Enantiospecific Synthesis Of Bioactive Styryllactones

The thesis entitled “Enantiospecific synthesis of bio-active stryllactones” comprise an introduction about stryllactone and two chapters describes the synthesis of stryllactones. Trees of the genus Goniothalamus of the plant family Annonaceae in South East Asia has been known for a long time for their proven as folkloric medicine. Stryryllactones were found to exhibit moderate to significant biological activity including antitumour, antifungal as well as antibiotic properties. Because of their unique and intriguing structures and the activity associated much effort has been centered on the development of methodology for the synthesis of these compounds. The structures and relative configurations of these compounds were determined either by X-ray crystallography or by extensive NMR spectral analysis and by mass spectroscopic techniques. The research group of McLaughlin isolated and characterized a series of styryllactones, possessing significant to marginal cytotoxic activity against human tumor cell lines. The structures and relative configurations of these compounds were determined either by X-ray crystallography or by extensive NMR spectral analysis. Classification of these styryllactones is based on the structural characteristics of the six different skeletons as shown in Figure 1. Figure 1:features styryllactone the genus In this thesis, enantioselective total synthesis of styryllactones ()-9-deoxygoniopypyrone 1, ()-goniopypyrone 2, ()-7-epi-goniofufurone 3, ()-7-epigoniodiol 4 and the putative structure of ()-etharvendiol 5 is presented. a) Total synthesis of ()-9-deoxygoniopypyrone, ()-goniopypyrone, ()-7-epigoniofufurone and ()-7-epi-goniodiol: Synthesis of the styrylalctones is relied on elaboration of the trihydroxy ester 11 derived from tartaric acid. Appropriate protection of the hydroxy groups and further modifications of the ester functionality (which can be transformed into the corresponding alcohol or aldehyde) is planned for the synthesis of the styryllactones 1-5. Accordingly, the bis-dimethylamide 9 derived from D-()-tartaric acid, was transformed to the -hydroxy amide 10 using a combination of Grignard reagent addition followed by reduction of the resultant ketone. Acid mediated deprotection of the acetonide with concomitant hydrolysis of the amide to the ester is accomplished in one pot by treating 10 with p-TSA in benzene/MeOH mixture Treatment of the trihydroxy ester with 2,2-dimethoxy propane in presence of p-TSA afforded the hydroxy ester 12 which was elaborated to the styrylalctones 9deoxygoniopypyrone, 7-epi-goniodiol, 7-epi-goniofufurone and goniopypyrone (Scheme-2). (Part of this work is published: Prasad, K. R.; Dhaware, M.G. Synlett. 2007, 11121114.; Prasad, K.R.; Dhaware, M.G. Synthesis 2007, 3697) b) Stereoselective synthesis of the putative structure of (+)-etharvendiol: In 1997, Bermejo et al isolated the styryl pyrone etharvendiol 5 from the ethanolic extract of stem bark from Goniothalamus arvensis. Hitherto, no synthesis of etharvendiol is reported in the literature. In this section, approach towards the synthesis of putative structure of etharvendiol will be discussed. Synthesis of etharvendiol 5 is anticipated by the elaboration of masked tetrol 15, comprising an alkene tether and four contiguous hydroxy groups installed with definite configuration. It is relied on exploiting the hydroxy directed lactonization via the oxidation of alkene in 15, and subsequent elaboration to 7. Bis-dimethylamide 9, derived from D-()-tartaric acid was identified as the suitable precursor for the synthesis of 15. Synthesis of masked tetrol 15 is accomplished from 9 involving a combination of selective Grignard additions and stereoselective reduction (Scheme 3). (For structural formula pl see the pdf file

Influence of Genetic and Non-genetic Factors on Fecal and Haemonchus Egg Counts in Osmanabadi Goats (Capra hircus) in Arid and Semi-arid Regions of Maharashtra

