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Human African trypanosomiasis, or sleeping sickness, is a neglected tropical disease caused by Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense and is invariably fatal unless treated. Current therapies present limitations in their application, parasite resistance, or require further clinical investigation for wider use. Our work, informed by previous findings, presents novel 4-[4-(4-methylpiperazin-1-yl)phenyl]-6-arylpyrimidine derivatives with promising antitrypanosomal activity. In particular, 32 exhibits an in vitro EC50 value of 0.5 µM against Trypanosoma brucei rhodesiense, and analogues 29, 30 and 33 show antitrypanosomal activities in the

Fluazuron is a novel veterinary pour-on antitick formulation which can be applied simultaneously with bovine reproduction management strategies. Considering the economic importance of the livestock industry in many countries, it is important to know whether antiparasitics such as fluazuron may cause embryonic loss. The aim of this study was to evaluate the toxicological effect of fluazuron on bovine oocytes during in vitro maturation. The best fluazuron concentrations were determined in a preliminary experiment on Chinese hamster ovary (CHO)-K1 cells and further used to compare fluazuron toxicity in both study models. Results of the annexin V and alkaline single cell gel electrophoresis assays demonstrated that fluazuron caused cytotoxicity and genotoxicity in bovine cumulus cells at all the concentrations tested (50, 75 and 100 μg fluazuron/mL). The evaluation of cortical granules and mitochondria distribution showed that cytoplasmic maturation was not affected by fluazuron treatment. However, a decrease in metaphase II + polar body, degenerate oocytes as well as disorganized chromatin in polar body were observed at all concentrations tested. Whereas the fertilization process was not altered by 50 μg/mL fluazuron, the embryo development rate decreased significantly. No significant differences were observed in any of the oxidative stress parameters assessed. This study contributes to a better understanding of fluazuron in bovines, suggesting that the antiparasitic may affect bovine reproduction and might cause embryo loss. • Fluazuron induces genotoxicity in CHO-K1 and genotoxicity and apoptosis in cumulus cells. • Fluazuron reduces metaphase II and polar body (PB) formation, degenerates oocytes, and disorganizes PB chromatin. • Embryo development rate decreased significantly after cumulus-oocyte cells exposure to 50 μg fluazuron/mL. • Fluazuron does not alter the oxidative stress parameters assessed in bovine cumulus cells and oocytes. [ABSTRACT FROM AUTHOR]

Background: This study aimed to investigate the antiparasitic and anti-inflammatory potential of pumpkin seed oil in mice infected with Trichinella spiralis by demonstrating its impact on MMP-9 expression and pathogenesis during the intestinal and muscular phases. Results: In this study, 100 mice were divided into five groups: an infected group, a pumpkin seed oil-treated group (1.5 mg/kg BW, administered three times per week), an albendazole-treated group, a native control group, and a pumpkin oil control group. Gas chromatography–mass spectrometry analysis of the pumpkin seed oil revealed a broad spectrum of biologically active compounds. The pumpkin seed oil treatment led to a significant reduction in the parasite burden, with a 75% decrease in adult worms and a 66% decrease in encysted larvae. Additionally, the infected animals treated with pumpkin oil exhibited a marked reduction in intestinal inflammation, characterized by a progressive increase in goblet cells. The number of encysted larvae in the diaphragm and muscle tissues was also significantly decreased. Furthermore, pumpkin seed oil treatment significantly reduced MMP-9 levels in both intestinal and muscular tissues, highlighting its potential to attenuate inflammation. Conclusion: These findings underscore the effectiveness of pumpkin seed oil as anti-inflammatory and antiparasitic agent. [ABSTRACT FROM AUTHOR]

Context: Ivermectin (IVM) and moxidectin (MOX), are widely used internal and external antiparasitic drugs for livestock. They enter into the aquatic environment because the treated animals metabolise only a small percentage of the administered doses, and the rest is eliminated through the faeces posing a risk to aquatic organisms. Aims: This study aimed to evaluate the responses of zooplankton to environmentally relevant concentrations of IVM and MOX spiked in cattle dung in a short-term exposure. Methods: We compared the composition of the community, density, species richness, diversity and total biomass between treatments with parasiticides and controls. Key results: The presence of both antiparasitic drugs altered the zooplankton community structure, leading to a shift in species composition. Cladocerans were the most affected, with a drastic reduction in their density. Additionally, a decrease in the density of copepods and an increase in the density of rotifers were observed in the MOX treatments. Conclusions: Both drugs caused a simplification of the zooplankton community as species richness and diversity decreased. Overall, MOX was more toxic than IVM. Implications: Our results suggest that long-term consequences on ecosystem services could arise, which merits the development of control and livestock management tools for the protection of these environments. Popular antiparasitic drugs for livestock, ivermectin and moxidectin, are posing threats to aquatic ecosystems. In a brief laboratory study, we investigated their impact on zooplankton when administered through cattle dung. Results showed a disruption in zooplankton communities, with moxidectin being more toxic. These findings could have serious implications for long-term ecosystem health, emphasising the urgent need for protective measures and sustainable livestock management practices. (Image credit: Camila J. Lorente.) [ABSTRACT FROM AUTHOR]

Cannabis sativa L. has garnered attention as a potential source for new antimicrobial agents, particularly due to the increased prevalence of microbial resistance to conventional antimicrobials and the emergence of multidrug-resistant pathogens. This review, conducted according to the PRISMA 2020 statement, systematically analyzed the antimicrobial properties of C. sativa extracts and cannabinoids against various bacteria, fungi, viruses, and parasites. Data were collected from the scientific literature (102 papers) and clinical trials (5 studies) from 2014 to June 2024. Findings revealed that cannabinoids, especially CBD, demonstrate significant antimicrobial activity against Gram-positive bacteria like MRSA, Gram-negative bacteria such as Pseudomonas aeruginosa, various Candida species, SARS-CoV-2, and HIV. Additionally, CBD showed efficacy against parasitic infections like Echinococcus granulosus and Leishmania species. These results suggest that cannabinoids may represent a new class of antimicrobial agents with unique and diverse mechanisms of action, potentially effective in broad-spectrum therapies. This study highlights the urgent need for further research and standardized clinical trials to validate these findings and to develop cannabinoid-based treatments. The antimicrobial properties of C. sativa align with WHO priorities and support global health initiatives, offering promising avenues for addressing antimicrobial resistance and improving public health outcomes. [ABSTRACT FROM AUTHOR]

Background/Objectives: Leishmaniasis, a neglected disease caused by Leishmania spp. including L. amazonensis, urgently requires new treatments. Polyalthic acid (PA), a natural diterpene from Copaifera spp., has previously demonstrated significant antiparasitic potential. This study evaluated the leishmanicidal effects of polyalthic acid (PA), alone and with amphotericin B (AmpB), on L. amazonensis promastigote and amastigote forms. Results: PA showed significant activity against promastigotes, with 50% effective concentration (EC50) values of 2.01 μM at 24 h and an EC50 of 3.22 μM against amastigotes after 48 h. The PA and AmpB combination exhibited a synergistic effect on both forms without inducing cytotoxicity or hemolysis. Morphological changes in promastigotes, including vacuole formation and cell rounding, were more pronounced with the combination. Conclusions: These findings suggest that PA and AmpB together could form a promising new treatment strategy against Leishmania infections, offering enhanced efficacy without added toxicity. [ABSTRACT FROM AUTHOR]

