Anti-hyperalgesic activity of crude extract and 7-methyljuglone of Diospyros lotus roots

This study was designed to evaluate the antihyperalgesic effect of crude extract of Diospyros lotus followed by the isolation and characterisation of 7-methyljuglone in acetic acid and formalin tests. The pretreatment of crude extract evoked dose-dependent inhibition of noxious stimulation with maximum effect of 56.78% in acetic acid-induced writhing test, which were 51.89% and 60.69% in first and second phases, respectively, at 100 mg/kg i.p. The structure of 7-methyljuglone was confirmed by spectroscopic analysis. 7-Methyljuglone evoked profound increase in pain threshhold dose dependently; when it was studied in acetic acid-induced writhing test with 63.73% pain attenuation while 51.22% and 65.44% pain amelioration in first and second phases, respectively, at 100 mg/kg i.p. In conclusion, crude extract and 7-methyljuglone of D. lotus roots possessed both peripheral and central antinociceptive potential and thus could be a useful new therapeutic agent.     

Antibacterial and antifungal properties of crude extracts and isolated compounds from Lychnophora markgravii

Abstract

Antimicrobial activity of dichloromethane and ethanol extracts and five compounds: pinostrobin (I), pinocembrin (II), tectochrysin (III), galangin 3-methyl ether (IV) and tiliroside (V) isolated from Lychnophora markgravii aerial parts against fifteen microorganisms was determined. The structures of these compounds were elucidated based on ESI-MS and NMR spectroscopic data. Both extracts showed antimicrobial activity against several tested microorganisms. Pinostrobin, tectochrysin and galangin 3-methyl ether showed the strongest antibacterial and antifungal effects.     

Design,synthesis and antifungal activities in vitro of novel tetralin compounds

Novel chiral tetralin compounds were designed and synthesized, and their antifungal activities in vitro were tested. The results showed that all of target compounds had potent antifungal activities, and were stronger than that of control compounds tetrahydroisoquinolines. The binding model of lead molecules in the active site of CYP51 of Candida albicans showed that lead compound specifically interacted with the amino acids residues in the active site, without binding with the heme of CYP51, which was different from azole antifungal drugs. The present study might afford a novel lead molecule to develop non-azole CYP51 inhihitars of fungi.     

Six new compounds from the heartwood of Diospyros maritima

Six new compounds, diospyrolide (1), diospyrolidone (2), diethyl (2R)-malate (3), 3-(E)-coumaroylbetulin-28-yl ethyl nonanedioate (4), 3-(E)-coumaroylbetulin-28-yl ethyl succinate (5), and 3-(E)-coumaroylbetulin-28-yl ethyl (2R)-2-hydroxysuccinate (6), have been isolated from the heartwood of Diospyros maritima. Compounds 1 and 2 are novel trinorlupanes, and 4, 5 and 6 are lupane derivatives. Their structures were determined using spectral and chemical methods.     

Chemometric QSAR studies of antifungal azoxy compounds

Summary Quantitative structure-activity relationships (QSARs) for 16 azoxy compounds with antifungal activity have been studied by the combined approach of a partial least-squares method and factorial design. The PLS model equation suggested the structural requirements of two substituents, R₁ and R₂, for the antifungal activity. The sterically bulky and hydrophobic R₁ substituents and electron-withdrawing R₂ substituents are favorable for the activity. We propose candidate compounds which are more potent than the compounds based on QSAR data. In this study, we show that the chemometric approach is a powerful tool for QSAR studies and drug design.Abbreviations PLS partial least squares - FD factorial design - MLR multiple linear regression - PPs principal properties     

Antibacterial and antifungal screening of Centaurium pulchellum crude extracts and main secoiridoid compounds

The main principles of C. pulchellum (Sw.) Druce, secoiridoid glycosides, have been studied as potent bioactive compounds. Here we scored their content in extracts of ten populations of this species. Antibacterial and antifungal assays of the extracts and pure secoiridoid glycosides were performed against eight bacterial strains and five fungal species. Methanol extracts from both aerial parts and roots exhibited excellent antibacterial (0.05-0.2 mg mL(-1)) and very good antifungal (0.1-2 mg mL(-1)) activity. Pure secoiridoid glycosides isolated from these extracts demonstrated very strong antibacterial (0.01-0.04 mg mL(-1)) and especially antifungal (0.001-0.1 mg mL(-1)) activity.     