Osmanabadi goats (Capra hircus) are reared in arid and semi arid region of India and play a role in economy of rural livelihood. Small ruminant practices in India faces major challenges of parasitic infestation hence, present study was carried out to see the effect of different genetic and non genetic factors on parasitic load of these goats in Udgir tehsil of Latur district of Maharashtra. The variation due to season, age, sex, farm and genotype of TaqI locus of MHC DRB1 gene on Fecal Egg Count (FEC) and Haemonchus Egg Count (HEC) in the flocks was studied. The study comprised of 84 animals and it was seen that the season and genotype were the significant factors affecting FEC and HEC in these flocks reared in organized and non-organized farm. The BB genotype had the lowest FEC suggesting that the BB genotype might be resistant to parasitic load

Predictive Data Analytics Framework Based on Heart Healthcare System (HHS) Using Machine Learning

Cardiovascular diseases (CVD) have recently outdid all other reasons of death universal in both developing and developed nations. Initial detection of cardiac conditions and continuing therapeutic supervision by experts can lower the death rate. However, accurate diagnosis of cardiac issues in all circumstances and 24-hour patient consultation by a doctor are still not feasible due to the increased intellect, effort, and expertise required. In this study, a basic concept for an Machine Learning (ML)-based heart disease prediction system was presented to identify impending heart disease using Machine Learning techniques. Despite the increasing number of empirical studies in this topic, particularly from underdeveloped countries, here lack many synthesised research articles in the field. In a time when the amount of data available is constantly increasing, predictive analytics has become more and more important as a tool for heart welfare services and human protection.  By utilising data collected from previous events to predict future patterns and outcomes, this state-of-the-art technology assists heart-care agencies in making more informed decisions about how to best serve their clients. However, as with any other data-driven technology, predictive analytics must be used appropriately to guarantee effective and ethical business operations. Healthcare forecasting has gained importance in recent years due to the growing popularity of AI (Artificial Intelligence) and ML (Machine Learning). In the healthcare sector, forecasting can also aid physicians in providing more precise and timely diagnoses. By anticipating likely medical events, medical staff can identify and treat individuals with greater efficiency and precision. This could lead to better patient outcomes and even cost savings.  These systems provide excellent therapeutic support and have the ability to diagnose illnesses by mimicking human cognition.  This study's included studies focus on forecasting the heart healthcare system (HHS) using machine learning algorithms. We implemented the system using the K-means Elbow technique for registration and notification, a decision tree for HHS, and MySQL for immunisation reminders

Determination of Toxic Metals in Indian Smokeless Tobacco Products

This study targets the lesser-known ingredients of smokeless tobacco products, i.e., the toxic metals, in Indian brands. The metals selected in the study included lead (Pb), cadmium (Cd), arsenic (As), copper (Cu), mercury (Hg), and selenium (Se). The differential pulse anodic stripping voltammetry (DPASV) technique was used for estimating the metals Pb, Cd, and Cu; square wave voltammetry for As; and the cold vapor atomic absorption technique for Hg. The resulting levels of the metals were compared to the daily consumption of the smokeless tobacco products. It was observed that almost 30% of gutkha brand samples exceeded the permissible levels of metals Pb and Cu, when compared to the provisional tolerable intake limits determined by the FAO/WHO. The reliability of data was assured by analyzing standard reference materials

Comprehensive evaluation of candidate reference genes for real-time quantitative PCR (RT-qPCR) data normalization in nutri-cereal finger millet [Eleusine Coracana (L.)]

