Percentage Of Growth Inhibition Research Articles

A comparative study of the antifungal efficacy and phytochemical composition of date palm leaflet extracts

Abstract This study rigorously evaluated the inhibitory effects of chloroform (PDCL) and methanol (PDML) extracts from date palm (Phoenix dactylifera L.) leaflets, in comparison to fosetyl-aluminum, against molecularly identified fungal strains Fusarium oxysporum (OR116511), Botrytis cinerea (OR116493), and Rhizoctonia solani (OR116530) isolated from date palm tree roots and fruits. We found that coumaric acid (1663.91 µg g−1) is one of the top four high-performance liquid chromatography-major phenols in the PDML extract, while the PDCL extract includes rosmarinic acid (291.08 µg g−1). The major flavonoids in the PDML extract are naringenin and kaempferol, whereas PDCL extract includes naringenin and quercetin. In the PDML extract, methyl 9-cis-11-trans-octadecadienoate (9.96%) is one of the top five gas chromatography–mass spectrometry major compounds; likewise, cis-13-octadecenoic acid (26.16%) is in the PDCL extract. The highest growth inhibition percentages of PDCL and PDML extracts were initiated against F. oxysporum (60.53 and 50.00%) at 150 µg mL−1, respectively, whereas inhibition against B. cinerea was realized at the highest concentration with 50.82%. Fosetyl-Al potently inhibited the growth of fungal isolates to varying degrees. Therefore, we could successfully employ PDCL extract to control the growth of F. oxysporum and B. cinerea and also use both extracts against R. solani.

Antimalarial Activity of Aqueous Extracts of Nasturtium (Tropaeolum majus L.) and Benzyl Isothiocyanate.

Malaria remains an important and challenging infectious disease, and novel antimalarials are required. Benzyl isothiocyanate (BITC), the main breakdown product of benzyl glucosinolate, is present in all parts of Tropaeolum majus L. (T. majus) and has antibacterial and antiparasitic activities. To our knowledge, there is no information on the effects of BITC against malaria. The present study evaluates the antimalarial activity of aqueous extracts of BITC and T. majus seeds, leaves, and stems. We used flow cytometry to calculate the growth inhibition (GI) percentage of the extracts and BITC against unsynchronized cultures of the chloroquine-susceptible Plasmodium falciparum 3D7 - GFP strain. Extracts and/or compounds with at least 70% GI were validated by IC50 estimation against P. falciparum 3D7 - GFP and Dd2 (chloroquine-resistant strain) unsynchronized cultures by flow cytometry, and the resistance index (RI) was determined. T. majus aqueous extracts showed some antimalarial activity that was higher in seeds than in leaves or stems. BITC's GI was comparable to chloroquine's. BITC's IC50 was similar in both strains; thus, a cross-resistance absence with aminoquinolines was found (RI < 1). BITC presented features that could open new avenues for malaria drug discovery.

Chemical and physical modification of graphene oxide nano-sheets using casein, Zn-Al layered double hydroxide, alginate hydrogel, and magnetic nanoparticles for biomedical applications

In our study, we developed a novel nanobiocomposite using graphene oxide (GO), casein (Cas), ZnAl layered double hydroxide (LDH), sodium alginate (Alg), and Fe3O4 magnetic nanoparticles. To synthesize the GO, we used a modified Hummer's method and then covalently functionalized its surface with Cas protein. The functionalized GO was combined with as-synthesized ZnAl LDH, and the composite was conjugated with alginate hydrogel through the gelation process. Finally, we magnetized the nanobiocomposite using in-situ magnetization. The nanobiocomposite was comprehensively characterized using FT-IR, FE-SEM, EDX, and XRD. Its biological potential was assessed through cell viability, hemolysis, and anti-biofilm assays, as well as its application in hyperthermia. The MTT assay showed high cell viability percentages for Hu02 cells after 24, 48, and 72 h of incubation. The nanobiocomposite had a hemolytic effect lower than 3.84 %, and the measured bacterial growth inhibition percentages of E. coli and S. aureus bacteria in the presence of the nanobiocomposite were 52.18 % and 55.72 %, respectively. At a concentration of 1 mg.mL−1 and a frequency of 400 kHz, the nanocomposite exhibits a remarkable specific absorption rate (SAR) of 67.04 W.g−1, showcasing its promising prospects in hyperthermia applications.

