Incidence of biofilms among the multidrug resistant E. coli, isolated from urinary tract infections in the Nilgiris district, South India.

Multidrug resistant uropathogenic Escherichia coli (MDRUPEC) significantly correlates with recurrent, complicated, and persistent urinary tract infection (UTI). The leading cause of multidrug resistance is the ability of E. coli to form biofilms.

1-Tetracosanol isolated from the leaves of Eupatorium glandulosum, accelerates wound healing by expressing inflammatory cytokines and matrix metalloproteinase.

Ethnopharmacological Relevance: The leave paste of the plant, Eupatorium glandulosum H. B & K, has been traditionally used to treat cuts and wounds by the tribal community of the Nilgiris district of Tamilnadu, India.

Aim Of The Study: The present study was carried out to investigate the wound healing potential of this plant extract and the compound, 1-Tetracosanol, isolated from the ethyl acetate fraction.

Repurposing of FDA Approved Drugs and Neuropep peptides as Anticancer Agents Against ErbB1 and ErbB2.

ErbB1 and ErbB2 are the most important biological targets in cancer drug discovery and development of dual inhibitors for the cancer therapy. FDA approved drugs and Neuropep peptides were used to fit into the ATP binding site of the tyrosine kinases; ErbB1 and ErbB2 proteins. Cytoscape, iGEMDOCK, HPEPDOCK and DataWarrior softwares were used to study the role of these agents as anticancer drugs.

Plant-based Natural Products as inhibitors for Efflux Pumps to Reverse Multidrug Resistance in : A Mini Review.

Wounds provide a favourable site for microbial infection. Wound infection makes the healing more complex and does not proceed in an orchestrated manner leading to the chronic wound. Clinically infected wounds require proper antimicrobial therapy.

Peptides for Dual Targeting of ErbB1 and ErbB2: Blocking EGFR Cell Signaling Transduction Pathways for Cancer Chemotherapy.

Cancer is one of the most deadly diseases involving dysregulated cell proliferation. Chemotherapeutic drugs have serious drawbacks of nonspecific toxicity and drug resistance. Tyrosine kinases are a significant class of enzymes of protein kinases.

Targeting of ErbB1, ErbB2, and their Dual Targeting Using Small Molecules and Natural Peptides: Blocking EGFR Cell Signaling Pathways in Cancer: A Mini-Review.

Cancer is one of the deadliest diseases involving dysregulated cell proliferation and has been the leading cause of death worldwide. The chemotherapeutic drugs currently used for treating cancer have serious drawbacks of non-specific toxicity and drug resistance. The four members of the human epidermal growth factor receptor (EGFR), namely, ErbB1/HER1, ErbB2/HER2/neu, ErbB3/HER3 and ErbB4/HER4, the trans-membrane family of tyrosine kinase receptors, are overexpressed in many types of cancers.

Plant-based Natural Products for Wound Healing: A Critical Review.

Wound healing is an intricate process consisting of four overlapping phases, namely hemostasis, inflammation, proliferation, and remodelling. Effective treatment of wounds depends upon the interaction of appropriate cell types, cell surface receptors, and the extracellular matrix with the therapeutic agents. Several approaches currently used for treating wounds, such as advanced wound dressing, growth factor therapy, stem cell therapy, and gene therapy, are not very effective and lead to impaired healing.

Plant Based Natural Products as Quorum Sensing Inhibitors in E. Coli: A Critical Review.

The existence of multidrug-resistant (MDR) E. coli (superbugs) is a global health issue confronting humans, livestock, food processing units, and pharmaceutical industries. The quorum sensing (QS) controlling ability of the E.

screening of FDA approved drugs against ACE2 receptor: potential therapeutics to inhibit the entry of SARS-CoV-2 to human cells.

An unknown coronavirus that emerged sometime at the end of 2019 in China, the novel SARS-CoV-2, now called COVID-19, has spread all over the world. Several efforts have been made to prevent or treat this disease, though not with success. The initiation of COVID-19 viral infection involves specific binding of SARS-CoV-2 to the host surface of the receptor, ACE2.

Structural and functional analysis of Chitinase-IV of : molecular modeling and dynamic simulation study.

is an important oil seed crop. The productivity of this plant, however, is known to be low due to the attack of plant pathogens. The plant chitinase-IV is known to hydrolyse the chitin present in the cell walls of the plant pathogens and thus enhance the plant defense systems.

Coronavirus disease - COVID-19: new perceptives towards epidemic to pandemic.

The sudden outbreak and uncontrolled spread of the novel coronavirus disease 2019 (COVID-19) has shocked the world to a degree never seen before. Due to the wide spread transmission of the virus, the number of infected cases worldwide has surpassed 16,421,958 and global death toll has spiked up to 6,52,308 from December 2019 to 27 July 2020. The virus has been labelled as a pandemic by the WHO.

In-silico design and synthesis of N9-substituted β-Carbolines as PLK-1 inhibitors and their in-vitro/in-vivo tumor suppressing evaluation.

A new series of β-Carboline/Schiff bases was designed, synthesized, characterised and biologically evaluated as inhibitors of PLK-1. The synthesized compounds exhibited strong to moderate cytotoxic activities against NCI-60 panel cell assay. Compound SB-2 was the most potent, particularly against colon with GI of 3-45 µM on NCI-60 panel cell lines.

Thiazolidinediones as antidiabetic agents: A critical review.

Thiazolidinediones (TZDs) or Glitazones are an important class of insulin sensitizers used in the treatment of Type 2 diabetes mellitus (T2DM). TZDs were reported for their antidiabetic effect through antihyperglycemic, hypoglycemic and hypolipidemic agents. In time, these drugs were known to act by increasing the transactivation activity of Peroxisome Proliferators Activated Receptors (PPARs).

