Chemical Composition,Antibacterial, Schistosomicidal,and Cytotoxic Activities of the Essential Oil of Dysphania ambrosioides (L.) Mosyakin & Clemants (Chenopodiaceae)

We have investigated the chemical composition and the antibacterial activity of the essential oil of Dysphania ambrosioides (L.) Mosyakin & Clemants (Chenopodiaceae) (DA‐EO) against a representative panel of cariogenic bacteria. We have also assessed the in vitro schistosomicidal effects of DA‐EO on Schistosoma mansoni and its cytotoxicity to GM07492‐A cells in vitro. Gas chromatography (GC) and gas chromatography‐mass spectrometry (GC/MS) revealed that the monoterpenes cis‐piperitone oxide (35.2%), p‐cymene (14.5%), isoascaridole (14.1%), and α‐terpinene (11.6%) were identified by as the major constituents of DA‐EO. DA‐EO displayed weak activity against Streptococcus sobrinus and Enterococcus faecalis (minimum inhibitory concentration (MIC) = 1000 μg/ml). On the other hand, DA‐EO at 25 and 12.5 μg/ml presented remarkable schistosomicidal action in vitro and killed 100% of adult worm pairs within 24 and 72 h, respectively. The LC₅₀ values of DA‐EO were 6.50 ± 0.38, 3.66 ± 1.06, and 3.65 ± 0.76 μg/ml at 24, 48, and 72 h, respectively. However, DA‐EO at concentrations higher than 312.5 μg/ml significantly reduced the viability of GM07492‐A cells (IC₅₀ = 207.1 ± 4.4 μg/ml). The selectivity index showed that DA‐EO was 31.8 times more toxic to the adult S. mansoni worms than GM07492‐A cells. Taken together, these results demonstrate the promising schistosomicidal potential of the essential oil of Dysphania ambrosioides.     

Chemical Composition,Antioxidant Properties, α‐Glucosidase Inhibitory,and Antimicrobial Activity of Essential Oils from Acacia mollissima and Acacia cyclops Cultivated in Tunisia

The genus Acacia is quite large and can be found in the warm subarid and arid parts, but little is known about its chemistry, especially the volatile parts. The volatile oils from fresh flowers of A. mollissima and A. cyclops (growing in Tunisia) obtained by hydrodistillation were analyzed by GC then GC/MS. Eighteen (94.7% of the total oil composition) and 23 (97.4%) compounds were identified in these oils, respectively. (E,E)‐α‐Farnesene (51.5%) and (E)‐cinnamyl alcohol (10.7%) constituted the major compounds of the flower oil of A. mollissima, while nonadecane (29.6%) and caryophyllene oxide (15.9%) were the main constituents of the essential oil of A. cyclops. Antioxidant activity of the isolated oils was studied by varied assays, i.e., 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) and 2,2‐azinobis 3‐ethylbenzothiazoline‐6‐sulfonic acid (ABTS); the isolated oils showed lowest IC₅₀ (4 – 39 μg/ml) indicating their high antioxidant activity. The α‐glucosidase inhibitor activity was also evaluated and Acacia oils were found to be able to strongly inhibit this enzyme with IC₅₀ values (81 – 89 μg/ml) very close to that of acarbose which was used as positive control. Furthermore, they were tested against five Gram‐positive and Gram‐negative bacteria and one Candida species. Essential oil of A. mollissima was found to be more active than that of A. cyclops, especially against Pseudomonas aeruginosa (MIC = 0.31 mg/ml and MBC = 0.62 mg/ml).     

Anti‐HSV‐1 and HSV‐2 Flavonoids and a New Kaempferol Triglycoside from the Medicinal Plant Kalanchoe daigremontiana

