Aerobic vaginitis, bacterial vaginosis, and vaginal candidiasis among women of reproductive age in Arba Minch, southern Ethiopia.

Reproductive tract infections (RTIs) are a persistent public health threat worldwide, particularly among women in low-income countries of Africa, including Ethiopia, where drug resistance is also a growing problem. It is crucial to address this problem to ensure women's health and well-being. A cross-sectional study was carried out among a cohort of 398 women of reproductive age who sought medical attention at the Gynecology Department of the Arba Minch General Hospital, southern Ethiopia, from January to June 2020. They were chosen through systematic random sampling, and a pre-tested structured questionnaire was used to collect the data. The collection of vaginal and/or cervical swabs were done to diagnose bacterial vaginosis (BV) and aerobic vaginitis (AV) using Nugent and AV score analyses, respectively. The swabs were subjected to standard microbiological culture techniques to detect the isolates causing AV and vaginal candidiasis (VC). The susceptibility profiles of the causative agents of AV were checked by the Kirby-Bauer disc diffusion technique. Descriptive and inferential statistical analyses were also done. Aerobic vaginitis was the predominantly diagnosed RTI (n = 122, 30.7%), followed by BV (n = 117, 29.4%) and VC (n = 111, 27.9%). The prominent bacteria of AV were Escherichia coli (n = 36, 34.2%) and Klebsiella pneumoniae (n = 30, 28.5%). The overall rate of multidrug-resistant (MDR) bacteria was 65.71% (n = 69). History of abortion (p = 0.01; AOR = 4.0, 95% CI = 2.1, 7.7) and the habit of using vaginal pH-altering contraceptives (p = 0.01; AOR = 4.7, 95% CI = 2.5, 8.8) have the greatest odds of RTI. The high prevalence of RTIs in our study warrants an urgent intervention to minimize the associated morbidities and complications. The overall rate of MDR bacterial isolates necessitates the implementation of an effective surveillance program in the study setting.

Factors Associated with Otitis Media Among Pediatrics in Two Government Hospitals in Arba Minch, Southern Ethiopia.

Background: Bacterial otitis media (OM) is a common infection among the pediatric community worldwide and is the first reason for prescribing antibiotics in pediatric practices. However, if not promptly diagnosed and appropriately treated, it may persist and cause severe intra- and extra-cranial hard-to-cure complications. Hence, knowing the magnitude, etiology, and antibiotic susceptibility profile is very important for the proper management. Methods: A cross-sectional study was carried out in 312 pediatrics (1 to 18 years) attending the Ear Nose Throat outpatient departments of the two title hospitals from 25 February to 30th August 2022. Patients were chosen through a systematic random sampling method. Data were obtained by means of a semi-structured questionnaire. Samples were collected to identify the causative bacteria as per microbiological guidelines. The antibiotic susceptibility test was done according to the Kirby-Bauer disc diffusion; SPSS version 25 was used for the analysis. Results: The overall prevalence of otitis media was 67.3% (n=210); CSOM showed a slight preponderance (n=107) Gram-negative bacteria and Gram-positive bacteria were present in 59.8% (n=137) and 40.1% (n=92), respectively. Otitis media was predominantly caused by S. aureus (n=52, 56.5%), followed by Proteus spp. (n=33, 24%). Gram-negative bacteria were highly resistant to co-trimoxazole, amoxicillin-clavulanic acid, piperacillin, and tetracycline, whereas their positive counterparts were considerably penicillin and co-trimoxazole resistant. Overall, 61.5 and 19.2% of the isolates were MDR and XDR, respectively. MRSA, MR-CoNs, and VRE were 38.4% (n=20), 17.1% (n=5), and 58.3% (n=12), respectively; 19.7% (n=25) of Gram-negative bacteria produced ESBL, and 7% (n=9) were carbapenem-resistant. History of exposure to loud noise [AOR=3.4; CI=1.14-10.23; P-value=0.028] and family history of smoking at home [AOR=2.9; CI=1.18-7.25; P-value=0.020] have the greatest odds of otitis media. Conclusion: Overall, the prevalence of otitis media is showing an upward trend, and MDR among bacterial isolates is increasing alarmingly.

