Maximum Growth Inhibition Research Articles

Characterization of phytochemical composition and bioactivity assessment of Pseudotrachydium kotschyi essential oils

Pseudotrachydium kotschyi is a native medicinal plant used as a local medicine from Lorestan province of western Iran having numerous biological properties. After GC−MS analysis of Pseudotrachydium kotschyi essential oils (PKEOs), some biological activities were investigated. Additionally, TNF-α and TGF-β1 were studied in Leishmania-infected macrophages (in vitro) and Carrageenan-induced paw edema in rats. Finally, anti-inflammatory and wound-healing potential of PKEOs were investigated in vivo in mice. Total components identified by GC−MS contained 53 molecules, among which Z-α-trans-Bergamotol (23.25%), Durylaldehyde (16.07%), and α-Bergamotene (10.48%) existed in the highest amount in PKEOs. Antimicrobial assay of PKEOs showed maximum growth inhibition against Listeria monocytogenes and Kluyveromyces marxianus at the dose of 625 μg/ml. PKEOs exhibited a high cytotoxicity on lung cancer cell line A549 at a dose of 4 mg/ml. Anti-Leishmania activity of PKEOs showed concentration of 5000 µg/ml that had similar potency of glucantime at 125 µg/ml. The highest anti-inflammatory effect of PKEOs for Carrageenan-induced paw edema was observed at 100 concentrations, with paw inflammation reduced by 83.70% after using PKEO ointment. The present study reports broad-spectrum biological functions for essential oil from P. kotschyi. However, these biological activities, including anti-proliferative, anti-Leishmania, anti-inflammatory, antimicrobial and wound-healing potential, were not studied in detail. Therefore, it may be attractive for investigating the detailed mechanistic and molecular aspects of biological activities of PKEOs. Considering that the present study is the first to report the biological activity of P. kotschyi, further studies on their metabolites are needed to replicate the present findings.

Effect of some bio-products on the growth of Helminthosporium maydis, causal agent of Southern Corn Leaf Blight by dual culture technique under in-vitro condition

Maize belongs to the family Poaceae, is the third most important cereal crop under irrigated and rainfed agricultural system in semi-arid and arid tropics and also known as queen of cereals. The yield of this crop is challenged by a number of biotic stresses among which maydis leaf blight disease caused by Helminthosporium maydis / Bipolaris maydis is very much important. Proper management of this disease should be followed for minimizing the loss due to a disease attack. Cultural, chemical and biological control measures are important ways of disease management. Control of plant diseases by using biocontrol agents and natural / plant products is an eco-friendly & sustainable approach. Considering the hazardous effects of fungicides and chemicals, in this experiment for the purpose of management of MLB of maize by using eco-friendly ways three bio-control agents and three natural products were tested against H. maydis under in-vitro condition. Two plant extracts Allium Sativum (garlic), Azadirachta indica (neem), three bioagents Trichoderma viride, Trichoderma harzianum, Pseudomonas fluorescence and one natural product cow urine were tested against the growth of Helminthosporium maydis under in-vitro condition. Among the six treatments minimum radial growth (1.13cm) & maximum growth inhibition (82.8%) of Bipolaris maydis was found in case of application of Trichoderma harzianum followed by Trichoderma viride (radial growth – 1.30cm & growth inhibition 80.21%) with no significant difference among them. The growth inhibition of 35.61% was recorded in case of Pseudomonas fluorescens respectively. Better result was obtained when three bio-control agents were applied but among the natural products better result (radial growth 4.47cm & growth inhibition 31.96%) was obtained with application of garlic bulb extract (10%) followed by application of neem extract (25.11). Six botanicals were evaluated in-vitro against Helminthosporium maydis. The result revealed that, bulb extract of garlic (Allium sativum) at 10 per cent concentration completely inhibited mycelial growth of the fungus. Among the six treatments minimum radial growth (1.13cm) & maximum growth inhibition (82.8%) of Bipolaris maydis was found in case of application of Trichoderma harzianum followed by application of Trichoderma viride (radial growth – 1.30 cm & growth inhibition 80.21%) with no significant difference among them. Better result was obtained when three bio-control agents were applied but among the natural products better result (radial growth 4.47cm & growth inhibition 31.96%) was obtained when garlic bulb extract (10%) was applied.

