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The biocatalytic potential of Bipolaris sorokiniana was investigated in its ability to modify the monoterpene geraniol and the sesquiterpene alpha-bisabolol as exogenous substrates, using phosphate buffer as reaction medium. The cultures showed a promising oxidative profile, with conversion of geraniol to 6-methyl-5-hepten-2-one (74.9% yield) in a 5-day incubation and alpha-bisabolol to bisabolol oxide B (84.2% yield), in a 7-day incubation. [ABSTRACT FROM AUTHOR]

Ofloxacin (OFX) is a fluorquinolone characterized by photochemical instability. With the goal to improve its photostability in aqueous solutions, the complexation of ofloxacin with β-cyclodextrin was investigated. The complexes showed a water solubility enhancement of approximately 2.6 times; nevertheless, the photodegradation of ofloxacin was not reduced. The complexes obtained were characterized by thermal and [SUP1]H nuclear magnetic resonance (NMR) analysis, which revealed an interaction between ofloxacin and β-cyclodextrin. The last analysis indicated that only parial inclusion of the N-methylpiperazinyl moiety occurred, which can explain the fact that photostabilization was not improved. This partial inclusion phenomenon could be explained also by computer-aided molecular modeling. [ABSTRACT FROM AUTHOR]

Background: Intensive prophylactic use of antifungals leads to the increase of drug resistance and the need for new and more effective treatments are real. Plants from Leguminosae family are rich in flavonoids, for which numerous biological activities have been described, including antifungal effects., Purpose: To screen methanolic extracts from Leguminosae species looking for alternative sources for antifungal agents (anti-dermatophyte and anti-Candida) and their innocuity., Methods: Antifungal activity was evaluated using the strains Candida albicans, C. krusei, C. glabrata, C. tropicalis, C. parapsilosis, Epidermophyton floccosum, Trichophyton mentagrophytes, T. rubrum and, Microsporum gypseum in the broth microdilution method. Later, the minimum inhibitory concentration (MIC) for Mimosa pigra, Eriosema heterophyllum, and Chamaecrista nictitans was determined. The most promising extract was fractionated and cytotoxicity and genotoxicity of the most active fraction were also assayed., Results: Fungicide and/or fungistatic activity against dermatophyte strains were presented by 60% of the methanolic extracts assayed. M. pigra, E. heterophyllum, and C. nictitans methanolic extracts could inhibit dermatophyte strains at concentrations ranging from 1.9 to 1000μg/mL. M. pigra showed the lowest MIC values for a dichloromethane fraction (1.9μg/mL) without DNA damage at 10 and 50μg/mL and 100% of cell viability of human leukocytes., Conclusion: Our results indicate that methanolic extracts from Leguminosae plants are potential sources of antifungal compounds, mainly the extract and fractions from M. pigra. The dichloromethane fraction from M. pigra did not showed in vitro toxicity according to the applied assays., (Copyright © 2017 Elsevier Masson SAS. All rights reserved.)

Ten N-monoalkylated diamines were synthesized and evaluated for in vitro activities against Trichomonas vaginalis and Giardia lamblia. Several compounds displayed a good inhibition of parasite growth, with MIC less or equal to 20μg/mL. N-hexadecil-1,4-butanediamine was found to be the most active compound in vitro against T. vaginalis with MIC of 2.5μg/mL, twice more active in comparison to the reference drug metronidazole (MTZ). Seven of the studied compounds showed a better anti-G. lamblia activity than MTZ., (Copyright © 2010. Published by Elsevier SAS.)

The treatment of neurological disorders and neurodegenerative diseases is related to the levels of acetylcholine (ACh) through the inhibition of acetylcholinesterase (AChE). Galanthamine, an important alkaloid isolated from the Amaryllidaceae family, is approved for the pharmacological treatment of Alzheimer's disease (AD) and acts by inhibiting the acetylcholinesterase (AChE) activity. In the present study, Ellman's method was used to verify the inhibition of AChE activity of some isoquinolines alkaloids such as galanthamine, montanine, hippeastrine and pretazettine. At the concentrations 1mM, 500 microm and 100 microm, galanthamine presented an AChE inhibition higher than 90%. Montanine inhibited, in a dose-dependent manner, more than 50% of the enzyme at 1mM concentration. With the concentrations 500 microm and 100 microm, 30-45% of AChE activity inhibition was detected. The alkaloids hippeastrine and pretazettine presented no significant inhibition of the AChE activity. The results demonstrate that montanine significantly inhibits AChE activity at the tested concentrations, suggesting the necessity of further investigations on this alkaloid use in treating neurological disorders., ((c) 2009 Elsevier GmbH. All rights reserved.)

Strictosidinic acid 10mg/kg, isolated from Psychotria myriantha leaves, were administered intraperitoneally to Wistar male rats (n=5-6). After 60 minutes, striatum was dissected, homogenized and injected onto HPLC-ED chromatographic system. It was observed a 28.7% reduction in the 5-HT levels followed up by an increase of 5-HIAA levels (29.4%). Furthermore there was a decrease of 8.0% in DA levels and an increase in the levels of metabolites DOPAC (21.5%) and HVA (52.5%). The results indicate that strictosidinic acid has a promising effect in the central nervous system, justifying more studies about the central actions of Psychotria compounds., (Copyright 2009 Elsevier GmbH. All rights reserved.)

The dichloromethane and n-butanol extracts obtained from fresh bulbs of Hippeastrum vittatum (Amaryllidaceae), collected in Southern Brazil, were evaluated for their cytotoxic activity in vitro against five human cell lines (HT29 colon adenocarcinoma, H460 non-small cell lung carcinoma, RXF393 renal cell carcinoma, MCF7 breast cancer, and OVCAR3 epithelial ovarian cancer), using the sulphorhodamine B assay. Both extracts showed potential antiproliferative activity. From CH(2)Cl(2) fraction, three alkaloids were isolated: lycorine, vittatine and montanine. The two last compounds were submitted to the antiproliferative assay and the highest level of cytotoxicity was found for the alkaloid montanine.

Brachycerine (1), an unusual alkaloid from the leaves of Psychotria brachyceras, was characterized through spectroscopic data interpretation and its stereochemistry established by NOE difference techniques. Brachycerine (1) was found to be restricted to shoots in rooted cuttings of P. brachyceras (0.018 +/- 0.004% dry weight), and accumulation was unaffected by root induction treatment with auxin.

The alcoholic and n-butanolic extracts of dried leaves of Stachytarpheta cayennensis (L.C. Rich) Vahl (Verbenaceae) was assessed in antiinflammatory and antinociceptive models. Intraperitoneal pretreatment with the dried extracts at doses ranging from 100 to 200 mg/kg, significantly inhibited carrageenin inducing edema formation. The active extracts were then fractionated and monitored with the same bioassay. The iridoid ipolamiide and the phenylethanoid glycoside acteoside were isolated from the active fraction and showed inhibitory effect on histamine and bradykinin induced contractions of guinea-pig ileum. The compounds also showed in vivo antiinflammatory activity when administered orally to rats mainly in the fourth hour after the administration of the phlogistic agent (70.22% and 93.99%, respectively). These results indicate that S. cayennensis shows antiinflammatory properties which seems to be due, at least partly, to the inhibition of bradyknin and histamine. The extracts also exhibited antinociceptive activity measured by the hot-plate test both i.p. and p.o. in doses ranging from 100 to 300 mg/kg.