Pharmacological activities of pyrazolone derivatives

Pyrazoline is a five member heterocyclic ring which is a versatile lead compound for designing potent bioactive agents. The review of the literature shows that the pyrazoline derivatives are quite stable and has inspired the chemists to synthesize the new pyrazoline derivatives. The past studies of pyrazoline derivative revealed that they are useful in pharmaceutical and agrochemical research. Pyrazoline derivatives display various pharmacological activities such as antitumor, antitubercular, antimicrobial, antibacterial, anti-inflammatory and antioxidant etc. and the pharmacological activities of different synthesized compound are reviewed in the present article

A short glimpse on promising pharmacological effects of Begenia ciliata

Bergenia ciliata is a potent indigenous folk medicine that has been proved fruitful in the treatment of various adverse conditions of the body. The major chemical constituents of plant include tannic acid, gallic acid, glucose, metarbin, albumen, bergenin, (+)-catechin, gallicin. Bergenia ciliata was subjected to bioactivity analysis. The plant has antitussive, antiulcer, antioxidant, antibacterial, hypoglycemic, toxicological activity. It was observed that root and leaves extract were promising as antifungal agent. The root and leaves extract were effective against Microsporum canis, Pleuroetus oustreatus and Candida albicans.   All the extracts except chloroform extract of root and leaves of Bergenia ciliata were found to possess hypoglycemic activity in Streptozotocin (STZ) treated rats. The methanolic extract exhibited significant anti-tussive activity in a dose-dependent manner. B. ciliata bear potent anti-neoplastic activities that may have prospective clinical use as precursor for preventive medicine. Methanolic and aqueous B. ciliata rhizome extracts were found to possess antioxidant activity, including reducing power, free radical scavenging activity and lipid peroxidation inhibition potential. Bergenia ciliata extracts exhibit a narrow spectrum antibacterial activity. The results obtained thus suggest that extracts of B. ciliata have promising therapeutic potential and could be considered as potential source for drug development by pharmaceutical industries

A REVIEW ON PHARMACEUTICAL PROCESS VALIDATION OF SOLID DOSAGE FORM [TABLETS]

The article gives an introduction and general overview on process validation of pharmaceutical tablet manufacturing process. Process Validation is one of the important steps in achieving and maintaining the quality of final product. Process validation emphasizes the role of statistical tools and analyses, knowledge, detection, and control of variability and thus gives assurance on consistency of quality product. The validation study provides the accuracy, sensitivity, specificity and reproducibility of the established and documented test methods employed by the manufacturer. Thus, validation is an essential part of the quality assurance. This review examines the need for pharmaceutical validation, the various approaches, process and steps to be monitored during tablet manufacturing process. Key words: Process Validation, Types, Validation Stages, Guidelines and Process.Â

PRODRUG AS A NOVEL APPROACH OF DRUG DELIVERY- A REVIEW

Prodrugs are bioreversible derivatives of drug molecules that undergo an enzymatic and/or chemical transformation in vivo to release the active parent drug, which can then exert the desired pharmacological effect. Prodrug design is a choice of approach in solving many of the problems like stability, toxicity, solubility, permeability and drug targeting that affect drug discovery and development. Prodrug design is fruitful approach for drug targeting by changing the physiochemical, biopharmaceutical or pharmacokinetic properties of drugs. About 10-14% of drugs approved worldwide can be classified as prodrugs. The present article takes a review of introduction, classification, applications of prodrug design in various areas of drug development and basic functional groups that are amenable to prodrug design.Keywords: Prodrugs, objectives, classification, application, functional groups, limitation

A SHORT COMPILATION ON ZIKA VIRUS TRANSMISSION AND ITS COMPLICATION DURING PREGNANCY

Zika virus, a mosquito borne flavivirus transmitted primar­ily by Aedes aegypti mosquitoes is a pathogen affecting humans. These vectors also trans­mit dengue and chikungunya virus and are found throughout much of the world, including parts of the United States. An estimated 80% of persons infected with Zika virus are asymptomatic. Microcephaly is the greater risk for the infant born from the Zika Virus infected pregnant mother. This virus also causes neurological syndromes. Zika virus disease can often be diagnosed by performing reverse transcriptase-polymerase chain reaction (RT-PCR) on serum. Keywords: Zika Virus, Pregnancy, Microcephaly, Aedes aegypti mosquito, Brazil

FOXO1 promotes the expression of canonical WNT target genes in examined basal-like breast and glioblastoma multiforme cancer cells

