Ring-fused 3β-acetoxyandrost-5-enes as novel neuroprotective agents with cholinesterase inhibitory properties

Isolation and Bioactivity Evaluation of Sesquiterpenes from an Alcyonarian of the Genus Lemnalia from the Saudi Arabian Red Sea

“…N-acetylcysteine (NAC) was used as the positive control. [31] Interestingly, metabolites 12 and 15 at 10 μM caused 80-85 % reduction in cell death, slightly better than or comparable to 100 μM NAC (Figure 5B). The protective effect mediated by 12 was found to be statistically significant.…”

“…The organic extract was subjected to a series of chromatographic separations to yield 31 sesquiterpenes (1-31, Figure 1), among which three (13, 14 and 28) are new natural products. The previously reported metabolites were identified by comparison of their spectroscopic and physical characteristics with those published in the literature as linardosinene D (1), [8] its C-11 epimer linardosi-nene E (2), [8] linardosinene C (3), [9] paralemnolin O (4), [10] paralemnolin P (5), [10] 7α-acetoxy-1(10)-α-epoxy-12-nornardosin-11-one (6), [11] 6α-acetyl-1(10)-α-13-nornardosin-7-one (7), [11,12] paralemnolin K (8), [3] the nardosinane 9, [13] paralemnolin J (10), [10] paralemnolin L (11), [10] paralemnolin M (12), [14] the eremophilanes 15 [3] and 16, [15,16] 1(10)-aristolen-2-one (17), [17] 1(10)-aristolen-12-ol (18), [18] lemnalactone (19), [19] 2-deoxy-12- oxolemnacarnol (20), [13] pathylactone A ( 21), [20] lemnardosinane I ( 22), [21] isoparalemnanone (23), [22] lineolemnene G (24), [2] paralemnolin H (25), [23] lemnolin A (26), [24] paralemnolin E (27), [23] paralemnolin D (29), [23] paralemnolin F (30) [23] and 4βacetoxy-2,8-neolemnadien-5-one (31). [25] Compound 13 was isolated as colorless oil, possessing the molecular formula C 17 H 26 O 3 as deduced from the HR-APCIMS measurements.…”

“…The levels of ELAM on the cell surface or IL-6 and ICAM-1 in the medium from the cultivation of HUVEC cells after 30 min of preincubation with the tested compounds and 24 h of stimulation with TNFα were detected using an enzyme-linked immunosorbent assay (ELISA), as previously described. [27] Evaluation of Neuroprotective Activity using the MPP + -induced and 3-NPA-induced Models of Neurodegeneration measured by propidium iodide as previously described [31] and the neuroprotective effect was expressed as a decrease in cell death compared to that of cells only with the neurotoxins.…”

“…[37] The human neuroblastoma cell line SH-SY5Y, obtained from the European Collection of Authenticated Cell Cultures (Salisbury, UK), was cultivated and differentiated as previously described. [31] All cells were maintained in a humidified CO 2 incubator at 37 °C using the standard trypsinization procedure twice or three times a week. Stock solutions of the tested compounds were prepared in DMSO.…”

Synthesis and Biological Activity of Some Bromophenols and Their Derivatives Including Natural Products

“…In the case of any failure or in the advanced stages of AD, the most common neurodegenerative disease, it is also hypothesized that BChE takes over AChE's role. [34] α-Glycosidase is a glycosidic hydrolase enzyme located on the brush border surface membrane of small intestine cells and hydrolyzes carbohydrates to glucose. α-Glycosidase is vital for the hydrolysis of carbohydrates.…”