Xinrui Zhou1, Kewu Zeng, Qi Wang, Xiaoda Yang, Kui Wang. 1. State Key Laboratories of Natural and Biomimetic Drugs and Department of Chemical Biology, Peking University, Beijing 100191, PR China.
Abstract
UNLABELLED: Cinnabar is one of traditional Chinese medicines widely used in many Asian countries. It is also a medicine with potential toxicity especially when taking overdose. Up to date, studies on the mechanism of the biological activity of cinnabar were still insufficient. AIM OF THE STUDY: To investigate the possible bioactive species from cinnabar after oral administration, which is the fundamental of biological effects of cinnabar. MATERIALS AND METHODS: Under mimetic intestinal and gastric conditions, the chemical components dissolved from cinnabar were analyzed by infrared spectroscopy (IR) and Raman spectroscopy. Furthermore, binding of mercuric species of cinnabar extractions to human serum protein (HSA) was characterized and their intestinal permeability was determined using the Caco-2 cell monolayer. The cytotoxicity of cinnabar extractions was assessed on human kidney-2 (HK-2) cell. RESULTS: Major dissolved species included mercuric polysulfide (i.e. HgS(2)(OH)(-) and Hg(3)S(2)Cl(2)). The apparent permeability coefficient (P(app)) of mercuric polysulfides was (1.6+/-0.3)x10(-6)cm/s, which is slightly lower than that of mercuric chloride (HgCl(2)). Unlike HgCl(2), mercuric polysulfides exhibited two tightly binding sites to HSA and had little effect on viability of HK-2 cells. CONCLUSION: Mercuric polysulfides, as the major dissolved components, may serve as the active species of cinnabar exhibiting pharmacological and/or toxicological effects. (c) 2010 Elsevier Ireland Ltd. All rights reserved.
UNLABELLED: Cinnabar is one of traditional Chinese medicines widely used in many Asian countries. It is also a medicine with potential toxicity especially when taking overdose. Up to date, studies on the mechanism of the biological activity of cinnabar were still insufficient. AIM OF THE STUDY: To investigate the possible bioactive species from cinnabar after oral administration, which is the fundamental of biological effects of cinnabar. MATERIALS AND METHODS: Under mimetic intestinal and gastric conditions, the chemical components dissolved from cinnabar were analyzed by infrared spectroscopy (IR) and Raman spectroscopy. Furthermore, binding of mercuric species of cinnabar extractions to human serum protein (HSA) was characterized and their intestinal permeability was determined using the Caco-2 cell monolayer. The cytotoxicity of cinnabar extractions was assessed on human kidney-2 (HK-2) cell. RESULTS: Major dissolved species included mercuricpolysulfide (i.e. HgS(2)(OH)(-) and Hg(3)S(2)Cl(2)). The apparent permeability coefficient (P(app)) of mercuric polysulfides was (1.6+/-0.3)x10(-6)cm/s, which is slightly lower than that of mercuric chloride (HgCl(2)). Unlike HgCl(2), mercuric polysulfides exhibited two tightly binding sites to HSA and had little effect on viability of HK-2 cells. CONCLUSION:Mercuric polysulfides, as the major dissolved components, may serve as the active species of cinnabar exhibiting pharmacological and/or toxicological effects. (c) 2010 Elsevier Ireland Ltd. All rights reserved.