35 research outputs found
Development of cucurbocitrin based nutraceutical formulation: A potential adjuvant herbal therapy in the management of hypertension
Nearly half of the hypertensive patients fail to manage their blood pressure despite pharmacological interventions, which reflects the dire need for adjuvant anti-hypertensive therapies. Nutraceutical formulations are attractive in this regard owing to their efficacy, ease of availability, and moderate pricing. The current investigation involves the formulation of cucurbocitrin nutraceutical tablets by direct compression method and evaluated for its anti-hypertensive effect in the management of hypertension. Cucurbocitrin is a natural compound prepared from Citrullus lanatus seeds belonging to the family Cucurbitaceae. The powder blend was examined for pre-compression studies such as angle of repose, bulk density, tapped density, Carrās index, Hausner's ratio, etc. Based on acute-oral toxicity results, two tablet formulations were prepared using a different dose of cucurbocitrin and evaluated for post-compression parameters such as friability, hardness, weight variation, disintegration time, and in vitro drug release studies. In vivo studies were also performed for both formulations using a 10% Glucose solution-induced hypertension model in albino rats to observe its anti-hypertensive activity. The study indicated that nutraceutical formulation was found to be effective in reducing hypertension in an animal model
PHAROH lncRNA regulates Myc translation in hepatocellular carcinoma via sequestering TIAR.
Hepatocellular carcinoma, the most common type of liver malignancy, is one of the most lethal forms of cancer. We identified a long non-coding RNA, Gm19705, that is over-expressed in hepatocellular carcinoma and mouse embryonic stem cells. We named this RNA Pluripotency and Hepatocyte Associated RNA Overexpressed in HCC, or PHAROH. Depletion of PHAROH impacts cell proliferation and migration, which can be rescued by ectopic expression of PHAROH. RNA-seq analysis of PHAROH knockouts revealed that a large number of genes with decreased expression contain a Myc motif in their promoter. MYC is decreased at the protein level, but not the mRNA level. RNA-antisense pulldown identified nucleolysin TIAR, a translational repressor, to bind to a 71-nt hairpin within PHAROH, sequestration of which increases MYC translation. In summary, our data suggest that PHAROH regulates MYC translation by sequestering TIAR and as such represents a potentially exciting diagnostic or therapeutic target in hepatocellular carcinoma
Implementing Decision Tree for Software Development Effort Estimation of Software Project
ABSTRACT: Effort estimation is one of the biggest problems faced by software industry. In software planning estimation of the effort is one of the most critical responsibilities. It is necessary to have good effort estimation in order to conduct well budget. The accuracy of the effort estimation of software projects is vital for the competitiveness of software companies. For the forecasting of software effort, it is important to select the correct software effort estimation techniques. Inaccurate effort estimation can be risky to an IT industry's economics and certainty due to poor quality or trait and stakeholder's disapproval with the software product. This paper presents M5P decision tree Technique, for effort evaluation in the field of software development
Possibility of the Existence of DonorāAcceptor Interactions in Bis(azole)amines: An Electronic Structure Analysis
Donor-stabilized
divalent NĀ(I) systems have recently gained attention
in the field of organic chemistry. Existence of low-valent nitrogenĀ(I)
species with moderate nucleophilicities in several pharmacophoric
functionalities is prompting extensive exploration in this field.
Quantum chemical analysis on the imidazole, oxazole, and thiazole
derivatives of thiazole-2-amine indicated that these species preferably
exist in the iminic state. Electronic structure analysis of these
systems suggested the existence of hidden divalent NĀ(I) character
in a neutral state (L ā NāR) and the explicit divalent
NĀ(I) character (L ā N ā L)<sup>+</sup> in the protonated
state. The strength of L ā N interaction in these systems was
analyzed, and the variations in the nucleophilicity trend at the coordinating
nitrogen center were rationalized by estimating the electronic (TEP
(Tolman electronic parameter) and MESP minimum (<i>V</i><sub>min</sub>)) as well as steric parameters (<i>r</i>-repulsiveness and Ī<i>H</i> elimination of CO group,
in L ā NiĀ(CO)<sub>3</sub>) of the coordinating ligands L. The
importance of energetically preferred ionic and tautomeric representations
of thiazol-2-amine derivatives in iminic and aminic forms was also
demonstrated by carrying out comparative docking analysis with the
enzyme lymphocyte-specific kinase (Lck)
Battle Against Coronavirus: Repurposing Old Friends (Food Borne Polyphenols) for New Enemy (COVID-19)
In
the era of extreme scientific development where the scientific community have
reached beyond moon, the entire world today is facing an immense problem due to
deadly effect of COVID-19 (coronavirus disease), originated in Wuhan.
Coronavirus is having dexterity to target immune compromised people very easily
and swiftly get transmitted to healthy individuals from infected ones.
Coronavirus infections are spreading very rapidly, and almost all the countries
around the world are having corona positive people and asymptomatic carriers. This
pandemic has created havoc both to human health and economy in lack of an
effective treatment against this disease. Due to time limitations and urgency
to find cure for COVID 19 we have undertaken the help of structure assisted
drug design approach which mainly involves virtual screening program which
identifies the structural leads which can target COVID-19 main protease (Mpro).
This protease is the key enzyme of coronavirus which plays crucial role in
virus replication and transcription, which can be targeted to retard the growth
of virus inside the host. In the
present work, the Phenol explorer database (version 3.6) containing 751
different food borne polyphenols were screened against the (Mpro) to identify suitable structural leads
with potential to inhibit this protease though High throughput modelling and
molecular docking approach. We identified six potential polyphenols belonging
to Sanguiin, Theaflavin gallate, Theaflavin digallate, Kaempferol,
Punicalagin and Protocatechuic acid chemical classes. All the six polyphenols
have much higher docking scores ā„ -9.8 kcal/mol as compared to peptidomimetic
inhibitor (N3) of COVID 19 virus Mpro. Pharmacokinetic and Drug
likeness predictions of these polyphenols were done using SwissADME web tool
where Protocatechuic acid shown fairly good results (1 Lipinski violation). The
studies suggest the dietary intake of āblack teaā can improve the
resistance to fight against COVID 19 virus in early stages of human infection. Importantly though, the enriched subset of six
compounds identified from the larger library has to be validated experimentally. </p