Diosmetin inhibits cell proliferation and promotes apoptosis through STAT3/c-Myc signaling pathway in human osteosarcoma cells

Background Diosmetin is a bioflavonoid compound naturally abundant in citrus fruits. It is found to perform a variety of activities, while its antitumor property in osteosarcoma, a malignant tumor with unmet clinical treatment, remained unknown. Methods Colony formation assay, cell cycle analysis and apoptosis analysis were conducted respectively to observe the effect of diosmetin on cell proliferation and apoptosis in human osteosarcoma cells. Western blot and immunoprecipitation were used to detect the expression of apoptotic molecules and activation of STAT3/c-Myc pathway in Saos-2 and U2SO cells. Results Diosmetin significantly inhibited cell proliferation, induced cell cycle arrest at G2/M phase and promoted cell apoptosis in both Saos-2 and U2SO cells. Moreover, Diosmetin downregulated the expression of anti-apoptotic protein Bcl-xL while upregulated the levels of pro-apoptotic proteins including cleaved Caspase-3, cleaved-PARP and Bax. Furthermore, diosmetin dose-dependently inhibited STAT3 phosphorylation, reduced the expression of its downstream protein c-Myc and impeded the interaction between STAT3 molecules. Conclusions These results suggest that diosmetin exerts anti-osteosarcoma effects by suppressing cell proliferation and inducing apoptosis via inhibiting the activation of STAT3/c-Myc signaling pathway, which provide the possibility for diosmetin to be a chemotherapeutic candidate for osteosarcoma.

In silico Analysis of Quercetin and its Analogues Against Targeted Proteins

Quercetin is a flavonoid compound present in many plants such as onions, tomatoes, apples, green tea, flax seeds, etc. It possesses antioxidant and anti-inflammatory effects that help control inflammation, kill cancer cells, and prevent heart disease. Wide evidence reveals quercetin's antitumor property to inhibit various cancers like breast, lung, nasopharyngeal, kidney, colorectal, pancreatic, prostate, and ovarian cancer. In this study, quercetin was docked against proteins such as Apoptic protein (APAF-1, BAX, BCL-2), Heat shock protein, Cytochrome p45O, Actin, Tyrosine-protein kinase hck. From the Insilico research completed, we can infer that quercetin and the analogs show great efficacy in finding against cancer and can be used in cancer care. These findings will help us understand the quercetin's binding ability with proteins and know-how quercetin is involved in the anti-cancer, antioxidant role.

Withaferin A Acts as a Novel Regulator of Liver X Receptor-α in HCC

Withaferin A, a steroidal lactone derived from the Withania somnifera plant has been known for its anti-cancerous effects on various types of cancer cells. However, its effect on the hallmarks of cancer such as proliferation, migration, invasion, and angiogenesis is still poorly understood. The antitumor property of Withaferin A and its molecular mechanism of action on hepatocellular carcinoma (HCC) cells is not yet completely established. In this study, we aimed to elucidate the novel molecular function of Withaferin A on HCC cells and its effect on various gene expression. Our results clearly showed that Withaferin A treatment to HCC cells inhibited proliferation, migration, invasion, and anchorage-independent growth. Further, we explored the Withaferin A target genes by blotting human angiogenesis, and cytokine arrays using conditioned media of Withaferin A treated QGY-7703 cells. We found that many of Nuclear factor kappa B (NF-κB), angiogenesis and inflammation associated proteins secretion is downregulated upon Withaferin A treatment. Interestingly, all these genes expression is also negatively regulated by nuclear receptor Liver X receptor-α (LXR-α). Here, we explored a novel mechanism that Withaferin-A activated LXR-α inhibits NF-κB transcriptional activity and suppressed the proliferation, migration, invasion, and anchorage-independent growth of these HCC cells. All these data strongly confirmed that Withaferin A is a potent anticancer compound and suppresses various angiogenesis and inflammatory markers which are associated with the development and progression of HCC. This beneficial and potential therapeutic property of Withaferin A will be very useful for the treatment of HCC.

