scholarly journals Pharmacokinetics of Marine-Derived Drugs

Marine Drugs ◽  
2020 ◽  
Vol 18 (11) ◽  
pp. 557 ◽  
Author(s):  
Alexander N. Shikov ◽  
Elena V. Flisyuk ◽  
Ekaterina D. Obluchinskaya ◽  
Olga N. Pozharitskaya

Marine organisms represent an excellent source of innovative compounds that have the potential for the development of new drugs. The pharmacokinetics of marine drugs has attracted increasing interest in recent decades due to its effective and potential contribution to the selection of rational dosage recommendations and the optimal use of the therapeutic arsenal. In general, pharmacokinetics studies how drugs change after administration via the processes of absorption, distribution, metabolism, and excretion (ADME). This review provides a summary of the pharmacokinetics studies of marine-derived active compounds, with a particular focus on their ADME. The pharmacokinetics of compounds derived from algae, crustaceans, sea cucumber, fungus, sea urchins, sponges, mollusks, tunicate, and bryozoan is discussed, and the pharmacokinetics data in human experiments are analyzed. In-depth characterization using pharmacokinetics is useful for obtaining information for understanding the molecular basis of pharmacological activity, for correct doses and treatment schemes selection, and for more effective drug application. Thus, an increase in pharmacokinetic research on marine-derived compounds is expected in the near future.

2020 ◽  
Vol 16 (6) ◽  
pp. 784-795
Author(s):  
Krisnna M.A. Alves ◽  
Fábio José Bonfim Cardoso ◽  
Kathia M. Honorio ◽  
Fábio A. de Molfetta

Background:: Leishmaniosis is a neglected tropical disease and glyceraldehyde 3- phosphate dehydrogenase (GAPDH) is a key enzyme in the design of new drugs to fight this disease. Objective:: The present study aimed to evaluate potential inhibitors of GAPDH enzyme found in Leishmania mexicana (L. mexicana). Methods: A search for novel antileishmanial molecules was carried out based on similarities from the pharmacophoric point of view related to the binding site of the crystallographic enzyme using the ZINCPharmer server. The molecules selected in this screening were subjected to molecular docking and molecular dynamics simulations. Results:: Consensual analysis of the docking energy values was performed, resulting in the selection of ten compounds. These ligand-receptor complexes were visually inspected in order to analyze the main interactions and subjected to toxicophoric evaluation, culminating in the selection of three compounds, which were subsequently submitted to molecular dynamics simulations. The docking results showed that the selected compounds interacted with GAPDH from L. mexicana, especially by hydrogen bonds with Cys166, Arg249, His194, Thr167, and Thr226. From the results obtained from molecular dynamics, it was observed that one of the loop regions, corresponding to the residues 195-222, can be related to the fitting of the substrate at the binding site, assisting in the positioning and the molecular recognition via residues responsible for the catalytic activity. Conclusion:: he use of molecular modeling techniques enabled the identification of promising compounds as inhibitors of the GAPDH enzyme from L. mexicana, and the results obtained here can serve as a starting point to design new and more effective compounds than those currently available.


2021 ◽  
Vol 2 (2) ◽  
pp. 197-206
Author(s):  
Luigi Della Gravara ◽  
Ciro Battiloro ◽  
Antonietta Letizia ◽  
Rosa Cantile ◽  
Vito D'Agnano ◽  
...  

Immunotherapy in the form of ICIs has revolutionized advanced NSCLC treatment algorithms, with ICI-containing combination treatments being the latest addition to approved regimens. However, PD-L1 still represents the only routinely assessed and validated biomarker apart from genetic drivers testing, impairing our capacity to personalize and guide treatment. Therefore, this paper aims to analyze the most promising emerging predictive biomarkers that could help us in the near future to select patients more effectively.


2021 ◽  
pp. 54-55
Author(s):  
Jayesh Kalbhande ◽  
Vicky Kuldeep

Drug resistance of bacteria is biggest challenge humanity is going to face in near future. Bacteria are rapidly developing resistant to multiple drugs and there are not many new drugs in pipeline. Infection because of drug resistant organism is a common cause of morbidity and mortality in intensive care unit. If acquisition of drug resistance by microorganism progresses at this rate, that time is not very far when we will be pushed in to preantibiotic era. We need to develop new strategies to combat drug resistant by microorganism. We report a case of highly drug resistant urinary tract infection caused by Klebsiella. This strain was resistant to both Inj. Meropenem and Inj. Amikacin. This case was successfully treated by combination of Inj. Meropenem and Inj. Amikacin and complete resolution of infection was observed.


Author(s):  
Sagar Chowdhury ◽  
Zahed Siddique

With the advancements of 3D modeling software, the use of CAD in design has become a standard practice. In recent years development in computer hardware and improvements in user friendliness of the CAD software has allowed designers to quickly and easily modify the CAD models. This modification capability allows CAD to be an integral part of the design process. Due to the increase in global competition, companies have become increasingly interested in fast and efficient design processes. One way to achieve improved efficiency is through better collaboration among designers working in common or similar projects and disciplines. A large design problem often requires specialized knowledge from several fields. Collaboration among the designers from these fields will ensure efficient design. Interaction among the designers can prevent redesign of similar components/subsystems, which requires the ability to share their designs. With the increase of collaboration, designers can now get access to large databases of 3D CAD models. But the challenge lies in search capabilities to identify common models from a large database. These considerations suggest that in the near future a challenge in 3D CAD industry will be how to find models of similar components and products. This paper presents an approach and its implementation to measure the similarity among a number of CAD models. The approach is based on the extraction and organization of information from the CAD models, which is followed by the suitable selection of commonality index and calculation of the commonality among a set of CAD models. A set of Vacuum cleaners are modeled and then compared to demonstrate the application of the approach.


