scholarly journals Chiral Derivatives of Xanthones with Antimicrobial Activity

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 314 ◽  
Author(s):  
Joana Araújo ◽  
Carla Fernandes ◽  
Madalena Pinto ◽  
Maria Tiritan
Keyword(s):  
Antimicrobial Activity ◽  
Natural Products ◽  
Drug Discovery ◽  
Biological Activities ◽  
World Health ◽  
Natural Sources ◽  
Drug Discovery And Development ◽  
The World ◽  
Health Organization ◽  
Derivatives Of

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.

scholarly journals Antiplasmodial natural products: an update

2019 ◽  
Vol 18 (1) ◽  
Author(s):  
Nasir Tajuddeen ◽  
Fanie R. Van Heerden
Keyword(s):  
Natural Products ◽  
Relevant Literature ◽  
World Health ◽  
Effective Control ◽  
Insecticide Treated Nets ◽  
Scientific Databases ◽  
The World ◽  
Significant Public Health ◽  
Public Health Challenge ◽  
Health Organization

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.

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
Keyword(s):  
Natural Products ◽  
Drug Delivery Systems ◽  
Drug Carriers ◽  
Water Soluble ◽  
World Health ◽  
New Approach ◽  
Bioactive Natural Products ◽  
The World ◽  
Poorly Water Soluble ◽  
Health Organization

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.

scholarly journals Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform

2019 ◽  
Vol 24 (3) ◽  
pp. 346-361 ◽  
Author(s):  
Carolina B. Moraes ◽  
Gesa Witt ◽  
Maria Kuzikov ◽  
Bernhard Ellinger ◽  
Theodora Calogeropoulou ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Trypanosoma Brucei ◽  
Value Chain ◽  
Neglected Tropical Diseases ◽  
World Health ◽  
Synthetic Compound ◽  
Antiparasitic Activity ◽  
Compound Libraries ◽  
Health Organization

According to the World Health Organization, more than 1 billion people are at risk of or are affected by neglected tropical diseases. Examples of such diseases include trypanosomiasis, which causes sleeping sickness; leishmaniasis; and Chagas disease, all of which are prevalent in Africa, South America, and India. Our aim within the New Medicines for Trypanosomatidic Infections project was to use (1) synthetic and natural product libraries, (2) screening, and (3) a preclinical absorption, distribution, metabolism, and excretion–toxicity (ADME-Tox) profiling platform to identify compounds that can enter the trypanosomatidic drug discovery value chain. The synthetic compound libraries originated from multiple scaffolds with known antiparasitic activity and natural products from the Hypha Discovery MycoDiverse natural products library. Our focus was first to employ target-based screening to identify inhibitors of the protozoan Trypanosoma brucei pteridine reductase 1 ( TbPTR1) and second to use a Trypanosoma brucei phenotypic assay that made use of the T. brucei brucei parasite to identify compounds that inhibited cell growth and caused death. Some of the compounds underwent structure-activity relationship expansion and, when appropriate, were evaluated in a preclinical ADME-Tox assay panel. This preclinical platform has led to the identification of lead-like compounds as well as validated hits in the trypanosomatidic drug discovery value chain.

scholarly journals Use of Natural Products in Leishmaniasis Chemotherapy: An Overview

2020 ◽  
Vol 8 ◽  
Author(s):  
Luiza F. O. Gervazoni ◽  
Gabrielle B. Barcellos ◽  
Taiana Ferreira-Paes ◽  
Elmo E. Almeida-Amaral
Keyword(s):  
Natural Products ◽  
New Drugs ◽  
World Health ◽  
Parasitic Disease ◽  
Research Groups ◽  
Chemical Structures ◽  
Development Of Resistance ◽  
The World ◽  
Health Organization ◽  
Therapeutic Compounds

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.

scholarly journals Screening Marine Natural Products for New Drug Leads against Trypanosomatids and Malaria

Marine Drugs ◽  
2020 ◽  
Vol 18 (4) ◽  
pp. 187 ◽  
Author(s):  
María Álvarez-Bardón ◽  
Yolanda Pérez-Pertejo ◽  
César Ordóñez ◽  
Daniel Sepúlveda-Crespo ◽  
Nestor M. Carballeira ◽  
...  
Keyword(s):  
Natural Products ◽  
High Throughput Screening ◽  
High Performance ◽  
Social Issues ◽  
Neglected Tropical Diseases ◽  
New Drugs ◽  
World Health ◽  
World Population ◽  
The World ◽  
Health Organization

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.

scholarly journals A Pharmacokinetic Study of Antimalarial 3,5-Diaryl-2-aminopyridine Derivatives