Neglected tropical diseases (NTDs) are a group of at least 20 infectious diseases that primarily affect tropical regions. Despite impacting 1.6 billion people worldwide, these diseases have not received adequate global priority and attention. Currently, NTDs caused by protozoa have limited therapeutic options, and the emergence of drug-resistant strains further exacerbates the situation. In recent years, several antimicrobial peptides (AMPs) have emerged as potential therapeutic candidates against NTDs. This review analyzes the contemporary trends of AMPs, explores their antiparasitic properties, and mechanisms of action against three parasitic protozoan NTDs: Chagas disease, human African trypanosomiasis, and leishmaniasis and one parasitic helminth NTD: lymphatic filariasis. Furthermore, notable drawbacks associated with AMPs are highlighted, and future research directions are proposed. Overall, this review points out the potential of AMPs as therapeutic agents for these three protozoan neglected tropical diseases and one parasitic helminth NTDs as well as emphasizes the imperative need for continued research in this field. [ABSTRACT FROM AUTHOR]

Abstract Background This study aimed to investigate the antiparasitic and anti-inflammatory potential of pumpkin seed oil in mice infected with Trichinella spiralis by demonstrating its impact on MMP-9 expression and pathogenesis during the intestinal and muscular phases. Results In this study, 100 mice were divided into five groups: an infected group, a pumpkin seed oil-treated group (1.5 mg/kg BW, administered three times per week), an albendazole-treated group, a native control group, and a pumpkin oil control group. Gas chromatography–mass spectrometry analysis of the pumpkin seed oil revealed a broad spectrum of biologically active compounds. The pumpkin seed oil treatment led to a significant reduction in the parasite burden, with a 75% decrease in adult worms and a 66% decrease in encysted larvae. Additionally, the infected animals treated with pumpkin oil exhibited a marked reduction in intestinal inflammation, characterized by a progressive increase in goblet cells. The number of encysted larvae in the diaphragm and muscle tissues was also significantly decreased. Furthermore, pumpkin seed oil treatment significantly reduced MMP-9 levels in both intestinal and muscular tissues, highlighting its potential to attenuate inflammation. Conclusion These findings underscore the effectiveness of pumpkin seed oil as anti-inflammatory and antiparasitic agent.

The present study evaluated the parasite activity of aqueous extracts (AE) of neem leaves (Azadirachta indica) on parasitized Nile tilapia (Oreochromis niloticus). Concurrent infection with Dactylogyrus sp. and Centrocestus formosanus metacercariae was observed after clinical and parasitological investigations. A 240 Nile tilapia fish represented the four groups in the experimental design. They were used to assess the efficiency of aqueous extracts (long bath, 7 days) against parasite-infested fish: the group without A. indica extract (control, T1), T2 (1.0 g/L), T3 (2.0 g/L), and T4 (3.0 g/L). Results revealed that neem extract groups reduced the mean intensity of parasites (Dactylogyrus sp., C. formosanus) more than the control group partially at T4 (3.0 g/L). Fish exposed to neem leaf extracts showed significant downregulation of inflammatory and pro-inflammatory and immune genes (IL-1ß, IL-8; IL-10, Cox-2, lysozyme, C3, and HSP70) along with a significant increase in antioxidative genes (SOD and CAT) partially at T4 (3 g/L). Histological examinations of fish liver and gill tissues exposed to neem extract showed a return to normal histoarchitecture, especially at T4. However, antioxidant (CAT and GSH) activities increased in gill and liver tissues exposed to A. indica extract, especially at T4. Compared to control fish, the MDA levels decreased significantly in fish treated with A. indica extract, partially in the T4 group. Immune indices (complement 3, nitric oxide, and lysozyme activity) of infected fish treated with A. indica leaves extract displayed the highest value compared to the control one, especially at T4. The study assumed that an aqueous extract of A. indica inclusion at the rate of 3.0 g/L in a long-term bath is recommended to increase the resistance against parasitic infection and improve Nile tilapia's health welfare. [ABSTRACT FROM AUTHOR]

Abstract The growing global threat of antimicrobial resistance endangers both human and animal life, necessitating the urgent discovery of novel antimicrobial solutions. Medicinal plants hold promise as sources of potential antimicrobial compounds. In this study, we investigated the phytochemical constituents and microbicidal capabilities of the ethanolic extract from Nigella sativa (black seed). Gas chromatography analysis (GC) identified 11 compounds, among them thymoquinone, and thymol, contributing to antimicrobial and antioxidant properties. Antimicrobial assays demonstrated notable inhibition zones against broad spectra of bacteria, including Pseudomonas aeruginosa, Escherichia coli, Salmonella typhi, Staphylococcus aureus, Enterobacter, and Bacillus subtilis, along with potent antifungal activity against Aspergillus niger, Penicillium, and Candida albicans. Notably, when combined with antibiotics, the extract displayed exceptional synergistic antimicrobial efficacy. The black seed extract demonstrated membrane-damaging activity and disrupted virulence factors that protect microbes from antimicrobial agents, including the formation of bacterial biofilm and protease secretion. Thymoquinone, the primary active constituent of the extract, exhibited similar antimicrobial and ant virulence properties. In silico analysis targeting key regulators of quorum sensing and biofilm formation in P. aeruginosa, such as RhlG, LasR, and PqsR, showed a remarkable affinity of thymol and thymoquinone for these targets. Moreover, the N. sativa extract exhibited dose-dependent cytotoxicity against both the promastigote and amastigote forms of Leishmania tropica parasites, hinting at potential antiparasitic activity. In addition to its antimicrobial properties, the extract displayed potential antioxidant activity at a concentration of 400 μg/mL.

The growing global threat of antimicrobial resistance endangers both human and animal life, necessitating the urgent discovery of novel antimicrobial solutions. Medicinal plants hold promise as sources of potential antimicrobial compounds. In this study, we investigated the phytochemical constituents and microbicidal capabilities of the ethanolic extract from Nigella sativa (black seed). Gas chromatography analysis (GC) identified 11 compounds, among them thymoquinone, and thymol, contributing to antimicrobial and antioxidant properties. Antimicrobial assays demonstrated notable inhibition zones against broad spectra of bacteria, including Pseudomonas aeruginosa, Escherichia coli, Salmonella typhi, Staphylococcus aureus, Enterobacter, and Bacillus subtilis, along with potent antifungal activity against Aspergillus niger, Penicillium, and Candida albicans. Notably, when combined with antibiotics, the extract displayed exceptional synergistic antimicrobial efficacy. The black seed extract demonstrated membrane-damaging activity and disrupted virulence factors that protect microbes from antimicrobial agents, including the formation of bacterial biofilm and protease secretion. Thymoquinone, the primary active constituent of the extract, exhibited similar antimicrobial and ant virulence properties. In silico analysis targeting key regulators of quorum sensing and biofilm formation in P. aeruginosa, such as RhlG, LasR, and PqsR, showed a remarkable affinity of thymol and thymoquinone for these targets. Moreover, the N. sativa extract exhibited dose-dependent cytotoxicity against both the promastigote and amastigote forms of Leishmania tropica parasites, hinting at potential antiparasitic activity. In addition to its antimicrobial properties, the extract displayed potential antioxidant activity at a concentration of 400 μg/mL. [ABSTRACT FROM AUTHOR]