Design, synthesis and molecular docking studies of novel triazole antifungal compounds

Based on the active site of Candida albicans lanosterol 14α-demethylase (CACYP51), novel triazole compounds structurally different from the current triazole drugs were designed and synthesized. In vitro antifungal activities showed that compounds 10,11, 16 and 20 exhibited strong activities. In addition, compounds 10,11 and 16 also displayed certain activities against fluconazole-resistant fungi.     

Antihepatotoxic and antioxidant activities of methanol extract and isolated compounds from Ficus chlamydocarpa

Free radicals, in particular radical oxygen species (ROS), play an important role in the aetiology and pathogenesis of various diseases. Current research in many countries focuses on the use of local medicinal plants as a promising source of liver protective agents. This paper describes the hepatoprotective effects of the methanol extract and four isolated compounds from Ficus chlamydocarpa on CCl4-induced liver damage, as well as the possible antioxidant mechanisms involved in this protection. The DPPH test, along with the beta-Carotene-Linoleic Acid Model System and Ferric-Reducing Antioxidant Power assays, as well as the inhibition of microsomal lipid peroxidation were used to measure radical-scavenging and antioxidant activities. Pretreatment of rats with the methanol extract of F. chlamydocarpa before CCl4 administration, significantly prevented serum increase of hepatic enzyme markers, glutamate oxaloacetate transaminase (GOT) and glutamate pyruvate transaminase (GPT), in a dose-dependent manner. The hepatoprotection was also associated with a significant enhancement in hepatic reduced glutathione (GSH) and a marked decrease of liver malondialdehyde (MDA). Among the four compounds 1-4, isolated from the methanol extract, alpha-amyrin acetate (1) and luteolin (4) showed a significant hepatoprotective activity, as indicated by their ability to prevent liver cell death and lactate dehydrogenase (LDH) leakage during CCl4 intoxication.     

Isolation of steroidal glycosides from Solanum xanthocarpum and studies on their antifungal activities

Isolation of the methanol extract of Solanum xanthocarpum resulted in the isolation and characterization of carpesterol (1) and four steroidal glycosides (2, 3, 4, and 5). The structures of these compounds were established by spectroscopic analysis. The antifungal activity of the steroidal compounds extracted from the fruits of S. xanthocarpum was investigated against Aspergillus niger and Trichoderma viride. The isolated compounds 1, 2, 3, 4, and 5 exhibited inhibitory effects on the radial growth of A. niger and Trichoderma viride.     

Acute toxicity and hepatotoxicokinetic studies of Tamarindus indica extract

Tamarindus indica is widely used as a food and beverage and in traditional medicine. The apparent lack of dose standardization in herbal medicine necessitates the evaluation of the lethality T. indica on Artemia salina nauplii and chicken embryos via in vitro and in vivo techniques. Furthermore, hepatotoxicokinetics of the crude extract and fractions on Wister rats was also assessed. At concentrations of 200, 20 and 2 μg/mL, crude extract and fractions showed brine shrimp death percentages ranging from 86.70% to 3.30% and the sub-fractions showed death percentage ranges of 46.70% to 3.30%. Calculated LD?? values ranged from 832 μg/mL to 5,019 μg/mL. Dosing Wister rats with 25% and 50% concentration of LD?? determined for crude extract and fractions on chicken embryos showed an elevation in the ALT and AST levels in the serum. Brine shrimps and chicken embryos showed a positive correlation, with R2 values of 0.541 and 0.588 (P ≤ 0.05) for fractions and subfractions, respectively, as media for the lethality assay. Dose standardization in folk herbal medicine is imperative as T. indica used as food and medicine has been shown to be toxic at high doses. Brine shrimp and chicken embryos may be comparably used as medium for toxicity assay.     

