1297302-80-7Relevant academic research and scientific papers
Synthesis method of berberrubine ester substances
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Paragraph 0032-0039; 0038-0043; 0070-0074, (2020/12/30)
The invention discloses a synthesis method of berberrubine ester substances. The method comprises the following steps: using 4-dimethylaminopyridine as a catalyst and dicyclohexylcarbodiimide as a deacidifying agent, directly reacting berrubine with carboxylic acid in a certain solvent to generate the berrubine ester substances with bioactivity, reacting for 1.5-2 hours at the temperature of between 40 and 60 DEG C, basically finishing the reaction, filtering to remove solid substances while the reaction is hot, freezing overnight to separate out a target object, filtering, washing, drying andthe like to obtain a yellow crude product, and finally, separating the crude product by using a methanol dichloromethane column with the volume ratio of 1: 10, and further purifying the product to obtain the product. The yield of the product is 85.2%-93.4%, and the purity of the product is greater than 96%. Compared with traditional synthesis of berberrubine ester, the method has the advantages that the reaction yield is high, and the product is good in color and luster and high in purity; the method has the advantages of mild reaction conditions, short reaction time, fewer byproducts, accessible raw materials, simple operation, easy post-treatment and the like.
Synthesis of 9-substituted derivatives of berberine as anti-HIV agents
Bodiwala, Hardik S.,Sabde, Sudeep,Mitra, Debashis,Bhutani, Kamlesh Kumar,Singh, Inder Pal
, p. 1045 - 1049 (2011/04/18)
Naturally occurring protoberberine alkaloids, berberine and berberrubine along with 9-substituted derivatives of berberine were assessed for the anti-human immunodeficiency virus (HIV) activity. Berberine was found to be the most active compound with an EC50 of 0.13 μM against HIV-1 NL4.3 virus in CEM-GFP cell lines. Berberrubine and two other compounds were found to be less active than berberine, at the same time they were less toxic than berberine. Enzyme based assay suggested that the anti-HIV activity of berberine and its analogs might be due to RTase inhibitory activity and some additional mechanisms.
