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To our knowledge, the present study is not only the first report describing the biotransformation of celastrol, but also the first one detailing a new compound, celastrol-29-O-β-glucoside, that is generated in the biotransformation process. Moreover, celastrol-29-O-β-glucoside may serve as a potential candidate in the future medicine application due to its higher water solubility and lower toxicity. Hypospadias is the second most common congenital malformation in males. Although the aetiology of hypospadias is not clear, it is generally