scholarly journals Dendrimers as Drug Carriers. A New Approach to Increase the Potential of Bioactive Natural Products

2006 ◽  
Vol 1 (7) ◽  
pp. 1934578X0600100
Author(s):  
Costas Demetzos

Nanotechnology is a challenging field in science and its application in medicine will bring significant advantages in the treatment of diseases. According to the World Health Organization there is a need for improved therapies against cancer, AIDS and Alzheimer's disease. The new therapies include the design of drug delivery systems, which are able to deliver new bioactive natural products to the target tissues. Dendrimers are hyperbranched polymers with well defined structure and molecular weight; they are composed of a central core and repeated branching units; they have a globular shape, low polydispersity and large void internal spaces that can be used for the encapsulation and delivery of many classes of compounds. Nanosystems, such as dendrimers, can achieve successful administration of poorly water-soluble compounds and those with narrow therapeutic indices.

2019 ◽  
Vol 18 (1) ◽  
Author(s):  
Nasir Tajuddeen ◽  
Fanie R. Van Heerden

Abstract Background Malaria remains a significant public health challenge in regions of the world where it is endemic. An unprecedented decline in malaria incidences was recorded during the last decade due to the availability of effective control interventions, such as the deployment of artemisinin-based combination therapy and insecticide-treated nets. However, according to the World Health Organization, malaria is staging a comeback, in part due to the development of drug resistance. Therefore, there is an urgent need to discover new anti-malarial drugs. This article reviews the literature on natural products with antiplasmodial activity that was reported between 2010 and 2017. Methods Relevant literature was sourced by searching the major scientific databases, including Web of Science, ScienceDirect, Scopus, SciFinder, Pubmed, and Google Scholar, using appropriate keyword combinations. Results and Discussion A total of 1524 compounds from 397 relevant references, assayed against at least one strain of Plasmodium, were reported in the period under review. Out of these, 39% were described as new natural products, and 29% of the compounds had IC50 ≤ 3.0 µM against at least one strain of Plasmodium. Several of these compounds have the potential to be developed into viable anti-malarial drugs. Also, some of these compounds could play a role in malaria eradication by targeting gametocytes. However, the research into natural products with potential for blocking the transmission of malaria is still in its infancy stage and needs to be vigorously pursued.


2020 ◽  
Vol 8 ◽  
Author(s):  
Luiza F. O. Gervazoni ◽  
Gabrielle B. Barcellos ◽  
Taiana Ferreira-Paes ◽  
Elmo E. Almeida-Amaral

Leishmaniasis is an infectious parasitic disease that is caused by protozoa of the genus Leishmania, a member of the Trypanosomatidae family. Leishmaniasis is classified by the World Health Organization as a neglected tropical disease that is responsible for millions of deaths worldwide. Although there are many possible treatments for leishmaniasis, these treatments remain mostly ineffective, expensive, and long treatment, as well as causing side effects and leading to the development of resistance. For novel and effective treatments to combat leishmaniasis, many research groups have sought to utilize natural products. In addition to exhibiting potential as therapeutic compounds, natural products may also contribute to the development of new drugs based on their chemical structures. This review presents the most promising natural products, including crude extracts and isolated compounds, employed against Leishmania spp.


Marine Drugs ◽  
2020 ◽  
Vol 18 (4) ◽  
pp. 187 ◽  
Author(s):  
María Álvarez-Bardón ◽  
Yolanda Pérez-Pertejo ◽  
César Ordóñez ◽  
Daniel Sepúlveda-Crespo ◽  
Nestor M. Carballeira ◽  
...  

