Selectivity of catechol O-methyltransferase has been examined for the three ring-fluorinated norepinephrines to elucidate the role of acidity of the phenolic groups in their methylation. Substitution of fluorine at the 5-position of norepinephrine reverses the selectivity of catechol O-methyltransferase so that p-O-methylation predominates. The 5-fluoro substituent also causes the pKa of the p-...

O presente projeto procurou produzir produtos semi-sintéticos orgânicospreferencialmente que possuam atividade biológica, através de reações click,utilizando como composto partida o timol, carvarol e eugenol. Os compostos estãopresentes nos óleos essenciais extraídos do orégano ( Origanum Vulgare ) tanto parao quanto carvacrol cravo da índia Eugenia caryophyllata para Osderivados foram produzid...

In this study, inclusion complexes (IC) of three cyclodextrin derivatives (HP-β-CD, HP-γ-CD, and M-β-CD) with eugenol (essential oil compound) were formed in highly concentrated aqueous solutions and then transformed into self-standing functional nanofibrous webs by electrospinning. The improved aqueous solubility of eugenol was confirmed by phase solubility diagrams, in addition, the phase sol...

Eugenol (C10H12O2) presents various therapeutic properties. Due to this fact, it arises interest into the pharmaceutic industry and has a commercial value. However, there is still low offer of product in market. The aim work was evaluate concentration essential oil from dried leaves O. gratissimum L., determine whether species bares promising characteristics as source eugenol. Fresh Ocimum L. w...

The substances belonging to the sterigmatocystin group bear a close structural relationship to aflatoxins. When demethylsterigmatocystin (DMST) was fed to Aspergillus parasiticus NIAH-26, which endogenously produces neither aflatoxins nor precursors in YES medium, aflatoxins B1 and G1 were produced. When dihydrodemethylsterigmatocystin (DHDMST) was fed to this mutant, aflatoxins B2 and G2 were ...

The purpose of this study was to evaluate the histopathological effect of eugenol and bis-eugenol on oral mucous membranes at the tissue organ level. Oral mucous membranes of mice were applied with three reagents, eugenol, bis-eugenol, and acetone (as the control). The control group showed a normal architecture. The eugenol group showed severe hyperkeratosis, parakeratosis, cellular edema, patc...

The present investigation was carried out to study the relationship between presence of cytotoxic compounds in Ocimum basilicum, Alhagi maurorum, Calendula officinalis and their parasite Cuscuta campestris. The cytotoxic activity of the pure compounds was performed by MTT assay against breast cancer cell lines (MCF-7 and MDA-MB-231) and normal breast cell line (MCF 10A). The induction of apopto...

The antifungal properties of eugenol were tested against ten plant pathogenic fungal species and detailed studies were conducted regarding in vitro activity of eugenol on Botrytis cinerea. The EC50 value of eugenol on mycelial radial growth of B. cinerea was 38.6 μg/ mL; however, eugenol had no bioactivity against conidia germination. B. cinerea hyphae treated with eugenol showed strong propidi...

A mechanism-based small molecular fluorescent probe has been developed to label active O(6)-methylguanine-DNA methyltransferase in live cells.

Methylation catalysed by catechol-O-methyltransferase (COMT) is the main pathway of catechol neurotransmitter deactivation in the prefrontal cortex. Low levels of this class of neurotransmitters are held to be causative of diseases such as schizophrenia, depression and Parkinson's disease. Inhibition of COMT may increase neurotransmitter levels, thus offering a route for treatment. Structure-ba...