In-vitro efficacy of fungicides against Phomopsis vexans caused Phomopsis blight in Brinjal

Phomopsis blight caused by Phomopsis vexans is one of the major constraints in the production of brinjal. In order to find out the effective fungicides against Phomopsis vexans experiment was carried out in-vitro evaluation of fungicides. The results of present investigation revealed that the maximum growth inhibition after seven days against Phomopsis vexans in-vitro condition was recorded in the treatment of carbendazim 87.46 per cent followed by propiconazole 86.29 per cent. Other fungicide treatments growth inhibition recorded hexaconazole and tebuconazole whereas 72.18 per cent and 64.83 per cent respectively. Copper oxychloride showed growth inhibition 54.20 per cent and minimum growth inhibition was noticed in copper hydroxide 47.40 per cent and this treatment.

Studies on fungicides against Rhizoctonia solani f.sp. Sasakii causing banded leaf and sheath blight of maize

Eight fungicides namely: Thiophenate-Methyl, Validamycin, Propineb, Difenoconazole, Carbendazim + Mancozeb, Carbendazim, Mancozeb and Hexaconazole were screened in-vitro by using poisoned food technique for their effect on inhibition of mycelium growth of Rhizoctonia solani f .sp. sasakii, the causal agent of banded leaf and sheath blight of maize. Among all fungicides screened, maximum inhibition of mycelium growth was observed in Difenoconazole, Thiophenate-Methyl and Hexaconazole, while maximum Percent disease reduction was observed in Validamycin followed by Difenoconazole. Maximum grain yield was recorded in Validamycin and Difenoconazole among the tested all fungicides.

Saccharothrix Algeriensis NRRL B-24137 Potentiates Chemical Fungicide Carbendazim in Treating Fusarium Oxysporum f.sp. Vasinfectum-Induced Cotton Wilt Disease.

Cotton (Gossypium hirsutum) wilt is one of the destructive disease caused by Fusarium oxysporum f. sp. vasinfectum and lead to 100% yield loss under favorable conditions. This study aims to estimate the potential of biological control agents Saccharothrix algeriensis NRRL B-24137 (SA) and chemical fungicides against cotton wilt pathogen under in-vitro and in-vivo conditions. The in-vitro study revealed that carbendazim showed maximum mycelia growth inhibition with a mean of 91% over control, which was further validated in glasshouse assay. In-vitro dual culture test of biocontrol agents with F. oxysporum determined that SA had a potential to inhibit mycelia growth by 68% compared to control. Further in glasshouse assay, the combination of the SA and carbendazim (10 µg/mL) showed a significant (p < 0.05) disease control. Moreover, results demonstrated that carbendazim and SA remarkably decreased the disease development up to 83% and subsequently, significant improvement was observed in the plant growth parameters (plant length, root length, and plant weight) compared to untreated plants. Conclusively, exploration and utilization of bioagent for fungal diseases in cotton may provide a better line with maximum efficacy and with lesser adverse effects, which will pave a way toward better consequences in fungal treatments.

Plectological and molecular identification of economically important wild Russulales mushrooms from Pakistan and their antifungal potential against food pathogenic fungus Aspergillus niger

Present study deals with the plectological and molecular analysis as well as use of economically important wild Russuloid mushrooms against food pathogenic fungus Aspergillus niger. Three different species of mushrooms viz., Russla laeta, R. nobilis, and R. nigricans were collected and identified from Himalayan range of Pakistan and are found as new records for this country. Major objective of this study was to highlight the importance of these wild creatures as antifungal agents against A. niger. For this purpose methanolic extract of selected mushrooms of different concentration levels viz., 1, 1.5, 2 and 3% were used. This activity is also first time reported from Pakistan by using this group of mushrooms. Results showed that all tested mushrooms exhibit growth inhibition of A. niger and can be used as biocontrol agents. R. nigricans showed maximum inhibition of fungus growth that is 62% at 3% concentrations while minimum inhibition was observed in R. nobilis at same concentration that is 43.6%.&#x0D; Bangladesh J. Plant Taxon. 27(1): 67-77, 2020 (June)

