In vitro activity of plant extracts and alkaloids against clinical isolates of extended-spectrum β-lactamase (ESBL)-producing strains

The antibacterial activity of 80% ethanol extracts of 10 medicinal plants collected in Yunnan (Southwest China), was tested against clinical isolates of extended-spectrum β-lactamase (ESBL)-producing strains. Their MIC values ranged between 1.56-12.50 mg/mL. The most active plant extract was Chelidonium majus L. (MIC = 1.56 mg/mL). Two potent isoquinoline alkaloids, 8-hydroxydihydrosanguinarine and 8-hydroxydihydrochelerythrine, were identified as the major active principles through bioassay-guided fractionation and identification of the active ethyl acetate fraction from C. majus, with minimum MIC/MBC values of 15.63/62.50 mg/mL.     

In vitro antioxidant activity of extracts of Sybaris liquorice roots from Southern Italy

The antioxidant properties of extracts of Sybaris liquorice roots have been assessed using 2,2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity assay. The extracts, obtained by Soxhlet extraction (Et(2)O, AcOEt, MeOH and BuOH) of the yellow (inner part) and brown (cortex) root powders ensuing from decortication of the raw dry roots, followed by separation and powderisation, were analysed for their scavenging activity by evaluating the colourimetric decrease in the absorbance of DPPH. The highest antioxidant activity (98.39?±?0.56%) was observed in the case of the Et(2)O extract of the brown powder, at a concentration of 3.33?mg?mL(-1). Moreover, the total phenolic content of the extracts was determined using the Folin-Ciocalteu reagent and expressed as milligram gallic acid equivalent per gram of dry extract. Our results show that the Et(2)O extract of the liquorice root cortex could be used as an attractive natural source of antioxidant additives for food, cosmetic or pharmaceutical applications.     

In vitro antioxidant activity of the water and ethanol extracts of Forsythia koreana flowers

The antioxidant activities of the water and ethanol extracts of F. koreana flowers were evaluated using DPPH, superoxide anion (?O(-2)), and nitric oxide (?NO) radical scavenging activity assays. The SC(50) values of the water extract of F. koreana on DPPH, ?O(-2) and ?NO were 48.39, 24.36 and 100.21 μg mL(-1), respectively. The SC(50) values of the ethanol extract of F. koreana on the aforesaid free radicals were 57.50, 49.00 and 146.08 μg mL(-1), respectively. Further, the total phenolic contents of both extracts were determined and expressed as milligram gallic acid equivalent (GAE) per gram of extract. The water extract exhibited a higher phenolic content (113.78 mg GAE?g(-1)), while the ethanol extract showed 94.53?mg GAE?g(-1). Our findings demonstrate that the water and ethanol extracts of F. koreana flowers might be potential natural sources of antioxidative additives for use in the food and other allied industries.     

A calorimetric study of plant–plant and plant–soil interactions of extracts from Ixorhea tschudiana

The effect of the CHCl₃ and MeOH extracts from aerial parts from the Northwestern Argentina endemic species Ixorhea tschudiana Fenzl. on germination of the dicot tomato and the monoct onion and on soil microbial activity was studied by calorimetric and calorespirometric experiments. The CHCl₃ extract inhibited seedling growth of tomato which increased with increasing concentrations. Seeds imbibed with 250 mg dm^?3 extract germinated 24 h later than control and those imbibed with 100 and 500 mg dm^?3 extract. This was reflected in the calculated low specific seedling growth rate (p_SGΔH_B) as determined from calorespirometric experiments. On the other hand, seedlings obtained in 500 mg dm^?3 extract showed shorter and thicker hairy roots than control with significantly higher p_SGΔH_B. Probably, the extract induces inhibition of water uptake by seedling roots. Germination was reduced 50% in onion seeds imbibed with 500 mg dm^?3 CHCl₃ extract which apparently is due to higher rate of imbibition during the first stages as determined for calorimetry. On the other hand, 83 and 250 mg kg^?1 of the MeOH and CHCl₃ extract seem to selectively inhibit the growth of certain microorganisms and to enhance the activity of soil actinomycetes. Two actinobacteria were isolated from soil treated with these concentrations of both extracts: Kocuria sp. and Kocuria rosea; this latter species is known as a keratinolytic agent and seems to degrade complex carbon compounds of the soil and those incorporated by the MeOH extract. Both Kocuria specie seem to be beneficial for the soil converting substrate into biomass and thus I. tschudiana could be used as a soil phytoremediator.     