2‐(1‐Methyl‐1H‐indazol‐5‐yl)‐N‐arylisonicotinamide Analogs: Synthesis, Anticancer Screening, SAR and ADMET Studies

AbstractIn this current research framework, we detailed the synthesis of ten novel 2‐(1‐methyl‐1H‐indazol‐5‐yl)‐N‐arylisonicotinamide analogs (3a–j). The synthesis of these compounds (3a–j) involved a three‐step process, employing the Suzuki‐Miyaura coupling reaction, which successfully linked 1‐methyl‐1H‐indazole with isonicotinamide to satisfactory yields. The synthesized compounds were characterized using various spectroscopic techniques. To assess their potential, the anticancer activity of compounds (3a–j) was evaluated following the National Cancer Institute (NCI US) protocol against nine panels comprising different cancer cell lines, at a concentration of 10−5 M. Growth percentage (GP) and percentage growth inhibition (PGI) were calculated for each compound. Notably, the CNS cancer cell line SNB‐75 exhibited a remarkable PGI of 99.16 percent, indicating high sensitivity to the tested compound 3e. Additionally, ADMET prediction suggested that most of the synthesized compounds possess drug‐like properties, with low adverse effects and toxicity. These findings represent a significant advancement, offering potential avenues for further developments in the field of cancer research.

Sensitivity to fungicides of Botrytis cinérea (Pers.) isolated from raspberry (Rubus idaeus L.)

Objective: To evaluate the sensitivity of B. cinerea isolated from raspberry to nine fungicides alone and in combination with potassium silicate. Design/methodology/approach: The study evaluates the sensitivity of four isolates obtained from four raspberry plantations in October 2022, which were identified in a previous study as B.cinerea based on morphological, morphometric and molecular characteristics, to nine fungicides alone and combined with potassium silicate. B. cinerea was planted in PDA culture medium modified with fungicides plus potassium silicate, and mycelial growth and mycelial growth inhibition percentage (PICM) were evaluated. A completely randomized design with six repetitions and two controls was used, an ANOVA and Tukey’s mean comparison test were performed. Results: B. cinerea isolated from CITAP showed lower growth with fluazinam (PICM = 100 ), while with azoxystrobin it presented a PICM equal to 0. B. cinerea isolated from Paso del Cristo and Sierra Negra 2 had lower growth with fluazinam (PICM = 100), while with boscalid and azoxystrobin it showed a PICM equal to 0. In Sierra Negra 1, iprodione controlled B. cinerea better with a PICM equal to 100, while azoxystrobin showed a PICM equal to 0. All the isolates were sensitive when fungicides were combined with potassium silicate. Findings/conclusions: All the isolates were sensitive to the fungicides fluazinam, fenhexamid, thiophanate methyl, captan, pyrimethanil, fludioxonil and iprodione. The isolates from Sierra Negra 1 and CITAP were sensitive to boscalid, while those from Sierra Negra 2 and Paso del Cristo were insensitive; 100 % of the isolates were insensitive to azoxystrobin, which suggests that they could be resistant; finally, potassium silicate potentiates the effect of fungicides.

Probiotic Potential of Bacillus Subtilis Strain I3: Antagonistic Activity Against Chalkbrood Pathogen and Pesticide Degradation for Enhancing Honeybee Health.

