Endemic in 149 tropical and subtropical countries, neglected tropical diseases (NTDs) affect more than 1 billion people annually, including 875 million children in developing economies. These diseases are also responsible for over 500,000 deaths per year and are characterized by long-term disability and severe pain. The impact of the combined NTDs closely rivals that of malaria and tuberculosis. Current treatment options are associated with various limitations including widespread drug resistance, severe adverse effects, lengthy treatment duration, unfavorable toxicity profiles, and complicated drug administration procedures. Natural products have been a valuable source of drug regimens that form the cornerstone of modern pharmaceutical care. In this review, we highlight the potential that remains untapped in natural products as drug leads for NTDs. We cover natural products from plant, marine, and microbial sources including natural-product-inspired semi-synthetic derivatives which have been evaluated against the various causative agents of NTDs. Our coverage is limited to four major NTDs which include human African trypanosomiasis (sleeping sickness), leishmaniasis, schistosomiasis and lymphatic filariasis.

Structure-activity relationship studies and Plasmodium life cycle profiling identifies panactive N-aryl-3-trifluoromethyl pyrido[1,2a]benzimidazoles which are efficacious in an in vivo mouse model of malaria.

The extensive use of praziquantel against schistosomiasis raises concerns about drug resistance. New therapeutic alternatives targeting critical pathways within the parasite are therefore urgently needed. Hemozoin formation in Schistosoma presents one such target. We assessed the in vitro antischistosomal activity of pyrido[1,2-a]benzimidazoles (PBIs) and investigated correlations with their ability to inhibit β-hematin formation. We further evaluated the in vivo efficacy of representative compounds in experimental mice and conducted pharmacokinetic analysis on the most potent. At 10 μM, 48/57 compounds resulted in >70% mortality of newly transformed schistosomula, whereas 37 of these maintained >60% mortality of adult S. mansoni. No correlations were observed between β-hematin inhibitory and antischistosomal activities against both larval and adult parasites, suggesting possible presence of other target(s) or a mode of inhibition of crystal formation that is not adequately modeled by the assay. The most active compound in vivo showed 58.7 and 61.3% total and female worm burden reduction, respectively. Pharmacokinetic analysis suggested solubility-limited absorption and high hepatic clearance as possible contributors to the modest efficacy despite good in vitro activity. The PBIs evaluated in this report thus merit further optimization to improve their efficacy and to elucidate their possible mode of action.

We have previously reported on the antischistosomal activity of pyrido[1,2-a]benzimidazole (PBI) derivatives. As a follow-up, we designed and prosecuted further structure−activity relationship (SAR) studies that incorporate N-aryl substitutions on the PBI scaffold. Investigations into the in vitro antischistosomal activity against newly transformed schistosomula (NTS) and adult worms revealed several leads with promising potency. Active compounds with a good cytotoxicity profile were tested in vivo whereby 6 and 44 induced noteworthy reduction (62−69%) in the worm load in the Schistosoma mansoni mouse model. Pharmacokinetic analysis on 44 pointed to slow absorption, low volume of distribution, and low plasma clearance indicating the potential of these compounds to achieve a long duration of action. Overall, our work demonstrates that PBI chemotype is a promising scaffold in the discovery of new antischistosomal leads.

Background: Virtual learning platforms gained unprecedented prominence after the coronavirus disease 2019 (COVID-19) outbreak. Assuring the quality of education and student satisfaction are critical, especially in developing countries often plagued with infrastructural limitations, including information technology. Objectives: This study was conducted to assess the perceptions of students at a Kenyan Pharmacy School of online learning with regards to affordability and overall effectiveness. Methods: A cross-sectional study was conducted using an online survey containing pre-determined questions aligned to achieve the research objectives. Results: Students in senior classes (Fifth year) viewed online learning more favourably and had fewer challenges with accessibility than students in the lower classes (First year to third year). Conclusion: The study identified areas of strength, such as convenience, time-efficiency, and self-initiative, as well as weaknesses, including inequitable access, internet connectivity challenges, and unsatisfactory lecturer digital competency, with relation to online learning.

Background: The downward trend in malaria cases and deaths is steadily reversed – 627,000 deaths in 2020 compared to 405,000 deaths in 2018. Drug resistance has compromised the effectiveness of currently available treatment options, with some reports documenting molecular markers of resistance to artemisinins in African countries in addition to the Greater Mekong subregion, which was initially associated with this kind of resistance. Therefore, the development of novel drugs is crucial to replenishing the antimalarial drug arsenal toward malaria eradication. In this review, we summarize the progress made in antimalarial drug discovery in the period 2000 – 2022, focusing on drug candidates which have made it to advanced preclinical trials (drugs tested in rodent species and at least one higher species such as dog or monkey) and beyond. Method: We searched Google Scholar and selected studies meeting these defined criteria. We highlight the medicinal chemistry optimization of these compounds; the preclinical/clinical evaluation and the mechanisms of action. Results and conclusion: Although the pipeline seems promising, the prospect of having an antimalarial medicine that meets the current target product profiles (TPPs) towards the malaria eradication agenda is far from reality. Some of the key TPP attributes required include multistage activity, resistance-proof; ability to achieve a single dose cure and safety across a wide range of patient populations. Clinical trials are ongoing for some promising molecules, inspiring optimism toward identifying better drugs that meet these defined TPPs. Until then, concerted research efforts should continue to be mounted to populate the antimalarial drug discovery and development pipeline.

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Numerous limitations encountered with mainstream Western Medicine, including exorbitant costs, side effects, ineffectiveness and unavailability continue to endear many to alternative herbal therapies. The World Health Organization recognizes the rampant use of herbal medicine, stating that over 80% of the global population uses this form of therapy either alone or alongside conventional therapies. In Kenya, herbal medicine is popular, and, in this review, we share a situational analysis of the industry, taking note of the opportunities and challenges that it offers. Importantly, we provide, in our opinion, easy to implement and financially friendly approaches towards improving the safety and appeal of herbal medicine practice in the country. We anticipate that the Kenyan scenario is replicated elsewhere across the continent and that, therefore, these insights may be similarly applicable.