Antibacterial Activity Against Multidrug-Resistant Clinical Isolates of Nine Plants from Chencha, Southern Ethiopia.

Background: The diminishing efficacy of antibiotics currently in use and the emergence of multidrug-resistant bacteria pose a grave threat to public health worldwide. Hence, new classes of antimicrobials are urgently required, and the search is continuing. Methods: Nine plants were chosen for the current work, which are collected from the highlands of Chencha, Ethiopia. Plant extracts containing secondary metabolites in various organic solvents were checked for antibacterial activity against type culture bacterial pathogens and MDR clinical isolates. The broth dilution technique was used to evaluate the minimum inhibitory and minimum bactericidal concentrations of highly active plant extracts, and time-kill kinetic and cytotoxic assays were performed using the most active plant extract. Results: Two plants (C. asiatica and S. marianum) were highly active against ATCC isolates. The EtOAc extract of C. asiatica produced the highest zone of inhibition ranging between 18.2±0.8-20.7±0.7 and 16.1±0.4-19.2±1.4 mm against Gram-positive and Gram-negative bacteria, respectively. The EtOH extract of S. marianum displayed zones of inhibition in the range of 19.9±1.4-20.5±0.7 mm against the type culture bacteria. The EtOAc extract of C. asiatica effectively curbed the growth of six MDR clinical isolates. The MIC values of C. asiatica against the Gram-negative bacteria tested were 2.5 mg/mL, whereas the corresponding MBC values were 5 mg/mL in each case. The MIC and MBC values were the lowest in the case of Gram-positive bacteria, ie, 0.65 and 1.25 mg/mL, respectively. A time-kill assay showed the inhibition of MRSA at 4 × MIC and 8 × MIC within 2 hours of incubation. The 24 h LD50 values of C. asiatica and S. marianum corresponding to Artemia salina were 3.05 and 2.75 mg/mL, respectively. Conclusion: Overall results substantiate the inclusion of C. asiatica and S. marianum as antibacterial agents in traditional medicines.

Mosquito larvicidal activity of pyrrolidine-2,4-dione derivatives: An investigation against Culex quinquefasciatus and molecular docking studies.

The pyrrolidine-2,4-dione derivatives were used to conduct a larvicidal test on Culex quinquefasciatus larvae of the second instar. Mannich base condensation method was used to synthesis the pyrrolidine-2,4-dione derivatives by grindstone method. The reaction conditions were mild, resulting in high yields. An analysis of the synthesized compounds was carried out using FTIR, 1H NMR, 13C NMR, mass spectrometry, and elemental analysis. Synthesized compounds (1a-h) were evaluated for larvicidal activities. Compound 1e (LD50: 26.06 µg/mL), and 1f (LD50: 26.89 µg/mL), and were notably more active against Culex quinquefasciatus than permethrin (LD50: 26.14 µg/mL). The docking studies also demonstrated that 1e, and 1f are potent larvicides with higher binding energy (-12.6 kcal/mol) than the control in the mosquito odorant binding protein (PDB ID: 3OGN). The larvicidal properties of lead molecules have made them important for use as insecticides.

Antibiofilm Potential of Alpha-Amylase from a Marine Bacterium, Pantoea agglomerans.

Bacterial biofilms are a big menace to industries and the environment and also in the health sector, accumulation of which is a major challenge. Despite intensive efforts to curb this issue, a definitive solution is yet to be achieved. Enzyme-templated disruption of the extracellular matrix of biofilm and its control and elimination are emerging as an efficient and greener strategy. The study describes the antibiofilm potential of alpha-amylase from the marine microorganism Pantoea agglomerans PCI05, against food-borne pathogens. Amylase exhibited stability in a wide pH range and retained 50% of its activity at temperatures as high as 100°C. Thermal analysis of the enzyme produced showed thermal stability, up to 130°C. From these findings, it can be envisaged that the alpha-amylase produced from P. agglomerans can be used for starch liquefaction; it was also evaluated for antibiofilm activity. Amylase from this marine bacterium was found to efficiently disrupt the preformed biofilms of food-borne pathogens such as Bacillus cereus, Serratia marcescens, Vibrio parahaemolyticus, Listeria monocytogenes, and Salmonella enterica enterica serotype Typhi based on the value of biofilm inhibitory concentrations.