To explore the potential of probiotic candidates beneficial for honeybee health through the modulation of the gut microbiome, bee gut microbes were isolated from bumblebee (Bombus terrestris) and honeybee (Apis mellifera) using diverse media and cultural conditions. A total of 77 bee gut bacteria, classified under the phyla Proteobacteria, Firmicutes, and Actinobacteria, were identified. The antagonistic activity of the isolates against Ascosphaera apis, a fungal pathogen responsible for chalkbrood disease in honeybee larvae, was investigated. The highest growth inhibition percentage against A. apis was demonstrated by Bacillus subtilis strain I3 among the bacterial strains. The presence of antimicrobial peptide genes in the I3 strain was detected using PCR amplification of gene fragments encoding surfactin and fengycin utilizing specific primers. The export of antimicrobial peptides by the I3 strain into growth medium was verified using liquid chromatography coupled with mass spectroscopy. Furthermore, the strain's capabilities for degrading pesticides, used for controlling varroa mites, and its spent growth medium antioxidant activity were substantiated. The survival rate of honeybees infected with (A) apis was investigated after feeding larvae with only medium (fructose + glucose + yeast extract + royal jelly), (B) subtilis I3 strain, A. apis with medium and I3 strain + A. apis with medium. Honeybees receiving the I3 strain + A. apis exhibited a 50% reduction in mortality rate due to I3 strain supplementation under experimental conditions, compared to the control group. In silico molecular docking revealed that fengycin hydrolase from I3 strain effectively interacted with tau-fluvalinate, suggesting its potential in bee health and environmental protection. Further studies are needed to confirm the effects of the I3 strain in different populations of honey bees across several regions to account for genetic and environmental variations.

Pharmaceutical Properties and Phytochemical Profile of Extract Derived from Purple Leaf Graptophyllum pictum (L.) Griff.

Graptophyllum pictum (L.) Griff is a medicinal shrub belonging to the Acanthaceae family and is traditionally used to treat various diseases. Therefore, this study aimed to evaluate the pharmaceutical properties and phytochemical profiles of the methanolic extract of G. pictum. G. pictum leaves was extracted using methanol. Antioxidant, cytotoxic on Michigan Cancer Foundation-7 (MCF-7) and HepG2, antidiabetic, and antibacterial properties were evaluated in vitro. Chemical profile of the extract was identified through qualitative (for phytochemicals), quantitative (for phenolic and flavonoid content), and gas chromatography-mass spectrometry (GC-MS) analysis. The results showed that the extract had potent antioxidant activity against 2,2-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) and 2,2-diphenyl-1-picrylhydrazyl radicals with IC50 values of 49.00 ± 3.20 µg/mL and 70.18 ± 3.27 µg/mL, respectively. It also exhibited cytotoxic effects on human breast (MCF-7) and liver (HepG2) carcinoma cells with growth inhibition percentages of 74.29 ± 1.53% and 64.90 ± 1.94%, respectively. The antidiabetic assay showed that the extract had inhibitory effects on α-glucosidase activity with IC50 value 194.59 ± 15.59 µg/mL, indicating its potential to be developed as an antidiabetic agent. Furthermore, it had antibacterial properties against four test strains, and the highest activity was found against Bacillus subtilis American Type Culture Collection 19659, with minimum inhibitory concentration and minimum bactericidal concentration values of 625 µg/mL and 1250 µg/mL, respectively. Phytochemical tests indicated the presence of alkaloids, flavonoid and terpenoids in the extract, with total phenolic content and total flavonoid content of 41.17 ± 2.38 mg gallic acid equivalents/g and 26.52 ± 0.61 mg quercetin equivalent/g, respectively. GC-MS analysis revealed that it contained several active compounds, including eicosane, 2,4-Di-tert-butylphenol, hentriacontane, tetracosane, octacosane, sulfurous acid, 2-methylhexacosane, docosane, heneicosane, 1-propene-1,2,3-tricarboxylic acid, tributyl ester, and pentacosane. The extract derived from G. pictum leaves was a potential source of therapeutic compounds, particularly for antioxidant, antidiabetic, anticancer, and antibacterial agents.

MTT Assay on Anticancer properties of the different extracts of roots of Lantana camara Linn.

