scholarly journals Synthesis of Some Novel and Potent Anti-Plasmodial Aminoalkyl Chalcone Derivatives

2020 ◽  
Vol 10 (5) ◽  
pp. 6076-6081
Keyword(s):  
Antimalarial Activity ◽  
World Health ◽  
Mice Model ◽  
Aromatic Rings ◽  
Plasmodium Parasite ◽  
Parasite Plasmodium ◽  
Parasite Plasmodium Falciparum ◽  
Health Organization ◽  
Death Cases

Malaria remains to be a health and an economic burden to many people living in Sub-Sahara and Africa. According to World health Organization (WHO) in 2017, 219 million cases of malaria worldwide were documented. Its increase by 2 million from the year 2016 resulted in 435 thousand deaths every day among 1190 deaths of young children more than cases 5 per day have been reported. Among the different species of plasmodium parasite, Plasmodium falciparum is mainly responsible for causing malaria in Africa whereas Plasmodium vivax is the most prevalent in countries outside Africa. Africa suffers from malaria a lot. Almost half of the world’s population is at risk of contracting malaria and approximately 90% of the death cases of Malaria in the world appear from Africa. In our research group in past, we have established that chalcones with an aminoalkyl moiety on one of the aromatic rings have promising in vitro antimalarial activity. We successively enhanced the bioavailability from 3% to 25% in mice model with the derivatization of the potential leads with the help of substitutions of the function groups at 4- position from -F to -CF3.

scholarly journals Assessment of Antimalarial Activity againstPlasmodium falciparumand Phytochemical Screening of Some Yemeni Medicinal Plants

2009 ◽  
Vol 6 (4) ◽  
pp. 453-456 ◽  
Author(s):  
Mohammed A. Alshawsh ◽  
Ramzi A. Mothana ◽  
Hassan A. Al-shamahy ◽  
Salah F. Alsllami ◽  
Ulrike Lindequist
Keyword(s):  
Medicinal Plants ◽  
Antimalarial Activity ◽  
Traditional Healers ◽  
Antiplasmodial Activity ◽  
World Health ◽  
Moderate Activity ◽  
Phytochemical Screening ◽  
Cissus Rotundifolia ◽  
Health Organization

Developing countries, where malaria is one of the most prevalent diseases, still rely on traditional medicine as a source for the treatment of this disease. In the present study, six selected plants (Acalypha fruticosa,Azadirachta indica,Cissus rotundifolia,Echium rauwalfii,Dendrosicyos socotranaandBoswellia elongata) commonly used in Yemen by traditional healers for the treatment of malaria as well as other diseases, were collected from different localities of Yemen, dried and extracted with methanol and water successfully. The antiplasmodial activity of the extracts was evaluated against fresh clinical isolates ofPlasmodium falciparum. The selectivity parameters to evaluate the efficacy of these medicinal plants were measured byin vitromicro test (Mark III) according to World Health Organization (WHO) 1996 & WHO 2001 protocols of antimalarial drug tests. Among the investigated 12 extracts, three were found to have significant antiplasmodial activity with IC50values less than 4 µg/ml, namely the water extracts ofA. fruticosa,A. indicaandD. socotrana. Six extracts showed moderate activity with IC50values ranging from 10 to 30 µg/ml and three appeared to be inactive with IC50values more than 30 µg/ml. In addition, preliminary phytochemical screening of the methanolic and aqueous extracts indicated the presence of saponins, tannins, flavonoids, terpenoids, polysaccharides and peptides.

Effective Antimalarial Activities of α-Hydroxy Diynes Isolated from Ongokea gore

Planta Medica ◽  
2018 ◽  
Vol 84 (11) ◽  
pp. 806-812 ◽  
Author(s):  
Joséphine Ntumba ◽  
Christian Tshiongo ◽  
Michel Mifundu ◽  
Raphäel Robiette ◽  
Kalulu Taba
Keyword(s):  
Seed Oil ◽  
Antimalarial Activity ◽  
World Health ◽  
Diphenyltetrazolium Bromide ◽  
The World ◽  
Health Organization ◽  
Structure Assignment ◽  
Drug Reference

