Antioxidant, Metabolic And Antitumor Activity Of Triterpenoids Combination With Cytostatics

Objective: To study the effect of betulin derivatives combination with 5-fluorouracil or hydrazine sulfate on the ROS generation, the SOD and LDH activity using rat blood, as well as the effect of combination drugs on Ehrlich carcinoma in experiments on mice. Methods: We used a chemiluminescence technique to study the ROS generation, and spectrophotometry to determine the MDA level and the SOD and LDH activity. The model of transplanted Ehrlich ascites carcinoma was investigated on mice using a cytological analysis of ascitic fluid cells according to Pappenheim`s method. Results: In vitro experiments on rat blood at the doses of 2, 5 and 10 μg per ml revealed the dose-dependent effect of combination drugs on the antioxidant properties. In plasma, the ROS generation and the MDA level increased by 10-300% in comparison with control at the doses of 5 and 10 μg per ml only. Still, the SOD and LDH activity in general increased by 10-130% in comparison with control under the action of the studied combination drugs. The study on mice showed the effectiveness of a combination of triterpenoids and cytostatics in Ehrlich ascites carcinoma therapy. The state and behavior of the animals improved, the volume of ascites fluid decreased by 40-50% after treatment for 10 d. Conclusion: The combination of betulin derivatives with cytostatics can be used as antitumor drugs in Ehrlich ascites carcinoma therapy that is due to metabolic plasticity, increased ROS generation in enhanced antioxidant enzyme protection.

A new triterpenoid isolated from fruits of Liquidambaris Fructus / 中草药

Objective: To study the chemical constituents from Liquidambaris Fructus (fruits of Liquidambar formosana). Methods: The constituents were isolated and purified by preparative TLC and silica gel, Sephadex LH-20, and ODS column chromatography, and their structures were elucidated on the basis of their physicochemical properties and spectral data. Results: Seven compounds were obtained from 70% ethanol extract of the fruits of Liquidambaris Fructus and identified as 11α-methoxyl-28-nor-β-amyrenone (1), 28-nor-β-amyrenone (2), 3-oxo-12α-hydroxy-oleanan-28, 13β-olide (3), 3α-acetoxyl-25-hydroxy-olean-12-en-28-oic acid (4), erythodiol (5), betulonic acid (6), and styracin (7), respectively. Conclusion: Compound 1 is a new triterpenoid named liquidaformone A, and compounds 5 and 7 are isolated from the plants of Liquidambar Linn. for the first time.

Chemical constituents in roots of Ilex cornuta / 中草药

Objective: To study the chemical constituents of the roots of Ilex cornuta. Methods: The compounds were isolated and purified by silica gel, Sephadex LH-20, medium pressure column chromatography, and semi-preparative liquid chromatography, and their structures were elucidated by chemical properties and spectroscop analyses. Results: Eight compounds were isolated and their structures were identified to be β-sitosterol (1), lupeol (2), betulonic acid (3), hede-ragenin (4), 3β-acetoxy-28-hydroxyurs-12-ene (5), ursolic acid (6), 19α-hydroxy ursolic acid (7), 3β-acetoxy-ursolic acid (8), 23-hydroxyl-methyl ursolate (9), heptanoic acid (10), β-daucosterol (11). Conclusion: Compounds 4,5,8, and 9 are obtained from this genus for the first time, and compound 3 is obtained from this plant for the first time.