Trichodina species can cause extensive fish mortality in an aquaculture system, and extensive use of commercial drugs affects the environment and health. The bacterial zinc nanoparticles (BZN) synthesized using Bacillus subtilis MS20 could be a suitable alternative to antiparasitic drugs. This work evaluates the antiparasitic properties of BZN against Trichodina heterodentata in Nile tilapia (Oreochromis niloticus). Furthermore, it explores BZN's effects on fish health, including growth performance, immunity, and microbial load. The BZN were 45nm in size and negatively charged at -23.6 meV. A total of 180 fish were divided into six groups. G1-G4 were non-trichodina-infected groups fed a diet supplemented with 0, 100, 200, and 500 mg/kg of BZN, the G5 was Trichodina-infected fish, and G6 was Trichodina-infected fish and treated with BZN (500 mg/kg). Fish were carefully observed for clinical alterations and mortalities. Blood and tissue samples were collected from different groups. Survival rates were 100% in the groups (G1-G4), 56.67% (G5), and 88 % (G6). The Trichodina-challenged group showed bad performance, especially in the survival rate (56 %) and body weight gain, lower erythrogram (Hb, RBCs, however, higher PCV%, which may indicate the inflammation in fish tissue), significant hypoglycemia, higher ALP activity and ammonia but lower protein content and significant increases were observed in serum amyloid A (SAA) and interleukin-6 (IL-6) values. Applying BZN 500 mg/kg to the challenged group maintains the parameters to control levels and alleviates the effect of Trichodina species infection. The histopathology of liver tissues supported the blood biochemistry results. The Trichodina-challenged fish showed extensive vacuolar degeneration of hepatocytes and massive necrosis of the pancreas hyperplastic proliferation of the epithelial lining of the secondary lamellae; meanwhile, BZN-treated groups showed normal liver and gill tissue structure. The BZN treatment significantly reduced the total bacterial count by 31-45% and Aeromonas count by 30-44%. Finally, it is concluded that using BZN 500 mg/kg significantly mitigates the Trichodina heterodentata infection in Nile Tilapia (Oreochromis niloticus) and enhances fish health. [ABSTRACT FROM AUTHOR]

Cryptosporidium parvum (C. parvum) is one of the most prevalent species infecting humans and animals. Currently, the only FDA-licensed drug to treat cryptosporidiosis is nitazoxanide (NTZ), with no efficacy in immunocompromised hosts. Citrus paradisi (C. paradisi) has demonstrated anti-protozoal activities. This study aimed to investigate the anti-cryptosporidiosis effect of C. paradisi peel extract, either alone or in mediating the green synthesis of chitosan silver nanoparticles (Cs/Ag NPs), compared to NTZ. Mice were sorted into nine different groups. The effectiveness of the treatments was evaluated using parasitology, histopathology, immunohistochemistry, and immunology. C. paradisi outperformed nitazoxanide regarding oocyst shedding (79% vs. 61%). The effectiveness of NTZ Cs/Ag NPs and Citrus Cs/Ag NPs was enhanced to 78% and 91%, respectively. The highest oocyst inhibition was obtained by combining NTZ and Citrus Cs/Ag NPs (96%). NF-κB, TNF-α, and Il-10 levels increased in response to infection and decreased in response to various treatments, with the highest reduction in the group treated with combined NTZ citrus Cs/Ag NPs. Combining C. paradisi with NTZ could have a synergistic effect, making it a potentially effective anti-cryptosporidiosis agent. Utilizing C. paradisi in the green synthesis of Cs/Ag NPs improves the therapeutic response and can be used to produce novel therapeutic antiparasitic drugs. [ABSTRACT FROM AUTHOR]

Brazil is home to some of the world's greatest biodiversity, providing an immeasurable number of new opportunities and unexplored sources of native plants for the development of products, extracts, foods, and compounds of social and economic interest. Among these, plants of the genus Eugenia stand out because of the large number of species found in Brazilian territory, many of which are endemic and exclusive to Brazil. These plants have emerged as potential sources for obtaining essential oils with relevant biological activities. In this context, the present review provides an overview of essential oils derived from the main native plants of Brazilian socio-biodiversity from the genus Eugenia with food value (Eugenia stipitata, Eugenia dysenterica, Eugenia involucrata, Eugenia brasiliensis, Eugenia klotzschiana, Eugenia uniflora, and Eugenia pyriformis) and their phytochemical profile and health beneficial effects. The compiled data showed that the essential oils of these plants are composed mainly of sesquiterpenes and, in smaller quantities, monoterpenes and other compounds. These compounds contribute to different biological activities, including antimicrobial, antioxidant, anticancer, and antiparasitic effects. These findings demonstrate that the essential oils of Brazilian native plants of the genus Eugenia can be a promising raw material for active ingredients to develop innovative and sustainable food products, drugs, and cosmetics. [ABSTRACT FROM AUTHOR]

Secondary metabolites produced by the fermentation of Streptomyces avermitilis bacterium are powerful antiparasitic agents used in animal health, agriculture and human infection treatments. Avermectin is a macrocyclic lactone with four structural components (A1, A2, B1, B2), each of them containing a major and a minor subcomponent, out of which avermectin B1a is the most effective parasitic control compound. Avermectin B1a produces two homologue avermectins (B1 and B2) that have been used in agriculture as pesticides and antiparasitic agents, since 1985. It has a great affinity with the Cl-channels of the glutamate receptor, allowing the constant flow of Cl- ions into the nerve cells, causing a phenomenon of hyperpolarization causing death by flaccid paralysis. The purpose of this work was to gather information on the production of avermectins and their biocidal effects, with special emphasis on their role in the control of pests and phytopathogenic diseases. The literature showed that S. avermitilis is an important producer of macrocyclic lactones with biocidal properties. In addition, avermectin contributes to the control of ectoparasites and endoparasites in human health care, veterinary medicine and agriculture. Importantly, avermectin is a compound that is harmless to the host (no side effects), non-target organisms and the environment. [ABSTRACT FROM AUTHOR]

Distributed throughout the environment are various microorganisms such as bacteria, fungi, parasites, and viruses. Although many are part of the human microbiome, many are pathogenic and cause infections ranging from mild to severe. In recent years, the identification of multidrug-resistant microorganisms has become a serious public health problem. The resulting infections call into question the therapeutic capacity of health systems and lead to approximately 70,000 deaths annually worldwide. The progressive resistance to antibiotics and antifungals has been a major challenge for the medical and pharmaceutical community, requiring the search for new compounds with antimicrobial properties. Several studies have demonstrated the potential of natural and synthesized flavonoids, especially the dimers of these molecules. In this review are presented many examples of dimeric flavonoids that have demonstrated antimicrobial activity against viruses, like influenza and Human Immunodeficiency Virus (HIV), protozoal infections, such as Leishmaniasis and Malaria, fungal infections by Candida albicans and Cryptococcus neoformans, and bacterial infections caused, for example, by Staphylococcus aureus and Escherichia coli. In the pursuit to find potential safe agents for therapy in microbial infections, natural dimeric flavonoids are an option not only for the antimicrobial activity, but also for the low toxicity usually associated with these compounds when compared to classic antimicrobials. [ABSTRACT FROM AUTHOR]

Visceral leishmaniasis (VL) is among the most neglected tropical diseases in the world. Drug cell permeability is essential for killing the intracellular residing parasites responsible for VL, making cell-permeating peptides a logical choice to address VL. Unfortunately, the limited biological stability of peptides restricts their usage. Sequence-specific oligo-N-substituted glycines ('peptoids') are a class of peptide mimics that offers an excellent alternative to peptides in terms of ease of synthesis and good biostability. We tested peptoids against the parasite Leishmania donovani in both forms, that is, intracellular amastigotes and promastigotes. N-alkyl hydrophobic chain addition (lipidation) and bromination of oligopeptoids yielded compounds with good antileishmanial activity against both forms, showing the promise of these antiparasitic peptoids as potential drug candidates to treat VL.