2015 ◽  
Vol 2015 ◽  
pp. 1-5 ◽  
Author(s):  
Ntokozo Dambuza ◽  
Peter Smith ◽  
Alicia Evans ◽  
Dale Taylor ◽  
Kelly Chibale ◽  
...  
Keyword(s):  
Half Life ◽  
Peak Plasma ◽  
World Health ◽  
African Region ◽  
Peak Plasma Level ◽  
Drug Candidates ◽  
The World ◽  
The Mean ◽  
Health Organization ◽  
Derivatives Of

Malaria caused by Plasmodium falciparum is responsible for approximately 80% of the incidence and 90% of deaths which occur in the World Health Organization (WHO) African region, with children and pregnant women having the highest incidence. P. falciparum has developed resistance, and therefore new effective candidate antimalarial drugs need to be developed. Previous studies identified 3,5-diaryl-2-aminopyridines as potential antimalarial drug candidates; therefore, derivatives of these compounds were synthesized in order to improve their desired properties and pharmacokinetic (PK) properties of the derivatives were investigated in a mouse model which was dosed orally and intravenously. Collected blood samples were analyzed using liquid chromatography coupled to mass spectrometer (LC-MS/MS). The mean peak plasma level of 1.9 μM was obtained at 1 hour for compound 1 and 3.3 μM at 0.5 hours for compound 2. A decline in concentration was observed with a half-life of 2.53 and 0.87 hours for compound 1 in mice dosed orally and intravenously, respectively. For compound 2 a half-life of 2.96 and 0.68 hours was recorded. The bioavailability was 69% and 59.7% for compound 1 and compound 2, respectively.

scholarly journals Overcoming the Challenges of Drug Discovery for Neglected Tropical Diseases

2013 ◽  
Vol 19 (3) ◽  
pp. 335-343 ◽  
Author(s):  
Kelly L. Johnston ◽  
Louise Ford ◽  
Mark J. Taylor
Keyword(s):  
Drug Discovery ◽  
Neglected Tropical Diseases ◽  
Integrated Control ◽  
Development Program ◽  
Control Measures ◽  
World Health ◽  
Poor People ◽  
Tropical Diseases ◽  
Drug Discovery And Development ◽  
Health Organization

Neglected tropical diseases (NTDs) are a group of 17 diseases that typically affect poor people in tropical countries. Each has been neglected for decades in terms of funding, research, and policy, but the recent grouping of them into one unit, which can be targeted using integrated control measures, together with increased advocacy has helped to place them on the global health agenda. The World Health Organization has set ambitious goals to control or eliminate 10 NTDs by 2020 and launched a roadmap in January 2012 to guide this global plan. The result of the launch meeting, which brought together representatives from the pharmaceutical industry, donors, and politicians, was the London Declaration: a series of commitments to provide more drugs, research, and funds to achieve the 2020 goals. Drug discovery and development for these diseases are extremely challenging, and this article highlights these challenges in the context of the London Declaration, before focusing on an example of a drug discovery and development program for the NTDs onchocerciasis and lymphatic filariasis (the anti- Wolbachia consortium, A·WOL).

scholarly journals PHYTOCHEMICALS AS POTENTIAL ANTIVIRAL AGENTS IN SARS-COV-2 THERAPY: AN UPDATE

Química Nova ◽  
2021 ◽  
Author(s):  
Nerilson Lima ◽  
Teresinha Andrade ◽  
Kojo Acquah ◽  
Marcone Oliveira ◽  
Kellyane Gois ◽  
...  
Keyword(s):  
Natural Products ◽  
Side Effects ◽  
Severe Acute Respiratory Syndrome ◽  
Antiviral Agents ◽  
World Health ◽  
Plant Metabolites ◽  
Structural Class ◽  
The World ◽  
Low Toxicity ◽  
Health Organization

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.

scholarly journals Potential Natural Products Against Respiratory Viruses: A Perspective to Develop Anti-COVID-19 Medicines

2021 ◽  
Vol 11 ◽  
Author(s):  
Marzieh Omrani ◽  
Mohsen Keshavarz ◽  
Samad Nejad Ebrahimi ◽  
Meysam Mehrabi ◽  
Lyndy J. McGaw ◽  
...  
Keyword(s):  
Natural Products ◽  
Perceived Risk ◽  
Influenza A ◽  
Viral Infections ◽  
Respiratory Viruses ◽  
World Health ◽  
Screening Programs ◽  
The World ◽  
Novel Coronavirus ◽  
Health Organization

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.

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