Finger millet (Eleusine coracana L.) is an annual herbaceous self-pollinating C4 cereal crop of the arid and semi-arid regions of the world. Finger millet is a food security crop proven to have resilience to changing climate and scores very high in nutrition. In the current study, we have assessed sixteen candidate reference genes for their appropriateness for the normalization studies in finger millet subjected to experimental regimes and treatments. Ten candidate reference genes (GAPDH, β-TUB, CYP, EIF4α, TIP41, UBC, G6PD, S24, MACP and MDH) were cloned and six (ACT, ELF1α, PP2A, PT, S21 and TFIID) were mined from the NCBI database as well as from the literature. Expression stability ranking of the finger millet reference genes was validated using four different statistical tools i.e., geNorm, NormFinder, BestKeeper, ΔCt and RefFinder. From the study, we endorse MACP, CYP, EIF4α to be most stable candidate reference genes in all ‘tissues’, whereas PT, TFIID, MACP ranked high across genotypes, β-TUB, CYP, ELF1α were found to be best under abiotic stresses and ‘all samples set’. The study recommends using minimum of two reference genes for RT-qPCR data normalizations in finger millet. All in all, CYP, β-TUB, and EF1α, in combination were found to be best for robust normalizations under most experimental conditions. The best and the least stable genes were validated for confirmation by assessing their appropriateness for normalization studies using EcNAC1 gene. The report provides the first comprehensive list of suitable stable candidate reference genes for nutritional rich cereal finger millet that will be advantageous to gene expression studies in this crop

Pearl Millet Aquaporin Gene PgPIP2;6 Improves Abiotic Stress Tolerance in Transgenic Tobacco

Pearl millet [Pennisetum glaucum (L) R. Br.] is an important cereal crop of the semiarid tropics, which can withstand prolonged drought and heat stress. Considering an active involvement of the aquaporin (AQP) genes in water transport and desiccation tolerance besides several basic functions, their potential role in abiotic stress tolerance was systematically characterized and functionally validated. A total of 34 AQP genes from P. glaucum were identified and categorized into four subfamilies, viz., plasma membrane intrinsic proteins (PIPs), tonoplast intrinsic proteins (TIPs), nodulin-26-like intrinsic proteins (NIPs), and small basic intrinsic proteins (SIPs). Sequence analysis revealed that PgAQPs have conserved characters of AQP genes with a closer relationship to sorghum. The PgAQPs were expressed differentially under high vapor pressure deficit (VPD) and progressive drought stresses where the PgPIP2;6 gene showed significant expression under high VPD and drought stress. Transgenic tobacco plants were developed by heterologous expression of the PgPIP2;6 gene and functionally characterized under different abiotic stresses to further unravel their role. Transgenic tobacco plants in the T2 generations displayed restricted transpiration and low root exudation rates in low- and high-VPD conditions. Under progressive drought stress, wild-type (WT) plants showed a quick or faster decline of soil moisture than transgenics. While under heat stress, PgPIP2;6 transgenics showed better adaptation to heat (40C) with high canopy temperature depression (CTD) and low transpiration; under low-temperature stress, they displayed lower transpiration than their non-transgenic counterparts. Cumulatively, lower transpiration rate (Tr), low root exudation rate, declined transpiration, elevated CTD, and lower transpiration indicate that PgPIP2;6 plays a role under abiotic stress tolerance. Since the PgPIP2;6 transgenic plants exhibited better adaptation against major abiotic stresses such as drought, high VPD, heat, and cold stresses by virtue of enhanced transpiration efficiency, it has the potential to engineer abiotic stress tolerance for sustained growth and productivity of crops

Failure Investigation of Primary Suspension Spring of Train Bogie based on Dynamic Analysis

The primary suspension system has a helical compression spring for axial and lateral deformation. The spring absorbs the shock at track curvature. The traditional system uses Chrome Vanadium spring materials that need to be replaced after 70-90 days. The static performance of the spring under different compressive loads is evaluated using finite element analysis. The maximum shear stress is the lowest for the 60Si2MnA material. Since the spring doesn’t fail in static conditions, dynamic analysis is carried out by using finite element analysis. The results given by the FFT analyser excitation frequency and natural frequency are close to each other.</jats:p

Stereoselective total synthesis of bioactive styryllactones: 9-deoxygoniopypyrone, goniopypyrone and 7-epi-goniofufurone

Stereoselective synthesis of the bioactive styryllactones (+)-9-deoxygoniopypyrone, (+)-goniopypyrone and (+)-7-epi-goniofufurone has been achieved from D-(-)-tartaric acid. The key step involves the elaboration of a trihydroxy ester to the title compounds utilizing high-yielding stereoselective transformations