Aquaculture serves as a source of protein and livelihood and is an alternative to capture fisheries, thereby reducing pressure on the wild. However, aquaculture tends to be limited by sustainability issues, which include overdependency on fishmeal, the high cost associated with fishmeal, the environmental impact of aquaculture activities, which may be detrimental to aquatic lives and the environment, and the use of antibiotics to treat diseases, which may have an adverse effect in their host or the environment. Efforts are being made toward attaining practical ways to enhance aquaculture sustainability. One such effort is using functional feed additives in feed formulation. Functional feed additives are dietary ingredients incorporated in feed formulations, not only for the usual provision of basic nutritional requirements as offered by traditional feed but also for growth and health enhancement; environmental and economic gain. This review emphasizes the importance of incorporating functional feed additives such as probiotics, prebiotics, symbiotics, and phytogenics. This study evaluates and presents holistic information on functional additives, their roles in enhancing aquaculture sustainability, and the challenges encountered in their application. [ABSTRACT FROM AUTHOR]

Ferroptosis is an iron-dependent form of regulated cell death characterized by glutathione (GSH) depletion, glutathione peroxidase 4 (GPX4) inactivation, and the build-up of lipotoxic reactive species. Ferroptosis-targeted induction is a promising therapeutic approach for addressing antimalarial drug resistance. In addition to being the primary source of intracellular energy supply and reactive oxygen species (ROS) generation, mitochondria actively participate in diverse forms of regulated cell death, including ferroptosis. Altered mitochondrial morphology and functionality are attributed to ferroptosis. Diverse mitochondria-related proteins and metabolic activities have been implicated in fine-tuning the action of ferroptosis inducers. Herein, we review recent progress in this evolving field, elucidating the numerous mechanisms by which mitochondria regulate ferroptosis and giving an insight into the role of the organelle in ferroptosis. Additionally, we present an overview of how mitochondria contribute to ferroptosis in malaria. Furthermore, we attempt to shed light on an inclusive perspective on how targeting malaria parasites' mitochondrion and attacking redox homeostasis is anticipated to induce ferroptosis-mediated antiparasitic effects. [ABSTRACT FROM AUTHOR]

Chalcones are polyphenols that belong to the flavonoids family, known for their broad pharmacological properties. They have thus attracted the attention of chemists for their obtention and potential activities. In our study, a library of compounds from 2′-hydroxychalcone's family was first synthesized. A one-step mechanochemical synthesis via Claisen–Schmidt condensation reaction under ball mill conditions was studied, first in a model reaction between a 5′-fluoro-2′-hydroxyacetophenone and 3,4-dimethoxybenzaldehyde. The reaction was optimized in terms of catalysts, ratio of reagents, reaction time, and influence of additives. Among all assays, we retained the best one, which gave the highest yield of 96% when operating in the presence of 1 + 1 eq. of substituted benzaldehyde and 2 eq. of KOH under two grinding cycles of 30 min. Thus, this protocol was adopted for the synthesis of the selected library of 2′-hydroxychalcones derivatives. The biological activities of 17 compounds were then assessed against Plasmodium falciparum, Leishmania donovani parasite development, as well as IGR-39 melanoma cell lines by inhibiting their viability and proliferation. Compounds 6 and 11 are the most potent against L. donovani, exhibiting IC50 values of 2.33 µM and 2.82 µM, respectively, better than the reference drug Miltefosine (3.66 µM). Compound 15 presented the most interesting antimalarial activity against the 3D7 strain, with IC50 = 3.21 µM. Finally, chalcone 12 gave the best result against IGR-39 melanoma cell lines, with an IC50 value of 12 µM better than the reference drug Dacarbazine (IC50 = 25 µM). [ABSTRACT FROM AUTHOR]

The aim of the present study was to evaluate and compare the chemical composition, antimicrobial, antiparasitic, and cytotoxic properties of the essential oils extracted from Rhanterium adpressum Coss. & Dur. (EORA) and Rhanterium suaveolens Desf. (EORS). The main compounds of EORA were myrcene (18.51%), α-pinene (14.36%), sabinene (13.55%), β-pinene (5.67%), and camphene (5.39%). While camphene (25.06%), α-pinene (13.14%), myrcene (9.74%), sabinene (8.27%), D-limonene (7.86%), and β-pinene (7.34%) constituted the major components of EORS. A potent antibacterial activity was also recorded against Escherichia coli with MIC = 5.72 mg/mL for EORA and MIC = 5.96 mg/mL for EORS. Concerning the antifungal effect, a remarkable efficiency was exerted against the two tested Candida albicans strains (MIC < 5.96 mg/mL) for EORS and against Candida albicans 26 (MIC = 5.72 mg/mL) for EORA. Furthermore, a promising antiparasitic ability was observed against Acanthamoeba castellanii (IC50 = 6.42±0.21 μg/mL) for EORS and against Leishmania amazonensis (IC50=9.66±1.46 μg/mL) for EORA. However, low cytotoxicity was recorded against macrophages J774-A1 (LC50 = 67.68±4.02 μg/mL) only for EORS. Based on the present findings, it may be concluded that the two tested EOs possess significant antimicrobial and antiparasitic activities with minimal cytotoxicity, so they can be used as new sources of antimicrobial and antiparasitic drugs. [ABSTRACT FROM AUTHOR]

In industrial aquaculture, producing at high stock densities is inevitable to maximize efficiency and harvest per unit volume. Antibiotics, disinfectants, and other chemicals have become necessary to prevent and control disease outbreaks in intensive fish farming practices. However, the negative impacts of the use of synthetic chemical drugs on environmental health have sparked discussions, making research into alternative treatments inevitable. Medicinal plants offer promising solutions for disease control due to their natural, biodegradable, and antimicrobial properties. The therapeutic properties of plants have been known and safely used in traditional medicine for a long time. The idea that medicinal plants can be utilized in aquaculture as a safer, sustainable, and environmentally friendly practice has begun to be embraced. Although numerous treatment protocols have been developed against metazoan parasites in aquaculture, managing protozoan parasites still poses a significant challenge. A detailed literature review has identified that more than 30 plant species have the potential to control many protozoan pathogens in fish, including Ichthyophthirius multifiliis and Cryptocaryon irritans. Studies highlight the effectiveness of plant-derived compounds in combating parasites and promoting growth, supporting immunity, serving as antibacterial agents, and even as anaesthetics. Since research on medicinal plants predominantly targets commercially valuable fish farming, there is a recognized need for expanded studies on their application in shellfish farming. Collaboration among researchers, institutions, and farmers is crucial in increasing awareness of local medicinal plants and promoting their use. The use of plants with medicinal properties in aquaculture represents a promising path for disease control and sustainable production. Adopting these natural alternatives could align with responsible agricultural practices and meet the urgent need to mitigate the environmental impacts of traditional treatments in the aquaculture industry. [ABSTRACT FROM AUTHOR]

The circular economy, which attempts to decrease agricultural waste while also improving sustainable development through the production of sustainable products from waste and by-products, is currently one of the main objectives of environmental research. Taking this view, this study used a green approach to synthesize two forms of silver nanoparticles: coated silver nanoparticles with olive leaf extract (Ag-olive) and uncoated pure silver nanoparticles (Ag-pure), which were produced by the calcination of Ag-olive at 550 °C. The extract and the fabricated nanoparticles were characterized by a variety of physicochemical techniques, including high-performance liquid chromatography (HPLC), thermal gravimetric analysis (TGA), X-ray diffraction (XRD), scanning electron microscopy (SEM), and transmission electron microscopy (TEM). Adult ticks (Hyalomma dromedarii) (Acari: Ixodidae) were used in this study to evaluate the antiparasitic activity of synthesized nanoparticles and extract. Furthermore, the antifungal activity was evaluated against Aspergillus aculeatus strain N (MW958085), Fuserium oxysporum (MT550034), and Alternaria tenuissiuma (MT550036). In both antiparasitic and antifungal tests, the as-synthesized Ag-olive showed higher inhibition activity than Ag-pure and olive leaf extract. The findings of this research suggest that Ag-olive may be a powerful and eco-friendly antiparasitic and antifungal agent. Ag-pure was also evaluated as a photocatalyst under sunlight for the detoxification of Eri-chrome-black T (EBT), methylene blue (MB), methyl orange (MO), and rhodamine B (RhB). [ABSTRACT FROM AUTHOR]