Lantana camara, considered a weed is an evergreen plant found throughout the world. Traditionally it has been used in the treatment of various ailments and has been supported by scientific investigation. Phytoconstituents present in almost all parts of this plant have been reported in various literature. This study has been done on the root part of Lantana camara, the dried and powdered root was subjected to continuous solvent extraction with Hexane followed by Ethyl Acetate and Methanol. Ethyl Acetate and Methanol extracts were evaluated for anticancer activity by MTT assay, MCF7 cell line was used with Cisplatin a known anti-cancer drug as a standard reference, and the measurements were carried out at wavelengths 570 and 630nm. The percentage of growth inhibition was calculated. The concentration of test extract needed to inhibit cell growth by 50% (IC50) value generated from the dose-response curve. IC50 values of Ethyl Acetate extract were greater than 500µg/ml and Methanol extract 450.05µg/ml.

Description and management of Aspergillus section Nigri causing post-harvest bulbs rot of onion

When onions are improperly stored, a post-harvest disease known as black mold of onion bulbs can result in considerable economic losses. Aspergillus section Nigri, one of many species, has been implicated in the development of black mold. In the present study, rot onion bulbs were collected from markets in Qena, Egypt. Thirteen Aspergillus section Nigri isolates were obtained and identified by morphological and molecular characterization. The ochratoxins potential of isolated A. section Nigri was tested, and three isolates were producers at the range of 1.5–15 ppm. For the presence of pks gene, no amplification product was detected. Using the fungal growth inhibition test, the isolates of A. niger were inhibited by eco-friendly materials Cement and Zeolite. Cement exhibited maximum percentage growth inhibition against the tested isolates at 74.7–86.7%. The pathogenicity activity of the A. niger isolates was tested by inoculation of healthy onion bulbs, other onion bulbs covered with Cement and Zeolite before inoculation by A. niger was used. The two treatments significantly reduced bulbs rot disease of onion than untreated bulbs. Seven and nine isolates showed 0% rot on covered bulbs by Cement and Zeolite, respectively as compared with inoculated onions, which exhibited rot ranging from 55 to 80%. Using eco-friendly materials with efficiency against post-harvest bulbs rot of onion was evaluated in this study.

DETERMINATION OF ANTIBIOSIS OF Trichoderma species AGAINST FUNGI ASSOCIATED WITH CORN (Zea Mays L.) SPOILAGE

Biological control of food spoilage microorganisms is gaining more attention because it is a safe and cheap technique. This study evaluated the antagonistic potential of Trichoderma species against corn spoilage fungi by plate co-culture technique for seven days. Fungal isolates from corn spoilage were examined morphologically and microscopically. The percentage growth inhibition (PGI) of Trichoderma species against the corn spoilage fungi were A. flavus (15%), A. niger (14%), A. terreus (62.9%), Fusarium spp. (5.9%), Nigrospora spp. (61.4%) and Penicillium spp. (62.5%). The result obtained in this study revealed that Trichoderma spp. had significant inhibitory effects against the growth of fungal pathogens associated with corn spoilage. Therefore, it could be explored for control of post-harvest fungal spoilage of corn. It is recommended that in order to compare the antagonistic strength of the Trichoderma species, different species of Trichoderma should be tested against the same spoilage fungi.

Exploring new quinazolin-4(3H)-one derivatives as CDK2 inhibitors: Design, synthesis, and anticancer evaluation.

