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Ophiopogonis japonicus is a famous medicinal plant in China with a long history of medicinal and food origin. It contains various chemical components, such as polysaccharides, steroidal saponins, alkaloids, flavonoids, etc. According to traditional Chinese medicine (TCM) theory, it has the efficacy of moistening the lungs and nourishing the yin, benefiting the stomach by generating fluids, and clearing the heart to get rid of vexation.

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Background: Androgenic anabolic steroids (AASs) are synthetic drugs structurally related to testosterone, with the ability to bind to androgen receptors. Their uncontrolled use by professional and recreational sportspeople is a widespread problem. AAS abuse is correlated with severe damage to the cardiovascular system, including changes in homeostasis and coagulation disorders.

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: , or star fruit, is a shrub known for its medicinal properties, especially due to bioactive metabolites identified in its roots and fruit with anti-cancer activity. However, the biological effects of its leaves remain unexplored. This study aimed to assess the effects of ethanolic extract from leaves on triple-negative breast cancer (TNBC), an aggressive subtype lacking specific therapy.

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A concise, transition metal-free four-step synthetic pathway has been developed for the synthesis of tetracyclic heterosteroidal compounds, 14-aza-12-oxasteroids, starting from readily available 2-naphthol analogues. After conversion of 2-naphthols to 2-naphthylamines by the Bucherer reaction, subsequent selective C-acetylation was achieved via the Sugasawa reaction and reduction of the acetyl group using borohydride, which resulted into the corresponding amino-alcohols. The naphthalene-based amino-alcohols underwent double dehydrations and double intramolecular cyclization with oxo-acids leading to one-pot formation of a C-N bond, a C-O bond and an amide bond in tandem, to generate two additional rings completing the steroidal framework.

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Proteome-Wide Identification and Comparison of Drug Pockets for Discovering New Drug Indications and Side Effects.

Molecules

January 2025

State Key Laboratory of Primate Biomedical Research, Institute of Primate Translational Medicine, Kunming University of Science and Technology, Kunming 650500, China.

Drug development faces significant financial and time challenges, highlighting the need for more efficient strategies. This study evaluated the druggability of the entire human proteome using Fpocket. We identified 15,043 druggable pockets in 20,255 predicted protein structures, significantly expanding the estimated druggable proteome from 3000 to over 11,000 proteins.

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