Antimalarial Properties Research Articles

A Comprehensive Review on the Synthesis of Mangiferin Derivatives and their Multiple Biological Activities

Mangiferin always draws the attention of traditional as well as modern medicinal chemists because of its ease of chemical derivatization and diverse biological activities, including anticancer, anti-inflammatory, neuroprotective, antidiabetic, analgesic, antimalarial, anticonvulsant, laxative, cardiotonic, hemopoietic, antioxidant, antimicrobial, antipsychotic, anticoagulant, and antihypertensive properties. This review focuses on a detailed and updated overview of the synthesis of mangiferin derivatives and their diverse biological activities, with examples from both patented and non-patented literature.

The Role of Traditional Medicinal Plants in Managing Malaria and HIV Co-Infection

Malaria and HIV co-infection presents a significant public health challenge, particularly in Sub-Saharan Africa, where co-morbidity rates are highest. Conventional therapies, including antiretrovirals and antimalarial drugs, are expensive and often associated with side effects that lead to noncompliance. Traditional medicinal plants offer an affordable and culturally accepted alternative. This review explores various plants used historically in the treatment of both malaria and HIV, focusing on their phytochemical constituents, mechanisms of action, and clinical efficacy. Plants such as Catharanthus roseus, Adenia venenata, and Morinda lucida have demonstrated antimalarial and antiviral properties, often through bioactive compounds like alkaloids and flavonoids. Additionally, integrating these traditional medicines with modern healthcare systems faces regulatory challenges, but there is promising potential for synergies in treatment efficacy. Further research, clinical trials, and interdisciplinary collaboration are necessary to validate these medicinal plants and improve the management of malaria and HIV co-infection. Keywords: Traditional medicinal plants, Malaria, HIV co-infection, Phytochemicals, Antimalarial properties.

Antimalarial and antioxidant properties of vernonia amygdalina ethanol leaf extract in mice infected with rodent malaria parasites

Antimalarial and antioxidant properties of vernonia amygdalina ethanol leaf extract in mice infected with rodent malaria parasites

Synthesis, Characterization and Computational Studies on (E)-4-(1-((2-hydroxyphenyl)imi no) hexyl)-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one

A coupling precursor, 4-hexanoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, 1 synthesized by the reaction of 3-methyl-1-phenyl-1H-pyrazol-5-one with hexanoyl chloride was reacted with 2-aminophenol to synthesize (E)-4-(1-((2-hydroxyphenyl)imino)hexyl)-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, 1a. The compounds were characterized by conventional spectroscopic techniques, 1H and 13C NMR, UV-Visible, FTIR spectroscopy and single crystal X-ray crystallograpic structural determinations and computational techniques. To augment the experimental data, DFT calculations were carried. Molecular dockings were used to predict the interactions between, 1a with some biological targets. The binding free energies in the Plasmepsin II active sites indicated anti−malarial activity against P. falciparum in epidermal growth factor receptor (EGFR) inhibition, anti-inflammatory properties against human peroxiredoxin 5, and anticancer properties. With binding energies less than −5.00 kcal/mol, the results indicate that 1a is a potential drug target for anti-inflammatory, anti-malarial and anti-cancer properties.

Advances in the study of artemisinin and its derivatives for the treatment of rheumatic skeletal disorders, autoimmune inflammatory diseases, and autoimmune disorders: a comprehensive review.

