Studies On Water-Solube Derivatives Of Celastrol And Studies On Quality Control And Antiinflammatory Of Shuluoshuanggan

Part 1 Study on Water-soluble Derivatives of CelastrolCelastrol , which having potent effects such as anti-oxygen, anti-inflammatory, sperm fertilizing ability depression, inhibition effect on neo-vasculanzationm, and etc, was isolated from root bark of Tripterygium wilfordii Hook, f., Celastrus orbiculatus Thumb., and etc. Recent studies showed that celastrol was a natural proteasesome inhibitor that had great potential for cancer prevention and treatment.Ring opening reaction, rearrangement reaction and other reactions would have occurred when celastrol was treated with acid. So, the reality is that celastrol was either incompletely or ineffectively absorbed after oral administration. Celastrol belonged to liposoluble triterpenoid. So it is impossible to prepare parenteral injection (celastrol in water). Water-soluble salts were always synthesized to improve solubility of such compounds, but unfortunately, which was hard for celastrol because of its poor stability with base. So it is difficult to synthesize water-soluble derivatives of celastrol by traditional neutralization reaction. In this paper, we are trying to find abnormal way to prepare water-soluble derivatives of celastrol, and suggestive of a promising enhancement on its therapeutic effect.In order to improve its solubility in wate, salts of celastrol were designed and synthesized from celastrol and meglumine, sodium bicarbonate, potassium bicarbonate, and sodium bisulfite, respectively. Sodium bisulfite derivative of celastrol was named NST-001, which is a good inhibitor on PC-3 mice-transplanted tumor.Part 2 Study on Quality Control and antiinflammatory of ShuluoshuangganScrophularia ningpoensis Hemsl., an indigenous plant, is cultivated as a medicinal plant in China. Its air dried roots are often used against fever, swelling, constipation, pharyngitis, neuritis and laryngitis in Chinese traditional medicine. Iridoid glycosides and phenylpropanoid glycoside are two main active components of Scrophularia ningpoensis Hemsl.. Shuluoshuanggan, which including iridoid glycosides and phenylpropanoid glycoside, is the effective fractions of Scrophularia ningpoensis Hemsl.. The representative composition of iridoid glycosides is harpagoside, and the representative compsition of phenylpropanoid glycoside is angoroside C. In our study, UV-spectrophotometry was established to determine the total phenylpropanoid glycoside, and angoroside C was used as the reference substance. Colorimetric method was established to determine the total iridoid glycosides, and harpagoside was used as the reference substance. The content of angoroside C and harpagoside were determined by HPLC.The results showed that the phenylpropanoid glycoside, iridoid glycosides in Shuluoshangdan were above 50% and 30%, respectively. The content of angoroside C and harpagoside were more than 25% and 20%, respectively, and the total content of angoroside C and harpagoside was more than 50%.