Kalanchoe daigremontiana (Crassulaceae) is a medicinal plant native to Madagascar. The aim of this study was to investigate the flavonoid content of an aqueous leaf extract from K. daigremontiana (Kd), and assess its antiherpetic potential. The major flavonoid, kaempferol 3‐O‐β‐d ‐xylopyranosyl‐(1 → 2)‐α‐l ‐rhamnopyranoside ( 1 ), was isolated from the AcOEt fraction (Kd‐AC). The BuOH‐soluble fraction afforded quercetin 3‐O‐β‐d ‐xylopyranosyl‐(1 → 2)‐α‐l ‐rhamnopyranoside ( 2 ) and the new kaempferol 3‐O‐β‐d ‐xylopyranosyl‐(1 → 2)‐α‐l ‐rhamnopyranoside‐7‐O‐β‐d ‐glucopyranoside ( 3 ), named daigremontrioside. The crude extract, Kd‐AC fraction, flavonoids 1 and 2 were evaluated using acyclovir‐sensitive strains of HSV‐1 and HSV‐2. Kd‐AC was highly active against HSV‐1 (EC₅₀ = 0.97 μg/ml, SI > 206.1) and HSV‐2 (EC₅₀ = 0.72 μg/ml, SI > 277.7). Flavonoids 1 and 2 showed anti‐HSV‐1 (EC₅₀ = 7.4 μg/ml; SI > 27 and EC₅₀ = 5.8 μg/ml; SI > 8.6, respectively) and anti‐HSV‐2 (EC₅₀ = 9.0 μg/ml; SI > 22.2 and EC₅₀ = 36.2 μg/ml; SI > 5.5, respectively) activities, suggesting the contribution of additional substances to the antiviral activity.     

Ciprofloxacin-Induced Antibacterial Activity is Reversed by Vitamin E and Vitamin C

In the present study, we investigated the possible involvement of oxidative stress in ciprofloxacin-induced cytotoxicity against several reference bacteria including Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 29213, and clinical isolate of methicillin-resistant Staphylococcus aureus (MRSA). Oxidative stress was assessed by measurement of hydrogen peroxide generation using a FACScan flow cytometer. The antibacterial activity of ciprofloxacin was assessed using the disk diffusion method and by measuring the minimum inhibitory concentration (MIC). Ciprofloxacin induced a dose-dependent antibacterial activity against all bacteria where the highest tested concentration was 100 ug/ml. Results revealed that E. coli cells were highly sensitive to ciprofloxacin (MIC = 0.21 μg/mL ± 0.087), P. aeruginosa and S. aureus cells were intermediately sensitive (MIC = 5.40 μg/mL ± 0.14; MIC = 3.42 μg/mL ± 0.377, respectively), and MRSA cells were highly resistant (MIC = 16.76 μg/mL ± 2.1). Pretreatment of E. coli cells with either vitamin E or vitamin C has significantly protected cells against ciprofloxacin-induced cytotoxicity. These results indicate the possible antagonistic properties for vitamins C or E when they are used concurrently with ciprofloxacin.     

Identification,cloning, and functional characterization of EmrD-3, a putative multidrug efflux pump of the major facilitator superfamily from <Emphasis Type="Italic">Vibrio cholerae</Emphasis> O395

A putative multidrug efflux pump, EmrD-3, belonging to the major facilitator superfamily (MFS) of transporters and sharing homology with the Bcr/CflA subfamily, was identified in Vibrio cholerae O395. We cloned the emrD-3 gene and evaluated its role in antimicrobial efflux in a hypersensitive Escherichia coli strain. The efflux activity of this membrane protein resulted in lowering the intracellular concentration of ethidium. The recombinant plasmid carrying emrD-3 conferred enhanced resistance to several antimicrobials. Among the antimicrobials tested, the highest relative increase in minimum inhibitory concentration (MIC) of 102-fold was observed for linezolid (MIC = 256 μg/ml), followed by an 80.1-fold increase for tetraphenylphosphonium chloride (TPCL) (156.2 μg/ml), 62.5-fold for rifampin (MIC = 50 μg/ml), >30-fold for erythromycin (MIC = 50 μg/ml) and minocycline (MIC = 2 μg/ml), 20-fold for trimethoprim (MIC = 0.12 μg/ml), and 18.7-fold for chloramphenicol (MIC = 18.7 μg/ml). Among the fluorescent DNA-binding dyes, the highest relative increase in MIC of 41.7-fold was observed for ethidium bromide (125 μg/ml) followed by a 17.2-fold increase for rhodamine 6G (100 μg/ml). Thus, we demonstrate that EmrD-3 is a multidrug efflux pump of V. cholerae, the homologues of which are present in several Vibrio spp., some members of Enterobacteriaceae family, and Gram-positive Bacillus spp.     

