Histone Modifications as Therapeutic Targets for Cancer

 

Ling Zhang1, Tao Wang1, Steven Bing Geng2, Ke Ren3* 

1Department of Biochemistry and Molecular Biology, Colorado State University, Fort Collins, CO, 80523

2Department of Chemical Engineering, Rensselaer Polytechnic Institute, Troy, NY, 12180

3Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198-6025

Abstract

Epigenetics are important factors in the development of oncogenesis. Methylation, acetylation and phosphorylation are major types of histone modifications and also major components of epigenetics. Cancer cells have been shown to display abnormal levels of histone modification. Recently, researchers have proved that cancer can be prevented via the disruption of histone modifications. This review summarizes the current understanding of histone modifications in carcinogenesis, and therapeutic approaches targeting histone modifications for cancer treatments.

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In vitro Cytotoxic and Thrombolytic Activity of Methanolic Extract of Bauhinia acuminata Leaves

 

Md. Naimul Islam1, Md. Abul Barakat Fahad1, Mohammad Robiul Hossain1, Mohammad Mamun ur Rashid1, Md. Reyad-ul-Ferdous2,3*, Mohsina Mukti2

1Department of Pharmacy, International Islamic University Chittagong, 154/A, College Road, Chittagong-4203, Bangladesh.
2Department of Pharmacy, North South University, Bashundhara, Dhaka-1229, Bangladesh.

3Department of Pharmacy, Progati Medical Institute, Dhaka-1207, Bangladesh.

Abstract

The present study was designed to investigate the cytotoxic and thrombolytic activity. Methanolic extract of leaves of B. acuminatewas assessed with the Brine shrimp lethality bioassay used to evaluate cytotoxicity. The methanolic extract of B. acuminata was assessed with human blood to evaluate thrombolytic effect. The extract showed remarkable cytotoxic activity, LC50 value of the extract was 15.41μg/ml compared to vincristin sulphate. It also evaluated for thrombolytic agent compared to streptokinase. It has the significant thrombolytic effect which was about 10.058%.These findings demonstrate that the leaves extract of B. acuminatahave significance cytotoxic andthrombolytic activities. This plant can be used in further investigation for lead compound isolation and other pharmacological activities.

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Formulation and Assessment of Mouth Dissolving Tablets of Repaglinide-ß-Cyclodextrin Complex

 

Lakahan Chadar1*, Vaibhav Shukla1,2, S K Jain3

1Oriental College of Pharmacy, Bhopal-462021, (M.P.), India

2Department of Pharmaceutical Sciences, Dr. K.N. Modi University, Newai, Tonk-304021, (Rajasthan), India

3Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar-470003, (M.P.), India

Abstract

The present study was carried out to develop mouth dissolving tablets of Repaglinide with a rationale of providing better patient compliance, will serve to provide effective mode of treatment to elderly, impaired and noncooperative patient suffering from diabetes. The Repaglinide-ß-cyclodextrin complex was prepared in order to increase the solubility of drug. The inclusion efficiency of different ratios of Repaglinide-ß-cyclodextrin complex was calculated, that shows the inclusion efficiency of 1:1 molar ratio complex is highest. The mouth dissolving tablets of Repaglinide (RCT1 to RCT5) were prepared by direct compression method using super disintegrants, for optimization of the diluents. The value of pre-compression of blends and post-compression tablets exhibited satisfactorily results. The formulation RCT3 complied with all the physical parameters such as hardness, friability and disintegration time, and taken for further studies. Nine different formulations (RCT6 to RCT14) were prepared by using various concentration of super disintegrant namely Crosscarmellose sodium, Crosspovidone and Sodium Starch Glycolate. Among all formulations studied, formulation RCT9 having crospovidone as disintegrant showed 56.5% drug release in 5 min. Therefore crospovidone is considered best superdisintegrant among Sodium starch glycolate and Crosscarmellose sodium.

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Evaluation of Protective Effect of Pleurotus ostreatus Against Insulin Producing RINm5F Cells

 

Amit Roy*, Ram Kumar Sahu, Pushpa Prasad

Columbia Institute of Pharmacy, Tekari, Raipur-493111 (C.G.), India

Abstract

Determination of antidiabetic activity by cell line method is one of the foremost techniques compared to in vivo animal model. It is fruitful in determining the mechanism of drugs. The RINm5F cells are considered to produces insulin and it is one of most widely used insulin-secreting cell lines. In the present study, we assessed the defensive property of Pleurotus ostreatus against RINm5F cells. The apoptosis of RINm5F cells were determined by providing the cell with ethanol extract of P. ostreatus in presence of streptozotocin (STZ). The STZ treated group significantly increases the apoptotic population compared to the normal group. The extract treated RINm5F cells manifested the decline in apoptotic population resembled to STZ treated RIN cells. The present study scientifically supported the protective effects of the P. ostreatus against the oxidative damage induced by STZ.

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Formulation Development and In-vitro Evaluation of Mouth Dissolving Tablets of Celecoxib Employing Distinctive Proportion of Disintegrating Agents

 

Daljit Masih1*, Rajesh Gupta2

1J.J.T. University, Chudela, Jhunjhunu, (Rajasthan), India

2Sri Sai College of Pharmacy, Pathankot, (Punjab), India

Abstract

In present study we planned to formulate and evaluate mouth dissolving tablets of Celecoxib using superdisintegrants agents namely Crospovidone and Sodium starch glycolate in various ratios. The mouth dissolving tablets were prepared by direct compression method using Crospovidone and Sodium starch glycolate. Tablets blends were evaluated for loose bulk density, tapped bulk density, compressibility index and angle of repose, shows satisfactory results. The compressed tablets were then evaluated for various physical tests like thickness, friability, hardness, weight variation, wetting time, water absorption ratio and disintegration test by using standard procedures. The results of all these tests were found to be satisfactory. The in-vitro dissolution study was carried out for 14 min using paddle method in phosphate buffer (pH 6.8) as dissolution media. The data of in-vitro dissolution of tablets revealed that 76 to 100% of drug release from various formulations at 14 min. The formulation C7 exhibited better results as compared to other formulations.

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Overview on Recent Researches on Floating Microspheres

 

Manish Negi*, Vikash Kumar Shukla, T. S. Easwari

IIIMT College of Medical Sciences, Mawana Road, Meerut-250001, (U.P.), India

Abstract

Conventional oral dosage forms offer no control over drug delivery, leading to fluctuations in plasma drug level. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Floating microspheres are especially suitable for achieving sustained or delayed release oral formulations with flexibility of blending to attain different release patterns, low risk of dose dumping as well as reproducible and short gastric retention time. The floating microspheres produces controlled delivery of drug and also enhance the bioavailability of drug. Floating microsphere is especially gaining attention due to their wide applicability in the targeting of drugs to the stomach. These floating microspheres have the advantage that they remain buoyant and distributed uniformly over the gastric fluid to avoid the vagaries of gastric emptying retention time of drugs. This review provides an overview of scientific work done in the formulation and development of various drug for floating microspheres.

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