Facile single step preparations of phyto-nanoparticles of iron in Calotropis procera leaf extract to evaluate their antifungal potential against Alternaria alternata

Green nanotechnology has become an emerging field for the control of plant disorders. In the current study, the leaf extract of Calotropis procera has been used as reducing and stabilizing agent and the preparation of iron nanoparticles has been optimised. For this purpose, the formation and morphological properties of green iron nanoparticles were investigated. The synthesized nanoparticles were characterized through fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD) analysis, scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) analysis. FTIR spectroscopy detected the presence of stabilising and reducing molecules such as OH, CH, OCO, CO and CO. XRD analysis confirmed the orthorhombic form and size (∼32 nm) of these nanoparticles. EDX analysis gave information about the presence of major elements in the samples while the spinal shaped morphology of prepared iron nanoparticles was described by SEM. After successful preparation, iron nanoparticles were evaluated for their potential antifungal activity. Using poisoned food technique, different concentrations of nanoparticles were used to assess growth inhibition of Alternaria alternata. Iron nanoparticles showed highly significant growth reduction and the maximum growth inhibition (87.9 %) was observed at 1.0 mg/mL concentration of nanoparticles. These results reveal that the iron nanoparticles, prepared in the leaf extract of C. procera are very efficient, cost-effective and eco-friendly. These proficient results suggest the large scale use of these green nanoparticles, as an effective alternative to chemical fungicide.

Management of collar rot disease in chickpea by Trichoderma species

Nine isolates of Trichoderma spp. were isolated from different agro- ecological regions of Nepal viz; Jumla, Palpa, Chitwan, Tarahara, Banke, Illam and Salyan and screened against Sclerotium rolfsii Sacc. Adreded soil borne phytopathogen causing collar rot of chickpea in chickpea; In-vitro efficacy of nine fungal antagonist (Trichoderma spp.) against Sclerotium rolfsii were screened. Pot experiment was done to find out the effective management of S. rolfsi through Tricoderma using different methods i.e. Seed treatment, soil drenching and soil application. All the tested isolates of Trichoderma spp. were found effective on mycelial growth inhibition and sclerotial parasitization of S. rolfsii. Trichoderma isolated from Palpa district showed maximum growth inhibition (%) of pathogen periodically after 48(93.78%), 72(96.00%), 96(97.96%) and 120(100.00%) hours of inoculation. Parasitized sclerotium showed minimum sclerotial germination on agar plates. Moreover, Trichoderma species isolated from Palpa districts showed second best percent mycelial growth inhibition periodically at 72(25.00%), 120(29.16%), 168(29.16%) and 216(29.16%).In pot experiment at 40 days after sowing, Seedling height was maximum in soil drenching with 30g per 100ml of water (22.27cm) and Mortality percentage of seedlings was least or highest disease control was observed in seed treated with 109cfu/ml (0.000%).

Development of nanoemulsion formulation of mustard oil, its chemical characterization and evaluation against post harvest anthracnose pathogens

Oil-in-water nanoemulsion (NE) formulations of mustard oil known for prominent antimicrobial activities have been prepared, characterized and tested against anthracnose pathogens Colletotrichum musae and Colletotrichum capsici. Physico-chemical properties viz., appearance, stability, pH, centrifugation, storage-stability, thermodynamic stress, persistent foam, droplets size and zeta potential were tested for the NE formulations. The NE formulations were prepared using low energy emulsification process with the optimized composition (w/w) of mustard oil (5%), Tween 20 and sodium dodecyl benzene sulfonate emulsifiers blend (20–30%), co-surfactants (4%), and de-ionized water. The required hydrophile-lipophile balance value for emulsifier blends was determined as 11.39–11.74. Only 3 (viz., NF2, NF3 and NF6) out of 15 NE formulations with transparent faint yellow color (pH 6.3) passed all the physico-chemical parameters tested. Among these, NF2 (foam height < 1 mL) was selected for further study. The average diameter (23 nm), polydispersity index (0.38) and zeta potential (− 12 mV) of mustard oil droplets in NF2 indicated the formation of a stable and homogeneous NE formulation. Application of NF2 exhibited low level of sensitivity to C. capsici and C. musae with maximum growth inhibition (6.2–7.3%) at 1.0% dose. Out of 18 phytochemicals detected in mustard oil by gas chromatography-mass spectrometry, 11 have been reported with antifungal properties including trans-13-octadecenoic acid with the highest relative abundance. The observed antifungal activity may be attributed to the presence of at least some or all the identified phtytochemicals in mustard oil. Further bio-assay on sensitive plant pathogenic fungi is underway to explore the application of the developed NE formulation.

