Synthesis and screening of clerodane diterpene analogues from 16 hydroxycleroda 3,13(14)-Z-diene 15,16-olide for potential anti-mycobacterial activity.

In recent years, clerodane diterpenes, a class of bioactive compounds, have come into the spotlight due to their amazing bioactivities. Three novel clerodane diterpene analogues were obtained by synthesising 16-hydroxycleroda-3,13(14)-Z-diene-15,16-olide (Lactone) with primary amines. Anti-tubercular activity was determined using Microplate Alamar Blue Assay. Among all the synthesised compounds from methanolic extract of seeds, results clearly showed that compounds 3 and 5 have significant anti TB activity with an MIC of 1.56 µg/ml against the Mycobacterium tuberculosis MTB H37Rv bacilli strain than the gold standard drugs pyrazinamide (3.13 µg/ml), ciprofloxacin (3.13 µg/ml), streptomycin (6.25 µg/ml) and rifampicin (6.25 µg/ml). Compound 5 exhibited significant antibacterial activity with zone of inhibition of 10.8 mm with Gram + ve and 7.95 mm with Gram -ve bacteria at a conc of 50 µg/ml respectively. In the current investigation, three novel heterocycles (compounds 3-5) of the diterpenoid were prepared, in high yield, using one-pot, efficient approach.

Data health risk assessment of nitrate contamination in groundwater of rural region in the Yerraguntla Mandal, South India.

The main objective of the present study was to determine the distribution levels of nitrate contamination in groundwater and its associated impact on human health risk in the Yerraguntla mandal, South India. For this 40 ground water samples were collected randomly during April 2018. Nitrate concentration in groundwater samples ranged from 2.50 to 760.12 mg/L, with a mean value of 86.13 mg/L. Most of the groundwater samples are exceeding the permissible limits of nitrate (45 mg/l). Hence health risk assessment of nitrate has been carried out. Hazard quotient (HQ) values for infants, children, male and female ranges from 0.05 to 14.25; 0.06 to 18.53; 0.04 to 12.18 and 0.05 to 14.62, respectively. The finding of data showed that HQ value was more than 1 in 42.5% of samples in groups of infants, children and female, and 35% of samples in group of male.

Data on physical impacts and hydrogeochemical assessment of inactive/abandoned mines in and around Southwestern parts of the Cuddapah basin using a conceptual site model (CSM).

The conceptual site model (CSM) has been designed for Inactive/abandoned mines in the SW part of Cuddapah basin, which gives an overview of Inactive/abandoned mine characterization in terms of physical impacts such as vertical openings, dangerous impoundments, location of steep slopes, waste processing facilities, steep portal abandoned barite mine and assessment of groundwater analytical data. To evaluate the groundwater quality and its suitability for domestic, drinking purposes, 44 groundwater samples were collected from the southwestern part of the Cuddapah basin, were examined for major cations and anions. The suitability of groundwater for drinking purposes is assessed by comparing with the World Health Organization (W.H.O) and Indian standards (IS).

Data on application of water quality index method for appraisal of water quality in around cement industrial corridor, Yerraguntla Mandal, Y.S.R District, A.P South India.

The present paper aims at determining the status and trends of groundwater quality by applying water quality index method from 22 villages around Cement industries, Yerraguntla Mandal, Y.S.R District, A. P South India. Water Quality Index (WQI) was calculated from fourteen physicochemical parameters like pH, EC, TDS, Total hardness, Total alkalinity, Sodium, potassium, Calcium, Magnesium, chloride, Bromide, nitrate, sulphate and fluoride. The computed WQI values range from 123 to 1121 and water quality varies from poor water to water unsuitable for drinking. Most of the groundwater from this place is not suitable for drinking.

Data on water quality index development for groundwater quality assessment from Obulavaripalli Mandal, YSR district, A.P India.

Groundwater is a vital resource for most developmental activities. Demand for groundwater is increasing due to paucity of surface water and recurrent failures of monsoons. Increasing demand for groundwater causes water level to decline and water quality to deteriorate. This data article is aimed to investigate the quality of drinking water of Obulavaripalli Mandal YSR district based on water quality Index (WQI). To evaluate WQI in the study area, twenty groundwater samples were collected and different physico-chemical parameters viz., pH, EC, TDS, TH, total alkalinity (TA), calcium (Ca2+), magnesium (Mg2+), chloride (Cl-), sulphate (SO4 2-) and fluoride (F-) were analyzed. WQI data for groundwater samples indicated that 30% of the samples fall under excellent rating, 40% of the samples fall under good category and another 30% of the groundwater is under poor category. Overall groundwater quality is not suitable for drinking purpose.

Adenosine receptors as targets for therapeutic intervention.