Background Parasitic infections challenge vertebrate health worldwide, and off-target effects of antiparasitic treatments may be an additional obstacle to recovery. However, there have been few investigations of the effects of antiparasitics on the gut microbiome in the absence of parasites. Methods We investigated whether two common antiparasitics—albendazole (ALB) and metronidazole (MTZ)—significantly alter the gut microbiome of parasite-free mice. We treated mice with ALB or MTZ daily for 7 days and sampled the fecal microbiota immediately before and after treatment and again after a two-week recovery period. Results ALB did not immediately change the gut microbiota, while MTZ decreased microbial richness by 8.5% and significantly changed community structure during treatment. The structural changes caused by MTZ included depletion of the beneficial family Lachnospiraceae, and predictive metagenomic analysis revealed that these losses likely depressed microbiome metabolic function. Separately, we compared the fecal microbiotas of treatment groups after recovery, and there were minor differences in community structure between the ALB, MTZ, and sham-treated control groups. Conclusions These results suggest that a healthy microbiome is resilient after MTZ-induced depletions of beneficial gut microbes, and ALB may cause slight, latent shifts in the microbiota but does not deplete healthy gut microbiota diversity. [ABSTRACT FROM AUTHOR]

Chagas disease, caused by the protozoan Trypanosoma cruzi, affects 6–7 million people worldwide. The dichloromethane extract obtained from the aerial parts of Gymnocoronis spilanthoides var subcordata showed trypanocidal activity in vitro. The fractionation of the dewaxed organic extract via column chromatography led to the isolation of three diterpenoids: ent-9α,11α-dihydroxy-15-oxo-kaur-16-en-19-oic acid or adenostemmoic acid B, (16R)-ent-11α-hydroxy-15-oxokauran-19-oic acid and ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic acid. These compounds showed IC50 values of 10.6, 15.9 and 4.8 µM against T. cruzi epimastigotes, respectively. When tested against amastigotes, the diterpenoids afforded IC50 values of 6.1, 19.5 and 60.6 µM, respectively. The cytotoxicity of the compounds was tested on mammalian cells using an MTT assay, resulting in CC50s of 321.8, 23.3 and 14.8 µM, respectively. The effect of adenostemmoic acid B on T. cruzi was examined at the ultrastructural level using transmission microscopy. Treatment with 20 μM for 48 h stimulated the formation of abnormal cytosolic membranous structures in the parasite. This compound also showed an anti-inflammatory effect in murine macrophages stimulated with LPS and other TLR agonists. Treatment of macrophages with adenostemmoic acid B was able to reduce TNF secretion and nitric oxide production, while increasing IL-10 production. The combination of adenostemmoic acid B with benznidazole resulted in greater inhibition of NF-kB and a decrease in nitrite concentration. The administration of adenostemmoic acid B to mice infected with trypomastigotes of T. cruzi at the dose of 1 mg/kg/day for five days produced a significant decrease in parasitemia levels and weight loss. Treatment with the association with benznidazole increased the survival time of the animals. In view of these results, adenostemmoic acid B could be considered a promising candidate for further studies in the search for new treatments for Chagas disease. [ABSTRACT FROM AUTHOR]

Currently, one of the primary challenges in salmon farming is caligidosis, caused by the copepod ectoparasites Caligus spp. The infection process is determined by the copepod's ability to adhere to the fish skin through the insertion of its chitin-composed filament. In this study, we examined several antimicrobial peptides previously identified in salmonid mucosal secretions, with a primary focus on their potential to bind to chitin as an initial step. The binding capacity to chitin was tested, with hepcidin and piscidin showing positive results. Further assessments involving cytotoxicity in salmonid cells RTgill-W1, SHK-1, RTS-11, and RT-gut indicated that the peptides did not adversely affect cell viability. However, hemolysis assays unveiled the hemolytic capacity of piscidin at lower concentrations, leading to the selection of hepcidin for antiparasitic assays. The results demonstrated that the nauplius II stage of C. rogercresseyi exhibited higher susceptibility to hepcidin treatments, achieving a 50% reduction in parasitic involvement at 50 µM. Utilizing fluorescence and scanning electron microscopy, we observed the localization of hepcidin on the surface of the parasite, inducing significant spherical protuberances along the exoskeleton of C. rogercresseyi. These findings suggest that cysteine-rich AMPs derived from fish mucosa possess the capability to alter the development of the chitin exoskeleton in copepod ectoparasites, making them therapeutic targets to combat recurrent parasitic diseases in salmon farming. [ABSTRACT FROM AUTHOR]

The search for new compounds that present low toxicity and high efficiency in the treatment of different diseases is a challenge. Therefore, this study brings as a novelty the synthesis, biological evaluation and a study of the mechanism of action in serum albumin of trimethoxy-benzylidene-hydrazine-carbothioamide compounds. The in silico results received that all compounds showed good oral availability and could be accepted as potential drug candidates. In cytotoxicity assays, the compounds promoted moderate to low toxicity against macrophage cells (82.90 ± 1.19 to 231.49 ± 1.96 µM) and Hepg2 (91.19 ± 1.09 to 254.64 ± 3.96 µM). In addition to not being hemolytic (< 10%). Regarding in vivo toxicity, they were not toxic in mice at a concentration of 2000 mg/kg (gavage). In in vitro biological assays, the compounds showed low antioxidant activity. The antifungal activity assays showed that the compounds were capable of inhibiting the growth of different strains of yeast. The compounds were also able to inhibit the growth of the parasite L. amazonensis in different promastigote (27.84–40.52 µM) and amastigote (29–49.71 µM) forms. Furthermore, they inhibited the growth of T.cruzi trypomastigotes (28.90–45.24 µM). Assays with albumin generally pleased that the compounds can be transported by these proteins without changes in the macromolecules. In this context, we can conclude that the compounds considered can promote different activities and can contribute to the arsenal of new drug candidate compounds that can act as new antifungal and antiparasitic agents. [ABSTRACT FROM AUTHOR]

Fish, as vertebrates, secrete various antimicrobial peptides (AMPs)—short, positively charged amino acid chains that are integral components of the innate immune systems across numerous species. AMPs exhibit a broad spectrum of inhibitory activities against viruses, fungi, bacteria, and parasites. The rise of antibiotic-resistant microorganisms and concerns over excessive antibiotic use has spurred interest in AMPs for their potential applications in aquaculture, medicine, food, agriculture, and animal husbandry. This study elucidates the potential of fish-derived AMPs as antibacterial, antiviral, anti-parasitic, and antifungal agents, as well as their roles as vaccine adjuvants, components of inactivated vaccines, anticancer agents, and methods for AMP isolation. The review concisely addresses the application-oriented properties of fish AMPs, emphasizing their broad-spectrum antimicrobial efficacy and practical utility.