Immunoassay‐based Techniques for Early and Specific Detection of Latent Postharvest Anthracnose in Mango

The postharvest anthracnose pathogen Colletotrichum gloeosporioides inciting latent or quiescent infection of mango was detected in early stages using immunoassay methods. Twenty‐five pathotypes isolated from different agroclimatic zones of Tamil Nadu, Karnataka and Pondicherry, India, revealed the variation in protein profile analysis (SDS‐PAGE). The polyclonal antibodies (PCA) were raised against the unfractioned mycelial protein (UMP) and a 40‐kDa polypeptide present in all pathotypes. Standardization of antigen and antiserum dilutions revealed that an antigen dilution of 1 : 200 (protein concentration of 20 μg/ml) and antiserum dilution of 1 : 100 (protein concentration of 40 μg/ml raised against UMP) and 1 : 200 (protein concentration of 20 μg/ml raised against 40 kDa polypeptide) was found to be optimum for the detection of anthracnose pathogen. Both antisera detected the C. gloeosporioides antigen in enzyme‐linked immunosorbent assays (ELISAs), dot immunobinding assays (DIBAs) and Western blots. The specificity in reaction was compared by isolating other Colletotrichum spp. from various hosts viz., C. lindemuthianum (beans), C. falcatum (sugarcane), C. musae (banana), C. capsici (chillies) and Botryodiplodia theobromae (mango). The antisera generated against UMP revealed the cross‐reaction with other host isolates and mango stem end rot pathogen (B. theobromae). The PCA raised against 40‐kDa polypeptide exhibited the specific reaction with C. gloeosporioides isolates in all the immunoassay techniques. By utilizing both PCA, the presence of latent infection was observed in healthy‐looking leaves, flowers and fruits in orchard conditions. The fruit tissues recorded high absorbance values followed by flowers and leaves in all the detection methods. The ELISA technique was also useful in assessing the pathogen inoculum at various biocontrol formulations sprayed mango trees under field conditions. The fluorescent pseudomonad strains mixture (KFP1 + FP7) amended with chitin sprayed at 30‐day intervals revealed the significant reduction in pathogen load than other formulations and unsprayed control.     

The effect of chemical and biological treatment on root and crown rot disease caused by Phytophthora cryptogea Pethybr. & Lafferty in Gerbera

Phytophthora root and crown rot (Phytophthora cryptogea) on gerbera is difficult to manage because most gerbera cultivars are susceptible to P. cryptogea. This study was conducted in order to determine the in vivo (pot experiment) efficacy of some fungicides and biofungicides. In pot experiments, fungicides were applied 7 days after inoculation with P. cryptogea, while biofungicide was applied 7 days before inoculation. In this study, soil drenches of five fungicides were tested. “Ametoctradin+dimethomorph (100 ml/day),” “mandipropamid+difenoconazole (60 ml/day),” “propamocarb+fosetyl‐Al (200 ml/day),” “mancozeb+metalaxyl‐M (250 g/day)” and “azoxystrobin+difenoconazole (100 ml/day)” active substances were used. Similarly, one biofungicide Bacillus amyloliquefaciens syn. MBI 600 (50 g/100 L) was applied by soil drenching. Efficacy of treatments was assessed according to the percentage of the root system which was visibly rotten at the end of the experiment. Root and crown rot severity was rated on a scale of 0 = 0% root system necrotic, 1 = 1%‐25% necrotic, 2 = 26%‐50% necrotic, 3 = 51%‐75% necrotic and 4 = 76%‐100% necrotic from 12 to 21 days. In this experiment, “azoxystrobin 200 g/L + difenoconazole 125 g/L” exhibited the highest efficacy against P. cryptogea with a ratio of 43.75%. The other fungicides and biofungicides ametoctradin 300 g/L + dimethomorph 225 g/L, mandipropamid 250 g/L + difenoconazole 250 g/L, propamocarb 530 g/L + fosety‐Al 310 g/L, mancozeb 64%+metalaxyl‐M 4% and Bacillus amyloliquefaciens syn. MBI 600 11% were ineffective. Importance should be given to management strategies of P. cryptogea of and more experiments should be carried out for a better understanding of the use of registered fungicides and biofungicides.     