Nanobased Antibacterial Drug Discovery to Treat Skin Infections of Staphylococcus aureus Using Moringa oleifera-Assisted Zinc Oxide Nanoparticle and Molecular Simulation Study.

In addition to the physical barrier, the epidermis acts as a natural barrier against microbial proliferation. It is prone to bacterial infections on the skin and in the nose, such as Staphylococcus aureus, as well as a variety of other skin illnesses. Green nanomaterial production, which eliminates the use of harmful chemicals while simultaneously reducing time, is gaining popularity in the nanotechnology area. Using the leaf extract of the pharmacologically valuable plant Moringa oleifera, we described a green synthesis of ZnO NPs (zinc oxide nanoparticles). ZnO NPs had a particle size of 201.6 nm and a zeta potential of -56.80 mV, respectively. A novel aminoketone antibacterial medication was synthesized and tested for antibacterial activity using ZnO NPs as a phytocatalyst in this work. This method produces high yields while maintaining efficient and gentle reaction conditions. Moringa oleifera extract can reduce ZnO to ZnO NPs in a straightforward manner. FT-IR, 1H-NMR, 13C-NMR, mass spectra, elemental analysis, and morphological analysis were used to synthesize and describe the antibacterial medicines (1a-1g) and (2a-2g). In addition, antibacterial activity was evaluated against bacteria such as Enterococcus faecalis and Staphylococcus aureus, and compound 1c (63 µg/mL, E. faecalis) and compound 2e (0.12 µg/mL, S. aureus) were found to be very active when compared to other medications. mupirocin is used as a reference. In addition, studies of in silico molecular docking for the bacterial DsbA protein were conducted. The strong molecules 1c (-4.3 kcal/mol) and 2e (-5.1 kcal/mol) exhibit a high binding affinity through hydrogen bonding, according to docking tests.

Antibacterial, Antifungal, and Cytotoxic Activity of Excoecaria agallocha Leaf Extract.

BACKGROUND: Mangroves contain several bioactive compounds, some of which have been used for centuries as remedies for several ailments. METHODS: Foliar parts of Excoecaria agallocha were extracted in organic solvents and in water using a Soxhlet apparatus and evaluated for antimicrobial activity against nine type-culture pathogens, six clinical isolates, and two fungal pathogens with agar well diffusion assays. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined by broth dilution and extracts further subjected to brine-shrimp cytotoxic assays using Artemia salina. Chemical constituents were analyzed with thin-layer chromatography (TLC), gas chromatography-mass spectroscopy (GC-MS), and Fourier-transform infrared spectroscopy (FT-IR). RESULTS AND DISCUSSION: Ethyl acetate extract displayed the broadest antimicrobial activity. Isolates of Staphylococcus aureus were found to be the most susceptible among the clinical and type-culture groups corresponding to inhibition zones: 17.3±1.1 and 23.5±1.3 mm in diameter, respectively. Anticandidal activity was found to be lower against Candida albicans and C. tropicalis (10.3±0.6 and 11.9±0.85 mm diameter). Also, this extract was found to be bactericidal for S. aureus and Micrococcus luteus (MBC:MIC ≤2). C cytotoxic activity LD50 was 521 µg/mL. On GC-MS, squalene [(6E, 10E, 4E, 18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene] was the major compound. Bioassay-guided (antibacterial) TLC revealed the presence of one major active fraction, F2, with an Rf value of 1.21. FT-IR analysis of this fraction also implied that it was squalene, which might have a functional role in the mechanism of chemical defense.

Potato Peels Mediated Synthesis of Cu(II)-nanoparticles from Tyrosinase Reacted with bis-(N-aminoethylethanolamine) (Tyr-Cu(II)-AEEA NPs) and Their Cytotoxicity against Michigan Cancer Foundation-7 Breast Cancer Cell Line.

