scholarly journals α-d-Glucopyranosyl-(1→2)-[6-O-(l-tryptophanyl)-β-d-fructofuranoside]

Molbank ◽  
10.3390/m1066 ◽  
2019 ◽  
Vol 2019 (2) ◽  
pp. M1066
Author(s):  
Kwaku Kyeremeh ◽  
Samuel Kwain ◽  
Gilbert Mawuli Tetevi ◽  
Anil Sazak Camas ◽  
Mustafa Camas ◽  
...  

The Mycobacterium sp. BRS2A-AR2 is an endophyte of the mangrove plant Rhizophora racemosa G. Mey., which grows along the banks of the River Butre, in the Western Region of Ghana. Chemical profiling using 1H-NMR and HRESI-LC-MS of fermentation extracts produced by the strain led to the isolation of the new compound, α-d-Glucopyranosyl-(1→2)-[6-O-(l-tryptophanyl)-β-d–fructofuranoside] or simply tortomycoglycoside (1). Compound 1 is an aminoglycoside consisting of a tryptophan moiety esterified to a disaccharide made up of β-d-fructofuranose and α-d-glucopyranose sugars. The full structure of 1 was determined using UV, IR, 1D, 2D-NMR and HRESI-LC-MS data. When tested against Trypanosoma brucei subsp. brucei, the parasite responsible for Human African Trypanosomiasis in sub-Saharan Africa, 1 (IC50 11.25 µM) was just as effective as Coptis japonica (Thunb.) Makino. (IC50 8.20 µM). The extract of Coptis japonica (Thunb.) Makino. is routinely used as laboratory standard due to its powerful antitrypanosomal activity. It is possible that, compound 1 interferes with the normal uptake and metabolism of tryptophan in the T. brucei subsp. brucei parasite.

Molbank ◽  
10.3390/m1070 ◽  
2019 ◽  
Vol 2019 (3) ◽  
pp. M1070 ◽  
Author(s):  
Dofuor ◽  
Kwain ◽  
Osei ◽  
Tetevi ◽  
Okine ◽  
...  

The plant Zanthoxylum zanthoxyloides (Lam.) Zepern. & Timler is one of the most important medicinal species of the genus Zanthoxylum on the African continent. It is used in the treatment and management of parasitic diseases in sub-Saharan Africa. These properties have inspired scientists to investigate species within the genus for bioactive compounds. However, a study, which details a spectroscopic, spectrometric and bioactivity guided extraction and isolation of antiparasitic compounds from the genus Zanthoxylum is currently non-existent. Tortozanthoxylamide (1), which is a derivative of the known compound armatamide was isolated from Z. zanthoxyloides and the full structure determined using UV, IR, 1D/2D-NMR and high-resolution liquid chromatography tandem mass spectrometry (HRESI-LC-MS) data. When tested against Trypanosoma brucei subsp. brucei, the parasite responsible for animal African trypanosomiasis in sub-Saharan Africa, 1 (IC50 7.78 µM) was just four times less active than the commercially available drug diminazene aceturate (IC50 1.88 µM). Diminazene aceturate is a potent drug for the treatment of animal African trypanosomiasis. Tortozanthoxylamide (1) exhibits a significant antitrypanosomal activity through remarkable alteration of the cell cycle in T. brucei subsp. brucei, but it is selectively non-toxic to mouse macrophages RAW 264.7 cell lines. This suggests that 1 may be considered as a scaffold for the further development of natural antitrypanosomal compounds.


2021 ◽  
Vol 01 ◽  
Author(s):  
Napoleon A. Mfonku ◽  
Gabriel T. Kamsu ◽  
Norbert Kodjio ◽  
Jie Ren ◽  
James A. Mbah ◽  
...  

Background: Typhoid fever is a major health burden in Sub-Saharan Africa. Conventional anti-typhoid drugs are becoming more and more unavailable to most patients in Africa due to the increased costs and emerging drug resistance. Therefore, there is a need for discovery of new antimicrobial agents to combat typhoid fever. Objective: This work aimed to investigate the bioactive components in Cyperus sphacelatus Rottb. (Cyperaceae) and test the antisalmonellal activity of the isolated compounds. Methods: Compound purification was done through column chromatography. Structure elucidation was accomplished based on the 1D and 2D NMR, IR and mass spectra. The biological assay was done using five bacterial strains, including Salmonella enterica subsp. enterica sérovars Typhi ATCC 6539 (STS), S. enterica subsp. enterica sérovars Typhi (ST), S. enteritidis (STE), S. enterica subsp. enterica sérovars Typhimurim (STM), and a resistant isolate of S. enterica subsp. enterica sérovars Typhi (ST566). Results: Three natural products were isolated from the methylene chloride extract of the rhizomes of C. sphacelatus, including a new furanoquinone, scabequinon-6(14)-ene (1) and two known compounds, cyperotundone (2) and vanillin (3). Compound 1 showed moderate antisalmonellal activity, with a minimal inhibitory concentration (MIC) of 32 µg/mL against STM and STS. The best inhibitory result was obtained with compound 2 on STM with a MIC of 8 µg/mL. Compound 2 also gave the best minimum bactericidal concentration (MBC) of 32 µg/mL on the STM strain. Conclusion: Discovery of the three antisalmonellal compounds from C. sphacelatus supports the addition of this plant to typhoid fever preparations.


