Anti-inflammatory modalities
a technology of inflammatory modalities and iodine, which is applied in the direction of drug compositions, immunological disorders, metabolism disorders, etc., can solve the problems of cholestosis, liver failure, and no existing therapy is without significant side effects, and achieves the effect of abstaining from cardiovascular side effects
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Synthetic Methods for Substituted Isoflavanones and Isoflavan-4-ols
Condensation of 2-bromoresorcinol with 4-hydroxyphenylacetic Acid
Synthesis of 1-(3-bromo-2,4-dihydroxyphenyl)-2-(4-hydroxyphenyl)-ethanone
[0124]
[0125]Borontrifluoride diethyl etherate (30 ml) was added to a mixture of 2-bromoresorcinol (5.0 g, 26 mmoles) and 4-hydroxyphenylacetic acid (3.0 g, 26 mmoles) in a round bottom flask fitted with a condenser and a magnetic stirrer. The mixture was heated at 100-110° C. for one and a half hour with stirring. The mixture was then cooled to room temperature and kept in a freezer overnight. The precipitated solid was filtered and recrystallised from ethanol to give deoxybenzoin as off-white crystals. The crystals were then collected and dried in a desiccator.
[0126]1H NMR (CDCl3): δ 4.16 (s, 2H, CH2), 6.61 (d, 1H, J 9.0 Hz, ArH), 6.80 (d, 2H, J 8.6 Hz, ArH), 7.12 (d, 1H, J 8.6 Hz, ArH), 7.75 (d, 1H, J 9.0 Hz, ArH).
[0127]Yield: 5.2 g, 69%
Cyclisation of 1-(3-bromo-2,4-dihydroxyphen...
experiment 1
[0179]Either vehicle (PEG 400:PBS1:1) Compounds 1 or 4 were administered at a dose rate of 1 mg / kg throughout the experiment until the mice were killed at day 17. Both compounds decreased colitis. In this assay, Compound 1 offered the better anti-inflammatory activity (based on a reduction in colonic ulceration, a delay in the onset of clinical signs, a reduction in the clinical score, a reduction in the occurrence and severity of clinical signs, reduced body weight loss and reduced time to recovery) than Compound 2.
[0180]The mean histology scores are shown FIG. 5, suggesting less colitis in those mice treated with Compounds 1 and 4. There was statistically significant (p=0.0135) less ulceration of the colonic epithelium from those mice given Compound 1 compared with those given vehicle alone.
[0181]The colonic inflammation induced by ingestion of DSS causes shortening of the colon, and thus protection conferred by test agents might be evidenced by a reduction in this shortening. The...
experiment 2
[0184]Either Compounds 1 and 2, at a dose of 1 mg / kg or vehicle were administered for 10 days prior to DSS being added to the drinking water to induce colitis, after which test compound was stopped. DSS was administered for 5 days and the mice killed 8 days later (day 23). Inflammation was reduced by both compounds, even though they were administered only prior to but not during its induction. See FIG. 9.
[0185]The amount and severity of mucosal ulceration was greater in the vehicle-treated group, but not significantly so.
[0186]Whilst there was a trend, there were no significant differences in colon length between either of the test groups and vehicle. There was a significant difference between the colon lengths of the mice which were not given DSS and vehicle group (p=0.0414). However, the colons of the Compound 1-treated groups were not statistically different in length from those of the control group, suggesting that Compound 1 protected against the inflammatory effects of DSS ing...
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