Minimum inhibitory concentration (MIC) of crude preparations of Brevibacillus laterosporus SA14 bioactive material compared to vancomycin and oxacillin, against clinical isolates of methicillin-resistant Staphylococcus aureus

Secondary metabolites, particularly bioactive compounds, from probiotic bacteria, are good candidates for replacing antibiotics to which bacteria have become resistant. In order to compare bioactive crude material from strain SA14 of Brevibacillus laterosporus with two antibiotics, the MICs of this bioactive crude and those of antibiotics vancomycin and oxacillin, against methicillin-resistant Staphylococcus aureus (MRSA), were determined. The result indicated that the MIC (3.6–19.2 μg/ml) of bioactive crude was higher than vancomycin (MIC = 1.28–2.56 μg/ml) when tested against MRSA. Interestingly, all tested strains of MRSA were susceptible to bioactive crude and were approximately 5.2-fold more potent than oxacillin (MIC > 100 μg/ml). Its activity against MRSA gives support for further evaluation, and the development of this substance for therapeutic use.     

2,6‐Dimethoxy‐1,4‐Benzoquinone Enhances Resistance Against the Rice Blast Fungus Magnaporthe oryzae

We investigated the effect of 2,6‐dimethoxy‐1,4‐benzoquinone (DMBQ) on induced resistance to Magnaporthe oryzae in rice. DMBQ concentrations greater than 50 μg/ml inhibited spore germination and appressorium formation in M. oryzae. When rice leaves pretreated with 10 μg/ml DMBQ, which did not show antifungal activity against spore germination and appressorium formation of M. oryzae, were inoculated with M. oryzae spores 5 days after DMBQ pretreatment, blast lesion formation was inhibited compared with control leaves pretreated with distilled water. In addition, infection‐inhibiting activity against M. oryzae was significantly enhanced in rice leaf sheaths pretreated with 10 μg/ml DMBQ. H₂O₂ generation was observed in rice leaves pretreated with DMBQ, and PAL, POX, CHS and PR10a were significantly expressed in these leaves. These results suggested that DMBQ can protect rice from blast disease caused by M. oryzae.     

Comparison of Polyphenol Profile and Antimutagenic and Antioxidant Activities in Two Species Used as Source of Solidaginis herba – Goldenrod

European Pharmacopoeia accepts two equivalent species Solidago canadensis L. and S. gigantea Aiton as goldenrod (Solidaginis herba). We compared phytochemical profile of both species from invasive populations in Poland. Further, we compared in vitro antimutagenic and antioxidant activities of solvent extracts from aerial (AP) and underground parts (UP). In S. gigantea, flavonoid profile was dominated by quercetin glycosides, with quercitrin as the major compound. In S. canadensis, quercetin and kaempferol rutinosides were two major constituents. Caffeoylquinic acids (CQAs) were less diverse with 5‐CQA as a main compound. In UP, over 20 putative diterpenoids were detected, mostly unidentified. Several CQAs were present in higher amounts than in AP. Antioxidant and antimutagenic activities were different between species and organs, with the strongest inhibition of lipid peroxidation by Et₂O and AcOEt fractions from AP of both species (IC₅₀ 13.33 – 16.89 μg/mL) and BuOH fraction from S. gigantea UP (IC₅₀ = 13.32 μg/mL). Chemical mutagenesis was completely inhibited by non‐polar fractions, but oxidative mutagenesis was inhibited up to 35% only by S. canadensis. No clear relationship was found between chemical profiles and antimutagenic activity. In conclusion, both species have diverse activity and their phytochemical profiles should be considered in quality evaluation. UP of these weeds can also provide potential chemopreventive substances for further studies.     

Antifungal Monoterpene Derivatives from the Plant Endophytic Fungus Pestalotiopsis foedan

A new monoterpene lactone, (1R,4R,5R,8S)‐8‐hydroxy‐4,8‐dimethyl‐2‐oxabicyclo[3.3.1]nonan‐3‐one ( 1 ), along with one related known compound, (2R)‐2‐[(1R)‐4‐methylcyclohex‐3‐en‐1‐yl]propanoic acid ( 2 ), were isolated from the liquid culture of the plant endophytic fungus Pestalotiopsis foedan obtained from the branch of Bruguiera sexangula. The structure and absolute configuration of 1 were determined on the basis of extensive analysis of NMR spectra combined with computational methods via calculation of the optical rotation (OR) and ¹³C‐NMR. Both compounds exhibited strong antifungal activities against Botrytis cinerea and Phytophthora nicotianae with MIC values of 3.1 and 6.3 μg/ml, respectively, which are comparable to those of the known antifungal drug ketoconazole. Compound 2 also showed modest antifungal activity against Candida albicans with a MIC value of 50 μg/ml.     