2009 ◽  
Vol 2009 ◽  
pp. 1-5 ◽  
Author(s):  
Cyrus J. Bacchi

Human Africa trypanosomiasis is a centuries-old disease which has disrupted sub-Saharan Africa in both physical suffering and economic loss. This article presents an update of classic chemotherapeutic agents, in use for >50 years and the recent development of promising non-toxic combination chemotherapy suitable for use in rural clinics.


2019 ◽  
Vol 6 (6) ◽  
pp. e610 ◽  
Author(s):  
Jean Rodgers ◽  
Israel Steiner ◽  
Peter G. E Kennedy

Human African trypanosomiasis (HAT) is caused by infection due to protozoan parasites of the Trypanosoma genus and is a major fatal disease throughout sub-Saharan Africa. After an early hemolymphatic stage in which the peripheral tissues are infected, the parasites enter the CNS causing a constellation of neurologic features. Although the CNS stage of HAT has been recognized for over a century, the mechanisms generating the neuroinflammatory response are complex and not well understood. Therefore a better understanding of the mechanisms utilized by the parasites to gain access to the CNS compartment is critical to explaining the generation of neuroinflammation. Contrast-enhanced MRI in a murine model of HAT has shown an early and progressive deterioration of blood-CNS barrier function after trypanosome infection that can be reversed following curative treatment. However, further studies are required to clarify the molecules involved in this process. Another important determinant of brain inflammation is the delicate balance of proinflammatory and counterinflammatory mediators. In mouse models of HAT, proinflammatory mediators such as tumor necrosis factor (TNF)-α, interferon (IFN)-γ, and CXCL10 have been shown to be crucial to parasite CNS invasion while administration of interleukin (IL)-10, a counter inflammatory molecule, reduces the CNS parasite burden as well as the severity of the neuroinflammatory response and the clinical symptoms associated with the infection. This review focuses on information, gained from both infected human samples and animal models of HAT, with an emphasis on parasite CNS invasion and the development of neuroinflammation.


2019 ◽  
Vol 4 (2) ◽  
pp. e001173 ◽  
Author(s):  
C Simone Sutherland ◽  
Fabrizio Tediosi

IntroductionProgramme to eliminate neglected tropical diseases (NTDs) have gained global recognition, and may allow for improvements to universal health coverage and poverty alleviation. It is hoped that elimination of human African trypanosomiasis (HAT) Trypanosoma brucei gambiense (Tbg) would assist in this goal, but the financial costs are still unknown. The objective of this analysis was to forecast the financial burden of direct costs of HAT Tbg to funders and society.MethodsIn order to estimate the total costs to health services and individuals: (1) potential elimination programmes were defined; (2) the direct costs of programmes were calculated; (3) the per case out-of-pocket payments (OOPs) by programme and financial risk protection indicators were estimated. The total estimated costs for control and elimination programme were reported up till 2020 in international dollars. The mean results for both direct programme costs and OOPs were calculated and reported along with 95% CIs.ResultsAcross sub-Saharan Africa, HAT Tbg maintaining ‘Control’ would lead to a decline in cases and cost US$630.6 million. In comparison, the cost of ‘Elimination’ programme ranged from US$410.9 million to US$1.2 billion. Maintaining ‘Control’ would continue to cause impoverishment and financial hardship to households; while all ‘Elimination’ programme would lead to significant reductions in poverty.ConclusionOverall, the total costs of either control or elimination programme would be near US$1 billion in the next decade. However, only elimination programme will reduce the number of cases and improve financial risk protection for households who are impacted by HAT Tbg.


Biology ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 1150
Author(s):  
Ruobing Zhou ◽  
Yuan Gao ◽  
Nan Chang ◽  
Tai Gao ◽  
Delong Ma ◽  
...  

Glossina morsitans is a vector for Human African Trypanosomiasis (HAT), which is mainly distributed in sub-Saharan Africa at present. Our objective was to project the historical and future potentially suitable areas globally and explore the influence of climatic factors. The maximum entropy model (MaxEnt) was utilized to evaluate the contribution rates of bio-climatic factors and to project suitable habitats for G. morsitans. We found that Isothermality and Precipitation of Wettest Quarter contributed most to the distribution of G. morsitans. The predicted potentially suitable areas for G. morsitans under historical climate conditions would be 14.5 million km2, including a large area of Africa which is near and below the equator, small equatorial regions of southern Asia, America, and Oceania. Under future climate conditions, the potentially suitable areas are expected to decline by about −5.38 ± 1.00% overall, under all shared socioeconomic pathways, compared with 1970–2000. The potentially suitable habitats of G. morsitans may not be limited to Africa. Necessary surveillance and preventive measures should be taken in high-risk regions.