Artemisinin and its derivatives are widely recognized as first-line treatments for malaria worldwide. Recent studies have demonstrated that artemisinin-based antimalarial drugs, such as artesunate, dihydroartemisinin, and artemether, not only possess excellent antimalarial properties but also exhibit antitumor, antifungal, and immunomodulatory effects. Researchers globally have synthesized artemisinin derivatives like SM735, SM905, and SM934, which offer advantages such as low toxicity, high bioavailability, and potential immunosuppressive properties. These compounds induce immunosuppression by inhibiting the activation of pathogenic T cells, suppressing B cell activation and antibody production, and enhancing the differentiation of regulatory T cells. This review summarized the mechanisms by which artemisinin and its analogs modulate excessive inflammation and immune responses in rheumatic and skeletal diseases, autoimmune inflammatory diseases, and autoimmune disorders, through pathways including TNF, Toll-like receptors, IL-6, RANKL, MAPK, PI3K/AKT/mTOR, JAK/STAT, and NRF2/GPX4. Notably, in the context of the NF-κB pathway, artemisinin not only inhibits NF-κB expression by disrupting upstream cascades and/or directly binding to NF-κB but also downregulates multiple downstream genes controlled by NF-κB, including inflammatory chemokines and their receptors. These downstream targets regulate various immune cell functions, apoptosis, proliferation, signal transduction, and antioxidant responses, ultimately intervening in systemic autoimmune diseases and autoimmune responses in organs such as the kidneys, nervous system, skin, liver, and biliary system by modulating immune dysregulation and inflammatory responses. Ongoing multicenter randomized clinical trials are investigating the effects of these compounds on rheumatic, inflammatory, and autoimmune diseases, with the aim of translating promising preclinical data into clinical applications.

Biological activities of metal complexes with Schiff base

Abstract Schiff bases are a class of synthetic compounds that form when primary amines combine with aldehydes or ketones. These compounds are incredibly important across various fields, such as biology, catalysis, and optics, due to their diverse features. One notable aspect is their ability to form complexes with transition metals, which opens up a wide range of potential uses, particularly in human systems. In the human body, Schiff base metal complexes display a range of biological actions, including antibacterial, antifungal, anticancer, and antimalarial properties. The versatility of Schiff bases in reacting with different transition metals gives these complexes intriguing potential for addressing biological issues and treating diseases. This article explores various examples of Schiff bases, metal complexes, and their associated ligands, highlighting their usefulness in a variety of biological applications. The potential of Schiff base metal complexes as valuable agents in resolving medical difficulties and advancing biomedical research is emphasized.

Computational Drug Design Approaches for the Identification of Novel Antidiabetic Compounds from Natural Resources through Molecular Docking, ADMET, and Toxicological Studies.

Type 2 diabetes mellitus (T2DM) is usually depicted by relative insulin deficiency, raised blood glucose levels, and the predominant risk factor, insulin resistance. Hence, the development of insulin sensitizer drugs targeting PPAR-γ receptors has expanded enormous interest as an attractive choice for T2DM treatment. Thiazolidinediones (TZD) enhance insulin sensitivity either by directly functioning on gene transcription of the PPARγ receptor related to glucose homeostasis or by systemic sensitization of insulin and, therefore, improved hyperglycemia in a wide range of patients. However, severe complications and adverse effects of TZDs necessitate the development of an efficacious and reliable insulin sensitizer from alternative resources. On the contrary, Nature is a rich source of anticipated effective and safer medicine; more than fifty percent of drugs on the market are developed from natural products. Hence, searching for a new PPAR-γ agonist from bioactive secondary compounds of medicinal plants along with greater efficacy and safety is a recognized and consistent tactic for developing novel antidiabetic agents. Pulicaria jaubertii is a fragrant perennial aromatic plant with anti-inflammatory, antidiabetic, antimicrobial, antimalarial, and insecticidal properties. The current study was designed to use a computer-aided drug design to explore the best antidiabetic compounds from P. jaubertii. Herein, the molecular docking study of 80 investigated ligands against the PPAR-γ receptor identifies the highest docking score for five ligands ranging from -8.9 kcal/mol to 8.0 kcal/mol, which is also more significant than the standard drug pioglitazone (-7.7 kcal/mol) determined by the PyRx 8.0 virtual screening software. GLN286, CYS285, SER289, TYR473, MET364, ARG288, ILE341, and LEU333 residues are found to be significant contributors to the non-bonded interaction between ligands and receptors. Molecular electrostatic potential (MEP), DFT, molecular orbital (MO), ADMET, and toxicological analyses were performed on the selected five high-scored ligands of P. jaubertii. Results documented that all investigated ligands, especially L4, show considerably excellent profiles in molecular docking, MEP, DFT, MO, ADMET, and toxicological predictions, suggesting our drug-designing approaches may contribute to the development of a novel antidiabetic drug for the treatment of T2DM from natural resources.

