Carvacrol Promotes Cell Cycle Arrest and Apoptosis through PI3K/AKT Signaling Pathway in MCF-7 Breast Cancer Cells / 中国结合医学杂志

OBJECTIVE@#To examine the role of carvacrol in modulating PI3K/AKT signaling involved in human breast cancer pathogenesis using in vitro experimental model MCF-7 cells.@*METHODS@#MTT and lactate dehydrogenase assays were performed with cells treated with different doses of carvacrol (0-250 p mol/L) at different time points (24 and 48 h). The nuclear morphology was assessed in MCF-7 cells with propidium iodide (PI) and acridine orange/ethidium bromide (AO/EB) staining and analyzed by fluorescence microscopy. Events like cell cycle arrest, apoptosis was observed by flow cytometric analysis and expressions of p-Rb, cyclin D1, cyclin-dependent kinase 4 (CDK4), CDK6, Bax, Bcl-2, PI3K/p-AKT was analyzed by immunoblot.@*RESULTS@#Carvacrol significantly reduced cell viability with the half maximal inhibitory concentration value of 200 µmol/L at 24 and 48 h (P<0.05). importantly, there was a significant increase in the accumulation of the G@*CONCLUSION@#Carvacrol significantly inhibited the breast cancer MCF-7 cell proliferation and induced apoptosis via suppressing PI3/AKT signaling pathway.

2-[[5-(Substituted-phenyl]-1,3,4-oxadiazol-2-yl]sulfanyl]-N-[1,3-thiazol-2-yl]acetamides: new bi-heterocycles as possible therapeutic agents

An electrophile, N-[1,3-thiazol-2-yl]-2-bromoacetamide [3], was synthesized by the reaction of 1,3-thiazole-2- amine [1] and 2-bromoethanoyl bromide [2] in an aqueous medium. A series of carboxylic acids, 7a-j, were converted into 1,3,4-oxadiazole heterocyclic core, through a series of three steps. The final compounds, 8a-j, were synthesized by stirring 7a-j and 3 in an aprotic polar solvent. The structural elucidation of the synthesized compounds was supported by IR, EI-MS, 1 H-NMR, and 13C-NMR spectral data. Title compounds were evaluated for enzyme inhibition against cholinesterases and alpha-glucosidase enzymes and their cytotoxic behavior was monitored using brine shrimp assay. The enzyme inhibitor potential of compounds was supported by molecular docking studies

Antioxidant, anticancer and antibacterial potential of zakhm-e-hayat rhizomes crude extract and fractions

Bergenia ciliata [locally known as Zakhm-e-hayat; wound healer] is commonly employed for wound healing, curing diarrhea and vomiting, fever, cough and pulmonary affections. Local community uses this plant as tea decoction with table salt. B. ciliata crude extract and its fractions were subjected to antibacterial, antioxidant effects as well as determination of total flavonoids and phenolics, DNA damage and anticancerous activities following standard protocols. Increased percentage inhibition of free radical in DPPH assay as well as elevated phenolic and flavonoid contents revealed antioxidant potential of this potent herb. Ethyl acetate and aqueous extracts showed IC50 of 0.7 and 0.3 mg/ml respectively, against H157 cell line. Antibacterial analysis showed MIC 0.4-10mg/ml for crude extract and fractions. The results obtained conclude that extracts of B. ciliata contain remedial latent and can be used as possible source for drug development by pharmaceutical industries

Evaluation of antioxidant potential and HPLC based identification of phenolics in Polygonum amplexicaule extract and its fractions