The synthesis of nanoparticles is most important in the context of cancer therapy, particularly copper nanoparticles, which are widely used. In this work, copper(II)-tyrosinase was isolated from potato peel powder. Copper nanoparticles (Tyr-Cu(II)-AEEA NPs) were synthesized via the reaction of tyrosinase with N-aminoethylethanolamine to produce Cu(II)-NPs and these were characterized by means of FT-IR, UV-Spectroscopy, XRD, SEM, TEM and a particle size analyzer. These Tyr-Cu(II)-AEEA NPs were tested as anticancer agents against MCF-7 breast cancer cells. Fluorescence microscopy and DNA fragmentation were also performed, which revealed the inhibiting potentials of Cu(II)-AEEA NPs and consequent cell death; Tyr-Cu(II)-AEEA NPs show potential cytotoxicity activity and this nano material could be contemplated as an anticancer medicament in future investigations.

Corrigendum: Synthesis and Cytotoxic Activity of Novel Indole Derivatives and Their in silico Screening on Spike Glycoprotein of SARS-CoV-2.

[This corrects the article DOI: 10.3389/fmolb.2021.637989.].

Synthesis and Cytotoxic Activity of Novel Indole Derivatives and Their in silico Screening on Spike Glycoprotein of SARS-CoV-2.

This work investigated the interaction of indole with SARS-CoV-2. Indole is widely used as a medical material owing to its astounding biological activities. Indole and its derivatives belong to a significant category of heterocyclic compounds that have been used as a crucial component for several syntheses of medicine. A straightforward one-pot three-component synthesis of indole, coupled with Mannich base derivatives 1a-1j, was synthesized without a catalyst. The products were confirmed by IR, 1H-NMR, 13C-NMR, mass spectra, and elemental analysis. The indole derivatives were tested for cytotoxic activity, using three cancer cell lines and normal cell lines of Human embryonic kidney cell (HEK293), liver cell (LO2), and lung cell (MRC5) by MTT assay using doxorubicin as the standard drug. The result of cytotoxicity indole compound 1c (HepG2, LC50-0.9 µm, MCF-7, LC50-0.55 µm, HeLa, LC50-0.50 µm) was found to have high activity compared with other compounds used for the same purpose. The synthesized derivatives have revealed their safety by exhibiting significantly less cytotoxicity against the normal cell line (HEK-293), (LO2), and (MRC5) with IC50 > 100 µg/ml. Besides, we report an in silico study with spike glycoprotein (SARS-CoV-2-S). The selective molecules of compound 1c exhibited the highest docking score -2.808 (kcal/mol) compared to other compounds. This research work was successful in synthesizing a few compounds with potential as anticancer agents. Furthermore, we have tried to emphasize the anticipated role of indole scaffolds in designing and discovering the much-awaited anti-SARS CoV-2 therapy by exploring the research articles depicting indole moieties as targeting SARS CoV-2 coronavirus.

Synthesis and Characterization of a Minophosphonate Containing Chitosan Polymer Derivatives: Investigations of Cytotoxic Activity and in Silico Study of SARS-CoV-19.

Chitosan is broadly used as a biological material since of its excellent biological activities. This work describes investigations of chitosan interaction with SARS-CoV-2, which is occupied by human respiratory epithelial cells through communication with the human angiotension-converting enzyme II (ACE2). The ß-chitosan derivatives are synthesized and characterized by FT-IR, nuclear magnetic resonance (1H and 13C NMR), mass spectrometry, X-ray diffraction, TGA, DSC, and elemental analysis. The ß-chitosan derivatives were screened for cytotoxic activity against the HepG2 and MCF-7 (breast) cancer cell lines. Compound 1h (GI50 0.02 µM) is moderately active against the HepG2 cancer cell line, and Compound 1c is highly active (GI50 0.01 µM) against the MCF-7 cancer cell line. In addition, chitosan derivatives (1a-1j) docking against the SARS coronavirus are found by in-silico docking analysis. The findings show that compound 1c exhibits notable inhibition ability compared with other compounds, with a binding energy value of -7.9 kcal/mol. Based on the molecular docking results, the chitosan analog is proposed to be an alternative antiviral agent for SARS-CoV2.

Correction: Gobinath, P., et al. Grindstone Chemistry: Design, One-Pot Synthesis, and Promising Anticancer Activity of Spiro[acridine-9,2'-indoline]-1,3,8-trione Derivatives against the MCF-7 Cancer Cell Line. Molecules 2020, 25, 5862.

