18 research outputs found

    OTX015 PROTACs: Emerging Novel Therapeutic Agents in Cancer Treatment

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    Cancer is a wide-spreading disease. Its count goes on increasing and became the second leading cause of death in respect of diseases. New cancer-targeting molecules are explored. In this study, we tried to collect information about one such molecule, OTX015. Articles were searched across reputed search engines and publishers such as Cochrane, EMBASE, The Lancet, PubMed, GoogleScholar, ScienceDirect, Wiley Online, Springer and Bentham Science by using different keywords: “OTX015”, “Cancer”, “Small molecule PROTACs”, “BRD/BET” and “BET inhibitors”. The quality papers were retrieved, studied, categorized into different sections, analyzed, and used for article writing.OTX015 is a novel molecule in clinical trials. It showed some promising results in various cancers as well as other diseases like latent-HIV with the least side-effects.This article will give an insight into Small Molecules as PROTACs, their advantages and disadvantages, OTX015 and its PROTAC ARV- 825. It is advised that more research/studies are required to be carried out to know more about OTX015 and other PROTACs, their advancements, receptors, and mechanism/ mode of action to know their abilities to work against proteins involving diseases

    Exploring the Potential of Curry Leaves for their Therapeutic Action

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    Curry leaves (Murryakoenigii), which are valued for their aromatic flavour, have been mainstay of Indian cuisine for ages. These leaves are becoming more well known for their potential to affect metabolic pathways in additional to their gastronomic value. The molecular mechanistic potential of curry leaves in relation to metabolic control is examined in this abstract. Curry leaves contain a variety of bioactive substance, such as antioxidant, anti-inflammatory agent, and substance that modulate insulin sensitivity, which have potential to have an effect on crucial metabolic processes. Their contribution to the management of oxidative stress, inflammation, blood sugar, cholesterol, weight, gut health, liver function, thermogenesis, and appetite regulation is discussed in this work. Although encouraging, more study is necessary to complete clarify the mechanism of action and to determine the efficacy of curry leaves in metabolic disorder

    Current Opinion on Food Sustainability for Liver Associated Health Problems: Facts and Myths with Case Study

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    The liver is the second-largest organ in our body which separates the nutrients and waste as they move through our biological process system and it additionally produces bile, a substance that carries toxins out of your body and aids in digestion. There are several myths associated with liver spread amongst masses. It is a vital necessity to make society devoid of such myths and aware of the real scenario. This review aimed to summarize the different facts and myths associated with health problems of liver and highlight the importance of food sustainability approach with the help of some case studies. A comprehensive literature search was conducted using various databases between 2006 and 2022 that focused on the various facts and myths associated with liver related health issues. Myths create nothing but false notions and fear amongst people. Some case studies were summarized to clear all the conflict statements commonly related with liver diseases in the society. Myths like nothing other than water is considered a good beverage for the liver, but recent studies have proven that measured quantities of coffee and herbal tea intake is healthy for the body. Additionally, coffee has a protective effect on the organ liver. Similarly, hepatitis can spread through casual contacts. Although it is proven that hepatitis B, C and autoimmune hepatitis, do not spread on having casual contact or sharing food and drink. A substantial myth states that blood tests can detect problems associated with the liver, but doctors rarely suggest blood tests for liver functioning. This review is focused to resolve several myths associated with the liver which are often considered true by masses