In vitro cytotoxic and antiviral activities of Ficus carica latex extracts

The latex of fig fruit (Ficus carica) is used in traditional medicine for the treatment of skin infections such as warts and also diseases of possible viral origin. Five extracts (methanolic, hexanic, ethyl acetate, hexane-ethyl acetate (v/v) and chloroformic) of this species were investigated in?vitro for their antiviral potential activity against herpes simplex type 1 (HSV-1), echovirus type 11 (ECV-11) and adenovirus (ADV). To evaluate the capacity of the extracts to inhibit the replication of viruses, the following assays were performed: adsorption and penetration, intracellular inhibition and virucidal activity. Observation of cytopathic effects was used to determine the antiviral action. The hexanic and hexane-ethyl acetate (v/v) extracts inhibited multiplication of viruses by tested techniques at concentrations of 78 μg mL(-1). These two extracts were possible candidates as herbal medicines for herpes virus, echovirus and adenovirus infectious diseases. All extracts had no cytotoxic effect on Vero cells at all tested concentrations.     

Phytochemical screening, antibacterial activity and in vitro interactions between Costus cf. arabicus L. with UV-A and aminoglycosides

In this study, the methanol extracts of of Costus cf. arabicus L. were evaluated for antibacterial activity against multiresistant strains of Escherichia coli and Staphylococcus aureus. The antibacterial and modulatory activity of the extracts was assayed by microdilution. The light-enhanced antibacterial activity was assayed by light regimen. The growth of the bacteria tested was not inhibited by the extracts. The minimum inhibitory concentration (MIC) values ranged from 512 to ≥1024 μg·m L(-1). However, the antibiotic activity of the aminoglycosides was synergistically enhanced when these extracts were associated in sub-inhibitory concentrations with the antibiotics. Both extracts showed activity against at two standard bacterial strains. Because of this, we suggest that the ethanol extracts of the stems and leaves of Costus cf. arabicus L. show potential antibacterial, light-induced and synergistic antibiotic activity. With such results, these extracts are proven to be a promising source of antibacterial and modulatory agents.     

Composition and in vitro antibacterial activity of essential oils from four Satureja species growing in Iran

The composition and in?vitro antibacterial activity of essential oils from four Satureja species (S. bachtiarica, S. khuzistanica, S. mutica and S. rechingeri) growing in Iran were determined. According to the results of GC-FID and GC-MS analysis, all oil samples were principally composed of phenolic constituents (carvacrol and/or thymol) with the percentages ranging from 41.2% (S. bachtiarica) to 77.7% (S. rechingeri). Determining antibacterial activities by the disc diffusion method against two Gram-positive and two Gram-negative bacteria revealed the maximum activity against Bacillus cereus with a range of minimum inhibitory concentration values from 0.25 to 1?mg?mL(-1) and minimum bactericidal concentration values from 0.5 to 1?mg?mL(-1). The oils of S. khuzistanica and S. rechingeri appeared to be more active in general than those of other species. In conclusion, the essential oils of studied Satureja species have the potential to be considered as alternatives for synthetic food preservatives.     

Textile with silver silica spheres: its antimicrobial activity against <Emphasis Type="Italic">Escherichia coli and Staphylococcus aureus</Emphasis>

The aim of this study was to investigate antimicrobial activity of textiles doped with silver in different forms. Three types of textiles were prepared and examined: textiles doped with commercially available Ag nanoparticles, textiles doped with commercial colloidal silver and textiles doped with silver silica SiO₂/Ag spheres. The specimens of silica submicron spheres were synthesized by the sol–gel method as a matrix for biological active silver. The results of microbiological tests revealed that among three kinds of Ag doped textiles only these doped with SiO₂/Ag spheres are bacteriostatically active. During the experiments minimal inhibiting bacteria growth concentration of active SiO₂/Ag spheres added to textiles was determined.     

GC–MS characterisation and antibacterial activity evaluation of Nigella sativa oil against diverse strains of Salmonella

Salmonella resistance is becoming a worldwide serious health issue in these days; therefore, it is an urgent need to develop some alternative approaches to overcome this problem. Twenty bacterial strains were isolated and purified from different environmental sources and confirmed as Salmonella by morphological and biochemical analyses. Further confirmation was done by 16s rRNA sequencing. Antibiotic susceptibility test was performed by well diffusion assay against different concentrations of Ceftriaxone and Ciprofloxacin. The behaviour of both antibiotics was different against diverse strains of Salmonella. Salmonella strains resistant to both antibiotics were analysed for antibacterial activity of natural extracts of Nigella sativa (black seeds). N. sativa oil was found to be more effective against Salmonella species for which even Ceftriaxone and Ciprofloxacin were ineffective. Gas chromatography and mass spectrometry analysis of N. sativa oil was also accomplished, exhibiting 10 compounds including thymoquinone, p-cymene, cis-carveol, thymol, α-phellandrene, α-pinene, β-pinene, trans-anethole, α-longipinene and longifolene.     

