A Two-Step Similarity-Based Method for Prediction of Drug’s Target Group.

A two-step similarity-based method for prediction of drug’s target group.

Protein Pept Lett. 2013 Mar; 20(3): 364-70
Chen L, Zeng WM

Determination of drug’s target protein is very important for studying drug-target interaction network, while drug-target interaction network is a key area in the drug discovery pipeline. Thus correct prediction of drug’s target protein is very helpful to promote the development of drug discovery. In this study, we developed a two-step similarity-based method to predict drug’s target group. In each step, a similarity score (obtained by graph representation in the first step, and chemical functional group representation in the second step) was employed to make prediction. Since some drugs can target proteins distributing in more than one group of proteins, the method provided a series of candidate target groups for each drug. As a result, the first-order prediction accuracy on training set and test set were 79.01% and 76.43%, respectively, which were much higher than the success rate of a random guess. The results show that using graph representation to encode drug is a good choice in this area. We expect that this contribution will provide some help to understand drug-target interaction network. HubMed – drug

MicroRNAs (miRNAs) in colorectal cancer: from aberrant expression towards therapy.

Curr Pharm Des. 2013; 19(7): 1242-52
Dassow H, Aigner A

MiRNAs are small noncoding RNA molecules that are often aberrantly over- or underexpressed in tumors, including colorectal cancer (CRC). Due to their capacity to regulate and thus fine-tune the expression of multiple target genes relevant in tumorigenesis,tumor progression, angiogenesis, metastasis and sensitivity towards chemotherapy, they influence various pivotal cellular processes with prognostic and therapeutic relevance in CRC.This review provides a comprehensive overview of miRNAs with established functional relevance in colorectal cancer, their established target genes and the resulting cellular and pathological phenotype(s). Furthermore, approaches towards therapeutic miRNA-based intervention are discussed. Those include viral or non-viral approaches of miRNA replacement therapy in the case of tumor-suppressing miRNAs, and multiple strategies for the inhibition of oncogenic miRNAs. Beyond the analysis of the functional relevance of a given miRNA as target molecule or a miRNA-based drug, several studies in preclinical in vivo models are described that provide the basis for possible future therapeutic intervention in man. HubMed – drug

Antiglycation, antioxidant and toxicological potential of polyphenol extracts of alligator pepper, ginger and nutmeg from Nigeria.

Asian Pac J Trop Biomed. 2012 Sep; 2(9): 727-32
Kazeem M, Akanji M, Hafizur RM, Choudhary M

To evaluate the antioxidant and antiglycation potential of polyphenols from three spices; alligator pepper, ginger and nutmeg.Polyphenol extracts of these spices were subjected to brine-shrimp lethality assay, phytotoxicity test, DPPH and superoxide anion radical scavenging as well as BSA-glucose antiglycation assay.Results obtained showed that polyphenol extract of ginger has the highest antioxidant potential with IC50 0.075 and 0.070 mg/mL for DPPH and superoxide anion radical scavenging assay while alligator pepper displayed highest antiglycation activity with IC50 0.125 mg/mL. However, nutmeg extract exhibited weakest cytotoxic and phytotoxic potential with LD50 4359.70 and 1490 µg/mL respectively.It can be concluded that the polyphenol extracts of alligator pepper, ginger and nutmeg displayed good antioxidant as well as antiglycation potential and are safe for consumption. HubMed – drug

Antihyperglycemic and antihyperlipidemic activity of ethyl acetate fraction of Rhododendron arboreum Smith flowers in streptozotocin induced diabetic rats and its role in regulating carbohydrate metabolism.

Asian Pac J Trop Biomed. 2012 Sep; 2(9): 696-701
Verma N, Amresh G, Sahu P, Rao ChV, Singh AP

To explore and identify the most potent antihyperglycemic fraction from the ethanol extract of Rhododendron arboreum (R. arboreum) flowers.Normal and streptozotocin induced diabetic rats were treated with all four fractions of R. arboreum flowers for short term and with fraction 3 for long term study. On completion of the treatment, a range of indicators were tested including fasting blood glucose, plasma protein, haemoglobin A1C, insulin secretion, body weight, blood lipid profile and carbohydrate metabolism regulating enzymes of liver.In short term study, the fraction 3 (Active fraction) produced a significant (P<0.000 1) reduction (73.6%) in blood glucose level at a dose of 200 mg/kg after the treatment in the diabetic rats. Administration of active fraction (200 and 400 mg/kg) once daily for 30 d in streptozotocin diabetic rats resulted in a significant (P<0.001 to P<0.000 1) fall in blood glucose level, hemoglobin A1C, serum urea and creatinine with significant but a increase in insulin level similar to standard drug glybenclamide. Further, the active fraction showed antihyperlipidemic activity as evidenced by significant (P<0.001 to P<0.000 1) decreases in serum serum total cholesterol, triglycerides, low density lipoprotein cholesterol and very low density cholesterol levels coupled together with elevation of high density lipoprotein cholesterol in the diabetic rats.The active fraction of R. arboreum flowers decreases streptozotocin induced hyperglycemia by promoting insulin secretion and glycolysis and by decreasing gluconeogenesis. HubMed – drug

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