Synthesis and larvicidal activity of indole derivatives against Aedes aegypti (Diptera: Culicidae)

In light of the challenges to control Aedes aegypti and the critical role that it plays as arbovirus vector, it is imperative to adopt strategies that provide fast, efficient and environmentally safe control of the insect population. In the present study, we synthesized six indole derivatives (C1‐C6) and examined their larvicidal activity and persistence against Ae. aegypti larvae, as well as their toxicity towards Raw 264.7 macrophages, Vero cells, Chlorella vulgaris BR017, Scenedesmus obliquus BR003, Caenorhabditis elegans N2 and Galleria mellonella. Among the bioactive compounds (C1, C2, C4 and C5), C2 exerted the strongest larvicidal activity against Ae. aegypti, with LC50 = 1.5 μg/ml (5.88 µM) and LC90 = 2.4 μg/ml (9.50 µM), indicating that the presence of chlorine or bromine groups in the aromatic ring improved the larvicidal activity of the indole derivatives. C1, C2, C4 and C5 did not reduce viability of RAW 264.7 macrophages, Vero cells, C. elegans N2 and G. mellonella. Compounds C1, C2 and C5 did not affect the growth of C. vulgaris BR017 and S. obliquus BR003. Analysis of larvicidal persistence under laboratory conditions revealed that the effect of compounds C1, C2, C4 and C5 lasted for 30 days and caused 100% of larvae mortality within few hours. Altogether, our findings demonstrate that the indole derivatives C1, C2, C4 and C5 effectively control Ae. aegypti larvae population, without clear signs of toxicity to mammalian cells, algae, C. elegans and G. mellonella.     

Chemical Composition,Antimicrobial and Cytotoxic Activity of Heracleum verticillatum Pančić and H. ternatum Velen. (Apiaceae) Essential Oils

In this work, the chemical composition, antimicrobial and cytotoxic activity of Heracleum verticillatum Pan?i? and H. ternatum Velen . root, leaf, and fruit essential oils were investigated. The composition was analyzed by GC and GC/MS. Heracleum verticillatum and H. ternatum root oils were dominated by monoterpenes, mostly β‐pinene (23.5% and 47.3%, respectively). Heracleum verticillatum leaf oil was characterized by monoterpenes, mainly limonene (20.3%), and sesquiterpenes, mostly (E)‐caryophyllene (19.1%), while H. ternatum leaf oil by the high percentage of phenylpropanoids, with (Z)‐isoelemicin (35.1%) being dominant constituent. Both fruit oils contained the majority of aliphatic esters, mostly octyl acetate (42.3% in H. verticillatum oil and 49.0% in H. ternatum oil). The antimicrobial activity of the oils was determined by microdilution method against eight bacterial and eight fungal strains. The strongest effect was exhibited by H. verticillatum root oil, particularly against Staphylococcus aureus, Salmonella typhimurium (MICs = 0.14 mg/ml, MBCs = 0.28 mg/ml), and Trichoderma viride (MIC = 0.05 mg/ml, MFC = 0.11 mg/ml). Cytotoxic effect was determined by MTT test against malignant HeLa, LS174, and A549 cells (IC₅₀ = 5.9 – 146.0 μg/ml), and against normal MRC‐5 cells (IC₅₀ > 120.1 μg/ml). The best effect was exhibited by H. verticillatum root oil on A549 cells (IC₅₀ = 5.9 μg/ml), and H. ternatum root oil against LS174 cells (IC₅₀ = 6.7 μg/ml).     

Chemical Characteristics,Antimicrobial, and Cytotoxic Activities of the Essential Oil of Egyptian Cinnamomum glanduliferum Bark

