Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin

Zuma, Nonkululeko H.; Smit, Frans J.; Kock, Carmen de; Combrinck, Jill M.; Smith, Peter J.; N’Da, David D.

doi:10.1016/j.ejmech.2016.07.027

Cited by 17 publications

(12 citation statements)

References 33 publications

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“…Malaria is a serious parasitic disease that has been spreading all over the world but mainly in Africa [ 1 ]. Artemisinin (ART), a peroxide-containing sesquiterpene lactone [ 2 , 3 ], is currently the most widely used and most effective anti-malarial drug [ 4 , 5 ]. It shows strong activity against malaria due to Plasmodium falciparum (a unicellular protozoan parasite that is the deadliest species of malaria-causing Plasmodium in humans) and plays a key role in the treatment and continuous control of malaria worldwide [ 6 ].…”

Section: Introductionmentioning

confidence: 99%

Electrospun Nanofibers of Polycaprolactone/Collagen as a Sustained-Release Drug Delivery System for Artemisinin

et al. 2021

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The application of artemisinin (ART) in the treatment of malaria has been restricted to a certain degree due to its inherent limitations, such as short half-life, poor solubility, limited bioavailability, and re-crystallization. Electrospun nanofibers loaded with ART provide an excellent solution to these limitations and yield sustained drug release as well as inhibition of drug re-crystallization. In this study, ART-loaded polycaprolactone (PCL)/collagen (Col) nanofibers with different proportions of polymers were prepared. ART-loaded PCL/Col nanofibers were characterized, and further ART anti-crystallization and release behaviors were studied. SEM was used to observe the morphology of PCL/Col nanofibers. X-ray diffraction (XRD) was used to characterize the physical state of ART in ART-loaded PCL/Col nanofibers. Fourier transform infrared spectroscopy (FTIR), water contact angle measurement, weight loss, degree of swelling, and drug release experiments can verify the differences in performance of ART-loaded PCL/Col nanofibers due to different polymer ratios. The release curve was analyzed by kinetics, showing sustained release for up to 48 h, and followed the Fickian release mechanism, which was shown by the diffusion index value obtained from the Korsmeyer-Peppas equation.

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Section: Introductionmentioning

confidence: 99%

Electrospun Nanofibers of Polycaprolactone/Collagen as a Sustained-Release Drug Delivery System for Artemisinin

et al. 2021

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“…The additive effects of ARSs in combined administration with immunosuppressants and the structure-activity relationship need to be further clarified. Investigation of the improved properties of ARSs analogs also facilitates the discovery of novel drug targets for kidney disease (Santos et al, 2015;Zuma et al, 2016;de Lange et al, 2018).…”

Section: Discussionmentioning

confidence: 99%

The Therapeutic Effect of Artemisinin and Its Derivatives in Kidney Disease

Xia

Liu

et al. 2020

Front. Pharmacol.

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Artemisinin (ARS) and its derivatives (ARSs) are recommended as the first-line antimalarial drugs for the treatment of malaria. Besides antimalarial function, its potent antiinflammatory and immunoregulatory properties, as well as the ability to regulate oxidative stress have brought them to a prominent position. As researchers around the world are continually exploring the unknown biological activities of ARS derivatives, experimental studies have shown much progress in renal therapy. This review aims to give a brief overview of the current research on ARSs applications for kidney treatment with the evaluation of therapeutic properties and potential molecular mechanisms.

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“…In an extension to the theme of modifying the artemisinin lactone ring, Zuma et al., generated a series of ester‐containing compounds, tethered to a truncated D‐ring (e. g., 43 ). While these compounds are yet to be assessed for improved metabolic stability, they did maintain excellent in vitro anti‐plasmodial activity, therefore providing an additional artemisinin derived scaffold which can be exploited to develop new antimalarials …”

Section: Antimalarial Agentsmentioning

confidence: 99%

Recent Highlights in Anti‐infective Medicinal Chemistry from South Africa

Veale

Müller

2020

ChemMedChem

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Global advancements in biological technologies have vastly increased the variety of and accessibility to bioassay platforms, while simultaneously improving our understanding of druggable chemical space. In the South African context, this has resulted in a rapid expansion in the number of medicinal chemistry programmes currently operating, particularly on university campuses. Furthermore, the modern medicinal chemist has the advantage of being able to incorporate data from numerous related disciplines into the medicinal chemistry process, allowing for informed molecular design to play a far greater role than previously possible. Accordingly, this review focusses on recent highlights in drug-discovery programmes, in which South African medicinal chemistry groups have played a substantive role in the design and optimisation of biologically active compounds which contribute to the search for promising agents for infectious disease.

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Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin

Cited by 17 publications

References 33 publications

Electrospun Nanofibers of Polycaprolactone/Collagen as a Sustained-Release Drug Delivery System for Artemisinin

Electrospun Nanofibers of Polycaprolactone/Collagen as a Sustained-Release Drug Delivery System for Artemisinin

The Therapeutic Effect of Artemisinin and Its Derivatives in Kidney Disease

Recent Highlights in Anti‐infective Medicinal Chemistry from South Africa

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