- Synthesis and evaluation of butein derivatives for in vitro and in vivo inflammatory response suppression in lymphedema
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Herein, we demonstrate that butein (1) can prevent swelling in a murine lymphedema model by suppressing tumor necrosis factor α (TNF-α) production. Butein derivatives were synthesized and evaluated to identify compounds with in vitro anti-inflammatory activity. Among them, 20 μM of compounds 7j, 7m, and 14a showed 50percent suppression of TNF-α production in mouse peritoneal macrophages after lipopolysaccharide stimulation. Compound 14a, exhibited the strongest potency with an in vitro IC50 of 14.6 μM and suppressed limb volume by 70percent in a murine lymphedema model. The prodrug strategy enabled a six-fold increase in kinetic solubility of compound 1 and five-fold higher levels of active metabolite in the blood for compound 14a via oral administration in the pharmacokinetics study. We suggest that the compound 14a could be developed as a potential therapeutic agent targeting anti-inflammatory activity to alleviate lymphedema progression.
- Kang, Hee,Ku, Jin-Mo,Lee, Jung-hun,Lee, Sukchan,Park, Kye Won,Roh, Kangsan,Song, Youngju
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- USE OF THE EXTRACT OF CAESALPINIA SAPPAN L. AND COMPOUNDS THEREFROM
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The present invention relates to an extract of Caesalpinia sappan L. having an angiogenesis inhibition activity and a use of the compound isolated therefrom, more precisely an extract of Caesalpinia sappan L. extracted by using water, alcohol or a mixture thereof , and a use of brazilin, sappanchalcone and brazilein isolated from the extract as an angiogenesis inhibitor. The extract of Caesalpinia sappan L. of the invention and a compound isolated therefrom have angiogenesis inhibition activity, so that they can be effectively used for the prevention and treatment of angiogenesis associated diseases such as vascular diseases, cardiovascular diseases, ophthalmic diseases, chronic inflammatory diseases, dermatological diseases, Alzheimer's disease, obesity and cancer.
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Page/Page column 26-27
(2008/06/13)
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