scholarly journals Natural Products: A Potential Source of Malaria Transmission Blocking Drugs?

2020 ◽  
Vol 13 (9) ◽  
pp. 251
Author(s):  
Phanankosi Moyo ◽  
Grace Mugumbate ◽  
Jacobus N. Eloff ◽  
Abraham I. Louw ◽  
Vinesh J. Maharaj ◽  
...  
Keyword(s):  
Natural Products ◽  
Mosquito Vector ◽  
Blocking Drug ◽  
Transmission Blocking ◽  
Antimalarial Agents ◽  
Challenges And Opportunities ◽  
Sexual Stages ◽  
Derivatives Of ◽  
Effective Transmission ◽  
Potential Use

The ability to block human-to-mosquito and mosquito-to-human transmission of Plasmodium parasites is fundamental to accomplish the ambitious goal of malaria elimination. The WHO currently recommends only primaquine as a transmission-blocking drug but its use is severely restricted by toxicity in some populations. New, safe and clinically effective transmission-blocking drugs therefore need to be discovered. While natural products have been extensively investigated for the development of chemotherapeutic antimalarial agents, their potential use as transmission-blocking drugs is comparatively poorly explored. Here, we provide a comprehensive summary of the activities of natural products (and their derivatives) of plant and microbial origins against sexual stages of Plasmodium parasites and the Anopheles mosquito vector. We identify the prevailing challenges and opportunities and suggest how these can be mitigated and/or exploited in an endeavor to expedite transmission-blocking drug discovery efforts from natural products.

Recent advances in transmission-blocking drugs for malaria elimination

2019 ◽  
Vol 11 (23) ◽  
pp. 3047-3088 ◽  
Author(s):  
Ishan Wadi ◽  
Mahendra Nath ◽  
Anupkumar R Anvikar ◽  
Pargat Singh ◽  
Abhinav Sinha
Keyword(s):  
Malaria Elimination ◽  
Scientific Community ◽  
Antimalarial Drugs ◽  
Clinical Development ◽  
Therapeutic Interventions ◽  
Blocking Drug ◽  
Transmission Blocking ◽  
Block Transmission ◽  
Effective Transmission ◽  
Novel Therapeutic

The scientific community worldwide has realized that malaria elimination will not be possible without development of safe and effective transmission-blocking interventions. Primaquine, the only WHO recommended transmission-blocking drug, is not extensively utilized because of the toxicity issues in G6PD deficient individuals. Therefore, there is an urgent need to develop novel therapeutic interventions that can target malaria parasites and effectively block transmission. But at first, it is imperative to unravel the existing portfolio of transmission-blocking drugs. This review highlights transmission-blocking potential of current antimalarial drugs and drugs that are in various stages of clinical development. The collective analysis of the relationships between the structure and the activity of transmission-blocking drugs is expected to help in the design of new transmission-blocking antimalarials.

scholarly journals Sexual Development in Non-Human Parasitic Apicomplexa: Just Biology or Targets for Control?

Animals ◽  
2021 ◽  
Vol 11 (10) ◽  
pp. 2891
Author(s):  
Teresa Cruz-Bustos ◽  
Anna Sophia Feix ◽  
Bärbel Ruttkowski ◽  
Anja Joachim
Keyword(s):  
Sexual Reproduction ◽  
Sexual Development ◽  
Current Knowledge ◽  
Life Cycles ◽  
Complex Life Cycles ◽  
Transmission Blocking ◽  
New Hosts ◽  
Sexual Stages ◽  
New Generation ◽  
Effective Transmission

The phylum Apicomplexa is a major group of protozoan parasites including gregarines, coccidia, haemogregarines, haemosporidia and piroplasms, with more than 6000 named species. Three of these subgroups, the coccidia, hemosporidia, and piroplasms, contain parasites that cause important diseases of humans and animals worldwide. All of them have complex life cycles involving a switch between asexual and sexual reproduction, which is key to their development. Fertilization (i.e., fusion of female and male cells) results in the formation of a zygote that undergoes meiosis, forming a new generation of asexual stages. In eukaryotes, sexual reproduction is the predominant mode of recombination and segregation of DNA. Sex is well documented in many protist groups, and together with meiosis, is frequently linked with transmission to new hosts. Apicomplexan sexual stages constitute a bottleneck in the life cycle of these parasites, as they are obligatory for the development of new transmissible stages. Consequently, the sexual stages represent attractive targets for vaccination. Detailed understanding of apicomplexan sexual biology will pave the way for the design and implementation of effective transmission-blocking strategies for parasite control. This article reviews the current knowledge on the sexual development of Apicomplexa and the progress in transmission-blocking vaccines for their control, their advantages and limitations and outstanding questions for the future.

scholarly journals Biguanide-Based Synthesis of 1,3,5-Triazine Derivatives with Anticancer Activity and 1,3,5-Triazine Incorporated Calcium Citrate Nanoparticles

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1028
Author(s):  
Monnaya Chalermnon ◽  
Sarocha Cherdchom ◽  
Amornpun Sereemaspun ◽  
Rojrit Rojanathanes ◽  
Tanatorn Khotavivattana
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Anticancer Agent ◽  
Drug Loading ◽  
Calcium Citrate ◽  
Colorectal Cancer Cell Lines ◽  
Triazine Derivatives ◽  
Further Development ◽  
Derivatives Of ◽  
Potential Use

Twelve derivatives of biguanide-derived 1,3,5-triazines, a promising class of anticancer agent, were synthesised and evaluated for their anticancer activity against two colorectal cancer cell lines—HCT116 and SW620. 2c and 3c which are the derivatives containing o-hydroxyphenyl substituents exhibited the highest activity with IC50 against both cell lines in the range of 20–27 µM, which is comparable to the IC50 of cisplatin reference. Moreover, the potential use of the calcium citrate nanoparticles (CaCit NPs) as a platform for drug delivery system was studied on a selected 1,3,5-triazine derivative 2a. Condition optimisation revealed that the source of citrate ions and reaction time significantly influence the morphology, size and %drug loading of the particles. With the optimised conditions, “CaCit-2a NPs” were successfully synthesised with the size of 148 ± 23 nm and %drug loading of up to 16.3%. Furthermore, it was found that the release of 2a from the synthesised CaCit-2a NPs is pH-responsive, and 2a could be control released under the acidic cancer environment. The knowledge from this study is perceptive for further development of the 1,3,5-triazine-based anticancer drugs and provide the platform for the incorporation of other drugs in the CaCit NPs in the future.

Advancements in capturing and mining mass spectrometry data are transforming natural products research

2021 ◽  
Author(s):  
Scott A. Jarmusch ◽  
Justin J. J. van der Hooft ◽  
Pieter C. Dorrestein ◽  
Alan K. Jarmusch
Keyword(s):  
Mass Spectrometry ◽  
Data Mining ◽  
Natural Products ◽  
Data Analysis ◽  
Community Participation ◽  
Mass Spectrometry Data ◽  
Metabolomics Data ◽  
Analysis Tools ◽  
Public Data ◽  
Potential Use

This review covers the current and potential use of mass spectrometry-based metabolomics data mining in natural products. Public data, metadata, databases and data analysis tools are critical. The value and success of data mining rely on community participation.

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