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A Water-Soluble prodrug for the Heat Shock-inducing compound Withaferin A

详细技术说明
None
*Abstract
The Whitehead Institute is seeking a licensee for the invention ΓÇ£A Water-Soluble prodrug for the Heat Shock-inducing compound Withaferin AΓÇØ. This invention describes the discovery and characterization of a new compound, 2,3-dihydrowithaerin-A-3├ƒ-O-sulfate, isolated from the medicinal plant Withania somnifera. The invention also provides a method for the production of large quantities of biologically active withanolide in an efficient, well-controlled and ecologically friendly manner. The new compound is easily converted into Withaferin A, known to inhibit cancer cell proliferation/survival and aggregation of F-actin filament, induce the cellular heat shock response, and exhibit neuroprotective activity in cell culture models of HuntingtonΓÇÖs disease. The methods provide a water soluble alternative to Withaferin A, which currently requires formulation in a complex emulsifying vehicle, and retention of characteristic bioactivities. The new compound described here is useful as a readily formulated prodrug of Withaferin A for enteral or parenteral administration in the treatment of cancers, neurodegenerative disorders, and inflammatory processed or pathological neoangiogensis.
国家/地区
美国

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