A modular synthetic
approach to strategically unique structural
analogues of the alkaloid yohimbine is reported. The overall synthetic
strategy couples the transition-metal-catalyzed decarboxylative allylation
of 2,2-diphenylglycinate imino esters with a scandium triflate-mediated
highly endo-selective intramolecular Diels–Alder (IMDA) cycloaddition
to generate a small collection of de-rigidified yohimbine analogues
lacking the ethylene linkage between the indole and decahydroisoquinoline
units. One compound generated in this study contains an unprecedented
pentacyclic urea core and appears to demonstrate increased cytotoxicity
against the gastric cancer cell line SGC-7901 in comparison to a pancreatic
cancer cell line (PATU-8988) and a normal human gastric mucosal cell
line (GES-1).
Cachexia denotes a complex metabolic syndrome featuring severe loss of weight, fatigue and anorexia. In total, 50-80% of patients suffering from advanced cancer are diagnosed with cancer cachexia, which contributes to 40% of cancer-associated mortalities. MicroRNAs (miRNAs) are non-coding RNAs capable of regulating gene expression. Dysregulated miRNA expression has been observed in muscle tissue, adipose tissue and blood samples from patients with cancer cachexia compared with that of samples from patients with cancer without cachexia or healthy controls. In addition, miRNAs promote and maintain the malignant state of systemic inflammation, while inflammation contributes to cancer cachexia. The present review discusses the role of miRNAs in the progression of cancer cachexia, and assess their diagnostic value and potential therapeutic value.
Contents1. Introduction 2. miRNAs in the development of cancer and cancer cachexia 3. miRNAs in muscular atrophy 4. miRNAs in adipose tissue depletion 5. Circulating miRNAs in cancer cachexia 6. Discussion and perspectives
Aim: To assess the anticancer activity of nanoparticles synthesized via a green method using American ginseng (AG). Methods: Stem-leaf saponins from AG (SAG) and heat-transformed stem-leaf saponins from AG (TSAG) were used to synthesize different SAG nanoparticles (SAG-NPs)
and TSAG nanoparticles (TSAG-NPs). The NPs were characterized, and their anticancer activity was assessed in vitro. Results: The NPs, which differed in size (16.69 nm∼253.8 nm), were spherical or polyhedral with a low PDI and good stability. The TSAG-NPs inhibited cancer
cells by inhibiting proliferation, promoting cancer cell apoptosis and directly leading cancer cells to necrosis. The small cell lung cancer cell line (SCLC) NCI-H446 was the most sensitive to the TSAG-AgNPs, with an IC50 value of 20.71±2.38 μg/mL, and the TSAG-AgNPs
inhibited invasiveness and reduced the risk of metastasis. Conclusion: TSAG-AgNPs, selected from many SAG-NPs and TSAG-NPs, are sensitive to SCLC and provide a new approach to the currently limited treatment.
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