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Boldine synthesis essay - Rota Patent
Fluorescent N-doped carbon dots (CDs) were derived from dried shrimps and rationally fabricated as a traceable drug delivery system for the targeted delivery of boldine to human breast cancer cells (MCF-7 cells). The MCF-7 cells were used to evaluate the anticancer ability of the boldine-loaded CDs. The CDs served as fluorescent carriers that simultaneously tracked and released the drug. The boldine release was triggered upon acidification of the intracellular vesicles, in which the carriers were located after their uptake by cancer cells, and there was further enhancement in the uptake of the boldine-loaded fluorescent CDs by the cancer cells. The synthesized blank CDs were also used as fluorescent probes for the imaging of SH-SY5Y (human neuroblastoma) cells and have potential applications in bioimaging and related fields. These results demonstrate the feasibility of using CDs as a traceable drug delivery system with the ability to deliver boldine drug into the target cells.
shows the antioxidant activity (expressed as Trolox equivalent activity capacity, TEAC) of synthesized compounds L5, L6, 1, and 2 at 1mM concentration in the FRAP assay compared to the natural precursor boldine (L1), the commercial drug oxaliplatin, and the commercial antioxidant BHT.
Tropical Plant Database File for Boldo - Peumus boldus
Four phenanthrene and one aporphine alkaloids semi-synthesized from boldine were evaluated for their inhibitory effect on reactive oxygen species (ROS) generation. ROS generation by neutrophils stimulated with -formyl-methionyl-leucyl-phenylalanine was inhibited in a concentration dependent manner. Alkaloids exerted similar inhibitory effect in the hypoxanthine–xanthine oxidase system than in stimulated neutrophils, which could be attributed to a direct ROS scavenging activity. None of the alkaloids assayed had any effect on xanthine oxidase activity. Therefore the synthesized alkaloids might constitute an alternative therapy in inflammation disorders in which ROS generation is involved.
The antioxidant activity of boldine (L1) and the 3-carboxyboldine (L5·HCl) and 3-carboxypredicentrine (L6·HCl) synthesized derivatives was investigated to compare the radical scavenger properties of the derivatives with the natural precursor. In addition, platinum(II) coordination compounds 1 and 2 were also tested to evaluate their antioxidant activity upon boldine derivative coordination. shows the antioxidant activity (expressed as IC50 values) of these compounds in the DPPH assay. For comparison, also includes the results for the commercial drug oxaliplatin and the commercial antioxidant Trolox.
Promising developments include the synthesis of picoplatin, ..
“A novel alkaloid antioxidant, Boldine and synthetic antioxidant, reduced form of RU486,inhibit the oxidation of LDL and atherosclerosis in LDLR(-/-) mice.” 2004 Apr; 173(2):203-10.
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