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  • Open access
  • 84 Reads
Synthesis and cytotoxic activities of some heterocyclic chalcones

Chalcone (1,3-diphenylprop-2-en-1-one) compounds are of natural or synthetic origins and posess a diversity in bioactivities. Recently, the inhibitory activities of heterocylic chalcones against differerent cancer cell lines have raised much concern. 

The study aimed at synthesizing some heterocylic chalcones and determining their in vitro cytotoxicity on rhabdomyosarcoma (RD) cell line. 

Heterocyclic chalcones in this study were developed on the basis of the idea that heteroaryl moieties either on ring A or ring B of chalcones might provide cytotoxicity on cancer cells. These compounds were prepared by Claisen-Schmidt condensation The in vitro cytotoxicity of the compounds on rhabdomyosarcoma (RD) cell line has been evaluated using the microculture tetrazolium (MTT) assay. 

A total of synthesized heterocyclic chalcones has been synthesized and their structures were elucidated by spectrometric methods. Bioassay results revealed that 5 out of 20 compounds showed activities against RD cells with IC50 values less than 20μM. Notably, cytotoxicity of (E)-1-(thiophen-2-yl)-3-(3,4,5-trimethoxy-phenyl)prop-2- en-1-one increased with decreasing concentration. It was showed as the most potential compound with IC50 at 12.51 μM (compare with taxol IC50 at 10.88μM).

The results demonstrate that heterocylic chalcones are promising compounds for developing anticancer drugs.  

  • Open access
  • 73 Reads
Central analgesic activity of Litsea polyantha Juss. bark extract

The sensation of pain is initiated in peripheral pain receptors (nociceptors) and its purpose is to draw attention to tissue damage. In order to test analgesic activity, it is obviously necessary to induce pain in the subject and then modify the response to, or perception of, this pain. Analgesic studies of the methanol (90% v/v) extract (MELP) of Litsea polyantha Juss. bark (Yield: 11.79% w/w) was carried out using healthy adult Swiss albino mice of either sex weighing between 20 to 25 g respectively. The experiment protocols were approved by the Institutional Animal Ethical Committee (621/02/ac/CPCSEA) prior to the conduct of the animal experiments. The animals were divided into 6 groups (n=6). Group I and II were used as control, received 10% v/v propylene glycol (PG) and distilled water (DW) at the dose of 10 ml/kg b.w. Group III, IV & V were treated with MELP (50, 75 and 100 mg/kg b.w., i.p.), respectively; Group VI received Morphine sulphate (10 mg/kg b.w., s.c.) an opioid analgesic as standard drug. A reduction in the tail withdrawal as compared to the control group was considered as evidence for the presence of analgesia. Tail flick latency was measured 30 min after the drug administration and Pain Inhibition Percentage (PIP) was calculated. MELP given by intraperitoneal route in mice showed significant and dose-dependent central analgesic activity (P<0.001) at all dose levels. MELP showed 22.2% – 60.4% increase in PIP in tail flick test and 21.2% – 67.8% increase in PIP in tail immersion method.

  • Open access
  • 104 Reads
MICROWAVE-ASSISTED EXTRACTION OF BIOACTIVE COMPOUNDS FROM SEEDS OF MILK THISTLE, BLACK CUMIN AND CORIANDER

The aim of the work was to compare the microwave-assisted extraction of coriander, black cumin and milk thistle seeds with the conventional process of extraction. Before the extraction material was crumbled, sieved and defatted. Obtained extracts were analyzed by means of the content of the antioxidants using ABTS, DPPH, Folin - Ciocalteu methods as well as the content of silibinin by HPLC (in case of milk thistle). By using these methods the content of reducing compounds, ability to scavenge free radicals and antioxidant capacity was evaluated in each case. It was shown that for the black cumin and milk thistle more effective was microwave extraction, but for the coriander conventional seems to be better. Extracts of black cumin and milk thistle obtained by microwave extraction have higher concentration of antioxidant compounds as compared to extracts from coriander. In case of coriander most effective a conventional extraction have been designated as more effective one.

  • Open access
  • 159 Reads
Preparation and Photosynthesis-Inhibiting Activity of 1-[(2-Chlorophenyl)carbamoyl]naphthalen-2-yl N‑Alkylcarbamates

In this study a series of eight 1-[(2-chlorophenyl)carbamoyl]naphthalen-2-yl N‑alkylcarbamates was prepared and characterized. The discussed compounds were prepared by microwave-assisted and conventional synthesis. The compounds were tested for their activity related to inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. The PET-inhibiting activity of the compounds was moderate; the highest activity within the series of compounds was observed for 1-[(2-chlorophenyl)carbamoyl]naphthalen-2-yl N-propylcarbamate, and the compounds were found to inhibit PET in photosystem II.

  • Open access
  • 101 Reads
Preparation of Hydrochlorothiazide Nanoparticles

Aqueous solubility and permeability through biomembranes are important parameters for drug bioavailability. Nanoparticles can be considered as a useful tool for improving properties of poorly soluble and/or permeable active ingredients. Hydrochlorothiazide (Class IV of BCS) was chosen as a model compound. Antisolvent precipitation – solvent evaporation and emulsion solvent evaporation methods were used as techniques for preparation of twelve samples containing hydrochlorothiazide nanoparticles. Water solutions of the surfactants sodium dodecyl sulfate and Tween 80 were used in mass concentrations of 1, 3 and 5%. Acetone and dichloromethane were used as solvents of model compound. The particle size of the prepared samples was measured by dynamic light scattering. The particle size ranged from 4.2 to 102.2 nm. Tween 80, that yielded nanoparticles <15 nm, was a preferable excipient to sodium dodecyl sulfate.

