Medicinal Chemistry and NMR Driven Discovery of Novel UDP-glucuronosyltransferase 1A Inhibitors That Overcome Therapeutic Resistance in Cells.

The UDP glucuronosyltransferases (UGT) deactivate many therapeutics via glucuronidation while being required for clearance of normal metabolites and xenobiotics. There are 19 UGT enzymes categorized into UGT1A and UGT2B families based on sequence conservation. This presents a challenge in terms of targeting specific UGTs to overcome drug resistance without eliciting overt toxicity.

H, C, N Backbone and sidechain chemical shift assignments of the C-terminal domain of human UDP-glucuronosyltransferase 2B17 (UGT2B17-C).

UDP-glucuronosyltransferases are the principal enzymes involved in the glucuronidation of metabolites and xenobiotics for physiological clearance in humans. Though glucuronidation is an indispensable process in the phase II metabolic pathway, UGT-mediated glucuronidation of most prescribed drugs (> 55%) and clinical evidence of UGT-associated drug resistance are major concerns for therapeutic development. While UGTs are highly conserved enzymes, they manifest unique substrate and inhibitor specificity which is poorly understood given the dearth of experimentally determined full-length structures.

Molecular Docking Analysis of Siddha Formulation Parangipattai Chooranam Against Vaginal Candidiasis.

Vulvovaginal candidiasis called by its name Vellai Noi as per Siddha terminology is considerably the second most common cause of vaginal inflammation in the women of middle-aged group. Candida albicans are prioritised top among other pathogens in mediating vaginal inflammation and its related symptoms. Candida albicans exerts its virulence by secreting the enzyme known as secreted aspartyl proteinases (SAP) which allows hassle-free adherence and growth of the opportunistic pathogen.

Modified RURS Elbow Guard: An Alternative Approach for Thumb Sucking.

Digit sucking or thumb sucking is one of the most common habits usually seen in children. These habits habitually lapse in mid-childhood. The continued persistence of these habits will bring about harmful unbalanced pressures to alveolar ridges, changes in the position of teeth, and occlusion which may result in abnormality if they are continued for a long time.

Translation and validation of oral health impact profile-14 questionnaire into Indian sign language for hearing-impaired individuals.

Objectives: To translate and cross-culturally adapt the oral health impact profile-14 (OHIP-14) questionnaire into Indian sign language (ISL) using a video format and to evaluate its psychometric properties.

Methods: The study was conducted among hearing-impaired individuals attending the National Institute of Speech and Hearing, Thiruvananthapuram, Kerala. The OHIP-14 was translated to ISL in a video format.

Iridium-catalyzed direct C-H arylation of cyclic -sulfonyl ketimines with arylsiloxanes at ambient temperature.

An iridium-catalyzed ortho-selective C-H arylation of cyclic N-sulfonyl ketimines has been achieved with environmentally benign aryl siloxanes. The reaction is highly efficient and proceeds at ambient temperature which is the key feature of the methodology considering the weak coordination nature of the substrate as well as the sluggish reactivity of siloxanes. A wide array of pharmaceutically relevant novel biaryls has been synthesized under operationally simple conditions.

Work-life Balance among Karnataka State Road Transport Corporation (KSRTC) Workers in Anekal Town, South India.

Context: Buses take up more than 90% of public transport in Indian cities and serve as a cheap and convenient mode of transport for all classes of society. However, the well-being of employees of this mode of transport is paramount in passenger and personal safety. As in any job, the person has to balance work and personal issues.

Screening for Mental Health Disorders among Pregnant Women Availing Antenatal Care at a Government Maternity Hospital in Bengaluru City.

Introduction: Antepartum anxiety and depression are two of the most common risk factors for the development of postpartum depression. Women are at a higher risk of developing depression and suffering from mental disorders during pregnancy and the postnatal period. Psychopathological symptoms during pregnancy have physiological consequences for the fetus, such as impaired blood flow leading to low birth weight, as well as cognitive delay and behavioral problems.

Finger nail creatinine and its role in confirming chronicity of renal failure.

It is often difficult to differentiate acute renal failure (ARF) from chronic renal failure (CRF) when the patient presents with advanced uremia for the first time. Assessments of kidney size, history of nocturia, and pallor are used as indirect indicators of CRF. Some investigators have proposed an estimation of finger nail creatinine concentrations to differentiate between ARF and CRF, as patients with CRF have higher nail creatinine concentrations.

Synthesis, growth and vibrational spectroscopic study of a novel coumarinoylthiazole.

An efficient route was developed for the synthesis of novel 3-(2-morpholinyl-4-phenylthiazol-5-oyl)coumarin (MPTC). FT-IR spectrum of MPTC was recorded and analyzed. The crystal structure data are also described.

A polyherbal ayurvedic drug--Indukantha Ghritha as an adjuvant to cancer chemotherapy via immunomodulation.

Indukantha Ghritha (IG) is a polyherbal preparation consisting of 17 plant components widely prescribed by ayurvedic physicians for various ailments. Though it is a known ayurvedic drug, no attempt has been made to scientifically validate its mechanism of action. Preliminary studies in our laboratory showed IG to possess considerable immunomodulatory effects with a Th1 type of immune response.

Guillain-Barre syndrome following dengue fever.

Guillain-Barre syndrome is a post infectious polyradiculoneuropathy. It is equally prevalent in both the adult and the pediatric populations. Guillain-Barre syndrome following dengue fever is not a classically described entity and has not been reported in children.

Loss of dendritic connectivity in CA1, CA2, and CA3 neurons in hippocampus in rat under aluminum toxicity: antidotal effect of pyridoxine.

Aluminum chloride (AlCl(3); 4 mg/kg) was injected into the cerebrospinal fluid of adult rats as a one time dose. Rapid Golgi stained sections of hippocampus were examined for detailed histology of neurons in CA1, CA2, and CA3 areas. The axonal length and number of dendritic branches were seen reduced 30 days later in aluminum (Al)-injected group when compared to vehicle-injected controls.

An epidemic of poliomyelitis in southern Kerala.

An epidemic of poliomyelitis was recognized in May 1987 when there was a sharp increase in the number of children with acute paralytic poliomyelitis admitted to the SAT Hospital in Trivandrum in Kerala State. From May through September, 392 cases were admitted; the total admitted cases in 1987 were 458 in contrast to 119 in 1986. Evidence for type 1 poliovirus infection was found in 33 (85%) of the 39 children in whom virological investigations were done during the epidemic.