    Antimicrobial Activity of Secondary Metabolites in Medicinal Plants: An Update

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    Plants have filled in as a significant wellspring of elements for conventional drugs for centuries. Verifiable records and present day ethno botanical field examines feature their significance in the conventional treatment of irresistible malady. Be that as it may, plants form just a minor level of present collection of FDA-endorsed antimicrobial medications. The present article gives an outline of active components of plants as hint for other wellspring of antimicrobial agents to be used in the battle against microscopic organisms. It additionally surveys the ethno botanical way to deal with sedate disclosure and talks about various inventive focuses for future medication revelation endeavours in this field. Without an uncertainty, antimicrobials are miracle tranquilizers. They have represented a very long time against different irresistible infections and spared a huge number of lives. The ongoing disappointment of antimicrobials because of the sensational rise of multidrug-safe microbes and fast spread of new diseases, be that as it may, prompts wellbeing associations and the pharmaceutical business worldwide to change their methodology and to expand improvement of antimicrobials against quickly rising anti-infection safe microorganisms. In spite of the fact that there is thinking about elective wellsprings of characteristic antimicrobial molecules from plants having different methods of activity, some of which have been utilized in regular medication for a considerable length of time and have appeared to have serious impacts contrasted with other antimicrobials. This examination portrays plant intensity as an elective hotspot for antimicrobial agents

    Exploration of Baicalin analogues against main Protease involved in Covid-19 as potential inhibitors involving in silico approaches

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    The proteolytic enzymesinvolved in the processing and replication of coronavirus serve a promising drug targetsfor coronavirus. Although a few numbers of vaccines have been made available, there is a great need for effective treatment to manageit. The current study involved the exploration of baicalin analogues as potential inhibitor of viral proteolytic enzyme. Utilizing various computational tools (scaffold morphing, molecular docking and pharmacokinetic studies), the B74 and B86 analogueswere screened as potential inhibitors of main protease. Accordingly, these analogues can be explored further in the search of promising therapy against the coronavirus infection

    Investigating Holistic Natural Strategies for The Management of Huntington's Disease

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    Huntington's disease (HD), a multifaceted neurological disorder, presents a complex clinical scenario. An autosomal dominant neurodegenerative ailment called Huntington's disease is brought on by increase in number of CAG (Cytosine-Adenine-Guanine) repeats, which causes the creation of a mutant Huntingtin protein (mHTT) resulting in neuronal death and mental disabilities in human beings. End signs and symptoms can include significant weight loss, difficulty swallowing or breathing, recurrent aspiration pneumonia, declined health and uncontrolled pain. The excessive production of ROS (Reactive Oxygen Species) in nervous tissues is considered a significant risk factor in most of the neurological diseases including HD. Transcriptional regulation, immunological system, and mitochondrial function are all disrupted by mHTT. Although natural products have shown promise in ameliorating symptoms, it is important to note that no singular "phytoconstituent" has been definitively linked to its therapeutic intervention. Nevertheless, certain naturally occurring compounds have exhibited promising outcomes in preclinical investigations. This article focuses on a few phytoconstituents that are known to have a variety of neuroprotective effects through a wide range of biological activities. By stimulating the Nrf2 (Nuclear factor erythroid 2-related factor) pathway and suppressing NF-κB (Nuclear Factor Kappa-light-chain-enhancer of activated B cells), astaxanthin, berberine, and sulfarophane increase the antioxidant and anti-inflammatory activity, resulting in neuroprotection. Curcumin leads to metal chelating effect and decline in reactive oxygen species which are certainly one among the vital processes to impede and manage the disorders causing neurodegeneration including HD. This affects the upregulation of HSPs (Heat Shock Proteins) which helps in HD management. Naringin reduces level of oxidative stress and inflammation by free radical scavenging, NF-κB stimulates cell survival and prevents apoptosis by upregulating anti-apoptotic genes expression and downregulating proapoptotic genes

    A Scoping Review and Preliminary Illustrative Analysis of Biomarkers in Stress-Related Psychiatric Illness: Diagnostic and Prognostic Implications

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    Stress is the body's response to any changes that might place it under mental, emotional, or physical strain and could either demand attention or prompt action. A stress reaction can be brought on by both internal and external factors. The conditions, demands, issues, and expectations you deal with every day are all regarded as external influences, as are your physical surroundings, your job, your contacts with others, your family, and all other related factors. The ability of your body to respond to and handle external stimuli depends on internal factors. Your ability to handle stress is influenced internally by your food habits, level of general health and fitness, mental health, and the amount of sleep and rest you get. Such demanding conditions could affect how certain stress hormone levels are regulated. Biomarkers such as mGlu2/3, 5-hydroxyindoleacetic acid (5-HIAA), serum alpha-amylase, amygdala reactivity, neuropeptide Y (NPY), heat shock proteins, cortisol, and catecholamines are used to assess the hormone imbalance. Disease prevention, early detection, and therapy are all possible uses for biomarkers. In this review, we looked at a wide range of stress-related biomarkers that might cause different psychiatric illnesses and how those conditions can, over time, alter a person's lifestyle