The essential oil isolated from the bark of Cinnamomum glanduliferum (Wall ) Meissn grown in Egypt was screened for its composition as well as its biological activity for the first time. The chemical composition was analyzed by GC and GC/MS. The antimicrobial activity of the oil was assessed using agar‐well diffusion method toward representatives for each of Gram‐positive bacteria, Gram‐negative bacteria, and fungi. The cytotoxic activity was checked using three human cancer cell lines. Twenty seven compounds were identified, representing 99.07% of the total detected components. The major constituents were eucalyptol (65.87%), terpinen‐4‐ol (7.57%), α‐terpineol (7.39%). The essential oil possessed strong antimicrobial activities against Escherichia coli, with an activity index of one and minimum inhibitory concentration (MIC) equaling to 0.49 μg/ml. The essential oil possessed good antimicrobial activities against methicillin‐resistant Staphylococcus aureus, Geotrichum candidum, Pseudomonas aeruginosa, Bacillus subtilis, Helicobacter pylori, Aspergillus fumigatus (MIC: 7.81, 1.95, 7.81, 0.98, 31.25, and 32.5 μg/ml, respectively). A considerable activity was reported against S. aureus and Mycobacterium tuberculosis (MIC; 32.5 and 31.25 μg/ml, respectively). The extracted oil was cytotoxic to colon (HCT‐116), liver (HepG2), and breast (MCF‐7) carcinoma cell lines with IC₅₀ of 9.1, 42.4, and 57.3 μg/ml, respectively. These results revealed that Egyptian Cinnamomum glanduliferum bark oil exerts antimicrobial and cytotoxic activities mainly due to eucalyptol and other major compounds.     

Chemical Profiling of the Essential Oils of Syzygium aqueum,Syzygium samarangense and Eugenia uniflora and Their Discrimination Using Chemometric Analysis

The essential oil compositions of the leaves of three related Myrtaceae species, namely Syzygium aqueum, Syzygium samarangense and Eugenia uniflora, were investigated using GLC/MS and GLC/FID. Altogether, 125 compounds were identified: α‐Selinene (13.85%), β‐caryophyllene (12.72%) and β‐selinene constitute the most abundant constituents in S. aqueum. Germacrene D (21.62%) represents the major compound in S. samarangense whereas in E. uniflora, spathulenol (15.80%) represents the predominant component. Multivariate chemometric analyses were used to discriminate the essential oils using hierarchical cluster analysis (HCA) and principal component analysis (PCA) based on the chromatographic results. The antimicrobial activity of the popularly used E. uniflora essential oil was assessed using broth microdilution method against six Gram‐positive, three Gram‐negative bacteria and two fungi. The oil showed moderate antimicrobial activity against Bacillus licheniformis exhibiting MIC and MMC of 0.63 mg/ml. The cytotoxic activity of E. uniflora essential oil was investigated against Trypanosoma brucei brucei (T. b. brucei) and MCF‐7 cancer cell line using MTT assay. It showed moderate activity against MCF‐7 cells with an IC₅₀ value of 76.40 μg/ml. On the other hand, T. brucei was highly susceptible to E. uniflora essential oil with IC₅₀ of 11.20 μg/ml, and a selectivity index of 6.82.     

Phytochemical Study of the Genus Salpichroa (Solanaceae), Chemotaxonomic Considerations,and Biological Evaluation in Prostate and Breast Cancer Cells

Twelve Salpichroa taxa have been phytochemically analyzed. From the aerial parts of S. scandens, four known salpichrolides A, C, I, S, and an unreported withanolide named salpichrolide V ( 1 ), were isolated. In S. dependens, S. gayi, S. glandulosa subsp. glandulosa, S. glandulosa subps. weddellii, S. leucantha, S. micrantha, S. microloba, S. proboscidea, S. ramosissima, S. tristis var. tristis, and S. weberbauerii, no withanolides were found. The chemical content of ca. 85% of the Salpichroa taxa is in agreement with molecular studies, which suggest that Salpichroa and Jaborosa, a genus considered morphologically close to Salpichroa, are distant in the systematic of the Solanoideae subfamily. Moreover, the in vitro cytotoxic activity of a set of natural salpichrolides and derivatives was examined against two prostate carcinoma cell lines (PC3 and LNCaP) and two human breast cancer cell lines (MCF‐7 and T47D). Several compounds showed moderate activity (IC₅₀ = 64.91 – 29.97 μm ).     

Synthesis and in vitro antitubercular activity of ferrocene-based hydrazones

We report here the synthesis and in vitro antitubercular activity of a new series of ferrocenyl derivatives. The quinoline-ferrocene hybrid 5 exhibited significant activity (MIC = 2.5-5 μg/ml) against Mycobacterium tuberculosis. Results indicate that such hybrid compounds provide an efficient approach for future pharmacological developments to fight against tuberculosis. Moreover, the antimalarial drug candidate ferroquine (FQ, SSR97193) was also evaluated mainly because of its structural similarity. FQ was found to display moderate inhibitory activity (MIC = 10-15 μg/ml) against M. tuberculosis. This new drug may offer an interesting alternative in endemic area where malaria and tuberculosis coexist.     

