Abstract
There is an urgent need for a water-soluble derivative of astragaloside IV for drug R&D. In the present study, a remarkably simple method for the preparation of such a water-soluble derivative of astragaloside IV has been developed. This protocol involves oxidative 2,2,6,6-tetramethylpiperidine-1-oxyl free radical (TEMPO)-mediated transformation of astragaloside IV to its carboxylic acid derivative, which is a new compound named astragalosidic acid. The structure of astragalosidic acid was elucidated by means of spectroscopic analysis. Its cardioprotective activity was investigated using an in vitro model of cardiomyocyte damage induced by hypoxia/reoxygenation in H9c2 cells. The oxidative TEMPO-mediated transformation proposed in the present study could be applied to other natural saponins, offering an effective and convenient way to develop a new compound with greatly improved structure-based druggability.
Highlights
IntroductionAstragali Radix is a well-known herbal drug in traditional Chinese medicine which has been used to treat numerous diseases for hundreds of years
Astragali Radix is a well-known herbal drug in traditional Chinese medicine which has been used to treat numerous diseases for hundreds of years.To date, more than 200 kinds of traditional Chinese medicine patent prescription containing Astragali Radix extract have been approved by the China Food and Drug Administration
More than 200 kinds of traditional Chinese medicine patent prescription containing Astragali Radix extract have been approved by the China Food and Drug Administration
Summary
Astragali Radix is a well-known herbal drug in traditional Chinese medicine which has been used to treat numerous diseases for hundreds of years. More than 200 kinds of traditional Chinese medicine patent prescription containing Astragali Radix extract have been approved by the China Food and Drug Administration. Despite its well-documented pharmacological effects [2,3], the druggability of astragaloside IV, related to its characteristics of solubility, dissolution, and gastrointestinal permeability, has always attracted research interest. Poor water solubility and poor dissolution in the gastrointestinal fluids of astragaloside IV is a limiting factor to in vivo bioavailability [4,5]. There is an immediate need for a water-soluble derivative of astragaloside IV using a low-cost preparation method in drug R&D
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