Antimicrobial and Antiproliferative Activities of Depside Compound Isolated from the Mycobiont Culture of Parmotrema austrosinense (Zahlbr.) Hale

Substances which are normally secondary metabolites in a lichen are known to possess various medicinal properties but little is known about the biological activities of compounds present in these mycobiont culture extract. The objectives of the present study were isolation and optimization of growth conditions of the mycelia from Parmotrema austrosinense and assess the antiproliferative and antimicrobial activities of acetone extracts. The extraction of bioactive compound from mycobiont culture was achieved by using acetone and standard Soxhlet extraction procedures. The culture extract was subjected to silica gel column chromatography and detection of compound in thin layer chromatography. HPLC, UV vis, IR spectra, microcrystallization and NMR were done for the purified compound. The antimicrobial activity in the extracts were assayed using the standard disc diffusion and broth microdilution protocol against microbial strains. The lecanoric acid in the extracts was purified and MTT method was applied to assess antiproliferative activity against DLA cancer cells. The culture extract containing lecanoric acid exhibited antimicrobial activity against the test strains with the Minimum Inhibitory Concentrations varied between 0.83±0.28 and 2.3±1.5 mg mL−1. The lecanoric acid inhibited the growth of DLA cancer cells with inhibitory concentration (IC50) of about 42±1.5 µg mL−1. Conclusion: The result of the present study suggests that this compound might possess potent antitumor property and should be further analysed using appropriate animal model and clinical trials.

Green coffee bean seed and their role in antioxidant–A review

All around the world, Coffee place an important position in the beverages. It contains phenolic acid as well as polyphenols. It has the property of antioxidant; mood enhances mood, and also increases alertness, reduces weight, efficiency against hypertension, and antitumor property because of its polyphenols and phenolic constituents. Chlorogenic acids (CGA) are the main components found in the fraction of phenols from green coffee beans. CGA has several therapeutic properties, which include antioxidant activities and also has hepatoprotective, hypoglycemic, and antiviral properties. Several essential compounds found in CGA in green coffee beans are caffeoylquinic acids, caffeoylquinic acids, feruloyl quinic acids, p-coumaroylquinic acids, and quinic acid. Therefore, this review highlighted the health benefits and anticancer activities of Green coffee bean.

Regioisomer-manipulating thio-perylenediimide nanoagents for photothermal/photodynamic theranostics

This work presents a facile means of accessing thio-perylenediimides that not only possess excellent antitumor property but provide a novel proof-of-concept means to improve therapeutic performance via the optimization of non-bonding interactions.

Research on Biological Properties of Ruthenium (III) Heterocyclic Schiff Base Complexes

A set of ruthenium complexes of +3 oxidation state were synthesized with the available ruthenium precursors and the synthesized Schiff base ligands. The complexes are formed by the substitution of the ligand in the octahedral metal precursors. Samples are characterized using analytical as well as spectroscopic techniques. To ascertain pharmacological properties binding study with DNA were carried out. Further, cleavage studies were performed with gel electrophoresis. The in vitro antitumor property was analysed in HeLa tumor cell lines.

Recent Progress of Adenosine Receptor Modulators in the Development of Anticancer Chemotherapeutic Agents

Increased risks of peripheral toxicity and undesired adverse effects associated with chemotherapeutic agents are the major medical hurdles in cancer treatment that worsen the quality of life of cancer patients. Although several novel and target-specific anticancer agents have been discovered in the recent past, none of them have proved to be effective in the management of metastatic tumor. Therefore, there is a continuous effort for the discovery of safer and effective cancer chemotherapeutic agent. Adenosine receptors have been identified as an important target to combat cancer because of their inherent role in the antitumor process. The antitumor property of the adenosine receptor is primarily attributed to their inherited immune response against the tumors. These findings have opened a new chapter in the anticancer drug discovery through adenosine receptor-mediated immunomodulation. This review broadly outlines the biological mechanism of adenosine receptors in mediating the selective cytotoxicity as well as the discovery of various classes of adenosine receptor modulators in the effective management of solid tumors.