2012 ◽  
Vol 2012 ◽  
pp. 1-9 ◽  
Author(s):  
Enock Matovu ◽  
Anne Juliet Kazibwe ◽  
Claire Mack Mugasa ◽  
Joseph Mathu Ndungu ◽  
Zablon Kithingi Njiru

Human African trypanosomiasis is a debilitating disease prevalent in rural sub-Saharan Africa. Control of this disease almost exclusively relies on chemotherapy that should be driven by accurate diagnosis, given the unacceptable toxicity of the few available drugs. Unfortunately, the available diagnostics are characterised by low sensitivities due to the inherent low parasitaemia in natural infections. Demonstration of the trypanosomes in body fluids, which is a prerequisite before treatment, often follows complex algorithms. In this paper, we review the available diagnostics and explore recent advances towards development of novel point-of-care diagnostic tests.


Author(s):  
Justin Brown

Human African Trypanosomiasis (HAT) threatens more than 55 million people in sub-Saharan Africa. The focus of this paper is the relationship that exists between ethnomedical and biomedical practitioners regarding treatment of HAT. The relationship has been one of conflict. Biomedical practitioners have attempted to remove ethnomedicine from African society. This practice has been unsuccessful, especially in rural regions. Ethnomedical practitioners have adopted some aspects of biomedicine, but inadequate application and resources limit their efficacy. The biomedical community, including the World Health Organization, has not recognized the resource potential within ethnomedicine. An examination of the areas of conflict reveals differences in the explanatory models of disease causation and treatment methods. There has been some progress toward a cooperative model of healthcare, but most biomedical practitioners disregard ethnomedical techniques as primitive and ineffective. The conclusion of this paper presents a bleak future for the prevention and treatment of HAT in Africa. This future may be avoided with an increased level of cooperation and understanding between the two systems.


eLife ◽  
2017 ◽  
Vol 6 ◽  
Author(s):  
Anneli Cooper ◽  
Hamidou Ilboudo ◽  
V Pius Alibu ◽  
Sophie Ravel ◽  
John Enyaru ◽  
...  

Reduced susceptibility to infectious disease can increase the frequency of otherwise deleterious alleles. In populations of African ancestry, two apolipoprotein-L1 (APOL1) variants with a recessive kidney disease risk, named G1 and G2, occur at high frequency. APOL1 is a trypanolytic protein that confers innate resistance to most African trypanosomes, but not Trypanosoma brucei rhodesiense or T.b. gambiense, which cause human African trypanosomiasis. In this case-control study, we test the prevailing hypothesis that these APOL1 variants reduce trypanosomiasis susceptibility, resulting in their positive selection in sub-Saharan Africa. We demonstrate a five-fold dominant protective association for G2 against T.b. rhodesiense infection. Furthermore, we report unpredicted strong opposing associations with T.b. gambiense disease outcome. G2 associates with faster progression of T.b. gambiense trypanosomiasis, while G1 associates with asymptomatic carriage and undetectable parasitemia. These results implicate both forms of human African trypanosomiasis in the selection and persistence of otherwise detrimental APOL1 kidney disease variants.


2017 ◽  
Vol 1 (6) ◽  
pp. 533-537
Author(s):  
Lorenz von Seidlein ◽  
Borimas Hanboonkunupakarn ◽  
Podjanee Jittmala ◽  
Sasithon Pukrittayakamee

RTS,S/AS01 is the most advanced vaccine to prevent malaria. It is safe and moderately effective. A large pivotal phase III trial in over 15 000 young children in sub-Saharan Africa completed in 2014 showed that the vaccine could protect around one-third of children (aged 5–17 months) and one-fourth of infants (aged 6–12 weeks) from uncomplicated falciparum malaria. The European Medicines Agency approved licensing and programmatic roll-out of the RTSS vaccine in malaria endemic countries in sub-Saharan Africa. WHO is planning further studies in a large Malaria Vaccine Implementation Programme, in more than 400 000 young African children. With the changing malaria epidemiology in Africa resulting in older children at risk, alternative modes of employment are under evaluation, for example the use of RTS,S/AS01 in older children as part of seasonal malaria prophylaxis. Another strategy is combining mass drug administrations with mass vaccine campaigns for all age groups in regional malaria elimination campaigns. A phase II trial is ongoing to evaluate the safety and immunogenicity of the RTSS in combination with antimalarial drugs in Thailand. Such novel approaches aim to extract the maximum benefit from the well-documented, short-lasting protective efficacy of RTS,S/AS01.


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