DCC/DMAP mediated esterification of hydroxy and non-hydroxy olefinic fatty acids with β-sitosterol:In vitro antimicrobial activity

<正>A new series of fatty alkenoates were synthesized using an appropriate synthetic route involving DCC and DMAP as catalysts. Compounds were characterized by their spectral data.All the synthesized compounds were evaluated for their in vitro antimicrobial activity.The minimum inhibitory concentration(MIC),minimum bacterial concentration(MBC) and minimum fungicidal concentration(MFC) were determined for test compounds as well as for reference standards.Among the compounds tested, compounds having hydroxy group at the fatty acid chain showed the most potent antibacterial as well as antifungal activities.     

Anti-allergic effect of the flavonoid myricitrin from Myrica rubra leaf extracts in vitro and in vivo

Flavonoids are ingested by the general population as anti-oxidant and anti-inflammatory agents. In this study, we investigated the effects of myricitrin, a flavonoid rich in Myrica rubra leaf, upon anti-inflammatory action. Myrica rubra leaf extracts inhibited pro-inflammatory TNFα production in a macrophage cell line, Raw264.7 cells. We observed that the serum IgE levels in the leaf extract-treated DO11.10, a mouse allergy model, were down-regulated. HPLC was performed to demonstrate that M. rubra leaf extracts contain a large amount of myricitrin. We observed an inhibitory effect of HPLC-purified myricitrin on TNFα production in Raw264.7 cells. Thus, myricitrin may be of potential interest in the management of inflammatory conditions.     

In vitro antitumor activity of titanocene alanine complex and its interaction with nucleic acids

Titanocene alanine complex, Cp2Ti(O2CCH(CH3)NH3+Cl-)2, has been found to have in vitro antitumor activity against Ehrlich ascites tumor cells. Study of the interaction between Cp2Ti(O2CCH(CH3)NH+Cl-)2 and DNA by UV-VIS spectra, fluorescence spectra, agarose gel elec-trophoresis reveals that Cp2Ti(O2CCH(CH3)NH3 Cl-)2 forms a stable compound with DNA in molar ratio 1:1 and reduces the migration rate of ccc-DNA band and oc-DNA band. However, unlike cis-platin, the complex does not induce nicking of DNA even after a long incubation at a high ratio of the complex to DNA. The results suggest that titanocene-based antitumor agents have different mechanism of action from cisplatin-like antitumor agents.     

In vitro antioxidant and radical scavenging of Guinean kinkeliba leaf (Combretum micranthum G. Don) extracts

The antioxidant properties of the water and ethanol leaf extracts of kinkeliba (Combretum micranthum) were investigated, including scavenging of the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical (IC?? values: 8.02?±?0.34 for the ethanol extract [KE] and 9.1?±?0.28 for the water extract [KW]), the 2,2'-azinobis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical (IC(50) values: 7.4?±?0.14 for KE and 11.8?±?0.01 for KW) and the hydroxyl radical (58.1% for KE and 61.1% for KW). The ferric thiocyanate method, reducing power, metal chelating activity, an assay of protein oxidation and the β-carotene-linoleic bleaching assay were also used. Butylated hydroxytoluene and ascorbic acid were used as the reference antioxidant compounds. At 20 mg mL?1 concentration, KW and KE provided 36.8% and 75.1% inhibition of lipid peroxidation of linoleic acid emulsion, respectively. The IC?? values of the ethanol extract in ABTS and DPPH tests were significantly lower than those from the water extract. Furthermore, crude polyphenols were extracted from kinkeliba leaf with 90% ethanol solution using a water bath treatment and then purified by a macroporous resin, AB-8. The polyphenols from kinkeliba leaf were subjected to analyses by RP-HPLC and ESI-MS. The dominant polyphenols in kinkeliba leaf were identified as gallic acid, rutin trihydrate, (+)-catechin and benzoic acid.     

