Synthesis, antimalarial activity evaluation and molecular docking studies of some novel dispiro-1,2,4,5-tetraoxanes

Kumawat, Mukesh Kumar; Chetia, Dipak

doi:10.3329/bjp.v10i4.24532

Cited by 8 publications

(5 citation statements)

References 14 publications

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“…The chloroquine sensitive (3D7) and chloroquine resistant (RKL-9) strains of the malaria parasite P. falciparum were obtained from the Parasite Bank of National Institute of Malaria Research (Indian Council of Medical Research), New Delhi. The strains of P. falciparum were maintained in fresh A+ erythrocytes suspended in RPMI-1640 medium supplemented with 25 mM HEPES, 1% D-glucose, 0.23% sodium bicarbonate, gentamycin (40 mg/ml), amphotericin-B (0.25 mg/ml) and 10% heat-inactivated AB+ serum at 37 °C and 5% CO 2 environment [32,33]. After every 24 h, the used medium was replaced with fresh medium supplemented with 10% heat-inactivated AB+ serum and the parasitemia level was maintained below 2%.…”

Section: In Vitro Culture Of Malaria Parasitesmentioning

confidence: 99%

In vitro antimalarial activity evaluation of two ethnomedicinal plants against chloroquine sensitive and resistant strains of Plasmodium falciparum

Gogoi

Gogoi²,

Chetia

2021

Clin Phytosci

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Background In this study, we selected two medicinal plants Citrus maxima (Burm.) Merr. and Artemisia nilagirica (C.B. Clarke) Pamp. on the basis of their traditional use in the treatment of fever associated with malaria in Assam (India) and evaluated their antimalarial potential against Plasmodium falciparum strains. Methods The properly processed plant parts of C. maxima (Burm.) Merr. and A. nilagirica (C.B. Clarke) Pamp. were extracted with different solvents from nonpolar to polar by cold maceration technique. After that antimalarial activities of the extracts were evaluated against both chloroquine sensitive (3D7) and resistant (RKL-9) strains of P. falciparum using Giemsa staining light microscopy technique. The most active extract(s) was further screened for cytotoxicity potential against murine macrophage RAW264.7 cell line using MTT assay. Then preliminary phytochemical screening and qualitative fingerprint analysis of the active extract(s) were done to check the presence of different secondary metabolites. Results From the in vitro study, the hydro-alcoholic extract of C. maxima (Burm.) Merr. and methanol extract of A. nilagirica (C.B. Clarke) Pamp. were found to be the most active against both 3D7 and RKL-9 strains. In the cytotoxicity study, the CC50 values of the active extracts were found to be > 100 μg/ml, which suggested the safety of the extracts. Then phytochemical and fingerprint analysis revealed the presence of various important plant secondary metabolites in both the extracts. Conclusion The findings of this study confirmed the presence of antimalarial potential of hydro-alcoholic extract of C. maxima (Burm.) Merr. and methanol extract of A. nilagirica (C.B. Clarke) Pamp without having any toxic effect. Both the extracts showed IC50 values below 5 μg/ml against 3D7 and RKL-9 strains.

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Section: In Vitro Culture Of Malaria Parasitesmentioning

confidence: 99%

In vitro antimalarial activity evaluation of two ethnomedicinal plants against chloroquine sensitive and resistant strains of Plasmodium falciparum

Gogoi

Gogoi²,

Chetia

2021

Clin Phytosci

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“…In contrast to P. falciparum and P. vivax, responsible for the vast majority of fatal cases, P. ovale and P. malariae cause a less severe form of malaria that is rarely fatal. A zoonotic species from Southeast Asia called P. knowlesi can infect humans in addition to causing malaria in macaques [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15] . According to the WHO report 2021, between 2000 and 2020, 10.6 million malaria mortality and 1.7 billion malaria cases were prevented worldwide.…”

Section: Introductionmentioning

confidence: 99%

4-Aminoquinolines as Antimalarial Agents: Review of A Medicinal Chemistry Perspective