Exploring the DNA Recognition of Compounds Based on Benzimidazole and Benzothiazole: A Concise Review

AbstractOver the course of three decades, benzimidazole as well as benzothiazole and its derivatives have been extensively investigated in oligo‐nucleotide therapy for their properties. These derivatives serve as valuable building blocks for creating pharmaceutical and biologically active molecules. With applications ranging across various therapeutic domains, including antiulcer, anticancer, and anthelmintic treatments, substituted benzimidazole/ benzothiazole derivatives have proven their versatility. This review provides a systematic and comprehensive overview of the latest advancements in benzimidazole/ benzothiazole‐based compounds within medicinal chemistry. These compounds exhibit diverse pharmacological activities such as anticancer, antibacterial, antifungal, anti‐inflammatory, analgesic, anti‐HIV, antioxidant, anticonvulsant, antitubercular, antidiabetic, antileishmanial, antihistaminic, antimalarial properties, among others. By presenting insights into the substitution patterns around the benzimidazole/benzothiazole nucleus, this review aims to assist medicinal chemists in developing structure–activity relationships (SAR) for benzimidazole/benzothiazole‐based drugs and compounds, thereby aiding in the advancement of medicinal research.

Effect of Justicia insularis Leaf Extract and Fractions on Oxidative Stress Markers, Liver Function Parameters and Liver Histology of Plasmodium berghei -Infected Mice

Justicia insularis (Family-Acanthaceae) is used in Ibibio ethnomedicine to treat malaria. The leaf extract and fractions of J. insularis were investigated for antioxidative stress and hepatoprotective activities in Plasmodium berghei-infected mice. The leaf extract (100-300 mg/kg, p.o.) exerted significant (p<0.05) antimalarial activity against P. berghei infection in curative test with ethyl acetate fraction demonstrating the highest activity. The extract/fractions treatment caused significant (p<0.05) reductions in liver enzymes (ALT, AST and ALP), total and conjugated bilirubin of the treated infected mice and also decreased significantly (p<0.05) total protein and albumin levels of the treated mice relative to control. The leaf extract and fractions further improved significantly (p<0.05) the levels of oxidative stress markers enzymes and molecules (CAT, GPx, GST, SOD) of the treated infected mice with no significant (p>0.05) effect on GSH. The MDA levels in the livers of the treated infected mice were significantly (p<0.05) reduced relative to control. Histology of liver sections revealed absence or significant reductions in pathological features in infected mice treated with leaf extract (100 mg/kg), DCM and ethyl acetate fractions compared to untreated infected mice. These results suggest that the leaf extract/fractions of Justicia insularis possess antioxidative stress and hepatoprotective potentials, which is an added advantage to its antimalarial property.

Antioxidant and antimalarial properties of hot aqueous leaf extracts of Setaria megaphylla, Ageratum conyzoides and Chromolaena odorata

This study investigated the antioxidant and antimalarial properties of leaf extracts of Setaria megaphylla, Ageratum conyzoides Linn, and Chromolaena odorata Linn, plants used in folkloric treatment of malaria. The plants were assessed for phenolic profile, antioxidant capacity and radical scavenging activities using standard methods. Single, binary and ternary combinations of the processed leaves were subjected to hot aqueous extraction, and evaluated for in vivo antiplasmodial efficacy against Plasmodium berghei NK 65 using Swiss albino mice. The plants’ total phenolic profile varied as S. megaphylla (Sm; 118.06 µg/ml) > C. odorata (Co; 116.58 µg/ml) > A. conyzoides (Ac; 73.01 µg/ml), with catechin, dihydrocytisine and tannin being the most abundant phenolics. Total antioxidant capacities (TAC) and reducing power potentials (RPP) of the plants increased with increase in extract concentrations with Sm showing highest TAC (1.49 ± 0.02 mgAAE/g) and RPP (0.47 ± 0.01 mgAAE/g) values. A similar trend was observed for the hydroxyl, nitric oxide and DPPH radicals scavenging potentials, showing dose-dependent increases in scavenging potentials but with no observed significant (p<0.05) differences in activities at the highest extract dose of 400 µg/ml. The in vivo antimalarial study demonstrated that the combination of A. conyzoides and S. megaphylla was the most effective, significantly reducing parasitemia without causing mortality in the mice. This research highlights the potential of S. megaphylla, A. conyzoides, and C. odorata, especially the combination of their extracts as source of effective anti-malarial agents, and further confirms the folkloric use of hot aqueous extracts of the plants in malaria treatment.