In the present work, five series of new 2,3-disubstituted quinazolin-4(3H)-ones 4a-c, 5a-d, 6a-g, 7a,b, and 9a-c were designed, synthesized, and screened in vitro for their cytotoxic activity against 60 cancer cell lines by the National Cancer Institute, USA. Five candidates 4c, 6a, 6b, 6d, and 6g revealed promising cytotoxicity with significant percentage growth inhibition in the range of 81.98%-96.45% against the central nervous system (CNS) (SNB-19), melanoma (MDA-MB-435), and non-small cell lung cancer (HOP-62) cell lines. The in vitro cytotoxic half maximal inhibitory concentration (IC50 ) values for the most active compounds 4c, 6a, 6b, 6d, and 6g against the most sensitive cell lines were evaluated. Additionally, screening their cyclin-dependent kinase 2 (CDK2) inhibitory activity was performed. Ortho-chloro-benzylideneamino derivative 6b emerged as the most potent compound with IC50 = 0.67 µM compared to Roscovitine (IC50 = 0.64 µM). The most active candidates arrested the cell cycle at G1, S phases, or both, leading to cell death and inducing apoptosis against CNS (SNB-19), melanoma (MDA-MB-435), and non-small cell lung cancer (HOP-62) cell lines. The molecular docking study verified the resulting outcomes for the most active candidates in the CDK2-binding pocket. Finally, physicochemical, and pharmacokinetic properties deduced that compounds 4c, 6a, 6b, 6d, and 6g displayed significant drug-likeness properties. According to the obtained results, the newly targeted compounds are regarded as promising scaffolds for the continued development of novel CDK2 inhibitors.

Exploring fungal endophytes as biocontrol agents against rice blast disease

The rice blast disease caused by &lt;i&gt;Pyricularia oryzae&lt;/i&gt; Cavara is among the most severe plant diseases in the world. The utilization of natural antagonists, such as fungal endophytes, can be a good method to control the spread of this disease. In the present study, 68 fungal isolates were obtained from 160 rice samples collected in Guilan province fields, Iran. Morphological and molecular characteristics were used for the identification of these fungi. According to the results, the fungal isolates were &lt;i&gt;Alternaria citri&lt;/i&gt; (Penz.) Mussat, &lt;i&gt;Alternaria infectoria&lt;/i&gt; Simmons, &lt;i&gt;Aspergillus fumigatus&lt;/i&gt; Fresen, &lt;i&gt;Fusarium verticillioides&lt;/i&gt; (Sacc.) Nirenberg, &lt;i&gt;Trichoderma harzianum&lt;/i&gt; Rifai, &lt;i&gt;Trichoderma virens&lt;/i&gt; (Mill., Giddens &amp; Foster) Arx, &lt;i&gt;Trichoderma viride&lt;/i&gt; Pers., &lt;i&gt;Ulocladium consortiale&lt;/i&gt; (Thum) Simmons, and &lt;i&gt;Pyricularia oryzae&lt;/i&gt; . Eight isolates that did not cause any plant disease were selected for biocontrol studies &lt;i&gt;in vitro&lt;/i&gt; . The dual culture, culture filtrate, slide culture, and volatile metabolites methods were used in search of natural endophytic antagonists of &lt;i&gt;Pyricularia oryzae&lt;/i&gt;. It was found that &lt;i&gt;T. harzianum, T. virens, T. viride, A. fumigatus&lt;/i&gt;, and &lt;i&gt;A. citri&lt;/i&gt; isolates caused the highest percentage of mycelial growth inhibition of &lt;i&gt;P. oryzae in vitro&lt;/i&gt;. In the greenhouse experiments, all of the studied isolates reduced the &lt;i&gt;P. oryzae&lt;/i&gt; disease rating, with &lt;i&gt;T. harzianum&lt;/i&gt; isolate being the most effective antagonist (27.36% reduction in the disease rating), followed by &lt;i&gt;T. virens, T. viride&lt;/i&gt;, and &lt;i&gt;A. fumigatus&lt;/i&gt; (20.75%, 17.92%, and 16.98%, respectively). Furthermore, in greenhouse conditions, these antagonistic fungi increased the height, fresh weight, and dry weight of plants. The results of this research showed that there are various fungi in the natural flora of rice plants that possess potential biological properties against rice blast disease that can be implemented into practice.