Kumawat

Sharma

YADAV

et al. 2022

Int J Life Sci Pharm Res

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Malaria is a potentially fatal parasitic disease brought on by five Plasmodium species, including Plasmodium falciparum, Plasmodium vivax, Plasmodium ovale, Plasmodium malariae, and Plasmodium knowlesi. The fast emergence of P. falciparum resistance to currently available treatments has increased health concerns in developing countries. The growth in resistance emphasizes the need for a novel, secure, and cost-effective antimalarial drug that can treat malaria resistant to multiple antimalarial drugs. Therefore, it has become crucial to create new therapeutic approaches to deal with the rise of parasites resistant to artemisinin. For the treatment of P. falciparum malaria in children living in areas with moderate to high transmission, as established by WHO, the malaria vaccine RTS, S has been authorized. The WHO recommends that governments consider this immunization against a human parasite when deciding the optimum subnational combination of measures for maximum impact. The current research synthesizes numerous 4-aminoquinoline derivatives successfully treating malaria and its diverse etiological species. Additionally crucial to the management and prevention of malaria are antibiotics. Effective and well-tolerated antimalarial medications include tetracycline and chloramphenicol, chloroquine, primaquine, pamaquine, and artemisinins are some of the drugs used to treat malaria; however, numerous new compounds have proven to be even more efficient. This review, based on literature reports, will give medicinal chemists ideas for new malaria drugs to develop. In addition, this review will help search for new antimalarial drug leads in the future.

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“…However, they need more consideration to be given to them in light of their potential to improve overall development cost and time efficiencies since they are often seen as routine analyses. Analytical techniques aim to determine the identification, purity, physical properties, as well as potency of the pharmaceuticals we Consume [5][6][7][8] . Drug testing against standards is supported by methods established for production, quality release, and long-term stability research [9][10][11][12][13] .…”

Section: Introductionmentioning

confidence: 99%

Caffeine in Tablet Dosage Form: Analytical Method Development and Validation by Using U.V. Spectroscopy

Kumawat¹,

Tewatia²,

Ajmal³

et al. 2022

Int J Life Sci Pharm Res

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Caffeine (1,3,7-trimethylpurine 2,6 dione) is a CNS stimulant. Caffeine is used as a drug having drug-addicted properties having a U.V. cutoff in the range of 272 nm to 297 nm in the U.V. spectrum. In this paper, we took a tablet with Caffeine as a single dose in solid dosage form with excipients that do not have a sharp peak in the U.V. spectrum range from 200 nm to 400 nm. The solvent used as a vehicle is a simple polar solvent with a U.V. cutoff at around 189nm to 191 nm. The U.V. spectrophotometer that we used is of Shimdzu having a double beam, which has two provisions to keep reference and sample at a time to complete sample analysis. Firstly we make a calibration curve of Caffeine with a polar solvent. For the research, development, and production of medicines, analytical technique related to creation and validation are essential. Therefore, in this study, a readily reproducible, straightforward, and quick technique of U.V. spectrophotometric quantitative measurement of Caffeine in the form of tablets is adopted. According to ICH criteria, the parameters to be examined include linearity, specificity, accuracy, precision, and robustness. Purified/deionized water was used as the diluent for the drug quantification at the wavelength of 248.5 nm. Beer-law Lambert's applies to Caffeine at concentrations between 10 and 50 g/ml. Recovery was used to test the method's accuracy, and the results ranged from 99.46 to 100.67%. This approach was used for routine analysis of Caffeine in tablet dosage form.

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Synthesis, antimalarial activity evaluation and molecular docking studies of some novel dispiro-1,2,4,5-tetraoxanes

Cited by 8 publications

References 14 publications

In vitro antimalarial activity evaluation of two ethnomedicinal plants against chloroquine sensitive and resistant strains of Plasmodium falciparum

In vitro antimalarial activity evaluation of two ethnomedicinal plants against chloroquine sensitive and resistant strains of Plasmodium falciparum

4-Aminoquinolines as Antimalarial Agents: Review of A Medicinal Chemistry Perspective

Caffeine in Tablet Dosage Form: Analytical Method Development and Validation by Using U.V. Spectroscopy

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