Guggulsterone is a phytosteroid derived from the oleo-gum resin of the critically endangered plant . This molecule has attracted increasing attention due to its excellent biochemistry potential and the compound has consequently been evaluated in clinical trials. With a low concentration in natural resources but wide medicinal and therapeutic value, chemists have developed several synthetic routes for guggulsterone starting from various steroid precursors. Moreover, numerous studies have attempted to modify its structure to improve the biological properties. Nowadays, green and sustainable chemistry has also attracted more attention for advanced chemical processes and reactions in steroid chemistry. The present review aimed to summarize the literature and provide an update about the improvements in the chemical synthesis and structural modification of guggulsterone from the view of green chemistry. Moreover, this review encompasses the improved activities of structurally modified guggulsterone derivatives. We expect that the information provided here will be useful to researchers working in this field and on this molecule.
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http://dx.doi.org/10.1039/d3md00432e | DOI Listing |
Diabetes Obes Metab
January 2025
School of Exercise and Health, Shanghai Frontiers Science Research Base of Exercise and Metabolic Health, Shanghai University of Sport, Shanghai, China.
Aims: To investigate the role of chemerin reduction in mediating exercise-induced Glucagon-like peptide-1 (GLP-1) secretion and the amelioration of pancreatic β-cell function in obesity.
Materials And Methods: Obesity models were established using wild-type and chemerin systemic knockout mice, followed by 8 weeks of moderate-intensity continuous aerobic exercise training. Serum chemerin levels, GLP-1 synthesis, glucose tolerance, pancreatic β-cell function, structure, and apoptosis were assessed.
Drug Des Devel Ther
January 2025
The Key Laboratory of Molecular Pharmacology, Liaocheng People's Hospital, Liaocheng, Shandong, People's Republic of China.
Background: Melanoma is a highly lethal form of skin cancer, and effective treatment remains a significant challenge. SPP86 is a novel potential therapeutic drug. Nonetheless, the specific influence of SPP86 on autophagy, particularly its mechanisms in the context of DNA damage and apoptosis in human melanoma cells, remains inadequately understood.
View Article and Find Full Text PDFDrug Des Devel Ther
January 2025
Department of Trauma Orthopedics, Affiliated Hospital of Jining Medical University, Jining, Shandong, 272007, People's Republic of China.
Purpose: Osteosarcoma (OS) is the most common malignant tumor associated with poor patient outcomes and a limited availability of therapeutic agents. Scutellarein (SCU) is a monomeric flavone bioactive compound with potent anti-cancer activity. However, the effects and mechanisms of SCU on the growth of OS remain unknown.
View Article and Find Full Text PDFHypertension, a major cause of cardiomyopathy, is one of the most critical risk factors for heart failure and mortality worldwide. Loss of metabolic flexibility of cardiomyocytes is one of the major causes of heart failure. Although Catestatin (CST) treatment is known to be both hypotensive and cardioprotective, its effect on cardiac metabolism is unknown.
View Article and Find Full Text PDF( ) is the world's most deadly infectious pathogen and new drugs are urgently required to combat the emergence of multi-(MDR) and extensively-(XDR) drug resistant strains. The bacterium specifically upregulates sterol uptake pathways in infected macrophages and the metabolism of host-derived cholesterol is essential for long-term survival Here, we report the development of antitubercular small molecules that inhibit the cholesterol oxidases CYP125 and CYP142, which catalyze the initial step of cholesterol metabolism. An efficient biophysical fragment screen was used to characterize the structure-activity relationships of CYP125 and CYP142, and identify a non-azole small molecule that can bind to the heme cofactor of both enzymes.
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