Samia Q Alghamdi,1 NF Alotaibi,2 Sameera N Al-Ghamdi,3 Laila S Alqarni,4 Touseef Amna,1 Shaima MN Moustafa,5 Ibrahim Hotan Alsohaimi,2 IA Alruwaili,2 AM Nassar2 1Department of Biology, Faculty of Science, Al-Baha University, Al-Baha, 65799 Saudi Arabia; 2Chemistry Department, College of Science, Jouf University, Sakaka, Saudi Arabia; 3Chemistry Department, Faculty of Science, Al-Baha University, Al-Baha, Saudi Arabia; 4Chemistry Department, College of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh, 11623 Saudi Arabia; 5Biology Department, College of Science, Jouf University, Sakaka, Saudi ArabiaCorrespondence: AM Nassar, Jouf University, Sakaka, Aljouf, 2014, Saudi Arabia, Tel +966555978016, Email amnassar@ju.edu.saBackground: Nowadays, recycling agricultural waste is of the utmost importance in the world for the production of valuable bioactive compounds and environmental protection. Olive leaf bioactive compounds have a significant potential impact on the pharmaceutical industry. These compounds possess remarkable biological characteristics, including antimicrobial, antiviral, anti-inflammatory, hypoglycemic, and antioxidant properties.Methods: The present study demonstrates a green synthetic approach for the fabrication of nickel oxide nanoparticles (NiO-olive) using aqueous wasted olive leaf extract. Calcination of NiO-olive at 500°C led to the fabrication of pure NiO nanoparticles (NiO-pure). Different techniques, such as thermal gravimetric analysis (TGA), Fourier-transform infrared spectra (FTIR), ultraviolet-visible spectra (UV-Vis), X-ray diffraction (XRD), scanning electron microscopy (SEM) fitted with energy-dispersive X-ray analysis (EDX), and transmission electron microscopy (TEM), were used to characterize both NiO-olive and NiO-pure. The extract and nanoparticles were assessed for antiparasitic activity against adult ticks (Hyalomma dromedarii) and antimicrobial activity against Bacillus cereus, Pseudomonas aeruginosa, Aspergillus niger, and Candida albicans.Results: From XRD, the crystal sizes of NiO-olive and NiO-pure were 32.94 nm and 13.85 nm, respectively. TGA, FTIR, and EDX showed the presence of olive organic residues in NiO-olive and their absence in NiO-pure. SEM and TEM showed an asymmetrical structure of NiO-olive and a regular, semi-spherical structure of NiO-pure. UV–Vis spectra showed surface plasmon resonance of NPs. Antiparasitic activity showed the highest mortality rate of 95% observed at a concentration of 0.06 mg/mL after four days of incubation. The antimicrobial activity showed the largest inhibition zone diameter of 33 ± 0.2 mm against the Candida albicans strain.Conclusion: Nanoparticles of NiO-olive outperformed nanoparticles of NiO-pure and olive leaf extract in both antiparasitic and antimicrobial tests. These findings imply that NiO-olive may be widely used as an eco-friendly and effective antiparasitic and disinfection of sewage.Keywords: biosynthesis, olive, NiO-NP, antiparasitic, antimicrobial]

Leishmaniasis is a neglected tropical disease that has affected more than 350 million people worldwide and can manifest itself in three different forms: cutaneous, mucocutaneous, or visceral. Furthermore, the current treatment options have drawbacks which compromise efficacy and patient compliance. To face this global health concern, new alternatives for the treatment of leishmaniasis have been explored. Curcumin, a polyphenol obtained from the rhizome of turmeric, exhibits leishmanicidal activity against different species of Leishmania spp. Although its mechanism of action has not yet been fully elucidated, its leishmanicidal potential may be associated with its antioxidant and anti-inflammatory properties. However, it has limitations that compromise its clinical use. Conversely, nanotechnology has been used as a tool for solving biopharmaceutical challenges associated with drugs, such as curcumin. From a drug delivery standpoint, nanocarriers (1–1000 nm) can improve stability, increase solubility, promote intracellular delivery, and increase biological activity. Thus, this review offers a deep look into curcumin-loaded nanocarriers intended for the treatment of leishmaniasis.

Background: Argulus is a common and widespread ectoparasite that causes major parasitic diseases and is a virus and bacteria carrier in the ornamental fish trade. Aims: The purpose of this study is to determine what types of phytochemicals are present in the essential oil extracted from turmeric rhizome (Curcuma longa L.) and to assess the efficacy of turmeric oil in eliminating Argulus spp. infestations in goldfish (Carassius auratus). Methods: The chemical composition and quantity of the major substances in essential oils from fresh turmeric rhizome were detected by Gas Chromatography/Mass Spectrometry (GC-MS). The antiparasitic effect of turmeric oils on Argulus spp. was tested at 12.5, 25, 50, 100, and 200 ppm and compared to 0.25 ppm Neguvon® (the positive control). The percentage of Argulus spp. killed, the percentage of the mean mortality rate, and the effectiveness of each test were evaluated. Results: By using GC-MS analysis, it was possible to identify the primary phytochemical component of turmeric essential oil as b-turmerone. The results obtained from the in vitro test indicated that there was a correlation between the concentration of turmeric essential oil and the average mortality rate of fish lice. The mean mortality of fish louse exposed to 200 ppm turmeric essential oil was higher than the mean mortality of fish louse exposed to Neguvon® (P [Open Vet J 2023; 13(12.000): 1645-1653]

Abstract Background The goal of current research work is to develop and optimize curcumin-encapsulated nanostructured lipid carriers and to enhance therapeutic effect of curcumin after oral administration. Method Curcumin-loaded nanostructured lipid carriers were developed by a single-step one-pot microwave-assisted technique. The preparation of curcumin-loaded nanostructured lipid carriers was optimized by employing two factors and three levels central composite design (Design Expert® software) taking concentration of lipid blend and surfactant as independent variables and particle size, polydispersity index, and zeta potential as dependent variables, to investigate the effect of formulation ingredients on the physicochemical characteristics of nanostructured lipid carriers. The optimized batch was investigated by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, high-resolution transmission electron microscopy, in vitro drug release, stability studies, cytotoxicity, and in vivo anthelmintic studies. Results The average particle size, polydispersity index, and zeta potential of the optimized batch were found to be 144 nm, 0.301, and − 33.2 mV, respectively, with an entrapment efficiency of 92.48%. The results of high-resolution transmission electron microscopy confirmed spherical shape of particles. In vivo antiparasitic studies included determining the duration of paralysis and eventual death of earthworms in the presence of test samples. The results of in vivo studies showed good anthelmintic potential for curcumin-loaded nanostructured lipid carriers as compared to albendazole in different concentrations. Cytotoxicity studies also confirmed the formulation to be nontoxic to Vero cells. In vitro drug release study showed 90.76 ± 0.01% release of curcumin in 24 h by following the Korsmeyer-Peppas model of release kinetics. Conclusion The aforementioned results imply that microwave-developed nanostructured lipid carriers could be promising drug carriers and will aid in their fabrication for oral administration as a possible alternative for the treatment of other parasitic infections. Graphical Abstract

Background/Objectives: Leishmaniasis, a neglected disease caused by Leishmania spp. including L. amazonensis, urgently requires new treatments. Polyalthic acid (PA), a natural diterpene from Copaifera spp., has previously demonstrated significant antiparasitic potential. This study evaluated the leishmanicidal effects of polyalthic acid (PA), alone and with amphotericin B (AmpB), on L. amazonensis promastigote and amastigote forms. Results: PA showed significant activity against promastigotes, with 50% effective concentration (EC50) values of 2.01 μM at 24 h and an EC50 of 3.22 μM against amastigotes after 48 h. The PA and AmpB combination exhibited a synergistic effect on both forms without inducing cytotoxicity or hemolysis. Morphological changes in promastigotes, including vacuole formation and cell rounding, were more pronounced with the combination. Conclusions: These findings suggest that PA and AmpB together could form a promising new treatment strategy against Leishmania infections, offering enhanced efficacy without added toxicity.