In the original article [...].

New Chitosan Polymer Scaffold Schiff Bases as Potential Cytotoxic Activity: Synthesis, Molecular Docking, and Physiochemical Characterization.

In this work, we synthesize the sulfonated Schiff bases of the chitosan derivatives 2a-2j without the use of a catalyst in two moderately straightforward steps with good yield within a short reaction time. The morphology and chemical structure of chitosan derivatives were investigated using FT-IR, NMR (1H-13C), XRD, and SEM. Furthermore, our chitosan derivatives were tested for their anticancer activity against the MCF-7 cancer cell line, and doxorubicin was used as a standard. In addition, the normal cell lines of the breast cancer cell MCF-10A, and of the lung cell MRC-5 were tested. Compound 2 h, with a GI50 value of 0.02 µM for MCF-7, is highly active compared with the standard doxorubicin and other compounds. The synthesized compounds 2a-2j exhibit low cytotoxicity, with IC50 > 100 µg/ml, against normal cell lines MCF-10A, MRC-5. We also provide the results of an in-silico study involving the Methoxsalen protein (1Z11). Compound 2h exhibits a higher binding affinity for 1Z11 protein (-5.9 kcal/mol) and a lower binding affinity for Doxorubicin (-5.3 kcal/mol) than certain other compounds. As a result of the aforementioned findings, the use of compound 2h has an anticancer drug will be researched in the future.

Antioxidant Activity of Telmisartan-Cu(II) Nanoparticles Connected 2-Pyrimidinamine and Their Evaluation of Cytotoxicity Activities.

Copper nanoparticles (Cu-Nps) are one of the promising materials for the advancement of nanoscience and technology. In this work, we synthesized telmisartan copper nanoparticles and 2-pyrimidinamines via Biginelli reaction using telmisartan copper nanoparticles (Cu-Nps) as a reusable catalyst. The synthesis of 2-pyrimidinamine derivatives (1a-c) was achieved in water and under solvent-free condition (Green chemistry approach). Synthesis of 2-pyrimidinamine with telmisartan copper nanoparticle (Cu-Nps-Pyr) unexpected product was also isolated from synthesis of 2-pyrimidinamine preparation. Antioxidant and cytotoxic activities were carried out both in 2-pyrimidinamine (1a-1c) and 2-pyrimidinamine with telmisartan copper nanoparticles (Cu-Nps-Pyr). The synthesized 2-pyrimidinamine derivatives (1a-c) were characterized from FT-IR, 1H and 13C NMR spectroscopy, mass and elemental analyses. The synthesized telmisartan copper nanoparticles (Cu-Nps) were characterized from UV spectroscopy, XRD, SEM, EDX, AFM (atomic force microscopy), profile, waviness, and roughness analyses. Antioxidant activity was screened based on ABTS·+ radical scavenging and linoleic acid peroxidation performance. Cu-Nps-Pyr-1b showed substantial antioxidant (97.2%) activity against ABTS·+ assay and 91.2% activity against AAPH assays compared with Trolox. Cytotoxicity was evaluated using HepG2, HeLa, and MCF-7 cell lines, the Cu-Nps-Pyr-1a is high in toxicities (GI50 = 0.01 µm) against the HeLa cancel cell line compared with doxorubicin. The developed copper NPs with 2-pyrimidinamine (Cu-Nps-Pyr) could provide promising advances as antioxidant activities; this nanocomposition could be considered an anticancer treatment in future investigations.

Grindstone Chemistry: Design, One-Pot Synthesis, and Promising Anticancer Activity of Spiro[acridine-9,2'-indoline]-1,3,8-trione Derivatives against the MCF-7 Cancer Cell Line.

