Rorifone

Chemical Properties

white or whitish crystalline powder. practically insoluble in water; slightly soluble in ether; freely soluble in ethyl acetate or chloroform; soluble in methanol and ethanol.

History

In the early 1970s of the last century in China, about 300 kinds of effective Chinese herbal medicines were explored for the treatment of chronic bronchitis, which was carried out as a national program. Rorifonum was obtained and developed under Rorifonum
this historical condition. Two crystals named rorifonum and rorifamide were obtained after studies on the chemical components of Rorippa Montana (Wall.) Small (hancai) by Shanghai Institute of Materia Medica. Using elemental analysis, spectral identification, and mass spectrometry, the chemical structure of these two compounds was finally determined. Rorifonum and rorifamide are the first discovered sulfone compounds with the effects of relieving cough and eliminating phlegm.
After a series of pharmacological studies, rorifonum had been proved effective in the expectorant and antibacterial experiments. Clinical trials also revealed that rorifonum has a certain effect of relieving cough and asthma. Synthetic compound of rorifonum and natural product have the same effects. However, the pharmacological effect of rorifamide was not obvious. Meanwhile, in order to find a new drug with higher efficacy and lower toxicity, the researchers synthesized a series of similar compounds, some of them showing significant expectorant activity in the animal models.

General Description

Rorifonum is an antichronic bronchitis sulfone derived from Rorippa(Rorippa Montana (Wall.) Small) which is distributed widely in China. The plant has been used as a folk medicine to relieve cough and asthma and also as a mucolytic agent. The results of clinical trials in Shanghai showed that the water decoction of Rorippa Montana (Wall.) Small (hancai) had a certain effect in some kind of chronic bronchitis.

Pharmacology

The pharmacological studies of rorifonum were unsystematic and the specific mechanism was unknown. At present, only a few pharmacological experiments were carried out including acute toxicity test, subacute toxicity test, expectorant test, antitussive experiment, and antibacterial experiment. The expectorant test with phenol red in mice showed rorifonum had the effect of expectorant, while the antitussive experiment by sulfur dioxide showed there was no obvious effect.

Clinical Use

Rorifine is mainly used for the treatment of patients with chronic bronchitis at protraction stage. At this stage, the effect of a single drug is weak and should be used in combination with other drugs. At present, the clinical application of rorifonum has been reduced.