ChemInform Abstract: Development of Estrogen Antagonists as Pharmaceutical Agents

ChemInform ◽  
2010 ◽  
Vol 28 (45) ◽  
pp. no-no
Author(s):  
S. RAY ◽  
I. DWIVEDY
2020 ◽  
Author(s):  
Jagjit S Soar

he current COVID-19 pandemic now believed to be based on the mutation of the SARS-CoV virus (first reported in 2002) to SARS-CoV-2 emerging in 2019, is naturally causing extreme worry and concern around the world with sometimes mixed and incoherent messages on how to deal with it. There is a plethora of information from previous epidemics caused by other coronaviruses such as severe acute respiratory syndrome, SARS (2002) and Middle East respiratory syndrome MERS (2012) from which we can extrapolate guidance on how to deal with the current pandemic. In the current absence of specific pharmaceutical agents, we propose assessing the extended tools that we already possess in our biological armoury to combat, prevent and control the spread of this virus. Using a set of precise criteria to locate such possible contenders, we conducted literature searches to find compounds that met these criteria. We have now reduced this to a shortlist of three agents that may be the best candidates. We propose vitamin C, vitamin D and Curcumin fit our criteria well. These compounds are widely available to the general public. They are available online and over-the-counter as supplements. Otherwise healthy individuals are safely able to self-administer these agents as a prophylactic to protect themselves and to enhance their immune response. This would be especially desirable for the elderly and at risk groups. These agents can also be used as adjunct therapy, particularly for those who may have early symptoms. This preventative therapy could be implemented whilst awaiting specific pharmaceutical drugs to emerge as a treatment for COVID-19. Our suggested compounds are a highly cost-effective way to potentially reduce the mortality that is regretfully mounting as a result of COVID-19 infection. The biological mode of action and the dosing of these compounds are summarised.


2017 ◽  
Vol 65 (4) ◽  

Within a clinical sports medical setting the discussion about doping is insufficient. In elite-sports use of pharmaceutical agents is daily business in order to maintain the expected top-level performance. Unfortunately, a similar development could be observed in the general population of leisure athletes where medical supervision is absent. As a sports physician you are facing imminent ethical questions when standing in between. Therefore, we propose the application of a standardised risk score as a tool to promote doping-prevention and launch the debate within athlete-physician-relationship. In the longterm such kind of risk stratification systems may support decision-making with regard to «protective» exclusion of sporting competition.


Author(s):  
N B Bhagat ◽  
A V Yadav ◽  
P R Mastud ◽  
R A Khutale

In this article we describe the optimizing parameters in the process of spherical crystallisation. Particle engineering of active pharmaceutical agents is an innovative area of research in pharmaceutical industry because of several advantages. Spherical crystallization is one of the particle engineering technique in which drug directly gets crystallized and agglomerated into spherical shape. The spherical crystals can be obtained by different methods like solvent change, Quasi-emulsion droplet, ammonia diffusion and neutralisation. The optimization of process of spherical crystallization is important for obtaining the ideal spherical crystal agglomerates. It includes stirring rate, selection of solvent, pH, temperature etc. which affects on the physico-chemical properties of crystals. These optimizing parameters play its specific role in formation of spherical crystals. Stirring rate affects the shape as well as size of the final agglomerates and solvent selection helps in the formation of maximum amount of agglomerates in the system. The factors like pH and temperature should be maintained in case of drugs which show polymorphism. Apart from this, several others physical phenomenon or parameters like interfacial tension and rate of crystallisation are also important for thorough optimization of process.  


2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Yawei Wang ◽  
Binlin Tang ◽  
Lei Long ◽  
Peng Luo ◽  
Wei Xiang ◽  
...  