Neglected Tropical Diseases (NTD) represent a serious threat to humans, especially for those living in poor or developing countries. Almost one-sixth of the world population is at risk of suffering from these diseases and many thousands die because of NTDs, to which we should add the sanitary, labor and social issues that hinder the economic development of these countries. Protozoan-borne diseases are responsible for more than one million deaths every year. Visceral leishmaniasis, Chagas disease or sleeping sickness are among the most lethal NTDs. Despite not being considered an NTD by the World Health Organization (WHO), malaria must be added to this sinister group. Malaria, caused by the apicomplexan parasite Plasmodium falciparum, is responsible for thousands of deaths each year. The treatment of this disease has been losing effectiveness year after year. Many of the medicines currently in use are obsolete due to their gradual loss of efficacy, their intrinsic toxicity and the emergence of drug resistance or a lack of adherence to treatment. Therefore, there is an urgent and global need for new drugs. Despite this, the scant interest shown by most of the stakeholders involved in the pharmaceutical industry makes our present therapeutic arsenal scarce, and until recently, the search for new drugs has not been seriously addressed. The sources of new drugs for these and other pathologies include natural products, synthetic molecules or repurposing drugs. The most frequent sources of natural products are microorganisms, e.g., bacteria, fungi, yeasts, algae and plants, which are able to synthesize many drugs that are currently in use (e.g. antimicrobials, antitumor, immunosuppressants, etc.). The marine environment is another well-established source of bioactive natural products, with recent applications against parasites, bacteria and other pathogens which affect humans and animals. Drug discovery techniques have rapidly advanced since the beginning of the millennium. The combination of novel techniques that include the genetic modification of pathogens, bioimaging and robotics has given rise to the standardization of High-Performance Screening platforms in the discovery of drugs. These advancements have accelerated the discovery of new chemical entities with antiparasitic effects. This review presents critical updates regarding the use of High-Throughput Screening (HTS) in the discovery of drugs for NTDs transmitted by protozoa, including malaria, and its application in the discovery of new drugs of marine origin.


Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 314 ◽  
Author(s):  
Joana Araújo ◽  
Carla Fernandes ◽  
Madalena Pinto ◽  
Maria Tiritan

According to the World Health Organization, the exacerbated use of antibiotics worldwide is increasing multi-resistant infections, especially in the last decade. Xanthones are a class of compounds receiving great interest in drug discovery and development that can be found as natural products or obtained by synthesis. Many derivatives of xanthones are chiral and associated with relevant biological activities, including antimicrobial. The aim of this review is to compile information about chiral derivatives of xanthones from natural sources and their synthesized examples with antimicrobial activity.


Química Nova ◽  
2021 ◽  
Author(s):  
Nerilson Lima ◽  
Teresinha Andrade ◽  
Kojo Acquah ◽  
Marcone Oliveira ◽  
Kellyane Gois ◽  
...  

In December 2019, the World Health Organization officially announced the discovery and fast spread of the new coronavirus disease (COVID-19), which is caused by the SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus 2), discovered in Wuhan, China. Since the beginning of the pandemic, there has been a global search for the discovery of antiviral candidates capable of treating the infection caused by SARS-CoV-2. However, none of them has shown proved efficacy and low toxicity for an effective dose. In view of this, research with plants based in natural products has been highlighted by the low toxicity of its metabolites and reduced side effects, since plants have been used for millennia in the treatment of various diseases. In this review, we highlight some plant species and plant metabolites belonging to the structural class of phenolic, alkaloids and terpenes with promising antiviral potential agains coronavirus that could be explored as potential candidates for drug prototypes in the treatment of COVID-19.


2021 ◽  
Vol 11 ◽  
Author(s):  
Marzieh Omrani ◽  
Mohsen Keshavarz ◽  
Samad Nejad Ebrahimi ◽  
Meysam Mehrabi ◽  
Lyndy J. McGaw ◽  
...  