Nutraceutical and Functional Food Potentials of African Black Elimi (Canarium schweinfurthii): A Review

Study’s Excerpt The potentials of Canarium schweinfurthii in traditional African medicine in treating various ailments due to its rich bioactive composition is extensively explored. 80 publications were synthesized to gather the plant’s diverse nutraceutical and functional properties. The plant has antimalarial, anti-cancer, and antioxidant effects, among others. Full Abstract Medicinal plants have been central to African traditional medicine for centuries, preceding the development of synthetic drugs. Africa is blessed with large medicinal plants that are either under-explored or yet to be studied. This study aimed to find relevant research works on Canarium schweinfurthii with the purpose of identifying a new research niche. One hundred eighteen (118) research journals were collected, and 80 publications were synthesized and used to identify non-repeated experiments on the functional and nutraceutical potentials of Canarium schweinfurthii. The results of the review revealed that different parts of the plant including leaves, stem bark, roots, fruits, seeds, flowers, gum, and resin were traditionally employed in treating a range of ailments, including diabetes, stomach ulcers, malaria, typhoid, leprosy, reproductive disorders, and fever which are attributed to plant’s richness for nutraceutical and functional properties, driven by the presence of bioactive compounds such as antioxidants, alkaloids, saponins, flavonoids, tannins, glycosides, and phenolic compounds. Nutraceutical and functional investigations of the plant have corroborated the antimalarial, anti-cancer, anti-diabetic, analgesic, antioxidant, antimicrobial, anti-bacterial, growth-promoting, nephroprotective, food preservative, anthelmintic, and termiticidal properties of the fruit pulp, fruit bark, stem bark, fruit oil, seed oil of Canarium schweinfurthii. This review recommends the plant for proper establishment of a foundation for the plant’s pharmaceutical application and underscores the need for further research.

Two-Dimensional Correlation Spectroscopy (2D-COS) Tracking of the Formation of Selected Transition Metal Compounds Cu(II) and Cd(II) With Cinchonine and Their Impact on Model Components of Erythrocytes.

Cinchonine is a quinoline alkaloid known for its antimalarial properties. Due to the advantages of using compounds of metal ions with alkaloids, a copper(II) compound with cinchonine was synthesized, and, for comparative purposes, a cadmium(II) compound with cinchonine. During the synthesis, the emerging interactions between the metal ion and cinchonine were studied. After crystallization, it was examined how the obtained compounds would interact with the model blood component, hematoporphyrin IX. Ultraviolet-visible (UV-Vis) spectroscopy, Raman spectroscopy, and attenuated total reflection Fourier transform infrared spectroscopy (ATR FT-IR) were used in the study. In the case of monitoring the synthesis, the best method turned out to be UV-Vis spectroscopy, combined with the possibility of two-dimensional correlation spectroscopy (2D-COS), which enabled the identification of peaks characteristic of the interactions of the cinchonine quinoline ring with metal ions. In turn, the obtained Raman spectra showed shifts of individual bands and changes in their intensity, and 2D-COS showed the sequence of formation of individual interactions, which confirmed the formation of cinchonine compounds with metals. ATR FT-IR also allowed us to compare the spectra of the substrates used in the synthesis with the crystallized compounds and thus confirm the formation of the expected compounds. Bands characteristic of π-π-stacking interactions between the quinoline ring and the tetrapyrrole ring of hematoporphyrin IX were also observed. Observed interaction with a model blood component may be important when designing drugs for antimalarial therapy.

Medicinally Privileged Natural Chalcones: Abundance, Mechanisms of Action, and Clinical Trials.

