Abstract
To obtained natural products with remarkable antibacterial activities, three 3-amino substituted (UA) derivatives 2, 3 and 4 were designed and synthesized, and their antibacterial activity were assayed using broth microdilution method. Compared to UA, there three derivatives present higher antimicrobial activities against methicillin-resistant Staphylococcus aureus (MRSA) with the minimum inhibitory concentrations of 16 to 32 μg/mL. Furthermore, their cytotoxicities to human hepatoma cell (BEL-7402) were evaluated using MTT method, and the results indicated that their derivatives had no toxicity (IC50 value was larger than 10 μM), while UA presented a certain cytotoxicity.
Highlights
Ursolic acid (UA), a pentacyclic triterpene, is widely distributed in various plants (Chen L 2011)
A new derivative (Zhang et al 2006) of phenylalanine on the carboxyl group of C-28 was synthesized, and presented remarkable inhibitory activity against PTP1B enzyme compared with UA
Li W et al (2018) synthesized a novel UA derivative using a nitrogen-containing heterocyclic scaffold and a privileged fragment at the C-28 position the derivative significantly repressed the proliferation of the breast cancer (BC) SUM149PT and HCC1937 cells in a dose-dependent manner, and exhibited decreased cytotoxicity compared with vehicle-treated cell lines
Summary
Ursolic acid (UA), a pentacyclic triterpene, is widely distributed in various plants (Chen L 2011). To obtain more efficient bioactivities, many derivatives at C-3 and C-28 positions of UA were designed and synthesized. Deng et al (2007) designed and synthesized a series of α-aminophosphonate conjugates of 3-O-βacetyl UA, some of them have significant anti-HIV activity and no cytotoxicity on HT-29 cells (human colon adenocarcinoma cell line).
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