, there was no relationship between opioid dose, bowel score, Dantron dose or Barthel Index. Higher doses of Dantron were associated with better physical functioning (but not opioid dose) suggesting that for any given dose of opioid, fitter patients were treated with larger doses of laxatives. Factors other than opioid dose and physical functioning may be more important in contributing to constipation in this group of patients. Less potent opioid drugs, such as codeine, are just as likely to cause constipation as more potent opioids.

Adverse effects of drugs used in the management of constipation and diarrhoea.[Pubmed:8136086]

Drug Saf. 1994 Jan;10(1):47-65.

Most laxatives, if used intermittently in the absence of contraindications, are relatively safe. Bulking agents may diminish absorption of some minerals and drugs, but this is not usually clinically significant. Ispaghula can cause serious allergic reactions. The chronic ingestion of stimulant laxatives has been blamed for the development of the 'cathartic colon', but there are no definitive studies which have demonstrated this. Dantron (danthron) preparations should only be used in older patients and the terminally ill because of the risk of hepatotoxicity with this drug. Oral oxyphenisatine should no longer be used. Senna would appear to be the stimulant laxative of choice during pregnancy and lactation. Bisacodyl is the polyphenolic derivative of choice. Lactulose, sorbitol and lactilol rarely cause significant adverse effects. Magnesium salt laxatives and phosphate enemas can cause serious metabolic disturbances in babies and young children. Liquid paraffin is contraindicated if there is any risk of aspiration. Interference with the absorption of fat soluble vitamins would not appear to be clinically significant. Docusate sodium may potentiate the hepatotoxicity of other drugs, but reports of this are rare. The role of cisapride in constipation has not been established. Antidiarrhoeal drugs are second line drugs whose use is aimed at minimising inconvenience and discomfort. No antidiarrhoeals can be recommended for children under 4 years of age. Loperamide is the drug of choice in older children and adults. The atropine component of diphenoxylate/atropine combinations can cause significant adverse effects. Bismuth salicylate is an inconvenient treatment for travellers' diarrhoea as large frequent doses of the liquid formulation are needed. Some bismuth can be absorbed and there is the potential to cause encephalopathy. Octreotide, methysergide and cholestyramine have a role for specific causes of diarrhoea only. Octreotide is effective in high output states from the small or large bowel, with few adverse effects. Clonidine and lidamidine may have a role in the treatment of chronic diabetic diarrhoea. The role of lidamidine in nondiabetic chronic diarrhoea has not been established.

Cleansing of the colon without enemas.[Pubmed:1215526]

Radiologe. 1975 Nov;15(11):421-6.

Several methods have been used to cleanse the large bowel prior to roentgen examination and rectoscopy for more than ten years. A method with administration of a salt solution (SALAX) in combination with different oral laxatives (Cascara sagrada, Dantron, Bisacodyl) without cleansing enemas is described. Hospitalized patients should have an individual preparation while ambulatory patients are almost completely cleansed if they carefully follow the given instructions.

Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.

Dantron,117-10-2,Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone,Natural Products, buy Dantron , Dantron supplier , purchase Dantron , Dantron cost , Dantron manufacturer , order Dantron , high purity Dantron