In vitro antimycobacterial activity and HPLC-DAD screening of phenolics from Ficus benjamina L. and Ficus luschnathiana (Miq.) Miq. leaves

The total phenolic content (Folin-Ciocalteu) of the leaves of Ficus benjamina and Ficus luschnathiana was evaluated and screened by HPLC-DAD. Ficus luschnathiana crude extract (CE) presented phenolic content higher than that of F. benjamina (149.92?±?3.65 versus 122.63?±?2.79?mg of GAE). Kaempferol (1.63?±?0.16?mg?g(-1) dry weight of CE) and chlorogenic acid (17.77?±?0.57?mg?g(-1) of butanolic fraction) were identified and quantified in F. benjamina, whereas rutin (1.39?±?0.20?mg?g(-1)), caffeic (1.14?±?0.13?mg?g(-1)) and chlorogenic (3.73?±?0.29?mg?g(-1)) acids were quantified in the CE of F. luschnathiana. Additionaly, rutin (15.55?±?1.92?mg?g(-1)) and quercetin (3.53?±?0.12?mg?g(-1)) were quantified in ethyl acetate and butanolic fractions, respectively. Antimycobacterial activity of CEs and fractions was evaluated against Mycobacterium smegmatis by broth microdilution method. Ethyl acetate fraction from F. benjamina and n-butanol fraction from F. luschnathiana displayed the highest inhibitory activity (MIC?=?312.50?μg?mL(-1) and 156.25?μg?mL(-1), respectively). Further studies are required to identify the compounds directly related to antimycobacterial activity.     

In vitro biological activity of aromadendrin-4′-methyl ether isolated from root extract of Ventilago madraspatana Gaertn with relevance to anticandidal activity

In this study, antimicrobial and antioxidant activities of the hexane extract of the root of Ventilago madraspatana were evaluated. Based on the significant bioactivity of crude hexane extract, an active compound was purified from the root extract. The active compound was further purified and identified as aromodendrin-4′-methyl ether by the ¹H NMR spectrum. The isolated compound significantly inhibited Staphylococcus epidermidis with the lowest MIC and MBC at 78 μg/mL (P < 0.05). The compound also exhibited significant anticandidal activity with MIC and MBC values of 312 and 625 μg/mL, respectively. The radical scavenging activity of aromodendrin-4′-methyl ether was evident by its lower IC₅₀ values of 60 μg/mL for DPPH scavenging and 3.2 μg/mL for ABTS scavenging. The compound also exhibited ferrous ion chelation and H₂O₂ scavenging activities. The study is an attempt to increase the industrial utility of V. madrasapatana.     

Documentation of bioactive principles of the flower from Caralluma retrospiciens (Ehrenb) and in vitro antibacterial activity – Part B

The purpose of this study was to explore the biocomponents of flowers from Caralluma retrospiciens (Ehrenb). The study investigated the FT-IR and GC–MS spectral analysis of flower from C. retrospiciens (Ehrenb). A flower concentrate (FC) was prepared and the functional groups were determined by FT-IR spectroscopy study. FT-IR analysis showed the presence of significant compounds at frequency 3287.45, 2850.32, 2595.91, 2524.69, 2041.07 cm⁻¹. The GC–MS study demonstrated the presence of unique pharmaceutically important compounds. The extract was characterized by the presence of unique compounds such as “7,8-Epoxylanostan-11-ol, 3-acetoxy”, “Pregnan-20-one, 5,6-epoxy-3-hydroxy-, (3á,5á,6á)-”, “Benzenepropanoic acid, 3,5-bis(1,1-dimethylethyl)-4-hydroxy-, methyl ester”, “Hexadecanoic acid, methyl ester”, “Dasycarpidan-1-methanol, acetate”, etc. The antibacterial effect of the FC showed a wide spectrum of activity against the screened human pathogenic bacteria. The activity was predominantly against Gram-negative bacteria.     

Synthesis of multivalent glycoclusters from 1-thio-β-D-galactose and their inhibitory activity against the β-galactosidase from E. coli

The synthesis of multivalent glycoclusters, designed to be compatible with biological systems, is reported. A variety of 1-thio-β-D-galactosides linked to a terminal triple bond through oligoethyleneglycol chains of variable lengths has been synthesized. Also, azide-containing oligosaccharide scaffolds were prepared from trehalose, maltose, and maltotriose by direct azidation with NaN(3)/PPh(3)/CBr(4). Click reaction between the thiogalactoside residues and the azide scaffolds under microwave irradiation afforded a family of glycoclusters containing 1 to 4 residues of 1-thio-β-D-galactose. The yields went from moderate to excellent, depending on the valency of the desired product. Deacetylation with Et(3)N/MeOH/H(2)O led to the final products. Complete characterization of the products was performed by NMR spectroscopy and HR-MS techniques. Their activities as inhibitors of β-galactosidase from E. coli were determined by using the Lineweaver-Burk method. The use of hydrophilic carbohydrate scaffolds for the synthesis of multivalent galactosides represents an interesting approach to improve their pharmacokinetics and bioavailability. In addition, the presence of the thioglycosidic bond will improve their stability in biological fluids.