Intravenous emulsions of triptolide as immunomodulators and anticancer agents
A technology of triptolide and emulsion, which is applied in the direction of antineoplastic drugs, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of increasing the susceptibility of patients
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[0045] Triptolide analogs for screening can be generated by combinatorial chemistry or other types of preparation methods, resulting in various chemical structures or substituents.
[0046] The active ingredient in the formulation is triptolide or a triptolide derivative, as described below. For example, this patent publication provides compounds of structure I:
[0047]
[0048] in
[0049] each R 6 independently selected from alkyl, alkenyl, alkynyl or aryl;
[0050] CR 2 R 3 is CHOH or C=O;
[0051] At most one of the X groups is hydroxyl and the remaining X groups are hydrogen.
[0052] In some embodiments of Structure I, CR 2 R 3 It is CHOH, which usually contains a para-hydroxy structure. In some embodiments, each X is hydrogen; however, in selected embodiments, exactly one of the represented groups X is hydroxyl. Positions of hydroxyl substitution typically include carbon 2 and carbon 16, as indicated in the numbering scheme above.
[0053] In some embodim...
example 1
[0173] emulsion preparation
[0174] Emulsion components include tricaprylin (g) 20%; soybean oil (g) 20%; phospholipids ([60%] L-α-lecithin, L-lecithin, σ61755) (g) 2%; Sodium (g) 0.2%; Glycerin (g) 2.5%; Water (ml) 55%
[0175] Emulsion formulation containing PG796 (MRx102)
[0176] 1. Weigh tricaprylin, soybean oil and phospholipid (L-lecithin), and put them into a 15mL conical plastic centrifuge tube or a suitable test tube (for example, use a plastic test tube to avoid breakage).
[0177] 2. Place the test tube over the bottom of the sonicator probe so that the tip of the sonicator is approximately 5 mm from the bottom of the test tube and the probe does not touch the side of the test tube. Clip it in place. Do not use cold water baths at this stage.
[0178] 3. Set the power level of the ultrasound generator to just below the microprobe limit with a 50% duty cycle. Turn on the sonicator for 20 seconds.
[0179] 4. Touch the test tube to assess its temperature, and ...
example 2
[0296] Cytotoxicity (MTT) test
[0297] Test compounds can be dissolved in DMSO at a concentration of 20 mM. Further dilutions can be done in RPMI1640 medium (GIBCO, Rockville, MD) supplemented with 10% fetal bovine serum (HyClone Laboratories, Logan, UT).
[0298] Cytotoxicity of compounds was determined in a standard MTT assay using Cell Proliferation Kit I (#1465007, Roche Diagnostics, Mannheim, Germany). Briefly, human T-cell lymphoma (leukemia) cells (4x10 5 ) were cultured in 96-well tissue culture dishes for 24 hours. The medium was then supplemented with 10 μl / well of MTT reagent for 4 hours, and then 0.1 ml / well of solubilizing reagent was added for another 16 hours. 570 nm (OD) was measured on a ThermoScan microplate analyzer (Molecular Devices, Menlo Park, CA). 570 ) at the optical density.
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