AbstractPro-inflammatory activation of adipose tissue macrophages (ATMs) is causally linked to obesity and obesity-associated disorders. A number of studies have demonstrated the crucial role of mitochondrial metabolism in macrophage activation. However, there is a lack of pharmaceutical agents to target the mitochondrial metabolism of ATMs for the treatment of obesity-related diseases. Here, we characterize a near-infrared fluorophore (IR-61) that preferentially accumulates in the mitochondria of ATMs and has a therapeutic effect on diet-induced obesity as well as obesity-associated insulin resistance and fatty liver. IR-61 inhibits the classical activation of ATMs by increasing mitochondrial complex levels and oxidative phosphorylation via the ROS/Akt/Acly pathway. Taken together, our findings indicate that specific enhancement of ATMs oxidative phosphorylation improves chronic inflammation and obesity-related disorders. IR-61 might be an anti-inflammatory agent useful for the treatment of obesity-related diseases by targeting the mitochondria of ATMs.


Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1109
Author(s):  
Cristina Adriana Dehelean ◽  
Iasmina Marcovici ◽  
Codruta Soica ◽  
Marius Mioc ◽  
Dorina Coricovac ◽  
...  

Despite the recent advances in the field of chemically synthetized pharmaceutical agents, nature remains the main supplier of bioactive molecules. The research of natural products is a valuable approach for the discovery and development of novel biologically active compounds possessing unique structures and mechanisms of action. Although their use belongs to the traditional treatment regimes, plant-derived compounds still cover a large portion of the current-day pharmaceutical agents. Their medical importance is well recognized in the field of oncology, especially as an alternative to the limitations of conventional chemotherapy (severe side effects and inefficacy due to the occurrence of multi-drug resistance). This review offers a comprehensive perspective of the first blockbuster chemotherapeutic agents of natural origin’s (e.g. taxol, vincristine, doxorubicin) mechanism of action using 3D representation. In addition is portrayed the step-by-step evolution from preclinical to clinical evaluation of the most recently studied natural compounds with potent antitumor activity (e.g. resveratrol, curcumin, betulinic acid, etc.) in terms of anticancer mechanisms of action and the possible indications as chemotherapeutic or chemopreventive agents and sensitizers. Finally, this review describes several efficient platforms for the encapsulation and targeted delivery of natural compounds in cancer treatment


2021 ◽  
Vol 27 ◽  
Author(s):  
Mina Shahriari-Khalaji ◽  
Maryam Zarkesh ◽  
Zahra Nozhat

: Bacterial nanocellulose (BNC) is one of the natural biopolymers with unique features, the most important of which are nontoxicity, biocompatibility, high tensile profile, nanofiber structure, and purity. The current review aimed to summarize the latest development in BNC-based biomaterials in cancer drug delivery. The original articles were found by searching key databases including PubMed, Scopus, and Web of Scientific and using key terms such as “bacterial nanocellulose OR bacterial cellulose OR BNC” AND “cancer OR carcinoma OR tumor”. The obtained data were in a wide timeframe and the English language. Totally, 350 articles were found from the three main databases (i.e., 106, 251, and 173 articles from PubMed, Scopus, and the Web of Science, respectively). In general, 32 articles met the inclusion criteria after duplicate removal and screening according to the aim of the present review study. In this review study, different applications of the bacterial nanocellulose were considered for cancer drug delivery in addition to describing advanced methods that may be applied to improve therapeutic potency while reducing the adverse effects of chemodrugs by decreasing their dosages. The high ratio of the surface area-to-volume and easy modifications of their chemical components lead BNC potential use as an appropriate matrix structure for the binding and controlled release of various pharmaceutical agents, specifically for topical or transdermal administrations. In addition, BNC-based products regulate the release of hydrophobic and hydrophilic compounds, therefore, provide appropriate materials related to cancer drug delivery. However, undoubtedly, further developments of BNC-based products as cancer drug delivery systems require more extensive investigations.


1993 ◽  
Vol 13 (7) ◽  
pp. 1055-1081
Author(s):  
R. N. Porrelli ◽  
P. J. Munson ◽  
D. Rodbard
Keyword(s):  

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