Purgative components in rhubarbs: adrenergic receptor inhibitors linked with glucose carriers

Fitoterapia. 2013 Dec:91:236-246. doi: 10.1016/j.fitote.2013.09.020. Epub 2013 Oct 2.

Abstract

Rhubarbs and their extractives have been used as cathartic for many years. There have been numerous breakthroughs in the pharmacological research of the drug. However, as the key point of the mechanism, the targets of the effective components still remain unclear. In this paper, with an in vitro system of isolated intestine, we found that both the rhubarb extractives and the anthraquinone derivatives can antagonize the adrenaline effectively. Furthermore, computer based docking provided the binding model of the anthraquinone derivatives and adrenergic receptor. Then, based on the results of the small intestinal promotion and purgative effect experiments in vivo, we built an "inhibitor-carrier" hypothesis to elucidate the mechanism of rhubarb. This work provided key massages for the pharmacological research of rhubarb, such a common and active medicinal plant, and might be of help for the development of new purgative drugs.

Keywords: Aloe-emodin (PubChem CID: 10207); Chrysophanol (PubChem CID: 10208); Emodin (PubChem CID: 3220); Large intestines; Physcione (PubChem CID: 10639); Rhein (PubChem CID: 10168); Rhubarb; Small intestines; β-Adrenal receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic Antagonists / pharmacology*
  • Anthraquinones / pharmacology*
  • Cathartics / pharmacology*
  • Drug Carriers
  • Drugs, Chinese Herbal / pharmacology*
  • Glucose
  • Intestinal Mucosa / metabolism
  • Intestines / drug effects*
  • Receptors, Adrenergic / metabolism*
  • Rheum / chemistry*

Substances

  • Adrenergic Antagonists
  • Anthraquinones
  • Cathartics
  • Drug Carriers
  • Drugs, Chinese Herbal
  • Receptors, Adrenergic
  • Glucose