Potential Pharmacological Inhibitors of Pim Kinase Under Clinical Trials.

Pim kinases, also known as Serine/Threonine kinases, are intensively studied protein drug targets in cancer research. They play crucial role in the regulation of signal transduction cascades that promote cell survival, proliferation and drug resistance. Pim kinases are overexpressed in several hematopoietic and solid tumors and support in vitro/in vivo malignant cell growth and survival, through cell cycle regulation and inhibition of apoptosis.

Novel HDAC8 inhibitors: A multi-computational approach.

Abnormal HDAC function triggers irregular gene transcription that hampers the essential cellular activities leading to tumour activation and progression. HDAC inhibition has, therefore, been reported as a potential target for cancer treatment. In the present study, a sequential computational framework was carried out to discover newer lead compounds, namely HDAC8 inhibitors for cancer therapy.

The Blood Brain Barrier and its Role in Alzheimer's Therapy: An Overview.

Background: Alzheimer's disease (AD) is the most frequent age related neurodegenerative disorder. It represents 70% of all dementia. Millions of people have been affected by AD worldwide.

Poly(malic acid) bearing Doxorubicin and N-Acetyl Galactosamine as a site-specific prodrug for targeting hepatocellular carcinoma.

In the past, several systems of drug delivery carriers have been designed with a high capacity to target specific cells and/or tissues and a reduced non-specific toxicity. In this context, we synthesized and characterized novel poly(malic acid) derivatives bearing Doxorubicin (Dox), Poly(ethylene glycol) (PEG) and/or N-Acetyl Galactosamine (NAcGal) for drug delivery. These poly(malic acid) derivatives were obtained by chemical modification of the carboxylic acid lateral groups of poly(malic acid) (PMLA).

Inhibitors of histone deacetylase as antitumor agents: A critical review.

Histone deacetylase (EC 3.5.1.

Development of sustained release antipsychotic tablets using novel polysaccharide isolated from Delonix regia seeds and its pharmacokinetic studies.

A natural polysaccharide was isolated from the seeds of Delonix regia. The isolated polysaccharide could maintain aqueous equilibrium between the dosage form and the surrounding medium due to its massive competence of water absorption (80.72%) and swelling index (266.

Targeting strategies for Human immunodeficiency virus: a combinatorial approach.

The battle between human and the Human immunodeficiency virus (HIV) is on, with both of them rapidly improving their attacking and defense strategies. Many therapeutic agents for HIV infection have been designed and developed, However there are various aspects, like novel targets against HIV, which are yet to be unfolded with a goal of designing and developing novel drug molecules against HIV. This article reviews the current status and innovative new options for antiretroviral therapy for HIV and also discusses the various mechanisms of action for each class of drugs, and the problems yet to be solved with respect to HIV as a target for improvised treatment against AIDS.

Synthesis, characterization, and in vitro drug release study of methacrylate diclofenac conjugate as macromolecular prodrug.

Diclofenac was covalently coupled to 2-hydroxyl ethyl methacrylate (HEMA) to get a monomeric drug derivative of diclofenac. This monomer was subjected to radicular polymerization to get poly(diclo-EMA) conjugate. The in vitro drug release study of the polymeric prodrug was carried out in buffers of pH 1.

Isolation and evaluation of a polysaccharide from Prunus amygdalus as a carrier for transbuccosal delivery of Losartan potassium.

An oral buccoadhesive drug delivery system for Losartan potassium using a hydrophilic polysaccharide, isolated from Prunus amygdalaus (Badam gum), was developed and evaluated for its potential to overcome the drawbacks associated with the conventional drug therapy. The results of the study indicate that the isolated polysaccharide has good physicochemical and morphological characteristics and is suitable for use as a mucoadhesive sustain release polymer in pharmaceutical dosage forms, to alleviate the drawbacks of the conventional drug therapy of Losartan potassium.

Poly(HEMA-Zidovudine) conjugate: a macromolecular pro-drug for improvement in the biopharmaceutical properties of the drug.

A macromolecular pro-drug of a known anti-viral agent Zidovudine (AZT) was synthesized and evaluated as a sustained drug delivery system. The pro-drug was synthesized by coupling the drug to 2-hydroxyethyl methacrylate (HEMA) through a succinic spacer to get a monomeric drug conjugate which was polymerized to obtain the polymeric pro-drug. The pro-drug was subjected for in-vitro drug release study in buffers of pH 1.

Antioxidant activity of Caesalpinia digyna root.

The antioxidant properties of three successive extracts of Caesalpinia digyna Rottler root and the isolated compound, bergenin, were tested using standard in vitro and in vivo models. The amount of the total phenolic compounds present was also determined. The successive methanol extract of Caesalpinia digyna root (CDM) exhibited strong scavenging effect on 2,2-diphenyl-2-picryl hydrazyl (DPPH) free radical, 2,2'-azino-bis(3-ethylbenzo-thiazoline-6-sulphonic acid) diammonium salt (ABTS) radical cation, hydrogen peroxide, nitric oxide, hydroxyl radical and inhibition of lipid peroxidation.

In vitro and in vivo studies on HPMC-K-100 M matrices containing naproxen sodium.

Controlled release (CR) matrix tablets of naproxen sodium were prepared by wet granulation using hydroxypropyl methyl cellulose (HPMC-K-100 CR) as the hydrophilic rate controlling polymer. The effect of the concentration of the polymer and different fillers on the in vitro drug release rate was studied. The studies indicated that the drug release can be modulated by varying the concentration of the polymer and the fillers.