Applications of pegylated curcumin derivative
A technology of pegylated curcumin and derivatives, which can be applied to medical preparations containing active ingredients, digestive systems, drug combinations, etc., can solve problems such as low oral availability, limited clinical application, and insolubility of curcumin in water.
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Embodiment 1
[0031] Example 1: Synthesis and Characterization of Pegylated Curcumin Derivatives
[0032] With reference to Chinese patent CN102134312A, a brief preparation method is provided. Taking curcumin and short-chain polyoxyethylene (Mr=400~800Da) as an example, the preparation process includes the following two simple steps: (1) β-mercaptopropionic acid and curcumin Reaction generates curcumin (Curc-SH) with mercapto end; (2) Michael addition reaction occurs between curcumin with mercapto end and monomethoxypolyoxyethylene acrylate to generate the amphiphilic curcumin compound shown in I .
[0033] Specifically, taking the polyethylene glycol curcumin derivative (Curc-mPEG454) shown in structure II as an example, curcumin and two short-chain polyethylene glycol monomethyl ether acrylates are combined through a β-mercaptopropionate bond. (Mr=454Da) connected, the structure is shown as II, its synthesis method and characterization refer to patent CN102134312A and patent US2012 / 00031...
Embodiment 2
[0041] Example 2: Effects on Lipid Metabolism and Hepatic Steatosis in C57BL / 6 Mice Induced by High Fat Diet
[0042] 1. Experimental method:
[0043] Choose 8-week-old male C57BL / 6 mice, 10 per group, and randomly divide them into four groups: (1) control group (Control): normal diet D12450B+normal saline, (2) high-fat group (HFD): high-fat diet D12492+ Normal saline, (3) high-fat group+curcumin derivative low-dose treatment group (50mg / kg, Curc-mPEG454), (4) high-fat group+curcumin derivative high-dose treatment group (100mg / kg, Curc- mPEG454), intraperitoneally injecting the corresponding drug once every other day, and after 16 weeks, the HITACHI 7600 automatic biochemical analyzer detected the levels of TG, TC, HDL-C, LDL-C and FFA in the blood, alanine aminotransferase (ALT) and aspartate aminotransferase ( AST), and HE staining to observe the changes of mouse liver tissue structure and lipid deposition. The data were analyzed using SPSS17.0 software, paired t-test was ...
Embodiment 3
[0073] Example 3: To high cholesterol diet C57BL / 6 and ApoE - / - Effects on lipid metabolism and antiatherosclerotic effects in knockout mice.
[0074] 1. Experimental method:
[0075] Selection of 8-week-old male C57BL / 6 and ApoE - / - Gene knockout mice were randomly divided into five groups: (1) C57BL / 6 normal diet group + normal saline group, (2) ApoE - / - Normal diet + normal saline group, (3) ApoE - / - Normal diet + Curc-mPEG45450mg / kg group, (4) ApoE - / - High cholesterol (D12109C) + normal saline group, (5) ApoE - / - High cholesterol (D12109C)+Curc-mPEG454 50mg / kg group, 6 rats in each group, intraperitoneal injection once every other day, after 12 weeks of continuous treatment, the levels of TG, TC, HDL, LDL and FFA in serum were measured, HE and oil red O Staining was used to observe the changes in mouse liver tissue structure and lipid deposition, frozen sections of mouse aortic root, and HE staining were used to observe and measure the histological characteristics an...
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