Phyto-toxic Influence of an Atrazine-based Selective Herbicide – Arda-force® on Onions (Allium cepa L)

Introduction: The constant impact on the environment occasioned by pollution, indiscriminate application of agricultural chemicals, security challenges and crisis in the Niger Delta ecological area of Nigeria has caused severe damage to plants, soil organisms and humans.&#x0D; Aim and Methodology: In this research, onions (Allium cepa L) was exposed to varying concentrations of an atrazine-based selective herbicide Arda-force® to estimate the phyto-toxic effects on the plant species using the Organization for Economic Co-operation and Development, (OECD) protocol #208.&#x0D; Results: The mean effective concentration (EC50) using root growth inhibition produced indications of phyto-toxicity to the exposed species at a concentration of 0.55 ± 0.06 mg/L. Similarly, the maximum root growth inhibition efficiency relative to the control was 65% as recorded in the highest test concentration of 1.25 mg/L.&#x0D; Discussion: The study indicated that constant application / indiscriminate use of the herbicide Arda-force® could cause deleterious influence on these plant and vegetable species, daily consumed by humans as a rich source of anti-oxidants.&#x0D; Conclusion: This study concluded that atrazine-based herbicide Arda-force® used in this assessment resulted in phyto-toxic effects to Allium cepa L. At the exposed concentrations of the herbicide to non-target specie – Allium cepa L. that are integral parts of the ecosystems, the ‘‘harmless’’ status of atrazine acclaimed by the United State Environmental Protection Agency (USEPA) is still very much in doubt.

Molecular docking studies and synthesis of a new class of chroman-4-one fused 1,3,4-thiadiazole derivatives and evaluation for their anticancer potential

γ-Secretase inhibitors (GSIs) are repurposed as cancer therapeutics based on the promising inhibition of NOTCH1 signalling pathway in various cancers. GSIs are a class of small-molecule compounds that target the Notch pathway and have been tested to treat various types of cancers in preclinical and clinical trials. Although GSIs elicit a response in some tumours as single agents and sensitize to cytotoxic and targeted therapies, they have not yet been approved for cancer therapy. A new series of chroman-4-one fused 1,3,4-thiadiazole derivatives has been synthesized with the help of different aromatic benzaldehydes, and the final compounds were characterized by FT-IR and 1HNMR. Chroman-4-one fused 1,3,4-thiadiazole derivatives were synthesized by the reaction of Schiff base derivatives with chroman-4-one fused 1,3,4-thiadiazole. All the synthesized compounds were screened for their anticancer activity. These compounds were evaluated for their anticancer activity against MDA-MB-231, MCF-7, and Vero cancer cell lines. Four of the compounds possessed good to moderate anticancer activity. Four of the synthesized compounds, i.e. 3a, 3c, 3i, and 3e, were found to possess maximum growth inhibition. In conclusion, the designed chromanone-1,3,4-thiadiazole scaffold is an interesting anticancer pharmacophore and considered as novel lead scaffold for any future optimization.

Formulation and evaluation of antifungal agent in a hydrogel containing nanoparticle of low molecular weight chitosan

