Estrogen receptor alpha (ER-α) antagonistic activity of phytoconstituents from Potentilla atrosanguinea and Potentilla fulgens in breast cancer.

The Potentilla genus has long been used traditionally as food and a folklore medicine. In the present study, aerial parts of two Potentilla species, Potentilla fulgens and Potentilla atrosanguinea, of western Himalayan origin, were studied for their anti-breast cancer activity. Ethyl acetate (PAA-EA, PFA-EA), methanolic (PAA-ME, PFA-ME) and hydro-methanolic extract (PAA-HM, PFA-HM) of the plants were tested for their antiproliferative activities against MCF-7 and T-47D breast cancer cell lines.

Recent Advancement in NMR Based Plant Metabolomics: Techniques, Tools, and Analytical Approaches.

Plant metabolomics, a rapidly advancing field within plant biology, is dedicated to comprehensively exploring the intricate array of small molecules in plant systems. This entails precisely gathering comprehensive chemical data, detecting numerous metabolites, and ensuring accurate molecular identification. Nuclear magnetic resonance (NMR) spectroscopy, with its detailed chemical insights, is crucial in obtaining metabolite profiles.

Design, synthesis, and evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents.

A series of new indole-tetrazole derivatives were designed and synthesized to develop potential anti-breast cancer agents. The compounds exhibited anti-proliferative activity against ER-α positive T-47D (IC = 3.82-24.

Identification of coumarin derivatives targeting acetylcholinesterase for Alzheimer's disease by field-based 3D-QSAR, pharmacophore model-based virtual screening, molecular docking, MM/GBSA, ADME and MD Simulation study.

Alzheimer's disease (AD) leads to gradual memory loss including other compromised cognitive abilities. Acetylcholinesterase (AChE), an important biochemical enzyme from the cholinesterase (ChE) family, is recognized as primary pharmacological target for treating AD. Currently marketed drugs for AD treatment are primarily AChE inhibitors and coumarin derivatives comprising a wide variety of pharmacological activities have proved their efficacy towards AChE inhibition.

Synthesis, and Studies of Indole-chalcone Derivatives Targeting Estrogen Receptor Alpha (ER-α) for Breast Cancer.

Background: Breast cancer is the prominent reason of death in women worldwide, and the cases are increasing day by day. There are many FDA-approved drugs for treating breast cancer. Due to drug resistance, and problems in selectivity, there is a need to develop more effective agents with few side effects.

Identification of 1,3,4-oxadiazoles as tubulin-targeted anticancer agents: a combined field-based 3D-QSAR, pharmacophore model-based virtual screening, molecular docking, molecular dynamics simulation, and density functional theory calculation approach.

Cancer is one of the most prominent causes of death worldwide and tubulin is a crucial protein of cytoskeleton that maintains essential cellular functions including cell division as well as cell signalling, that makes an attractive drug target for cancer drug development. 1,3,4-oxadiazoles disrupt microtubule causing G2-M phase cell cycle arrest and provide anti-proliferative effect. In this study, field-based 3D-QSAR models were developed using 62 bioactive anti-tubulin 1,3,4-oxadiazoles.

Chemical Composition, and Evaluation of Essential Oil from and Linn for Lung Cancer.

Background: Medicinal plants play an essential role in everyday life; plants highly contain therapeutic phytoconstituents commonly used to treat various diseases. This paper discusses the Chemical composition, antiproliferative activity and study of essential oil extracted from (family Lamiaceae) and (family Apiaceae).

Objective: In present study GC-MS was used to identify the chemical constituents from and .

Structure-based Virtual Screening and Molecular Dynamic Simulation Approach for the Identification of Terpenoids as Potential DPP-4 Inhibitors.

Background: Diabetes mellitus is a metabolic disorder where insulin secretion is compromised, leading to hyperglycemia. DPP-4 is a viable and safer target for type 2 diabetes mellitus. Computational tools have proven to be an asset in the process of drug discovery.

Identification of terpenoids as dihydropteroate synthase and dihydrofolate reductase inhibitors through structure-based virtual screening and molecular dynamic simulations.

Bacterial infections are rising, and antimicrobial resistance (AMR) in bacteria has worsened the scenario, requiring extensive research to find alternative therapeutic agents. Terpenoids play an essential role in protecting plants from herbivores and pathogens. The present study was designed to focus on in silico evaluation of terpenoids for their affinity towards two necessary enzymes, i.

Synthesis and Studies of 4-phenyl thiazol-2-amine Derivatives as Putative Anti-breast Cancer Agents.

