Valorization of Carapa procera Oil and Evaluation in vitro of Antimalarial Activity of Its Bitter Content

Joachim, Muyumba Nsomue; Naomie, Bolangongo Mpandu; Mulula, A.; Haddy, Mbuyi Katshiatshia; Kashishi, K. T.; Kalulu, Taba; Ntumba, Joséphine K.

doi:10.9734/irjpac/2022/v23i330462

Cited by 2 publications

(1 citation statement)

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“…Natural medical compounds have always been considered as an inspiration for new antimalarial, antibacterial, antifungal, antiviral, antioxidants, antiinflammatory drugs development [7][8][9][10][11][12][13] . Among these natural medical compounds with many biological activities, there is also the class of Chalcones and Quinolones.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, In-vitro Antimalarial Activity and In silico Molecular Docking Study of Amino Chalcone Derivatives from 1-(2-aminophenyl)-3-(4- substituted-phenyl) prop-2-en-1-one and Dihydroquinolone Derivatives

Mulula

Bouzina

Nsomue

et al. 2023

Journal of Advanced Pharmacy Research

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Background: Malaria is one of the major global health problems in developing countries and faced to the increased resistance of Plasmodium falciparum against existing malarial agents, it is important to look for new antimalarial compounds that will be active in multiple stage of Plasmodium falciparum's life cycle. Objective: The goal of this work was to synthesize Amino Chalcone derivatives and Dihydroquinolone derivatives, then evaluate their antimalarial activity by standard computational and biological methods. Methods: These amino chalcones were synthesized by the Claisen-Schmidt condensation and by intramolecular cyclization of substituted amino chalcones for the Dihydroquinolones derivatives. Their structures have been determined by NMR ( 1 H and 13 C). The in-vitro antimalarial assays were carried out by using the maturation test of trophozoites into schizonts. The molecular docking of these compounds was performed by AutoDock vina program using Plasmodium falciparum dihydrofolate reductase-thymidylate synthase (PfDHFR-TS) (PDB ID 1J3I) as target protein. Results: All synthesized amino chalcones and dihydroquinolone derivatives were active against Fresh clinical isolates of Plasmodium falciparum with a range of EC50 ranging from 1.56 to 25µg/mL. However, the 2phenyl-2, 3-dihydroquinolin-4-(1H)-one (DHQ 2) and 2-(4-methoxyphenyl)-2, 3-dihydroquinolin-4-(1H)-one (DHQ 4) showed excellent antimalarial activity with IC50 of 3.125 and 1.56 µg/mL, respectively. Whereas the IC50 of Chloroquine use as reference was 1.56µg/mL. Based on absorption, distribution, metabolism and excretion (ADME) properties, all synthetized compounds satisfied the Lipinski rule. Conclusion: The results suggest that these synthesized compounds (DHQ 2 and DHQ 4), could be used, after in vivo and clinical tests, like antimalarial supplement or even replace current drug therapies.

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Section: Introductionmentioning

confidence: 99%

Synthesis, In-vitro Antimalarial Activity and In silico Molecular Docking Study of Amino Chalcone Derivatives from 1-(2-aminophenyl)-3-(4- substituted-phenyl) prop-2-en-1-one and Dihydroquinolone Derivatives

Mulula

Bouzina

Nsomue

et al. 2023

Journal of Advanced Pharmacy Research

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Understanding the role of storage reserve mobilization during seed germination and initial seedling growth in species of the genus Carapa

de Carvalho,

Nascimento,

Fernandes

et al. 2024

Botany

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A physiological and metabolic database for various species of Amazonian plants is crucial to the species selection and sustainable utilization of their diversity. We hypothesized that understanding the mobilization of Carapa seed reserves and water uptake during germination could provide insights into the physiological behavior and propagation to differentiate species of the same genus. Given this, the mobilization mechanisms of primary reserves, water uptake, and enzymatic activities in seeds of two species of Carapa (C. guianensis and C. vasquezii) were investigated. The lipid content was high in both species, with a value of 63.7±4.7% for C. guianensis and 55±1.5% for C. vasquezii. C. guianensis showed higher values for the other evaluated reserves. The protein profile highlights a band between 15 and 25 kDa in C. guianensis. As for the enzymatic activities investigated (lipase, amylase, protease, acid phosphatase), C. guianensis showed greater activity for most of them, except for acid phosphatase. Overall, the species showed different metabolic strategies and dynamics regarding the water uptake and use of reserves. Our findings indicate that distinct metabolic pathways are employed during the germination and initial seedling growth stages of two Carapa species. This trait can potentially guide the use and preservation of these species.

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Valorization of Carapa procera Oil and Evaluation in vitro of Antimalarial Activity of Its Bitter Content

Cited by 2 publications

References 1 publication

Synthesis, In-vitro Antimalarial Activity and In silico Molecular Docking Study of Amino Chalcone Derivatives from 1-(2-aminophenyl)-3-(4- substituted-phenyl) prop-2-en-1-one and Dihydroquinolone Derivatives

Synthesis, In-vitro Antimalarial Activity and In silico Molecular Docking Study of Amino Chalcone Derivatives from 1-(2-aminophenyl)-3-(4- substituted-phenyl) prop-2-en-1-one and Dihydroquinolone Derivatives

Understanding the role of storage reserve mobilization during seed germination and initial seedling growth in species of the genus Carapa

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