We report novel SIRT1 ligands that bind and modulate the activity of SIRT1 within cells and enhance its enzymatic activity. From a pool of aptamers we identify circular AC3 as having anticancer activity.
Recently, plant-derived compounds have been attracted increasable attention as alternative cancer remedies to enhance cancer prevention and healing, and as efficient antimicrobials, because of their low toxicity, low cost and fewer side effects. Ellagic acid (EA) is a natural phenolic constituent; previous studies have reported its antitumor properties when used in in vitro models. In this study, we have investigated the activity of a low concentration of EA against four different human cancer cell lines (SK-N-SH, Caov-3, SW-1088 and BxPC-3) which are very hard in the treatment and there is no available data about EA influence on them. Additionally, the effect of EA has assessed against (H. Pylori (Helicobacter pylori), P.aeruginosa (Pseudomonas aeruginosa), A. tumefaciens: Agrobacterium tumefaciens (Rhizobium radiobacter) and E. herbicola: Enterobacter agglomerans (Erwiniaherbicola) and two are Gram-positive bacterium S. aureus (Staphylococcus aureus) and C. acnes (Cutibacterium acnes)) strains which are resistant to the antibiotics. The results suggest that EA may have a potential role as an adjunct therapy for neuroblastoma, ovarian, pancreatic and astrocytoma cancers, in addition to its activity as an antimicrobial agent as it has been proved in this study against H. pylori, P.aeruginosa, A. tumefaciens, E. herbicola, S. aureus and C. acnes strains.
Sirutins 1-7 (SIRT1-7) is an enzyme that depends on NAD+ to be activated, making it a member of the 3rd class of Deacetylase enzymes. SIRT1-7’s activity is involved with metabolism, cell survival and/or death as well as DNA repair, gene repression, inflammatory responses, the aging process, neuroprotection in addition to possibly helping with the treatment of cancer. Molecules that could have a modifying effect on SIRT1-7’s activity has caught a great attention recently, owing to the fact of how beneficial this enzyme could be. In this review, we attempt to shed a light on these activator compounds and their use in Sirutin activation therapy, particularly SIRT1, for it is the most researched type. One of these compounds is Resveratrol, a natural compound that –due to its SIRT 1 activation potential – could help in the treatment of obesity, prevention of tumor formation as well as decrease in heart function and neuronal loss related to aging; however, Resveratrol has poor bioavailability, which is why structurally reformulated compounds and molecules have been developed. Other molecules that are different from Resveratrol such as SRT1720, SRT2104 and SRT2379 in addition to others, have been used and shown greater activation potential for SIRT1 than Resveratrol.
Conocarpus erectus L. is a perennial, evergreen shrub belonging to Combretaceae family. Conocarpus plant reported to contain phenolic acid, flavonoids, lignan, terpenes and tannins. Aim of study was to isolate lupeol from hexane fraction and gallic acid from ethyl acetate fraction and investigate the effects of (hexane and ethyl acetate) fractions on viability of pancreatic AsPC-1 and breast MCF-7 cell lines by MTT assay. The presence of lupeol in the hexane and gallic acid in the ethyl acetate extracts was detected by TLC. The identification of isolated lupeol and gallic acid by HPTLC and HPLC comparing with standard lupeol and gallic acid. Structural elucidation of isolated compounds done by FTIR and UV spectrophotometer. The cytotoxic activity showed more at high concentration (30µg/ml) in both ethyl acetate and hexane fractions against MCF-7 cell line, the percentage of cellular inhibition for ethyl acetate at 30mg/ml was (73% and 79%) more than the hexane fraction in which the inhibition was (60% and 76%) at 48hr and 72 hr respectively. Furthermore, the cytotoxic activity more at high concentration (30µg/ml) in both fractions against AsPC-1 cell line with cellular inhibition (58% and 70%) for ethyl acetate fraction and (50% and 66%) for hexane fraction in compared with Cisplatin.
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