  • Open access
  • 54 Reads
In situ solid phase microwave assisted synthesis of silver/nickel substituted phosphomolybdate nanoparticles using organic driving agent

A solid state microwave assisted technique was used for facile and eco-friendly synthesis of silver/nickel substituted salt of phosphomolybdate nanoparticles. This solid phase reaction was promoted using urea as organic driving agent under microwave treatment with the power of 360 W for 7 min. The structural and morphological characterizations revealed the formation of mixed silver/nickel ammonium salt of phosphomolybdate with Keggin-type structure and uniform nano-sized particulate morphology with the average size about 41 nm. The experimental strong point of this strategy is the use of a facile, one-pot and solid state method for synthesis of nanomaterials at short time without any acidic conditions. As a result, this method can be proposed as an instrumental way to fabricate various macromolecules of polyoxometalate in nanoscale.

  • Open access
  • 117 Reads
Microwave-Assisted Organic-Template Synthesis of Iron Oxide Particles

Iron oxide is widely known as a catalyst, pigment and gas sensitive material. There are many developed methods for the synthesis of Iron oxide such as: sol-gel, electrochemical techniques, sputtering, vapor deposition and hydrothermal. Mentioned methods have proven to be advantageous in different aspects, but recently attentions has drawn to methods which are both eco-friendly and commercially feasible. Template synthesis using Xanthan gum and water as the solvent is a green approach. Xanthan gum (XG) is a water-soluble heteropolysaccharide including hydroxyl units along its backbone and branches can provide xanthan gum with capability of forming hydrogel networks. In this study, Fe(NO3)3.9H2O is used as the Iron source, glycine and ammonium nitrate are co-oxidizers and Xanthan gum is the template. The synthesis of Iron oxide particles and the removal of template are undertaken by microwave radiation. Physical properties of products depend on the power and duration of microwave exposure. The prepared samples are characterized by Fourier-Transform Infrared spectroscopy (FT-IR), powder X-Ray Diffraction (XRD) and SEM.

  • Open access
  • 64 Reads
Synthesis of naphthothiophene derivatives through polar Diels-Alder reactions employing 5-nitrobenzothiophene as electrophile. Microwave irradiation vs classical thermal conditions

Herein we report a simple, economical and efficient one-step procedure to synthesize the naphtho[2,1-b]thiophene ring system in good to excellent yield through the polar Diels-Alder reactions of 5-nitro-3-acetylbenzothiophene and dienes of different nucleophilicity. In thermal conditions the reactions were developed in molecular solvents; moreover the reaction system was exposed to microwave irradiation as a complement of reaction conditions.

  • Open access
  • 110 Reads
Calcium Bromide is an Efficient Catalyst for Synthesis of Dihydropyrimidones Under Microwave Condition

An efficient and ecofriendly method was developed for synthesis of a series of dihydropyrimidinone derivatives through three-component one-pot cyclocondensation between substituted benzaldehydes, beta ketoester and urea/thiourea using calcium bromide as a catalyst under microwave irradiation in a solvent-free condition. The merits of this method is solvent free approach, low catalyst loading, shorter reaction time, simple workup procedure, catalyst is easily available, inexpensive and easy to handling. Using this procedure, we synthesized 25 different biologically active dihydropyrimidine.

  • Open access
  • 81 Reads
Development of a novel molecularly imprinted stir-bar for isolation of aflatoxins

Mycotoxins are natural substances produced as secondary metabolites by a wide variety of different species of filamentous fungi. One of the most important groups in terms of occurrence and toxicity, is the group of aflatoxins (AFs). The major members of this group are aflatoxin B1, B2, G1, G2, M1 and M2. Exposure to AFs can cause chronic and acute toxic effects or death, as they can be carcinogenic, mutagenic, teratogenic and immunosuppressive. AFB1 is considered as the strongest carcinogen of natural origin and it is normally predominant in crops as well as in food products. Aflatoxin M1 is a major metabolite of aflatoxin B1 in humans and animals and it may be present in milk from animals fed with contaminated feed. Although the toxicity of M1 is about ten times lower than B1, it is known for its hepatotoxic and carcinogenic effects. Solid phase extraction (SPE) or the clean-up with organic solvents or immunoaffinity columns (IAC) have been frequently applied in the analysis of mycotoxins from cereals and/or milk. IAC in combination with HPLC are increasingly used as reference method due to their high selectivity and good elimination of matrix interferences. However, the cost of analysis is usually high. In recent years, molecularly imprinted polymers (MIP) have been become very popular and promising materials for extracting different analytes. AFs are too toxic to be used in MIP preparation and template bleeding may be an additional problem, especially when dealing with very low levels. For this reason, a dummy template was preferred for MIP synthesis. A rapid and selective extraction method based on magnetic MIP (MMIP) has been developed for the isolation of aflatoxins (B1, B2, G1, G2, M1) using a combination of imprinted polymer and magnetite. The successful MMIP stirring “cake” (used as a stir-bar) has been combined with HPLC-MS/MS for the determination of AFM1 in milk powder (infant formulas) to demonstrate its applicability to real samples.

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