Women, Green approch for the synthesis of bioactive steroid derivatives

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Abstract

Cortisone is a naturally-occurring corticosteroid metabolite that is also used as a pharmaceutical prodrug. The corticosteroids market is expected to witness a CAGR of 4.3%, during the period 2020-2025. Cortisone is very well known for its therapeutic effects but due to its numerous side effects, especially in prolonged and high-dose therapies, the development of the pharmaceutical industry is currently aimed at finding new compounds with similar activities but with minor or no side effects so the main aim of the research has been to develop new drugs with better therapeutic activities while trying to obtain a decrease in the side effects that derive from their use. Biotransformations are an important methodology toward more sustainable industrial processes according to the principles of “green chemistry”.

In this work we have focused the attention on the biotransformation of cortisone with Rhodococcus rhodnii strain as two completely new compounds were obtained. Studies on in vitro biological activity of these molecules have shown that both compounds were not cytotoxic to human keratinocyte cells and can be considered as non-genotoxic for Ames test, furthermore, studies on antioxidant properties have shown that both compounds presented a very high antioxidant activity Regarding the anti-inflammatory activity both compounds inhibited the TNFα-stimulated espression and secretion of NFkB target cytokines, inhibited also COX activity and can activate the glucocorticoid receptor. Finally both compounds display neuroprotective properties

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