AbstractThree diynes, octadec-17-ene-9,11-diynoate ethyl (1), 8-hydroxy-octadeca-13,17-diene-9,11-diynoate ethyl (2), and 8-hydroxy-octadec-13-ene-9,11-diynoate ethyl (3), were isolated from Ongokea gore seed oil. The structure assignment of these three compounds was based according to chemical and spectroscopic data. They were screened against Plasmodium falciparum, the parasite that causes malaria. In vitro micro-test (Mark III, supported by the World Health Organization) was developed to assess the response of P. falciparum to the isolated three compounds, and statistical analysis were performed for determination of the concentration that inhibits 50% of the parasite maturation (IC50). Two of the three diynes (2 and 3) showed a very effective in vitro antimalarial activity with an IC50 of 4.5 and 1.7 µM, respectively. Compound 3 exhibited better activity than quinine (IC50 1.9 µM), the drug reference, while compound 1 had no antimalarial activity (IC50 > 125 µM). In the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) cytotoxicity screening, all compounds showed no toxicity (mean IC50 of 90 µM for each compound).

scholarly journals RNA Vaccines in Cancer Treatment

2010 ◽  
Vol 2010 ◽  
pp. 1-12 ◽  
Author(s):  
Anita Bringmann ◽  
Stefanie Andrea Erika Held ◽  
Annkristin Heine ◽  
Peter Brossart
Keyword(s):  
Immune Responses ◽  
World Health ◽  
Western World ◽  
Death Rates ◽  
Specific Strategy ◽  
The World ◽  
Health Organization ◽  
Year 2000 ◽  
Death Cases

The Cancer Report from the World Health Organization states that in the year 2000 12% of all death cases worldwide were caused by cancer. In the western world, the cancer death rates are often devastating, being at about 25%. This fact stresses the urgency to find effective cures against malignant diseases. New approaches in the treatment of cancer focus on the development of immunotherapies to fight the disease. Besides other methods, the usage of tumor-specific RNA as part of vaccines is investigated lately. RNA, administered alone or used for transfection of dendritic cells, shows several advantages as a vaccine including feasibility, applicability, safeness, and effectiveness when it comes to the generation of immune responses. This review concentrates on results from in vitro experiments and recent trials using RNA vaccines to present an overview about this specific strategy.

Natural products from the traditional Moroccan pharmacopoeia: A potential lead for the prevention and treatment of COVID-19

2020 ◽  
Vol 11 (SPL1) ◽  
pp. 1278-1285
Author(s):  
Mohamed Yafout ◽  
Amine Ousaid ◽  
Ibrahim Sbai El Otmani ◽  
Youssef Khayati ◽  
Amal Ait Haj Said
Keyword(s):  
Medicinal Plants ◽  
Plant Extracts ◽  
Molecular Mechanisms ◽  
Scientific Literature ◽  
Treatment Protocol ◽  
World Health ◽  
The World ◽  
Health Organization ◽  
Promising Source

The new SARS-CoV-2 belonging to the coronaviruses family has caused a pandemic affecting millions of people around the world. This pandemic has been declared by the World Health Organization as an international public health emergency. Although several clinical trials involving a large number of drugs are currently underway, no treatment protocol for COVID-19 has been officially approved so far. Here we demonstrate through a search in the scientific literature that the traditional Moroccan pharmacopoeia, which includes more than 500 medicinal plants, is a fascinating and promising source for the research of natural molecules active against SARS-CoV-2. Multiple in-silico and in-vitro studies showed that some of the medicinal plants used by Moroccans for centuries possess inhibitory activity against SARS-CoV or SARS-CoV-2. These inhibitory activities are achieved through the different molecular mechanisms of virus penetration and replication, or indirectly through stimulation of immunity. Thus, the potential of plants, plant extracts and molecules derived from plants that are traditionally used in Morocco and have activity against SARS-CoV-2, could be explored in the search for a preventive or curative treatment against COVID-19. Furthermore, safe plants or plant extracts that are proven to stimulate immunity could be officially recommended by governments as nutritional supplements.

Treatment Options in COVID-19: The Role of Bioavailable Antiviral Ribonucleoside Analog on NHC in vitro

2020 ◽  
Author(s):  
Lara Bittmann
Keyword(s):  
World Health Organization ◽  
Clinical Picture ◽  
Treatment Options ◽  
World Health ◽  
Wuhan City ◽  
The World ◽  
Novel Coronavirus ◽  
Health Organization

On December 31, 2019, WHO was informed of cases of pneumonia of unknown cause in Wuhan City, China. A novel coronavirus was identified as the cause by Chinese authorities on January 7, 2020 and was provisionally named "2019-nCoV". This new Coronavirus causes a clinical picture which has received now the name COVID-19. The virus has spread subsequently worldwide and was explained on the 11th of March, 2020 by the World Health Organization to the pandemic.

Antimicrobial peptides for the treatment of pulmonary tuberculosis, allies or foes?