Chalcones have been utilized for centuries as foods and medicines across various cultures and traditions worldwide. This paper concisely overviews their biosynthesis as specialized metabolites in plants and their significance, potential, efficacy, and possibility as future medicines. This is followed by a more in-depth exploration of naturally occurring chalcones and their corresponding mechanisms of action in human bodies. Based on their mechanisms of action, chalcones exhibit many pharmacological properties, including antioxidant, anti-inflammatory, anticancer, antimalarial, antiviral, and antibacterial properties. Novel naturally occurring chalcones are also recognized as potential antidiabetic drugs, and their effect on the GLUT-4 transporter is investigated. In addition, they are examined for their anti-inflammatory effects, focusing on chalcones used for future pharmaceutical utilization. Chalcones also bind to specific receptors and toxins that prevent bacterial and viral infections. Chalcones exhibit physiological protective effects on the biological degradation of different systems, including demyelinating neurodegenerative diseases and preventing hypertension or hyperlipidemia. Chalcones that are/were in clinical trials have been included as a separate section. By revealing the many biological roles of chalcones and their impact on medicine, this paper underlines the significance of naturally occurring chalcones and their extension to patient care, providing the audience with an index of topic-relevant information.

Natural and Synthetic Capsaicin Analogues: A Comprehensive Review of Biological Effects and Synthetic Pathways.

Capsaicin analogs, whether sourced from natural origins or synthesized de novo, have garnered significant attention across diverse scientific disciplines. This comprehensive investigation explores the expansive domain of medicinal chemistry and pharmacology, focusing on capsaicin and its analogs. Notably, these analogs exhibit a wideranging pharmacological spectrum, with a particular emphasis on their potent antitumor properties. Researchers frequently explore structural modifications, particularly in region C, consistently enhancing their pharmacological activities. A highlighted finding is that analogs with alterations in both regions A and C manifest a diverse array of effects, spanning from anti-obesity to protection against ischemia. They also demonstrate anti- Alzheimer's, anti-fibrotic, anti-inflammatory, anti-diabetic, antimalarial, and anti-epileptic properties. This underscores the potential of structural adaptations in these regions, expanding the therapeutic applications of capsaicin-like compounds. Additionally, manipulations in regions B and C result in compounds that possess antioxidant and anti-obesity properties, providing valuable insights for the development of novel compounds. The therapeutic potential of capsaicin analogs opens innovative avenues for drug design and development, promising to address a broad spectrum of diseases and enhance global quality of life. Moreover, this article meticulously examines various synthetic methodologies for synthesizing capsaicin analogs, complementing the main review. These methodologies distinguish themselves through their simplicity, mild reaction conditions, and reliance on readily available commercial reagents. The accessible synthesis pathways enable researchers from diverse backgrounds to explore these compounds, fostering investigations and potential therapeutic applications.

From Traditional Use to Modern Evidence: The Medicinal Chemistry of Antimalarials from Genus Artemisia.

While the use of plants in traditional medicine dates back to 1500 B.C., modern advancements led to the development of innovative therapeutic techniques. On the other hand, in the field of anti-infective agents, lack of efficacy and the onset of resistance stimulate the search for novel agents. Genus Artemisia is one of the most diverse among perennial plants with a variety of species, properties, and chemical components. The genus is known for its therapeutic values and, in particular, for its role in the origin of antimalarial agents derived from artemisinin. In this review, we aim to provide an updated overview of the evolution of natural and natureinspired compounds related to the genus Artemisia that have been proven, in vitro and in vivo, to possess antimalarial properties. An overview of the chemical composition and a description of the ethnopharmacological aspects will be presented, as well as an updated report on in vitro and in vivo evidence that allowed the translation of artemisinin and its derivatives from traditional chemistry into modern medicinal chemistry. The biological and structural properties will be discussed, also dedicating attention to the challenging tasks that still are open, such as the identification of optimal combination strategies, the routes of administration, and the full assessment of the mechanism of action.

An Investigation of In Vitro Anti-Cancer Efficacy of Dihydroartemisinin-Loaded Bovine Milk Exosomes Against Triple-Negative Breast Cancer.