The research aimed to formulate and prepare hydrogel of low molecular weight chitosan nanoparticles with the help of antifungal agents such as clotrimazole and Nystatin for the topical application. Using the ionic gelation process, placebo and nanoparticles containing drugs were prepared. By cationic interaction is suitable for pH, and gel sodium tripolyphosphate is used as a crosslinker which cross-links the chitosan particles to form the gel, interaction between drug and polymer was observed during the formulation development. Formulated nanoparticle with chitosan and nystatin and clotrimazole showed the mean diameter 273.7nm, 983nm, and 501nm. Clotrimazole and Nystatin had encapsulation capacity was about 74.6% and 63.0%, respectively. In vitro drug release at pH 4.7 chitosan molecules are examined for the version of clotrimazole and nystatin.it has noticed that both the formulation shows sustained drug release about 12 hours. Using SEM, nanoparticles are directed for surface morphology character; it shows that nanoparticles are smooth and spherical in structure. Chitosan itself has the antimicrobial property; it was carried out for the antifungal activity against the fungus Candida Albicans along with the prepared formulations drugs for the comparative study. And the result showed that clotrimazole had maximum fungal growth inhibition next followed by the nystatin and chitosan is least. This inhibitory effect was due to the parameter such as zeta potential and particle size of chitosan nanoparticles. And it shows the least antifungal activity of nanoparticles, which are formulated from the TMC. Hence CTZ and Chitosan were formulated and applied as a natural antifungal agent into nanoparticle to increase the fungal activity. According to the ICH Q1A (R2) guidelines, stability studies are conducted to prove no degradation of the drug. The prepared formulation of chitosan nanoparticles based hydrogel incorporated with clotrimazole and nystatin are promising and significant properties for the efficient treatment of topical fungal infections

Applying GC-MS analysis to identify chemical composition of Iranian propolis prepared with different solvent and evaluation of its biological activity.

Background:Propolis as a natural product has shown beneficial effects on human health. This study was aimed to investigate the chemical compositions and biological activity of three different extracts of propolis from two distinct geographic areas in Iran.Methods:The chemical composition of Iranian propolis extracts that were collected in the Spring of 2016 from two provinces in northern Iran: Ardabil and Polur in Mazandaran Province were measured through gas chromatography-mass spectrometry (GC-MS) methods. In addition, antimicrobial activity and cytotoxicity effect on HN5 and LNCaP cell lines were evaluated. The data were analyzed using one-way ANOVA and p<0.05 was considered as significant.Results:The GC-MS analysis identified the presence of compounds that belonged to the different groups such as aromatics acids and their related esters, flavonoid and flavonoid derivatives and terpenes. Flavanone was the most dominant compound of flavonoids. The maximum growth inhibition was observed against S. aureus of ethanolic extract of propolis (p<0.05). Moreover, cytotoxicity showed that ethanolic and dichloromethane extracts had more inhibitory effects on cell lines than the water extract.Conclusion:The results determined that extracts had the highest percentage of flavonoids. Therefore, it is expected that the synergistic effect of the main components of propolis is related to the increase of biological activity of propolis.

Efficacy of biocontrol agents against Fusarium oxysporum F. SP. Corianderi causing wilt of coriander under in vitro condition

A laboratory experiment was conducted to find out the efficacy of different fungal and bacterial biocontrol agents against coriander wilt pathogen Fusarium oxysporum f. sp. corianderi. Among the seven antagonistic fungi tested using dual culture technique, Trichoderma harzianum JAU isolate 1 showed maximum reduced mycelial growth of Fusarium oxysporum f. sp. corianderi (46.23) than rest of antagonistic fungi. Whereas, the least effective biocontrol agent found was Trichoderma hamatum (NBA11 Tha 1) with 28.69 per cent mycelial growth inhibition of test fungus in vitro. The antagonistic actions of selected seven bacterial biocontrol agents were evaluated against the test fungus by dual culture technique (ring method). Among different bacterial antagonists, Pseudomonas fluorescens found significantly superior over rest of the biocontrol agents and showed maximum inhibition of mycelial growth of F. oxysporum f. sp. corianderi (99.76%). While, the least effective biocontrol agent found was Bacillus subtilis (KT894726) with 72.08 per cent mycelial growth inhibition of test fungus in vitro.