2018 ◽  
Vol 24 (10) ◽  
pp. 1138-1147
Author(s):  
Bruno Rivas-Santiago ◽  
Flor Torres-Juarez
Keyword(s):  
Pulmonary Tuberculosis ◽  
Antimicrobial Peptides ◽  
Experimental Models ◽  
New Drugs ◽  
World Health ◽  
Public Health Issue ◽  
Health Organization ◽  
Drug Resistant Strains

Tuberculosis is an ancient disease that has become a serious public health issue in recent years, although increasing incidence has been controlled, deaths caused by Mycobacterium tuberculosis have been accentuated due to the emerging of multi-drug resistant strains and the comorbidity with diabetes mellitus and HIV. This situation is threatening the goals of World Health Organization (WHO) to eradicate tuberculosis in 2035. WHO has called for the creation of new drugs as an alternative for the treatment of pulmonary tuberculosis, among the plausible molecules that can be used are the Antimicrobial Peptides (AMPs). These peptides have demonstrated remarkable efficacy to kill mycobacteria in vitro and in vivo in experimental models, nevertheless, these peptides not only have antimicrobial activity but also have a wide variety of functions such as angiogenesis, wound healing, immunomodulation and other well-described roles into the human physiology. Therapeutic strategies for tuberculosis using AMPs must be well thought prior to their clinical use; evaluating comorbidities, family history and risk factors to other diseases, since the wide function of AMPs, they could lead to collateral undesirable effects.

Detoxifying Action of Aqueous Extracts of Mucuna pruriens Seed and Mimosa pudica Root Against Venoms of Naja nigricollis and Bitis arietans

2020 ◽  
Vol 14 (2) ◽  
pp. 134-144 ◽  
Author(s):  
Matthew P. Ameh ◽  
Mamman Mohammed ◽  
Yusuf P. Ofemile ◽  
Magaji G. Mohammed ◽  
Ada Gabriel ◽  
...  
Keyword(s):  
Phospholipase A2 ◽  
Plant Extracts ◽  
Fibrinolytic Activity ◽  
Neglected Tropical Diseases ◽  
World Health ◽  
Mucuna Pruriens ◽  
Phytochemical Analysis ◽  
Mimosa Pudica ◽  
Health Organization

Background: The World Health Organization included snakebite envenomation among Neglected Tropical Diseases in 2017. The importance of natural products from plants is enormous, given that most prescribed drugs originate from plants. Among this is Mucuna pruriens and Mimosa pudica, with many registered patents asserting their health benefits. Objective: This study investigated the in vitro neutralizing effects of Mucuna pruriens seed and Mimosa pudica root extracts on venoms of Naja nigricollis and Bitis arietans. Methods: In mice, the LD50 and phytochemical analysis of M. pruriens and M. pudica plant extracts were carried out prior to the evaluation of their haemolytic and fibrinolytic effect. Their effects on the activities of phospholipase A2 (PLA2) were also assessed. Results: At a concentration of 50 mg/ml, both plant extracts were found to neutralize the fibrinolytic activity of N. nigricollis, but 400 mg/ml was required to neutralize the fibrinolytic activity of B. arietans. In haemolytic studies, 50 mg/ml concentration of M. pruriens extract suppressed haemolysis caused by N. nigricollis venom by 70% but at the same concentration, M. pudica extract reduced haemolysis by 49.4%. M. pruriens, at 50 mg/ml concentration, only inhibited phospholipase A2 activity by 7.7% but higher concentrations up to 400mg/ml had no effect against the venom of N. nigricollis; at 200 mg/ml. M. pudica extract inhibited PLA2 activity by 23%. Conclusion: The results suggest that M. pruriens and M. pudica may be considered as promising antivenom agents for people living in a snake-bite prone environment.

ARIMA model for forecasting COVID-19 Death cases in India (Preprint)

2020 ◽  
Author(s):  
Jeya Sutha M
Keyword(s):  
Arima Model ◽  
Public Health Emergency ◽  
World Health ◽  
The People ◽  
The World ◽  
The Status ◽  
The Government ◽  
Health Organization ◽  
Spread Of Infection ◽  
Death Cases

UNSTRUCTURED COVID-19, the disease caused by a novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), is a highly contagious disease. On January 30, 2020 the World Health Organization declared the outbreak as a Public Health Emergency of International Concern. As of July 25, 2020; 15,947,292 laboratory-confirmed and 642,814 deaths have been reported globally. India has reported 1,338,928 confirmed cases and 31,412 deaths till date. This paper presents different aspects of COVID-19, visualization of the spread of infection and presents the ARIMA model for forecasting the status of COVID-19 death cases in the next 50 days in order to take necessary precaution by the Government to save the people.