In this study, the synthesis of one-pot 10-phenyl-3,4,6,7-tetrahydro-1H-spiro [acridine-9,2'-indoline]-1,3,8-trione derivatives was achieved via a four-component cyclocondensation reaction, which was carried out in solvent-free conditions, and using p-toluenesulfonic acid (p-TSA) as a catalyst. The product was confirmed by FT-IR, 1H-NMR, 13C-NMR, mass spectra, and elemental analysis. Furthermore, the anticancer activity was screened for all compounds. Among these compounds, compound 1c was more effective (GI50 0.01 µm) against MCF-7 cancer cell lines than standard and other compounds. Therefore, the objective of this study was achieved with a few promising molecules having been demonstrated to be potential anticancer agents.

Cytotoxic, larvicidal, nematicidal, and antifeedant activities of piperidin-connected 2-thioxoimidazolidin-4-one derivatives.

The objective of this study was to investigate brine shrimp cytotoxicity, larvicidal, nematicidal, and antifeedant activities of novel piperidin-connected 2-thioxo-imidazolidin-4-one derivatives. The activities of target compounds were compared with some naturally occurring (-)-pinidinol, hydantocidin, and positive controls. Target compounds were synthesized via cyclocondensation method. The compounds were synthesized and then characterized by infrared spectroscopy, 1H NMR, 13C NMR, mass spectral, and elemental analyses. Brine shrimp cytotoxicity assay was investigated using freshly hatched, free-swimming nauplii of Artemiasalina. Larvicidal screening was performed against urban mosquito larvae (Culex quinquefasciatus). Nematicidal activity was evaluated using juvenile nematodes of Meloidogyne javanica. Regarding antifeedant activity, marine-acclimated Oreochromis mossambicus fingerlings were used. Compounds 3a-c (piperidin-connected 2-thioxoimidazolidin-4-one) were found to be lethal to the second instar larvae of mosquito, which produced LD50 values of 1.37, 6.66, 6.51 µg/mL, compared to compounds (-) pinidinol and hyantocidin LD50 values of 18.28 and 22.11 µg/mL respectively. Compound 3a-c was found to kill 100% of fish fingerlings within 6 h at 20 µg/mL, with LD50 values of 1.54, 1.79, 1.52 µg/mL, compared to compounds (-) pinidinol and hyantocidin with LD50 values of 10.21 and 21.05 µg/mL respectively. Compound 3c with LD50 value of 1.57 µg/mL demonstrated high nematicidal activity compared to compound 3a, 3b, (-) Pinidinol and Hyantocidin LD50 values of 6.45, 2.42, 14.25, 26.30 µg/mL respectively. Therefore, the 2-thioxoimidazolidin-4-one with piperidin ring showed high potential cytotoxic, larvicidal, nematicidal, and antifeedent activities.

Effective synthesis of some novel pyrazolidine-3,5-dione derivatives via Mg(II) catalyzed in water medium and their anticancer and antimicrobial activities.

Novel pyrazolidine-3,5-dione derivatives (2a-g, 4a-g, and 6a-g) were synthesized by an easy-to-perform Mg(II) acetylacetonate-catalyzed reaction with high yields using water as the reaction medium. Synthesized compounds were screened for anticancer and antimicrobial activities. The compound 6c (LD50 19.1 µg/mL) showed anticancer activity higher than that of all other compounds against MCF-7 breast cancer cell line. Results of antimicrobial activities revealed that the compound 4d (MIC 0.5 µg/mL) had higher activity than ciprofloxacin against Staphylococcus aureus, whereas the compound 2b (MIC 0.5 µg/mL) had higher activity than clotrimazole against Candida albicans. Overall results of this study envisaged that the compounds 2b, 4d, and 6c have the potential to be developed as anticancer and antimicrobial agents. Novel pyrazolidine-3,5-dione derivatives (2a-g, 4a-g, and 6a-g) were synthesized via an easy-to perform Mg(II) catalysis in water medium. The synthesized compounds were screened for anticancer and antimicrobial activities.

Synthesis of novel benzopyran-connected pyrimidine and pyrazole derivatives via a green method using Cu(ii)-tyrosinase enzyme catalyst as potential larvicidal, antifeedant activities.

