Brushapathy Miriyala

Bio: Brushapathy Miriyala is an academic researcher from University of Mississippi. The author has contributed to research in topics: Aspergillus niger. The author has an hindex of 1, co-authored 1 publications receiving 37 citations.

Microbial transformation of artemisinin to 5-hydroxyartemisinin by Eurotium amstelodami and Aspergillus niger

Abstract: Transformation of the anti-malarial drug artemisinin by the fungi Eurotium amstelodami and Aspergillus niger were investigated. Cultures were grown in sucrose/malt broth with artemisinin for 14 days and extracted with ethyl acetate. Extracts were characterized by liquid chromatography. Two metabolites from each fungal extract were isolated and identified using mass spectrometry and nuclear magnetic resonance. 5β-hydroxyartemisinin and 7β-hydroxyartemisinin were isolated in 63 and 32% yields, respectively, from the extract of E. amstelodami, and 80 and 19%, respectively, from the extract of A. niger.

Controlled oxidation of remote sp3 C—H bonds in artemisinin via P450 catalysts with fine tuned regio and stereoselectivity

Abstract: The selective oxyfunctionalization of isolated sp3 C–H bonds in complex molecules represents a formidable challenge in organic chemistry. Here, we describe a rational, systematic strategy to expedite the development of P450 oxidation catalysts with refined regio- and stereoselectivity for the hydroxylation of remote, unactivated C–H sites in a complex scaffold. Using artemisinin as model substrate, we demonstrate how a three-tier strategy involving first-sphere active site mutagenesis, high-throughput P450 fingerprinting, and fingerprint-driven P450 reactivity predictions enabled the rapid evolution of three efficient biocatalysts for the selective hydroxylation of a primary and a secondary C–H site (with both S and R stereoselectivity) in a relevant yet previously inaccessible region of this complex natural product. The evolved P450 variants could be applied to provide direct access to the desired hydroxylated derivatives at preparative scales (0.4 g) and in high isolated yields (>90%), thereby enabling ...

Biodegradation of Pharmaceuticals by Fungi and Metabolites Identification

Abstract: Pharmaceutical compounds comprise a widely employed group of therapeutic agents now considered as emerging micropollutants. This chapter summarizes the state of the art in the degradation of pharmaceuticals by fungi in liquid matrices (with emphasis on white-rot fungi), including the use of both whole cells and fungal enzymes. The identification of the metabolites produced as well as the proposed degradation pathways available for some drugs are discussed. The information is organized according to the activity of the pharmaceutical compounds, grouped in: anti-inflammatory/analgesic drugs, psychiatric drugs, lipid regulators, antibiotics and other antimicrobial agents, b-blockers, estrogens, and iodinated contrast media. Considering the interest in potential application of fungal treatments in future real scale bioremediation of effluents, the ecotoxicology of the process is included when available.

Artemisinin derivatives: a patent review (2006 – present)

Abstract: Introduction: The isolation of artemisinin from an ancient Chinese remedy in the early 1970s heralded the beginning of a new era in antimalarial drug therapy culminating in artemisinin-based combination therapies currently being the mainstay of malaria treatment worldwide. Ongoing research on this compound and its derivatives has revealed its potential use in treating other infectious and noninfectious diseases. Areas covered: This review provides a summary of patents published globally from January 2006 to June 2012 covering promising artemisinin derivatives and artemisinin-based drug combinations developed for use in various therapeutic areas. Expert opinion: The diversity of semi-synthetic artemisinin derivatives has been limited to the same design strategy of modifying the artemisinin molecule at the same positions due to inherent synthetic challenges. To address this, future endeavors should include: the use of biotransformation strategies to modify other positions in the sesquiterpene ring while ret...