scholarly journals Localization of ferrochelatase in Plasmodium falciparum

2004 ◽  
Vol 384 (2) ◽  
pp. 429-436 ◽  
Author(s):  
Sundaramurthy VARADHARAJAN ◽  
B. K. Chandrashekar SAGAR ◽  
Pundi N. RANGARAJAN ◽  
Govindarajan PADMANABAN
Keyword(s):  
Plasmodium Falciparum ◽  
De Novo ◽  
Enzymic Activity ◽  
Malarial Parasite ◽  
Parasite Genome ◽  
Marker Proteins ◽  
Parasite Plasmodium ◽  
Theoretical Predictions ◽  
Parasite Plasmodium Falciparum

Our previous studies have demonstrated de novo haem biosynthesis in the malarial parasite (Plasmodium falciparum and P. berghei). It has also been shown that the first enzyme of the pathway is the parasite genome-coded ALA (δ-aminolaevulinate) synthase localized in the parasite mitochondrion, whereas the second enzyme, ALAD (ALA dehydratase), is accounted for by two species: one species imported from the host red blood cell into the parasite cytosol and another parasite genome-coded species in the apicoplast. In the present study, specific antibodies have been raised to PfFC (parasite genome-coded ferrochelatase), the terminal enzyme of the haem-biosynthetic pathway, using recombinant truncated protein. With the use of these antibodies as well as those against the hFC (host red cell ferrochelatase) and other marker proteins, immunofluorescence studies were performed. The results reveal that P. falciparum in culture manifests a broad distribution of hFC and a localized distribution of PfFC in the parasite. However, PfFC is not localized to the parasite mitochondrion. Immunoelectron-microscopy studies reveal that PfFC is indeed localized to the apicoplast, whereas hFC is distributed in the parasite cytoplasm. These results on the localization of PfFC are unexpected and are at variance with theoretical predictions based on leader sequence analysis. Biochemical studies using the parasite cytosolic and organellar fractions reveal that the cytosol containing hFC accounts for 80% of FC enzymic activity, whereas the organellar fraction containing PfFC accounts for the remaining 20%. Interestingly, both the isolated cytosolic and organellar fractions are capable of independent haem synthesis in vitro from [4-14C]ALA, with the cytosol being three times more efficient compared with the organellar fraction. With [2-14C]glycine, most of the haem is synthesized in the organellar fraction. Thus haem is synthesized in two independent compartments: in the cytosol, using the imported host enzymes, and in the organellar fractions, using the parasite genome-coded enzymes.

scholarly journals Virtual Screening and Statistical Analysis in the Design of New Caffeine Analogues Molecules with Potential Epithelial Anticancer Activity

2018 ◽  
Vol 24 (5) ◽  
pp. 576-594 ◽  
Author(s):  
Josivan da Silva Costa ◽  
Karina da Silva Lopes Costa ◽  
Josiane Viana Cruz ◽  
Ryan da Silva Ramos ◽  
Luciane Barros Silva ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Binding Free Energy ◽  
Inhibitory Effect ◽  
Parametric Models ◽  
World Health ◽  
Pharmacokinetic Properties ◽  
Clinically Significant ◽  
Health Organization

About 132 thousand cases of melanoma (more severe type of skin cancer) were registered in 2014 according to the World Health Organization. This type of cancer significantly affects the quality of life of individuals. Caffeine has shown potential inhibitory effect against epithelial cancer. In this study, it was proposed to obtain new caffeine-based molecules with potential epithelial anticancer activity. For this, a training set of 21 molecules was used for pharmacophore perception procedures. Multiple linear regression analyses were used to propose mono-, bi-, tri-, and tetra-parametric models applied in the prediction of the activity. The generated pharmacophore was used to select 350 molecules available at the ZINCpharmer server, followed by reduction to 24 molecules, after selection using the Tanimoto index, yielding 10 molecules after final selection by predicted activity values > 1.5229. These ten molecules had better pharmacokinetic properties than the other ones used as reference and within the clinically significant limits. Only two molecules show minor hits of toxicity and were submitted to molecular docking procedures, showing BFE (binding free energy) values lower than the reference values. Statistical analyses indicated strong negative correlations between BFE and pharmacophoric properties (high influence on BFE lowering) and practically null correlation between BFE and BBB. The two most promising molecules can be indicated as candidates for further in vitro and in vivo analyzes.

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