THE ENDOPHYTIC FUNGUS EPICOCCUM NIGRUM: ISOLATION, MOLECULAR IDENTIFICATION AND STUDY ITS ANTIFUNGAL ACTIVITY AGAINST PHYTOPATHOGENIC FUNGUS FUSARIUM SOLANI

Fusarium solani is a soil-borne fungus that causes fusarium dry rot disease in Upper Egypt. In this study, endophytic fungi from the Helwan University campus were collected, separated, and classified according to their morphological traits. Based on morphological and molecular characteristics, Epicocum nigrum was isolated and identified from E. milii leaves; other endophytic fungi were recovered and recognised morphologically from E. hirta leaves. The endophytic isolates were examined for their antifungal activity against F. solani on PDA plates using the dual culture technique, which exhibited a variable growth inhibition percentage. E. nigrum showed a highly inhibited percentage (94%) after 5 days. As well, E. nigrum metabolites were extracted by different solvents (e.g., ethyl acetate, dichloromethane, and chloroform: methanol, 2:1), and the crude extracts were active against F. solani compared to the control. The antifusarial activity was mostly reported in the ethyl acetate extract. Both light microscopy and scanning electron microscopy showed that higher concentrations of ethyl acetate extract caused a change in hyphal aggregation and spore formation in F. solani. Identification of antifungal components in ethyl acetate extract using GC-MS analysis revealed the presence of 2, 2, 3, 3, 4, 4-Hexadeutero Octadecanal, 2, 2-Dideutero Octadecanal, and Isochiapin B as major components that could have antifungal and antimicrobial substances. These results suggest using E. nigrum extracts for controlling phytopathogenic F. solani.

EVALUATION OF IN VITRO CYTOTOXIC POTENTIAL OF DIFFERENT CARMUSTINE FORMULATIONS AGAINST U-87 MG HUMAN GLIOBLASTOMA CELL LINE

Glioblastoma (GBM) is a frequent as well as violent type of brain tumor. In this research work, different carmustine formulations were prepared and screened for their cytotoxic activity against U-87 MG glioblastoma and normal human fibroblast L-929 cell lines. The flexible liposomes embedded in situ nasal gel exhibited maximum percentage of growth inhibition against U-87 MG glioblastoma cell line, and in situ nasal gel exhibited lowest percentage of growth inhibition against U-87 MG glioblastoma cell lines. Flexible liposomes embedded in situ nasal gel is observed to be safe and biocompatible against normal human fibroblast L-929 cell line. In cellular uptake study, U-87 MG cell line treated with flexible liposomes embedded in situ thermoreversible intranasal gel emitted stronger and higher intensity fluorescence. It seems that the presence of flexible liposomes embedded in situ thermoreversible nasal gel inside the tumor cells, and would be the best carmustine delivery approach for the management of GBM.

Growth inhibition of Salmonella by Leuconostoc species isolated from buffalo milk curd

Traditional fermented products are considered to be a niche for microbial diversity. Probiotics offer a unique approach for addressing the threat of antibiotic resistance. Therefore, the aim of the present study was to isolate Leuconostoc spp. from Buffalo milk curd, an artisanal fermented dairy product in Bangladesh and assess their growth inhibition competence against Salmonella sp. A total of 50 isolates were isolated and purified from five freshly prepared buffalo milk curd samples using two different media, with glucose or sucrose as the carbon source. Among these pure isolates, 37 were identified as presumptive Leuconostoc spp. The biochemical identification using the VITEK 2 system confirmed that 59.5% of the isolates were Leuconostoc mesenteroides ssp. cremoris, while 40.5% were Leuconostoc pseudomesenteroides. Out of the identified isolates, twelve had a similarity of over 97%, and twenty-five had a similarity of less than 96%. Consequently, these twelve isolates were tested for their antimicrobial activity against Salmonella sp. using two in vitro methods, agar well diffusion and microbroth. The isolate M1L1 exhibited the highest inhibitory zone (15 mm) and showed 55.6% growth inhibition by the agar well diffusion and microbroth assay, respectively, suggesting a similar efficacy between the two methods. Notably, five other isolates also displayed inhibitory zones ranging from 13 to 15 mm and growth inhibition percentages of 37 to 52%. Overall, the isolated Leuconostoc spp. could be utilized as probiotics to combat pathogenic microorganisms. Ann. Bangladesh Agric. (2023) 27 (1): 93-104