Repurposing drugs offers several advantages, including reduced time and cost compared to developing new drugs from scratch. It leverages existing knowledge about drug safety, dosage, and pharmacokinetics, expediting the process of clinical trials and regulatory approval. Dihydroartemisinin (DHA) is a semi-synthetic and active metabolite of all artemisinin molecules and is FDA-approved for the treatment of malaria. Apart from having anti-malarial properties, DHA also possesses anticancer properties. However, its pharmacological actions are limited by toxicity and solubility problems. To overcome these challenges and enhance its anticancer effectiveness, we designed an exosomal formulation of DHA. We isolated exosomes from bovine milk using differential ultracentrifugation and loaded DHA using sonication. Scanning and transition electron microscopy revealed a size of roughly 100nm, with a spherical shape. Furthermore, in pH 7.4 and 5.5, the exosomes exhibited burst release followed by sustained release. Multiple in vitro cell culture tests demonstrated that Exo-DHA exhibited enhanced anticancer activity, including cytotoxicity, cellular uptake, generation of reactive oxygen species (ROS), disruption of mitochondrial membrane potential, and inhibition of colony formation. Additional evidence supporting Exo-DHA's anti-migration ability came from transwell migration and scratch assays. Based on these results, it was concluded that the anticancer efficacy of DHA was improved when loaded into bovine milk-derived exosomes. While the in vitro results are encouraging, more in vivo testing in suitable animal models and biochemical marker analysis are warranted.

Mesua assamica (King & Prain) kosterm. bark ethanolic extract attenuates rheumatoid arthritis via down-regulating TLR4/NF-κB/COX-2/iNOS and activation of Nrf2/HO-1 pathways: A comprehensive study on in-vitro and in-vivo models

Ethnopharmacological relevanceRheumatoid arthritis (RA) is a multifactorial, polygenic inflammatory disease. Mesua assamica (King & Prain) Kosterm. (MA) is an endangered medicinal plant indigenous to South Asia, primarily to Assam in India. The tree bark is claimed to possess anti-inflammatory, anti-diabetic, anti-cancer, and anti-malarial properties; nevertheless, its role in RA has not been elucidated. Hence, this study aims to investigate the in-vitro and in-vivo anti-arthritic effects of Mesua assamica bark ethanolic extract (MAE). Aim of the studyThis study aims to investigate the anti-rheumatic potential of MAE in-vitro on RAW 264.7 cells for its anti-oxidant and anti-inflammatory activities and in-vivo on the CFA-induced adjuvant arthritis in the rat model. Materials and methodsWe investigated the possible therapeutic effects of MAE in-vitro using RAW 264.7 cells triggered by LPS. Meanwhile, adult Wistar rats were injected intradermally with 100 μl of CFA to induce arthritis, and they were given MAE orally at doses of 100 and 200 mg/kg for up to 28 days. Paw volume analysis, X-ray radiography, anti-oxidant levels analysis, gene and protein expression studies, and histological analysis were carried out to assess the effects of MAE in-vivo. ResultsMAE significantly mitigated the inflammation by reducing ROS levels and dropped the nitrite, PGE2, and COX-2 levels enhanced by LPS in-vitro. At the same time, MAE treatment reduced the paw and joint inflammation and increased the immune organ index in the CFA rats. Histopathology data revealed that MAE mitigated the CFA-induced lesions of the ankle joints and synovial tissues. Similarly, MAE significantly abated the secretion of pro-inflammatory cytokines, inhibited the protein expression of TLR4, NF-кB, COX-2, and iNOS, as well as improved the Nrf2 and HO-1 levels in-vitro and in-vivo. ConclusionAll the results highlighted the anti-rheumatic potential of MAE in RA in-vitro and in-vivo by inhibiting the TLR4/NF-кB/COX-2/iNOS and promoting the Nrf2/HO-1 signaling axis.

Noscapine shows antimalarial activity against Plasmodium falciparum 3D7, its clinical isolate Pf140/SS, and Plasmodium berghei ANKA

Objective: To evaluate the antimalarial activity of noscapine against Plasmodium falciparum 3D7 strain (Pf3D7), its clinical isolate (Pf140/SS), and Plasmodium berghei ANKA (PbA). Methods: Using ring-stage survival assay, phenotypic assessments, and SYBR-green-based fluorescence assay, the antimalarial activities of noscapine were assessed compared with dihydroartemisinin (DHA) in in vivo and in vitro studies. In addition, hemolysis and cytotoxicity tests were carried out to evaluate its safety. RT-PCR assay was also conducted to determine the effect of noscapine on papain-like cysteine protease Plasmodium falciparum falcipain-2 (PfFP-2). Results: The antimalarial efficacy of noscapine against Pf3D7 and Pf140/SS was comparable to DHA, with IC50 values of (7.68±0.88) and (5.57±0.74) nM/mL, respectively, and >95% inhibition of PbA infected rats. Noscapine also showed a safe profile, as evidenced by low hemolysis and cytotoxicity even at high concentrations. Moreover, PfFP-2 expression was significantly inhibited in both noscapine-treated Pf3D7 and Pf140/SS (P<0.01). Conclusions: Noscapine has antimalarial properties comparable to standard antimalarial DHA with better safety profiles, which may be further explored as a therapeutic candidate for the treatment of malaria.