Background: Breast cancer (BC) is the second-leading cause of cancer-related fatalities in women after lung cancer worldwide. The development of BC is significantly influenced by estrogen receptors (ERs). The problem with current cancer treatments is selectivity, target specificity, cytotoxicity, and developing resistance.

Effectiveness of Selective Estrogen Receptor Modulators in Breast Cancer Therapy: An Update.

Background: Breast cancer is considered to be 2most common cancer subtype investigated worldwide. It is mainly prevalent in postmenopausal women. Estrogen Receptor (ER) is a primary transcription factor for the survival and growth of tumors.

Flavonoids as P-glycoprotein inhibitors for multidrug resistance in cancer: an approach.

Cancer has become a leading cause of mortality due to non-communicable diseases after cardiovascular disease worldwide and is increasing day by day at a daunting pace. According to an estimate by 2040 there will be 28.4 million cancer cases.

Chemical composition and evaluation of essential oil from leaves for lung cancer.

Chemical composition of the essential oil (EO) of leaves was studied by gas chromatography-mass spectrometry. Forty-five constituents were identified in the oil hydrodistilled from the sample collected from Ghudda Village, Bathinda (Pb), India of which eucalyptol (34.39%) and ledol (9.

Thiazole and Related Heterocyclic Systems as Anticancer Agents: A Review on Synthetic Strategies, Mechanisms of Action and SAR Studies.

Background: Cancer is the second leading cause of death worldwide. Many anticancer drugs are commercially available, but lack of selectivity, target specificity, cytotoxicity, and development of resistance lead to serious side effects. Several experiments have been going on to develop compounds with minor or no side effects.

New pentacyclic triterpene from Lodd. as anticancer agent for breast cancer targeting estrogen receptor-.

One new (compound ) along with two previously known ursane type triterpenoids (compounds and ) were purified by chromatographic techniques from ethyl acetate extract of aerial parts of and characterized by HRMS, 1 D and 2 D-NMR. Compounds (ursolic acid), (euscaphic acid) and (3,20-dihydroxy 2-oxo-urs-12-en-28-oic acid) were tested for their antiproliferative activity along with standard bazedoxifene. Compounds and were found to be of higher activity (3.

Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies.

Breast cancer is the second most leading cause of death among women. Multiple drugs have been approved by FDA for the treatment of BC. The major drawbacks of existing drugs are the development of resistance, toxicity, selectivity problem.

Recent Development in Indole Derivatives as Anticancer Agent: A Mechanistic Approach.

Background: Cancer accounts for several deaths each year. There are multiple FDA approved drugs for cancer treatments. Due to the severe side effects and multiple drug resistance, the current drug therapies become ineffective.

Engagement of phytoestrogens in breast cancer suppression: Structural classification and mechanistic approach.

Cancer is the world's devastating disease, and breast cancer is the most common reason for the death of women worldwide. Many synthetic drugs and medications are provided with their beneficial actions, but all of these have side effects and resistance problems. Natural remedies are coming forward to overcome the disadvantages of synthetic drugs.

Antimicrobial flavonoids as a potential substitute for overcoming antimicrobial resistance.

Background: Infectious diseases are the leading cause of death in 21 century due to antimicrobial resistance and scarcity of new molecules to undertake rising infections. There could be a multiple reasons behind antimicrobial resistance whether it is increased drug metabolism or bacterial endotoxins. The demand of effective medication is increasing day by day to treat microbial infections and combat antimicrobial resistance.

Comprehensive temporal reprogramming ensures dynamicity of transcriptomic profile for adaptive response in Taxus contorta.

Plants respond to the environmental perturbations by triggering the dynamic changes within the transcriptome. The assessment of these oscillations within the transcriptome would offer insights into the ecological adaptation of the plants. We evaluated how the transcriptome of Taxus contorta swings under natural conditions to elucidate its adaptive response.

Tetrazoles as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies.

Cancer is a leading cause of death worldwide. Even after the availability of numerous drugs and treatments in the market, scientists and researchers are focusing on new therapies because of their resistance and toxicity issues. The newly synthesized drug candidates are able to demonstrate in vitro activity but are unable to reach clinical trials due to their rapid metabolism and low bioavailability.

Synthesis and In Silico Studies of C-4 Substituted Coumarin Analogues as Anticancer Agents.

Background: Coumarin is a fused ring system and possesses the enormous capability of targeting various receptors participating in the cancer pathway. Coumarin and its derivatives were found to exhibit very rare toxicity and other side effects. It has been found its immense anticancer potential depends on the nature of the group present and its pattern of substitution on the basic nucleus.