Porous silicon nanostructures: Synthesis, characterization, and their antifungal activity

Abstract The use of synthetic pesticides has come under scrutiny, and there has been a subsequent shift toward the investigation of alternative methods for the treatment of plant diseases. One notable advancement in this field is the utilization of porous silicon (PS) powder as a sustainable antifungal agent. The synthesis of PS nanoparticle (PS-NP) powder was carried out using the environmentally friendly ultrasonication process. X-ray powder diffraction, Fourier transform infrared spectroscopy, Raman spectroscopy, UV-VIS absorbance, and photoluminescence were some of the methods used to characterize PS-NPs. The different characterization methods revealed the formation of a nanocrystalline structure possessing a cubic Si crystalline quality. The crystal size of PS-NPs, as determined from X-ray diffractometer data, ranges from 36.67 to 52.33 nm. The obtained PS has a high band gap of 3.85 eV and presents a photoluminescence peak at 703 nm. The antifungal activity of the synthesized PS-NPs was assessed against three molecularly characterized fungi, namely Rhizoctonia solani, Fusarium oxysporum, and Botrytis cinerea, which were obtained from tomato plants. The concentration of PS-NPs at 75 µg/mL exhibited the highest enhancement in growth inhibition percentages as compared to the control group. R. solani had the highest inhibition percentage of 82.96%. In conclusion, the encouraging structural properties and antimicrobial capabilities of PS-NPs pave the way for their application across diverse technological industries. To the best of our knowledge, this is the first in vitro study of PS-NPs to evaluate their fungal control efficiency.

Microemulsion of essential oil of Citrus aurantium var. dulcis for control of Aleurocanthus woglumi and evaluation of selectivity against Aschersonia aleyrodis and Ceraeochrysa cornuta

The aim of this study was to develop a microemulsion from the essential oil of Citrus aurantium var. dulcis (EOCA) as an alternative to synthetic pesticides, and to evaluate its efficacy against Aleurocanthus woglumi and selectivity towards the natural enemies Aschersonia aleyrodis and Ceraeochrysa cornuta. Chemical composition of the essential oil determined by gas chromatography coupled with mass spectrometry revealed limonene, myrcene, linalool and α-pinene as major components. The microemulsion was prepared using a ternary diagram illustrating the composition of water, essential oil, surfactant (procetyl AWS) and co-surfactant (ethanol). Selected microemulsions were characterized by polarized light microscopy, revealing to be isotropic with a Newtonian behaviour when measuring the shear stress against shear rate. The mean droplet size of microemulsions ranged from 53.69 nm to 2.22 μm. The insecticidal activity was evaluated by assessing three application routes, namely, contact, systemic and translaminar. Selectivity of microemulsions was determined by the percentage of growth inhibition (PGI) of fungi on A. aleyrodis and by contact on eggs and larvae of C. cornuta. The oil (LC50 = 36.07 mg/mL) in its pure form had a lower insecticidal effect on A. woglumi than the microemulsions (LC50 = 18.65 mg/mL). The microemulsions showed systemic insecticidal activity with approximately 90% mortality at 72 h (LC90 = 55.50 mg/mL). On A. aleyrodis, the microemulsion interfered with biomass production, which was concentration dependent. At a concentration of 15.68 mg/mL, a 91% inhibition of biomass production were observed. In the selectivity experiments against C. cornuta, the microemulsions were selective for eggs and larvae, and did not interfere with its predatory capacity.