Exploring antimalarial and antioxidant properties of hydrazone ligands and their transition metal complexes: Insights through molecular docking and ADMET studies

Malaria is a leading cause of death in many parts of the world and has a profound impact on public health and poses significant challenges to healthcare systems in endemic regions. Malaria is a severe and sometimes fatal disease caused by Plasmodium parasites and its one significant aspect of malaria pathophysiology is its relationship with oxidative stress, a condition characterized by an imbalance between the production of free radicals and the body’s ability to detoxify these reactive products or repair the resulting damage. So, in the present research, to identify effective agents for malaria and oxidative stress, microassay and DPPH protocols were applied to previously synthesized and well characterized octahedral hydrazone ligands (1–2) and their Co(II), Ni(II), Cu(II), Zn(II) metal complexes (3–10), which were derived from 2-methoxy-1-naphthaldehyde, 3,5-bis(trifluoromethyl)benzohydrazide, 3-bromo-5-ethoxy-4-hydroxybenzaldehyde. The biological assessment indicated that complexes (8, 9, 10) were particularly effective in inhibiting malaria and oxidative infections as compared to other compounds. Among these, zinc(II) complex (10) exhibited the highest efficacy for malaria and oxidative stress, with an IC50 values of 0.59 ± 0.13 and 2.12 ± 0.17 µM which are comparable with quinine and ascorbic acid, correspondingly. Additionally, molecular docking studies against the 8E1Z and 1U5A proteins along with ADMET investigations were also support the superior efficacy of complex (10), demonstrating the lowest binding affinity, favorable binding modes and drug likeness ability.

One-pot synthesis of N'-(thiophen-2-ylmethylene)isonicotinohydrazide Schiff-base as a corrosion inhibitor for C-steel in 1 M HCl: Theoretical, electrochemical, adsorption and spectroscopic inspections

Although carbon steel (CS) is an essential component utilized in many industries, it regrettably corrodes when exposed to acidic conditions. Schiff bases have recently become more concerned with the corrosion prevention of CS. Hydrazides and the related compounds shown to be effective inhibitors of CS corrosion in acids. These compounds are commonly employed as origins or intermediates to several key molecules in the synthesis of organic compounds, and they are highly sought after due to their wide range of biological and therapeutic applications. They have anti-bacterial, anti-malarial, anti-fungal, and anticancer properties, as well as corrosion protection. Hence, the inhibitory effectiveness of a new synthesized (E)-N'-(thiophen-2-ylmethylene) isonicotinohydrazide (TMNH) Schiff-base for the corrosion of CS in 1 M HCl was explored. The structure of TMNH was validated by FT-IR and 1H NMR spectroscopy. A number of chemical, spectral, and electrochemical techniques such as potentiodynamic polarization (PDP), electrochemical impedance spectroscopy (EIS), and mass loss (ML) have been used to evaluate its anticorrosion power. PDP measurements showed that it is a mixed-type inhibitor. In addition, EIS measurements showed that Rct increased sharply from 37 without the corrosion inhibitor to 589 Ω cm-2 in the presence of 1 mM TMNH and from PDP scans, the corresponding icorr decreased dramatically from 0.6158 to 0.0314 μA cm-2. ML tests have proven their effectiveness, achieving an inhibitory efficiency of 95.3 %. Adsorption studies were also conducted to determine the nature of the corrosion retardation mechanism. The TMNH inhibitor was spontaneously chemically/physically adsorbed onto the CS surface following the Langmuir isotherm. Statistical calculations were also applied to verify the accuracy of the experimental results. The Monte Carlo model showed that the inhibitory molecules adsorbed flat on only one side, increasing the chances of adsorption.