Production and Application of Syringomycin E as an Organic Fungicide Seed Protectant against Pythium Damping‐off

Syringomycin E (SRE) is a cyclic lipodepsinonapeptide with potent antifungal activity and is produced by certain strains of Pseudomonas syringae pv. syringae. In this study, its potential as an organic‐compatible agrofungicide and vegetable seed treatment against the soilborne pathogen Pythium ultimum var. ultimum was examined. A variant of P. syringae pv. syringae strain B301D with enhanced SRE‐producing capabilities was isolated and grown in a bioreactor with SRE yields averaging 50 mg/l in 40 h. SRE was extracted and purified through a large‐scale chromatography system using organic‐compatible processes and reagents. The minimum concentrations of the purified product required to inhibit 50 and 90% of P. ultimum oospore germination were determined as 31.3 and 250 μg/ml, respectively. Drench treatment of cucumber seeds in P. ultimum‐infested potting medium (500 oospores/g) with 50 μg/ml SRE or water with no SRE resulted in 90.2 ± 4.5% and 65.7 ± 4.6% germination rates, respectively. Seed coating with 0.03% (w/w) SRE allowed 65.7 ± 4.6% seedlings to germinate on naturally infested soil while 100.0 ± 0.0% of non‐coated seeds were unable to germinate due to Pythium infection. Organic‐compatible and scalably produced SRE is potentially a novel organic fungicide seed protectant.     

Variation in Polyphenolic Profiles,Antioxidant and Antimicrobial Activity of Different Achillea Species as Natural Sources of Antiglycative Compounds

A comparative study was carried out on the methanolic extracts from six Achillea species and the examined polyphenols from these plants on the formation of advanced glycation end‐products (AGE) in vitro. A. pachycephala which was richer in flavonoids (15 mg quercetin/g W) and phenolics (111.10 mg tannic acid/g DW) with substantial antioxidant activity (IC₅₀ = 365.5 μg/ml) presented strong anti‐AGE properties. Chlorogenic acid, luteolin, quercetin and caffeic acid were identified as the major polyphenols in the extracts by HPLC. In general, polyphenolic content follows the order of A. pachycephalla > A. nobilis > A. filipendulina > A. santolina > A. aucheri > A. millefolium. Most extracts exhibited marked anti‐AGE ability in the bovine serum albumin (BSA)/methylglyoxal (MG) system, though A. pachycephala showed the highest potential. The formation of AGEs was assessed by monitoring the production of fluorescent products and circular dichroism (CD) spectroscopy. Diminution in free radical production (assessed by 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) assays) is discussed as potential mechanism for delay or reduced AGE. The results demonstrate the antiglycative, antioxidant and antimicrobial potential of Achillea species which can be attributed to polyphenols content and the effectiveness on generation of AGEs, thus Achillea species can be considered as natural sources for slowing down glycation related diseases.     

Evidence of Phytoalexins in Rhizome of Atractylodis Maceocephalae Koidz Infected with Sclerotium rolfsii sacc Following Treatment with the Polysaccharides of Chrysanthemum indicum

Atractylenolides compounds (atractylenolide‐I, atractylenolide‐II and atractylenolide‐III) extracted from Atractylenolides macrocephala were analysed for their differential presence in the rhizome of both the infected and healthy plants and its fungitoxicity on prophylactic treatment with polysaccharides of Chrysanthemum indicum against Sclerotium rolfsii. It was evident that the plant under stress by pathogen has instigated the significant synthesis and accumulation of atractylenolide‐II and atractylenolide‐III in the rhizome of plants as a result of elicitation with polysaccharides of C. indicum. Our results also showed that the absence of atractylenolide‐II in the rhizome made the plant susceptible to S. rolfsii. Furthermore, on in vitro antifungal studies, exogenous application of atractylenolide‐II with the concentration of 200 μg/ml showed a significant inhibitory effect on mycelial growth by achieving a 77.23% antifungal activity rate, and a minimal inhibitory effect at a concentration of 12.5 μg/ml with atractylenolide‐II. To our knowledge, this novel study on phytoalexins in A. macrocephala suggested that A. macrocephala plants produce elevated levels of atractylenolide‐II and atractylenolide‐III in a pattern typical of phytoalexins, in response to an eliciting treatment after infection.