Influence of basil oil extract on the antioxidant and antifungal activities of nanostructured carriers loaded with nystatin

The combination of basil oil, natural antifungal, and nystatin has the potential to prevent the extension of topical fungal infections towards systemic infections. The aim of this study was to develop formulations based on basil oil and nystatin with the desired antifungal and antioxidant activity and low toxicity by using lipid nanocarriers. The synthesized nanocarriers showed spherical and homogeneous particles with main diameters less than 150 nm, as determined by TEM. The scanning calorimetric study revealed an imperfect crystallization in the core of lipid nanocarriers. Quantitative results suggested that basil oil concentration affects encapsulation efficiency. The prepared nanocarriers guaranteed an increased nystatin encapsulation by using 3% basil oil content. Chemiluminescence assay proved that the protective activity against oxygen free radicals was influenced by nystatin concentration. The in vitro antifungal studies revealed a better activity of the nanocarriers loaded with 1% nystatin in comparison with 0.5% loading.     

Antibacterial, antifungal and cytotoxic activities of two flavonoids from Retama raetam flowers

We have investigated the antibacterial, antifungal and cytotoxic activities of two flavonoids isolated from Retama raetam flowers using the disc diffusion and micro-dilution broth methods. The cytotoxic activity was tested against Hep-2 cells using the MTT assay. The compounds licoflavone C (1) and derrone (2) were active against Pseudomonas aeruginosa and Escherichia coli (7.81-15.62 μg/mL) and showed important antifungal activity. Strong antifungal activity against Candida species (7.81 μg/mL) was for example found with compound 2. The tested compounds also showed strong cytotoxicity against Hep-2 cells. These two compounds may be interesting antimicrobial agents to be used against infectious diseases caused by many pathogens.     

Synthesis of polyfunctionally substituted heteroaromatic compounds via benzotriazolyl chalcones with antimicrobial and antifungal activities

The utility of both 3‐(1‐benzotriazolyl) chalcone derivatives 3a‐c and 2‐(1‐benzotriazolyl)‐1,4‐pentadien‐3‐one (18) in the synthesis of some new 2‐(1H)‐pyridone, pyridine, pyrazole and isoxazole derivatives is reported. Antimicrobial and antifungal screening of some selected examples from the synthesized products were carried out. The structure of the newly synthesized compounds was elucidated by elemental analysis, ir, ¹H and ¹³C nmr investigations.     

Natural antifungal compounds from the peels of Ipomoea batatas Lam

Three antifungal compounds have been isolated for the first time from the peels of Ipomoea batatas Lam. Their structures were established on the basis of 1D and 2D NMR spectra data as well as ESI-MS and IR analysis. Urs-13(18)-ene-3β-yl acetate was found to possess a weak activity against Sporothrix schenckii and Trichophyton metagrophytes fungi with an MIC value of 50 μg/mL each. Stigmasterol and 3-friedelanol were equally active against T. metagrophytes.     

Chemical composition,protoscolicidal effects and acute toxicity of Pistacia atlantica Desf. fruit extract

The present study was designed to evaluate the chemical composition and scolicidal effects of Pistacia atlantica Desf. extract against protoscoleces of hydatid cysts and its acute toxicity in mice model. Various concentrations of the methanolic extract (5–50 mg/mL) were used for 10–60 min. Viability of protoscoleces was confirmed using eosin exclusion test (0.1%). Acute toxicity was also determined in mice model. The main components were β-myrcene (41.4%), α-pinene (32.48%) and limonene (4.66%). Findings demonstrated that P. atlantica extract at the concentrations of 25 and 50 mg/mL after 20 and 10 min of exposure killed 100% protoscoleces. The LD₅₀ of the intraperitoneal injection of the P. atlantica methanolic extract was 2.43 g/kg and the maximum non-fatal dose was 1.66 g/kg. Obtained results showed the potential of P. atlantica extract as a natural source with no significant toxicity for the production of new scolicidal agent to use in hydatid cyst surgery.     

Larvicidal, antimycobacterial and antifungal compounds from the bark of the Peruvian plant Swartzia polyphylla DC

The 95% ethanol extract of the bark of Swartzia polyphylla DC (Fabaceae) possesses important larvicidal, antimycobacterial and antifungal activity in vitro. Bioassay-guided studies performed on the crude ethanol extract afforded T-cadinol as the larvicidal and anti-Mycobacterium tuberculosis principle, while the antifungal activity of the extract is due to the presence of the flavonoids biochanin A and dihydrobiochanin A.