Assessment Of Anticancer Activity Research Articles

Amino acid sequence determination, in silico tertiary structure prediction and anticancer activity assessment of l-glutaminase from Bacillus cereus

Microbial glutaminase has been extensively used as antitumor drug in pharmaceutical industry from past few decades. The structural analysis based on homology modeling predicted a hypothetical 3D model structure for l-glutaminase from Bacillus cereus MTCC 1305 using peptide sequence data obtained from MALDI-TOF MS and template model of X-ray crystal structure of l-glutaminase from Bacillus subtilis (PDB: 1MKI_A). The model was found more reliable with 98.8 % residues in the favored region of Ramachandran plot. The predicted model structure was further refined using ANOLEA, QMEAN score and GROMOS 96 force field with total energy of −11,636.01 kJ/Mol and Z-score value as −1.41. Active site of predicted model was found to be enriched with 11 conserved amino acid residues like Ser73, ASN125, Asn176, Val270, Gln72, Cys204, Val270, Ser271, Tyr200, Lys76, Phe105, Tyr252. The docking approach showed good binding affinity of predicted model towards l-glutamine with favorable ΔG docking score. The anticancer activity of this enzyme was confirmed against colon carcinoma (HCT-116) cell line with IC50 value of 99.79 μg/ml.

Development and Assessment of Anti Cancer Activity of Phytosome Using Isolated Compound from Clerodendron Paniculatum Linn Root Extract

Development and Assessment of Anti Cancer Activity of Phytosome Using Isolated Compound from Clerodendron Paniculatum Linn Root Extract

Assessment of anticancer activity: A comparison of dose–response effect of ethyl acetate and methanolic extracts of Pergularia daemia (Forsk)

BackgroundOral cancer is the sixth most common malignancy worldwide and is thus an important cause of death and morbidity. Although several drugs have been developed for the treatment of oral cancer, naturally occurring phytochemicals have been recommended by nutritionists and health experts to treat various types of cancer. Pergularia daemia is a well-known herb distributed across India, finding many uses in medicine. AimThe present study was mainly designed to determine the dose–response effect of the whole plant extract of P. daemia on experimental oral carcinogenesis. Materials and methodsMale golden Syrian hamsters were painted with 0.5% of 7,12-dimethylbenz[a]anthracene (DMBA) in liquid paraffin on the left buccal pouch to induce oral cancer, thrice a week for 14 weeks. The anticancer effect of the ethyl acetate and methanolic extracts of P. daemia was observed to be dose dependent (100, 200, and 300mg/kg body weight (bwt)) by assessing the bwt, tumor incidence, changes in oxidant/antioxidant levels, and histological alterations of control and experimental animals. ResultsOur results showed that of the three doses used, the high dose (300mg/kg bwt) exhibited excellent antioxidant activity in comparison to the other two doses. Moreover, our findings suggest that the methanolic extract significantly inhibited cancer development to a greater extent than the ethyl acetate extract. ConclusionThus, it could be concluded that the whole plant of P. daemia presents an easily accessible source of natural antioxidants, and regular consumption can reduce the incidence of oral cancer.

BmKn-2 scorpion venom peptide for killing oral cancer cells by apoptosis.

Scorpion venom peptides recently have attracted attention as alternative chemotherapeutic agents that may overcome the limitations of current drugs, providing specific cytotoxicity for cancer cells with an ability to bypass multidrug-resistance mechanisms, additive effects in combination therapy and safety. In the present study, BmKn-2 scorpion venom peptide and its derivatives were chosen for assessment of anticancer activities. BmKn-2 was identified as the most effective against human oral squamous cells carcinoma cell line (HSC-4) by screening assays with an IC50 value of 29 μg/ml. The BmKn-2 peptide killed HSC-4 cells through induction of apoptosis, as confirmed by phase contrast microscopy and RT-PCR techniques. Typical morphological features of apoptosis including cell shrinkage and rounding characteristics were observed in treated HSC-4 cells. The results were further confirmed by increased expression of pro-apoptotic genes such as caspase-3, -7, and -9 but decrease mRNA level of anti-apoptotic BCL-2 in BmKn-2 treated cells, as determined by RT-PCR assay. In summary, the BmKn-2 scorpion venom peptide demonstrates specific membrane binding, growth inhibition and apoptogenic activity against human oral cancer cells.