Investigation of oxidative potential of mahasudarshan churna using goat liver as in-vitro experimental model

Antifungal chemotherapy depends on bio-chemical alterations between fungi and mammals. Unlike bacteria, which are prokaryotes, both fungi and mammals are eukaryotes and the biochemical differences between them are not significant. However, there are some differences (in structure & metabolism) and focus is on these differences that act as targets for development of antifungal agents. The current recommendation of standard TB chemotherapy, called Directly observed treatment (DOTS) is a therapy of six month in which consists an first two-month phase of cure with four first-line drugs i.e. isoniazid, Rifampicin, Pyrazinamide, and Ethambutol. In this study large number of compounds is manufactured in which Most of the tested molecules showed maximum bacteriological growth inhibition at tested concentration. The combinations (7e, 7g, 7h, 7i and 7u) exhibited bacteriological growth inhibition at concentration of less than 40.0μg/ml against both microorganisms. Compounds (7o) showed growth of inhibition at 2.5μg/ml against both microorganisms. Additional challenging for all compounds at lower concentrations is mandatory to compare their activity through standard Streptomycin at its MIC to get exact MIC the manufactured combinations. Thus it can be concluded that designed 1, 3, 4-oxadiazole derivatives (7a-v) were manufactured successfully using planned synthetic outline. After manufactured the molecules were characterized using spectroscopy analysis and tested for the biological activity. All combinations showed anti-bacterial action at tested concentration against both gram positive and gram negative organisms and one of the compound 7o showed activity at concentration <2.5 μg/ml. Thus, these 1, 3, 4-oxadiazole results can then act as a potential principal for drug discovery of novel anti-infective agents.

Development and preclinical pharmacology of a novel dCK inhibitor, DI-87

BackgroundDeoxycytidine kinase (dCK) is an essential enzyme for production of nucleotides via the salvage pathway; DI-87 is a novel dCK inhibitor in preclinical development for use in anticancer therapy. The current study utilizes PET imaging to evaluate PK-PD relationships and to determine optimal dosing of the drug. MethodsNSG mice bearing CEM tumors had plasma and tumor PK assessed using mass spectrometry following oral administration of DI-87. dCK inhibition was assessed after a single dose of oral DI-87 followed by a [18F]CFA PET probe and PET imaging. Tumor growth inhibition was assessed by orally administering DI-87 with concurrent intraperitoneal thymidine. ResultsDI-87 had an in vitro EC50 of 10.2 nM with low protein binding. Peak DI-87 concentrations were observed between 1–3 h and 3–9 h in plasma and tumor, respectively, with tumor concentrations less than one third of plasma. Full dCK inhibition, as evaluated by PET imaging, was observed as early as 3 h following 25 mg/kg dosing and was maintained for 12 h, with full recovery of enzyme activity after 36 h. When DI-87 was administered as repeated doses in combination with thymidine, full dCK inhibition was maintained at 12 h (25 mg/kg twice daily dose) and led to maximal tumor growth inhibition. ConclusionsDI-87 is a promising new compound for use in combination therapy against tumors expressing dCK. Utilizing a [18F]CFA PET probe targeting the pathway of interest allowed for efficient and accurate identification of the optimal dose for growth inhibition.

Ultraviolet/peroxydisulfate degradation of ofloxacin in seawater: Kinetics, mechanism and toxicity of products

The ultraviolet/peroxydisulfate (UV/PDS) system was used to degrade ofloxacin (OFL) in fresh water, synthetic marine aquaculture water and synthetic seawater. The comparison of the reaction degradation rate constants proved that the order of reaction rate was the following: synthetic seawater (0.77 min−1) > synthetic marine aquaculture water (0.74 min−1) > freshwater (0.30 min−1). Bromide (Br−) and bicarbonate (HCO3−) promote the degradation of OFL, whereas chloride (Cl−) inhibits the degradation. The piperazine ring of OFL was the main reactive group, and atoms N1, C6, C7 and N2 were identified as the reaction sites. Based on the intermediate and final products, the possible degradation pathways of OFL in the three kinds of water were proposed. Additionally, during the UV/PDS treatment of synthetic marine aquaculture water containing Cl− and Br−, the oxidation products of OFL showed a slight toxicity to Chlorella pyrenoidosa (C. pyrenoidosa) and Priacanthus tayenus (P. tayenus). The maximum growth inhibition rate of the products to C. pyrenoidosa was 9.72%. The products also caused liver cells of P. tayenus to be damaged and reduced the species richness and diversity of intestinal microorganism. Nevertheless, compared with the products degraded by traditional disinfection methods using NaClO, the biological toxicities were much lower. UV/PDS can be used for seawater as a new alternative disinfection method.