Targeting apoptosis; design, synthesis and biological evaluation of new benzoxazole and thiazole based derivatives

Several novel approaches to target Bcl-2 proteins and apoptotic pathways have been identified in recent years for the treatment of different types of cancer including colorectal cancer. However, no effective treatments were yet developed for colorectal cancer. Twenty two novel benzoxazole and thiazole−based compounds were designed, synthesized, and evaluated as potential Bcl-2 inhibitors with anti−proliferative activity. Compounds 8g, 12e and 13d showed good to moderate anti−proliferative activity against most of the NCI 60 cell line panel with mean growth inhibition percent of 45.13, 42.29 and 29.25%, respectively. They showed the greatest cell growth inhibition percent to HCT-116 cell line with the values of 68.0, 59.11 and 43.44%, respectively. The aforementioned compounds were furtherly investigated for their effect on HCT-116 cell cycle, and they showed increase in the total apoptosis with 17, 22, and 5%, respectively. Also, the apoptotic effect of compounds 8g, 12e and 13d, were tested by their effect on altering caspase-3 expression level in HCT-116 human cell line. The three compounds showed an increase in the caspase-3 levels by 6, 8 and 3 folds, respectively in comparison with the same untreated ones. Moreover, they were evaluated for their in–vitro Bcl-2 inhibitory activity and they showed percent inhibition of 60.2, 69.2 and 50.0%, respectively. Finally, the most potent compounds 8g and 12e showed 3.864 and 2.834 folds increase in Bax level compared to the control respectively. On the other hand, Bcl-2 was down−regulated to 0.31 and 0.415 folds compared to the control. The induction of apoptosis through increase in caspase 3 expression and down−regulation of Bcl-2 is the suggested mechanism of action.

Crystal structure, spectroscopy, DFT, and thermal studies of 3-cyano-2(1H)-pyridones as potential anticancer agents.

A series of 3-cyano-2(1H)-pyridones 4a-c were efficiently synthesized using an expeditious microwave-assisted multicomponent approach. Single-crystal XRD analysis revealed the presence of six independent molecules in the asymmetric unit cell for all compounds, with the crystal packing stabilized by a network of cyclic dimers formed by N-H⋯O[double bond, length as m-dash]C and C-H⋯O[double bond, length as m-dash]C intermolecular interactions. Additional supramolecular interactions, including C-H⋯π, C-N⋯π, and π⋯π, and C-H⋯X (for halogenated derivatives, i.e., 4b and 4c), appear crucial for crystal stabilization. Density Functional Theory (DFT) calculations were employed to understand the electronic structures and potential binding affinities. Comprehensive spectroscopic characterization by FT-IR, UV-Vis, NMR, and HMRS techniques confirmed the structures of all synthesized compounds. Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) were employed to evaluate the thermal stability of these compounds. The in vitro anticancer activity was evaluated against a panel of 60 human cancer cell lines, demonstrating promising activity against non-small-cell lung and breast cancer cell lines. Notably, compounds 4a and 4c exhibited the highest anticancer activity against the HOP-92 and MCF7 cell lines, with growth inhibition percentages (GI%) of 54.35 and 40.25, respectively.

Repurposed organoselenium tethered amidic acids as apoptosis inducers in melanoma cancer via P53, BAX, caspases-3, 6, 8, 9, BCL-2, MMP2, and MMP9 modulations.

Organoselenium (OSe) agents hold promise for preventing cancer due to their potential ability to fight cancer development and protect cells from oxidative damage. Herein, OSe-based maleanilic and succinanilic acids were tested to estimate their antitumor activities against fifteen cancer cell lines. Besides, their potential safety and selectivity were further investigated against two normal cell lines, namely, human skin fibroblasts (HSF) and olfactory ensheathing cell line (OEC) using the growth inhibition percentage (GI%) assay. Moreover, the apoptotic potential of the superior anticancer candidates (8, 9, 10, and 11) was evaluated against P53, BAX, Caspase-3, Caspase-6, Caspase-8, Caspase-9, BCL-2, MMP2, and MMP9 apoptotic markers. Additionally, to enhance our understanding and predict the inhibitory potential of the examined compounds as potential anticancer agents, a thorough structure-activity relationship (SAR) analysis was conducted. On the other hand, molecular docking and ADMET studies were performed for the examined candidates as well. Overall, our findings point to significant anticancer activities of the organoselenium tethered amidic acids, suggesting their promising cytotoxic potential as effective anticancer drugs.