Non-linear assessment of anticancer activity of 17-picolyl and 17-picolinylidene androstane derivatives – Chemometric guidelines for further syntheses

The present paper deals with prediction of cytotoxic activity of 17-picolyl and 17-picolinylidene androstane derivatives toward androgen receptor negative prostate cancer cell line (PC-3). The prediction was achieved applying artificial neural networks (ANNs) method on the basis of molecular descriptors. The most important descriptors (skin permeability (SP), Madin–Darby canine kidney cell permeability (MDCK) and universal salt solubility factor (S+SF)) were selected by using stepwise selection coupled with partial least squares method. The ANN modelling was carried out in order to obtain reliable models which can facilitate further synthesis of androstane derivatives with high antiproliferative activity toward PC-3 cell line. The modelling procedure resulted in three ANN models with the best statistical performance. The obtained results show that the established ANN models can be applied for required purpose.

Target genes involved in antiproliferative effect of modified ginseng extracts in lung cancer A549 cells.

Lung cancer is the most common cancer and the leading cause of cancer-related deaths. Panax ginseng has long been used to treat cancer and other diseases worldwide. Most of the pharmacological actions of ginseng are attributed to a variety of ginsenosides, which are often metabolized by intestinal bacteria into more effective forms. In this study, we found that the antiproliferative activity of ginseng was increased after enzymatic processing of ginseng saponin (50% inhibitory concentration, >70 μg/ml). To elucidate the mechanism by which modified ginseng extract (MGX) induced cell death in human lung cancer cells, the gene expression profiles of A549 cells regulated by MGX were assayed using Agilent PrimeView Human Gene Expression Arrays. The expression of 17 genes involved in the regulation of cell signaling, cell metabolism, transport, and cytoskeleton-regulation was up-regulated, whereas the expression of 16 genes implicated in invasion and metastasis and cellular metabolism was down-regulated in MGX-treated A549 cells. Moreover, nuclear staining with 4',6-diamidino-2-phenylindole revealed that MGX clearly caused nuclear condensation and fragmentation which are observed in apoptosis cell. These results elucidate crucial anticancer mechanisms of MGX and provide potential new targets for the assessment of anticancer activity of MGX.

In Vitro Antioxidant and Anti-HIV Activity of Endophytic Coumarin from Crotalaria pallida Aiton

In the present study, four different endophytic fungi (Aspergillus flavus, A. niger, Fusarium oxysporum and F. solani) were isolated from different parts of Crotalaria pallida. Soxhlet and Microwave-Assisted Extraction (MAE) methods were used to determine the amount of coumarin in methanol extracts. Best results were obtained with MAE (50% aqueous ethanol, two heating cycles of 5min, 500C). The isolated compound was analyzed with an appropriate HPLC procedure. Standard various methods strongly confirms the presence of coumarin in MAE extracts of endophytes. Coumarin and Ortho-coumaric acid was purified from extracts using column chromatography and was used for in vitro anti-HIV and anticancer activity assessment. The methanol extracts of A. niger and F. oxysporum showed potent antioxidant activity in ABTS, FRAP and DPPH. In vitro anti-HIV activity was done against glycohydrolase enzyme (á-glucosidase, β-glucorinidase and lysozyme). The o-coumaric acid showed strong inhibition of these viral replicating enzymes. The results of the present investigation clearly indicate that endophytes, A. niger and F. oxysporum contained coumarins and displayed potent antioxidant and anti-HIV activity.

The assessment of anti-cancer activities and saponin profiles of Gynostemma pentaphyllum saponins obtained from different regions of China

The assessment of anti-cancer activities and saponin profiles of Gynostemma pentaphyllum saponins obtained from different regions of China