[Study on anti-cataract effect of gigantol combined with syringic acid and their mechanism].

Abstract

OBJECTIVE:

To study the anti-cataract effect of gigantol combined with syringic acid and their action mechanism.

METHOD:

H202-induced lens oxidative injury in vitro rat model was establish to observe the impact of gigantol combined with syringic acid on lens transparency under a dissecting microscope. D-galactose-induced cataract rat model was established to observe the impact of gigantol combined with syringic acid on lens transparency under a slit-lamp. UV spectrophotometry was adopted to detect the inhibitory activity of gigantol combined with syringic acid against AR. Molecular docking method was used to detect binding sites, binding types and pharmacophores of gigantol combined with syringic acid in prohibiting aldose reductase.

RESULT:

Both in vitro and in vivo experiments showed a good anti-sugar cataract activity in the combination of gigantol and syringic acid and a better collaborative effect than single component-gigantol and syringic acid and positive control drug Catalin. Molecular docking and dynamic simulation showed their collaborative AR-inhibiting amino acid residue was Asn160 and the major acting force was Van der Waals' force, which formed common pharmacophores.

CONCLUSION:

Gigantol combined with syringic acid shows good anti-cataract, their action mechanism is reflected in their good collaborative inhibitory effect on AR.

• Authors: Hongxing Diao, Yanqun Yi, Hui Qi, Xinxin Gao, Hua Fang, Xiaoyong Wei, Qiong Gu, Ling Wang, Zhengtao Wang, Lianquan Gu
• Journal: Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica (Zhongguo Zhong Yao Za Zhi) Vol. 37 Issue 16 Pg. 2429-34 (Aug 2012) ISSN: 1001-5302 [Print] China
• PMID: 23234143 (Publication Type: English Abstract, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Bibenzyls
• Gallic Acid
• gigantol
• Guaiacol
• syringic acid
• Aldehyde Reductase

Topics

• Aldehyde Reductase (antagonists & inhibitors)
• Animals
• Bibenzyls
• Cataract (drug therapy, enzymology)
• Drug Synergism
• Female
• Gallic Acid (analogs & derivatives, pharmacology)
• Guaiacol (analogs & derivatives, pharmacology)
• Humans
• In Vitro Techniques
• Lens, Crystalline (drug effects, enzymology)
• Male
• Rats
• Rats, Wistar