SYNTHESIS OF CURCUMIN DERIVATIVES - Scribd

All compounds had stronger inhibitory effects than curcumin as determined by the MTT assay except IND-3 in lung cancer H1299 cells. Among the seven curcumin-related compounds tested, IND-4 exhibited exceptionally potent inhibitory effects on the growth of cultured PC-3, BxPC-3, HT-29 and H1299 cells. The IC50 for this compound was ≤1 µM in all four cell lines, indicating that IND-4 was approximately 20-fold more active than curcumin. As shown in , the IC50 values of all seven curcumin-related compounds ranged from 0.64 to 18.94 µM in the four cancer cell lines studied.

CAVACURMIN® is manufactured using a 95%, low-VOC (volatile organic compounds) curcumin extract.

CAVACURMIN® is a physical mixture of gamma-cyclodextrin and a 95% turmeric () extract (not just curcumin). Gamma-cyclodextrin is a non-allergenic, vegetarian oligosaccharide used as hydrophilic carrier to improve the bioavailability of the water-insoluble curcuminoids, especially curcumin, by a factor greater than 40.


05/01/2018 · SYNTHESIS OF CURCUMIN DERIVATIVES

[11] Ammon HP, et al, Mechanism of antiinflammatory actions of curcumine and boswellic acids.

Curcuminoids are substances of great interest because of their important pharmacological activities, particularly anti-inflammatory, anticarcinogenic, and anti-Alzheimer’s activities. In this study, we report the first procedure and effect of processing for the high, efficient, and useful purification of curcumin, demethoxycurcumin, and bisdemethoxycurcumin from turmeric powder. Purification involves high-speed countercurrent chromatographic (HSCCC) separation of these curcuminoids using a simple two-phase solvent system composed of -hexane/chloroform/methanol/water (5/10/7.5/2.5, v/v). The HSCCC-fractionated effluent peaks indicated that the peak resolutions were 1.7 between curcumin and demethoxycurcumin and 2.1 between demethoxycurcumin and bisdemethoxycurcumin for 25 mg of loaded turmeric powder. These purified substances were analyzed by liquid chromatography−tandem mass spectrometry with scan and daughter scan negative modes, and the wide absorbance from 200 to 500 nm was monitored by photodiode array detection. The separation yielded 1.1 mg of curcumin, 0.6 mg of demethoxycurcumin, and 0.9 mg of bisdemethoxycurcumin (>98% purity). Moreover, the antioxidant effect of curcuminoids was measured by a 1,1-diphenyl-2-picrylhydrazil assay. The order of antioxidant activity was purified curcumin > purified demethoxycurcumin > purified bisdemethoxycurcumin > turmeric powder. Curcumin, demethoxycurcumin, and bisdemethoxycurcumin can be used for various evaluations of their pharmacological activities.


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The relative absorption of CAVACURMIN® was compared to standard 95% curcumin extract and two leading commercial products claiming to have enhanced bioavailability in a clinical setting.

Degradation of Curcumin: From Mechanism to …

Curcumin is the main bioactive ingredient in turmeric extract and widely consumed as part of the spice mix curry or as a dietary supplement. Turmeric has a long history of therapeutic application in traditional Asian medicine. Biomedical studies conducted in the past two decades have identified a large number of cellular targets and effects of curcumin. In vitro curcumin rapidly degrades in an autoxidative transformation to diverse chemical species, the formation of which has only recently been appreciated. This paper discusses how the degradation and metabolism of curcumin, through products and their mechanism of formation, provide a basis for the interpretation of preclinical data and clinical studies. It is suggested that the previously unrecognized diversity of its degradation products could be an important factor in explaining the polypharmacology of curcumin.

Degradation of Curcumin: From Mechanism to Biological Implications

12 individuals (fasted overnight) were given three different bioavailable curcumin preparations and standard curcumin orally – with a one-week washout period in between the four formulations. After product intake, blood was drawn hourly for 12 hours and analyzed (spiked plasma samples). Blood concentration and the relative absorption of curcumin and its derivatives were determined.

From Mechanism to Biological Implications

CAVACURMIN® was around 40 times more efficiently absorbed compared to pure curcumin powder and some leading commercial curcumin supplement products. The highly superior performance of CAVACURMIN® was demonstrated by the fact that the curcumin uptake was at least 4.6 times higher than the next-best commercial curcumin formulation in this clinical study (see graphs 1 and 2).