A series of benzopyran-connected pyrimidine (1a-g) and benzopyran-connected pyrazole (2a-i) derivatives were synthesized via Biginelli reaction using a green chemistry approach. Cu(ii)-tyrosinase was used as a catalyst in the synthesis of compounds 1a-g and 2a-ivia the Biginelli reaction. The as-synthesized compounds were characterized by IR, 1H NMR, 13C NMR, mass spectroscopy, and elemental analysis. The as-synthesized compounds were screened for larvicidal and antifeedant activities. The larvicidal activity was evaluated using the mosquito species Culex quinquefasciatus, and the antifeedant activity was evaluated using the fishes of Oreochromis mossambicus. The compounds 2a-i demonstrated lethal effects, killing 50% of second instar mosquito larvae when their LD50 values were 44.17, 34.96, 45.29, 45.28, 75.96, and 28.99 µg mL-1, respectively. Molecular docking studies were used for analysis based on the binding ability of an odorant binding protein (OBP) of Culex quinquefasciatus with compound 2h (binding energy = -6.12 kcal mol-1) and compound 1g (binding energy = -5.79 kcal mol-1). Therefore, the proposed target compounds were synthesized via a green method using Cu(ii)-enzyme as a catalyst to give high yield (94%). In biological screening, benzopyran-connected pyrazole (2h) was highly active compared with benzopyran-connected pyrimidine (1a-g) series in terms of larivicidal activity.

Evaluation of antioxidant and anticancer activities of chemical constituents of the Saururus chinensis root extracts.

Evaluation of antioxidant and anticancer activities were screened by various Saururus chinensis root extracts. Four solvents (ethyl acetate, methanol, ethanol, and water) extracts were investigated for their total flavonoids, phenol contents and their antioxidant activity of DPPH (2,2-diphenyl-1-picrylhydrazyl), NO (nitric oxide), H2O2 (hydrogen peroxide), ABTS 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonicacid)diammonium assays, FRAP (ferric reducing ability of plasma) assays and anticancer activity. The total phenolic and flavonoid content of extracts were determined by using FC (Folin-Ciocalteu) and AlCl3 colorimetric assay method. Total flavonoid content in these plants ranged from 24.7 to 72.1 mg g-1 and amount of free phenolic compounds was between 11.2 and 67.1 mg g-1 extract. The all extracts have significant levels of phenolics and flavonoids content. Anticancer activity was screened for MCF-7 breast cancer cell line. Ethanol extract shows significant of antioxidant activity and water extract shows significant of anticancer activity compared with standard (BHT) butylated hydroxy toluene. These ethanol and water extracts could be considered as a natural source for using antioxidant, and anticancer agents compared to commercial available synthetic drugs.

Antimicrobial, anticoagulant, and cytotoxic evaluation of multidrug resistance of new 1,4-dihydropyridine derivatives.

A new series of 1,4-dihydropyridine derivatives (2a-h, 3a-e, and 4a-e) were systematically designed and synthesized via ultrasound irradiation methods with easy work-up and good yields. Compounds structures were confirmed by IR, 1H NMR, 13C NMR, and mass spectra. The synthesized compounds were screened for both antimicrobial and anticoagulant activities. Compound 2e (MIC: 0.25 µg/mL) was highly active against Escherichia coli and compound 2c (MIC: 0.5 µg/mL) was also highly active against Pseudomonas aeruginosa compared with ciprofloxacin. (MIC: 1 µg/mL) The antifungal activity of 2c (MIC: 0.5 µg/mL) against Candida albicans was high relative to that of clotrimazole (MIC: 1 µg/mL). Anticoagulant activity was determined by activated partial thromboplastin time (APTT) and prothrombin time (PT) coagulation assays. Compound 4-(4-hydroxyphenyl)-2,6-dimethyl-N3,N5-bis(5-phenyl-1,3,4-thiadiazol-2-yl)-1,4-dihydropyridine-3,5-dicarboxamide 3d (>1000 s in APTT assays) was highly active in anticoagulant screening compared with the reference of heparin. Cytotoxicity was evaluated using HepG2 (liver), HeLa (cervical), and MCF-7 (breast) cancer cell lines, with high toxicities observed for 2c (GI50 = 0.02 µm) against HeLa cell line and 2e (GI50 = 0.03 µm) equipotant against MCF-7 cell line. Therefore, the compounds 2e, 2c and 3d can serve as lead molecules for the development of new classes of antimicrobial and anticoagulant agent.