Biology Open ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. bio055632

ABSTRACTFirst Person is a series of interviews with the first authors of a selection of papers published in Biology Open, helping early-career researchers promote themselves alongside their papers. Komal Panchal is first author on ‘Miro, a Rho GTPase genetically interacts with Alzheimer's disease-associated genes (Tau, Aβ42 and Appl) in Drosophila melanogaster’, published in BiO. Komal is a PhD student in the lab of Dr Anand K. Tiwari at the Institute of Advanced Research (IAR), Koba Institutional Area, Gujarat, India, investigating the possible molecular basis of Alzheimer's disease.


2018 ◽  
Vol 27 (11) ◽  
pp. 1581-1587 ◽  
Author(s):  
Hong-Meng Chuang ◽  
Tina Emily Shih ◽  
Kang-Yun Lu ◽  
Sheng-Feng Tsai ◽  
Horng-Jyh Harn ◽  
...  

Although the clinical application of new drugs has been shown to be effective in slowing disease progression and improving the quality of life in patients with pulmonary fibrosis, the damaged lung tissue does not recover with these drugs. Thus, there is an urgent need to establish regenerative therapy, such as stem cell therapy or tissue engineering. Moreover, the clinical application of mesenchymal stem cell (MSC) therapy has been shown to be safe in humans with idiopathic pulmonary fibrosis (IPF). It seems that a combination of MSC transplantation and pharmaceutical therapy might have additional benefits; however, the experimental design for its efficacy is still lacking. In this review, we provide an overview of the mechanisms that were identified when IPF was treated with MSC transplantation or new drugs. To maximize the therapeutic effect, we suggest that MSC transplantation is combined with drug application for synergistic effects. This review provides clinicians and scientists with the most efficient medical options, in the hope that this will spur on future research and lead to an eventual cure for this disease.


Author(s):  
Hindustan Abdul Ahad ◽  
Haranath Chinthaginjala ◽  
Gangireddy Jayasimha Reddy ◽  
Pasupuleti Dheeraj Krishna ◽  
Syed Rahamathulla ◽  
...  

The United States Food and Drug Administration (USFDA) is one of the main regulated agencies wherein the submission and approval of the new drugs is done. This review is based on the process of submission to the ANDA as per FDA norms as described in paragraph IV submission in Federal Food, Drug, and Cosmetic Act (FD and C Act). No drug would exist in the market until it gets accepted by regulatory authorities. The ANDA submission is for those firms seeking to copy branded drugs before running out of patents to get profit on them. A generic applicant must provide in its application a "certification" that a patent submitted to FDA by the brand-name drug's sponsor and scheduled in FDA's Approved Drug Products with Therapeutic Equivalence Evaluations (the Orange Book). A Generic Product must meet the standards recognized by FDA in Reference listed drugs (RLD). This study concludes the process of ANDA submission to FDA and acts correlated to the submission in paragraph IV, the details of ANDA filling in the eCTD format and overview of the review process the checklist to the applicant.


Buildings ◽  
2019 ◽  
Vol 9 (7) ◽  
pp. 164 ◽  
Author(s):  
Georgios Pardalis ◽  
Krushna Mahapatra ◽  
Giangiacomo Bravo ◽  
Brijesh Mainali

In this paper, we examine factors affecting owners’ intention for renovation of their detached houses. Furthermore, we analyze their interest in choosing a one-stop-shop (OSS) service for the renovation, even though such a concept is not yet established in Sweden, but emerging in other parts of Europe. Our study is based on responses to an online questionnaire survey of 971 house owners residing in Kronoberg Region in Sweden. About 76% of the respondents intend to renovate in the near future, with approximately 71% of them preferring to renovate individual components of their dwelling and 5% to renovate their whole house in steps. House owners of younger age, higher income, higher education, and those with an interest for environmental issues, were the ones most interested in physical renovations, which improves energy efficiency of the building. For those house owners, one-stop-shop can facilitate the decision-making process, and help them to choose those measures that will improve their quality of life. Approximately 20% of the respondents had a positive view towards an one-stop-shop, which is an indicator that market for such a service exists. Parameters such as quality of work, cost and energy savings and specification of measures to be adopted are the key for the promotion of one-stop-shop. Additionally, house owners want to have a certain level of involvement in the selection of actors performing the renovation. Moreover, financial incentives, e.g., loans, do not play a significant role for the selection of one-stop-shop, but act as complementary motive for house owners.


Blood ◽  
2013 ◽  
Vol 122 (23) ◽  
pp. 3723-3734 ◽  
Author(s):  
Michael Hallek

AbstractThe management of chronic lymphocytic leukemia (CLL) is undergoing profound changes. Several new drugs have been approved for CLL treatment (fludarabine, bendamustine, and the monoclonal antibodies alemtuzumab, rituximab, and ofatumumab) and many more drugs are in advanced clinical development to be approved for this disease. In addition, the extreme heterogeneity of the clinical course and our improved ability to foresee the prognosis of this leukemia by the use of clinical, biological, and genetic parameters now allow us to characterize patients with a very mild onset and course, an intermediate prognosis, or a very aggressive course with high-risk leukemia. Therefore, it becomes increasingly challenging to select the right treatment strategy for each condition. This article summarizes the currently available diagnostic and therapeutic tools and gives an integrated recommendation of how to manage CLL in 2013. Moreover, I propose a strategy how we might integrate the novel agents for CLL therapy into sequential treatment approaches in the near future.


Sign in / Sign up

Export Citation Format

Share Document