INSECTICIDAL AND ANTIBACTERIAL POTENTIAL OF SYZYGIUM AROMATICUM (L.) MERRILL AND PERRY

The present study was designed to appraise the insecticidal and antibacterial potential of Clove, Syzygium aromaticum (L.) against some laboratory hosts and Escherichia coli respectively. The phytochemicals constituents were extracted with two solvents methanol and acetone. The result of the phytochemical analysis revealed that methanol extract has alkaloids, steroids, tannins, saponins, flavonids, cardiac glycosides, phenolic compounds and aromatic acids but in acetone extract all the constituents are similar as methanolic extract except aromatic acids. Results of the repellent activity observed against Tribolium castaneum and Corcyra cephalonica implies that silver based nanoparticles from methanol extract of 1% concentration showed maximum repellent activity of 71% against T.castaneum. Antibacterial efficacy of clove extracts tested against Gram negative bacterium E. coli revealed that 1% of methanolic extract of clove is found to have maximum growth inhibition (25mm). Results of the larvicidal activity tested against Bombyx mori recorded 100% mortality in 4% acetone extracts of clove. Keywords: Syzygium aromaticum, Tribolium castaneum, Corcyra cephalonica, Bombyx mori, Repellent activity, Larvicidal ac

EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex

Deregulation of the PRC2 complex, comprised of the core subunits EZH2, SUZ12, and EED, drives aberrant hypermethylation of H3K27 and tumorigenicity of many cancers. Although inhibitors of EZH2 have shown promising clinical activity, preclinical data suggest that resistance can be acquired through secondary mutations in EZH2 that abrogate drug target engagement. To address these limitations, we have designed several hetero-bifunctional PROTACs (proteolysis-targeting chimera) to efficiently target EED for elimination. Our PROTACs bind to EED (pKD ∼ 9.0) and promote ternary complex formation with the E3 ubiquitin ligase. The PROTACs potently inhibit PRC2 enzyme activity (pIC50 ∼ 8.1) and induce rapid degradation of not only EED but also EZH2 and SUZ12 within the PRC2 complex. Furthermore, the PROTACs selectively inhibit proliferation of PRC2-dependent cancer cells (half maximal growth inhibition [GI50]= 49-58nM). In summary, our data demonstrate a therapeutic modality to target PRC2-dependent cancer through a PROTAC-mediated degradation mechanism.

Carbamazepine toxicity and its co-metabolic removal by the cyanobacteria Spirulina platensis

Bioremediation of pharmaceutical-contaminated wastewater using microalgae has attracted increasing attention. Cyanobacteria, which are important prokaryotic microalgae, are widely distributed in different water environments, and have the advantages of simple culture and a fast growth rate. However, studies on either the toxicity of pharmaceutical contaminants (PhCs) to cyanobacteria or the removal of PhCs by cyanobacteria are scarce. In this study, carbamazepine (CBZ) and Spirulina platensis were selected as model PhCs and cyanobacteria, respectively. CBZ (>1 mg/L) had toxicity effects on S. platensis, showing maximal growth inhibition (34.0%) at 100 mg/L after 10 days of cultivation. At CBZ < 25 mg/L, S. platensis showed a trend similar to that of eukaryotic microalgae in increasing superoxide dismutase and catalase activities and content of chlorophylls, carotenoids, carbohydrates, and lipids. These results indicated that S. platensis had a similar protective mechanism to CBZ toxicity as that of the eukaryotic microalgae. Increasing CBZ concentration (50–100 mg/L) significantly decreased these biochemical characteristics and photosynthetic activity owing to the serious damage of the structure and function of S. platensis. However, with increasing cultivation time, the growth and photosynthetic activity of S. platensis recovered from the toxicity of CBZ. S. platensis showed a maximum of 30.97 ± 1.30% removal of CBZ (1 mg/L), mainly through biodegradation. Addition of 0.3 mg/L glucose enhanced this removal efficiency to 50.13 ± 2.51% via co-metabolism. These findings indicated that S. platensis can be used for the removal of CBZ or other PhCs from wastewater.