New flavonol methyl ether from the leaves of Vitex peduncularis exhibits potential inhibitory activity against Leishmania donovani through activation of iNOS expression
| Autor: | Prasenjit Rudrapaul, Surajit Bhattacharjee, Niranjan Das, Utpal Chandra De, Indrajit Sil Sarma, Biswanath Dinda |
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| Předmět: |
Vitex pinnata
Methyl Ethers Flavonols Sodium Leishmania donovani Intracellular Space chemistry.chemical_element Nitric Oxide Synthase Type II Gene Expression Regulation Enzymologic Nitric oxide Cell Line Vitex chemistry.chemical_compound Griess test Drug Discovery Humans Amastigote Nitrites Pharmacology biology Macrophages Organic Chemistry Nitric oxide synthase 2 General Medicine biology.organism_classification Leishmania Plant Leaves chemistry Biochemistry biology.protein |
| Zdroj: | Scopus-Elsevier |
| Popis: | One new flavonol methyl ether (1), along with four known compounds from the leaves of methanol extract of Vitex peduncularis Wall and three known compounds from the leaves of methanol extract of Vitex pinnata Linn (Verbenaceae) were isolated. The chemical structure of the new compound was established by detailed spectroscopic studies. The in vitro antileishmanial activities of 1 against both Leishmania donovani promastigote and amastigote forms were evaluated. To characterize the effector mechanism of compound 1 against Leishmania parasite infected THP-1 macrophage cells, RT-PCR analysis of inducible nitric oxide synthase 2 (iNOS2) was done followed by measurement of nitric oxide generation by Griess reaction. Pentostam (sodium antimonygluconate) was used as reference drug. Compound 1 exhibited better antileishmanial activity than sodium antimonygluconate (SAG) (having IC50 values for promastigote, 2.4 and 58.5 μM and for amastigotes, 0.93 and 36.2 μM, respectively). Compound 1 was less toxic than SAG towards THP-1 having CC50 of 123.7 μM and 364.3 μM, respectively. Moreover, compound 1 was found to induce a potent host-protective response by enhancing NO generation and iNOS2 expression in infected macrophages to prevent the progression of Leishmania parasite. |
| Databáze: | OpenAIRE |
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