OBJECTIVE This study determined the in vitro efficacy of 6 common anthelmintics (eprinomectin, ivermectin, milbemycin oxime, moxidectin, selamectin, and fenbendazole) on motility (viability) of infectious third-stage larvae (L3) of Crenosoma vulpis, Angiostrongylus vasorum, and Aelurostrongylus abstrusus, which are important causes of canine and feline cardiopulmonary disease. SAMPLES First-stage larvae (L1) from C vulpis, An vasorum, and Ae abstrusus. PROCEDURES Naïve Limax maximus slugs were fed 1,000 to 2,000 L1 and held at 16 °C for at least 4 weeks to produce live L3. Approximately 50 to 100 L3/well were subsequently incubated in culture media alone or media containing 6 separate test anthelmintics at 4 concentrations, to bracket expected in vivo drug plasma levels in anthelmintic-treated dogs and cats. Drug effects on L3 motility (viability) were analyzed by multilevel logistic models, generating doseresponse relationships. Experiments were completed 1-9/2019. RESULTS Drug concentration estimates corresponding to a 50% larval mortality rate identified that C vulpis was the most sensitive species to the anthelmintics tested. Ae abstrusus was most susceptible to moxidectin and selamectin, while An vasorum was insusceptible to all anthelmintics tested, except for selamectin at high drug concentrations. CLINICAL RELEVANCE The in vitro anthelmintic response to antiparasitic agents may guide and improve disease therapy and prevention. Considering the observed lack of efficacy against L3, monthly anthelmintic treatment for protection against An vasorum infection in dogs would primarily rely on the anthelmintic's adulticidal activity. Maximal preventive control for An vasorum would, therefore, require at least 1 treatment administered a minimum of 1 week after the end of the transmission season. [ABSTRACT FROM AUTHOR]

Fatalities caused by infectious diseases (i.e., diseases caused by parasite, bacteria, and viruses) have become reinstated as a major public health threat globally. Factors such as antimicrobial resistance and viral complications are the key contributors to the death numbers. As a result, new compounds with structural diversity classes are critical for controlling the virulence of pathogens that are multi-drug resistant. Derivatization of bio-active organic molecules with organometallic synthons is a promising strategy for modifying the inherent and enhanced properties of biomolecules. Due to their redox chemistry, bioactivity, and structural diversity, organometallic moieties make excellent candidates for lead structures in drug development. Furthermore, organometallic compounds open an array of potential in therapy that existing organic molecules lack, i.e., their ability to fulfill drug availability and resolve the frequent succumbing of organic molecules to drug resistance. Additionally, metal complexes have the potential towards metal-specific modes of action, preventing bacteria from developing resistance mechanisms. This review's main contribution is to provide a thorough account of the biological efficacy (in vitro and in vitro) of metal-based complexes against infectious diseases. This resource can also be utilized in conjunction with corresponding journals on metal-based complexes investigated against infectious diseases. [ABSTRACT FROM AUTHOR]

Background: Argulus is a common and widespread ectoparasite that causes major parasitic diseases and is a virus and bacteria carrier in the ornamental fish trade. Aim: The purpose of this study is to determine what types of phytochemicals are present in the essential oil extracted from turmeric rhizome (Curcuma longa L.) and to assess the efficacy of turmeric oil in eliminating Argulus spp. infestations in goldfish (Carassius auratus). Methods: The chemical composition and quantity of the major substances in essential oils from fresh turmeric rhizome were detected by gas chromatography/mass spectrometry (GC-MS). The antiparasitic effect of turmeric oils on Argulus spp. was tested at 12.5, 25, 50, 100, and 200 ppm and compared to 0.25 ppm Neguvon® (the positive control). The percentage of Argulus spp. killed, the percentage of the mean mortality rate, and the effectiveness of each test were evaluated. Results: By using GC-MS analysis, it was possible to identify the primary phytochemical component of turmeric essential oil as b-turmerone. The results obtained from the in vitro test indicated that there was a correlation between the concentration of turmeric essential oil and the average mortality rate of fish lice. The mean mortality of fish louse exposed to 200 ppm turmeric essential oil was higher than the mean mortality of fish louse exposed to Neguvon® (p < 0.05). In an in vivo study, the effectiveness of 12.5 ppm turmeric essential oil against parasites was 44.44%, 55.46%, and 62.83% at 24, 48, and 72 hours, respectively. Conclusion: In summary, the efficacy of turmeric essential oil against fish louse has been shown both in vitro and in vivo studies. [ABSTRACT FROM AUTHOR]

Brazilian Amazon contains over 30,000 plant species and foods rich in bioactive compounds such as terpenes, phenolic acids, alkaloids, and flavonoids, of potential health benefits (antioxidant, antimicrobial, antiparasitic, anticancer, gastroprotection, prebiotic effects, among others). The existence of residues from non-edible parts of plants (leaves, roots, stems, branches, barks) or fruit wastes (peel, bagasse, seeds) in the agri-food industry and its supply chain is an important challenge in food loss and waste management. In this critical review several Amazon species, focusing on extracts/essential oils from nonedible parts or wastes, were analyzed in terms of phytochemicals, biological activity, and underlying mechanisms. We hope this review emphasizes the importance of Amazon's sustainability initiatives on population health due to the potential shown against cancer, infectious diseases, and prevention of oral diseases. It is urgent to think about the conversion of amazon food wastes and co-products into high-added-value raw materials to develop novel drugs, food packaging systems, or nutraceutical foods. [ABSTRACT FROM AUTHOR]

Background: The goal of current research work is to develop and optimize curcumin-encapsulated nanostructured lipid carriers and to enhance therapeutic effect of curcumin after oral administration. Method: Curcumin-loaded nanostructured lipid carriers were developed by a single-step one-pot microwave-assisted technique. The preparation of curcumin-loaded nanostructured lipid carriers was optimized by employing two factors and three levels central composite design (Design Expert® software) taking concentration of lipid blend and surfactant as independent variables and particle size, polydispersity index, and zeta potential as dependent variables, to investigate the effect of formulation ingredients on the physicochemical characteristics of nanostructured lipid carriers. The optimized batch was investigated by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, high-resolution transmission electron microscopy, in vitro drug release, stability studies, cytotoxicity, and in vivo anthelmintic studies. Results: The average particle size, polydispersity index, and zeta potential of the optimized batch were found to be 144 nm, 0.301, and − 33.2 mV, respectively, with an entrapment efficiency of 92.48%. The results of high-resolution transmission electron microscopy confirmed spherical shape of particles. In vivo antiparasitic studies included determining the duration of paralysis and eventual death of earthworms in the presence of test samples. The results of in vivo studies showed good anthelmintic potential for curcumin-loaded nanostructured lipid carriers as compared to albendazole in different concentrations. Cytotoxicity studies also confirmed the formulation to be nontoxic to Vero cells. In vitro drug release study showed 90.76 ± 0.01% release of curcumin in 24 h by following the Korsmeyer-Peppas model of release kinetics. Conclusion: The aforementioned results imply that microwave-developed nanostructured lipid carriers could be promising drug carriers and will aid in their fabrication for oral administration as a possible alternative for the treatment of other parasitic infections. Highlights: Curcumin-loaded nanostructured lipid carriers (Cr-NLCs) were prepared by a fast and easy single-step one-pot microwave-assisted technique. Implementation of 2 factors at 3 levels with central composite design (Design Expert® software) to investigate the influence of the formulation ingredients on the physicochemical properties of the NLCs. Optimized batch of Cr-NLC demonstrated nanosized particles with improved drug release characteristics, excellent entrapment efficiency and augmented physical stability. The anthelmintic potential of Cr-NLC was determined by a study on earthworms and was compared with albendazole. A cytotoxicity study was performed on Vero cells and evaluated in terms of IC50 value. [ABSTRACT FROM AUTHOR]

