جستجوی مقالات مرتبط با کلیدواژه "سیتوتوکسیک" در نشریات گروه "پزشکی"

Chemotherapy is one of the most common methods available for the treatment of cancer. Resistance to anticancer drugs can result in failures in chemotherapy of cancers. Therefore, investigation is necessary for the discovery of new drugs. Homoisoflavonoids are well-known natural products that possess a wide range of pharmacological activities. Hence, synthesis and assessment of cytotoxicity of homoisoflavonoids containing morpholinoethoxy moiety and their molecular docking simulation were taken into consideration.

Two 7-morpholinoethoxyhomoisoflavonoids synthesized via three steps including SN2 reaction of 7-hydroxychromanine with morpholino ethyl chloride hydrochloride in the basic media under reflux condition to produce intermediate 3. The second step included aldol condensation of the intermediate with suitable aldehydes in the presence of gaseous HCl in ethanol, and finally neutralization with NaOH 5%. The structures of the products were confirmed using IR, 13CNMR, and 1HNMR techniques. Cytotoxic effects of final products on HT-29 and 3T3 cell lines were assessed. To evaluate the binding mode of compounds with tubulin protein, docking simulation was performed by using MOE.

Two morpholinoethoxy homoisiflavonoids were prepared with moderate to good production yield. Cytotoxic evaluation of these compounds showed satisfactory results. The results of molecular docking simulation showed an acceptable binding energy of the interaction between the ligands with the tubulin protein binding site: (E)-7-(2-morpholinoethoxy)-3-(3,4,5-trimethoxybenzylidene) chroman-4-one= -7.3727 Kcal/mol and (E)-3-(4-methoxybenzylidene)-7-(2-morpholinoethoxy) chroman-4-one released -7.6838 Kcal/mol per mole of energy.

The results showed that compound (E)-3-(4-methoxybenzylidene)-7-(2-morpholinoethoxy) chroman-4-one has higher cytotoxicity than (E)-7-(2-morpholinoethoxy)-3-(3,4,5-trimethoxybenzylidene) chroman-4-one against HT-29 and 3T3 cell lines. The in-silico results confirmed the results obtained from in vitro experiments and showed three interactions between ligand (E)-3-(4-methoxybenzylidene)-7-(2-morpholinoethoxy)chroman-4-one and αThr179, αThr145, and αTyr224 amino acids in tubulin active site.

Sea urchin immune responses are directly exposed to potentially pathogenic microorganisms and develop defence responses mainly based on immunocytes and humoral factors contained in the coelomic fluid. In addition, the polyhydroxylated 1, 4-naphthoquinone pigments are found to possess excellent antimicrobial, antialgal and antioxidant activities. The present research aimed to study the bioactive potentials (antioxidant, antibacterial and cytotoxic) of coelomic fluid and pigments shells and spines of sea urchin, Echinodermata mathaei species.

The coelomic fluid and pigments shell and spine of sea urchin were isolated using buffered mode and hydrogen chloride (HCl), respectively. Then, antioxidant [reducing power, DPPH radical (1, 1-diphenyl 2-picryhydrazyl) scavenging, and total antioxidant capacity), antibacterial (minimum inhibitory concentration or MIC) and cytotoxic potentials were evaluated.

The free cells of the coelomic fluid had the highest activity in the all antioxidant methods, and the coelomocyte lysate had the highest antibacterial activity. All the differences were significant at the level of P < 0.05.

The result of this research indicated that coelomic fluid and pigments shell and spine of sea urchin, Echinodermata mathaei species, have potent antioxidant activity and the ability for scavenging cytotoxic effects. This suggests that sea urchin shells and spines, most of which are discarded as waste after removal of gonads, would be a new bioresource for natural antioxidants.

Since the incidence rate of colon carcinoma is growing significantly and natural products and medicinal plants are widely used in cancer treatment، the cytotoxic effects of two unstudied medicinal plants have been studied.

Different concentration of the hexane، chloroform and ethanol fractions of Uvaria grandiflora Roxb. (leaves and stem barks) and Diospyros wallichii King&Gamble. (fruits and stem barks) were subjected to cytotoxic investigation against HTC-116 cell line by using MTT technique. In this study، quercetin was used as a positive control.

The chloroform fraction of Uvaria grandiflora Roxb. stem barks and the chloroform fraction of Diospyros wallichii King&Gamble. Fruits exhibit the highest growth inhibiting activities among all the tested samples with the GI50 value of 3. 85 µg/ml and 4. 58 µg/ml، respectively.

From the obtained results، it was concluded that the Naphthoquinones derivatives from Diospyros wallichii and Flavonoids from Uvaria grandiflora are responsible for pharmacological and biological activities. Therefore، more investigations and isolations are recommended.

It is well known that marine microorganisms have been recognized as an important and untapped resource for novel bioactive compounds. Actinomycetes are gram positive bacteria showing a filamentous growth. They are a group of organisms widespread in nature and play a significant role in the future of drug development.

Marine bacteria strains of Streptomyces griscoloalbus were isolated from soft coral Sinularia erecta in Persian Gulf. Growth and fermentation character of the Streptomyces griscoloalbus were estimated. Cytotoxic activity of fermentation medium was tested by brine shrimp bioassay. Semi purification on the culture extract was performed.

Toxic extract was applied on KB cells ( human epidermoid carcinoma of mouth ) and results of neutral red test were IC50= 4.19 g/ml from acetone extract and IC 50 = 44.97 g/ml. For methanol extract, cytotologic effects of the acetone extract on KB cells was studied and morphological changes were also studied.

The morphological changes in Kb cells due to the cytotoxic extract of the bacteria has made it a good candidate for the production of cytotoxic drugs in the future.