These results indicate that compounds affected HSV-1 mostly before adsorption and might interact with the viral envelope. Thymol exhibited a high selectivity index and seems to be a promising candidate for topical therapeutic application as antiviral agent for treatment of herpetic infections.
The current phytochemical investigation on Buxus hyrcana Pojark. has resulted in the isolation of the triterpenoid alkaloids 1-10. The structures of five new alkaloids, hyrcanone (1), hyrcanol (2), hyrcatrienine (3), N(b)-dimethylcycloxobuxoviricine (4), and hyrcamine (5), were elucidated by means of modern spectroscopic techniques, while the known alkaloids, buxidin (6), buxandrine (7), buxabenzacinine (8), buxippine-K (9) and E-buxenone (10), were identified by comparing their spectral data with those reported earlier. Compounds 1 and 3-9 were found to be acetyl- and butyrylcholinesterase inhibitors. The IC50 values were estimated to be in the range of 83.0-468.0 microM against AChE and 1.12-350.0 microM against BChE. The structure-activity relationship studies suggested that the presence of dimethylamino moieties at C(3) and C(20) is the most important factor influencing the activity of these compounds against the cholinesterase enzymes. All compounds were also evaluated for cytotoxicity on a fibroblast cell line with incubation of 24 h. No cytotoxic effects were exerted by any compound.
The genus Eremurus is native to Eastern Europe and temperate Asia. Particularly, Eremurus persicus (Joub. & Spach) Boiss. is highly valued in traditional foods and medicine. Scientific knowledge about E. persicus chemical composition and bioactivity is required. Therefore, the present study is aimed to determine the volatile composition of E. persicus essential oil (EO) by means of gas chromatography coupled to flame ionization/mass spectrometry detection. Moreover, the antioxidant, antimicrobial, anticancer, and acetylcholinesterase inhibitory activities of the EO were tested. Interestingly, the anti-dermatophyte potency was close to that of the drug griseofulvin, with minimum fungicidal concentration ranging between 0.7 and 4.5% depending on the fungi strain. The EO was also effective against hepatocellular carcinoma (Hep-G2) and breast adenocarcinoma (MCF-7) human cancer cell lines in a concentration (200-1500 ng/mL)-dependent manner, with a decrease of the cell viability up to 65% and 52%, respectively. The E. persicus EO was rich in terpenes and oxygenated terpene derivatives. Individually, limonene (16.25%), geranylgeraniol (15.23%), n-nonanal (9.48%), geranyl acetone (9.12%), benzene acetaldehyde (8.51%), linalool (7.93%), α-pinene (6.89%), and 1,8-cineol (5.22%) were the most abundant volatile compounds and could be chosen as analytical markers of this essential oil. In conclusion, our results suggested that this EO possesses a wide range of bioactive properties that could be useful in nutraceutical, functional foods and cosmeceutical formulations.
Three new triterpenoid alkaloids, (+)-N-benzoylbuxahyrcanine [(20S)-3beta-benzoylamino-20-dimethylaminobux-9(11)-ene-10alpha-ol] (1), (+)-N-tigloylbuxahyrcanine [(20S)-20-(dimethylamino)-3beta-(2'-methyl-2'-butenoylamino)bux-9(11)-en-10alpha-ol] (2), and (+)-N-isobutyroylbuxahyrcanine [(20S)-20-(dimethylamino)-3beta-(2'-methylpropanoyl)bux-9(11)-en-10alpha-ol] (3), have been isolated from the leaf extracts of Buxus hyrcana collected in Iran. Their structures were determined using spectroscopic methods. The structures of compounds 1 and 2 were unambiguously confirmed by single-crystal X-ray diffraction techniques. Compounds 1-3 were evaluated for their acetylcholinesterase and butyrylcholinesterase inhibitory activities, and compound 2 was found to be active against both enzymes.
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