Synthesis of new dihydroberberine and tetrahydroberberine analogues and evaluation of their antiproliferative activity on NCI-H1975 cells

Abstract

<jats:p>Dihydroberberine (DHBER), the partially reduced form of the alkaloid berberine (BER), is known to exhibit important biological activities. Despite this fact, there have been only few studies that concern the biological properties of functionalized DHBER. Attracted by the potentiality of this latter compound, we have realized the preparation of new arylhydrazono-functionalized DHBERs, starting from BER and some α-bromohydrazones. On the other hand, also the fully reduced form of BER, namely tetrahydroberberine (THBER), and its derivatives have proven to present different biological activities. Therefore, the obtained arylhydrazono-functionalized DHBERs were reduced to the corresponding arylhydrazono-THBERs. The antiproliferative activity of both arylhydrazono-DHBERs and -THBERs has been evaluated on NCI-H1975 lung cancer cells.</jats:p>

Synthesis and Biological Characterization of the New Glycolipid Lactose Undecylenate (URB1418)

“…The test compound was then removed and fresh medium added. After 24 h of incubation, cell growth was analyzed by both water-soluble tetrazolium (WST)-8 and SRB assays, which estimate the metabolic activity of the cells and their protein content, respectively [41,42]. Color development was monitored in a multi-well plate reader (BioRad Laboratories, Hercules, CA, USA) and data expressed as cell growth (%) vs. untreated control cells.…”

The effects of Acyclovir administration to NCI-H1975 non-small cell lung cancer cells

“…Briefly, cells (5000/well) were seeded in 96-well plates and then treated with ACV (3-100 μM) for 24, 48, and 72 h or CDDP (3-100 μM) for 24 h as a positive control. At each experimental time point, cells were fixed using 50% aqueous trichloroacetic acid for 1 h at 4 • C, rinsed with water and incubated for 30 min with 0.4% SRB solution (Sigma-Aldrich, St. Louis, USA) (Farabegoli et al, 2017;Mari et al, 2020). After rinsing with 1% acetic acid and solubilizing in 10 mM Tris, absorbance was measured at 570 nm in each well by a microplate reader (Thermo Fisher Scientific, Milan, Italy).…”

Canadine Platinum(IV) Complexes Targeting Epithelial–Mesenchymal Transition as Antiproliferative and Antimetastatic Agents

“…In view of these stimulating facts and as a continuation of our interest in developing novel antitumor agents, − it was of great interest for us to design novel platinum(IV) conjugates with EMT suppressing and immunoregulating properties. Isoquinoline alkaloids are an important group of natural bioactive products, which display a wide variety of pharmacological properties such as antimicrobial, antibacterial, antifungal, antitumor, etc. − Canadine (CND) as a unique isoquinoline alkaloid shows much potential as antiproliferative and antimetastasis agents. − The mechanism detection revealed that CND was potent in inhibiting the EMT process, , inhibiting inflammation, and further modulating immune responses. , Accordingly, we intended to incorporate CND into the platinum(IV) system as a functional ligand with the aim of discovering novel platinum(IV) agents with potent antiproliferative and antimetastatic properties.…”

“…30−32 Canadine (CND) as a unique isoquinoline alkaloid shows much potential as antiproliferative and antimetastasis agents. 33−35 The mechanism detection revealed that CND was potent in inhibiting the EMT process, 36,37 inhibiting inflammation, and further modulating immune responses. 38,39 Accordingly, we intended to incorporate CND into the platinum(IV) system as a functional ligand with the aim of discovering novel platinum(IV) agents with potent antiproliferative and antimetastatic properties.…”