914394-75-5Relevant academic research and scientific papers
Curcumin glucuronides: Assessing the proliferative activity against human cell lines
Pal, Ashutosh,Sung, Bokyung,Bhanu Prasad, Basvoju A.,Schuber Jr., Paul T.,Prasad, Sahdeo,Aggarwal, Bharat B.,Bornmann, William G.
, p. 435 - 439 (2014)
A gram scale synthesis of the glucuronide metabolites of curcumin were completed in four steps. The newly synthesized curcumin glucuronide compounds 2 and 3 along with curcumin 1 were tested and their anti-proliferative effects against KBM-5, Jurkat cell, U266, and A549 cell lines were reported. Biological data revealed that as much as 1 μM curcumin 1 exhibited anticancer activity and almost 100% cell kill was noted at 10 μM on two out of four cell lines; while curcumin mono-glucuronide 2 as well as di-glucuronide 3 displayed no suppression of cell proliferation.
No-carrier-added radiohalogenations utilizing organoboranes: The synthesis of iodine-123 labeled curcumin
Kabalka, George W.,Yao, Min-Liang
, p. 1638 - 1641 (2009)
The use of organoborane intermediates for radiohalogenations is briefly reviewed. The synthesis of an iodine-123 labeled curcumin derivative using a newly developed radio-iodination technique is reported.
Curcumin-4-OCH2CO2H strontium, and synthesis, activity and application thereof
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Paragraph 0012; 0016; 0017, (2020/12/30)
The invention discloses curcumin-4-OCH2CO2H strontium, a preparation method of curcumin-4-OCH2CO2H strontium, anti-osteoporosis activity of curcumin-4-OCH2CO2H strontium, and application of curcumin-4-OCH2CO2H strontium in preparation of anti-osteoporosis medicines.
Novel curcumin analogue, preparation method and application thereof
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Paragraph 0095-0097, (2019/10/01)
The invention relates to a novel curcumin analogue. The analogue is obtained by modifying curcumin with a substituent common in natural products. Specifically, the general structural formula of the analogue is shown as the specification, wherein R1 and R2
DRUG COMPOSITION FOR PARENTERAL ADMINISTRATION
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Page/Page column 0031; 0032, (2019/05/16)
Provided is a curcumin pharmaceutical preparation that is highly water soluble, can maintain the concentration of free curcumin in the blood sufficiently high by being administered parenterally, can effectively obtain a pharmacological action of curcumin,
Design, synthesis, and evaluation of curcumin analogues as potential inhibitors of bacterial sialidase
Kim, Bo Ram,Park, Ji-Young,Jeong, Hyung Jae,Kwon, Hyung-Jun,Park, Su-Jin,Lee, In-Chul,Ryu, Young Bae,Lee, Woo Song
, p. 1256 - 1265 (2018/08/28)
Sialidases are key virulence factors that remove sialic acid from the host cell surface glycan, unmasking receptors that facilitate bacterial adherence and colonisation. In this study, we developed potential agents for treating bacterial infections caused by Streptococcus pneumoniae Nan A that inhibit bacterial sialidase using Turmeric and curcumin analogues. Design, synthesis, and structure analysis relationship (SAR) studies have been also described. Evaluation of the synthesised derivatives demonstrated that compound 5e was the most potent inhibitor of S. pneumoniae sialidase (IC50 = 0.2 ± 0.1 μM). This compound exhibited a 3.0-fold improvement in inhibitory activity over that of curcumin and displayed competitive inhibition. These results warrant further studies confirming the antipneumococcal activity 5e and indicated that curcumin derivatives could be potentially used to treat sepsis by bacterial infections.
Synthesis and characterization of 18F-labeled hydrazinocurcumin derivatives for tumor imaging
Shin, Sarah,Koo, Hyun-Jung,Lee, Iljung,Choe, Yearn Seong,Choi, Joon Young,Lee, Kyung-Han,Kim, Byung-Tae
, p. 96733 - 96745 (2015/11/24)
Fluorine-substituted hydrazinocurcumin derivative 1 and its dimethyl-substituted form at the C2 and C6 positions (2) were synthesized and their radiolabeled forms, [18F]1 and [18F]2, were evaluated for tumor imaging. In vitro and in vivo metabolism studies showed that the two radioligands were resistant to reductive metabolism, probably due to the presence of a pyrazole ring. In cellular uptake studies, [18F]1 and [18F]2 exhibited comparable uptake by human umbilical vascular endothelial cells and rat C6 glioma cells. Inhibition of radioligand uptake to a similar extent by HC and curcumin suggests that these radioligands may share the same binding sites as those for HC and curcumin. Positron emission tomography imaging of C6 glioma xenografted mice acquired 30 and 60 min after radioligand injection showed that [18F]2 had markedly higher tumor uptake than [18F]1, which was consistent with biodistribution data (3.20 ± 0.35% ID per g vs. 0.98 ± 0.31% ID per g, respectively). However, the two radioligands showed similar levels of tumor-to-background uptake ratio, except for the significantly higher uptake of [18F]1 by the small intestine, indicating its more rapid clearance. The results of this study will guide further structural modifications of these radioligands to enhance tumor-to-background uptake ratios.
"Clicked" bivalent ligands containing curcumin and cholesterol as multifunctional Aβ oligomerization inhibitors: Design, synthesis, and biological characterization
Lenhart, James A.,Ling, Xiao,Gandhi, Ronak,Guo, Tai L.,Gerk, Phillip M.,Brunzell, Darlene H.,Zhang, Shijun
scheme or table, p. 6198 - 6209 (2010/11/02)
In our effort to develop multifunctional compounds that cotarget beta-amyloid oligomers (AβOs), cell membrane/lipid rafts (CM/LR), and oxidative stress, a series of bivalent multifunctional Aβ oligomerization inhibitors (BMAOIs) containing cholesterol and curcumin were designed, synthesized, and biologically characterized as potential treatments for Alzheimer's disease (AD). The in vitro assay results established that the length of spacer that links cholesterol and curcumin and the attaching position of the spacer on curcumin are important structural determinants for their biological activities. Among the BMAOIs tested, 14 with a 21-atom-spacer was identified to localize to the CM/LR of human neuroblastoma MC65 cells, to inhibit the formation of AβOs in MC65 cells, to protect cells from AβOs-induced cytotoxicity, and to retain antioxidant properties of curcumin. Furthermore, 14 was confirmed to have the potential to cross the blood-brain barrier (BBB) as demonstrated in a Caco-2 cell model. Collectively, these results strongly encourage further optimization of 14 as a new hit to develop more potent BMAOIs.