The emergence of viral pneumonia caused by a novel coronavirus (CoV), known as the 2019 novel coronavirus (2019-nCoV), resulted in a contagious acute respiratory infectious disease in December 2019 in Wuhan, Hubei Province, China. Its alarmingly quick transmission to many countries across the world and a considerable percentage of morbidity and mortality made the World Health Organization recognize it as a pandemic on March 11, 2020. The perceived risk of infection has led many research groups to study COVID-19 from different aspects. In this literature review, the phylogenetics and taxonomy of COVID-19 coronavirus, epidemiology, and respiratory viruses similar to COVID-19 and their mode of action are documented in an approach to understand the behavior of the current virus. Moreover, we suggest targeting the receptors of SARS-CoV and SARS-CoV-2 such as ACE2 and other proteins including 3CLpro and PLpro for improving antiviral activity and immune response against COVID-19 disease. Additionally, since phytochemicals play an essential role in complementary therapies for viral infections, we summarized different bioactive natural products against the mentioned respiratory viruses with a focus on influenza A, SARS-CoV, MERS, and COVID-19.Based on current literature, 130 compounds have antiviral potential, and of these, 94 metabolites demonstrated bioactivity against coronaviruses. Interestingly, these are classified in different groups of natural products, including alkaloids, flavonoids, terpenoids, and others. Most of these compounds comprise flavonoid skeletons. Based on our survey, xanthoangelol E (88), isolated from Angelica keiskei (Miq.) Koidz showed inhibitory activity against SARS-CoV PLpro with the best IC50 value of 1.2 μM. Additionally, hispidulin (3), quercetin (6), rutin (8), saikosaponin D (36), glycyrrhizin (47), and hesperetin (55) had remarkable antiviral potential against different viral infections. Among these compounds, quercetin (6) exhibited antiviral activities against influenza A, SARS-CoV, and COVID-19 and this seems to be a highly promising compound. In addition, our report discusses the obstacles and future perspectives to highlight the importance of developing screening programs to investigate potential natural medicines against COVID-19.


2020 ◽  
Vol 16 (7) ◽  
pp. 649-656 ◽  
Author(s):  
Shreeya V. Deshmukh ◽  
Bala Prabhakar ◽  
Yogesh A. Kulkarni

Background: Diabetes is a metabolic disorder associated with abnormally high levels of glucose in the blood due to inadequate production of insulin or inadequate sensitivity of cells to the action of insulin. Diabetes has become an increasing challenge in the world. The predicted diabetic population according to the World Health Organization is 8.7% between the age group 20-70 years. There are many complications linked to prolonged high blood glucose levels, such as microvascular complications and macrovascular complications. Vitamins play an important role in glucose metabolism and the potential utility of supplementation is relevant for the prevention and/or management of diabetes mellitus and its complications. Methods: Literature search was performed using various dataset like PUBMED, EBSCO, ProQuest, Scopus and selected websites like the National Institute of Health and the World Health Organization. Result: Water-soluble vitamins have been thoroughly studied for their activity in diabetes and diabetic complications. Conclusion: Water-soluble vitamins like B1, B3, B6, B7, B9 and B12 have notable effects in diabetes mellitus and its related complications like nephropathy, neuropathy, retinopathy and cardiomyopathy.


2021 ◽  
Vol 9 (1) ◽  
pp. 165
Author(s):  
Saman Fouladirad ◽  
Horacio Bach

The Coronavirus disease 2019 (COVID-19), caused by the novel coronavirus SARS-CoV-2, was first reported in December 2019 in Wuhan, Hubei province, China. This virus has led to 61.8 million cases worldwide being reported as of December 1st, 2020. Currently, there are no definite approved therapies endorsed by the World Health Organization for COVID-19, focusing only on supportive care. Treatment centers around symptom management, including oxygen therapy or invasive mechanical ventilation. Immunotherapy has the potential to play a role in the treatment of SARS-CoV-2. Monoclonal antibodies (mAbs), in particular, is a relatively new approach in the world of infectious diseases and has the benefit of overcoming challenges with serum therapy and intravenous immunoglobulins preparations. Here, we reviewed the articles published in PubMed with the purpose of summarizing the currently available evidence for the use of neutralizing antibodies as a potential treatment for coronaviruses. Studies reporting in vivo results were summarized and analyzed. Despite promising data from some studies, none of them progressed to clinical trials. It is expected that neutralizing antibodies might offer an alternative for COVID-19 treatment. Thus, there is a need for randomized trials to understand the potential use of this treatment.


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