Ferroptosis is an iron-dependent form of regulated cell death characterized by glutathione (GSH) depletion, glutathione peroxidase 4 (GPX4) inactivation, and the build-up of lipotoxic reactive species. Ferroptosis-targeted induction is a promising therapeutic approach for addressing antimalarial drug resistance. In addition to being the primary source of intracellular energy supply and reactive oxygen species (ROS) generation, mitochondria actively participate in diverse forms of regulated cell death, including ferroptosis. Altered mitochondrial morphology and functionality are attributed to ferroptosis. Diverse mitochondria-related proteins and metabolic activities have been implicated in fine-tuning the action of ferroptosis inducers. Herein, we review recent progress in this evolving field, elucidating the numerous mechanisms by which mitochondria regulate ferroptosis and giving an insight into the role of the organelle in ferroptosis. Additionally, we present an overview of how mitochondria contribute to ferroptosis in malaria. Furthermore, we attempt to shed light on an inclusive perspective on how targeting malaria parasites’ mitochondrion and attacking redox homeostasis is anticipated to induce ferroptosis-mediated antiparasitic effects.

Based on the demonstrated and reported trypanocidal, leishmanicidal, and antiplasmodial activities of two menthol prodrugs, it was decided to proceed with preformulation studies, which are of key relevance in the drug discovery process. The aim of this study is to examine the stability and permeability of two new menthol prodrugs with antiparasitic activity. To determine the stability of menthol and its prodrugs, the corresponding studies were carried out in buffered solutions at pH values of 1.2, 5.8, and 7.4 at 37 °C. In silico permeability studies were performed using the free PerMM software and then in vitro permeability studies were performed using a biomimetic artificial membrane (BAM). Permeability studies conducted in silico predicted that both menthol and its prodrugs would pass through biological membranes via flip-flop movement. This prediction was subsequently confirmed by in vitro BAM permeability studies, where it was observed that the menthol prodrugs (1c and 1g) exhibited the highest Papp (apparent permeability) value compared to the parent compound. The study reveals that menthol prodrugs exhibit stability at a pH of 5.8 and possess sufficient in vitro permeability values as preformulation parameters.

Cryptosporidium parvum (C. parvum) is one of the most prevalent species infecting humans and animals. Currently, the only FDA-licensed drug to treat cryptosporidiosis is nitazoxanide (NTZ), with no efficacy in immunocompromised hosts. Citrus paradisi (C. paradisi) has demonstrated anti-protozoal activities. This study aimed to investigate the anti-cryptosporidiosis effect of C. paradisi peel extract, either alone or in mediating the green synthesis of chitosan silver nanoparticles (Cs/Ag NPs), compared to NTZ. Mice were sorted into nine different groups. The effectiveness of the treatments was evaluated using parasitology, histopathology, immunohistochemistry, and immunology. C. paradisi outperformed nitazoxanide regarding oocyst shedding (79% vs. 61%). The effectiveness of NTZ Cs/Ag NPs and Citrus Cs/Ag NPs was enhanced to 78% and 91%, respectively. The highest oocyst inhibition was obtained by combining NTZ and Citrus Cs/Ag NPs (96%). NF-κB, TNF-α, and Il-10 levels increased in response to infection and decreased in response to various treatments, with the highest reduction in the group treated with combined NTZ citrus Cs/Ag NPs. Combining C. paradisi with NTZ could have a synergistic effect, making it a potentially effective anti-cryptosporidiosis agent. Utilizing C. paradisi in the green synthesis of Cs/Ag NPs improves the therapeutic response and can be used to produce novel therapeutic antiparasitic drugs.

Secondary metabolites produced by the fermentation of Streptomyces avermitilis bacterium are powerful antiparasitic agents used in animal health, agriculture and human infection treatments. Avermectin is a macrocyclic lactone with four structural components (A1, A2, B1, B2), each of them containing a major and a minor subcomponent, out of which avermectin B1a is the most effective parasitic control compound. Avermectin B1a produces two homologue avermectins (B1 and B2) that have been used in agriculture as pesticides and antiparasitic agents, since 1985. It has a great affinity with the Cl-channels of the glutamate receptor, allowing the constant flow of Cl- ions into the nerve cells, causing a phenomenon of hyperpolarization causing death by flaccid paralysis. The purpose of this work was to gather information on the production of avermectins and their biocidal effects, with special emphasis on their role in the control of pests and phytopathogenic diseases. The literature showed that S. avermitilis is an important producer of macrocyclic lactones with biocidal properties. In addition, avermectin contributes to the control of ectoparasites and endoparasites in human health care, veterinary medicine and agriculture. Importantly, avermectin is a compound that is harmless to the host (no side effects), non-target organisms and the environment.

Rauwolfia serpentina (serpentina) and peperomia pellucida (pansit-pansitan) were used as the raw materials for creating different mixtures to determine which concentration is faster in exterminating Rhipicephalus sanguineus latrille (common ticks). The process used was decoction, the harvested extract was used for the creation of the spray mixtures. The process used three different preparations of mixture concentration with variants concentration ratio of serpentina/pansit-pansitan as: mixture 1 with 50%/50%; mixture 2 with 75%/25%, and mixture 3 with 25%/75%. The study recorded the testing times in exterminating the ticks as: mixture 1 had the results in 1.5 hours (sprayed once), 1.33 hours (sprayed twice), and 1.25 hours (sprayed thrice); mixture 2 had the results in 3.5 hours (sprayed once), 3.42 hours (sprayed twice), and 3.33 hours (sprayed thrice); and mixture 3 had the results in 1.5 hours (sprayed once), 1.42 hours (sprayed twice), and 1.33 hours (sprayed thrice). The experiment showed that mixture 1 and mixture 3 almost had the same results, if not for a few second differences, mixture 1 was always faster than mixture 3, while mixture 2 was left behind for a few hours. Therefore, mixture 1 is the best concentration to exterminate the ticks in a controlled environment.

The increasing resistance to antiparasitic drugs and limited availability of new agents highlight the need to improve the efficacy of existing treatments. Ivermectin (IVM) is commonly used for parasite treatment in humans and animals, however its efficacy is not optimal and the emergence of IVM-resistant parasites presents a challenge. In this context, the physico-chemical characteristics of IVM were modified by nanocrystallization to improve its equilibrium water-solubility and skin penetration, potentially improving its therapeutic effectiveness when applied topically. IVM-nanocrystals (IVM-NC) were prepared using microfluidization technique. The impact of several process/formulation variables on IVM-NC characteristics were studied using D-optimal statistical design. The optimized formulation was further lyophilized and evaluated using several in vitro and ex vivo tests. The optimal IVM-NC produced monodisperse particles with average diameter of 186 nm and polydispersity index of 0.4. In vitro results showed an impressive 730-fold increase in the equilibrium solubility and substantial 24-fold increase in dissolution rate. Ex vivo permeation study using pig's ear skin demonstrated 3-fold increase in dermal deposition of IVM-NC. Additionally, lyophilized IVM-NC was integrated into topical cream, and the resulting drug release profile was superior compared to that of the marketed product. Overall, IVM-NC presents a promising approach to improving the effectiveness of topically applied IVM in treating local parasitic infections.