The synchronous occurrence of primary renal cell carcinoma with gastric cancer is very rare. We report a case of 41 year old male who presented on 05/07/2011 to M S Ramaiah hospital, Bangalore with history of fever, pain abdomen and malena. Ultrasound abdomen and pelvis showed large heterogenous mass arising from the upper pole of left kidney. Computed tomography of the abdomen showed left renal cell carcinoma. Renal biopsy showed features consistent with renal cell carcinoma - clear cell type. Oesophagogastroduodenoscopy revealed gastric polypoidal growth. Gastric biopsy from the growth revealed poorly differentiated adenocarcinoma of stomach. We report this case to highlight a rare occurrence of synchronous malignancy of stomach and kidney.

Sirtuins: the future insight.

Sirtuins are evolutionary conserved NAD+ dependent acetyl-lysine deacetylases and ADP ribosyltransferases dual-function enzymes involved in the regulation of metabolism and lifespan. Sirtuins represent a promising new class of III NAD dependent histone deacetylases that regulate a number of physiological processes, originally identified in yeast. Sirtuins regulate various normal and abnormal cellular and metabolic processes, including tumorgenesis, neurodegeneration and processes associated with type 2 diabetes and obesity. Several age-related diseases such as Alzheimer's disease and longevity have also been linked to the functions of sirtuins. Because of these associations, the identification of small molecules sirtuin modulators has been of significant interest.

Drug-receptor interactions.

In present-day pharmacology and medicine, it is usually taken for granted that cells contain a host of highly specific receptors. Drugs act on the cell membrane by physical and/or chemical interactions. This is usually through specific drug receptor sites known to be located on the membrane. These are defined as proteins on or within the cell that bind with specificity to particular drugs, chemical messenger substances or hormones and mediate their effects on the body. Today, the concept of specific receptors for drugs and transmitters lies at the very heart of pharmacology. However, it is only relatively recently that the notion of drug-specific receptors has become widely accepted, with considerable doubts being expressed about their existence as late as the 1960s.

Prevalence of attention deficit disorder among preschool age children.

Attention deficit hyperactivity disorder (ADHD) is one of the most common childhood onset psychiatric disorders. Although the onset of ADHD is prior to the age of seven years, there is a paucity of data on the prevalence of the disorder in preschool age children. This study was performed to determine the prevalence rate of ADHD in preschool age children in kindergartens of south west, Mumbai. One thousand two hundred fifty (599 males and 651 females) children aged between 4-6 years, were selected from 40 kindergartens in 6 localities in south west Mumbai. The Conner's index questionnaire was completed for each child by teachers and parents. Parents of children whose scores were positive for ADHD (>15) were interviewed by a psychiatrist and the ADHD was diagnosed based on DSM-IV criteria Schedule for affective disorders. One hundred fifty two (12.2%) children were diagnosed to have ADHD. The prevalence of ADHD in preschool age school in south west of Mumbai is consistent with previous studies in other countries. This study recommends the need for diagnosis and treatment of ADHD in preschool age children.

Role of pharmacogenomics in the drug development.

Individuals respond differently to drugs and sometimes the effects are unpredictable. Differences in DNA that alter the expression or function of proteins targeted by drugs can contribute significantly to the variation in the individuals responses. The use of pharmacogenomics is to identify genetic polymorphisms that predispose patients to adverse drug effects that, although they may occur in only a small subset of the people treated with a new medication, are sufficiently toxic to jeopardise further development of the drug for all patients. Given the potential value of knowing all the possible factors that influence the effects of new agents, it is likely that pharmacogenomics will have an increasingly important role in drug discovery and development. This article briefly reviews concepts that underlie the emerging fields of pharmacogenetics and pharmacogenomics, with an emphasis on the pharmacogenetics of drug metabolism. Although only a few examples will be provided to illustrate concepts and to demonstrate the potential contribution of pharmacogenetics to medical practice, it is now clear that virtually every pathway of drug metabolism will eventually be found to have genetic variation.

Delusional parasitosis--study of 3 cases.

Delusional disorder-somatic (parasitosis) type is a rare psychiatric disorder which poses a challenge to diagnostic and therapeutic skills. Pimozide, a highly specific dopamine blocker has shown promising results in the 3 cases illustrated here. These cases were seen over a period of 3 years. All the three patients believed that an insect has entered through the ear and is burrowing tracts/laying multiple eggs. They approached the ENT surgeons or neurosurgeon with a fear that their brain will be invaded. On psychiatric evaluation, no past or present history of major psychiatric illness was found. Premorbid personalities were well adjusted. Only for two patients, acute moderate stressors were detected. Delusions disappeared by the end of 2 wks but therapy was continued for 5 months.