There is a growing interest for the plant-based medicines in pharmaceutical industry. Plant derived Antioxidants have gained huge importance regarding their medicinal value. The present study was designed to establish pharmaceutical value of Polygonum amplexicaule for their antioxidant activity using shoot, leaf and rhizome crude methanolic extract along with their n-butanolic, ethanolic, ethyl acetate and aqueous fractions. DPPH assay was used to assess antioxidants, which shows the maximum activity by crude methanolic extract of leaves [CMEL] having IC[50] 1.03 [micro]g/mL where all other fractions showed IC[50] in a range of 1.03-58.2 [micro]g/mL. The DNA plasmid protection assay showed that 10 ppm and 100 ppm concentrations of crude methanolic extracts [rhizome and leaf], aqueous fractions [shoot and leaf extract], n-butanolic fractions [shoot and leaf extract] and ethanolic fraction [rhizome extract] have DNA protection properties. TLC and HPLC based Identification of different antioxidants present in shoot, leaf and rhizome crude extracts and their fractions showed the presence of gallic acid, quercetin, catechin, caffeic acid, rutin, myricetin and kaempferol. This study suggested that this plant have high content of antioxidants, which needs to be investigated further for their medicinal and/ cosmaceutical applications

Synthesis, characterization, biological evaluation and QSAR of some Schiff base esters: promising new antitumor, antioxidant and anti-inflammatory agents

We report the synthesis, characterization, biological evaluation and quantitative structure-activity relationship of some Schiff base esters as promising new antitumor, antioxidant and anti-inflammatory agents. The Schiff base esters were synthesized by two synthetic routes using variably substituted hydroxy benzaldehydes with para amino phenol in appreciable yields. All the newly synthesized esters have been characterized by [1]H-NMR, [13]C-NMR, FT-IR techniques and elemental analysis. The synthesized esters were examined for antioxidant, antitumor and anti-inflammatory potentials through different bioassays and quantitative structure-activity relationship was studied. Bioassays showed encouraging results and indicated that some of these title compounds may have potential for further pharmacological investigations

Antioxidant and cytotoxic activities and phytochemical analysis of euphorbia wallichii root extract and its fractions

Euphorbia wallichii a perennial herb growing mainly in Himalayas has been widely used in folk medicines for its medicinal properties. In the present study, the crude methanolic root extract [CME] and its fractions; n-Hexane Fraction [NHF], n-Butanol Fraction [NBF], Chloroform Fraction [CHF], Ethyl acetate Fraction [EAF] and Aqueous Fraction [AQF] of this plant specie were investigated for antioxidant and cytotoxic activities and phytochemical analysis. Antioxidant activity was determined by using 2,2-diphenyl-1-picryl-hydrazyl free radical [DPPH] and DNA protection assay performed on pBR322 plasmid DNA. In both these assays, promising results were obtained for CME as well as other fractions. The IC[50] values for DPPH assay were in a range of 7.89 to 63.35 mocrog/ml in which EAF showed the best anti-oxidant potential and almost all the tested samples showed certain level of DNA protection. The cytotoxic activity was assessed by using Sulforhodamine B [SRB] assay on human cell lines; H157 [Lung Carcinoma] and HT144 [Malignant Melanoma]. The IC[50] values of the tested samples ranged from 0.18 to 1.4 mg/mL against H157 cell line whereas against HT144 cell line the IC[50] values ranged from 0.46 to 17.88 mg/mL with NBF fraction showing maximum potential for both. Furthermore, the phytochemical analysis of CME and its fractions showed the presences of flavonoids, saponins, tannins, terpenoides and cardiac glycosides with varying concentrations

Antimalarial activity of three Pakistani medicinal plants

This study was conducted to determine the in vitro anti-malarial activity of three medicinal plants, Picrorhiza kurroa, Caesalpinia bonducella and Artemisia absinthium of Pakistan. Different extracts of various parts of these plants were prepared by maceration and percolation, and were evaluated for their antimalarial activity. Aqueous, cold alcoholic and hot alcoholic extracts of Picrorhiza kurroa showed 34%, 100% and 90% inhibition in growth of Plasmodium falciparum, respectively, at 2.00 mg/ml. While aqueous, cold alcoholic and hot alcoholic extracts of Caesalpinia bonducella showed 65%, 56% and 76% inhibition in growth of Plasmodium falciparum, respectively at same concentrations. In the case of Artemisia absinthium, aqueous, cold alcoholic and hot alcoholic extract of Artemisia absinthium showed 35%, 55% and 21% inhibition in growth of Plasmodium falciparum, respectively at 2.00 mg/ml. In our study, extracts of Picrorhiza kurroa were found good for traditional therapy with highly significant results