Basal-like breast cancer (BBC) and glioblastoma multiforme (GBM) are aggressive cancers associated with poor prognosis. BBC and GBM have stem-cell-like gene expression signatures, which are in part driven by forkhead box O (FOXO) transcription factors. To gain further insight into the impact of FOXO1 in BBC, we treated BT549 cells with AS1842856 and performed RNA sequencing. AS1842856 binds to unphosphorylated FOXO1 and inhibits its ability to directly bind to DNA. Gene Set Enrichment Analysis (GSEA) indicated that a set of WNT pathway target genes, including lymphoid enhancer-binding factor 1 (LEF1) and transcription factor 7 (TCF7), were robustly induced after AS1842856 treatment. These same genes were also induced in GBM cell lines U87MG, LN18, LN229, A172 and DBTRG upon AS1842856 treatment. In contrast, follow-up RNA interference (RNAi) targeting of FOXO1 led to reduced LEF1 and TCF7 gene expression in BT549 and U87MG cells. In agreement with RNAi experiments, CRISPR Cas9-mediated FOXO1 disruption reduced the expression of canonical WNT genes LEF1 and TCF7 in U87MG cells. The loss of TCF7 gene expression in FOXO1 disruption mutants was restored by exogenous expression of the DNA-binding-deficient FOXO1-H215R. Therefore, FOXO1 induces TCF7 in a DNA-binding-independent manner, similar to other published FOXO1-activated genes such as TCF4 and hes family bHLH transcription factor 1 (HES1). Our work demonstrates that FOXO1 promotes canonical WNT gene expression in examined BBC and GBM cells, similar to results found in Drosophila melanogaster, T-cell development and murine acute myeloid leukemia (AML) models

Thyroid isthmus agenesis

The thyroid gland is the largest of all endocrine glands and is placed anteriorly in the lower neck in level with fifth cervical and first thoracic vertebrae. It is "H" shaped with two large lateral lobes, connected by a narrow isthmus in the midline. The gland bears very important clinical significance; both physiologically and pathologically and; a wide range of variations and anomalies of the gland have been reported. We report a case of complete agenesis of thyroid isthmus found during routine cadaveric dissection for the purpose of teaching learning of medial undergraduates at our department. This anomaly is quite uncommon and bears important clinical importance in wide fields of surgical and medical specialties. The embryological basis of the anomaly is high separation of a thyroglossal duct, which can give rise to two independent thyroid lobes with no isthmus

Screening of Maize Genotypes against Southern Leaf Blight (Bipolaris maydis) during Summer Season in Nepal

Abstract A study was conducted from 29 March 2014 to 27 July 2014 at the Institute of Agriculture and Animal Science, Paklihawa, Rupandehi with the objective of screening 13 maize genotypes against southern leaf blight caused by Bipolaris maydis. Field experiment was laid out in a randomized complete block design with three replications. Disease scoring was done as percentage of leaf area infected on individual plant at 5 days intervals starting from 63 days after sowing, for 3 times, and disease severity and mean AUDPC were calculated and yield was recorded. Among the tested genotypes, disease severity varies significantly. Disease symptoms appeared first in Yellow Popcorn, 64.00 days after sowing (DAS) with the highest severity and at last in RML-32/RML-17 (79.00 DAS) with the least score in field. The 13 genotypes differed significantly in mean AUDPC values. RML-32/RML-17 (AUDPC value 5.90) appeared most resistant, followed by RML-4/RML-17 (AUDPC value 11.50), while Yellow Popcorn (AUDPC value 71.99) was most susceptible among the tested genotypes. Highest maize yield (3.43 metric ton ha ) on Yellow Popcorn. Maximum SPAD value above cob was recorded in RML-4/RML-17 (45.62) followed by S03TLYQ-AB-01 (44.88) while minimum in Yellow popcorn (30.60). So, Yellow popcorn has the highest (3.16) and RML-32/RML-17 (0.08) lowest total AUDPC above cob. Similarly maximum SPAD value below cob was recorded in RML-4/RML-17 (44.37), while minimum in Yellow popcorn (28.82). So, Yellow popcorn has the highest (8.75) and RML-32/RML-17 (0.41) has lowest total AUDPC below cob. The genotypes RML-4/RML-17 and RML-32/RML-17 appeared resistant to SLB with maximum yield. These genotypes could be used as the sources of resistance in breeding program and could be developed to resistant varieties grown under tropical and subtropical climatic conditions during summer season. The genotype Yellow popcorn being highly susceptible to SLB with a maximum mean AUDPC and minimum yield, can be used as susceptible check for breeding purpose and different varietal screening