    Green chemistry and catalysis: An emerging sustainable approach in synthetic chemistry

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    This tutorial review summarizes the basic new concepts of green chemistry in relation to education and pharmaceutical industries. The origin and history of Green analytical chemistry is described in detail. Basic twelve principles are well summarized with suitable examples of each principle such as oxidation of alcohol, enzymatic reactions, and non-covalent derivatization. This article also covers the concept of E-factor for waste minimization, detailed various solvent selection guidelines and tools for betterment of synthetic pathways at laboratory and industrial level. The efficiency of green chemistry in organic synthesis for greenness of traditional organic synthesis methods are discussed. Nowadays, there is a constant need to add catalysts for chemical synthesis to minimize or downsize the risks correspondent with chemical manufacture. Catalyst helps to enhance air quality by reducing harmful gas emissions such as NOx. It cuts down on the use of VOCs (volatile organic compounds). It developed an alternative catalytic method which substitutes the usage of chlorine-based intermediates in chemical synthesis and processes. Biocatalysts is a term used to describe compounds that aid in the stimulation of biological reactions. In the fine chemical industry, cleaner biocatalytic alternatives are replacing traditional chemical operations

    IDENTIFICATION OF NOVEL 5-STYRYL-1,2,4-OXADIAZOLE/TRIAZOLE DERIVATIVES AS THE POTENTIAL ANTI-ANDROGENS THROUGH MOLECULAR DOCKING STUDY

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    Objective: To identify the novel and simple bioactive antiandrogens, that can overcome to side effects as well as drug resistance.Methods: The AutoDock Vina (ADT) 1.5.6 software is used for molecular docking purposes. The molecular structures were drawn in ChemBiodraw ultra and by the help of ChemBiodraw 3D, all structures were energy minimized by MM2 method and converted to pdb extension file which is readable at the ADT interface.Results: Total ten compounds from both series were shown better binding affinity than R-bicalutamide including oxadiazole and triazole series. Among these pk42 and pk46 were studied in-depth which showed best binding affinity to the androgen receptor. The cis-isomers were found better than their trans-isomer.Conclusion: Novel 5-styryl-1,2,4-oxadiazole/triazole derivatives were studied through molecular modeling using Autodock Vina. The potent compounds which showed better binding affinity than R-bicalutamide like pk24 and 46 were further analyzed for their interactions. The conformational effect also found significant in binding to the androgen receptor

    Identification of Novel Coixol-Based Derivatives as the Potential Anti-diabetic Agents Through Molecular Docking Studies

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    Objective: The objective of this study was to design and identify the novel promising anti-diabetic agents based on the naturally existing potent insulin secretagogue coixol that can improve the potency overcome the adverse effects of existing medicines. Methods: The Auto Dock Vina (ADT) 1.5.6 and PyMOL software were used for molecular docking and visualization purposes. The molecular structures were drawn in Chem Draw 16.0 and by the help of Chem Bio draw three dimensions, all structures were energy minimized by MM2 method and converted to PDB extension file which is readable at the ADT interface. Result: Total 254 designed molecules from each series 1–4 were checked for binding score with the receptor 5yw7. Out of that total 12 molecules from each series were selected on the basis of their binding affinity in each series. Among these coixol (Natural product), DP322, DP330, and DP422 were studied in-depth. Conclusion: Coixol-based derivatives which scored best binding affinity such as DP332, DP330, and DP422 were shown promising result on the interaction with the K+ ATP sensitive Potassium channel protein (5yw7). The entire study suggests that these novel coixol-based derived molecules could be a promising lead for the further discovery and investigation of insulin sensitizing agents for the treatment of diabetes
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