946576-30-3Relevant academic research and scientific papers
9-O-butyl-13-(4-isopropylbenzyl)berberine, KR-72, is a potent antifungal agent that inhibits the growth of Cryptococcus neoformans by regulating gene expression
Bang, Soohyun,Kwon, Hyojeong,Hwang, Hyun Sook,Park, Ki Duk,Kim, Sung Uk,Yong,Bahn
, (2014)
In this study we explored the mode or action of KR-72, a 9-O-butyl-13-(4-isopropylbenzyl)berberine derivative previously shown to exhibit potent antifungal activity against a variety of human fungal pathogens. The DNA microarray data revealed that KR-fl treatment significantly changed the transcription profiles of C. neoformans, affecting the expression of more than 2,000 genes. Genes involved in translation and transcription were mostly upregulated, whereas those involved in the cytoskeleton, intracellular trafficking, and lipid metabolism were downregulated. KR-fl also exhibited a strong synergistic effect with the antifungal agent FK506. KR-72 treatment regulated the expression of several essential genes, including ECM16, NOP14, HSP10 and MGE1, which are required for C. neoformans growth. The KR-72-mediated induction of MGEI also likely reduced the viability of C. neoformons by impairing cell cycle or the DNA repair system. In conclusion, KR-fl showed antifungal activity by modulating diverse biological processes through a mode of action distinct from those of clinically available antifungal drugs such as polyene and azole drugs.
Berberrubine Derivatives Having Antifungal Activities
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Page/Page column 12-13, (2010/12/18)
The present invention relates to a berberrubine derivative having superior antifungal activity, more particularly to a berberrubine derivative having inhibitory activity against chitin synthase, which participates in the synthesis of chitin and is essenti
Synthesis and antifungal activity of a novel series of 13-(4- isopropylbenzyl)berberine derivatives
Park, Ki Duk,Cho, Sung Jin,Moon, Jae Sun,Kim, Sung Uk
supporting information; experimental part, p. 6551 - 6554 (2010/12/19)
By replacing the methyl group of 13-(4-isopropylbenzyl)berberine 2 with various acyl, alkyl, and benzyl groups via the demethylated intermediate, 13-(4-isopropylbenzyl)berberrubine 4, a novel series of 9-O-alkyl-13-(4- isopropylbenzyl)berberine derivatives was synthesized and examined for antifungal activities against various human pathogenic fungi. The introduction of various alkyl groups led to enhanced antifungal activity but that of acyl groups resulted in decrease of the activity. Among them, 9-O-butyl-13-(4- isopropylbenzyl)berberine 6d exhibited the most potent antifungal activities against Cryptococcus neoformans, Candida species (MIC = 0.25-1 μg/ml), and Aspergillus species (MIC = 2-4 μg/ml). The compound was found to be relatively safe up to 900 mg/kg in oral administration to mice.
